Chlorpropamid

Chlorpropamid Uses, Dosage, Side Effects, Food Interaction and all others data.

Chlorpropamid 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 β 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 β 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. Chlorpropamid 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.

Chlorpropamid, a second-generation sulfonylurea antidiabetic agent, is used with diet to lower blood glucose levels in patients with diabetes mellitus type II. Chlorpropamid is twice as potent as the related second-generation agent glipizide.

Chlorpropamid
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Chlorpropamid
Availability	Discontinued
Generic	Chlorpropamide
Chlorpropamide Other Names	Chlorpropamid, Chlorpropamide, Chlorpropamidum, Clorpropamida
Related Drugs	Farxiga, metformin, Trulicity, Lantus, Victoza, Tresiba, Levemir
Type
Formula	C₁₀H₁₃ClN₂O₃S
Weight	Average: 276.74 Monoisotopic: 276.033540689
Protein binding	Highly bound to plasma proteins.
Groups	Approved, Investigational
Therapeutic Class
Manufacturer
Available Country
Last Updated:	September 19, 2023 at 7:00 am

Uses

Chlorpropamid is a sulfonylurea used in the treatment of non insulin dependent diabetes mellitus.

For treatment of NIDDM in conjunction with diet and exercise.

Chlorpropamid is also used to associated treatment for these conditions: Diabetes Insipidus, Type 2 Diabetes Mellitus

How Chlorpropamid works

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.

Toxicity

IPN-RAT LD₅₀ 580 mg/kg

Food Interaction

Avoid alcohol.
Take before a meal. Take 30 minutes before a meal.
Take on an empty stomach. Food decreases the rate of absorption.

[Moderate] GENERALLY AVOID: Alcohol may cause hypoglycemia or hyperglycemia in patients with diabetes.

Hypoglycemia most frequently occurs during acute consumption of alcohol.

Even modest amounts can lower blood sugar significantly, especially when the alcohol is ingested on an empty stomach or following exercise.

The mechanism involves inhibition of both gluconeogenesis as well as the counter-regulatory response to hypoglycemia.

Episodes of hypoglycemia may last for 8 to 12 hours after ethanol ingestion.

By contrast, chronic alcohol abuse can cause impaired glucose tolerance and hyperglycemia.

Moderate alcohol consumption generally does not affect blood glucose levels in patients with well controlled diabetes.

A disulfiram-like reaction (e.g., flushing, headache, and nausea) to alcohol has been reported frequently with the use of chlorpropamide and very rarely with other sulfonylureas.

MANAGEMENT: Patients with diabetes should avoid consuming alcohol if their blood glucose is not well controlled, or if they have hypertriglyceridemia, neuropathy, or pancreatitis.

Patients with well controlled diabetes should limit their alcohol intake to one drink daily for women and two drinks daily for men (1 drink = 5 oz wine, 12 oz beer, or 1.5 oz distilled spirits) in conjunction with their normal meal plan.

Alcohol should not be consumed on an empty stomach or following exercise.

Chlorpropamid Drug Interaction

Moderate: fluticasone / salmeterol, fluticasone / salmeterol, carvedilol, carvedilolMinor: esomeprazole, esomeprazoleUnknown: amoxicillin / clavulanate, amoxicillin / clavulanate, raloxifene, raloxifene, atorvastatin, atorvastatin, acetaminophen, acetaminophen, montelukast, montelukast, tiotropium, tiotropium, ampicillin / sulbactam, ampicillin / sulbactam

Chlorpropamid Disease Interaction

Major: cardiovascular risk, DKA, renal/liver diseaseModerate: hypoglycemia, G6PD deficiency, hyponatremia

Elimination Route

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.