Glibenclamide Pharmacology

Glibenclamide

About Glibenclamide
Second generation sulfonylurea, Oral anti-diabetic.
Mechanism of Action of Glibenclamide
The drug exerts it`s action by increasing insulin release from the pancreas and by improving glucose tolerance. It acts on the "sulfonylurea receptors" on pancreatic ?-cell membrane and reduces conductance of ATP sensitive K+ channels and thus causes depolarization. This enhances Ca2+ influx and degranultion and thus increases insulin secretion rate at any glucose concentration. It primarily increases 2nd phase insulin secretion and has little effect on 1st phase. It also slows hepatic degradation of insulin and minor action of reducing glucagon release and increasing Somatostatin release. It also exerts extrapancreatic action; by sensitizing the target tissues such as liver to insulin action. It increases the number of insulin receptors and through a post receptor action improving translation of receptor activation.
Pharmacokinets of Glibenclamide
Absorption: Well absorbed orally
Distribution: Distributed in a protein bound form
Metabolism: Completely metabolized in to inactive metabolites in liver
Excretion: Excreted through urine and faeces as metabolites.
Onset of Action for Glibenclamide
30 to 60 minutes
Duration of Action for Glibenclamide
18 to 24 hours
Half Life of Glibenclamide
4 to 6 hours
Side Effects of Glibenclamide
1. Hypoglycemia
2. Nausea
3. Vomiting
4. Diarrhoea
5. Constipation
6. Headache
7. Presthesia
8. Weight gain
9. Hypersensitivity reactions
10. Rashes
11. Photosensitivity
12. Purpura
13. Transient leucopenia
14. Agranulocytosis
Contra-indications of Glibenclamide
1. Hypersensitivity to the drug
2. Diabetic ketoacidosis
3. Diabetic coma
4. Renal impairment
Special Precautions while taking Glibenclamide
1. Hepatic impairment
2. Malnourished and deliberate individuals
3. Strenous exercise and irregular meals may leads to hypoglycemia
Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
Contraindicated
Indications for Glibenclamide
1. Non insulin dependent diabetes mellitus.
Interactions for Glibenclamide
Hypoglycaemic effect of glibenclamide is enhanced by: Anticoagulants, Androgens, Chloramphenicol, Clofibrate, Fenfluramine, Fluconazole, Gemfibrozil, Histamine H2 antagonists, Magnesium Salts, Methyldopa, MAOIs, Phenylbutazone, Probenecid, Salicylates, Sulfinpyrazone, Sulfonamides, TCAs, & Urinary acidifiers.
Hypoglycemic effect of glibenclamide inhibited by the following drugs: Beta-blockers, Cholestyramine, Diazoxide, Hydantoins, Rifampicin, Thiazide diuretics & Urinary alkalisers.
Charcoal: Reduces the absorption of glibenclamide thus reducing its efficacy or toxicity.
Digitalis glycosides: Co-administration results in increased digitalis serum levels.

Typical Dosage for Glibenclamide
Oral: Starts with 2.5mg once daily with breakfast. Adjust the dosage by increments of 2.5mg daily.
Maximum dose: 15mg/day
Maintenance dosage: 1.25 to 15mg once daily with breakfast or in divided doses; if gastrointestinal disturbances occur.
Schedule of Glibenclamide
G
Storage Requirements for Glibenclamide
Store at room temperature below 25 degree C.in a well closed container. Protect from light. Keep out of reach of children.
Effects of Missed Dosage of Glibenclamide
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.
Effects of Overdose of Glibenclamide
Mild hypoglycemia can be treated with oral glucose and dosage adjustment. If there is loss of consciousness or neurological findings the patient should receive rapid injection of dextrose 50%; followed by continuous infusion of dextrose 10% at a rate to maintain blood glucose levels greater than 100mg/dl. Monitor patient for 24 to 48 hours.

Home Delivery for Glibenclamide in Your City

Medicine India is just a publishing medium for medicine related information and does not provide services or sales of medicines including glibenclamide.

However, we do publish a comprehensive directory of Pharmacies, Chemists and Druggists in cities all over India. You can use this directory to find the medicine stores in your city (or area) that provide home delivery services for glibenclamide and other medicines and health products. Home delivery services for glibenclamide may be free or they may cost you depending on the pharmacy and the minimum order requirements. It would be best to get this clarified while placing the order.

Please be aware that you should take glibenclamide only if a doctor has recommended or prescribed it. Some or all pharmacies who provide a home delivery service for medicines might insist on a prescription for glibenclamide before they complete the sale. You can get this information while placing the order for glibenclamide with the pharmacy.

Glibenclamide is a generic medicine name and there are several brands available for it. Some of the brands for glibenclamide might be better known than glibenclamide itself. If the pharmacy that's willing to deliver medicines to your home doesn't have glibenclamide in stock, you can ask for one of the branded alternatives for glibenclamide.