Tolbutamide (Ornase™)
Tolazamide (Tolinase™)
Chlorpropamide (Diabenese™) |
Sulfonylureas
(1st generation) |
Increases insulin production in
the pancreas. |
Tolbutamide: 0.25–2.0 g/day in divided doses; maximum, 3 g/day
Tolazamide: 100–1,000 mg/day in divided doses; maximum, 1 g/day
Chlorpropamide: 100–500 mg/day twice a day; maximum, 750 mg/day |
Hypoglycemia, weight gain,
hyperinsulinemia
Disulfiram reaction with alcohol |
Chlorpropamide remains active for up to
60 hours. Use extreme caution with elderly
patients or patients with hepatic or renal
dysfunction. |
All are metabolized in liver. Periodic evaluation
of liver function is suggested. |
Use of these agents is not recommended unless the patient has a wellestablished
history of taking them. Second-generation sulfonylureas
provide more predictable results with fewer side effects and more
convenient dosing. |
Glyburide (Micronase™, Diabeta™,
Glynase™)
Glipizide (Glucotrol, Glucotrol XL™)
Glimepiride (Amaryl™) |
Sulfonylureas
(2nd generation) |
Increases insulin production in
the pancreas. |
Glyburide: 1.25–5 mg/once or twice a day; maximum, 20 mg/day
Glynase: 0.75–12.0 mg/day; maximum 12 mg/day
Glipizide: 2.5–20.0 mg/once or twice a day; maximum, 40 mg/day;
or XL* 2.5–10.0 mg/once or twice a day; maximum, 20 mg/day
Glimepiride: 1–8 mg/day; maximum, 8 mg/day |
Hypoglycemia, weight gain,
hyperinsulinemia |
Clearance may be diminished in patients
with hepatic or renal impairment. |
|
Glipizide is preferred with renal impairment.
Doses >15 mg should be divided.
Glimepiride indicated for use with insulin.
Shown to have some insulin-sensitizing effect. |
| Repaglinide (Prandin™) |
Meglitinide |
Increases insulin release from pancreas. |
New diagnosis or A1C <8%, 0.5 mg;
A1C >8%, 1–2 mg, 15–30 min before each meal;
increase weekly until results are obtained;
maximum, 16 mg/day |
Hypoglycemia, weight gain,
hyperinsulinemia |
Use with caution on patient with hepatic
or renal impairment. |
|
Patients should be instructed to take medication no more than
30 minutes prior to a meal. If meals are skipped or added, the
medication should be skipped or added as well. Approved for use as
monotherapy or in combinatin with TZD or metformin. |
| Nateglinide (Starlix™) |
Phenylalanine derivative |
Increases insulin release from pancreas. |
60–120 mg before each meal |
Minimal risk of hypoglycemia |
Currently no contraindications available.
Use with caution with moderate to severe
hepatic disease. |
Periodic evaluation of liver function tests. |
Approved as monotherapy or in combination with metformin or
TZD. Has only a 2-hour duration of action. If meals are skipped
or added, the medication should be skipped or added as well. |
Metformin (Fortamet™,
Glumetza™, Glucophage™) |
Biguanide |
Primarily decreases hepatic glucose production.
Minor increase in muscle glucose uptake which
may improve insulin resistance. |
500 mg/day twice a day with meals, increase by 500 mg every 1–3 wk,
twice or three times a day; usually most effective at 2,000 mg/day;
maximum, 2,550 mg/day
Long acting form Glucophage XR™: 500mg once/day, max dose 2000mg once/day |
Nausea, diarrhea, metallic taste,
possible lactic acidosis |
Due to increased risk of lactic acidosis,
should not use if suspect frequent alcohol
use, liver or kidney disease, or CHF. |
Contraindicated if serum creatinine is:
>1.5 mg/dL in men or >1.4 mg/dL women.
Do not use if creatinine clearance is abnormal.
Monitor hematological and renal function annually. |
Especially beneficial in obese patients due to potential for weight
loss, improved lipid profile, and lack of potential for hypoglycemia
requiring supplemental carbohydrate intake. Discontinue for 48 hr
after contrast dye procedures. |
| Rosiglitazone (Avandia™) |
Thiazolidinedione |
Decreases insulin resistance, increasing glucose
uptake, fat redistribution; minor decrease in
hepatic glucose output; preserves -cell function;
decreases vascular inflammation. |
Initially 4 mg/day in single or divided doses.
Increase to 8 mg/day in 12 wk, if needed;
maximum, 8 mg/day with or without food |
Minor weight increase of 3–6 lbs.,
edema |
Should not be used in patients with
CHF or hepatic disease. Can cause
mild-to-moderate edema. |
Avoid initiation if ALT >2.5X upper limit of
normal. Measure ALT periodically. Discontinue
if ALT >3X upper limit of normal. |
Approved for use as monotherapy and in combination with
metformin, sulfonylureas, or insulin.
Less interactions associated with CYP-450. |
| Pioglitazone (Actos™) |
Thiazolidinedione |
Decreases insulin resistance, increasing glucose
uptake, fat redistribution; minor decrease in
hepatic glucose output; preserves -cell function;
decreases vascular inflammation. |
Initially 15 or 30 mg/day;
maximum with or without food 45 mg for monotherapy,
30 mg for combination therapy |
Minor weight increase of 3–6 lbs.,
edema |
Should not be used in patients with
CHF or hepatic disease. Can cause
mild-to-moderate edema. |
Avoid initiation if ALT >2.5X upper limit of
normal. Measure ALT periodically. Discontinue
if ALT >3X upper limit of normal. |
Avoid initiation if ALT >2.5X upper limit of normal. Measure ALT
periodically. Discontinue if ALT >3X upper limit of normal. |
Acarbose (Precose™)
Miglitol (Glyset™) |
Alpha-glucosidase
inhibitor |
Slows absorption of complex carbohydrate
from GI tract. |
25 mg/day; increase by 25 mg/day every 4–6 wk;
maximum, split dose before meals (with first bite of food)
300 mg/day(150 mg/day for weight <60 kg) |
Gas and bloating, sometimes
diarrhea for both drugs |
Should not be used if GI disorders
are concurrent. |
Avoid if serum creatinine is >2.0 mg/dL.
Monitor serum transaminase every 3 months
for 1st year of therapy. |
Approved for use as monotherapy and in combination
with metformin, sulfonylureas, or insulin. If used with
hypoglycemic agents, such as sulfonylureas or insulin,
must treat hypoglycemia with glucose not sucrose. |
Combinations |
Glucovance™
(Glyburide and Metformin) |
Sulfonylureas and
Biguanide |
Decreases hepatic glucose production and
increases insulin secretion. |
Ratios of glyburide and metformin (in mg):1.25/250, 2.5/500, 5/500.
Initial: 1.25/250 once or twice a day, increased every 2 weeks.
2nd line: 2.5–5/500 twice a day, increased every1–2 weeks.
Average dose 7.5/1,500.
Maximum dose should not exceed 20 mg glyburide/2,000 mg metformin daily. |
Hypoglycemia, weight gain,
lactic acidosis |
Should not be used if suspect frequent
alcohol use, liver or kidney disease,
or CHF. |
Same caveats as individual components. |
Patients may frequently use 2 different dose tablets to
attain desired daily dosage and results. Discontinue for
48 hr after procedure using contrast dye. |
Metaglip™
(Glipizide and Metformin) |
Sulfonylureas and
Biguanide |
Decreases hepatic glucose production and
increases insulin secretion. |
Ratios of glipizide and metformin (in mg): 2.5/250, 2.5/500, 5/500.
Initial: 2.5/250 once or twice a day, increased every 2 weeks.
2nd line: 2.5–5/500 twice a day, increased every 1– 2 weeks.
Maximum doseshould not exceed 20 mg glipizide/2,000 mg metformin daily. |
Hypoglycemia, weight gain,
lactic acidosis |
Should not be used if suspect frequent
alcohol use, liver or kidney disease,
or CHF. |
Same caveats as individual components. |
Patients may frequently use 2 different dose tablets to
attain desired daily dosage and results. Discontinue for
48 hr after procedure using contrast dye. |
Avandamet™
(Rosiglitazone and Metformin) |
Thiazolidinedione and
Biguanide |
Decreases hepatic glucose production,
increases glucose uptake, decreases insulin
resistance, and preserves -cell function. |
Ratios of rosiglitazone and metformin: 1 mg/500 mg, 2 mg/500 mg,
4 mg/500 mg, 2 mg/1,000 mg, 4 mg/1,000 mg twice a day;
dosage individualized based on current therapy.
Maximum, 8 mg/2,000 mg per day. |
Edema, possible lactic acidosis |
Should not be used if suspect frequent
alcohol use, liver or kidney disease,
or CHF. |
Same caveats as individual components. |
Less expensive than using agents separately. Reported
decrease in GI upset associated with metformin and
weight increase associated with rosiglitazone. Discontinue
for 48 hr after procedure using contrast dye. |
Actoplus Met™
(Pioglitazone and Metformin) |
Thiazolidinedione and
Biguanide |
Decreases hepatic glucose production,
increases glucose uptake, decreases insulin. |
Ratios of pioglitazone and metformin: 15 mg/500 mg, 15 mg/850 mg |
Same caveats as individual
components. |
Same caveats as individual components. |
Same caveats as individual components. |
Same caveats as individual components. |
Avandaryl™
(Rosiglitazone and Glimepiride) |
Thiazolidinedione and
Sulfonylurea |
Decreases insulin resistance and increases
insulin secretion. |
Ratios of rosiglitazone and glimepiride: 4 mg/1 mg, 4 mg/1 mg |
Same caveats as individual
components. |
Same caveats as individual components. |
Same caveats as individual components. |
Same caveats as individual components. |
