International generic name
Drug form and composition
Tablets. One tablet contains 5 mg Glibenclamide.
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.
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.
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
The most frequent side effect is hypoglycemia with CNS manifestations. Very rare
may appear skin allergy reactions, photosensibility, gastrointestinal disorders,
and vasomotor disorders.
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
30 tablets of 5 mg.