Trade Names:Glucotrol- Tablets 5 mg- Tablets 10 mg
Trade Names:Glucotrol XL- 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.
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.
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.
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.
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