Chlorpropamide


Thông tin thuốc gốc
Chỉ định và Liều dùng
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.
Cách dùng
Should be taken with food.
Chống chỉ định
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.
Thận trọng
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.
Phản ứng phụ
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.
Thông tin tư vấn bệnh nhân
Adhere strictly to the prescribed diabetic diet.
MonitoringParameters
Monitor blood glucose, glycosylated Hb level, signs and symptoms of hypoglycaemia.
Quá liều
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.
Tương tác
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.
Tác dụng
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.
Đặc tính

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)

Bảo quản
Store between 20-25°C. Protect from light.
Phân loại MIMS
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.

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