Glimepirid

General characteristics. Structure:

Active ingredient: 1 mg, 2 mg, 3 mg, 4 mg or 6 mg of a glimepirid.

Excipients: lactoses monohydrate, cellulose microcrystallic, sodium carboxymethylstarch, povidone, polysorbate, magnesium stearate.

The drug reducing glucose level in blood.

Pharmacological properties:

Pharmacodynamics. Peroral hypoglycemic means derivative of sulphonylurea. Stimulates insulin secretion with pancreas β-cells, increases insulin release. Increases sensitivity of peripheral fabrics to insulin.

Pharmacokinetics. At multiple dose inside in a dose of 4 mg/days of Cmax in blood serum it is reached approximately in 2.5 h and makes 309 ng/ml; there is a linear dependence between a dose and Cmax, and also between a dose and AUC. Meal does not exert considerable impact on absorption.

Vd about 8.8 l. Linkng with proteins of plasma makes more than 99%.

Clearance - about 48 ml/min.

Is exposed to metabolism. The hydroxylated and carboxylated metabolites of a glimepirid are formed, apparently, owing to metabolism in a liver and are found in urine and in Calais.

T1/2 makes 5-8 h. After reception of a glimepirid in high doses of T1/2 increases. After a single dose in a dose of a glimepirid, marked radioactivity, 58% of radioactivity also 35% - in Calais were found in urine. Not changed active agent in urine was not found.

T1/2 of the hydroxylated and carboxylated metabolites of a glimepirid made, respectively, about 3-6 h and 5-6 h.

At patients with renal failures (with low KK) the tendency to increase in clearance of a glimepirid and to decrease in its average concentration in blood serum was observed. Thus, this category of patients does not have an additional risk of cumulation of a glimepirid.

Indications to use:

Diabetes mellitus 2 types (non-insulin-dependent) in case of inefficiency of a dietotherapy and an exercise stress.

Route of administration and doses:

The initial and maintenance dose is established individually on the basis of results of regular control of level of glucose in blood and in urine.

The initial dose makes 1 mg of 1 times/days. If necessary the daily dose can be gradually increased (by 1 mg in 1-2 weeks) to 4-6 mg.

The maximum dose makes 8 mg/days.

Features of use:

Use at pregnancy and feeding by a breast. It is contraindicated to use at pregnancy. In case of the planned pregnancy or at pregnancy approach the woman should be transferred to insulin.

In the period of a lactation it is necessary to transfer the woman to insulin. In pilot studies it is established what глимепирид is allocated with breast milk.

Use at abnormal liver functions. It is contraindicated at a liver failure.

Use at renal failures. It is contraindicated at a renal failure (including the patient who is on a hemodialysis).

With care apply at patients with the associated diseases of endocrine system influencing carbohydrate metabolism (including dysfunctions of a thyroid gland, adenogipofizarny or adrenocortical insufficiency).

In stressful situations (at the injury, surgical intervention, infectious diseases which are followed by fever) there can be a need for temporary transfer of the patient on insulin.

It is necessary to consider that symptoms of a hypoglycemia can be maleficiated or be absent absolutely at elderly patients, patients with NTsD or receiving simultaneous treatment by beta adrenoblockers, a clonidine, Reserpinum, guanetidiny or other sympatholytics.

At achievement of compensation of a diabetes mellitus sensitivity to insulin increases; in this regard in the course of treatment the need for a glimepirida can decrease. In order to avoid development of a hypoglycemia it is necessary to lower timely a dose or to cancel глимепирид. Dose adjustment also should be carried out at change of body weight of the patient or at change of his way of life, or at emergence of other factors promoting development hypo - or a hyperglycemia.

Upon transition on глимепирид from other drug it is necessary to take degree and duration of effect of the previous hypoglycemic means into account. There can be a need for the temporary termination of treatment in order to avoid the additive effect.

In the first weeks of treatment the risk of development of a hypoglycemia can increase that demands especially strict observation of the patient. Treat the factors promoting development of a hypoglycemia: irregular, defective food; changes of a usual diet; alcohol intake, especially in combination with the admission of meal; change of the usual mode of exercise stresses; simultaneous use of other medicines. The hypoglycemia can be quickly stopped by immediate reception of carbohydrates.

During treatment regular control of level of glucose in blood and urine, and also concentration of glycated hemoglobin is necessary.

Influence on ability to driving of motor transport and to control of mechanisms. During treatment it is necessary to abstain from occupations potentially dangerous types of activity requiring special attention and speed of psychomotor reactions.

Side effects:

From a metabolism: hypoglycemia, hyponatremia.

From the alimentary system: nausea, vomiting, a sensation of discomfort in epigastriums, abdominal pains, diarrhea, increase in activity of hepatic transaminases, a cholestasia, jaundice, hepatitis (up to development of a liver failure).

From system of a hemopoiesis: thrombocytopenia, leukopenia, erythropenia, granulocytopenia, agranulocytosis, pancytopenia, hemolitic anemia.

From an organ of sight: passing vision disorders.

Allergic reactions: itch, urticaria, skin rash; seldom - диспноэ, falling of the ABP, an acute anaphylaxis, an allergic vasculitis, a photosensitization.

Interaction with other medicines:

Strengthening of hypoglycemic action of a glimepirid is possible at simultaneous use with the insulin or other hypoglycemic drugs, APF inhibitors, Allopyrinolum, anabolic steroids and male sex hormones, chloramphenicol derivative of coumarin, cyclophosphamide, Disopyramidum, fenfluraminy, feniramidoly, fibrata, fluoxetine, guanetidiny, isophosphamides, MAO inhibitors, Miconazolum, PASK, pentoksifilliny (at injection introduction in high doses), phenylbutazone, azapropazony, oksifenbutazony, probenetsidy, hinolona, salicylates, Sulfinpyrazonum, streptocides, tetracyclines.

Weakening of hypoglycemic action of a glimepirid is possible at simultaneous use with acetazoleamide, barbiturates, corticosteroids, diazoxide, diuretics, Epinephrinum (adrenaline) and other sympathomimetics, a glucagon, purgatives (after prolonged use), niacin (in high doses), estrogen and progestogens, fenotiaziny, Phenytoinum, rifampicin, hormones of a thyroid gland.

At simultaneous use blockers of histamine H2 receptors, a clonidine and Reserpinum are capable both to potentiate, and to reduce hypoglycemic action of a glimepirid.

Against the background of use of a glimepirid strengthening or weakening of action of derivatives of coumarin is possible.

Ethanol can strengthen or weaken hypoglycemic action of a glimepirid.

Contraindications:

Diabetes mellitus of 1 type (insulin-dependent), ketoacidosis, a prekoma, a coma, a liver failure, a renal failure (including the patients who are on a hemodialysis), pregnancy, a lactation, hypersensitivity to a glimepirid, other derivatives of sulphonylurea and streptocides.

Storage conditions:

To store at a temperature not above 25 °C in the places not available to children. Period of validity 2 years.

Issue conditions:

According to the recipe

Packaging:

On 30 or 60 tablets in blister strip packagings and in cardboard packs.