Product Information
Registration Status: ActiveANTI-D TABLET 250mg is approved to be sold in Singapore with effective from 1990-03-28. It is marketed by BEACONS PHARMACEUTICALS PTE LTD, with the registration number of SIN04087P.
This product contains Chlorpropamide 250mg in the form of TABLET. It is approved for ORAL use.
This product is manufactured by BEACONS PHARMACEUTICALS PTE LTD in SINGAPORE.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
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.
Indication
For treatment of NIDDM in conjunction with diet and exercise.
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.
Pharmacokinetics
- 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.
- Distribution
- Metabolism
- 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.
- Elimination
Toxicity
IPN-RAT LD50 580 mg/kg
Active Ingredient/Synonyms
1-(P-Chlorobenzenesulfonyl)-3-propylurea | 1-(P-Chlorophenylsulfonyl)-3-propylurea | 1-Propyl-3-(P-chlorobenzenesulfonyl)urea | 4-chloro-N-((Propylamino)carbonyl)benzenesulfonamide | 4-chloro-N-[(Propylamino)carbonyl]benzenesulfonamide | Chlorpropamid | Chlorpropamide | Chlorpropamidum | Clorpropamida | N-(4-Chlorophenylsulfonyl)-n'-propylurea | N-(P-Chlorobenzenesulfonyl)-n'-propylurea | N-Propyl-n'-(P-chlorobenzenesulfonyl)urea | N-Propyl-n'-P-chlorophenylsulfonylcarbamide | Chlorpropamide |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.