- Tablets 5 mg
- Tablets 10 mg
- Tablets, extended release 5 mg
- Tablets, extended release 10 mg
Decreases blood glucose by stimulating insulin release from pancreas and by increasing tissue sensitivity to insulin.
Bioavailability is 100% (immediate-release); 90% (extended-release). T max is 1 to 3 h (immediate-release); 6 to 12 h (extended-release). Food delays absorption by about 40 min.
The mean apparent Vd is about 10 L. Protein binding is 98% to 99%.
Mean t ½ is 2 to 5 h. Mean total Cl is about 3 L/h. About 80% is excreted in urine and 10% in feces as metabolites.
Indications and Usage
Adjunct to diet to lower blood glucose in patients with non-insulin-dependent diabetes mellitus (type 2) whose hyperglycemia cannot be controlled by diet alone.
Hypersensitivity to sulfonylureas; diabetes complicated by ketoacidosis, with or without coma; sole therapy of insulin-dependent (type 1) diabetes mellitus; diabetes when complicated by pregnancy.
Dosage and AdministrationAdults
PO 5 mg/day 30 min before breakfast. Adjust dose in 2.5 to 5 mg/day increments based on blood glucose response. Divided doses may be given (single daily dose max, 15 mg; total daily dose max, 40 mg).Elderly or patients with liver disease
PO 2.5 mg/day initially.
Store in tightly closed container at room temperature.
Produces disulfiram-like reactions (eg, facial flushing, headache, breathlessness).Androgens, chloramphenicol, clofibrate, fenfluramine, fluconazole, gemfibrozil, histamine H 2 antagonists, magnesium salts, methyldopa, monoamine oxidase, oral anticoagulants, phenylbutazone, probenecid, salicylates, sulfinpyrazone, sulfonamides, tricyclic antidepressants, urinary acidifiers
Hypoglycemic effects may be increased.Beta-blockers, cholestyramine, diazoxide, hydantoins, rifampin, thiazide diuretics, urinary alkalinizers
May decrease hypoglycemic effect.Food
Absorption is delayed when taken with food. Give drug about 30 min before meal.
Laboratory Test Interactions
Mild-to-moderate elevations in BUN and creatinine.
May have increased risk of CV mortality when compared with patients treated with diet alone.
Allergic skin reactions; eczema; pruritus; erythema; urticaria; morbilliform or maculopapular eruptions; lichenoid reactions; photosensitivity.
GI disturbances (eg, nausea, epigastric fullness, heartburn); diarrhea.
Mild diuresis; elevated BUN and creatinine.
Cholestatic jaundice; elevated LFT results.
Leukopenia; thrombocytopenia; aplastic anemia; agranulocytosis; hemolytic anemia; pancytopenia; hepatic porphyria.
Disulfiram-like reaction; weakness; paresthesia; fatigue; malaise.
Category C . Insulin is recommended to maintain blood glucose levels during pregnancy. Prolonged severe neonatal hypoglycemia can occur if sulfonylureas are administered at time of delivery.
Safety and efficacy not established.
Elderly and debilitated patients are particularly susceptible to hypoglycemic action. Hypoglycemia may be difficult to recognize in elderly.
Use drug with caution and monitor renal function frequently.
Use drug with caution and monitor liver function frequently.
Prolonged hypoglycemia, tingling of lips and tongue, hunger, nausea, lethargy, yawning, confusion, agitation, nervousness, tachycardia, sweating, tremor, convulsions, stupor, coma.
- Remind patient to take medication on empty stomach 30 min before meals.
- Teach patient to self-monitor blood glucose.
- Emphasize importance of following diabetic diet.
- Inform patient that this drug is not substitute for exercise and diet control and that patient should follow prescribed regimens.
- Instruct patient to inform health care provider that they are taking this drug.
- Advise patient to carry identification stating that patient is diabetic.
- Inform patient to contact health care provider if symptoms of hypoglycemia occur (eg, fatigue, excessive hunger, profuse sweating, numbness of extremities).
- Tell patient to notify health care provider if symptoms of hyperglycemia occur (eg, excessive thirst or urination, urinary glucose or ketones).
- Instruct patient to report these symptoms to health care provider: nausea, vomiting, diarrhea, heartburn, sore throat, rash, unusual bruising or bleeding or other physical complaints.
- Advise patient not to take any medication (including OTC) or alcohol without consulting health care provider.
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