Chemical: Drug
chlorpropamide

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Annotated Labels

  1. FDA Label for chlorpropamide and G6PD
  2. HCSC Label for chlorpropamide and G6PD



PharmGKB contains no Clinical Variants that meet the highest level of criteria.

Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

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Overview

Generic Names
  • chlorporpamide
Trade Names
  • 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
  • Insulase
  • Meldian
  • Melitase
  • Mellinese
  • Millinese
  • Novo-Propamide
  • Oradian
  • Stabinol
Brand Mixture Names

PharmGKB Accession Id

PA448966

Type(s):

Drug

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 beta 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 beta 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.

Source: Drug Bank

Indication

For treatment of NIDDM in conjunction with diet and exercise.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

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.

Source: Drug Bank

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.

Source: Drug Bank

Food Interaction

Take 30 minutes before meal.|Avoid alcohol.|Food reduces the rate of absorption.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

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.

Source: Drug Bank

Protein Binding

Highly bound to plasma proteins.

Source: Drug Bank

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.

Source: Drug Bank

Half-Life

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

Source: Drug Bank

Toxicity

IPN-RAT LD 50 580 mg/kg

Source: Drug Bank

Route of Elimination

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

Source: Drug Bank

Chemical Properties

Chemical Formula

C10H13ClN2O3S

Source: Drug Bank

Isomeric SMILES

CCCNC(=O)NS(=O)(=O)c1ccc(cc1)Cl

Source: OpenEye

Canonical SMILES

CCCNC(=O)NS(=O)(=O)C1=CC=C(Cl)C=C1

Source: Drug Bank

Average Molecular Weight

276.74

Source: Drug Bank

Monoisotopic Molecular Weight

276.033540689

Source: Drug Bank

SMILES

CCCNC(=O)NS(=O)(=O)C1=CC=C(Cl)C=C1

Source: Drug Bank

InChI String

InChI=1S/C10H13ClN2O3S/c1-2-7-12-10(14)13-17(15,16)9-5-3-8(11)4-6-9/h3-6H,2,7H2,1H3,(H2,12,13,14)

Source: Drug Bank

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Curated Information ?

Drug Targets

Gene Description
ABCC8 (source: Drug Bank )
KCNJ1 (source: Drug Bank )

Drug Interactions

Interaction Description
acebutolol - chlorpropamide Decreased in symptoms of hypoglycemia and increase in time required for the body to compensate for hypoglycemia (source: Drug Bank )
acebutolol - chlorpropamide Acebutolol may decrease symptoms of hypoglycemia and increase the time required for the body to compensate for hypoglycemia. (source: Drug Bank )
aspirin - chlorpropamide The salicylate increases the effect of sulfonylurea (source: Drug Bank )
aspirin - chlorpropamide Acetylsalicylic acid increases the effect of sulfonylurea, chlorpropamide. (source: Drug Bank )
atenolol - chlorpropamide The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank )
atenolol - chlorpropamide The beta-blocker, atenolol, may decrease symptoms of hypoglycemia. (source: Drug Bank )
bisoprolol - chlorpropamide The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank )
bisoprolol - chlorpropamide The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia. (source: Drug Bank )
carvedilol - chlorpropamide The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank )
carvedilol - chlorpropamide The beta-blocker, carvedilol, may decrease symptoms of hypoglycemia. (source: Drug Bank )
chloramphenicol - chlorpropamide The agent increases the effect of sulfonylurea (source: Drug Bank )
chloramphenicol - chlorpropamide The agent increases the effect of sulfonylurea (source: Drug Bank )
chlorpropamide - acebutolol The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank )
chlorpropamide - acebutolol The beta-blocker, acebutolol, may decrease symptoms of hypoglycemia. (source: Drug Bank )
chlorpropamide - aspirin The salicylate increases the effect of sulfonylurea (source: Drug Bank )
chlorpropamide - atenolol The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank )
chlorpropamide - atenolol The beta-blocker, atenolol, may decrease symptoms of hypoglycemia. (source: Drug Bank )
chlorpropamide - betaxolol The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank )
chlorpropamide - betaxolol The beta-blocker, betaxolol, may decrease symptoms of hypoglycemia. (source: Drug Bank )
chlorpropamide - bevantolol The beta-blocker, bevantolol, may decrease symptoms of hypoglycemia. (source: Drug Bank )
chlorpropamide - bisoprolol The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank )
chlorpropamide - bisoprolol The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia. (source: Drug Bank )
chlorpropamide - carteolol The beta-blocker, carteolol, may decrease symptoms of hypoglycemia. (source: Drug Bank )
chlorpropamide - carvedilol The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank )
chlorpropamide - carvedilol The beta-blocker, carvedilol, may decrease symptoms of hypoglycemia. (source: Drug Bank )
chlorpropamide - chloramphenicol The agent increases the effect of sulfonylurea (source: Drug Bank )
chlorpropamide - chloramphenicol The agent increases the effect of sulfonylurea (source: Drug Bank )
chlorpropamide - clofibrate The agent increases the effect of sulfonylurea (source: Drug Bank )
chlorpropamide - clofibrate The agent increases the effect of sulfonylurea (source: Drug Bank )
chlorpropamide - diazoxide Diazoxyde/sulfonylurea: antagonism of action (source: Drug Bank )
chlorpropamide - diazoxide Antagonism. (source: Drug Bank )
chlorpropamide - dicumarol The agent increase the effect of sulfonylurea (source: Drug Bank )
chlorpropamide - dicumarol The agent increase the effect of sulfonylurea (source: Drug Bank )
chlorpropamide - esmolol The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank )
chlorpropamide - esmolol The beta-blocker, esmolol, may decrease symptoms of hypoglycemia. (source: Drug Bank )
chlorpropamide - glucosamine Possible hyperglycemia (source: Drug Bank )
chlorpropamide - isocarboxazid The MAO inhibitor increases the effect of hypoglycemic agent (source: Drug Bank )
chlorpropamide - labetalol The beta-blocker, labetolol, may decrease symptoms of hypoglycemia. (source: Drug Bank )
chlorpropamide - metoprolol The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank )
chlorpropamide - metoprolol The beta-blocker, metoprolol, may decrease symptoms of hypoglycemia. (source: Drug Bank )
chlorpropamide - nadolol The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank )
chlorpropamide - nadolol The beta-blocker, nadolol, may decrease symptoms of hypoglycemia. (source: Drug Bank )
chlorpropamide - oxprenolol The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank )
chlorpropamide - oxprenolol The beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia. (source: Drug Bank )
chlorpropamide - penbutolol The beta-blocker, penbutolol, may decrease symptoms of hypoglycemia. (source: Drug Bank )
chlorpropamide - phenelzine The MAO inhibitor increases the effect of hypoglycemic agent (source: Drug Bank )
chlorpropamide - phenylbutazone Phenylbutazone increases the effect of the hypoglycemic agent (source: Drug Bank )
chlorpropamide - phenylbutazone Phenylbutazone increases the effect of the hypoglycemic agent (source: Drug Bank )
chlorpropamide - pindolol The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank )
chlorpropamide - pindolol The beta-blocker, pindolol, may decrease symptoms of hypoglycemia. (source: Drug Bank )
chlorpropamide - practolol The beta-blocker, practolol, may decrease symptoms of hypoglycemia. (source: Drug Bank )
chlorpropamide - propranolol The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank )
chlorpropamide - propranolol The beta-blocker, propranolol, may decrease symptoms of hypoglycemia. (source: Drug Bank )
chlorpropamide - repaglinide Similar mode of action-questionable association (source: Drug Bank )
chlorpropamide - rifampin Rifampin decreases the effect of sulfonylurea (source: Drug Bank )
chlorpropamide - rifampin Rifampin decreases the effect of sulfonylurea (source: Drug Bank )
chlorpropamide - salsalate The salicylate, salsalate, increases the effect of the sulfonylurea, chlorpropamide. (source: Drug Bank )
chlorpropamide - somatropin recombinant Somatropin may antagonize the hypoglycemic effect of chlorpropamide. Monitor for changes in fasting and postprandial blood sugars. (source: Drug Bank )
chlorpropamide - sotalol The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank )
chlorpropamide - sotalol The beta-blocker, sotalol, may decrease symptoms of hypoglycemia. (source: Drug Bank )
chlorpropamide - sulfacytine Sulfonamide/sulfonylurea: possible hypoglycemia (source: Drug Bank )
chlorpropamide - sulfadiazine Sulfonamide/sulfonylurea: possible hypoglycemia (source: Drug Bank )
chlorpropamide - sulfadiazine Sulfonamide/sulfonylurea: possible hypoglycemia (source: Drug Bank )
chlorpropamide - sulfadoxine Sulfonamide/sulfonylurea: possible hypoglycemia (source: Drug Bank )
chlorpropamide - sulfadoxine Sulfonamide/sulfonylurea: possible hypoglycemia (source: Drug Bank )
chlorpropamide - sulfamerazine Sulfonamide/sulfonylurea: possible hypoglycemia (source: Drug Bank )
chlorpropamide - sulfamethazine Sulfonamide/sulfonylurea: possible hypoglycemia (source: Drug Bank )
chlorpropamide - sulfamethazine Sulfonamide/sulfonylurea: possible hypoglycemia (source: Drug Bank )
chlorpropamide - sulfamethizole Sulfonamide/sulfonylurea: possible hypoglycemia (source: Drug Bank )
chlorpropamide - sulfamethoxazole Sulfonamide/sulfonylurea: possible hypoglycemia (source: Drug Bank )
chlorpropamide - sulfamethoxazole Sulfonamide/sulfonylurea: possible hypoglycemia (source: Drug Bank )
chlorpropamide - sulfapyridine Sulfonamide/sulfonylurea: possible hypoglycemia (source: Drug Bank )
chlorpropamide - sulfasalazine Sulfonamide/sulfonylurea: possible hypoglycemia (source: Drug Bank )
chlorpropamide - sulfasalazine Sulfonamide/sulfonylurea: possible hypoglycemia (source: Drug Bank )
chlorpropamide - sulfisoxazole Sulfonamide/sulfonylurea: possible hypoglycemia (source: Drug Bank )
chlorpropamide - timolol The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank )
chlorpropamide - timolol The beta-blocker, timolol, may decrease symptoms of hypoglycemia. (source: Drug Bank )
chlorpropamide - tranylcypromine The MAO inhibitor increases the effect of hypoglycemic agent (source: Drug Bank )
chlorpropamide - trisalicylate-choline The salicylate, trisalicylate-choline, increases the effect of the sulfonylurea, chlorpropamide. (source: Drug Bank )
clofibrate - chlorpropamide The agent increases the effect of sulfonylurea (source: Drug Bank )
clofibrate - chlorpropamide The agent increases the effect of sulfonylurea (source: Drug Bank )
esmolol - chlorpropamide The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank )
esmolol - chlorpropamide The beta-blocker, esmolol, may decrease symptoms of hypoglycemia. (source: Drug Bank )
isocarboxazid - chlorpropamide The MAO inhibitor increases the effect of hypoglycemic agent (source: Drug Bank )
labetalol - chlorpropamide The beta-blocker, labetalol, may decrease symptoms of hypoglycemia. (source: Drug Bank )
metoprolol - chlorpropamide The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank )
metoprolol - chlorpropamide The beta-blocker, metoprolol, may decrease symptoms of hypoglycemia. (source: Drug Bank )
nadolol - chlorpropamide The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank )
nadolol - chlorpropamide The beta-blocker, nadolol, may decrease symptoms of hypoglycemia. (source: Drug Bank )
oxprenolol - chlorpropamide The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank )
oxprenolol - chlorpropamide The beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia. (source: Drug Bank )
phenelzine - chlorpropamide The MAO inhibitor increases the effect of the hypoglycemic agent (source: Drug Bank )
phenylbutazone - chlorpropamide Phenylbutazone increases the effect of the hypoglycemic agent (source: Drug Bank )
phenylbutazone - chlorpropamide Phenylbutazone increases the effect of the hypoglycemic agent (source: Drug Bank )
pindolol - chlorpropamide The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank )
pindolol - chlorpropamide The beta-blocker, pindolol, may decrease symptoms of hypoglycemia. (source: Drug Bank )
propranolol - chlorpropamide The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank )
propranolol - chlorpropamide The beta-blocker, propranolol, may decrease symptoms of hypoglycemia. (source: Drug Bank )
repaglinide - chlorpropamide Similar mode of action - questionable association (source: Drug Bank )
rifampin - chlorpropamide Rifampin decreases the effect of sulfonylurea (source: Drug Bank )
rifampin - chlorpropamide Rifampin decreases the effect of sulfonylurea (source: Drug Bank )
timolol - chlorpropamide The beta-blocker decreases the symptoms of hypoglycemia (source: Drug Bank )
timolol - chlorpropamide The beta-blocker, timolol, may decrease symptoms of hypoglycemia. (source: Drug Bank )
voriconazole - chlorpropamide Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP). (source: Drug Bank )

Curated Information ?

Relationships from National Drug File - Reference Terminology (NDF-RT)

May Treat
Contraindicated With

Publications related to chlorpropamide: 1

No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Pharmacogenetics of glucose-lowering drug treatment: a systematic review. Molecular diagnosis & therapy. 2007. Bozkurt Ozlem, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
0378-0197-01
DrugBank:
DB00672
ChEBI:
3650
KEGG Drug:
D00271
PubChem Compound:
2727
PubChem Substance:
150222
46506402
Drugs Product Database (DPD):
156728
ChemSpider:
2626
Therapeutic Targets Database:
DAP000923
FDA Drug Label at DailyMed:
baa54287-8065-da1a-f19e-ce8daf61bd01

Clinical Trials

These are trials that mention chlorpropamide and are related to either pharmacogenetics or pharmacogenomics.

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NURSA Datasets

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No NURSA datasets available.

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