International generic name

Glibenclamide

Drug form and composition

Tablets. One tablet contains 5 mg Glibenclamide.

Indications

Insulin-dependent diabetes in adults with partially preserved synthesis of insulin. In patients with resistance to other antidiabetic medicines.

Dosage and administration

The doctor defines the dose individually. Usually the treatment begins with low doses (2.5 mg), given in the morning, whereas ones weekly the serum glucose profile is monitored. In case of insufficient effect the daily dose is increased up to 5-10 mg daily, taken once or in two parts, after nutrition. Maximal dose should not exceed 15 mg /24 hours.

Contraindications

Insulin-dependent diabetes; diabetic ketoacidosis; pregnancy; patients with severe renal and liver dysfunction; registered individual hypersensitivity to Glibenclamid.

Special warnings and precautions

In elderly patients with hepatal and renal failure Glibenclamid should be administered with care, in order to prevent severe hypoglycemia. During the treatment alcohol consumption should be avoided; otherwise the risk of hypoglycemia exists. As the Glibenclamid is excreted in the mother milk, the breastfeeding should be discontinued.

Drug interactions

In concomitant administration of β-blockers, H2-blockers, cumarin derivatives, sulphonamides, tetracycline, salicylates, chloramphenicol, clofibrate, and MAO-inhibitors the hypoglycemic effect of the Glibenclamid is increased. Glibenclamid potentiates the anticoagulant effect of warfarin. Corticosteroids, phenothiazines, estrogen and gestegen hormones, and oral contraceptives cause a decrease of the Glibemclamid effects.

Adverse reactions

The most frequent side effect is hypoglycemia with CNS manifestations. Very rare may appear skin allergy reactions, photosensibility, gastrointestinal disorders, and vasomotor disorders.

Pharmacological mechanisms

The main effect of the SUP (including Glibenclamid) is increasing of the β-cell insulin release as a response to the serum glucose level. Glibenclamid is bound to the surface receptors of the β-cell membrane, inhibiting ATP-sensitive potassium channels and causing depolarization of the cell membrane. Depolarization leads to potassium channel opening, which enables extracellular calcium to enter the cell. Increased intracellular calcium concentration enhances the bounding of calcium to the transport protein calmodulin. This leads to microfilament contraction and release of insulin-containing granules. Increased insulin secretion cause consequent reduction of the serum glucose, which improves β-cell sensitivity to glucose and potentiates insulin secretion.

Supplied

30 tablets of 5 mg.

Expiry

3 years.