Диабрекс

General characteristics. Structure:

Active agent: глимепирид 1 mg, 2 mg, 3 mg, 4 mg or 6 mg;

Other components: lactoses monohydrate, sodium krakhmalglikolit, cellulose microcrystallic, K30 povidone, magnesium stearate, dyes: tablets of 1 mg – ferrous oxide red (E172); tablets of 2 mg – ferrous oxide yellow (E172), indigo carmine (E132); tablets of 3 mg – ferrous oxide yellow (E172); tablets of 4 mg – indigo carmine (E132); tablets of 6 mg – yellow "sunset" (E110).

Pharmacological properties:

Pharmacodynamics. Glimepirid is a peroral glucose-lowering drug which belongs to group of derivatives of sulphonylurea of the third generation. Its hypoglycemic action is based on insulin release stimulation by the functioning pancreas beta cells. Contacting specific receptors on a membrane of beta cells of a pancreas, глимепирид causes closings of K+ ATP-dependent - channels, increase in comparison of ATF/ADF in cytoplasm that causes depolarization of membranes. Thereof results opening of potentsialzavisimy Sa2+-channels, Sa2+-zavisimy an exocytosis of secretory granules is stimulated and an insulin exit in blood increases. Unlike medicines of the first and second generation глимепирид contacts other subunit of a receptor of sulphonylurea with a molecular weight of 65 kd that gives the chance to reduce influence of drug on cardiovascular system and to protect beta cells from an anesthesia and premature exhaustions. Except antihyperglycemic effect, medicine shows pozapankreatichesky action – increases sensitivity of peripheral fabrics to insulin, suppresses a gluconeogenesis.
The effect of medicine is dozozavisimy, and the round-the-clock control of glycemia level at patients with a diabetes mellitus ІІ type is reached at single use of a glimepirid.

Pharmacokinetics. Absorption. Glimepirid has absolute bioavailability (100%). At intake of 100% of a dose it is soaked up. The concomitant use of food does not influence degree absorption, can only slow down a little it. The maximum concentration of medicine in plasma is reached in 2 - 3 hour after use.

Distribution. Distribution volume insignificant also makes 8, 8 l (113 ml/kg), the general clearance 47, 8 ml/min. Linkng with proteins – more than 99, 5%.

Metabolism. Glimepirid completely metabolizut by oxidative biotransformation. The main metabolites is: cyclohexyl-hydroxy to the metilena derivative (M1) and carboxyl derivative (Sq.m). In the course of biotransformation of a glimepirid to M1 derivative P450 cytochrome ІІ takes participation to C9. Further with participation of one or several cytosolic M1 enzymes metabolizut with formation of Sq.m derivative.

Elimination (removal). The average elimination half-life of medicine makes 5 - 8 hour, and metabolites of M1 and Sq.m – 3 - 6 and 5 - 6 hour, respectively. At use of drug in the highest doses this indicator can last. Through kidneys eliminirut 58% of the accepted drug dose, and 35% – with bile in the form of metabolites.
Comparison of pharmacokinetics at one - and reusable use did not show serious differences. Glimepirid does not show ability to cumulation.
Pharmacokinetic parameters did not differ at men and women, and also at persons of younger and advanced age (65 years are more senior).
At persons with low clearance of creatinine it is revealed a tendency to increase in clearance of a glimepirid, decrease in its concentration in a blood plasma. However elimination of metabolites is slowed down. Though in such patients it is impossible to allow drug cumulation.

Indications to use:

Treatment of a diabetes mellitus ІІ type, at inefficiency of a diet and the dosed exercise stresses.

Route of administration and doses:

Pill is taken inside, without chewing, just before or in the period of a breakfast or the main first reception of food, washing down with a glass of water, 1 time a day.
The drug dose is established individually on the basis of data about the level of a glycemia and glucosuria.
The recommended initial dose makes 1 mg of Diabreks a day.
In case of not collateral to control of glycemia level the dose is gradually increased to 4 - 6 mg of a glimepirid a day, adding on 1 mg at an interval of 1 - 2 week.
The maximum daily dose of a glimepirid makes 8 mg.
Efficiency of pharmacotherapy is estimated on the basis of clarification of level of glikozirovanny hemoglobin (HbA1c) each 3 - 6 months.

Upon transition the initial dose of Diabreks makes 1 mg a day of other sugar-lowering means. Depending on its reached effect it is possible to increase gradually as it is described above.

Duration of a course of treatment is defined individually, depending on the reached control of glycemia level.

Features of use:

In a case the admission of a dose of Diabreks cannot increase it at the following reception.

If at Diabreks's use in a dose of 1 mg the patient had hypoglycemia signs, then it demonstrates that it is possible to control glycemia level by means of a diet and the dosed exercise stresses.
During treatment there can be a need for reduction of a dose of Diabreks as drug also increases sensitivity of peripheral fabrics to insulin. Dose adjustment is required also in case of change of body weight of the patient or to lifestyle, or emergence of factors which can increase risk of emergence hypo - or a hyperglycemia.
Диабрекс appoint with care to patients with associated diseases of bodies of endocrine system which influence carbohydrate metabolism (a thyroid gland, a front share of a hypophysis, bark of adrenal glands).
Alcohol can strengthen or weaken antihyperglycemic effect of medicine. The patient has to know that medicine does not replace maintenance of a diet and performance of the dosed exercise stresses.
If at Diabreks's use in the maximum doses it is not possible to reach desired therapeutic effect, then it is reasonable to appoint drug in a combination with metformin or drugs of insulin. The combination therapy is begun under the supervision of the doctor in the conditions of an endocrinological hospital.

Диабрекс – Metforminum
The dose of previously used drug is not changed, and additional drug is appointed at first in the minimum dose, further, if necessary, increasing it to maximum.

Диабрекс – an insulin therapy
At patients with insufficient control of level of a glycemia at use of the maximum dose of Diabreks, in case of need, it is possible to begin an insulin therapy at the same time. Selection of a dose of drug of insulin is begun with minimum and, depending on glycemia level indicators, gradually increased.

Influence on ability to manage vehicles and moving mechanisms which demand considerable concentration of attention.
In an initiation of treatment, at irregular reception of Diabreks or upon transition from one glucose-lowering drug to another perhaps fluctuations of level of a glycemia that, in turn, can influence attention and speed of response. And it can affect ability to manage transport and work with difficult mechanisms.

Side effects:

Preferential medicine is transferred well. Development of a hypoglycemia mostly can be caused to medicine overdoses, bad food, heavy exercise stresses, endogenous disturbances of carbohydrate metabolism, injuries, cross by interaction with other medicines or alcohol.
From digestive tract: nausea, vomiting, diarrhea, a sensation of discomfort in epigastric area, pain in a stomach, increase in activity of transaminases, very seldom a cholestasia, jaundice, hepatitis are possible.
From system of blood: thrombocytopenia, a leukopenia, anemia, a granulocytopenia, an agranulocytosis, a pancytopenia, hemolitic anemia which is reverse and a picture of blood is gradually normalized after drug withdrawal.
Allergic reactions: itch, enanthesis, small tortoiseshell. Very seldom a photosensitization, an allergic vasculitis, диспноэ, lowered arterial pressure, shock.
Other reactions: a vision disorder which preferential arise in an initiation of treatment through change of level of glucose in blood and over time disappear. Hyponatremia.

Interaction with other medicines:

The hypoglycemic effect of Diabreks is strengthened: the insulin drugs, other sugar-lowering means, APF inhibitors, Allopyrinolum, anabolic steroids, male sex hormones, chloramphenicol derivative of coumarin, cyclophosphamide, Disopyramidum, фенфлурамин, фенирамидол, fibrata, fluoxetine, гуанетидин, isophosphamide, MAO, PASK inhibitors, Miconazolum, пентоксифиллин (at injection introduction in high doses), phenylbutazone, азапропазон, оксифенбутазон, пробенецид, hinolona, salicylates, Sulfinpyrazonum, streptocides, tetracyclines, тритоквалин, trofosfamida.

The hypoglycemic effect of Diabreks is weakened: acetazoleamide, barbiturates, corticosteroids, diazoxide, diuretics (saluretics and thiazide diuretics), Epinephrinum and other sympathomimetics, a glucagon, purgatives (at prolonged use), niacin (in high doses), niacin derivatives, estrogen and progestins, hormones of a thyroid gland, rifampicin, фенотиазин, Phenytoinum.

H2 receptors blockers, clonidine, beta-blockers and Reserpinum can how to strengthen and weaken antihyperglycemic effect of medicine.

Glimepirid can strengthen or weaken action of derivatives of coumarin.

Contraindications:

Диабрекс it is not necessary to apply at patients with hypersensitivity to a glimepirid or other components of drug, at a diabetes mellitus І type, ketoacidosis, a prekoma, a coma, a heavy hepatic unsufficiency and/or kidneys (including at patients who are on dialysis), during pregnancy and a lactation, at hypersensitivity to derivatives of sulphonylurea and sulfanamide drugs. Children's age.

Overdose:

Symptoms: a hypoglycemia which is followed by the strengthened potovydeleniye, feeling of alarm, tachycardia, increase in arterial pressure, heartbeat, pain in heart, arrhythmia; headache, dizziness, bulimia, nausea, vomiting, apathy, drowsiness, concern, aggression, disturbance of concentration of attention, depression, consciousness disturbance, tremor, paresis, sensitivity disturbance, spasms. Development of a coma is possible.

Treatment: appoint glucose orally or intravenously, carry out correction of a diet. In hard cases of the patient it is necessary to hospitalize.

Storage conditions:

To store in unavailable to children, the dry place at a temperature of 15 - 25 °C.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in 1 blister; on 1 or 3 blisters in cardboard packaging for tablets on 2 mg and 4 mg; on 3 blisters in cardboard packaging for tablets on 1 mg and 3 mg.