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Chlorpropamide information from DrugsUpdate  

See Available Brands of Chlorpropamide in India

P - Caution when used during pregnancy
L - Caution when used during lactation
FI - Food *

Chlorpropamide is a drug in the sulphonylurea class used to treat type 2 diabetes mellitus. It is a long-acting sulphonylurea. It has more side effects than other sulphonylureas and its use is no longer recommended.

Pharmacodynamics

Pharmacokinetics

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.


Duration
24 hours.

Absorption
Readily absorbed from the GI tract (oral).

Distribution
Crosses the placenta; enters breast milk. Protein-binding: Extensive.

Metabolism
Hepatic (80%).


Excretion
Urine (as metabolites and unchanged drug); 35 hours (elimination half-life).

Chlorpropamide Indications / Chlorpropamide Uses

Information Not Available

Chlorpropamide Adverse Reactions / Chlorpropamide Side Effects

GI disturbances; hypoglycaemia; cholestatic jaundice; agranulocytosis, lymphocytosis, thrombocytopenia, aplastic anaemia, haemolytic anaemia; nausea, vomiting, epigastric pain; weakness, paraesthesia, headache and sensitivity reactions, syndrome of inappropriate anti-diuretic hormone secretion.


Potentially Fatal: Hypoglycaemia especially in elderly with renal or hepatic disease.

Precautions

General

Macrovascular Outcomes
There have been no clinical studies establishing conclusive evidence of macrovascular risk reduction with Chlorpropamide or any other antidiabetic drug.

Hypoglycemia
All sulfonylurea drugs including Chlorpropamide are capable of producing severe hypoglycemia, which may result in coma, and may require hospitalization. Patients experiencing hypoglycemia should be managed with appropriate glucose therapy and be monitored for a minimum of 24 to 48 hours. Proper patient selection, dosage, and instructions are important to avoid hypoglycemic episodes. Regular, timely carbohydrate intake is important to avoid hypoglycemic events occurring when a meal is delayed or insufficient food is eaten or carbohydrate intake is unbalanced. Renal or hepatic insufficiency may affect the disposition of Chlorpropamide and may also diminish gluconeogenic capacity, both of which increase the risk of serious hypoglycemic reactions.

Elderly, debilitated or malnourished patients, and those with adrenal or pituitary insufficiency are particularly susceptible to the hypoglycemic action of glucose-lowering drugs. Hypoglycemia may be difficult to recognize in the elderly, and in people who are taking beta-adrenergic blocking drugs. Hypoglycemia is more likely to occur when caloric intake is deficient, after severe or prolonged exercise, when alcohol is ingested, or when more than one glucose-lowering drug is used.
Because of the long half-life of Chlorpropamide, patients who become hypoglycemic during therapy require careful supervision of the dose and frequent feedings for at least 3 to 5 days. Hospitalization and intravenous glucose may be necessary.

Loss of Control of Blood Glucose
When a patient stabilized on any diabetic regimen is exposed to stress such as fever, trauma, infection, or surgery, a loss of control may occur. At such times, it may be necessary to discontinue Chlorpropamide and administer insulin.
The effectiveness of any oral hypoglycemic drug, including Chlorpropamide, in lowering blood glucose to a desired level decreases in many patients over a period of time, which may be due to progression of the severity of the diabetes or to diminished responsiveness to the drug. This phenomenon is known as secondary failure, to distinguish it from primary failure in which the drug is ineffective in an individual patient when first given. Adequate adjustment of dose and adherence to diet should be assessed before classifying a patient as a secondary failure.

Geriatric Use
The safety and effectiveness of Chlorpropamide in patients aged 65 and over has not been properly evaluated in clinical studies. Adverse event reporting suggests that elderly patients may be more prone to developing hypoglycemia and/or hyponatremia when using Chlorpropamide. Although the underlying mechanisms are unknown, abnormal renal function, drug interaction and poor nutrition appear to contribute to these events.

Hemolytic Anemia
Treatment of patients with glucose 6-phosphate dehydrogenase (G6PD) deficiency with sulfonylurea agents can lead to hemolytic anemia. Because Chlorpropamide belongs to the class of sulfonylurea agents, caution should be used in patients with G6PD deficiency and a non-sulfonylurea alternative should be considered. In post-marketing reports, hemolytic anemia has also been reported in patients who did not have known G6PD deficiency.

Special Precautions

May cause intolerance to alcohol; higher risk of hypoglycemia in patients who are malnourished, elderly, patients with adrenal or pituitary insufficiency, taking more than one glucose-lowering drug, on β-adrenergic blockers or after prolonged period of exercise. Pregnancy and lactation.

Other Drug Interactions

Abrupt withdrawal of phenobarbital or rifampicin may result in hypoglycaemia. Clofibrate potentiates chlorpropamide action. Probenecid decreases excretion. Alcohol impairs recovery from chlorpropamide-induced hypoglycaemia. Facial flushing with alcohol ingestion.


Potentially Fatal: Phenylbutazone, large doses of salicylates and coumarins potentiate the action of chlorpropamide. Chloramphenicol, in large doses, reduces urinary excretion. Thiazide diuretics reduce insulin release. Phenytoin and verapamil also reduce insulin release. Corticosteroids are potent antagonists of insulin and lead to marked deterioration in glucose tolerance. Oral contraceptives also antagonise insulin action. β-blockers lead to mild deterioration in glucose tolerance.

Other Interactions

Food Interactions: Absorption delayed but bioavailability not affected.

Dosage

Oral Type 2 diabetes mellitus
Adult: Initially, 250 mg daily as a single dose in the morning. Subsequent doses may be changed by 50-125 mg at intervals of 3-5 days.
Maintenance: 100-500 mg daily.
Max dose: 750 mg daily. Max Dosage: Oral

Cranial diabetes insipidus
Adult: Initially, 100 mg daily increased if necessary. Max dose: 350-500 mg daily.

Food(before/after)

Should be taken with food

List of Contraindications

Chlorpropamide and Pregnancy

Caution when used during pregnancy


Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Chlorpropamide and Lactation

Caution when used during lactation

Chlorpropamide and Children

Information Not Available

Chlorpropamide and Geriatic

Information Not Available

Chlorpropamide and Other Contraindications

Type 1 DM, ketoacidosis, diabetic coma, severe infections or trauma. Renal, thyroid or hepatic impairment, porphyria.

Storage

Information Not Available

Lab interference

Information Not Available

Chlorpropamide brands in India:

Chlorformin Copamide

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