Tolazamide

Trade Names:
Tolazamide
- Tablets 100 mg
- Tablets 250 mg
- Tablets 500 mg

Pharmacology

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Decreases blood glucose by stimulating release of insulin from pancreas.

Pharmacokinetics

Absorption

Tolazamide T _max is 3 to 4 h. The drug is well absorbed from the GI tract.

Metabolism

There are 5 major metabolites ranging in hypoglycemic activity from 0% to 70%.

Elimination

Tolazamide t _½ is 7 h. Tolazamide is excreted principally in the urine (85%), and 7% in feces over a 5-day period.

Onset

Onset of action of tolazamide is 4 to 6 h.

Peak

Time to peak effect of tolazamide is 4 to 6 h.

Duration

Duration of action is 10 h.

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.

Unlabeled Uses

Temporary adjunct to insulin therapy in selected patients with non–insulin-dependent diabetes mellitus to improve diabetic control.

Contraindications

Hypersensitivity to sulfonylureas; diabetes complicated by ketoacidosis, with or without coma; sole therapy of insulin-dependent (type 1) diabetes mellitus; gestational diabetes.

Dosage and Administration

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.

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.

Drug Interactions

Increased hypoglycemic effect.

Decreased hypoglycemic effect.

Charcoal can reduce the absorption; depending on clinical situation, this will reduce sulfonylureas efficacy or toxicity.

Coadministration may result in increased digitalis serum levels.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Increased risk of cardiovascular mortality.

CNS

Dizziness; vertigo.

Dermatologic

Allergic skin reactions; eczema; pruritus; erythema; urticaria; morbilliform or maculopapular eruptions; lichenoid reactions.

GI

Nausea; epigastric fullness; heartburn; cholestatic jaundice.

Genitourinary

Mild diuresis.

Hematologic

Leukopenia; thrombocytopenia; aplastic anemia; agranulocytosis; hemolytic anemia; pancytopenia; hepatic porphyria.

Metabolic

Hypoglycemia.

Miscellaneous

Disulfiram-like reaction; weakness; paresthesia; fatigue; malaise.

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Elderly

Elderly and debilitated patients are particularly susceptible to hypoglycemic action of sulfonylureas.

Renal Function

Use drug with caution and monitor renal function frequently.

Hepatic Function

Use drug with caution and monitor liver function frequently.

Hypoglycemia

Tolazamide may produce severe hypoglycemia, which may be more difficult to recognize in elderly or in patients receiving beta-blockers.

Disulfiram-like syndrome

Administration with alcohol may include facial flushing reaction and occasional breathlessness. This reaction has been reported more commonly with other sulfonylureas.

Hyperglycemia

Hyperglycemia is major risk factor in development of diabetic complications. Measurement of glycosylated hemoglobin and self-monitoring of blood glucose are useful.

Loss of blood glucose control

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.

Overdosage

Symptoms

Hypoglycemia including symptoms of the following: tingling of lips and tongue, nausea, lethargy, confusion, agitation, nervousness, tachycardia, sweating, tremor, hunger, convulsions, stupor, coma.

Patient Information

• Teach signs and symptoms of hypoglycemia (eg, profuse sweating, excessive hunger, weakness, dizziness, tremor, tachycardia, anxiety, numbness of extremities) and of hyperglycemia (eg, excessive thirst or urination, urinary glucose or ketones, fever, sore throat, unusual bleeding or rash). Remind patient to keep source of quick-acting sugar available at all times.
• When adjusting the dose, tell patient to check urine for ketones and blood for glucose 3 times a day; 1 to 2 times a day after stable control is established. Tell patient to notify health care provider if planning surgery or experiencing vomiting, injury, infection, or fever.
• Demonstrate correct technique for performing blood glucose and urine glucose and ketone tests, and ensure correct return demonstrations.
• Tell patient to report repeated abnormal glucose or ketone results to health care provider.
• Emphasize importance of continuing diet restrictions and exercise regimen.
• Caution about disulfiram-like syndrome (eg, facial flushing, abdominal cramping, nausea) when consuming alcohol. Advise patient to avoid alcohol.
• Inform patient that therapy will not cure disease.

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