Active ingredient: Chlorpropamide - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

• Hypoglycemic Agents
• Sulfonylureas

Dosage Forms

• Tablet

Brands / Synonyms

Adiaben; Apo-Chlorpropamide; Asucrol; Catanil; Chlorodiabina; Chloronase; Chloropropamide; Chlorpropamid; Chlorpropamide Bp/ Usp; Clorpropamide; Diabaril; Diabechlor; Diabenal; Diabenese; Diabeneza; Diabet-Pages; Diabetoral; Diabinese; Diamel Ex; Dynalase; Glisema; Glucamide; Hexathane; Insulase; Meldian; Melitase; Mellinese; Millinese; Novo-Propamide; Oradian; Stabinol

Indications

For managing hyperglycemia in Non-insulin-dependent diabetes mellitus (NIDDM).

Pharmacology

Chlorpropamide, a second-generation sulfonylurea antidiabetic agent, is used with diet to lower blood glucose levels in patients with diabetes mellitus type II. Chlorpropamide is twice as potent as the related second-generation agent glipizide.

Mechanism of Action

Sulfonylureas such as Chlorpropamide likely bind to ATP-sensitive potassium-channel receptors on the pancreatic cell surface, reducing potassium conductance and causing depolarization of the membrane. Depolarization stimulates calcium ion influx through voltage-sensitive calcium channels, raising intracellular concentrations of calcium ions, which induces the secretion, or exocytosis, of insulin.

Absorption

Not Available

Toxicity

IPN-RAT LD₅₀ 580 mg/kg

Biotrnasformation / Drug Metabolism

Not Available

Contraindications

DIABINESE is contraindicated in patients with:

1. Known hypersensitivity to the drug.

2. Diabetic ketoacidosis, with or without coma. This condition should be treated with insulin.

Drug Interactions

The hypoglycemic action of sulfonylurea may be potentiated by certain drugs including nonsteroidal anti-inflammatory agents and other drugs that are highly protein bound, salicylates, sulfonamides, chloramphenicol, probenecid, coumarins, monoamine oxidase inhibitors, and beta adrenergic blocking agents. When such drugs are administered to a patient receiving DIABINESE, the patient should be observed closely for hypoglycemia. When such drugs are withdrawn from a patient receiving DIABINESE, the patient should be observed closely for loss of control.

Certain drugs tend to produce hyperglycemia and may lead to loss of control. These drugs include the thiazides and other diuretics, corticosteroids, phenothiazines, thyroid products, estrogens, oral contraceptives, phenytoin, nicotinic acid, sympathomimetics, calcium channel blocking drugs, and isoniazid. When such drugs are administered to a patient receiving DIABINESE, the patient should be closely observed for loss of control. When such drugs are withdrawn from a patient receiving DIABINESE, the patient should be observed closely for hypoglycemia.

Since animal studies suggest that the action of barbiturates may be prolonged by therapy with chlorpropamide, barbiturates should be employed with caution. In some patients, a disulfiram-like reaction may be produced by the ingestion of alcohol.

A potential interaction between oral miconazole and oral hypoglycemic agents leading to severe hypoglycemia has been reported. Whether this interaction also occurs with the intravenous, topical, or vaginal preparations of miconazole is not known.