Glibenclamidum

General characteristics. Structure:

Active ingredient: 5 mg of Glibenclamidum.

Drug the reducing glucose level in blood.

Pharmacological properties:

Pharmacodynamics. Glibenclamidum has hypoglycemic effect.

Specifically stimulates beta cells of the insular device, strengthens insulin secretion by a pancreas. Activity is shown preferential at kept insulin - synthetic function of a pancreas. Recovers physiological sensitivity of beta cells to a glycemia. Exponentiates effect of insulin (endogenous and exogenous) as increases number of receptors to insulin, improves insulin - receptor interaction and recovers transduction of a post-receptor signal.

Increase in concentration of insulin in plasma and lowering of the level of glucose occur gradually that reduces risk of emergence of hypoglycemic states. Increases sensitivity of insulin receptors to insulin in peripheral fabrics and causes extra pancreatic effects. Increases utilization of glucose in a liver and muscles, stimulates formation of a glycogen in them. Favorably influences exchange processes, reduces the content in plasma of not esterified fatty acids. Has antidiuretic effect, lowers thrombogenic properties of blood.

Action develops in 2 h after reception, reaches a maximum in 7-8 h and continues 8-12 h.

Pharmacokinetics. It is quickly and almost completely absorbed from digestive tract. Cmax after a single dose is reached in 1-2 h. Contacts proteins of plasma for 99%. Practically does not get through a placental barrier. The elimination half-life is equal to 4-11 h. In a liver completely turns into two inactive metabolites (approximately equal quantities are formed), one of which is excreted with urine, and the second is brought with bile.

Indications to use:

Glibenclamidum is applied at a moderately severe diabetes mellitus, preferential at patients 40 years with an excess weight at which it is not possible to normalize disbolism one diet are more senior; at primary or secondary resistance to other streptocides having hypoglycemic properties; the patient receiving insulin to 30 PIECES a day for the purpose of the best normalization of carbohydrate metabolism, and at an opportunity and for an insulin dose decline.

Glibenclamidum can be appointed also in a combination with guanyl guanidines or insulin.

Route of administration and doses:

Medicine is appointed inside by 1-3 times a day in 20-30 minutes prior to food. The initial dose is selected individually. The size of a dose depends on age, weight of a current of a diabetes mellitus, concentration of glucose of blood on an empty stomach and in 2 h after food. The initial dose at elderly patients makes 1 mg (1/5 tablets) a day.

The average daily dose fluctuates from 2,5 (1/2 tablets) to 15 mg (3 tablets). Doses more than 15 mg a day do not increase expressiveness of hypoglycemic effect. In the absence of compensation of a diabetes mellitus within 4-6 weeks it is necessary to resolve an issue of carrying out a combination therapy with guanyl guanidines or insulin.

When replacing hypoglycemic medicines with similar type of action Glibenclamidum is appointed according to the scheme which is stated above, and the previous drug is cancelled at once. When replacing guanyl guanidines the initial daily dose of Glibenclamidum makes 2,5 mg (1/2 tablets), if necessary the daily dose increases each 5-6 days by 2,5 mg (1/2 tablets) before achievement of compensation.

Features of use:

The use of food is obligatory no later than in 1 h after administration of drug. During therapy regular control of content of glucose in blood and urine is necessary. At a physical and emotional overstrain, change of a diet drug dose adjustment is necessary.

At treatment by Glibenclamidum the refusal of alcohol intake (disulfiramopodobny reaction and the expressed hypoglycemia is possible), long stay in the sun is obligatory.

Clinical manifestations of a hypoglycemia can mask at reception of beta adrenoblockers, a clonidine, Reserpinum, guanetidin.

Influence on ability to drive the car and potentially dangerous mechanisms: during treatment it is necessary to be careful during the driving of motor transport and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

From a nervous system and sense bodys: headache, dizziness, change of flavoring feelings.

From bodies of digestive tract: abnormal liver function, cholestasia, dyspepsia.

From bodies of a hemopoiesis and system of a hemostasis: seldom – thrombocytopenia, hypoplastic or hemolitic anemia, a leukopenia, an eosinophilia, an agranulocytosis, a pancytopenia.

Allergic reactions: skin rashes, itch.

Others: hypoglycemia, proteinuria, late skin porphyria, fever, arthralgia, polyuria, increase in body weight, photosensitization.

Interaction with other medicines:

Drug is synergist of indirect anticoagulants.

The means acidifying urine (ammonium chloride, Calcii chloridum, ascorbic acid in high doses) strengthen effect of glibenclamide.

Antifungal means of systemic action (derivatives of azoles), ftorkhinolona, tetracyclines, chloramphenicol, H2 blockers, beta adrenoblockers, inhibitors of an angiotensin-converting enzyme, non-steroidal anti-inflammatory drugs, monoamine oxidase inhibitors, Clofibratum, безафибрат, пробенецид, paracetamol, Etioniamidum, anabolic steroids, пентоксифиллин, Allopyrinolum, cyclophosphamide, Reserpinum, streptocides, insulin exponentiate a hypoglycemia.

Barbiturates, fenotiazina, diazoxide, glucocorticoid and thyroid hormones, estrogen, gestagena, glucagon, adrenomimetichesky drugs, the lithium salts derivative of niacin and saluretics weaken hypoglycemic effect. Rifampicin accelerates an inactivation and lowers efficiency of Glibenclamidum.

Contraindications:

Hypersensitivity (including to sulfanamide drugs, thiazide diuretics), diabetic prekomatozny and coma, ketoacidosis, extensive burns, surgical interventions and injuries, intestinal impassability, stomach paresis, heavy disturbances of microcirculation, the expressed abnormal liver functions and/or kidneys, a leukopenia, a diabetes mellitus of type 1, pregnancy, feeding by a breast, the states which are followed by disturbance of absorption of food, development of a hypoglycemia (including infectious diseases).

Overdose:

Symptoms: a hypoglycemia (feeling of hunger, the increased sweating, sharp weakness, heartbeat, a tremor, uneasiness, a headache, dizziness, sleeplessness, irritability, a depression, wet brain, disturbance of the speech and sight, consciousness disturbance), a hypoglycemic coma.

Treatment: if the patient in consciousness – to accept sugar inside, at a loss of consciousness – introduction of 50% of solution of glucose (50 ml intravenously and inside), continuous intravenous infusion of 5-10% of solution of glucose, intramuscular introduction of a glucagon of 1-2 mg, diazoxide inside on 200 mg each 4 h or 30 mg intravenously within 30 minutes, monitoring of level of a glycemia. At wet brain the mannitol and dexamethasone are shown.

Issue conditions:

According to the recipe

Packaging:

Tablets on 5 mg No. 50 in a blister strip packaging 10x5 or in bank.