Actions and Spectrum:

The action of chlorpropamide inhibits the secretion of the alpha-glucosidase enzyme in the small intestine’s brush border. By inhibiting alpha-glucosidase, chlorpropamide slows the absorption of carbohydrates from the gut. It leads to a reduction in postprandial hyperglycemia.

DRUG INTERACTION

Contraindicated  

Serious Use Alternative  

Monitor Closely  

Minor  

Frequency Not Defined:

Hypoglycemia

Headache

Dizziness

Anorexia

Liver failure

Aplastic anemia

Nausea

Vomiting

Disulfiram-reactions

Blood dyscrasias

Dermatologic reactions

Black Box Warning:

It is essential to follow the dosage and administration instructions for the medication carefully.

Contraindication/Caution:

Patients with type 1 diabetes show contraindications for chlorpropamide. It is also contraindicated in patients with severe renal or hepatic impairment, as these patients may be at increased risk for adverse effects from the drug.

chlorpropamide should be used with caution in elderly patients.

Pregnancy consideration:

Category C.

Breastfeeding warnings:

The excretion of the drug in breast milk is unknown.

Pregnancy category:

Category A: well-controlled and Satisfactory studies do not show risk to the fetus in the first/later trimester.

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.

Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.

Category N: No data is available for the drug under this category.

Pharmacology

chlorpropamide is a sulfonylurea antidiabetic drug. It is used to lower blood sugar levels in people with type 2 diabetes. It is a first-generation sulfonylurea. It has been used for an extended period and is generally less potent than newer second-generation sulfonylureas. Such as glipizide and glimepiride.

Pharmacodynamics:

It stimulates the release of insulin from the pancreas, which reduces blood glucose levels. Chlorpropamide also increases insulin sensitivity and slows glucose absorption from the gastrointestinal tract. Its effects last for approximately 24 hours.

Pharmacokinetics:

Pharmacokinetics studies how a drug is absorbed, distributed, metabolized, and eliminated by the body. The following parameters can describe the pharmacokinetics of chlorpropamide.

Absorption

chlorpropamide is well absorbed after oral administration and reaches maximum plasma concentrations within 2-4 hours.

Distribution

chlorpropamide has a low protein binding affinity and is widely distributed in the body. Metabolism

It is metabolized in the liver by CYP2C9 and has a half-life of approximately 40 hours.

Elimination and excretion

The drug is excreted in the urine, primarily as its metabolites.

Administration:

chlorpropamide is administered orally, typically taken as a tablet, once daily with a meal. The dosage is adjusted based on the patient’s blood glucose levels and response to treatment.

It is essential to monitor blood glucose regularly and adjust the dose as necessary to prevent hypoglycemia. Following a balanced diet and regular exercise while taking chlorpropamide is also essential.

Patient information leaflet

Generic Name: chlorpropamide.

Pronounced: klor-proe-pa-mide

Why do we use chlorpropamide?

chlorpropamide is used to treat type 2 diabetes.