Classifications: hormone; sulfonylurea antidiabetic; Therapeutic: antidiabetic, sulfonylurea
Pregnancy Category: C
100 mg, 250 mg, 500 mg tablets
Orally effective sulfonylurea hypoglycemic structurally and pharmacologically related to tolbutamide but about 5 times more
potent. Lowers blood glucose primarily by stimulating pancreatic beta cells to secrete insulin.
Antidiabetic action is a result of stimulation of the pancreas to secrete more insulin in the presence of blood sugar; it
requires functioning beta cells.
Mild to moderately severe type 2 diabetes mellitus that cannot be controlled by diet and weight reduction and that is uncomplicated
by acidosis, ketosis, coma. Effective in primary or secondary failures to other sulfonylurea
Known sensitivity to sulfonylureas and to sulfonamides; type 1 diabetes complicated by ketoacidosis; infection; trauma;
pregnancy (category C). Safety in lactation or children is not established.
Older adults; renal disease; renal failure, renal impairment.
Route & Dosage
|Type 2 Diabetes Mellitus
Adult: PO 100 mg1 g q.d. to b.i.d. a.c., may adjust dose by 100250 mg/d at weekly intervals (max: 1 g/d)
- Give in the morning with or before meals.
- Divide dose of more than 500 mg and give b.i.d.
- Crush tablet if patient is unable to swallow it whole. Be sure to give with an allowable fluid, not dry.
- Store at 15°30° C (59°86° F) in a tightly closed container unless otherwise directed. Keep
drug out of the reach of children.
Adverse Effects (≥1%) GI:
Nausea, vomiting, cholestatic jaundice
. Metabolic: Hypoglycemia
elicits disulfiram-type reaction in some patients; oral anticoagulants
, chloramphenicol, clofibrate, phenylbutazone, mao inhibitors
, probenecid, sulfonamides
may potentiate hypoglycemic actions; thiazides
may antagonize hypoglycemic effects; cimetidine
may increase tolazamide levels, causing hypoglycemia
. Herbal: Ginseng, karela
may potentiate hypoglycemic effects.
Slowly from GI tract. Onset:
60 min. Peak:
46 h. Duration:
1015 h (up to 20 h in some patients). Distribution:
Distributed in highest concentrations in liver, kidneys, and intestines; crosses placenta; distributed into breast milk. Metabolism:
Extensively in liver. Elimination:
85% in urine, 15% in feces. Half-Life:
Assessment & Drug Effects
- Be aware that reduction of dose frequently alleviates most mild to moderately severe hypoglycemic symptoms.
- Observe patients with a history of ketoacidosis or coma closely, especially during the early adjustment period.
Patient & Family Education
- Check blood glucose and urine daily for sugar and acetone. Important to continue close medical supervision for first 6 wk
- Be aware that doses >1000 mg/d rarely provide improvement in diabetic control.
- Do not take OTC preparations unless approved or prescribed by physician.
- Understand that alcohol can precipitate a disulfiram-type reaction.