DRAFT CRITERIA  DOCUMENT
     FOR 1,1,1-TRICHLOROETHANE
           FEBRUARY  1984
       HEALTH EFFECTS  BRANCH
  CRITERIA AND STANDARDS  DIVISION
      OFFICE OF DRINKING  WATER
U.S. ENVIRONMENTAL  PROTECTION  AGENCY
      WASHINGTON, D.C.  20460

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                         TABLE OF CONTENTS

                                                            PAGE


   I.   SUMMARY	 I    -  1

  II.   CHEMICAL AND PHYSICAL PROPERTIES	 II   -  1

 III.   METABOLISM AND PHARMACOKINSTIC EFFECTS	 Ill  -  1

         A.  Metabolism		 Ill  -  1

             1.  Absorption	 Ill  -  1
             2.  Distribution	 Ill  -  6
             3.  Biotransformation	 Ill  - 11
             4.  Excretion	 Ill  - 15

         B.  Pharraacodynamic Effects -
               Animal and Human....	 Ill  - 19
  •A,
             1.  CMS .Effects	...;..., Ill  - 19
             2.  Cardiotoxicity	
             3.  Hepatotoxicity and Nephrotoxicity	
             4 .  Pneumotoxicity	

  IV.     HUMAN EXPOSURE*	 IV   -  1

   V.     HEALTH EFFECTS - ANIMAL	  V   -  1

         1.  Acute Toxicity	 . V      1
         2.  Subacute Toxicity	  V   -5
         3.  Chronic Effects	  V   -  9
         4.  M,utagenicity	  V   - 12
         5.  Carcinogenicity	  V   - 16
         6.  Teratogenicity	  V   - 19

  VI .     HEALTH EFFECTS - HUMANS	  VI  -  1

         1.  Acute Toxicity	  VI  -  1
         2.  Subacute Toxicity	  VI  -  5
         3.  Epidemiology....,	  VI  -  5

 VII.     HUMAN RISK ASSESSMENT	  VII-  1

         1.  Current Levels of Exposure..	  VII. -  1
         2 .  Existing Guidelines and Standards	  VII,-.^ ,,1
                                                          ,'',--.,> r- '• i • •
VIII.     QUANTIFICATION OF TOXICOLOGICAL  EFFECTS	VI!II;;- I

  IX.     REFERENCES.	 Ji.HiX.i~  1

                     /.
   *Prepared by the Science and Technology Branch

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                            TABLES
                                                         PAGE
Table II   - 1


Table III  - 1

Table III  - 2


Table III  - 3
Table III


Table III


Table V


Table VI


Table VI


Table VI


Table VII

Table VII

Table VIII



Table VIII


Table VIII


Table VIII
Figure II -
      Physical Properties of Methyl           II
      Chloroform

      Absorption of Methyl Chloroform         III

      Physical Properties and Absorption      III
      of Inhaled Vapors

      Concentrations of Methyl Chloroform     III
      in Tissues of Mice Following Inhala-
      tion Exposure

- 4   Methyl Chloroform Excretion in Exhaled  III
      Breath

- 5   Liver Effects of Methyl Chloroform and
      Other Chlorinated Hydrocarbons          III

- 1   Effects of Trichloroethane Isomers on
      Mice                                      V

- 1   Urinary Metabolite Concentration in      VI
      Workers Exposed to Methyl Chloroform

- 2   Result of Physical Examinations of       VI
      Workers Exposed to Methyl Chloroform

- 3   Exclusions from Healthy Category by      VI
      Class of Disorder

- 1   Chloroethane Exposures and Production   VII

- 2   Chloroethane Exposure Standards         VII

- 1   Summary of Effects in Mice After        VIII
      Continuous Inhalation Exposure to
      Methyl Chloroform

- 2   RMCL and Health Advisory for Methyl     VIII
      Chloroform

- 3 '  Mutagenicity Testing of Methyl Chloro-  VIII
      form

- 4   Estimated Lifetime Cancer Risk to       VIII
      Humans at a Dose of 1 ug/liter

                FIGURES

  1  Metabolic Route Suggested for Methyl     III
     Chloroform

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                              PREFACE



           The  objective of this  document is  to assess  the



 health  effect  information of  the contaminant 1,1,1-Trichloroethane



 in  drinking  water and to quantify toxicological effects.



-To  achieve this objective, data  on pharmacokinetics, assessment



 of  human exposure,  acute and  chronic  health  effects  in animals,



 human health effects including epidemiology  and mechanisms  of



 toxicity were  evaluated.  Only the reports which were  considered



 pertinent for  the derivation  o,f  the maximum  contaminant level



 are cited in the document. Particular attention was paid



 toward  the utilization of primary references for the assessment



 of  health effects.   Secondary references were used  rarely.



 For comparison, standards and criteria developed by  other



 organizations  are discussed in Section VIII, Quantification of



 Toxicological  Effects.

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                             1-1
I.  SUMMARY

          In 1978, the estimated production of methyl chloroform

in the U.S. amounted to 623 million pounds.  Methyl chloroform

is used extensively for industrial metal cleaning, and in the

manufacturing of adhesives and various aerosol products.   All

of these quantities, whether used industrially or for consumer

products are eventually transmitted into the environment,

primarily in the form of atmospheric emissions.


          The atmospheric level of methyl chloroform has  been

generally measured in the low parts per billion (ppb) or

parts per trillion (ppt) range.  Methyl chloroform undergoes

a slow photochemical decomposition in the troposphere to

produce carbon monoxide, hydrogen chloride, phosgene, and

various other halogenated products.


          Methyl chloroform has been detected in the drinking

water of several cities throughout the United States.  It may

be of interest to note that near manufacturing sites, methyl

chloroform has been detected also in surface and ground water.


          Inhalation is the major route of exposure in humans,

followed by food and water consumption, and dermal contact.
                 f
Methyl chloroform, in its unmetabolized form, is rapidly

excreted in the breath after exposure.  For example, within

the first hour after human inhalation of a single breath of

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                             1-2





methyl chloroform, 44% of the dose was excreted on the breath



unchanged.  Rats treated with an- injected dose or inhalation dose



excreted 98.7% on the breath in an unchanged form.  Metabolism



studies conducted on methyl chloroform indicated the fate of



the compound in rats, mice, and man is relatively similar.



The initial step in the biotransformation of methyl chloroform



is the formation of the metabolic trichloroethanol which



subsequently is excreted from the body as trichloroacetic



acid or as trichloroethanol glucuronide.





          Inhalation  (exposure) estimations have been made



for occupational exposure concentrations of methyl chloroform



in the air surrounding various industries ranging widely from



1.5-16.6 in the metal industry to 12.0-118.0 ppm in soldering



degreasing plants.  Concentrations which have been reported



to cause transient, mild eye irritations have been in the



range of 500-1000 ppm range.  Regression analysis has indicated



a linear relationship between vapor concentrations of methyl



chloroform and the levels of urinary metabolites.






          The odor threshold of methyl chloroform covers a



wide range (16 - 700 ppm) suggesting that individual



sensitivity may play a part in determining resultant irritation



and sensivity of various organs.  The American Conference of



Governmental Industrial Hygienists has recommended a Threshold



Limit Value of 350 ppm.

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                              1-3


          Methyl  chloroform has been found  in  small  amounts

 as  a  contaminant  in  various food  stuffs.  Amounts of this

 compound  in meat,  oils,  fats,  tea, -fruits,  and vegetables

 ranged from 1  to  10  ug/kg.  These levels  are reportedly higher

-than  the  concentrations  found in  drinking water of U.S. cities.


          The  predominant health  effects  of exposure to

 anesthetic  levels of methyl chloroform is the  narcotic effect

 on  the central nervous system (CNS).   Man is the most responsive
                              \
 species in  demonstrating such CNS effects of methyl  chloroform.

 Most  studies showed  behavioral or narcotic  changes on

 experimental animals at much  higher  levels  of  exposure than

 those reported for man.   The  effects of methyl chloroform in

 the CNS are similar  to a general  anesthetic agent; these are

 functional  changes which, according  to available reports, are

 entirely reversible.  Inhalation  of  high  concentrations of

 methyl chloroform for extended time  periods could be fatal

 without any occurrence of organic or toxicological symptoms.

 Nausea and  prolonged restlessness have been observed as side

 effects in  humans receiving anesthetic doses,  but consciousness

 returns within minutes after  breathing air  free of the compound.


          The Romberg test  (a neurological  test which measures

 proprioceptive control)  has been  used to  measure the narcotic

 effects of  methyl chloroform  within  the range  of 500 ppm  (no

 CNS effects) to 2,650 ppm.  Impairment of motor control has been

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                             1-4






demonstrated in humans with concentrations as low as 350



ppm.  However, this finding was not collaborated by other



investigators.






          It is generally believed that high concentrations



of the chlorinated hydrocarbons can sensitize the heart of



some individuals and thereby make the heart abnormally



responsive to epinephrine.  One of the effects of epinephrine



in man and animals is cardiotoxicity.  Since methyl chloroform



either has arrthymic effects of its own or makes epinephrine



effects more pronounced, there is a potential for serious



cardiac effects resulting from exposure during excitement or



stress when the body normally releases high levels of



epinephrine. If an additional factor of an old cardiac scar



or other cardiovascular problem is added, there is a



physiological potential for serious cardiac effect from high



levels of exposure.





          The subcutaneous absorption of methyl chloroform



appears to be dependent on the area of exposure.  The rate of



absorption during exposure may affect its toxic potential.






          Biochemical effects on the liver also occur with



methyl chloroform exposure.  The liver changes occurring in



man and experimental animals after exposure are not secondary



to either CNS or cardiac effects of this solvent.

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                             1-5
However, these changes consist of actual cellular or bio-



chemical damage while the CNS effects like those of most



anesthetic agents are reversible.






     Human liver effects have been assessed in some



reports by measuring urinary urobilinogen (a bile pigment



processed by liver cells and released only in small amounts



by a healthy liver).  Serumvis frequently analyzed for enzymes



(SGPT and SCOT) which increase  in liver disease.  The exposure



level resulting in liver change has been delineated in humans



and experimental animals.  Animal toxicity data have shown



that the guinea pig is the most sensitive species to the



liver effects of methyl chloroform.  Fatty changes in rodent



livers were reported after chronic exposure at 1,000 ppm in



four studies.  However, animal experiments investigating the



influence of methyl chloroform on liver function yield



controversial results highly dependent on species, dose and



treatment schedule.  Results vary from no organic damage in



guinea pigs at 1,500 ppm at 7 hr/day for 3 months to actual



damage at the 1,000 ppm for 30-90 min/day exposure for 3 months.






          Repeated exposure to methyl chloroform has been



shown to increase the excretion of metabolites in both animals



and man, probably by the mechanism of enzyme induction.  The

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                             1-6
importance of this induction is twofold.  First, it is a

mechanism by which man and anima-1 excrete methyl chloroform

more rapidly on chronic exposure; because of this apparent

capability/ fewer chronic effects would be expected to occur

with methyl chloroform compared with compounds that deposit

in tissues.  Second, stimulation or induction of some of these

liver enzymes changes the action of many presecription and

non-prescription drugs since the same enzymes that are induced

by methyl chloroform are responsible for the metabolism of

many types of drugs (i.e., sedative hypnotics and anti-

psychotics).  Thus, some drugs may have reduced or increased

effects  in persons chronically exposed to methyl chloroform.


          Nephrotoxicity, as measured by tubular damage,

phenosulfonpthalein, glucose, and protein excretion data

has been investigated in animals and man with reference to

methyl chloroform.  Although some kidney damage has been

reported in laboratory animals, it appears that methyl

chloroform damages the liver before it affects the kidneys.



          The National Cancer Institute (NCI) conducted
              s
carcinogenesis bioassays on methyl chloroform.  Rats and mice

were orally dosed with methyl chloroform five times per week

for 78 weeks.  Rats received either 1,500 or 750 mg/kg of  the

compound; mice  (male and female) received either 5,615 or
                              6

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                             1-7






2,807 mg/kg.  The dose levels administered in both experiments



were sufficiently high to result in early death within each



group; a maximum of 40% of the initial groups remained alive



by end of dosing.  Within the survival groups, no consistent



pattern of cancerous tumors was observed.  Due to the low



survival rate, statistical analysis could not be performed in



either study.






     The CAG has calculated an upper-limit cancer risk



estimate based on the 1983 NCI bioassay.  This study showed a



marginally statistically significant increase in hepatocellula



carcinomas in femal^mice receiving 1500 or 3000 mg/kg methyl



chloroform by gavage in corn oil five times per week for 103



weeks.  The responses were 6.1%, 10.2%, and 20.4% for the



control, low-dose, and high dose groups, respectively.  They



stated that consuming 2 liters of water per day over a lifetime



at a methyl chloroform concentration of 2200 ug/L, 220ug/L



or 22 ug/1 would increase the risk of one excess cancer per



10,000 (10-4), 100,000 (10~5), or 1,000,000 (10~6) people



exposed, respectively.





Chronic Animal Studies






          Although a number of studies have indicated chronic



changes in the heart, nervous reflex activity, respiratory



function, and hepatic changes resulting from "long-term"



exposure to methyl chloroform, most of these studies have

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                             1-8
used continuous exposures, which are not typical of the

ingestion through water.  Therefore, studies investigating the

chronic effects of long-term exposure to methyl chloroform

should be conducted that utilize exposure schedules to those

encountered through water.



Mutagenicity, Teratogenicity, Carcinogenicity.

                           \
          Mutagenic properties of methyl chloroform have been

investigated yielding weakly positive responses in certain

Ames tests to negative responses in some other test systems.

There are three studies on the teratogenic and fetal toxicity

of methyl chloroform, two of which were via inhalation and

one by ingestion.  The results of these suggested that methyl

chloroform was not teratogenic to mice or rats at given levels

of exposure.


        In the repeat NCI bioassay in rats and mice, there

was an increase in hepatocellular carcinomas occurrence in

low and high dose males and high dose females.  NCI concluded

that (1) methyl chloroform was not carcinogenic for male rats

(2) the study was considered inadequate for carcinogenesis

evaluation in female rats,  (3) the association between the

administration of methyl chlorofjrAn and the increased incidences

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                             1-9
of hepatocellular carcinomas in male mice was considered

equivocal, and (4) methyl chlorof£4m was carcinogenic for

feamle mice, causing an increased incidence of hepatocellular

carcinomas.


Synergistic Effects


     Ingestion of ethanol was shown to increase the hepato-

toxicity of methyl chloroform.  However, from a review of
                           \
the literature, it is evident that research must be intitated

to answer important questions concerned with exposure to

methyl chloroform and that a concerted effort must be directed

toward determining the possible additive, synergistic or

inhibitory effects of methyl chloroform, in combination with

other hydrocarbons and organic solvents, on dose-response

relationships.

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                              II-l


II.  CHEMICAL AND PHYSICAL PROPERTIES


          1,1,1-Trichloroethane  (-CH30013),  also  called

methyl chloroform, is a colorless nonflammable liquid which  has

a characteristic odor.  Its line formula  is:

                   H   Cl
                   I     I
                 H-C	C-C1
                   I     I
                   H   Cl

                            \

          Table II-l shows some of its important chemical and

physical properties.

          TABLE II-l.  PHYSICAL PROPERTIES  OF METHYL CHLOROFORM
Solubility in water @  25°C	0.44 gm/100 gm
Boiling point @ 760 torr	74°C
Vapor pressure @ 20°C	100 torr
Vapor density (air =  1)	4.6
Molecular weight	133.41
          In the atmosphere, methyl chloroform is subject to

free radical attack and reaction with hydroxyl radicals is

the principal way in which  it is scavenged from the atmosphere.

Photo-oxidation products of methyl chloroform include hydrogen

chloride, carbon oxides, phosgene, and acetyl chloride

(Christiansen elt al^. , 1972).  The principal tropospheric

photo-oxidation product has been reported to be trichloroacetal-

dehyde.

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                             II-2






          In water, methyl chloroform is slowly hydrolyzed to



predominantly acetic and hydrochloric acids  (Billing e_t al.,



1975).  Billing e_t a_l.  (1975) reported a half-life of hydrolysis



of 6 months at 25°C.






          Anhydrous methyl chloroform is generally noncorrosive,



but in the presence of  water it can react  to  form hydrochloric



acid, which is a corrosive of metals (Keil, 1979).  Addition



of epoxides can neutralize l;he generated acid  (Keil, 1979).



Anhydrous methyl chloroform when heated to 360° to 440°C,



decomposes to 1,1-dichloroethylene and hydrogen chloride.



When methyl chloroform  is heated in the presence of water at



temperatures between 75° and 160°C, it decomposes upon



contact with metallic chlorides or sulfuric acid to acetyl



chloride, acetic acid,  and acetic anhydride.  Noweir e_t al.



(1972) have observed that when methyl chloroform comes in



contact with iron, copper, zinc, or aluminum, at elevated



temperatures, phosgene  is produced.
                               10

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                            III-l

III.  METABOLISM AND PHARMACODYNAMIC EFFECTS

A.  Metabolism

1.  Absorption

          In assessing the relationship of absorption of
methyl chloroform, one needs to consider the types of action
involved in the chlorinated hydrocarbons.  They are all
neurodepressants and they are all affected by the rate of
absorption during exposure by inhalation, the most common
route of exposure in man.

          Differences in the rate of absorption, as reflected
in the partition coefficients, could account for the
approximately ten-fold greater toxicity of the 1,1,2-isomer
over the toxicity of methyl chloroform (Fairchild e_t al.,
1977).  The blood/air partition coefficients are 1.4 for
methyl chloroform and 44.2 for 1,1,2-trichloroethane (Morgan,
et^ al., 1972).  The body content of the latter will increase
much more rapidly than the former during exposure to equal
concentrations of vapor.  Following exposure, the body content
of methyl chloroform will decrease much more rapidly by
excretion in breath than that of its 1,1,2-isomer, leaving
less in the body to be metabolized.
                              11

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                             III-2
*
t



           According  to  Stewart and Dodd (1964),  cutaneous



 absorption depends on the area of  exposure.   Methyl  chloroform



 is  more  readily absorbed through the skin than is  trichloroethy-



 lene.  Because  continuous immersion of both  hands  in methyl



 chloroform for  30 minutes has been estimated to  be equivalent



 to  a 30-minute  vapor exposure to 100-500 ppm of  the



 compound,  skin  absorption would present only a limited health



 hazard.   In Stewart  and Dodd's experiments,  both male and



 female subjects ranging in age from 25 to 62 years were used.
                               v


 Three  kinds of  hand  exposure were  tested:  thumb immersion;



 total  hand immersion; and topical  hand application,  which



 consisted of brief  immersion, withdrawal,  solvent  evaporation,



 and reimmersion. Alveolar air samples were  measured during



 and following exposure.  Methyl chloroform in the  alveolar



 air increased rapidly during immersion and dropped off slowly



 following exposure.   The results are shown in Table  III-l.



 Considerable effort  was taken that the exposure  through the



 skin was not confounded by vapor inhalation.   Periodically,



 during the.skin exposure, samples  of breathing zone  air were



 analyzed.   Inhalation,  as a source of the methyl chloroform



 in  this  experiment,  was not a factor (Stewart and  Dodd, 1964).

                  S

 Male and female human subjects ranging in age from 25 years



 to  62  years were used.   Three types of exposures were tested:



 thumb  immersion, hand immersion, and topical application on



 the hand.





                               12

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                            III-3





The experiment was carefully designed to prevent the subjects



from inhaling the chemical.  The authors concluded that



cutaneous absorption presents no health hazard since immersion



of both hands for 30 minutes is equivalent to a 30-rainute



vapor exposure to 100-500 ppm of the chemical.








                         Table III-l





               ABSORPTION OF METHYL CHLOROFORM

Length of
exposure
(min)
30
30
30
Type of
exposure
Thumb (immersion
Hand (immersion)
Hand (topical)
ppm
Average Peak
breath
concentration
) 1.0
21.5
0.65

Average breath
concentration
2 hr postexposure
0.31
1.55
0.31

Adapted from:  Stewart and Dodd (1964).









          Fuk£bori, e_t a^l. (1976) studied the percutaneous



absorption of methyl chloroform applied on 12.5 cm^ of the



skin of the forearm^  Four men ranging from 24 years to 51



years of age were used.  Application of the chemical for two



hours a day on five consecutive days resulted in a maximum





                              13

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                             III-4






concentration of 7 ppm in the expired  air  and  9 mg/ml  in  the



blood immediately after termination of  the daily application.



Comparable results were obtained when  both hands were  immersed



in the test compound 11 times a day for 10 minutes on  four



consecutive days.  The concentration of methyl chloroform



obtained in the alveolar air in these experiments was  comparable



to that after exposure for  two hours to 10-20 ppm in the air.
          Using   ci_iabeie(f| halogenated hydrocarbons, Morgan



e_t al . (1970) compared the blood-air partition coefficient,



solubility, and excretion rates of various halogenated



hydrocarbons  (Table III - 2).  For the excretion studies,



approximately 5 mg of labeled material was administered



by a single breath inhalation to human subjects.  The subjects



held their breath for 20 seconds to ensure maximum absorption.



Exhaled air was trapped in granulated charcoal and the radioactivity



in the charcoal traps was measured by gamma-ray scintillation



spectrometry.  In comparison to other halogens, the amount of



methyl chloroform which was excreted was very high, indicating



a low level of retention.  Urinary excretion of total 38ci



was less than 0.01 percent per minute with most compounds.





          The uptake of non-labeled methyl chloroform from



air containing 0, 100, 350, and 500 ppm of the compound  was



studied in 20 male and female subjects by Stewart, e_t al.



(1975).  Subjects were exposed to each concentration  for 1,  3,






                              14

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                            III-5


                         Table III-2



    PHYSICAL PROPERTIES AND ABSORPTION OF INHALED VAPORS*
Compound
  Blood/Air
  Partition     Solubility
Coefficients  (g/100 ml water)
             Total Excretion
             in Breath After
                1 hour as
             Percent of Dose
Methyl
Chloroform
1,1,2-Tri-
1.4
44.2
0.44
0.44
44
2.9
chloroethane

1,1,2-Tri-
chloroethylene
      9.5
0.10
10
* Adapted from Morgan et al. (1970)
and 7.5 hours.  Breath samples were taken from 1 minute to 71

hours after exposure, and were analyzed for unmetabolized compound,

Curves of the methyl chloroform remaining in the breath were

plotted to estimate the magnitude of exposure.  Breathing 350

ppm methyl chloroform for 1 hour, for example, produces a

breath level of about 165 ppm, which declines to under 1 ppm

at 23 hours.  On the other hand, breathing the same concentration

(350 ppm) for 7.5 hours gives a breath concentration of

approximately 244 ppm which declined to approximately 7 ppm

after 16 hours.  The authors found that the rate of methyl

chloroform excretion was a function of exposure duration.

                              15

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                             III-6





The data generated a family  of post-exposure breath decay



curves that could be used to estimate the magnitude of exposure






          Stewart, et al. (1961) measured human urine samples



following 15 minutes of exposure to methyl chloroform; some



samples contained up to 2 ppm of the compound, some contained



only a trace, and some urine samples contained none at all.





          Morgan, et al.  (1970) demonstrated that in man, the



amount of absorption of methyl chloroform is increased by



inhaling the vapor and holding the breath.





Summary





          Absorption of methyl chloroform is most commonly



experienced in man primarily via inhalation, and secondarily



through dermal absorption.   The rate of absorption during



exposure possibly affects the toxic potential of the specific



chlorinated hydrocarbon in question.






2.  Distribution





          Holmberg, e_t al_. (1977), studied the distribution



of methyl chloroform in mice during and after inhalation.



Solvent concentrations in the kidney and brain were about the



same at a given exposure concentration, but concentrations in



the liver were twice those observed in the kidney and brain



following exposures to 100 ppm or more  (Table III-3).






                              16

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                                          III-7
                                       Table II1-3

                      CONCENTRATIONS OF METHYL CHLOROFORM IN TISSUES
                         OF MICE FOLLOWING INHALATION EXPOSURES*

Concentration
(ppm)
10
100
1,000
5,000
10,000
Exposure
Time (h)
24
24
6
3
6
1,1, 1-Trichloroe thane
Blood
0.6 +
6.3 +
36 +
165 +
404 +
0.16 f/
3.0
16
25
158
Concentration (ug/g
Liver
1.5 +
12.2 +
107 +
754 +
1429 +
0.3
4.6
38
226
418
Kidney
1.1
5.9
60
153
752
-I- 0.2
+ 2.2
± 16
-f 27
+ 251
tissue)
Brain
0.8
6.2
57
156
739
± 0.1
± 1«3
1 17
+ 24
+ 170

f/ Mean j- SDM

*Adapted from:  Holmberg et al., 1977.

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                            III-8






A pharmacokinetic model with both uptake and elimination of



the first order best fitted the empirical data.  Hake, e_t al.



(1960) reported that 0.09 percent of a  large dose of methyl



chloroform was retained in the skin of  rats as the parent



compound after 25 hours of administration of an intraperitoneal



(I.P.) dose  (700 rag per kg).  The blood contained 0.02 percent,



the fat 0.02 percent and other sites 0.1 percent of the dose



administered.  The blood, body fat, and other sites contained



0.02, 0.02, and 0.1% of the"1 administered dose, respectively.








          Astrand, et al. (1973) and Astrand (1975) found



that the uptake of methyl chloroform and other solvents into



the alveolar air and arterial blood was dependent on pulmonary



ventilation and blood circulation which are affected by the



intensity of physical work.  In these experiments, 12 men



(ages 21-28) were treated for 30 minutes with 250 ppm or 350



ppm of methyl chloroform during rest and exercise (50-150



watts, a unit of workload as measured on a bicycle ergometer).








The concentration of the chemical in the alveolar air (180 ppm)



and arterial blood (5 ppm) was nearly the same at an exposure



of 350 ppm at rest and at 250 ppm during light exercise-



Monster, et al. (1979) exposed six male human volunteers
                              18

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                              III-9
(ages  27-34) for  four hours to  70 ppm methyl  chloroform at

rest,  145 ppm at  rest,  and 142  ppm at rest combined with work

loads  (two times  30  minutes,  100  watts).  During the work

load,  the lung clearance of methyl chloroform increased 2-3

times  the value at rest.  In  the  post-exposure period, the

concentration of  methyl chloroform in exhaled  air paralleled

that in  blood; the concentration  of the chemical in the blood
                             i
was 8.2  + 2.5 times  higher 'than that in exhaled  air.  There

was no significant difference in  the concentration of the

chemical in the blood or exhaled  air of subjects in the rest

group  (145 ppm exposure) and  that in the rest/work group

(142 ppm exposure).   The slopes of the concentration curves

     in  blood and exhaled  air at 20  hours, 50 hours and 100 hours

     after exposure corresponded to  a half-life of methyl chloroform

     of  about 9 hours,  20  hours, and 26 hours, respectively.


              Four male Sprague-Dawley rats were exposed to 955

     ppm of methyl  chloroform for 73 minutes, and the concentration

     measured in the breath until it was undetectable (Bcettner

     and Muranko, 1969).  Stewart, et al. (1961) had  exposed humans

     to  similiar levels and compared the data.  One hour following

  exposure,  human breath contained 1.85 times the  concentration


                                  19

-------
                            111-10





of methyl chloroform as that  in rat-expired air; 10 hours



following exposure, human breath contained four times the



concentration  in rat-expired  air.  These results showed that



humans and rats differ in any or all of the parameters of



absorption, elimination, or retention.





          Concentrations of methyl chloroform in the expired



air sample of  rats and man were compared at 1 hour following



different exposure indices, usually calculated as the product



of concentration and time (Stewart, e_t a_l. 1961).  The results



indicated that the concentration of the solvent was of greater



importance than the elapsed time from inhalation in determining



post-exposure  breath concentration.  Additional studies with



concentrations from 100 to 1,000 ppm confirmed that when the



concentration  of the chlorinated hydrocarbon is sufficient to



cause rapid saturation, the concentration of methyl chloroform



or total chlorinated hydrocarbon in expired air is proportional



to the concentration of the compound rather than the time of



treatment, once the saturation limit is reached.






Summary





          Autopsies of humans dying from acute exposure of



methyl chloroform, reveal tissue concentrations according to



the following order:  liver > brain > kidney > muscles > lung >



blood.  In pregnant animal studies, methyl chloroform is readily
                              20

-------
                            III-ll

absorbed (both inhaled and  ingested) by the fetuses.  Comparison
studies of rat and human responses  indicate that both species
differ in parameters of absorption, elimination, or retention
of methyl chloroform.

3.  Biotransformation

          The primary metabolites of methyl chloroform are
trichloroethanol and trichloroacetic acid  (TCA) as shown in
                           \
Figure III-l  (Hake, et al.  1960; Ikeda and Ohusuji, 1972).
                       Figure  III-l

    Metabolic  Route  Suggested  for Methyl Choloroform
          METHYL
        CHLOROFORM                       TRICHLOROETHANOL
                         oxidation
        CC13  -  CH3     	—>         CC13 - CH2OH
                                glucuronide
                                conjugation           oxidation
                      CClo  -  CH20 -  glue.
                                            TRICHLOROACETIC ACID
                                               CC13COOH
Adapted  from:   Hake,  et  al.  (1960);  Ikeda  and  Ohtsuji  (1972).
                               21

-------
                            111-12


          On the basis of in vitro experiments with normal

gut flora, it appears that microbial degradation is not an

important process in metabolic degradation  (McConnell, e_t al.

1975).

          Hake and co-workers  (1960) injected one female and

two male rats (170 to 183 g) intraperitoneally with 700 mg/kg

of methyl chloroform-l-14C.  About 50% of the urinary

radioactivity occurred as 2,2,2-trichloroethanol in the form
                           \
of glucuronide conjugate.  The other 50% volatilized at room

temperature.  It was suggested that methyl chloroform

metabolized by an initial oxidation to trichloroethanol and

subsequent oxidation to small quantities of trichloroacetic

acid.  In this study, 98.7% of the injected radioactivity was

exhaled as unchanged compound, and 0.5% as -^CC>2.  Only 0.85%

of injected radioactivity was  recovered in urine, and only

half of that was identified as a metabolite, indicating

insignificant bioaccumulation.


          The studies on metabolism by Ikeda and Ohtsuji (1972)

compared the metabolism of methyl chloroform using both

inhalation dosage (a route of  greater interest to human

work) and i.p. injection of 200 ppm for 8 hours.  Eight

studies of six 50g Wistar rats per study were used.  All

urine excreted in 48 hours was collected.  Trichloroacetic
                              22

-------
                            111-13



acid (0.5 mg/kg body weight) and trichloroethanol  (3.1 mg/kg

body weight) were found.  A dose of 2.78 mmol/kg body weight

of methyl chloroform was also  injected i.p. into a similar

group of rats to check the effects of the dosage route.  The

results of the urine analysis  following i.p. injection were

essentially the same as those  obtained on the inhalation

experiments.  The relative levels of trichloroethanol and

trichloroacetic acid seen inslkeda's experiments may indicate

that the acid is derived from  the alcohol.


          Fukabori and co-workers (1976) reported the metabo-

lism of methyl chloroform in humans after skin application

to two sites.


          Site I

          Forearm skin, 2 hr/day for 5 days

          Metabolites in urine:  Trichloroethanol, 2 to 6

                                  rag/day (Day 1)

                                 Trichloroacetic acid, slight

                                   increase with increased
                                   exposure

          Site II

            Dip both hands, seven times per day for 4 days,

            Metabolite in urine:  Trichloroethanol, 5 to 15

            mg/day
                               23

-------
                            111-14

It should be noted that most of the methyl chloroform was in
the expired air.  The concentrations of the unchanged solvent
ranged from 5 to 11 ppm  (days 1 and 4) respectively, when hands
were dipped in the solvent.

Summary

          Trichloroethanol and trichloroacetic acid are the
primary metabolites of methyl chloroform.  Various metabolic
studies in animals of methyl^chloroform have been cited noting
that regardless of dosage route (inhalation or ingestion) the
results of urine analysis were essentially the same.  Human
metabolic profiles after skin application of methyl chloroform
indicate both trichloroethanol and trichloroacetic acid
(increasing slightly with an increased exposure) in urine.
However, most methyl chloroform was found unchanged (98.7%)
in the expired air.

4.  Excretion

          Pulmonary excretion rates in man in the first hour
following exposure to methyl chloroform were 44% (Morgan, e_t
al., 1970).  In a series of chlorinated compounds, excretion
rates were inversely proportional to the lipid solubility of
the compound.
                              24

-------
                             111-15


          A summary of the excretion of methyl chloroform  in

expired air sample is given  in  Table III-4.



                         Table  III-4


        METHYL CHLOROFORM EXCRETION  IN EXHALED BREATH
Route
Species
 % Dose exhaled
  unmetabolized
 Reference
Skin
contact
Inhalation
Injection
   (i.p.)
 Humans
 Humans
 Rats
Peak breath level
14% of estimated
150 ppm dose

44% in 1 hour
> 99% of 77 mg/kg
Stewart and Dodd
 (1964)
Morgan,  et al.
  (1970)

Hake, e_t al.
  (1960)
           In  the  studies  of Hake,  e_t  al.  (1960),  over  99% of

the  i.p.-injected methyl  chloroform was excreted  by  rats via

the  pulmonary route  (98.7% unchanged,  0.5%  metabolized) and

less  than  1%  via  the  urine (0.85%  of  dose,  half  identified as

the  glucuronide of trichloroethanol).  Boettner  and  Muranko

(1969)  have used  animal pulmonary  excretion data  for estimation

of exposure in humans.
                               25

-------
                             111-16








          Ikeda and Ohusuji  (1972) compared the metabolism of



methyl chloroform after exposing Wistar rats  (70 g body



weight) of both sexes to the vapor (200 ppm for eight hours)



and after intraperitoneal  injection  (2.78 mmole/kg).  Urine



was collected for 48 hours.  The total trichloro-compounds



were estimated colorimetrically by Fujiwara reaction after



oxidation of the urine.  Trichloroacetic acid (TCA) was



determined by the same colorimetric method without oxidation.



The difference between the total trichloro-compounds (after



oxidation) and TCA  (without  oxidation) was calculated to be



trichloroethanol (TCE-).  Regardless of the role of administration



of methyl chloroform, 48-hour urine samples contained 0.5



mg/kg  (body weight) of TCA and 3.1 mg/kg of TCE.





          The publication  of recent technical reports on the



pharmacokinetics of methyl chloroform provide the disposition



characteristics of  the chemical in rats and mice (Schumann,



et al. 1982a, 1982b).  The animals were exposed via inhalation



to 150 or 1,500 ppm of radiolabeled material  for 6 hours.



The elimination of  the radioactivity was measured for 72 hours.



Following exposure  to 150  or 1,500 ppm, both  species excreted



greater than 96% of administered radioactivity during -the



first  24 hours.  The primary route of elimination from the



body was via exhalation of unchanged methyl chloroform.  In



the rat, approximately 94% and 98% of the total administered
                              26

-------
                            111-17




radioactivity was eliminated in expired air after exposure to


150 or 1,500 ppm, respectively.   In the mice, the percentages


were 87% and 97% of the respective exposure concentrations.


The remaining radioactivity was detected as CC>2 in the expired


air and as nonvolatile radioactivity  in urine, feces, carcass

and cage wash.  Mice were found to metabolize two or three

times more methyl chloroform on a body weight basis compared


to rats.  The authors stated that (1) since the biotransformation
                            \
of methyl chloroform occured to such  a limited extent,

saturation of its metabolism did  not  impair markedly on the


distribution or elimination of the parent chemical, (2) the


body burden, end-exposure blood level, and tissue concentration

of methyl chloroform were found overall to increase in direct


proportion with the exposure level, and (3) radiolabeled


methyl chloroform was more concentrated in the fat of both

species than in the liver or kidneys  immediately after


exposure  (however it was rapidly  cleared from the fat so that

by 24 hr  < 2% of the initial radioactivity remained).



          Morgan, et al. (1970) measured pulmonary excretion


of 38Cl-labeled methyl chloroform and trichloroethylene in


man following a single breath administration; the former was


expired more rapidly than the latter  during the first hour


(i.e., 44% and 10% of the inhaled dose).
                               27

-------
                            111-18






          With low level exposure  (about 183 ppm), Monzani



et al. (1969) observed that (a) only one of 18 workers



excreted trichloroacetic acid  in the urine, and  (b) that



excretion was at a level of 9.72% ing/liter of urine.






        In 1968, Tada and co-workers exposed two male subjects



by inhalation to a series of chlorinated hydrocarbons.  The



urinary excretion of trichloroacetic acid was increased by



repeated exposures.  However,  the increase was not proportional



to vapor concentration and exposure duration.





          Tada (1969) repeatedly exposed humans to 200-400



ppm methyl chloroform.  There  was an increase in urinary



excretion of trichloroacetic acid with a maximum reached in



4-5 days.  The urinary acid levels fluctuated during the



day; the author suggested that the total 24-hour excretion



was related  to time and intensity  (vapor concentration), of




exposure.





          Methyl chloroform was still found at a level of 0.1



ppm in the breath of an individual after 1 month of exposure



to a mixture of 370 ppm of the compound and 130 ppm



trichloroethylene, 7 hours/day for 5 days (Stewart, et al. 1969)



Methyl chloroform was also present in alveolar air 1 month



after exposure to concentrations ranging from 420-612 ppm



for 6.5 to 7 hours/day for 5 days  (Stewart, e_t a_l. 1961).
                               28

-------
                             111-19

Summary



          Methyl chloroform  and  its metabolite  (identified and

unidentified) have been  shown  to be excreted  (unchanged) in

man and rats via the lungs and urine.   In rats, methyl

chloroform has been administered by 2 routes, inhalation and

intraperitoneal injection.   Alveolar air was the main route

of excretion in both cases.  Clinical studies indicate that

exposure to methyl chloroform  and resulting urinary levels of
                             \
trichloroacetic acid are related to time and intensity of exposure
b.  Pharmacodynamic Effects  (Animal and Human)


          Like other halogenated hydrocarbons, methyl chloroform

influences the functions of  the CNS, heart, lungs, liver and kidneys




1.  Central Nervous System  (CNS) Effects


          In the late 1800's, methyl chloroform was considered

superior to chloroform because it produces general anesthesia

with minimal excitation and  salivation.  Lazarew  (1929)

determined the concentration causing complete narcosis to be

45 mg/1 and the minimal fatal concentration 65 mg/1.  The ratio

between the concentration of the vapor causing the death and

that producing the loss of reflexes and that producing death

in mice was found to be 20,  as compared with 15 for chloroform.
                              29

-------
                            111-20





          Kranz, et al^.  (1959) estimated the dosage in dogs



to be 0.45 g/kg for induction of anesthesia and 0.80 g/kg for



causing respiratory failure.  The^ anesthetic index of methyl



chloroform was 1.77 for  dogs and 2.15 for monkeys, which



provide greater margins  of safety than those of chloroform.



Dornette and Jones (I960) used 1% to 2.6% methyl chloroform



(10,212 to 26,500 ppm) with 80% nitrous oxide for anesthesia



induction in 50 human subjects.  The volunteers were kept



anesthetized up to 2 hours,^maintained with increased methyl



chloroform levels of 0.6%-2.25% (6,127 to 22,982 ppm),



administered with decreased nitrous oxide-oxygen.  The



investigators attributed 75% of the anesthetic effect to



methyl chloroform and the remaining to nitrous oxide-oxygen



mixture.  Light anesthesia was induced within 2 minutes, and



recovery of reflexes occurred 3 to 5 minutes after discontinuing



the anesthetic agent.  Siebecker, e_t al. (1960) studied the



human electroencephalogram (EEC)in methyl chloroform (plus



nitrous oxide) anesthesia and found patterns similar to




halothane-





          The Romberg test (a neurological test that measures



proprioceptive control with a subject standing, feet together,



eyes closed) has been used to measure the narcotic or anesthetic-



like effects of methyl chloroform.  Stewart, e_t al. (1961)
                               30

-------
                             111-21



found 6 subjects failed  to perform  a  normal  test  after  15

minutes exposure at 2,650 ppm  (starting  at zero concentration),

but noted no CNS effects at  500  ppm.   Torkelson,  e_t  al.  (1958)

found positive Romberg tests in  all three subjects exposed  to

methyl chloroform at 1,740-2,180 ppm.  Lightheadedness

occurred in three of the four  subjects exposed to 1,000  ppm

for 70-75 minutes.



          Chemical tests of  motor reflex have demonstrated
                             \
reversible narcotic effects  by methyl  chloroform  in  human

subjects exposed to 250  ppm  (Gambarale and Hultengren, 1973),

450 ppm (Salvini, e_t al. 1971),  1,000  ppm for 70  to  75

minutes (Torkelson, e_t al. 1958), and  to 900 ppm  for 20  to  73

minutes (Stewart e_t al.  1961).   Stewart, e_t al. (1961) found

no CNS effects with balance  and  coordination tests following

methyl chloroform exposure at  500 ppm  for 3 hours, but observed

CNS effects in four of the five  subjects exposed  at  the  same

level for a longer time  (6.5 to  7 hours) (Stewart, e_t al. 1969)



          Stahl, e_t al.  (1969) reviewed  six fatal cases  of

exposure; autopsy samples showed the  concentration of solvent

to be: 0.32; 2.7; 9.3; 50.0; 56.0;  and 59.0 milligrams per

100 g brain tissue.  Kleinfeld and  Feiner (1966)  noted high,

but unquantitated, levels in brain  after a death  from methyl

chloroform.


                               31

-------
                            111-22
Summary


          The Romberg test  (a neurological test which measures

proprioceptive control) has been used to measure the narcotic

effects of methyl chloroform within the range from 500 ppm

(no CNS effects) to 2,650 ppm.  Impairment in motor control

after exposure to methyl chloroform has been demonstrated in
                            \
humans with concentrations  as low as 250 ppm, but CNS effects

appear to be dependent on methyl chloroform concentration as

well as exposure time.  Human autopsies following death due

to methyl chloroform show high, but unquantitated levels of

methyl chloroform in brain  tissues.
                               32

-------
                            111-23





2.  Cardiotoxicity





          The proarrhythmic activity of methyl chloroform has



been investigated in the dog.  Administration of methyl



chloroform to two dogs to induce anesthesia without premedication



was reported by Renmick et a_l. (1949) to have resulted in



sudden death.  Further experiments with five dogs under



barbital anesthesia showed that ventricular extrasystoles and



ventricular tachycardia were, regular occurrence when epinephrine



was injected after administration of repeated small doses of



methyl chloroform.  Maximum sensitization of the heart occurred



after administration of 0.25-0.40 ml/kg of methyl chloroform;



greater amounts raised the threshold dose of epinephrine,



partly because of severe hypotension.  They concluded that



epinephrine itself, however, is known to induce ventricular



extrasystoles and tachycardia, and the effects noted may have



been due, at least in part, to epinephrine.  Reinhardt, e_t



al. (1973) found the minimal concentration that causes



sensitization in the dog to be 27.8 mg/1.  The effective



concentration was 40.7 mg/1 in another group of dogs examined



by Clark and Tinston (1973).





          Somani and Lum (1965) and Lucchesi (1965) administered



133.6 mg/kg of methyl chloroform intratracheally and injected



epinephrine (10 ug/kg) intravenously.  This combination caused
                               33

-------
                            111-24


ventricular fibrillation.  However, dogs pretreated with a

beta-adrenergic blocking agent failed to exhibit any cardiotoxic

effects.


          The death of a young seaman due to methyl chloroform

abuse resulted in cardiac changes  (Travers, 1974).  Progressive

hypotension and bradycardia and several instances of cardiac

arrest resulted in death 24 hours after collapse.  Autopsy
                            \
showed right atrial and ventricular dilatation.


          Inhalation of high levels of methyl chloroform

produces a decrease in heart rate and blood pressure during

the first few minutes of exposure.  These effects have been

reported at 6,250 ppm for rabbits  (Truhaut, e_t al. 1972);

8,000 ppm for dogs (Herd, e_t al_. 1974); 25,000 and 50,000 ppm

for monkeys (Belej, et al. 1974).



          Cellular hypertrophy in the tissues following methyl

chloroform exposure (which is a sign of cardiovascular

toxicity) has been reported in several studies (Griffiths, et_

al. 1972; Adams, e_t al. 1950; Horiguchi and Horiguchi, 1971;

Rice, et al. 1967).  Huroan autopsy reports have mentioned

tissue congestion following deaths due to methyl chloroform,

expecially after prolonged abuse or high exposure (Hall and

Hine, 1966; Stahl, et al. 1969; Hatfield and Maykoski, 1970).
                               34

-------
                            111-25


Summary


          Methyl chloroform-induced cardiotoxicity has been found

in animal experiments  (dogs, rabbits, and monkeys) and in

human autopsy reports, where cellular hypertrophy in the

cardiac tissues following methyl chloroform abuse or high

exposure has been present.


3.  Hepatotoxicity and Nephrotoxicity
                            v

          Liver cell damage produces an increase in cytoplasmic

transaminase, followed by lactic dehydrogenase (LDH) from the

mitochondria.  To determine the organ source of these enzyme

level changes after methyl chloroform exposure, the LDH must

be electrophoretically fractionated.


          Platt and Cockrill (1969) found increases in only

two of seven enzymes measured in rats given methyl chloroform

(1,650 mg/kg) orally in liquid paraffin for 7 days.  The

NADPH2~cytochrome C reductase and glutamate dehydrogenase

activity of rat liver were significantly increased in the

treated animals.


          Klaassen and Plaa (1969) found no elevation in liver

triglycerides within the first 36 hours after exposing rats

to methyl chloroform at 3,800 mg/kg (75% of the LD50).
                              35

-------
                            111-26






          Six controlled human studies showed that the urinary



urobilinogen was the most sensitive test for ascertaining



hepatotoxicity in subjects exposed to methyl chloroform



(approximately 500 ppm or above)  (Stewart, e_t al_. 1961).  The



serum glutamic oxaloacetic transaminase (SCOT) values and the



15 minute phenosulfonphthalein (PSP) excretion deviated



somewhat from pre-exposure values, but remained within normal



limits.






          The lowest concentration of methyl chloroform that



resulted in hepatic effects was reported by McNutt, e_t al.



(1975) who found significantly elevated triglyceride levels



in mice exposed to 250 ppm for 4  and 13 weeks.  MacEwen, et



al. (1974), however, failed to produce elevated liver



triglycerides in mice exposed continuously to 250 ppm for 100



days, but observed the effects at 1,000 ppm.





          Krantz, e_t al. (1959) found no effects from methyl



chloroform on phenosulfonphthalein retention time in an



anesthetized dog, but repeated administration of the anesthesia



resulted in hepatic pathology in  one of the four rats.





          Horiguchi and Horiguchi (1971) reported congestion



of the liver and bile duct inflammation in male mice exposed



to 1,000 ppm of methyl chloroform (2 hours, nine times).
                               36

-------
                            111-27


          Plaa (1976) summarized in Table  III - 5 work on

trichloroethylene, methyl chloroform, and perchloroethylene

with respect to liver toxicity.  The table shows that toxicity

is a function of the test used for all the halogenated compounds.


          Hanasono, et al.  (1975) exposed male rats to 1.0 ml

methyl chloroform/kg interperiotoneally 3 days after admin-

stration of alloxan which produced diabetes symptoms but no

serum glutamic pyruvic transaminase (SGPT)or triglyceride

change.  The hepatotoxic effects of methyl chloroform in con-

trol and diabetic rats are  evident from SGPT and trigylceride

levels, observed as follows:



                            SGPT        Triglyceride in liver
                         (units/ml)      	(mg/g tissue)

Controls                    42 + 2          5.7 + 0.5

Diabetic                    65 + 19        21.6 + 13.1



          Rice, e_t al. (1967) gave rats methyl chloroform (2

ml/kg) 24 hours before performing hemodynamic measurements on

the isolated, perfused livers.  Under in_ vitro conditions,

hepatic blood flow was not  changed by the pre-treatment,

although carbon tetrachloride did change blood flow character-

istics in the same experimental series.  A subcapsular

inflammatory reaction was found in the livers of animals

pretreated with methyl chloroform.


                              37

-------
                                       Table III-5
                          LIVER EFFECTS OF METHYL CHLOROFORM AND
                              OTHER CHLORINATED HYDROCARBONS
                   Relative potency rankings of the subject halogenated
                                   hydrocarbons in mice
   Compounds
24-HR LD5o)
(mmole/kg)
   Compounds
 (BSP Re-
tention ED50)
 (mmole/kg)
Compounds
   SGPT Ele-
vation ED5Q )
 (mmole/kg)
Trichloroethylene
Perchloroethylene
Methyl chloroform
   Compound
    24
    28
    37
Trichloroethylene
Methyl chloroform
Perchloroethylene
      23     Methyl chloroform
      27     Trichloroethylene
      32 •-   Perchloroethylene
                     Potency ratios of the three subject solvents for
                         SGPT elevation or BSP retention in mice
                   2.5
                  18
                  28
              BSP Retention potency
                 ratio (LD50/ED5Q)
                                  SGPT Elevation potency
                                    ratio (LD50/ED50)
Methyl chloroform
Trichloroethylene
Perchloroethylene
                       1.4
                       1.0
                       0.9
                                           1.5
                                           1.3
                                           1.0
                                            38

-------
                                          111-29
                                 Table III-5  (Continued)

             Severity of liver injury induced by minimal lethal doses of the
                   tnree subject solvents; SGPT elevation being used as
                            the index of hepatic dysfunction^T

                                             SGPT (R-F units)
                   	Compound	Dogs        Mice

                   Perchloroethylene         400          Nil
                   Methyl chloroform         350           65
                   Trichloroethylene         250           90
3y The ranking is:  most potent first and least potent last.

Adapted from:  Plaa (1976).
                                39

-------
« •




                               111-30
            Using  in vitro experimental  conditions,  Fuller, et



  al.  (1970)  found an  increase  in  the metabolism  of  hexobarbital,



  meprobamate, and zoxazolamine  in rats  following  the  inhalation



  of methyl chloroform (2,500 to 3,000 ppm)  for 24 hours.



  There was an increase  rn vitro of  the  metabolism of  these



  three compounds  by hepatic microsomal  enzymes under  the



  influence of methyl  chloroform.





            The  inhalation of methyl chloroform at a level of



  approximately  10,000 ppm for  4 to  6 hours  had no effect on



  liver function of ethanol-exposed  rats,  although other



  chlorinated/hydrocarbons exhibited increased hepatotoxicity



  (Cornish and Adefuin,  1966).   Cornish, e_t  al. (1973) also



  failed  to demonstrate  increased  hepatotoxicity  due to methyl



  chloroform  in  rats pretreated  with phenobarbital.  Carbon



  tetrachloride  was more hepatotoxic in  the  phenobarbital-



  treated rats.





            Ingestion  of ethanol was reported by  Klaassen and



  Plaa  (1966) to increase the hepatotoxicity of methyl chloroform,



  Ethanol (60%)  was administered by  gavage at doses of 5 mg/kg.



  In one  experiment, a dose of  ethanol was given  on each of 3



  days before intraperitoneal administration of methyl chloroform



  in corn oil (0.02 ml/g) at doses of 2.5-2.75 ml/kg.  In



  another experiment,  a  single  dose  of ethanol was given 12



  hours before the methyl chloroform.  In  both experiments, BSP






                                 40

-------
                            111-31





retention was significantly higher in the ethanol pre-treated



rats than in control rats given only methyl chloroform.  SGPT



activity was not affected in this" experiment by methyl



chloroform at a dose of 2.5 ml/kg with or without alcohol pre-



treatment, and kidney function as measured by PSP excretion



was similarly not affected by methyl chloroform doses of 2.0



ml/kg.  SGPT activity was also not different from controls in



dogs given methyl chloroform doses of 0.85 ml/kg, with or



without ethanol pre-treatment (Klaassen and Plaa, 1967).





          Isopropyl alcohol or acetone administered by gavage



to male Swiss-Webster mice 18 hours before i.p. injection of



methyl chloroform did not alter the response of SGPT activity



to the administered methyl chloroform (Traiger and Plaa, 1974).



The doses of methyl chloroform used in this experiment were



1.0, 2.0 and 2.5 ml/kg.  The latter dose caused increases in



SGPT activity, but the increases were not affected by isopropyl



alcohol or acetone pretreatment.





          In laboratory animals, liver function appears to be



readily influenced by methyl chloroform.  Klaassen and Plaa



(1967) reported disturbances in liver functions in dogs.



Similarly, rabbits exhibited hepatic function changes.





          Adams, e_t al. (1950) reported no adverse effects



in guinea pigs given 1,500 ppm of methyl chloroform for 7
                              41

-------
                            111-32





hours/day for 3 months.  Conversely, Torkelson, e_t al^. (1958)



reported liver effects in animals exposed to both 1,000 and



2,000 ppm levels of methyl chloroform for 30 to 90 minutes/day



for 3 months.  Klaassen and Plaa (1966) noted enlargement of



hepatocytes with cellular infiltration and vacuolation in



mice following methyl chloroform treatment.  Slight hepatic



narcosis occurred only when the dosage was in the lethal



range.  Von Oettingen (1964) suggested that the mechanism of



hepatic changes is a functidn of the lipid solubility of the



methyl chloroform.





          Signs of hepatic effects include retention of BSP



and change in SGPT activity following injection or inhalation



of methyl chloroform.  Gehring (1968) found the £050 for SGPT



activity was 2.91 g/kg in mice, whereas Klaassen and Plaa



(1966) found a value of 3.34 g/kg for the same effect.  The



inhalation EV$Q for SGPT activity in mice was 13,662 ppm for



approximately 10 hours (Gehring, 1968).





          Plaa and Larson (1965) reported that only one of



the nine mice given methyl chloroform (3,400 mg i.p./kg)



exhibited significant proteinurea.  In another trial, mice



exhibited swelling of the convoluted tubules of the kidney



after a similar dose of methyl chloroform.  However, no



necrosis was observed in these studies.  Renal toxicity



(tubular damage) in mice was also observed in another study





                              42

-------
                            111-33

(Klaassen and Plaa, 1966).  These authors studied renal
function patterns in dogs exposed to methyl chloroform and
found renal changes as determined by phenolsulfonphthalein
glucose, and protein excetion data, but no histopatho-
logical changes (klaassen and Plaa, 1967).  According to
these data, the kidney is less affected by methyl chloroform
than the liver.

          Stewart (1971) reported several instances of apparent
kidney toxicity related to methyl chloroform exposure in
humans.  According to a human ingestion study, elevated serum
bilirubin and evidence of kidney injury associated with
hematuria and proteinurea were seen.  In other studies
exposures to the solvent (900 ppm for 20 minutes) produced
elevated urinary urobilinogen in one subject, and some evidence
of adverse effects on kidneys (dye clearance rate, hematuria)
was observed in six subjects after exposure to 500 ppm of
methyl chloroform for 78 minutes.  Five of the seven subjects
exposed to methyl chloroform (0 to 2,650 ppm) for 15 minutes
exhibited a few erythrocytes in the urine and/or a positive
urinary urobilinogen  (Steware, e_t a_l. 1961).

Summary
          Various experiments using rats, dogs, and mice to
determine the influence of methyl chloroform on liver function
provide conflicting results due to variation in animal species,

                              43

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                            111-34





dose, and treatment schedule.  For example, guinea pig



experiments have shown: 1) no organ damage following exposure



to 1,500 ppm of methyl chloroform for 7 hours/day for 3



months, and again, 2) liver damage due to 1,000 ppm of methyl



chloroform for 30 to 90 minutes/day for 3 months.





          Nephrotoxicity, as measured by tubular damage, PSP,



glucose, and protein excretion data has been investigated in



animals and man with reference to exposure to methyl chloroform,



Although some kidney damage in laboratory animals has been



reported, it appears that methyl chloroform affects the liver



before it damages the kidneys.





4.   Pneumotoxicity





          Irritation of the lungs and respiratory tract as a



result of methyl chloroform inhalation has been observed in



industrial workers and experimental animals (Stewart, et al.



1961; 1969; Salvini, e_t a_l. 1971).  Humans occupationally



exposed to methyl chloroform by inhalation and skin contact



for  prolonged periods complained of irritation of the upper



respiratory tract (Weitbrecht, 1965).  American industrial



workers, who were chronically exposed to the compound at low



levels also have complained of respiratory tract irritation



(Vandervort and Thoburn,  1975; Hervin, 1975).  Nearly all



National Institute for Occupational Safety and Health Hazard
                               44

-------
                            111-35








Evaluation Reports on methyl chloroform, when instituted by



worker complaint, were due to strong solvent odor and throat



irritation (1978).  In nearly all cases the levels in ambient



air were far below the maximum allowable concentrations.



There is no idication in the literature that the lungs of man



or animals become hypersensitive following repeated inhalation,



but the irritation is apparently a matter of concern.





          In animal studies,^structural changes in the lungs



were seen in guinea pigs exposed to 1,000 ppm of methyl



chloroform for 72 minutes/day (69 exposures), and to 2,000



ppm for 12 minutes/day for 69 exposures.  On the other hand,



1,000 ppm for 36 minutes/day (69 exposures) produced no lung



irritation (Torkelson, e_t al. 1958).  Prendergast, e_t al.



(1967) exposed several animal species to 370 ppm of methyl



chloroform continuously for 90 days but observed only non-



specific inflammatory changes in the lungs.





          MacEwen and Vernot (1974) reported that the most



significant effect seen in rats continuously exposed to methyl



chloroform by inhalation for 100 days was respiratory disease.
                              45

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                            111-36


Lung changes were seen in approximately half of the rats

exposed to 250 and 1,000 ppm.


          Pulmonary congestion in animal inhalation experiments

has been widely reported, particularly for chronic (or high-

level) exposures to methyl chloroform (Horiguchi and Horiguchi,

1971).  Pulmonary edema and congestion, however, are consistent

with cardiovascular insufficiency rather than primary lung
                           \
effects.  The lung effects appear to be limited to irritation,

and are reported to be transitory in humans, even following

moderately high exposures to the compound (Weitbrecht, 1965).


Summary


          The possibility of increased pneumotoxicity due to

"additive" exposure to various levels of methyl chloroform

from food and drinking water contamination cannot be ignored.

However, the effects of the compound through ingestion would

be less severe than effects from inhalation since the small

amount of compound is eliminated via the gastrointestinal tract

in the urine and feces.
                              46

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 V.  HEALTH EFFECTS  IN ANIMALS                                |

 1.  Acute Toxicity

           Lazarew  (1929)  exposed  an  unspecified  number  of

 mice to methyl chloroform to determine  the  minimum concentration

_required to produce prostration,  loss of  reflexes  and death

 within 2 hours of exposure (Table V-l).


           Table V-l EFFECTS OF  TRICHLOROETHANE ISOMERS  ON  MICE
                                  Minimum Concentration  for  Response
                                  Within  2 Hours  of  Exposure  (mg/1)

 Compound                 Proneness         Loss of Reflex      Death


 Methyl  chloroform           40                   45            65
 l,l,22trichloroethane       10                   15            60
 Adapted  from:   Lazarew  (1929)


            Lazarew  assigned  toxicity  ratings  to  the  12  compounds

 based  on concentrations  required  to  produce  prostration.

 Higher indices  meant  greater  toxicity.   The  index  for  methyl

 chloroform was  3.5 compared to 14 for 1,1,2-trichloroethane,

 meaning  that the 1,1,2-isomer was 4  times  as toxic  as  the

 methyl chloroform  isomer.   The acute oral  L£>$Q  for  methyl

 chloroform, as  determined  in  several species of animals,  is

 reported by Torkelson, e_t  al.  (1958) to range from  5.7 to

 14.3 g/kg.  Unfortunately,  little other toxicological  data
                                47

-------
                             V-2
involving oral ingestion are available.  LDsg values that



were derived upon administration of methyl chloroform by routes



other than oral illustrate the difficulty in using such data



to predict consequences of ingestion of the chemical.  In



contrast with an oral LDsg value of 11 g/kg in the mouse



(Torkelson, e_t a_l. , 1958), the LV$Q is approximately 16 g/kg



for subcutaneous injection (Plaa, e_t aJL. 1958) and approximately



4.9 g/kg for intraperitoneal injection (Klaassen and Plaa,



1966). By administering equivalent intraperitoneal and oral



doses of carbon tetrachloride to rats, Nadeau and Marchand



(1973) demonstrated that significantly higher hepatic



concentrations of carbon tetrachloride and more extensive



hepatotoxicity are manifested in the animals given the compound



intraperitoneally.





          Despite the problems that are inherent in extrapolating



data from one route of chemical exposure to another, we may



gain qualitative insight into the toxicity of methyl chloroform



by examining information from studies in which the oral route



was not used.  Plaa and his colleagues found methyl chloroform



to be the least hepatotoxic of a series of alkyl halocarbons



that were given subcutaneously (Plaa et al., 1958) and



intraperitoneally  (Klaassen and Plaa, 1966) to mice and



intraperitoneally to dogs  (Klaaassen and Plaa, 1967) and rats



(Klaassen and Plaa, 1969).  Near-lethal quantities of methyl
                               48

-------
                             V-3

chloroform were generally required  to produce hepatotoxicity.
The authors observed little to no evidence of nephrotoxicity.
In contrast to methyl chloroform  (ED$Q  =  2.5 ml/kg for SGPT
elevation in mice), its congener  1,1 , 2-trichloroethane was
much more toxic (EDso =0.1 ml/kg), and tetrachloroethylene
was of equivalent potency (EDso =2.9 ml/kg).
          In laboratory animals, as well as humans, the
primary hazard of inhalation of high concentrations of methyl
chloroform is excessive depression of the CNS.  Adams e_t al .
(1950) reported the 3-hour LCso in rats to be 18,000 ppm.
They observed that recovery of several test species of animals
from marked depression of the CNS was rapid and uneventful.
The lowest and shortest exposure that elicited histological
change in tissues of the rat was 8,000 ppm for 7 hours.  This
treatment produced an increase in liver weight and fatty
vacuolation of hepatocytes.  Dis-turbance of vestibular function
in rabbits infused intravenously with methyl chloroform was
observed by Larsby e_t al . (1978) when blood levels exceeded
75 ppm of methyl chloroform.  Also, levels of methyl chloroform
in the cerebrospinal fluid were approximately one-third of
that in the blood.  Although this vestibular disturbance is
physiologically significant, it should be noted that Gamberale
and Hultengren (1973) observed inhibition of psychophysiological
function in humans with blood levels of only 3-5 ppm of methyl
chloroform.
                              49

-------
                             V-4

          A second hazard associated with acute exposure to
vapor containing high concentrations of methyl chloroform is
cardiovascular toxicity.  The aforementioned accounts of
cardiotoxic effects of methyl chloroform in humans  (Bass,
1970; Dornette and Jones, 1960) have been confirmed in studies
of dogs.  Reinhardt e_t al.  (1973) found methyl chloroform to
be more potent than trichloroethylene in inducing arrhymias
in dogs given epinephrine concomitantly.  The lowest effective
concentration of methyl chloroform was 5,000 ppm.  However,
Egle et al. (1976) did not  detect adverse cardiovascular
effect in dogs that had been exposed to 5,000 and 10,000 ppm
methyl chloroform in a Freon propellant.  They attributed the
disparity between their own findings and those of Reinhardt et
al.  (1973) to differences in the experimental design.  Herd ejt al.
(1974) found methyl chloroform to exert a biphasic action
on the cardiovascular system of anesthetized dogs, which was
characterized by an initial decrease in blood pressure that
was associated with peripheral vasodilation as well as reflex
chronotropic and inotropic  effects on cardiac function, and
subsequent depression of cardiac function.  In a study of the
biochemical mechanism of methyl chloroform's cardiotoxicity,
Herd and Martin (1975) observed inhibition of respiratory
function and alteration of  permeability characteristics in
mitochondria that were isolated from rats.  Herd et al. (1974)
emphasized that studies are needed to determine whether low-level

                              50

-------
                             V-5



exposure to methyl chloroform may be injurious to the

cardiovascular system.



          In constrast to previous findings of microsomal

enzyme induction in mice  (Lai and Shah, 1970) and rats  (Fuller,

1970) that inhaled 3,000 ppm methyl chloroform for 24 hours,


inhibition of microsomal drug metabolism was observed in rats

given approximately 1.4 g/kg orally (Vaino e_t al. , 1976) and

in mice 1.0 ml/kg of undiluted methyl chloroform intraperitoneally
                            \
(Shah and Lai, 1976).  The animals were sacrificed 24 hours

following administration of methyl chloroform.  Shah and Lai

(1976) further demonstrated that dilution of methyl chloroform

with dimethylsulfoxide (DMSO) potentiated the effect, while

methyl chloroform, diluted with olive oil, reduced the inhibitory

effect.  Shah and Lai suggested two factors that may be

important are (a) the augmentation (or retardation) of absorption

of chemicals by the use of different vehicles and (b) whether

the chemical enters the systemic circulation directly (via

inhalation) or is taken at once to the liver by way of the

portal circulation (after intraperitoneal circulation).




2.  Subacute Toxicity



          MacEwen, e_t al. (1974) exposed monkeys to 250 ppm

and 1,000 ppm methyl chloroform for 14 weeks via inhalation.
                              51

-------
                             V-6






There were no significant changes in hemoglobin, red blood cell



(RBC) and white blood cell (WBC) counts, Na K alkaline phosphatase,



SCOT, SGPT, creatinine, chloride, glucose, blood urea nitrogen,



albumin, globulin, total protein, calcium, cholesterol, total



bilirubin, and serum triglycerides.  Additionally, no pathol-



ogical changes were detected at these concentrations.






          Adams, et al. (1950) exposed one female monkey



to 3,000 ppm of methyl chloroform for 7 hr/day  (53 exposures)



over 74 days via inhalatioA.  The monkey was necropsied and



no pathological changes were found in the lungs, heart,



liver, kidneys, lymph nodes, spleen, adrenals,  pancreas,



stomach, small and large intestines, bladder, thyroid gland,



and skeletal muscles.





          Prendergast, e_t a_l_. (1967) exposed squirrel monkeys



to methyl chloroform by inhalation as follows:  2,700 ppm (8



hr/day) for 6 weeks, 450 ppm (continuously) for 90 days; and



165 ppm (continuously) for 90 days.  The monkeys exposed to



2,700 ppm lost 3% of their body weight, but no microscopic



pathological changes were seen, whereas the animals given 450



ppm exhibited a weight loss equalling 4% and lung inflammation.



The monkeys exposed to 165 ppm gained weight but showed signs




of lung congestion.
                              52

-------
                             V-7



          Prendergast, e_t al.  (1967) exposed beagle dogs to


methyl chloroform by inhalation as follows:  2,700 ppm  (8


hr/day) for 6 weeks; 450 ppm (continuously) for 90 days; and


165 ppm (continuously) for  90  days.  Dogs given 2,700 ppm


lost 2% of their body weight and showed blood leukopenia, but


no changes in the lungs; whereas dogs exposed to 450 ppm


gained weight (5% less controls) but exhibited lung inflammation


Dogs given 165 ppm gained weight normally, but showed sporadic


lung congestion.
                            \


          Adams, e_t al.  (1950) exposed female albino rabbits


to 5,000 ppm of methyl chloroform by inhalation (7 hr/day)


for a total of 44 days.  The animals manifested a slight


depression of growth rate but  no other pathological changes


were reported.



          Prendergast, et al.  (1967) exposed guinea pigs to


methyl chloroform by inhalation as follows:  2,700 ppm  (8


hr/day) for 6 weeks; 450 ppm (continuously) for 90 days; and


165 ppm (continuously) for  90  days.  Guinea pigs exposed to


2,700 at dose fl were all normal.  Dose #2 animals had  non-


specific lung inflammation,  but clinical chemistry and  blood


were normal; dose #3 animals showed sporadic lung congestion,


but, as with dose #2, clinical chemistry and blood were normal.


All animals at all doses survived.
                               53

-------
                             V-8





          Adams, et al. (1950) exposed 71 mixed strain, mixed



sex, guinea pigs (roughly divided into male/female dose



groups) to methyl chloroform as follows:






Dose fl:   45 days, 5,000 ppm, 7 hr/day, 5 days/week,



           32 exposures



Dose |2:   29 days, 3,000 ppm, 7 hr/day, 5 days/week,



           20 exposures



Dose #3:   60 days, 1,500 ppm, 7 hr/day, 5 days/week,



           44 exposures



Dose .#4:   92 to 93 days, 650 ppm, 7 hr/day, 5 days/



           week, 65 to 66 exposures



Dose #5:   57 to 58 days, 650 ppm, 7 hr/day, 5 days/



           week, 40 to 41 exposures





Significant decreases in growth rate occurred at all doses.



Organ weights and clinical chemistry were normal at all dose



levels.  Microscopic pathology was normal at 1,500 ppm or



less (doses #3, #4, and #5).  At 5,000 ppm (dose #1), there



was slight centrilobular fatty infiltration in the livers but



no necrosis; slight testicular degeneration also occurred.



At 3,000 ppm (dose #2), the livers showed slight centrilobular



fatty infiltration, with small fat-staining globules in the



central hepatocytes.
                              54

-------
v                               V-9


   Summary


             The  studies  discussed above present strong  evidence

   that  laboratory animals (dogs,  rabbits,  monkeys)  under a wide

   variety  of dosage  and  treatment schedules presented symptoms

   such  as  weight losses/or depressed growth rate,  and lung

   inflammations,  etc.,  but no pathological changes  were detected

   at the  subacute toxic  levels of methyl chloroform used in the

   various  studies.   As  acute toxicity levels of methyl  chloroform
                               \
   were  approached for specific animal models, hepatotoxicity

   increased  significantly.


   3. Chronic Effects
             McNutt e_t al .  (1975)  exposed mice continuously to

   250  and  1,000 ppm methyl chloroform for up to 14 weeks.

   Sacrifices were performed at weekly intervals to ascertain

   the  development of any histopathologic abnormalities.

   Hepatocytic vacuolations and significant increases  in  liver

   weight and triglyceride  content were observed throughout the

   study in animals exposed to 1,000 ppm.  After weeks of exposure

   to 1,000 ppm methyl chloroform, a number of ultrastructural

   alterations were observed in centrilobular hepatocytes,

   including proliferation  of smooth endoplasmic reticulum.

   Such a structural alteration would be expected in light of

   the  reports of microsomal enzyme induction by Fuller,  ejt al.
                                 55

-------
(1970) and Shah and Lai (1976).  McNutt, et al.  (1975) saw a '



return to normal of each of the indices at 2 and 4 weeks



after exposure.  Mild or moderate ultrastructural alterations



and increases in liver weight and triglycerides were occasionally



observed in the animals that were exposed to 250 ppm during a



14-week study.  Thus, this exposure level might be considered



a threshold for a biological effect of methyl chloroform in



the mouse.  Platt and Cockrill (1969) studied biochemical



changes in rat livers in response to a series of aliphatic



halocarbons.  The authors found that seven daily oral doses



of 1.65 g/kg enhanced the cytoplasmic and microsomal protein



content without producing any hepatotoxic effects.  Savolainen,



et al. (1977) recently reported slight decreases in brain



ribonucleic acid (RNA)and liver microsomal P-450 in rats



inhaling 500 ppm of methyl chloroform (6 hours daily) for 4



or 5 days.  The significance of these latter findings is



uncertain.





          Two lifetime feeding study that have been reported



were conducted as a part of the National Cancer Institute



Bioassay Program (NCI, 1977, NCI, 1983).  In an initial range-



finding study, oral doses ranging from 1,000 to 10,000 mg/kg



methyl chloroform in corn oil were given to male and female



mice and rats 5 days weekly for 6 weeks.  The highest "noeffect"



dose for rats was 3,160 mg/kg while that for mice was 5,620



mg/kg.  Indices of toxicity that were evaluated included





                              56

-------
                             V-ll






body weight and gross evidence of organ damage.  A chronic



dosing study was then initiated but had to be discontinued



because of undefined intoxication in rats receiving 3,000



mg/kg.  In the final chronic study, male and female rats



received 750 or 1,500 mg/kg of methyl chloroform in corn oil



by gavage five times weekly for 78 weeks.  Similarly, male



and female mice were given methyl chloroform doses that were



increased during the study when it became apparent that larger



quantities of the chemical could be tolerated.  The time-



weighted averages for the two dose levels in mice for the 78-



week regimen were approximately 2,800 and 5,600 mg/kg.



Diminished body weight gain and decreased survival time were



manifested in both mice and rats.  Surprisingly, the incidence



of histopathologic change was no greater for methyl chloroform



dosed than, for control animals of either species.  No other



indices of toxicity were evaluated.





          A repeat carcinogenesis bioassay of methyl chloro-



form was conducted by administering the test chemical in corn



oil by gavage to groups of 50 male and 50 female F344/N rats



at doses of 375 and 750 mg/kg body weight.  Groups of 50 male



and 50 female B6C3F1 mice received 1,500 or 3,000 mg/kg body



weight.  Methyl chloroform was administered five times per



week for 103 weeks.  Groups of rats and mice of each sex



received corn oil by gavage on the same schedule and served



as vehicle controls.  Rats: Mean body weights for control



and dosed rats were comparable throughout the two year study.
                               57

-------
                             V-12
there were no tumors in rats considered to be related to



administration of methyl chloroform.  However, the large



number of accidental deaths among- dosed females  (25 low dose,



17 high dose) and dosed males  (14 low dose, 8 high dose) reduced



the sensitivity of this study  for detecting late-appearing tumors



in these groups.  Mice: Survival of high dose male mice (28/50)



was significantly (P < 0.01) less than that of the vehicle



controls (44/50).  There was a significant (P <  0.05) dose



response trends and increased  incidences of hepatocellular



carcinomas in low and high dose male and in high dose female



mice.



          A number of long-term animal studies of the toxic



potential of inhaled methyl chloroform have been conducted



over the last 20 years.  These studies have been directed



largely towards assessing potential hazards of methyl chloroform



in occupational exposure situations.  Daily exposure of a



variety of species to 500 ppm  of methyl chloroform over a 6-



month period elicited no recognizable adverse effect, but



1,000 ppm produced fatty and enlarged livers in  guinea pigs



(Torkelson, e_t a_l. , 1958).  Rowe, e_t a_l. (1963) reported



similar findings when testing  a solvent mixture  consisting of



approximately 75% methyl chloroform and 25% tetrachloroethylene.



However, guinea pigs in the latter study did show some decrease



in body weight gain, which was attributed to reduced food



consumption, as well as an increase in liver weight.  In
                           58

-------
                              V-13
 studies of response to even lower concentrations,  Prendergast,
 et  a_l.  (1967)  exposed rats, guinea pigs,  dogs, rabbits,  and
 monkeys to methyl chloroform vapor continuously for 90 days.
 They  observed  depressed body weight in rabbits and dogs
 inhaling 370 ppmf but no adverse effects  in any species
 inhaling 135 ppm.  Eben and Kimerly (1974)  detected no evidence
 of  hepatorenal injury,  hematologic change,  or histopathologic
 alteration in  rats that received 200 ppm  of methyl chloroform
 8 hours daily  (5  days a wee)c)  for 14 weeks.

 Summary
           Daily exposure to 500  ppm of methyl chloroform  over
 a 6 - month period elicited no recognizable adverse effects
 in  rats,  guinea pigs  and other animal  species,   however,
 1000 ppm produced fatty and enlarged livers in guinea  pigs.

 4.  Mutagenicity

           The  mutagenicity  of  methyl chloroform has  been
evaluated  in the  B6C3F1  mouse  using  a  host-mediated  assay with
Schizosaccharomyces bombe (Lobrien e_t  a1.,  1979).   The investi-
gators  have reported  that methyl  chloroform administered by
gavage  at  500 mg/kg did  not  increase the  incidence  of mutations
in J3.  bombe measured  after  treatment following  3,  6, and 16
hours.  No information was provided  concerning  whether or
not testing was conducted to determine  the  ability  of methyl
                              59

-------
                             V-14

chloroform to induce mutations ^n vitro.  In addition, no
data are presented concerning a determination of the toxicity
of the substance to mice after acute exposure to arrive at a
maximum tolerated dose for conducting the host mediated
assay.  Therefore, it makes it difficult to assess the signi-
ficance of the results.

          Two tests of the mutagenic potential of methyl
chloroform in bacteria were reported to have been conducted
using protocols designed to «prevent evaporation of methyl
chloroform and thereby ensure exposure of the indicator
organisms.  Both tests were reported to yield positive results
(Simmon e_t al.1977 and Snow e_t al. 1979).  The testing
performed by Simmon and coworkers was conducted using the
standard battery of Salmonella typhimurium strains TA 1535,
TA 1537, TA 1538, TA 98, and TA 100, both with and without
metabolic activation of rat liver microsome S9 fraction.  The
concentrations used for testing were 0, 100, 200, 300, 400,
500, 750, and 1000 ug/g - liter desiccator.  A weak dose-
related response was observed for TA 100 both with and without
metabolic activation.  The exact purity of the methyl chloroform
sample tested was not given but was reported to be high.

          In their studies, Snow e_t al. (1979) tested two
samples of methyl chloroform in Salmonella strain TA 100 both
with and without metabolic activation.  Testing conducted with
                               60

-------
                             V-15

metabolic activation employed an S9  fraction obtained from
methyl chloroform induced Syrian golden hamster liver micro-
somes.  Similar to the study performed by  Simmon et al.  (1977),
precautions were reported to have been taken to prevent evapo-
ration of methyl chloroform.  Doses  of 0,  500, 750, 1000, and
1500 ul/5.€ liter modular incubator  chamber were employed.
Positive response was obtained  for TA 100  to the two samples
of methyl chloroform tested.  One of the sample was from
Aldrich (97% methyl chlorofo,rm  stabilized  with 3% p-dioxane)
and the other was from PPG  Industries (reported to be purified
sample).

          In a chronic inhalation study, 96 male and 96 female
rats were exposed to methyl chloroform at  levels of 1,750 or
875 ppm for 6 hr/day, 5 days/week, for 12  months (Quast, e_t
al. 1978).  Cytogenic examination of bone  marrow cells from
rats sacrificed after 12 months indicated  neither chromosomal
damage nor chromatid aberrations in  male rats.  The number
of scorable chromosome spreads  for the female rats was very
low overall; consequently data  on female rats were not pre-
sented.
          A test of cell transformation using the Fischer rat
embryo cell line F170 was performed  with methyl chloroform
and other solvents.  The transformed cells produced fibrosarcomas
                               61

-------
                             V-16



in rats when they were inoculated.  The potency of the methyl


chloroforminduced transformation was similar to that produced


by trichloroethylene  (Price, e_t a_l. 1978).



          Henschler e_t al.  (1977) tested the mutagenic


potential of methyl chloroform by the Ames test using Salmonella


tester strain TA 100  (a highly sensitive strain).  Methyl


chloroform was non-mutagenic in both activated and unactivated


tests.


                            \
Summary


          Mutagenicity testing of methyl chloroform has proven


inconclusive.  The above discussion of various test systems


evaluating the mutagenicity of methyl chloroform yielded the


following results:  2 positive (methyl chloroform is weakly


mutagenic)> 3 negative, and 1 inconclusive.  The inconsistent


findings  concerning the mutagenic potential of methyl chloroform


could not be thoroughly evaluated since sufficient scientific


data were not given by the various investigators in their


reports.  Scientific data such as: protocol design, maximum


tolerated dose, purity of experimental compound, controls


(negative, postive), etc. were not presented in detail.



5.  Carcinogenicity



          Although a variety of neoplasms were observed in


methyl chloroform treated rats and mice and their respective
                              62

-------
                             V-17





controls, no positive correlation relationship was found



between treatment and incidence of neoplasm.  The shortened



lifespans of the rats and mice made an assessment of ingested



methyl chloroform carcinogenicity impossible  (National Cancer



Insititute, 1977).  In the earlier studies, rats of the



Osborne-Mendel strain and B6C3F1 mice (50 of each sex of



each rodent) were given methyl chloroform orally in corn oil



at each of two dose levels 5 days/week for 78 weeks.





          Rats on chronic studies received high and low doses



of 1,500 or 750 mg/kg; mice received adjusted doses averaging



5,615 or 2,807 mg/kg.  The methyl chloroform used in the



carcinogenicity studies was technical grade.  Male and female



weanlings were started on the test at 5 weeks of age and



sacrificed at 96 weeks of age.  Initially, the doses for male



and female mice were 4,000 and 2,000 mg/kg body weight.  During



the 10th week of the study, doses were increased to 5,000 and



2,500 mg/kg.  During the 20th week of the study, doses were



again increased to 6,000 and 2,000 mg/kg and maintained at



these levels to the end of the study-





          At death, all animals were necropsied except those



in which autolysis had occurred.  Approximately 29 different



tissues were fixed informalin, sechoned, stained, and examined



microscopically.  Comparison of the numbers and distribution
                              63

-------
                             V-18





of lesions in treated and control groups revealed no excess



of histopathological lesions that could be related to treatment,





          The median survival of all groups except the female



control mice was lower than would normally be expected.  This



may be due, in part, to the chronic murine pneumonia which



was prevalent and was the most probable cause for the high



incidence of natural deaths.





          In the repeat NCI bioassay study (1983), Fischer



344/N rats and B6C3F1 mice were gavaged with daily doses of



375 or 750 mg/kg body weight (rats) and 1,500 or 3,000 mg/kg



body weight of methyl chloroform in corn oil, respectively.



The compound was administered to groups of 50 rats and 50



mice (each sex) five times per week for 103 weeks.  There was



no change in mean body weights for control and dosed rats,



however, mean body weights of dosed male and female mice were



slightly lower than those of the vehicle controls.  No methyl



chloroform related tumors were observed in rats, but the



large number of accidental deaths among dosed females (25 low



dose; 17 high dose) and dosed males (14 low dose; 8 high



dose) reduced the sensitivity of this study for detecting



late-appearing tumors in those groups.





          In mice, (NCI, 1983), there was an increase in



hepatocellular carcinomas occurrence in low and high dosed



male and in high dosed female mice:  males - vehicle control





                              64

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                             V-19






16/50, low dose 24/50, high dose 20/50; females - vehicle



control 3/49, low dose 5/49, high dose 10/49.  NCI



concluded that: (1) methyl chloroform was not carcinogenic for



male F344/N rats (2) the study was considered inadequate for



carcinogenesis evaluation in female P344/N rats, (3) the



association between the administration of methyl chloroform



and the increased incidences of hepatocellular carcinomas in



male B6C3fl mice was considered equivocal, and (4)  methyl



chloroform was carcinogenic for female B6C3F1 mice, causing



an increased incidence of hepatocellular carcinomas.





          Price, e_t al. (1978) demonstrated the _in vitro



transforming potential of methyl chloroform (99.9 percent



pure) using the Fischer rat embryo cell system (F1706).  Rat



embryo cell cultures were treated with methyl chloroform,



diluted in growth medium, for 48 hours.  After nine subcultures,



the transformed cells  (characterized by morphology and



formation of macroscopic foci in semi-soft agar) were inoculated



into newborn Fischer rats.  After 68 days, the transformed



cells had grown as undifferentiated fibrosarcomas at the



inoculation sites in all tested animals.  Acetone,  the negative



control, did not induce tumors after 82 days of inoculation



(Price, et al. 1978).






Summary



In the repeat NCI bioassay in rats and mice, there was an increase



in hepatocellular carcinomas occurrence in low and high dose males



and high dose females.  NCI concluded that (1) methyl chloroform






                              65

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                             V-20
was not carcinogenic for male rats, (2) the study was considered
inadequate for carcinogenesis evaluation in female rats, (3)
the association between the administration of methyl chloroform
and the increased incidences of hepatocellular carcinomas
in male mice was considered equivocal, and (4) methyl chloroform
was carcinogenic for female mice, causing an increased incidence
of hepatocellular carcinomas.
                           \
6.  Teratogenicity

          Schwetz, e_t a_l. (1975) assayed for reproductive and
teratogenic effects in Sprague-Dawley rats (250 g) and Swiss
Webster mice (25 to 30 g) exposed to 875 ppm of methyl
chloroform by inhalation for 7 hr/day from gestation day 6 to
gestation day 15.  The compound was a commercial grade
preparation and contained 5.5% or about 50 ppm inhibitors.
Caesarian sections were performed on gestation day 21 (rats)
and 18 (mice).  Livers in treated maternal rats were heavier
than those in the controls (p < 0.05), but no significant
changes in hepatic weights were reported in mice.  No
teratogenic effects were seen in all exposed rats and mice
for the following parameters:  weight gain; percent fetal
resorptions; average litter size; fetal body measurements;
fetal gross anomalies; skeletal anomalies; microscopic
examination and maternal carboxyhemoglobin content.
                              66

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                             V-21
          Lane et al. (1982) studied the effects of methyl


chloroform in drinking water on teratogenicity and reproduction


in mice.  Male and female ICR Swiss mice received methyl


chloroform at concentrations of 0, 0.58, 1.75 or 5.83 mg/ml.


These concentrations were designed to yield daily methyl


chloroform doses of 0, 100, 300 or 1,000 mg/kg.  The


investigators stated that:  (1) there appeared to be no dose-


dependent effects on fertility, gestation, viability, or

                           v
lactation indices, (2) pup survival and weight gain were not


adversely affected, and (3) methyl chloroform failed to


produce significant dominant lethal mutations or terata in


either of the two generations tested.



Summary



          Rats and mice have been studied for the teratogenic


potential of methyl chloroform.  No effects were evident in


exposed animals for the following parameters:  weight gain,


percentage fetal reabsorption, average litter size, fetal


body measurements, gross skeletal anomalies, and maternal


carboxyhemoglobin content.  There are some indications that


mating and fertility indices of exposed animals were lower,


and some abnormalities appeared, but were not statistically


significant.  Thus, methyl chloroform-induced teratogenicity


has not been established.
                              67

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                VI.  HEALTH EFFECTS IN HUMANS







          1.  Acute Toxicity





          The primary toxic effects of short-term, high-level



exposure to methyl chloroform in humans are characterized by



depression of the CNS.  In the majority of reports of human



fatalities resulting from methyl chloroform inhalation,



death is attributed to a functional depression of the CNS.



Levels of methyl chloroform in the victims' blood varied



considerably, ranging from 60 (Hatfield and Maykoski, 1970;



Stahl e_t al., 1969) to 720 ppm (Hall and Hine, 1966).  The



highest concentrations of methyl chloroform were found in the



brains of victims (Caplan e_t al., 1976; Stahl e_t al., 1969).



Due to problems that are inherent in analyses of volatile



toxicants in autopsy samples, it is difficult to establish



lethal methyl chloroform concentrations in blood or tissues.





          Inhalation of high concentrations of methyl chloroform



can cause irritation of the respiratory tract and minimal



organ damage, as well as depression of the CNS.  Acute



pulmonary congestion, an edema typically found in fatalities



result from  inhalation of methyl chloroform (Bonventre e_t



al., 1977; Caplan et al_., 1976).  There are also scattered



reports of modest fatty vacuolation in the liver  (Caplan, e_t



al. 1976; Hall and Hine, 1966; Stahl, et al.1969).   In most
                              68

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                            VI-2





such instances, there probably would have been insufficient



time between exposure and death for hepatotoxicity to be



fully expressed.  Stewart (1971)-reported the case histories



of four individuals who were monitored clinically after being



overcome by methyl chloroform vapors.  In each case, recovery



from depression of the central nervous system was quite rapid



and largely uneventful.  However, one of the four patients



exhibited elevated urinary urobilinogen but no alteration of



other indices of hepatotoxfcity.  These studies indicate that



methyl chloroform possesses a limited capacity to exert



hepatic injury in cases of acute, high-level inhalation exposure





          Clinical experience and scientific investigations



suggest that acute high-level inhalation of methyl chloroform



can adversely affect the cardiovascular system of humans.



Dornette and Jones (1960) used concentrations of 10,000-26,000



ppm methyl chloroform to anesthetize surgery patients.  They



noted that both induction of and recovery from anesthesia



were quite rapid.  No evidence of respiratory depression or



hepatotoxicity was seen.  However, there were disturbing



cardiovascular effects including diminished systolic pressure,



premature ventricular contractions, and, in one patient, even



cardiac arrest.  Positive urinary urobilinogen was found



ranging from 7 hours to 20 hours after exposure.
                              69

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                            VI-3





          Bass (1970) reported a syndrome called "sudden sniffing



death" in persons dying abruptly while inhaling volatile



solvents for self-intoxication.  Methyl chloroform was one of



the most suspect solvents in such incidents.  The fatalities



were attributed to cardiac arrhythmias that resulted from a



combined action of the solvent and endogenous biogenic amines.





          A single account of methyl chloroform ingestion by



a human has appeared in the literature (Stewart and Andrews,



1966).  A 47-year-old male Mistakenly drank 1 oz. of methyl



chloroform (approximately 0.6 g/kg).  He became nauseated



within 30 minutes and developed progressively severe vomiting



and diarrhea over the next few hours.  Urinalysis and clinical



chemistry tests revealed evidence of only minimal hepatorenal



injury early in the course of hospitalization.  After treating



the vomiting and diarrhea symptoms, the patient was asymptomatic



during a 2-week observation period.





          Since depression of the CNS is the predominant



effect of methyl chloroform on humans, certain manifestations



of the depression should be the most sensitive index of the



pathophysiological action of small quantities of the solvent.



Early studies with volunteers indicate that inhalation of 500



ppm of methyl chloroform for several hours has no significant



effect other than transient, mild eye irritation (Stewart, e_t al.



1961 Torkelson, e_t a_l. 1958).  Stewart and his co-workers





                              70

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                             VI-4



(1969) concluded in a later study that 500 ppm of the chemical


may be excessive for persons who are particularly susceptible


to the chemical's depressant effects on the CNS.  In a recent


investigation, inhalation of 350 ppm of methyl chloroform for


4 hours was not effective, whereas 450 ppm elicited subjective


complaints of transient eye irritation and dizziness (Salvini,


e_t a_l. 1971).  Although a number of psychophysiological tests


did not reveal a statistically significant degree of functional

                             \
inhibition, lower scores resulted when tests were conducted


during methyl chloroform exposure than when under control


conditions.  Results of an investigation by Gamberale and


Hultengren (1973) indicated that inhalation of 350 ppm of


methyl chloroform can significantly inhibit psychophysiological


functions in humans.  Five performance tests were used, 2


were tests of perceptual speed and the others were tests of


simple reaction time, choice reaction time, and manual


desterity.  Blood levels in the "inhibited" subjects averaged


approximately 3-4 ppm, although the investigators noted wide


intersubject differences in blood and alveolar air concentrations,


Gamberale and Hultengren concluded that it would be difficult,


with any degree of accuracy, to set a threshold for the vapor


concentration of methyl chloroform that would not alter function


of the central nervous system.  Their tests of psychophysio-


logical function are certainly more sensitive and objective


than the indices used in the earlier studies of Torkelson, e_t al.



                              71

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                            VI-5
(1958) and Stewart, et al. (1961, 1969).  Nevertheless, the


current U.S. threshold limit value for occupational exposure


to methyl chloroform remains at 350 ppm.  This standard is


designed to protect the majority of workers from raucous


membrane irritation and performance inhibition.



          2.  Subacute Toxicity



          Short-term exposure to methyl chloroform appears to
                           \

be no more harmful to humans or laboratory animals than does


acute exposure.  Stewart, et al. (1969) exposed humans via


inhalation to 500 ppm methyl chloroform for 6.5 hours daily


for five consecutive days.  They observed some objective and


subjective signs of depression of the central nervous system,


but no evidence of toxicity upon examination for neurological,


respiratory, and hepatorenal function.  There were also a


small accumulation of methyl chloroform and an increase in


urinary trichloroethanol levels.



          3.  Epidemiology



          Seki and his colleagues (1975) surveyed four Japanese


printing factories where methyl chloroform, the sole organic


solvent in the entire process, was used to remove excess ink.


Duration of workday/workweek and operational procedures were


essentially uniform.  Enclosure of vapor sources and installation


of exhaust systems were, in the authors' opinion, mainly responsible



                              72

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                            VI-6



for variation in vapor concentration.  The subjects were


23-53 year-old men and had been exposed to methyl chloroform


vapor for at least 5 years.  Laboratory tests, including


peripheral hemograms, blood specific gravity and urinalysis


for urobilinogen and protein, were not described.  A Japanese


version of the Cornell Medical Index health questionnaire


was answered by all subjects.  A test of vibrational sense


was performed as well as urinalysis for trichloracetic acid


and methyl chloroform.  Decrease in urinary metabolite levels
                            \

provided the basis for calculation of biologic half-life.


The vapor concentration of methyl chloroform in the workroom


air was determined by gas-liquid chromotography.  A preliminary


study revealed a fairly constant vapor concentration regardless


of time and location of sampling.  The respective data are


presented in Tables VI-1, VI-2, and VI-3.



          The authors found, through regression analysis, a


linear relationship between the vapor concentration of methyl


chloroform and level of urinary metabolites (trichloroacetic


acid and methyl chloroform), and for this reason they concluded


that the urinary metabolite level was a good index of methyl


chloroform exposure.  The biological half-life of methyl


chloroform was found to be 8.7 + 1.8 hours.



          In a detailed study of one worker, a steady increase


in urinary metabolite concentrations toward the weekend as



                              73

-------
                            VI-7


well as significant metabolite excretion on Sunday, suggested

that methyl chloroform accumulated in the body.  Total

metabolite increase was primarily attributed to methyl chloroform,


          No dose-dependent difference in health, as reflected

by the medical questionnaire, was found in any of the workers.

The authors recommended, based on accumulation of methyl

chloroform in the body, a subtraction from the maximum "no

adverse effect" level for short-term exposures to establish a

threshold limit value (TLV)1, for repeated exposures  (Seki, e_t

al. 1975).  The odor threshold has been reported to be as

high as 700 ppm or as low as 16 ppm.


                          TABLE VI-1


             Urinary Metabolite Concentration in
             Workers Exposed to Methyl Chloroform
Exposure Concentration    Metabolite Concentration  No. Examined
           (ppm)                    (mg/1)*
Trichloroacetic acid Trichloroethanol
4

25

53


(0.

(1.

(2.
0.6
5-1.1)
2.4
3-4.6)
3.6
4-5.5)

(0

(3

(6
1.2
.5-2.6)
5.5
.6-8.6)
9.9
.8-14.5)
10

26

10


* Geometric mean with SD in parenthesis

Adapted from:  Seki et al. (1975)
                              74

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                            VI-8
                          TABLE VI-2
              Results of Physical Examinations
           of Workers Exposed to Methyl Chloroform

Exposure
Concentration
(ppm)
4
25
28
53
No.
Examined

,66
33
55
42
No. of Healthy
Subjects*

60
30
48
36

Percentage

91
91
87
86

* Adapted from Seki et al. (1975).
                              75

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                            VI-9
                          TABLE VI-3

               Exclusions from Healthy Category
                     By Class of Disorder

Class of Disorder
Cardiovascular
Hepatic
Gastrointestinal
Renal
Bone
CNS
No. Percent Affected
10 5
3 1
4 2
2 1
1 <1
1 <1

Adapted from Seki et al. (1975)
                              76

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          Hervin (1975) determined that the total daily

exposure to methyl chloroform was not at a personally hazardous

level after an evaluation of 35 employees in a textile dye plant,

Breath and area air were sampled and the highest level found

was 220 mg/3 (40.5 ppm) in a 1.3-liter breath sample.


          Giles and Rostand (1975) measured air levels,

interviewed 15 employees, and studied the plant insurance

records in another evaluation of an industrial site.  The

breathing zone and area samples obtained were 7-18 ppm and 14
                            \
ppm, respectively.  No hazard was seen with this exposure.

NIOSH has investigated additional workplace sites to evaluate

worker exposure to methyl chloroform and adverse action.

Methyl chloroform levels were below those allowed in the

workplace (Giles and Philbim, 1978; Markel, 1978; Gilles, 1977).


          Maroni e_t al. (1977) studied 29 women working at a

factory manufacturing platinic and steel spinerets.  Twenty-

two of the women were exposed to methyl chloroform in a work-

place where it was the only solvent used.  Seven were employed

in the same factory with no known exposure to methyl chloroform.

Air concentrations in the exposed areas ranged from 110 to 990

ppm with only one worker in the area with the higher

concentrations (720-990 ppm).  Women were subdivided into

three groups according to extent of exposure:  I (7 workers)
                              77

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                            VI-11








110 ppm, II (7 workers) 140-160 ppm, and III (8 workers)



990 ppm.  The mean length of employment was 6 years.






          No significant differences were observed between



the exposed and unexposed females with respect to clinical



features, maximal motor conduction velocity, conduction



velocity of slow fibers and psychometric data.  However,



since the study group was so small and had a wide range in



age, and the methods of data collection may not have been



adequately standardized, the negative results of this study



may not be conclusive and do not provide information on the



population risks associated with exposure to methyl chloroform.





          Kramer, et. al. (1978) conducted a study of textile



workers at., a plant using methyl chloroform and compared them



with a group of workers at an adjacent plant not using methyl



chloroform matched by age (5 years), race, sex, job description,



shift, and socio-economic status.  Most exposures were from 1



to 5 years at time weighted average levels of 100-250 ppm,



determined from work histories and industrials hygiene surveys.



The methyl chloroform contained 4% stabilizers; small quantities



of fluorocarbon 113 were used in 1973.  Primary emphasis was



on cardiovascular effects via nurse administered questionnaires,



blood parameters including enzyme assays, blood pressures, and
                              78

-------
                            VI-12
electrocardiograms.  No evidence of adverse effects on the



cardiovascular system, CNS, or liver was found in this study.



Collection of data does not appea'r to have been standardized



to avoid bias.





          The limitations of this study in terms of design,



duration of exposure, and non-specificity of endpoint variables



make the results difficult to apply to determinations of risk



of exposure to methyl chloroform.





Summary





          Transient eye irritation and upper respiratory



irritation from exposure to methyl chloroform vapors have



been reported at concentrations in excess of 500 ppm.



Regression analysis has indicated a linear relationship between



vapor concentration of methyl chloroform and the levels of



urinary metabolites (trichloroacetic acid and methyl chloroform).



The odor threshold of methyl chloroform covered a wide range



(16-700 ppm) indicating that individual sensitivity may play



a part in determining irritation and other health effects.
                              79

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                            VII-1

                  VII HUMAN RISK ASSESSMENT


          1.  Current Levels of Exposure

          Exstimates of human exposure to chloroethanes via

ingestion are not available.  NIOSH (1978) estimated that of

over five million workers exposed to chloroethanes by

inhalation and dermally, 4.5 million are exposed to 1,2-

dichloroethane or methyl chloroform (Table VII-1).
                            \
          Workers, who are occupationally exposed to

chloroethanes, by inhalation and/or dermally represent a

special group at risk.  Epidemiological studies have not

disclosed a relationship between exposure to chloroethanes

and cancer; however, four chloroethanes have proved to be

carcinogenic in at least one species of rodent (NCI 1978).

Those individuals who are exposed to known hepatotoxins or

have liver disease may constitute a group at risk.

          2.  Existing Guidelines and Standards

          OSHA standards and NIOSH recommended standards are

based on exposure by inhalation (Table VII-2).  Based on

information available in 1976, NIOSH recommended that

occupational exposures to 1,2-dichloroethane do not exceed 5
                              80

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                            VII-2
                         TABLE VII-1
            CHLOROETHANE EXPOSURES AND PRODUCTION
     Chemical
Estimated number
       of
workers exposed
 Annual
Production
quantities
 (pounds)
monochloroe thane
1,1-dichloroe thane
1 , 2-dichloroethane
methyl chloroform
1,1, 2-trichloroe thane
1,1,1, 2-tetrachloroethane
1,1,2, 2-tetrachlorbe thane
pen tachloroe thane
hexachloroe thane
113,000
^ 4,600
1,900,000
2,900,000
112,000
a
11,000
a
1,500
670 million
b
8 billion
630 million
c
b
c
b
b,d
(1976)

(1976)
(1976)






aNIOSH estimates not available.

bDoes not appear to be commercially produced in the United States,

cDirect production information not available.

d730,000 kg were imported in 1976.


Adapted from:  NIOSH (1978)
                              81

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                            VII-3



                         Table VII-2

               CHLOROETHANE EXPOSURE STANDARDS
                                               OSHA
                                             Exposure
                                             Standard
                Chemical                       (ppm)
            monochloroethane                   1,000

            1,1-dichloroethane                   100

            1,2-dichloroethane                    50
                             \
            methyl chloroform                    350

            1,1,2-trichloroethane                 10

            1,1,1,2-tetrachloroethane            none

            1,1,2,2-tetrachloroethane              5

            pentachloroethane                    none

            hexachloroethane                       1



*NIOSH has tentative plans for a Criteria Document for a
 Recommended Standard for this substance.

Adapted from:  NIOSH (1978).


ppm (20 mg/m3) determined as a time-weighted average for up to

a 10-hour work day, 40-hour work week.  Peak concentrations

should not exceed 15 ppm (60 mg/m3) as determined by a 15-minute

sample.
                              82

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                            VIII-1

VIII.  Quantification of Toxicological Effects


     The quantification of toxicological effects of a chemical

consists of an assessment of the non-carcinogenic and carcino-

genic effects.  In the quantification of non-carcinogenic

effects, an Adjusted Acceptable Daily Intake  (AADI) for the

chemical is determined.  For ingestion data,  this approach

is illustrated as follows:

     Adjusted ADI =    (NOAEL or MEL in mg/kg)(70 kg)
                     (Uncertainty  factor)(2 liters/day)

The 70 kg adult consuming 2 liters of water per day is used

as the basis  for the calculations.  A "no-observed-adverse-effect-

level" or a "minimal-effect-level" is determined from animal

toxicity data or human effects data.  This level is divided

by an uncertainty factor because,  for these numbers which are

derived from  animal studies, there is no universally acceptable

quantitative method to extrapolate from animals to humans,

and the possibility must be considered that humans are more

sensitive to  the toxic effects of  chemicals than are animals.

For human toxicity data, an uncertainty factor  is used to

account for the heterogeneity of the human population in

which persons exhibit differing sensitivity to  toxins.  The

guidelines set forth by the National Academy  of Sciences

(Drinking Water and Health, Vol. 1, 1977) are used in estab-

lishing uncertainty factors.  These guidelines  are as follows:

an uncertainty factor of 10 is used if there  exist valid

experimental  results on ingestion  by humans,  an uncertainty

-------
;                             VIII-2

 factor  of  100 is used if there exist valid results on long-

 term feeding  studies on experimental animals,  and an uncertainty

 factor  of  1000 is used if only limited data are available.

      In the quantification of carcinogenic effects,  mathematical

 models  are used to calculate the estimated excess cancer

 -risks associated with the consumption of a chemical  through

 the  drinking  water.  EPA's Carcinogen Assessment Group has

 used the multistage model, which is linear at  low doses and

 does not exhibit a threshold, to extrapolate from high dose
                               \
 animal  studies to low doses of the chemical expected in the

 environment.   This model estimates the upper bound (95%

 confidence limit) of the incremental excess cancer rate that

 would be projected at a specific exposure level for a 70 kg

 adult,  consuming 2 liters of water per day, over a 70 year

 lifespan.  Excess cancer risk rates also can be estimated

 using other models such as the one-hit model,  the Weibull

 model,  the logit model and the probit model.  Current

 understanding of the biological mechanisms involved  in cancer

 do not  allow  for choosing among the models.  The estimates

 of incremental risks associated with exposure  to low doses

 of potential  carcinogens can differ by several orders of

 magnitude  when these models are applied. The linear, non-

 threshold  multi-stage model often gives one of the highest

 risk estimates per dose and thus would usually be the one

 most consistent with a regulatory philosophy which would

 avoid underestimating potential risk.

-------
                            VIII-3



     The scientific data base, which is used to support the



estimating of risk rate levels as well as other scientific



endeavors, has an inherent uncertainty.  In addition, in



many areas, there exists only limited knowledge concerning



the health effects of contaminants at levels found in drinking



water. Thus, the dose-response data gathered at high levels of



exposure are used for extrapolation to estimate responses at



levels of exposure nearer to the range in which a standard



might be set. In most cases, data exist only for animals; thus,



uncertainty exists when the data are extrapolated to humans.



When estimating risk rate levels, several other areas of



uncertainty exist such as the effect of age, sex, species



and target organ of the test animals used in the experiment,



as well as the exposure mode and dosing rates.  Additional



uncertainty exists when there is exposure to more than one



contaminant due to the lack of information about possible



additive, synergistic or antagonistic interactions.



A. Non-carcinogenic Effects



     The toxic effects of 1,1,1-trichloroethane (methyl



chloroform) in animals and humans following acute and chronic



exposure at high doses are (1) fatty vacuolation and increase



in liver weight; (2) manifestations of depression of the



central nervous system; (3) transient eye irritation and



dizziness? and (4) cardiovascular changes including increase



in systolic pressure and premature ventricular contractions.



     Effects of acute exposure to methyl chloroform in rats



were reported by Adams et al. (1950).  The investigators

-------
                            VIII-4

stated that the 3-hour LCso in rats was 18,000 ppm.  The
lowest and shortest exposure that elicited histological
change in tissues of rats was 8,000 ppm for 7 hours.  This
produced an increase in liver weight and fatty vacuolation
of hepatocytes.
     McNutt et al. (1975) exposed mice continuously (inhalation)
to 250 and 1,000 ppm methyl chloroform for 14 weeks.  Control
mice were exposed to room airy  Serial sacrifice of exposed
and control mice from 1 to 14 weeks demonstrated significant
changes in the centrilobular hepatocytes of animals in the
1000 ppm group.  There was also an evidence of liver
triglyceride accumulation in the 1000 ppm.  Findings
are summarized in Table VIII-1.
     Electron microscopic evaluation of mice liver in the
above study (McNutt et al., 1975) revealed that cytoplasmic
alterations were most severe in centrilobular hepatocytes in
the 1000 ppm group and were mild to minimal in the 250 ppm
group.  These alterations consisted of vesiculation of the
rough endoplasmic reticulum, with loss of attached polyri-
bosomes, increased smooth endoplasmic reticulum, microbodies,
and' triglyceride droplets.  There was also present necrosis
of individual hepatocyes which was associated with an acute
inflammatory infiltrate and hypertrophy of Kupfler cells.
The investigators stated that the comparison of these findings
to the results obtained by other investigators studying

-------
                            VIII-5

dichloromethane indicates that the pathologic changes observed
                         TABLE VIII-1

    SUMMARY OF EFFECTS IN MICE AFTER CONTINUOUS INHALATION
                EXPOSURE TO METHYL CHLOROFORM3
Parameter
Food/water intake
Liver wt/100 gm. b.w.
250 ppm

Not significantly
different from
control

Not significantly
different from
control except at
8 and 9 week intervals
Light microscopic observation;
Lipid contents
Significantly different
at 13-week interval
Electron microscopic observations;
1,000 ppm

Not significantly
different from
control

Significantly
different from
control
Significantly
different at
2-14 week intervals
Cytoplasmic
alterations^5
Mild to minimum in        Severe in
centrilobular             centrilobular
hepatocytes               hepatocytes
                   necrotic hepatocytes
                   (associated with focal
                   infiltrates of neutro-
                   philic leukocytes in
                   the hepatic lobules)
a.
   Adapted from McNutt et al.  (1975) Lab. Invest. 32:642-654.

   Alteration consisted of;  (i) vesiculation of the rough
   endoplasmic reticulum, (ii) loss of attached polyribosomes
   and (iii) increased smooth  endoplasmic reticulum microbodies
   and triglyceride droplets.

-------
;                             VII1-6

with methyl  chloroform were similar to those observed with

dichloromethane.

     Exposure  to  500 ppm (7 hours/day, 5 days/ week  for  6

months)  produced  no effect on rats (#20),  guinea  pigs (#8),

rabbits  (12) and  monkeys (*2), when compared with controls

in terms of  growth, organ weights, hematologic values, gross

pathology and  histopathology (Torkelson et al., 1958).   The

 investigators  reported that female guinea pigs which were

 found  to be  the most sensitive in previous experiments were
                               \
 able to  tolerate  1,000 ppm for 0.6 hours/day with no detectable

 adverse  effects.   Male rats tolerated exposure of 0.5 hours/day

 to 10,000 ppm  with no organic injury.

     Epidemiological evidence cannot be related to the

 exposure levels of methyl chloroform with confidence; how-

 ever,  exposures of workers to methyl chloroform and  its

 association  with  observed health effects - fatigue,  dizzi-

 ness,  nervous  system disorders, etc. is worth mentioning.

     Two lifetime feeding or gavage studies have  been

 conducted as a part of the National Cancer Institute

 (NCI)  Bioassay Program (1977; 1983).  In the first study,

male and female rats were given 750 or 1,500 mg/kg methyl

 chloroform  in  corn oil by gavage 5 times weekly for 78

weeks.   Similarly, male and female mice received approximately

 2,800  and 5,600 mg/kg for 78 weeks.  Diminished body weight

gain and decreased survival time were manifest in both rats

and mice. The incidence .of histopathological change was

no greater  for methyl chloroform than for control animals

-------
                            VIII-7

of either species.   No  other  indices  of  toxicity  were
evaluated.
     In the second NCI  bioassay  study (1983),  Fischer  344/N
rats and B6C3F1 mice were  gavaged with daily doses of  375
or 750 mg/kg body weight  (rats)  and 1,500 or 3,000 mg/kg
body weight (mice) of methyl  chloroform  in  corn oil, respectively,
The compound was administered fives times per  week for  103
weeks.  The report stated  that:  (1) methyl  chloroform was
not considered tumorgenic  for male rats  and this  study
.was inadequate for tumorigenic evaluation in female rats
because of the large number of accidental deaths  and because
of the high dose being  toxic;  (2) the association between
the administration of methyl  chloroform  and the increased
incidences of tumors in male  B6C3F1 mice was considered
equivocal, whereas there was  a significant  increase in  tumor
incidence in female  B6C3F1 mice.
     Lane et al.  (1982) have  reported results  of  methyl
chloroform in drinking  water  on  reproduction and  development
in mice.  A multi-generation  reproduction study was carried
out in mice in addition to screening  for dominant lethal and
teratogenic effect of methyl  chloroform. Male and female
Swiss mice received  methyl chloroform at concentrations of 0,
0.58, 1.75 or 5.83 mg/ml to yield daily  doses  of  0, 100, 300,
or 1,000 mg/kg.  There  appeared  to be no dose-dependent
effects on fertility, gestation, viability, or location
indices.  Pup survival  and weight gain were not adversely

-------
                            VIII-8


affected.  Methyl chloroform also failed  to produce significant


dominant lethal mutations or terata  in either of the two


generations tested.  The results of  these studies could not


be used in the development  of  a QTEL because animals were


maintained only for  35 days on test  solution containing


-specified concentrations of methyl chloroform and also the


study did not identify a dose-response level at which an


effect occurred.


     Synergistic/additive effects and other related effects
                               \

such as resulting from multiple chemical  exposure with


respect to methyl chloroform have not been studied in either


in vitro or in vivo  systems.



B. Quantification of Non-carcinogenic Effects


     The liver of the mammalian system appears to be the


sensitive endpoints  with respect to  the adverse health effects.


There are limited data concerning the dosage, duration of


exposure and the effects on the central nervous system.


     Liver toxicity  should  be  considered  as an endpoint


for estimating Adjusted Acceptable Daily  Intake  (ADI) for


methyl chloroform.   The compound has been shown to cause


hepatocytic vacuolation and increase in liver weight and


triglyceride content in animals.  In the  absence of definitive


information on the chronic  toxicity  of ingested methyl


chloroform, HAS  (1980) had  calculated the chronic Suggested


No Adverse Response  Level  (SNARL), 3.8 mg/1, based on the

-------
                            VIII-9

lowest dose used in the NCI bioassay (1977) in animals.

Similarly,  U.S. EPA (AWQD, 1980) and (ODW) have also considered

the lowest  dose of 750 mg/kg of methyl chloroform administered

orally in calculating ADI and Health Advisories, respectively.

These levels are shown in Table VIII-2.  However, in view of

recent findings of NCI bioassay in rats and mice and lack of

chronic ingestion studies of methyl chloroform in animals for

quantifying non-carcinogenic effect, it may be prudent to

consider inhalation study in animals (McNutt et al., 1975),

in addition to data of repeat NCI bioassay (1983) even

though the  inhalation studies in animals may not meet all

criteria necessary for quantifying non-carcinogenic effects.


                         TABLE VIII-2

            HEALTH ADVISORY FOR METHYL CHLOROFORM
Non-CA
CA
NAS-SNARL
3.8 mg/la
EPA-HA
1 .07 mg/lb
AWQD- AD I
18.7 mg/lc
WHO
-
NOTE:

- Not available.

a Based on NCI bioassay study in rats - 750 mg/kg (NCI, 1977)
  and ^ is calculated for an adult weighing 70 kg consuming
  2 liters of water and contribution from water being 20%
  (NAS, 1980) .

b Based on NCI bioassay study in rats - 750 mg/kg (NCI, 1977)
  and is calculated for a 10 kg child consuming 1 liter of
  water and contribution from water being 20% (U.S. EPA Health
  Advisory, 1980) .

c Based on NCI bioassay study in rats - 750 mg/kg (NCI, 1977)
  and is calculated for an' adult weighing 70 kg consuming 2
  liters of water and assuming 100% of exposure from water
  (U.S. EPA - AWQD, 1981) .

-------
                           VIII-10


     McNutt et al.  (1975) exposed male mice continuously

(inhalation) to 250 (1,365 mg/m3) or 1,000 ppm  (5,460 mg/m3)

methyl chloroform for 14 weeks.  Control mice were exposed

to room air.  Serial sacrifice of exposed and control mice

from 1 to 14 weeks demonstrated significant changes in the

centrilobular hepatocytes of animals in the 1,000 ppm (5,460

mg/m3) group and mild to minimal in the 250 ppm  (1,365

mg/m3) group.  These changes consisted of vesiculation of
                             \
the rough endoplasmic reticulum, with loss of attached

polyribosomes, increased smooth endoplasmic reticulum, micro-

bodies, and triglyceride droplets.  No no-observed-adverse-

effect-level (NOAEL) can be identified but a MEL  (Minimum

Effect Level) of 250 ppm (1,365 mg/m3) can be used.  An ADI

based upon these data could be derived as follows:
                                20.1o     1.33?
  (1365 mg/m3)(l m3/hr)(6 hrs)(I3.3%) = Q^&4 mg/1 (or
          (1000) (2 1/d)               &,cig ^TOW mg/kg/day
                                          for a  70 kg adult)

Where: 1,365 mg/m3  (250 ppm) = MEL

       1 m3/hr = Ventilation volume for a 70 kg  adult

       6 hrs = Exposure assumed to be saturable  and therefore
               equivalent to exposure for 24-hour period

       l«li*a% = Assumed percent body burden metabolized
               (Schumann et al., 1982)

       1000 = Uncertainty factor appropriate to. MEL in animals
              with no equivalent data in the human

       70 kg - Average body weight of an adult

       2 I/day = Water consumption per day for  an adult
                                                   hiv{
                                                            Us lie

-------
                              11

Strength; Serial sacrifice of exposed mice from 1 to 14 weeks

demonstrated significant changes in the centrilobular

hepatocytes of animals.


Weakness; (1) Route of exposure is inhalation and the period

of continuous exposure was for 98 days.  (2) Percent body

burden of methyl chloroform following 24-hr continuous exposure

is not available.  (Calculations are based on 6-hr inhalation

exposure results.)


NCI repeat ingestion study in rats

     Methyl chloroform was administered in corn oil by gavage

to groups of 50 male and 50 female rats (F344/N) at doses of

375 and 750 rag/kg body weight.  Methyl chloroform was given

5 times per week for 103 weeks.

     No biologically significant tumor pathology was observed

in these rats.  The increase in intestinal cell testicular

tumors was not considered to be related to the administration

of methyl chloroform in the high dose group.  However, the

survival of high dose female rats in the present study was

significantly less (P < 0.001) than that of the vehicle

control.  A large number of accidental deaths due to gavage

errors occurred among dosed female and male rats (25 low

dose and 17 high dose females and 14 low dose and 8 high

dose males).   An ADI based upon low dose,  375 mg/kg, may be

derived as follows;

   (375 mg/kg)(5 days)(70 kg)  = 9.38 mg/1 =9.4 rag/1
    (7 days)(2 I/day)(1,000)

-------
                              12

   re: 375 mg/kg = observed  adverse  effect dose
      5/7 = fraction converting  from 5  to 7  day exposure
      70 kg = average weight  of  an  adult
      1000 = uncertainty  factor
      2 I/day = adult consumption of water per day

   •ength; The exposure is  via  ingestion  and for a lifetime

   13 weeks) .


   ikness; This study suffers from one important criteria and

   at is poor survival of animals  at  the  end of 103 weeks of

   posure.  A large number  of deaths  in animals occurred over

   e 103 weeks of exposure  either  due to  gavage error or to

   e toxicity of methyl chloroform administration in high

   se groups of animals.  The survival rate for animals  at

  ie end of the 103 week exposure  is  shown below:

                    Survival  of  Animals

                 Control          Low Dose       High  Dose
     Animal          0             375 mg/kg       750 mg/kg

     Female       29/50               10/50           5/50
     Male         -36/50               20/50          26/50

     Since no methyl chloroform effects  were  observed in the

 epeat NCI bioassay in rats, the  ingestion dose level of 375

 g/kg would have been appropriate for the derivation of an

 iDI.  However, the repeat  study  in rats  suffers from the

 ligh  death rate either from gavage error or toxic effects of

 nethyl chloroform (in high doses) in animals.  The percent

 teaths in the female rats  at end  of  the  103 week period were

42%, 80%, and 90% in the control, low dose (375 mg/kg), and

high dose (750 mg/kg), respectively.  Therefore use of  this

study in the derivation of an  ADI is highly questionable for

-------
                           VIII-14



species, sex, type of neoplasm, or site of occurrence.  It



was concluded that the carcinogenicity could not be determined



from this study (NCI, 1977).



     A repeat carcinogenesis bioassay of methyl chloroform was



conducted by administering the test chemical in corn oil by



gavage to groups of 50 male and 50 female F344/N rats at doses



of 375 and 750 mg/kg body weight.  Groups of 50 male and 50



female B6C3F1 mice received 1,500 or 3,000 mg/kg body weight.



Methyl chloroform was administered five times per week for 103



weeks.  Groups of rats and mice of each sex received corn oil



by gavage on the same schedule and served as vehicle controls.



Rats; Mean body weights for control and dosed rats were



comparable throughout the two year study.  There were no tumors



in rats considered to be related to administration of methyl



chloroform.  However, the large number of accidental deaths



among dosed females (25 low dose, 17 high dose) and dosed



males (14 low dose, 8 high dose) reduced the sensitivity of



this study for detecting late-appearing tumors in these groups.



Mice; Survival of high dose male mice (28/50) was significantly



(P < 0.01) less than that of the vehicle controls (44/50).  There



was a significant (P < 0.05)- dose response trend and increased



incidences of hepatocellular carcinomas in low and high dose



male and in high dose female mice.



     Dow Chemical Co. (Quast et al. 1978) studied groups of



Sprague-Dawley rats exposed by inhalation (6 hours/day, 5



days/ week, over one-half'of a lifetime).  Rats were treated



for 12 months and observed until death or until they reached

-------
                           VIII-15



the age of 31 months.  The dose of 875 and 1,750 ppm were 2.5



and 5 times the threshold limit value of 350 ppm, respectively.



There are two shortcomings of this study: 1) the animals were



treated for only 12 months rather than a lifetime but observed



for another 12 months, and (2) it is not evident that the



maximum tolerated dose was used during the treatment period.



The only sign of toxicity was an increased incidence of



focal hepatocellular alterations in female rats at the highest



dosage.



     Methyl chloroform has been tested for its ability to



cause point mutations in bacteria, point mutations and gene



conversion in yeast, and for cytogenetic abnormalities in



rats.  The results of these studies are summarized in Table



VIII-3.



     Henschler et al. (1977) and Taylor et al. (1977) reported



that methyl chloroform was not mutagenic in the bacterial system,



Salmonella/S9.  The experimental details given in their reports



were inadequate to verify the conclusions of the investigators.



However, other investigators (Simmon et al., 1977 and Snow



et al., 1979) independently reported that methyl chloroform



was mutagenic in various Salmonella typhimurium strains



(both with and without metabolic activation).



     Methyl chloroform also was tested for mutagenic potential



employing yeast as an indicator organism (Litton Bionetics,



1975 and Loprieno et al., 1979).  The results of these tests



indicated that methyl chloroform was not mutagenic in the



test system Saccharomyces cerevisiae or Schizosaccharomyes



bombe.

-------
                                              VIII-16

                                            TABLE VII1-3

                         Mutagenicity Testing of Methyl Chloroform
Test
System

A. Bacteria
Activation
  System
   Salmonella/59      PCB induced liver,
   (spot test and     lung and testes S9
   plate incorporation)
   Salmonella/S9
   Salmonella/59
   Salmonella/59
   (plate incor-
   poration)

   Salmonella/59
PCB induced rat liver
microsomes S9 mix

PCB induced rat liver
microsome S9 mix

Aroclor-activated rat
liver microsome S9 mix
Methyl chloroform
induced Syrian hamster
liver microsome S9 mix
Result
                         99% formulation + ive,
                         Other formulations - ive
- ive
+ ive for TA 100
- ive
  ive
Reference
                              Litton, 1975
Henschler
 et al. (1977)

Simmon et al.
 (1977)

Taylor et al.
 (1977)
Snow et al.
 (1979)
B. Yeast
   Saccharomyces
   cerevisiae
   (gene conversion)

   Schizosaccharo-
     myces
   (forward mutation)
PCB induced rat liver    - ive
S9 mix
Host mediated assay      - ive
B6C3F1 mice
                              Litton,  1975
                              Loprieno et al
                               (1979)

-------
                           VIII-17

D. Quantification of Carcinogenic Effects

     Using methodology described in detail elsewhere, (U.S.EPA,

1980) the EPA's Carcinogen Assessment Group (CAG, memo dated

April 29, 1983) and the National Academy of Sciences (WAS, 1983)

have calculated estimated incremental excess cancer risks associated

with exposure to methyl chloroform in drinking water, extra-

polating from data obtained in the NTP repeat Bioassay in mice

(NCI, 1983) with this compound.  CAG and NAS derived their

estimates based on a statistically significant increase in

hepatocellular carcinomas in mice receiving 1500 or 3000

mg/kg methyl chloroform by gavage in corn oil.  The ranges of

concentrations are summarized in Table VIII-4.


                         Table VIII-4

Drinking Water Concentrations and Estimated Excess Cancer Risks

                         Range of Concentrations (ug/1)a
Excess Lifetime
Cancer Risk                 CAGb            •NASC
ID'4
10-5
10-6
0
2200
220
22
0.00
1680
168
16.8
0.00

a Assumes the consumption of two liters of water per day by 70
  kg adult over a lifetime; number represents 95% upper bound
  confidence limit

b (McGaughy, 1983)

c (NAS, 1983)

-------
                           VIII-18

The CAG calculated that consuming 2 liters of water per day

having a methyl chloroform concentration of 2200 ug/1, 220

ug/1 or 22 ug/1 would increase the risk of one excess cancer

per 10,000 (10~4), 100,000 (10"5) or 1,000,000 (10~6) respec-

tively, per lifetime.  Similarly, the NAS also calculated

excess cancer risk values based on same NCI repeat bioassay

data using the multistage model.  They stated that consuming

2 liters of water per day over a lifetime at a methyl chloroform

concentration of 1680 ug/1, 168 ug/1 or 16.8 ug/1 would

increase the risk of one excess cancer per 10,000 (10~4),

100,000 (10~5), or 1,000,000 (10~6) people exposed, respectively.

The slight difference between CAG and NAS values is due to

the fact that CAG has taken into consideration hepatocellular

carcinomas observed in the female mice whereas the NAS have

included in the derivation of risk values the results of both

male and female mice hepatocellular carcinomas.

     In the quantification of toxicological effects for a

chemical, consideration should be given to subgroups within

the general population which are at greater than average risk

upon exposure to the chemical.  For methyl chloroform, animal

studies have not been carried' out to characterize adverse

effects in the aged or newborn.

     Methyl chloroform has also been shown to have interaction

with other chemicals.  Ingestion of ethanol was shown to

increase the hepatotoxicity of methyl chloroform.  However,
                          *
ingestion of isopropyl alcohol or acetone prior to administration

of methyl chloroform did not alter the response of enzyme activity,

-------
                           VIII-19






     The latest bioassay data on 1,1,1-trichloroethane is




currently undergoing audit by NTP and a final report has not




been issued.  Therefore, this proposal will use the non cancer




inhalation data as the basis for the proposed RMCL.  This




approach will be amended if the final NTP report determines




that 1 ,1 ,1-trichloroethane was carcinogenic under the condition




of the text.

-------
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Bell, Z.G., Jr.  1978.  PPG Industries, Inc., Pittsburgh,
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-------
                             IX-2
Brass, H.J.  1977.  The National Organics Monitoring Survey:
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-------
                             IX-3
Dornette, W. and J. Jones.  1960.  Clinical experiences with
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-------
                             IX-4
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                             IX-5
Henschler, D., E. Eder, T. Neudecker, and M. Metzler.   1977.
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                            IX-13
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