Brands, Medical Use, Clinical Data
- Hypoglycemic Agents
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
For managing hyperglycemia in Non-insulin-dependent diabetes mellitus (NIDDM).
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.
IPN-RAT LD50 580 mg/kg
Biotrnasformation / Drug Metabolism
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.
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drugs are withdrawn from a patient receiving DIABINESE, the patient should be observed closely for loss of
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drugs are withdrawn from a patient receiving DIABINESE, the patient should be observed closely for hypoglycemia.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.