Trade Names:Tolazamide- Tablets 100 mg- Tablets 250 mg- Tablets 500 mg
Decreases blood glucose by stimulating release of insulin from pancreas.
Tolazamide T max is 3 to 4 h. The drug is well absorbed from the GI tract.
There are 5 major metabolites ranging in hypoglycemic activity from 0% to 70%.
Tolazamide t ½ is 7 h. Tolazamide is excreted principally in the urine (85%), and 7% in feces over a 5-day period.
Onset of action of tolazamide is 4 to 6 h.
Time to peak effect of tolazamide is 4 to 6 h.
Duration of action is 10 h.
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.
Temporary adjunct to insulin therapy in selected patients with non–insulin-dependent diabetes mellitus to improve diabetic control.
Hypersensitivity to sulfonylureas; diabetes complicated by ketoacidosis, with or without coma; sole therapy of insulin-dependent (type 1) diabetes mellitus; gestational diabetes.
PO 100 to 250 mg/day with breakfast or first main meal. If fasting blood sugar (FBS) is less than 200 mg/dL, initial dose is 100 mg/day or if FBS is greater than 200 mg/dL, initial dose is 250 mg/day. In malnourished, underweight, elderly patients use 100 mg/day. May adjust dose by 100 to 250 mg/wk as needed to a maximum of 1000 mg/day. If more than 500 mg/day is required, give in divided doses twice daily. Doses greater than 1 g/day are not likely to improve control.Maintenance dose
PO Usual dose is 100 to 1000 mg/day with the average 250 to 500 mg/day. Following initiation of therapy, dosage adjustment is made in increments of 100 to 250 mg at weekly intervals based on patient's blood glucose response.
Increased hypoglycemic effect.Beta-blockers, calcium channel blockers, cholestyramine, corticosteroids, diazoxide, estrogens, hydantoins, isoniazid, nicotinic acid, oral contraceptives, phenothiazines, rifampin, sympathomimetics, thiazide diuretics, thyroid agents, urinary alkalinizers
Decreased hypoglycemic effect.Charcoal
Charcoal can reduce the absorption; depending on clinical situation, this will reduce sulfonylureas efficacy or toxicity.Digitalis glycosides
Coadministration may result in increased digitalis serum levels.
None well documented.
Increased risk of cardiovascular mortality.
Allergic skin reactions; eczema; pruritus; erythema; urticaria; morbilliform or maculopapular eruptions; lichenoid reactions.
Nausea; epigastric fullness; heartburn; cholestatic jaundice.
Leukopenia; thrombocytopenia; aplastic anemia; agranulocytosis; hemolytic anemia; pancytopenia; hepatic porphyria.
Disulfiram-like reaction; weakness; paresthesia; fatigue; malaise.
Category C .
Safety and efficacy not established.
Elderly and debilitated patients are particularly susceptible to hypoglycemic action of sulfonylureas.
Use drug with caution and monitor renal function frequently.
Use drug with caution and monitor liver function frequently.
Tolazamide may produce severe hypoglycemia, which may be more difficult to recognize in elderly or in patients receiving beta-blockers.
Administration with alcohol may include facial flushing reaction and occasional breathlessness. This reaction has been reported more commonly with other sulfonylureas.
Hyperglycemia is major risk factor in development of diabetic complications. Measurement of glycosylated hemoglobin and self-monitoring of blood glucose are useful.
Stress (including fever, trauma, infection, or surgery) or secondary failure (wherein drug's effectiveness in lowering blood glucose diminishes over time) may precipitate loss of blood glucose control.
Hypoglycemia including symptoms of the following: tingling of lips and tongue, nausea, lethargy, confusion, agitation, nervousness, tachycardia, sweating, tremor, hunger, convulsions, stupor, coma.
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