Glibenclamide Other names: Glyburide

Chemical formula: C₂₃H₂₈ClN₃O₅S  Molecular mass: 494.004 g/mol  PubChem compound: 3488

Interactions

Glibenclamide interacts in the following cases:

Alcohol

In very rare cases, an intolerance to alcohol may occur. Both acute and chronic alcohol intake, or excessive alcohol ingestion by people who drink occasionally, may attenuate the hypoglycaemic effect of glibenclamide or dangerously potentiate it by delaying its metabolic inactivation. Disulfiram-like reactions have occurred very rarely following the concomitant use of alcohol and glibenclamide.

Mild to moderate renal impairment

Dose adjustment is required in patients with mild to moderate renal impairment. In those patients, treatment should be started at the lowest dose levels and should be strictly followed, to avoid hypoglycaemic reactions.

Mild to moderate hepatic impairment

Dose adjustment is required in patients with mild to moderate hepatic impairment. In those patients, treatment should be started at the lowest dose levels and should be strictly followed, to avoid hypoglycaemic reactions.

Η₂-receptor antagonists, clonidine, reserpine

H2-receptor antagonists, clonidine, and reserpine may lead to either potentiation or weakening of the blood-glucoselowering effect.

Drugs potentiating the blood-glucose lowering effect

Potentiation of the blood-glucose-lowering effect and, thus, in some instances hypoglycaemia may occur when taking other drugs, including:

Insulin and other, oral antidiabetics, ACE inhibitors, anabolic steroids and male sex hormones, chloramphenicol, coumarin derivatives, cyclophosphamide, disopyramide, fenfluramine, fenyramidol, fibrates, fluoxetine, ifosfamide, MAO inhibitors, miconazole, para-aminosalicyclic acid, pentoxifylline, phenylbutazone, azapropazone, oxyphenbutazone, probenecid, quinolones, salicylates, sulfinpyrazone, sulfonamides, sympatholytic agents such as beta-blockers and guanethidine, clarithromycin, tetracyclines, tritoqualine, trosfosfamide.

Coumarin derivatives

Glibenclamide may either potentiate or weaken the effect of coumarin derivatives.

Drugs weakening the blood-glucose lowering effect

Weakening of the blood-glucose-lowering effect and, thus, raised blood glucose levels may occur when taking other drugs, including:

Acetazolamide, barbiturates, corticosteroids, diazoxide, diuretics, epinephrine and other sympathomimetic agents, glucagon, laxatives, nicotinic acid, oestrogens and progestogens, phenothiazines, phenytoin, thyroid hormones, rifampicin.

Beta-blockers, clonidine, guanethidine, reserpine

Under the influence of sympatholytic medicinal products such as beta-blockers, clonidine, guanethidine, and reserpine, the signs of adrenergic counter-regulation to hypoglycaemia may be reduced or absent. The symptoms of hypoglycaemia may also be milder or absent where hypoglycaemia develops gradually or where there is autonomic neuropathy.

Ciclosporin

Glibenclamide may increase ciclosporin plasma concentration and potentially lead to its increased toxicity. Monitoring and dose adjustment of ciclosporin are therefore recommended when both medicinal products are co-administered.

Colesevelam

Colesevelam binds to glibenclamide and reduces glibenclamide absorption from the gastrointestinal tract. No interaction was observed when glibenclamide was taken at least 4 hours before colesevelam. Therefore, glibenclamide should be administered at least 4 hours prior to colesevelam.

G6PD deficiency

Treatment of patients with G-6-phosphate-dehydrogenase deficiency with sulfonylurea agents can lead to haemolytic anaemia. Since Glibesyn 5mg Tablets belongs to the class of sulfonylurea agents, caution should be used in patients with G-6-phosphate-dehydrogenase deficiency and a non-sulfonylurea alternative should be considered.

Allergy to sulphonamide derivatives

Persons allergic to other sulphonamide derivatives may develop an allergic reaction to glibenclamide as well.

Pregnancy

Glibesyn must not be taken during pregnancy. The patient must change over to insulin during pregnancy.

Based on a limited amount of published data, the use of glibenclamide during the first trimester does not seem to cause an increase in congenital malformations. With respect to the second and third trimester published data did not find fetotoxic effects. Animal studies do not indicate a teratogenic potential.

Glibenclamide crosses the placenta mostly in small amounts; however, transfer is highly variable among patients.

In pregnant women insulin is recommended for blood sugar control.

Nursing mothers

Glibesyn must not be taken by breast-feeding women. If necessary the patient must change over to insulin, or must stop breast-feeding.

Carcinogenesis, mutagenesis and fertility

Women of childbearing potential / Contraception

Women of childbearing potential planning a pregnancy should be switched from oral glibenclamide to insulin. Glibenclamide should not be given during pregnancy.

Fertility

Clinical data are not available.

Effects on ability to drive and use machines

Glibenclamide has moderate influence on the ability to drive and use machines since it may increase the risk of hypoglycaemia. This may not be relevant for the target population. However, reduced alertness may also be of concern when participating in road traffic (e.g. cycling) or in play (e.g. skateboarding).

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