Chlorpropamide


Concise Prescribing Info
Indications/Uses
Type 2 DM.
Dosage/Direction for Use
Adult : PO Initial: 250 mg/day in the morning. 5-7 days after treatment initiation, subsequent doses may be increased or decreased by 50-125 mg/day at intervals of 3-5 days until optimum therapeutic control is achieved. Maintenance: 100-500 mg/day.
Dosage Details
Oral
Type 2 diabetes mellitus
Adult: Initially, 250 mg daily as a single dose in the morning. 5-7 days after treatment initiation, subsequent doses may be increased or decreased by 50-125 mg daily at intervals of 3-5 days until optimum therapeutic control is achieved. Maintenance: 100-500 mg daily.
Elderly: Initial: 100-125 mg daily. 5-7 days after treatment initiation, subsequent doses may be increased or decreased by 50-125 mg daily at intervals of 3-5 days until optimum therapeutic control is achieved.
Renal Impairment
Severe: Contraindicated.
Hepatic Impairment
Severe: Contraindicated.
Administration
Should be taken with food.
Contraindications
Type 1 DM, diabetic ketoacidosis (w/ or w/o coma) or other acute complications (e.g. major surgery, severe infection or severe trauma), thyroid impairment. Severe hepatic and renal impairment.
Special Precautions
Hypersensitivity to sulfonamides. Patient w/ condition associated w/ fluid retention, G6PD deficiency. Mild to moderate hepatic and renal impairment. Elderly, debilitated and malnourished patients. Pregnancy and lactation.
Adverse Reactions
GI disturbances (e.g. anorexia, nausea, vomiting, epigastric discomfort, abdominal cramps, constipation, diarrhoea), vague neurologic symptoms (e.g. headache, weakness, paraesthesia), syndrome of inappropriate secretion of antidiuretic hormone, jaundice, skin eruptions, blood dyscrasias, pruritus, urticaria, maculopapular eruptions and photosensitivity reactions, porphyria cutanea tarda, leucopenia, thrombocytopenia, haemolytic anaemia, wt gain.
Potentially Fatal: Severe hypoglycaemia.
Patient Counseling Information
Adhere strictly to the prescribed diabetic diet.
MonitoringParameters
Monitor blood glucose, glycosylated Hb level, signs and symptoms of hypoglycaemia.
Overdosage
Symptoms: Hypoglycaemia. Management: Mild hypoglycaemic symptoms w/o loss of consciousness or neurologic findings may be treated w/ oral glucose and adjustments in drug dosage and/or meal patterns. For hypoglycaemic coma, admin rapid IV inj of concentrated (50%) glucose soln followed by continuous infusion of a more dilute (10%) glucose soln.
Drug Interactions
Diminished therapeutic effect w/ thiazide diuretics. Protein-bound drugs (e.g. oral anticoagulants, hydantoins, salicylates, other NSAIDs, sulfonamides) may potentiate hypoglycaemic action of chlorpropamide. Increased plasma concentrations w/ certain antifungals (e.g. miconazole, fluconazole).
Food Interaction
Concurrent alcohol use may cause disulfiram-like reaction.
Action
Description: Chlorpropamide stimulates the secretion of endogenous insulin from β-cells of the pancreas. It also exhibits antidiuretic activity by enhancing vasopressin in the renal tubules.
Onset: 1 hr.
Duration: 24 hr.
Pharmacokinetics:
Absorption: Readily absorbed from the GI tract. Time to peak plasma concentration: W/in 2-4 hr.
Distribution: It crosses the placenta and enters breast milk. Volume of distribution: 0.13-0.23 L/kg. Plasma protein binding: 90%.
Metabolism: Undergoes extensive hepatic metabolism (approx 80%) primarily by CYP2C9 isoenzyme.
Excretion: Via urine as metabolites and unchanged drug. Half-life: Approx 35 hr.
Chemical Structure

Chemical Structure Image
Chlorpropamide

Source: National Center for Biotechnology Information. PubChem Database. Chlorpropamide, CID=2727, https://pubchem.ncbi.nlm.nih.gov/compound/Chlorpropamide (accessed on Jan. 21, 2020)

Storage
Store between 20-25°C. Protect from light.
References
Anon. Chlorpropamide. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 15/08/2014.

Buckingham R (ed). Chlorpropamide. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 15/08/2014.

Chlorpropamide Tablet (Mylan Pharmaceuticals Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 15/08/2014.

Diabinese Tablets. U.S. FDA. https://www.fda.gov/. Accessed 15/08/2014.

McEvoy GK, Snow EK, Miller J et al (eds). Chlorpropamide. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 15/08/2014.

Disclaimer: This information is independently developed by MIMS based on Chlorpropamide from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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