Glimepiride

Chemical name

3-Этил-2,5-дигидро-4-мети л-N-[2-[4-[[[[(4-метилциклог ексил)амино]карбонил]��мино]сульфонил]фенил] этил]-2-оксо-1H-пиррол-1-��арбоксамид

Gross

C24-H34-N4-O5-S

Characteristics

White or jeltovato-bely crystalline powder almost odourless, nerastvorim almost in the water.

Of drugs

The drugs-gipoglikemicescoe. It stimulates the secretion and release of insulin beta-kletkami pancreas improves insulin postprandialny / C-peptidnyi response lowers giperglikemia without increasing insulin / C-peptida prandial. Increases sensitivity of peripheral tissues to insulino (экстрапанкреатическ��е Effects). Gipoglikemiceski effect reaches its maximum after 2-3 hours; Lasted for more than 24 hours and off for 2 weeks. The glucose and glikozilirovannogo hemoglobin (HbA1c) become dozozawisimo (at the time of appointment from 1 to 4 mg / day). A number of patients, particularly high-prandial glucose, the effect is achieved with the dose of 6 mg. Decreases risk of retino-, neiro- and nefropatii. The combined application can reduce insulin dose for obesity patients by 38%. In experiments on animals have been detected cases mutagennogo, carcinogenic and tertogennogo actions, the impact on Fertillnosti.posle intake of fully absorbed from the digestive tract. Time to C_max - 2-3 pm Volume of 8.8 litres (113 ml / kg), the overall Cl - 47.8 ml / min, tying with plasma protein is close to 100%. The liver virtually all oxidized and циклогексилгидроксим етил-деривата (with the participation of zitohroma IIC9 P450), with 1 / 3 pharmacological activity glimepirida to continue (with the participation of one or more enzymes zitozolnah) to the active carboxylic metabolita. T_1/2 5-8 hours Excreted primarily in the form of metabolites in the urine (60% imposed dose) and faeces (40%). Not koumouliruet.

Indications

Diabetes mellitus type 2.

Restrictions on the use of

Children's age (safety and effectiveness of their use in children to be determined).

Pregnancy and lactation

Contraindicated. In the case of pregnancy is necessary as soon as possible to move patientku for treatment of insulin. At the time of treatment should stop breastfeeding.

Contraindications

Hypersensitivity, diabetes mellitus type 1 diabetic ketoacidosis, diabetic precoma and coma insufficient liver and kidneys, cachexia, pregnancy, breast-feeding.

Side-Effects

From the circulatory system and blood (blood, gemostaz) : rarely drop AD thrombocytopenia, lakopenia, granulozitopenia, agranulozitos, eritropenia, pancitopenia, haemolytic and aplastic Anemia.so the nervous system and sensory organs : dizziness, headache, transient violation Zrenia.so part of the intestine : nausea, vomiting, stomachache, a sense of gravity in epigastralna area, diarrhea, vnutripechenochny Holetaz.so the metabolism : Gipoglikemia.prochie : to raise transaminaz, giponatriemia, skin allergies later cutaneous porphyria, and fatigue. Seldom-cough, hepatitis, allergic vasculit, photosensitization.

Patient interaction

Gipoglikemia increase NPVS etc. preparations with a high degree of binding to plasma proteins (sulfonamida, chloramphenicol, cumarins, probenecid), MAO inhibitors, insulin, beta-adrenoblokatora, miconazole, allopurinol, ACE inhibitors, PASC, pentoksifillin (with Injecting a high dose), hinolona, 25.06.1997, the male sex hormones, salicilata, tetratziklin, tritokvalin, trifosfamid. The effect of weakening (of giperglikemia) tiazidnye dioretiki, corticosteroids, fenotiazina, tireoidnye hormones, estrogena, oral contraceptives, phenytoin, nikotinova acid simpatomimetiki, isoniazid, barbiturates, acetazolamide, rifampicin, laxatives (and long-term use). Alcohol can both enhance or weaken gipoglikemicescuu activity. Propranolol increases C_max, AUC and T_1/2 (average 20%). Impact (marginally) gipokoagulyatia caused varfarinom. Recombinant alfa-interferona increased risk of violations of the thyroid gland.

Overdosing

Symptoms : hypoglycaemia until Koma.lechenie development : in / bolusnoe in a 50% solution of glucose, and then cefuroxim 10% glucose solution. If the patient is in the minds, it is recommended sweet hot water. There is a need for constant monitoring and maintenance of the vital functions, the concentration of glucose in the blood (at the level of 5.5 mmol / l) for a period of at least 48 hours (subject to repeated episodes gipoglikemii).

Precautions

Treatment begin only if diet and exercise do not normalize the glucose in the blood. At the beginning of therapy in the selection of doses that the concentrations of glucose and prandial every 4 hours; Continue to monitor the level of prandial glucose and the glucose in the daily urine periodically (every six months) to determine glycolic haemoglobin. The lack of effect or weakening of the (secondary resistance) to a combination of insulin. Against the backdrop of continuing treatment giperglikemia possible as a result of various effects of stress-fever, trauma, infection, surgery (in these cases temporarily appoint insulin). High risk of gipoglikemii exists in a weakened and depleted patients, and napochechnikova, lectures or liver failure. Probability gipoglikemii more alcohol, skipping meals, the lack of calories in the food, heavy and prolonged exercise. Be wary of during the drivers of vehicles and people skills relate to the high concentration of attention.

Dosing and Administration

Inside, squeezed enough liquid once before the first admission abundant food (usually before breakfast). Initial daily dose of 1-2 mg, in the later phase (within 2-3 weeks) increased to 4-6 mg. The maximum daily dose of 6 mg. In patients with renal insufficiency (more sensitive to gipoglikemicescomu Denver) recommended initial dose of 1 mg followed by the gradual titraciei.

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