ARV Drug
Generic Name
(Abbreviation)
Trade Name
|
Formulation
|
Dosing Recommendationsa
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Recommendations for Use in Pregnancy
|
PKs in Pregnancyb
|
Concerns in Pregnancy
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NRTIs |
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NRTIs are recommended for use as part of combination regimens, usually including two NRTIs with either an NNRTI or one or more PIs. Use of single or dual NRTIs alone is not recommended for treatment of HIV infection. |
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See text for discussion of potential maternal and infant mitochondrial toxicity. |
Preferred Agents |
Lamivudine
(3TC)
Epivir |
Epivir
150-, 300-mg tablets or 10-mg/mL oral solution |
Epivir
150 mg BID or
300 mg once daily
Take without regard to meals.
|
Because of extensive experience with 3TC in pregnancy in combination with ZDV, 3TC plus ZDV is a recommended dual-NRTI backbone for pregnant women. |
PK not significantly altered in pregnancy; no change in dose indicated.24 High placental transfer to fetus. |
No evidence of human teratogenicity (can rule out 1.5-fold increase in overall birth defects).25 Well tolerated; short-term safety demonstrated for mothers and infants. If hepatitis B coinfected, possible hepatitis B flare if drug stopped postpartum; see Special Situations: Hepatitis B Virus Coinfection. |
Combivir
3TC 150 mg + ZDV 300 mg |
Combivir
1 tablet BID |
Epzicom
3TC 300 mg + ABC 600 mg |
Epzicom
1 tablet once daily |
Trizivirc
3TC 150 mg + ZDV 300 mg + ABC 300 mg |
Trizivir
1 tablet BID |
Zidovudine
(AZT, ZDV)
Retrovir |
Retrovir
100-mg capsules,
300-mg tablets,
10-mg/mL IV solution,
10-mg/mL oral solution |
Retrovir
300 mg BID or
200 mg TID
Take without regard to meals.
|
Because of extensive experience with ZDV in pregnancy in combination with 3TC, ZDV plus 3TC is a recommended dual-NRTI backbone for pregnant women. |
PK not significantly altered in pregnancy; no change in dose indicated.26 High placental transfer to fetus. |
No evidence of human teratogenicity (can rule out 1.5-fold increase in overall birth defects).25 Well tolerated; short-term safety demonstrated for mothers and infants. |
Combivir
ZDV 300 mg +
3TC 150 mg |
Combivir
1 tablet BID |
Trizivirc
ZDV 300 mg + 3TC 150 mg + ABC 300 mg |
Trizivir
1 tablet BID |
Alternative Agents |
Abacavir
(ABC)
Ziagen |
Ziagen
300-mg tablets or 20-mg/mL oral solution |
Ziagen
300 mg BID or
600 mg once daily
Take without regard to meals.
|
Alternative NRTI for dual-NRTI backbone of combination regimens. See footnote regarding use in triple-NRTI regimen.c |
PK not significantly altered in pregnancy; no change in dose indicated.27 High placental transfer to fetus |
No evidence of human teratogenicity (can rule out 2-fold increase in overall birth defects).25 Hypersensitivity reactions occur in ~5%–8% of non-pregnant individuals; a much smaller percentage are fatal and are usually associated with re-challenge. Rate in pregnancy unknown. Testing for HLA-B*5701 identifies patients at risk of reactions28,29 and should be done and documented as negative before starting ABC. Patients should be educated regarding symptoms of hypersensitivity reaction. |
Epzicom
ABC 600 mg +
3TC 300 mg |
Epzicom
1 tablet once daily |
Trizivirc
ABC 300 mg + ZDV 300 mg + 3TC 150 mg |
Trizivir
1 tablet BID |
Emtricitabine
(FTC)
Emtriva |
Emtriva
200-mg capsule
or 10-mg/mL oral solution |
Emtriva
200-mg capsule once daily or
240-mg (24-mL) oral solution once daily
Take without regard to meals.
|
Alternative NRTI for dual-NRTI backbone of combination regimens. |
PK study shows slightly lower levels in third trimester, compared with postpartum.30 No clear need to increase dose. High placental transfer to fetus. |
No evidence of human teratogenicity (can rule out 2-fold increase in overall birth defects).25 If hepatitis B coinfected, possible hepatitis B flare if drug stopped postpartum; see Special Situations: Hepatitis B Virus Coinfection. |
Truvada
FTC 200 mg + TDF 300 mg |
Truvada
1 tablet once daily |
Atripla
FTC 200 mg + EFVd 600 mg + TDF 300 mg |
Atripla
1 tablet at or before bedtime
Take on an empty stomach to reduce side effects. |
Tenofovir Disoproxil Fumarate
(TDF)
Viread |
Viread
300-mg tablet |
Viread
1 tablet once daily
Take without regard to meals. |
Alternative NRTI for dual-NRTI backbone of combination regimens. TDF would be a preferred NRTI in combination with 3TC or FTC in women with chronic HBV infection. Because of potential for renal toxicity, renal function should be monitored. |
AUC lower in third trimester than postpartum but trough levels adequate.31 High placental transfer to fetus.7,32-35 |
No evidence of human teratogenicity (can rule out 2-fold increase in overall birth defects).25 Studies in monkeys at doses approximately 2-fold higher than that for human therapeutic use show decreased fetal growth and reduction in fetal bone porosity within 2 months of starting maternal therapy.36 Clinical studies in humans (particularly children) show bone demineralization with chronic use; clinical significance unknown.37,38 If hepatitis B coinfected, possible hepatitis B flare if drug stopped postpartum; see Special Situations: Hepatitis B Virus Coinfection. |
Truvada
TDF 300 mg + FTC 200 mg |
Truvada
1 tablet once daily |
Atripla
TDF 300 mg +
EFVd 600 mg + FTC 200 mg |
Atripla
1 tablet at or before bedtime
Take on an empty stomach to reduce side effects. |
Use in Special Circumstances |
Didanosine
(ddI)
Videx EC,
generic didanosine (dose same as Videx EC) |
Videx EC
125-, 200-, 250-, 400-mg capsules
Buffered tablets (non-EC) no longer available
Videx
10-mg/mL oral solution
|
Body weight ≥60kg: 400 mg once daily; with TDF, 250 mg once daily
Body weight <60kg: 250 mg once daily; with TDF, 200 mg once daily
Take 1/2 hour before or 2 hours after a meal.
Preferred dosing with oral solution is BID (total daily dose divided into 2 doses).
|
Because of the need to administer on empty stomach and potential toxicity, ddI should be used only in special circumstances where preferred or alternative NRTIs cannot be used. ddI should not be used with d4T. |
PK not significantly altered in pregnancy; no change in dose indicated.39 Moderate placental transfer to fetus. |
In the APR, an increased rate of birth defects with ddI compared to general population was noted after both first trimester (19/409, 4.6%, 95% CI, 2.8–7.2) and later exposure (20/460, 4.3%, 95% CI 2.7–6.6). This difference may have been due to maternal characteristics such as older age or more advanced disease among women using ddI. No specific pattern of defects was noted and clinical relevance is uncertain. Lactic acidosis, sometimes fatal, has been reported in pregnant women receiving ddI and d4T together.40,41 |
Stavudine
(d4T)
Zerit |
Zerit
15-, 20-, 30-,
40-mg capsules or 1-mg/mL oral solution |
Body weight ≥60 kg:
40 mg BID
Body weight <60 kg:
30 mg BID
Take without regard to meals.
WHO recommends 30-mg BID dosing regardless of body weight.
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Because of potential toxicities, d4T should be used only in special circumstances where preferred or alternative NRTIs cannot be used. d4T should not be used with ddI or ZDV. |
PKs not significantly altered in pregnancy; no change in dose indicated.9 High placental transfer. |
No evidence of human teratogenicity (can rule out 2-fold increase in overall birth defects).25 Lactic acidosis, sometimes fatal, has been reported in pregnant women receiving ddI and d4T together.40,41 |
NNRTIs |
|
|
NNRTIs are recommended for use in combination regimens with 2 NRTI drugs. |
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Hypersensitivity reactions, including hepatic toxicity, and rash more common in women; unclear if increased in pregnancy. |
Preferred Agents |
Nevirapine
(NVP)
Viramune |
200-mg tablets or
50-mg/5-mL oral suspension |
200 mg once daily for 14 days (lead-in period); thereafter, 200 mg BID
Take without regard to meals.
Repeat lead-in period if therapy is discontinued for >7 days.
In patients who develop mild-to-moderate rash without constitutional symptoms during lead-in, continue lead-in dosing until rash resolves, but ≤28 days total.
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NVP should be initiated in pregnant women with CD4 T-lymphocyte (CD4-cell) counts >250 cells/mm3 only if benefit clearly outweighs risk because of the increased risk of potentially life-threatening hepatotoxicity in women with high CD4-cell counts. Elevated transaminase levels at baseline also may increase the risk of NVP toxicity. Women who become pregnant while taking NVP-containing regimens and are tolerating them well can continue therapy, regardless of CD4-cell count. |
PK not significantly altered in pregnancy; no change in dose indicated.42-44 High placental transfer to fetus. |
No evidence of human teratogenicity (can rule out 2-fold increase in overall birth defects).25 Increased risk of symptomatic, often rash-associated, and potentially fatal liver toxicity among women with CD4-cell counts >250/mm3 when first initiating therapy;45,46 unclear if pregnancy increases risk. |
Use in Special Circumstances |
Efavirenzd
(EFV)
Sustiva |
50-, 200-mg capsules or 600-mg tablets |
600 mg once daily at or before bedtime
Take on an empty stomach to reduce side effects. |
Non-pregnant women of childbearing potential should undergo pregnancy testing before initiation of EFV and counseling about the potential risk to the fetus and desirability of avoiding pregnancy while on EFV-containing regimens. Alternate ARV regimens that do not include EFV should be strongly considered in women who 1) are planning to become pregnant or 2) are sexually active and not using effective contraception, assuming these alternative regimens are acceptable to the provider and are not thought to compromise the health of the woman. Because the risk of neural tube defects is restricted to the first 5–6 weeks of pregnancy and pregnancy is rarely recognized before 4–6 weeks of pregnancy, and unnecessary ARV drug changes during pregnancy may be associated with loss of viral control and increased risk of perinatal transmission, EFV may be continued in pregnant women receiving an EFV-based regimen who present for antenatal care in the first trimester, provided there is virologic suppression on the regimen (see HIV-Infected Pregnant Women Who are Currently Receiving Antiretroviral Treatment). |
AUC decreased during third trimester, compared with postpartum, but nearly all third-trimester subjects exceeded target exposure and no change in dose is indicated.47 Moderate placental transfer to fetus. |
FDA Pregnancy Class D; significant malformations (anencephaly, anophthalmia, cleft palate) were observed in 3 of 20 infants (15%) born to cynomolgus monkeys receiving EFV during the first trimester at a dose resulting in plasma levels comparable to systemic human therapeutic exposure. There are 4 retrospective case reports and 1 prospective case report of neural tube defects in humans with first-trimester exposure and 1 prospective case of anophthalmia with facial clefts;25,48,49 relative risk unclear. |
Atripla
EFVd 600 mg + FTC 200 mg + TDF 300 mg |
Atripla
1 tablet once daily at or before bedtime |
Insufficient Data to Recommend Use |
Etravirine
(ETR)
Intelence |
100-, 200-mg tablets |
200 mg BID
Take following a meal. |
Safety and PK data in pregnancy are insufficient to recommend use during pregnancy. |
Limited PK data in pregnancy; in 4 pregnant women, drug levels and AUC similar to those in non-pregnant adults, suggesting no dose modification needed.50 |
Limited experience in human pregnancy. Only 23 first-trimester exposures have been reported to APR. No evidence of teratogenicity in rats and rabbits. |
Rilpivirine
(RPV)
Endurant |
25-mg tablets |
25 mg once daily with a meal. |
Safety and PK data in pregnancy are insufficient to recommend use during pregnancy. |
No PK studies in human pregnancy, placental transfer rate unknown. |
No published experience in human pregnancy. No evidence of teratogenicity in rats or rabbits. |
Complera
RPV 25 mg +
TDF 300 mg +
FTC 200 mg |
Complera
1 tablet once daily |
PIs |
|
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PIs are recommended for use in combination regimens with 2 NRTI drugs. |
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Hyperglycemia, new onset or exacerbation of diabetes mellitus, and diabetic ketoacidosis reported with PI use; unclear if pregnancy increases risk. Conflicting data regarding preterm delivery in women receiving PIs (see text). |
Preferred Agents |
Atazanavir (ATV)
Reyataz (combined with low-dose RTV boosting) |
100-, 150-, 200-, 300-mg capsules |
ATV 300 mg + RTV 100 mg once daily
Second and third trimester:
Some experts recommend increased dose (ATV 400 mg + RTV 100 mg once daily) in all pregnant women in the second and third trimesters
ATV package insert recommends increased dose (ATV 400 mg + RTV 100 mg once daily) in the following situations:
- With TDF or H2-receptor antagonist (not both; use of both with ATV not recommended) in ARV-experienced pregnant patients
- With EFVd in ARV-naive patients (Concurrent use of ATV with EFV in ARV-experienced patients is not recommended because of decreased ATV levels.)
Take with food.
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Preferred PI for use in combination regimens in pregnancy. Should give as low-dose RTV-boosted regimen, may use once-daily dosing. Several studies have shown decreased ATV plasma concentrations with standard dosing during pregnancy.32,51,52 Use of an increased dose during the second and third trimesters resulted in plasma concentrations equivalent to those in non-pregnant adults on standard dosing.53 Although some experts recommend increased ATV dosing in all women during the second and third trimesters, the package insert recommends increased ATV dosing only for ARV-experienced pregnant women in the second and third trimesters also receiving either TDF or an H2-receptor antagonist or ARV-naive pregnant women receiving EFV. ATV should not be used in patients receiving both TDF and H2 receptor antagonists or in ARV-experienced patients also taking EFV. |
Two of three intensive PK studies of ATV with RTV boosting during pregnancy and the PK study described in the recently approved product label suggest that standard dosing in pregnancy results in decreased plasma concentrations, compared with non-pregnant adults. 32,35,51,52 ATV concentrations further reduced ~25% with concomitant TDF use.32,35 Low placental transfer to fetus.32,51 |
No evidence of human teratogenicity (can rule out 2-fold increase in overall birth defects).25 Theoretical concern regarding increased indirect bilirubin levels causing significant exacerbation in physiologic hyperbilirubinemia in neonates has not been observed in clinical trials to date.32,35,51,52,54 |
Lopinavir + Ritonavir
(LPV/r)
Kaletra |
Tablets: (LPV 200 mg + RTV 50 mg) or
(LPV 100 mg + RTV 25 mg)
Oral solution: Each 5 mL contains LPV 400 mg + RTV 100 mg
Oral solution contains 42% alcohol and therefore may not be optimal for use in pregnancy. |
LPV/r 400 mg/100 mg BID
Second and third trimester:
Some experts recommend increased dose (LPV/r 600 mg/150 mg BID) in second and third trimesters.
With EFVd or NVP (PI-naive or PI-experienced patients):
LPV/r 500 mg/125 mg tablets BID (Use a combination of two LPV/r 200 mg/50 mg tablets + one LPV/r 100 mg/25 mg tablet to make a total dose of LPV/r 500 mg/125 mg)
or
LPV/r 533 mg/133 mg oral solution (6.5mL) BID.
Tablets:
Take without regard to meals.
Oral solution:
Take with food.
Not used in pregnancy: Adult dosage of LPV/r 800 mg/200 mg once daily is not recommended for use in pregnancy.
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PK studies suggest dose should be increased to 600 mg/150 mg BID in second and third trimesters, especially in PI-experienced patients. If standard dosing is used, monitor virologic response and LPV drug levels, if available. Once-daily LPV/r dosing is not recommended during pregnancy because there are no data to address whether drug levels are adequate with such administration |
AUC decreased in second and third trimesters with standard dosing.55-57 AUC with dose of LPV/r 600 mg/150 mg twice daily in third trimester in U.S. women resulted in AUC similar to that in non-pregnant adults taking
LPV/r 400 mg/100 mg dose twice daily.30 Low placental transfer to fetus.
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No evidence of human teratogenicity (can rule out 2-fold increase in overall birth defects).25 Well tolerated; short-term safety demonstrated in Phase I/II studies. |
Ritonavir
(RTV)
Norvir
When used as low-dose booster with other PIs
|
100-mg capsules
100-mg tablets
80-mg/mL oral solution
Oral solution contains 43% alcohol and therefore may not be optimal for use in pregnancy.
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As PK booster for other PIs:
100–400 mg per day in 1–2 divided doses (Refer to other PIs for specific dosing recommendations.)
Tablets:
Take with food.
Capsule and oral solution: Take with food if possible, which may improve tolerability.
|
Should only be used in combination with second PI as low-dose RTV “boost” to increase levels of second PI because of low drug levels in pregnant women when used as a sole PI and poor tolerance when given as full dose. |
Phase I/II study in pregnancy showed lower levels during pregnancy compared with postpartum.58 Minimal placental transfer to fetus. |
No evidence of human teratogenicity (can rule out 2-fold increase in overall birth defects).25 Limited experience at full dose in human pregnancy; should be used as low-dose RTV boosting with other PIs. |
Alternative Agents |
Darunavir
(DRV)
Prezista (must be combined with low-dose RTV boosting) |
75-, 150-, 400-, 600-mg tablets |
ARV-naive patients:
(DRV 800 mg + RTV 100 mg) once daily
ARV-experienced patients:
(DRV 800 mg + RTV 100 mg) once daily if no DRV resistance mutations
(DRV 600 mg + RTV 100 mg) BID if any DRV resistance mutations
Some experts recommend use of only twice-daily dosing (DRV 600 mg + RTV 100 mg BID) during pregnancy.
Unboosted DRV is not recommended.
Take with food.
|
Safety and PK data in pregnancy are limited. DRV may be considered when preferred and alternative agents cannot be used. Must give as low-dose RTV-boosted regimen. |
In PK study of women in the third trimester and postpartum, third-trimester DRV average plasma concentrations were decreased by 23%–28% with once- and twice-daily dosing and third-trimester DRV trough concentrations were low, especially with once-daily dosing.59 Some experts recommend use of only twice-daily dosing during pregnancy and investigation of use of an increased twice-daily dose is under way. Low placental transfer to fetus.59 |
Insufficient data to assess for teratogenicity in humans. No evidence of teratogenicity in mice, rats, or rabbits but low bioavailability limited exposure. Limited experience in human pregnancy. |
Saquinavir
(SQV)
Invirase
(available as capsules and tablets. SQV must be combined with low-dose RTV boosting.) |
500-mg tablets or
200-mg capsules |
(SQV 1000 mg + RTV 100 mg) BID
Unboosted SQV is not recommended.
Take with meals or within 2 hours after a meal.
|
PK data on SQV capsules and the tablet formulation in pregnancy are limited. RTV-boosted SQV capsules or SQV tablets are alternative PIs for combination regimens in pregnancy and are alternative initial ARV recommendations for non-pregnant adults. Must give as low-dose RTV-boosted regimen. |
Limited PK data on capsules and the 500-mg tablet formulation suggest that 1000-mg SQV capsules /100 mg RTV given twice daily achieves adequate SQV drug levels in pregnant women.60 Minimal placental transfer to fetus. |
Insufficient data to assess for teratogenicity in humans. No evidence of teratogenicity in rats or rabbits but low bioavailability limited exposure. Well tolerated; short-term safety demonstrated for mothers and infants for SQV in combination with low-dose RTV. Baseline ECG recommended before starting because PR and/or QT interval prolongations have been observed and drug is contraindicated in patients with pre-existing cardiac conduction system disease. |
Use in Special Circumstances |
Indinavir
(IDV)
Crixivan
(combined with low-dose RTV boosting) |
100-, 200-, 400- mg capsules |
With RTV:
(IDV 800 mg + RTV 100–200 mg) BID
Take without regard to meals.
Not used in pregnancy: Adult dosage of IDV (without RTV) 800 mg every 8 hours is not recommended for use in pregnancy.
|
Because of twice-daily dosing, pill burden, and potential for renal stones, IDV should only be used when preferred and alternative agents cannot be used. Must give as low-dose RTV-boosted regimen. |
Two studies including 18 women receiving IDV 800 mg TID showed markedly lower levels during pregnancy compared with postpartum, although suppression of HIV RNA levels was seen.61,62 In a study of RTV-boosted IDV (400 mg IDV/100 mg RTV twice daily), 82% of women met the target trough level.63 Minimal placental transfer to fetus. |
No evidence of human teratogenicity (can rule out 2-fold increase in overall birth defects).25 Theoretical concern regarding increased indirect bilirubin levels, which may exacerbate physiologic hyperbilirubinemia in neonates, but minimal placental passage. Use of unboosted IDV during pregnancy is not recommended. |
Nelfinavir
(NFV)
Viracept |
250-, 625-mg tablets
50-mg/g oral powder
|
1250 mg BID
Take with food.
Not used in pregnancy: Adult dosage of NFV 750 mg TID is not recommended for use in pregnancy.
|
Given PK data and extensive experience with use in pregnancy, NFV might be considered in special circumstances for prophylaxis of transmission in women in whom therapy would not otherwise be indicated when alternative agents are not tolerated. In clinical trials of initial therapy in non-pregnant adults, NFV-based regimens had a lower rate of viral response compared with LPV/r- or EFV-based regimens but similar viral response to ATV- or NVP-based regimens. |
Adequate drug levels are achieved in pregnant women with NFV 1250 mg given twice daily, although levels are variable in late pregnancy.43,64,65 In a study of women in their second and third trimesters dosed at 1250 mg twice daily, women in the third trimester had lower concentration of NFV than those in the second trimester.65 In a study of the new 625-mg tablet formulation dosed at 1250 mg twice daily, lower AUC and peak levels were observed during the third trimester than postpartum.66 Minimal to low placental transfer to fetus. |
No evidence of human teratogenicity (can rule out 2-fold increase in overall birth defects).25 Well tolerated; short-term safety demonstrated for mothers and infants. |
Insufficient Data to Recommend Use |
Fosamprenavir (FPV)
Lexiva (a prodrug of amprenavir) (recommended to be combined with low-dose RTV boosting) |
700-mg tablet or 50-mg/mL oral suspension |
ARV-naive patients:
- FPV 1400 mg BID or
- (FPV 1400 mg + RTV 100–200 mg) once daily or
- (FPV 700 mg + RTV 100 mg) BID
PI-experienced patients (once-daily dosing not recommended):
- (FPV 700 mg + RTV 100 mg) BID
With EFV:
- (FPV 700 mg + RTV 100 mg) BID or
- (FPV 1400 mg + RTV 300 mg) once daily
Tablet:
Take without regard to meals (if not boosted with RTV tablet).
Suspension:
Take without food.
FPV with RTV tablet: Take with meals.
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Safety and PK data in pregnancy are insufficient to recommend routine use during pregnancy in ARV-naive patients. Recommended to be given as low-dose RTV-boosted regimen. |
With RTV boosting, AUC is reduced during the third trimester. However, exposure is greater during the third trimester with boosting than in non-pregnant adults without boosting and trough concentrations achieved during the third trimester were adequate for patients without PI resistance mutations.67 Low placental transfer to fetus. |
Insufficient data to assess for teratogenicity in humans. Increased fetal loss in rabbits but no increase in defects in rats and rabbits. Limited experience in human pregnancy. |
Tipranavir
(TPV)
Aptivus (must be combined with low-dose RTV boosting) |
250-mg capsules or
100-mg/mL oral solution |
(TPV 500 mg + RTV 200 mg) BID
Unboosted TPV is not recommended.
TPV taken with RTV tablets:
Take with meals.
TPV taken with RTV capsules or solution:
Take without regard to meals.
|
Safety and PK data in pregnancy are insufficient to recommend routine use during pregnancy in ARV-naive patients. Must give as low-dose RTV-boosted regimen. |
Limited PK studies in human pregnancy. Moderate placental transfer to fetus reported in one patient.68 |
Insufficient data to assess for teratogenicity in humans. No teratogenicity in rats or rabbits. Limited experience in human pregnancy. |
Entry Inhibitors |
Insufficient Data to Recommend Use |
Enfuvirtide
(T20)
Fuzeon |
- Injectable—supplied as lyophilized powder
- Each vial contains 108 mg of T20; reconstitute with 1.1 mL of sterile water for injection for delivery of approximately 90 mg/1 mL.
|
90 mg (1mL) SQ BID |
Safety and PK data in pregnancy are insufficient to recommend use during pregnancy in ARV-naive patients. |
Limited PK studies in human pregnancy. No placental transfer to fetus, based on very limited data.68,69 |
Insufficient data to assess for teratogenicity in humans. No evidence of teratogenicity in rats or rabbits. Minimal data in human pregnancy.68,70 |
Maraviroc
(MVC)
Selzentry |
150-, 300-mg tablets |
- 150 mg BID when given with strong CYP3A inhibitors (with or without CYP3A inducers) including PIs (except TPV/r)
- 300 mg BID when given with NRTIs, NVP, RAL, T-20, TPV/r, and other drugs that are not strong CYP3A inhibitors or inducers
- 600 mg BID when given with CYP3A inducers, including EFV, ETR (without a CYP3A inhibitor)
Take without regard to meals.
|
Safety and PK data in pregnancy are insufficient to recommend use during pregnancy in ARV-naive patients. |
No PK studies in human pregnancy. Unknown placental transfer rate to fetus. |
Insufficient data to assess for teratogenicity in humans. No evidence of teratogenicity in rats or rabbits. Limited experience in human pregnancy. |
Integrase Inhibitors |
Use in Special Circumstances |
Raltegravir
(RAL)
Isentress |
400-mg tablets |
400 mg BID
With rifampin:
800 mg BID
Take without regard to meals.
|
Safety and PK data in pregnancy are limited; can be considered for use in special circumstances when preferred and alternative agents cannot be used. |
During third trimester, RAL PK showed extensive variability but RAL exposure was not consistently altered compared with postpartum and historical data. The standard dose appears appropriate during pregnancy.71 Variable but high placental transfer to fetus.71,72 |
Insufficient data to assess for teratogenicity in humans. Increased skeletal variants in rats, no increase in defects in rabbits. Limited experience in human pregnancy. |