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Home / Drugs / Starting with C / Chlorpropamide 		 
Chlorpropamide
  

Chlorpropamide is an oral antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM). It belongs to the sulfonylurea class of insulin secretagogues, which act by stimulating β cells of the pancreas to release insulin. Sulfonylureas increase both basal insulin secretion and meal-stimulated insulin release. Medications in this class differ in their dose, rate of absorption, duration of action, route of elimination and binding site on their target pancreatic β cell receptor. Sulfonylureas also increase peripheral glucose utilization, decrease hepatic gluconeogenesis and may increase the number and sensitivity of insulin receptors. Sulfonylureas are associated with weight gain, though less so than insulin. Due to their mechanism of action, sulfonylureas may cause hypoglycemia and require consistent food intake to decrease this risk. The risk of hypoglycemia is increased in elderly, debilitated and malnourished individuals. Chlorpropamide is not recommended for the treatment of NIDDM as it increases blood pressure and the risk of retinopathy (UKPDS-33). Up to 80% of the single oral dose of chlorpropramide is metabolized, likely in the liver; 80-90% of the dose is excreted in urine as unchanged drug and metabolites. Renal and hepatic dysfunction may increase the risk of hypoglycemia.
BrandsAdiaben
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
Insulase
Meldian
Melitase
Mellinese
Millinese
Novo-Propamide
Oradian
Stabinol
CategoriesHypoglycemic Agents
Sulfonylureas
Antidiabetic
ManufacturersBarr laboratories inc
Clonmel healthcare ltd
Duramed pharmaceuticals inc sub barr laboratories inc
Halsey drug co inc
Ivax pharmaceuticals inc
Mylan pharmaceuticals inc
Par pharmaceutical inc
Pliva inc
Sandoz inc
Superpharm corp
Teva pharmaceuticals usa inc
Usl pharma inc
Watson laboratories inc
Pfizer laboratories div pfizer inc
PackagersCentral Texas Community Health Centers
Direct Dispensing Inc.
Dispensing Solutions
H and H Laboratories
Major Pharmaceuticals
Murfreesboro Pharmaceutical Nursing Supply
Mylan
Nucare Pharmaceuticals Inc.
PCA LLC
PD-Rx Pharmaceuticals Inc.
Pfizer Inc.
Pharmedix
Physicians Total Care Inc.
Pliva Inc.
Prepackage Specialists
Prescript Pharmaceuticals
Qualitest
UDL Laboratories
Wyeth Pharmaceuticals
SynonymsChlorporpamide

indication

For treatment of NIDDM in conjunction with diet and exercise.

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 bind to ATP-sensitive potassium channels 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.

toxicity

IPN-RAT LD50 580 mg/kg

biotransformation

Up to 80% of dose is metabolized likely through the liver to to 2-hydroxylchlorpropamide (2-OH CPA), p-chlorobenzenesulfonylurea (CBSU), 3-hydroxylchlorpropamide (3-OH CPA), and p-chlorobenzenesulfonamide (CBSA); CBSA may be produced by decomposition in urine. It is unknown whether chlorpropamide metabolites exert hypoglycemic effects.

absorption

Readily absorbed from the GI tract. Peak plasma concentrations occur within 2-4 hours and the onset of action occurs within one hour. The maximal effect of chlorpropamide is seen 3-6 hours following oral administration.

half life

Approximately 36 hours with interindividual variation ranging from 25-60 hours. Duration of effect persists for at least 24 hours.

route of elimination

80-90% of a single oral dose is excreted in the urine as unchaged drug and metabolites within 96 hours.

drug interactions

Acebutolol: Acebutolol may decrease symptoms of hypoglycemia and increase the time required for the body to compensate for hypoglycemia.

Acetylsalicylic acid: Acetylsalicylic acid may increase the effect of the sulfonylurea, chlorpropamide.

Atenolol: The beta-blocker, atenolol, may decrease symptoms of hypoglycemia.

Betaxolol: The beta-blocker, betaxolol, may decrease symptoms of hypoglycemia.

Bevantolol: The beta-blocker, bevantolol, may decrease symptoms of hypoglycemia.

Bisoprolol: The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia.

Carteolol: The beta-blocker, carteolol, may decrease symptoms of hypoglycemia.

Carvedilol: The beta-blocker, carvedilol, may decrease symptoms of hypoglycemia.

Chloramphenicol: Chloramphenicol may increase the effect of sulfonylurea, chlorpropamide.

Clofibrate: Clofibrate may increase the effect of sulfonylurea, chlorpropamide.

Diazoxide: Antagonism.

Dicumarol: Dicumarol may increase the effect of sulfonylurea, chlorpropamide.

Esmolol: The beta-blocker, esmolol, may decrease symptoms of hypoglycemia.

Glucosamine: Possible hyperglycemia

Labetalol: The beta-blocker, labetalol, may decrease symptoms of hypoglycemia.

Metoprolol: The beta-blocker, metoprolol, may decrease symptoms of hypoglycemia.

Nadolol: The beta-blocker, nadolol, may decrease symptoms of hypoglycemia.

Oxprenolol: The beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia.

Penbutolol: The beta-blocker, penbutolol, may decrease symptoms of hypoglycemia.

Phenylbutazone: Phenylbutazone increases the effect of the hypoglycemic agent

Pindolol: The beta-blocker, pindolol, may decrease symptoms of hypoglycemia.

Practolol: The beta-blocker, practolol, may decrease symptoms of hypoglycemia.

Propranolol: The beta-blocker, propranolol, may decrease symptoms of hypoglycemia.

Rifampin: Rifampin may decrease the effect of sulfonylurea, chlorpropamide.

Salsalate: The salicylate, salsalate, increases the effect of the sulfonylurea, chlorpropamide.

Somatropin recombinant: Somatropin may antagonize the hypoglycemic effect of chlorpropamide. Monitor for changes in fasting and postprandial blood sugars.

Sotalol: The beta-blocker, sotalol, may decrease symptoms of hypoglycemia.

Sulfacytine: Sulfonamide/sulfonylurea: possible hypoglycemia

Sulfadiazine: Sulfonamide/sulfonylurea: possible hypoglycemia

Sulfadoxine: Sulfonamide/sulfonylurea: possible hypoglycemia

Sulfamerazine: Sulfonamide/sulfonylurea: possible hypoglycemia

Sulfamethazine: Sulfonamide/sulfonylurea: possible hypoglycemia

Sulfamethizole: Sulfonamide/sulfonylurea: possible hypoglycemia

Sulfamethoxazole: Sulfonamide/sulfonylurea: possible hypoglycemia

Sulfapyridine: Sulfonamide/sulfonylurea: possible hypoglycemia

Sulfasalazine: Sulfonamide/sulfonylurea: possible hypoglycemia

Sulfisoxazole: Sulfonamide/sulfonylurea: possible hypoglycemia

Timolol: The beta-blocker, timolol, may decrease symptoms of hypoglycemia.

Trisalicylate-choline: The salicylate, trisalicylate-choline, increases the effect of the sulfonylurea, chlorpropamide.

Voriconazole: Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).

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