Directory Metaboliki Gipoglikemicakie synthetic and other means Repowide
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Repowide

Chemical name

(+)-2-Этокси-альфа-[[(S)-ал ьфа-изобутил-о-пипери��инобензил]карбамоил]- n-толуиловая acid

Gross

C27-H36-N2-O4

Of drugs

The drugs-gipoglikemicescoe. Atf-zawisimae blocking potassium channels in the membranes functionally active beta-kletok ostrovkovogo apparatus pancreas is depoliarizatia them and the opening of calcium channels inducyruya incretia insulin. Insulinotropony response to a meal is for 30 minutes after application, and with the declining levels of glucose in the blood during mealtimes (insulin concentrations between meals is not increasing). In experiments in vivo and in animals have been identified mutagennogo, tertogennogo, carcinogenic actions and the impact on Fertilnosti.bystro and completely absorbed from the digestive tract. C_max achieved through 1 h at 9.8; 18.3; 26 and 65.8 ng / ml after administration of doses of 0.5; 1; 2 and 4 mg respectively; To the reception with their food C_max will likely fall by about 20%. The plasma rapidly reduced within 4 hours Absolute bioavailability 56%, tying with blood plasma proteins very high (more than 98%), the distribution-31 litres (after the / in the healthy volunteers). Virtually biotransformiroetsa in the liver (oxidation and bonding with glukuronova acid), forming inactive metabolites. T_1/2-1 p.m. Place for a period of four to six hours, mostly with jelchew through blood (90%) and urine (less than 8%).

Indications

Diabetes mellitus type 2 in the face of nutrition and physical loads, including Combined treatment with metforminom (with the poor diet and physical exercise, or alone or repaglinidom metforminom).

Restrictions on the use of

Nor should appoint children and patients over 75 years of age, the safety and efficacy of therapy in patients these age categories to be decided.

Pregnancy and lactation

Contraindicated. At the time of treatment should stop breastfeeding.

Contraindications

Hypersensitivity, diabetes mellitus type 1 diabetic ketoacidosis with coma or not, serious violations of the liver and / or kidney problems, pregnancy, breast-feeding.

Side-Effects

Hypoglycaemia, the vision, neuralgia, tranzithornoe increase in liver enzymes, allergic reactions.

Patient interaction

Beta-adrenoblokatora, chloramphenicol, indirect combined (coumarin derivatives), NPVS, probenecid, salicilata, MAO inhibitors, sulfonamida, alcohol, 25.06.1997 reinforce blockers calcium channel corticosteroids, dioretiki (especially tiazidove), isoniazid, niazin, oral contraceptives, fenotiazina, phenytoin, simpatomimetiki, tireoidnye hormones-weakening effect. Erythromycin, and ketokonazol miconazole weaken, and barbiturates, carbamazepine and rifampicin-increase metabolism.

Overdosing

Symptoms : hypoglycaemia (sense of hunger, a sense of fatigue and weakness, headache, anxiety, anxiety, drowsiness, trouble sleeping, nightmares, changes in behaviour such as observed in Puerto Rico, lack of concentration, the speech and vision sputannosti consciousness, paleness, nausea, heart palpitations, convulsions, cold sweat, coma, etc.). Treatment : at a moderate gipoglikemii, without neurological symptoms and loss of consciousness-reception carbohydrates (sugar, or glucose) inwards and dose adjustment or diet. In severe (convulsions, loss of consciousness, coma), in / in a 50% glucose solution followed infuziei 10% solution to maintaining the level of glucose in the blood of at least 5.5 mmol / O

Precautions

To use caution in patients with impaired liver or kidney, which had been weakened patients and the upcoming extensive operational intervention.

Dosing and Administration

Inside for 15-30 minutes before meals usually three times a day before the main meals. Dose picked individually. Initial dose of 0.5 mg. The doses are not less than 1-2 weeks after the start of treatment, based on the level of glycemia. The maximum single dose of 4 mg daily to 16 mg. If a patient has another oral gipoglikemicescoe means, or the glikozilirovannogo haemoglobin greater than or equal to 8%, the recommended initial dose of 1 mg.

See also

All products of this group