tolazamide (Rx)

Frequency Not Defined

Hypoglycemia

Dermatologic reactions

Heartburn

Dizziness

Vertigo

Anorexia

Constipation

Nausea/vomiting

Cholestatic jaundice and hepatitis may occur rarely which may progress to liver failure

Contraindications

Hypersensitivity, sulfa allergy

Type I diabetes, diabetic ketoacidosis

Cautions

Patients with hypoglycemia, stress due to infection, fever, trauma, or surgery

May cause loss of glycemic control due to secondary failure

First generation sulfonylurea

Intermediate acting agent

Tolazamide demonstrates weak diuretic effect

Pregnancy Category: C

Lactation: not known if crosses into breast milk, avoid

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Mechanism of Action

Initial effect is to increase beta-cell insulin secretion

May also decrease rate of hepatic glucose production, increases insulin receptor sensitivity, and increases number of insulin receptors

Pharmacokinetics

Half-Life: 7 hr

Duration: 14-24 hr

Onset: 20 minutes

Protein binding: 94%

Peak hypoglycemic effect: 4-6 hr

Metabolism: Hepatic to less active metabolites

Metabolites: Inactive metabolites

Excretion: Urine (85%); feces (7%)