Glimepiride tablets 4mg, no. 30

The initial and maintenance dose is set individually based on the results of regular monitoring of blood and urine glucose levels.

The initial dose is 1 mg 1 time / day.

If necessary, the daily dose can be gradually increased (by 1 mg in 1-2 weeks) to 4-6 mg. The maximum dose is 8 mg / day.

glimepiride

• Type 1 diabetes mellitus (insulin dependent),

• ketoacidosis

• precom,

• coma,

• liver failure,

• renal failure (including patients on hemodialysis),

• pregnancy,

• breastfeeding period,

• children and adolescents up to 18 years old,

• hypersensitivity to glimepiride, other sulfonylurea derivatives and sulfonamides.

pharmachologic effect

Oral hypoglycemic agent, a sulfonylurea derivative. Stimulates insulin secretion by? -Cells of the pancreas, increases insulin release. Increases the sensitivity of peripheral tissues to insulin.

Pharmacokinetics

With repeated oral administration at a dose of 4 mg / day, Cmax in serum is reached after about 2.5 hours and is 309 ng / ml; there is a linear relationship between dose and Cmax, as well as between dose and AUC. Food intake does not significantly affect absorption. Vd about 8.8 liters. Plasma protein binding is more than 99%. Clearance - about 48 ml / min. Metabolized. Hydroxylated and carboxylated metabolites of glimepiride are formed, apparently due to metabolism in the liver and are found in urine and feces. T1 / 2 is 5-8 hours. After taking glimepiride in high doses, T1 / 2 increases. After a single oral dose of glimepiride labeled with radioactivity, 58% of radioactivity was found in urine and 35% in feces. The unchanged active substance was not detected in the urine.T1 / 2 of the hydroxylated and carboxylated metabolites of glimepiride were about 3-6 hours and 5-6 hours, respectively. In patients with impaired renal function (with low CC), there was a tendency to an increase in the clearance of glimepiride and to a decrease in its mean serum concentrations. Thus, in this category of patients, there is no additional risk of glimepiride cumulation.

Side effect

From the side of metabolism: hypoglycemia, hyponatremia. From the digestive system: nausea, vomiting, epigastric discomfort, abdominal pain, diarrhea, increased activity of hepatic transaminases, cholestasis, jaundice, hepatitis (up to the development of liver failure). From the hematopoietic system: thrombocytopenia, leukopenia, erythropenia, granulocytopenia, agranulocytosis, pancytopenia, hemolytic anemia. From the side of the organ of vision: transient visual impairment. Allergic reactions: itching, urticaria, skin rash; rarely - dyspnea, drop in blood pressure, anaphylactic shock, allergic vasculitis, photosensitivity.

Application during pregnancy and lactation

Contraindicated in pregnancy. In the event of a planned pregnancy or upon the onset of pregnancy, a woman should be switched to insulin. During lactation, a woman should be transferred to insulin. In experimental studies, it was found that glimepiride is excreted in breast milk.

Application for violations of liver function

Contraindicated in liver failure.

Application for impaired renal function

Contraindicated in renal failure (including patients on hemodialysis).

Application in children

Contraindicated for use in children and adolescents under the age of 18 years.

Use in elderly patients

Use with caution in elderly patients.

special instructions

Use with caution in patients with concomitant diseases of the endocrine system that affect carbohydrate metabolism (including dysfunction of the thyroid gland, adenohypophyseal or adrenocortical insufficiency). In stressful situations (trauma, surgery, infectious diseases accompanied by fever), it may be necessary to temporarily transfer the patient to insulin. It should be borne in mind that the symptoms of hypoglycemia may be mitigated or completely absent in elderly patients, patients with NCD, or receiving concomitant treatment with beta-blockers, clonidine, reserpine, guanethidine or other sympatholytics. When diabetes compensation is achieved, insulin sensitivity increases; in this regard, during treatment, the need for glimepiride may decrease.To avoid the development of hypoglycemia, it is necessary to promptly reduce the dose or cancel glimepiride. Dose adjustment should also be carried out when the patient's body weight changes or when his lifestyle changes, or when other factors appear that contribute to the development of hypo- or hyperglycemia. When switching to glimepiride from another drug, it is necessary to take into account the degree and duration of the effect of the previous hypoglycemic agent. It may be necessary to temporarily discontinue treatment to avoid an additive effect. In the first weeks of treatment, the risk of hypoglycemia may increase, which requires particularly strict monitoring of the patient. Factors contributing to the development of hypoglycemia include: irregular, malnutrition; changes in your diet; alcohol consumption,especially in combination with skipping meals; change in the usual mode of physical activity; simultaneous use of other drugs. Hypoglycemia can be quickly treated with immediate carbohydrate intake. During the treatment period, regular monitoring of blood and urine glucose levels, as well as the concentration of glycated hemoglobin is necessary.

Influence on the ability to drive vehicles and mechanisms

During the period of treatment, one should refrain from engaging in potentially hazardous activities that require increased attention and speed of psychomotor reactions.

Drug interactions

An increase in the hypoglycemic effect of glimepiride is possible with simultaneous use with insulin or other hypoglycemic drugs, ACE inhibitors, allopurinol, anabolic steroids and male sex hormones, chloramphenicol, coumarin derivatives, cyclophosphamide, disopyramide, fenframidamidolamine, fibeniramine, fibenyethoramine , miconazole, PASK, pentoxifylline (when injected in high doses), phenylbutazone, azapropazone, oxyphenbutazone, probenecid, quinolones, salicylates, sulfinpyrazone, sulfonamides, tetracyclines. The weakening of the hypoglycemic effect of glimepiride is possible with simultaneous use with acetazolamide, barbiturates, corticosteroids, diazoxide, diuretics, epinephrine (adrenaline) and other sympathomimetics,glucagon, laxatives (after prolonged use), nicotinic acid (in high doses), estrogens and progestogens, phenothiazine, phenytoin, rifampicin, thyroid hormones. With the simultaneous use of blockers of histamine H2-receptors, clonidine and reserpine can both potentiate and reduce the hypoglycemic effect of glimepiride. Against the background of the use of glimepiride, an increase or decrease in the action of coumarin derivatives is possible. Ethanol can enhance or weaken the hypoglycemic effect of glimepiride.clonidine and reserpine are capable of both potentiating and reducing the hypoglycemic effect of glimepiride. Against the background of the use of glimepiride, an increase or decrease in the action of coumarin derivatives is possible. Ethanol can enhance or weaken the hypoglycemic effect of glimepiride.clonidine and reserpine are capable of both potentiating and reducing the hypoglycemic effect of glimepiride. Against the background of the use of glimepiride, an increase or decrease in the action of coumarin derivatives is possible. Ethanol can enhance or weaken the hypoglycemic effect of glimepiride.