Glibenclamide

Chemical name

5-Хлор-N-[2-[4-[[[(циклогек��иламино)карбонил]ами��о]сульфонил]фенил]эти л]- 2-metoksibenzamid

Gross

C23-H28-Cl-N3-O5-S

Characteristics

Melkochristalliceski powder white (or white with kremovatam shade). Virtually nerastvorim water, little soluble in alcohol.

Of drugs

The drugs-gipoglikemicescoe, гипохолестеринемичес кое. Specifically stimulates beta ostrovkovogo apparatus increases insulin incretia pancreatic cancers. Activity is mostly stored in the инсулин-синтетическо�� the pancreas. Restores physiological sensitivity to beta-kletok fast. Potenziruet effect of insulin (endogenous and exogenous), as increases the number of receptors to insulino improves insulin-retseptornoe interaction and restores transduktia postretseptonego signal. Increasing concentrations of insulin in plasma and lowering glucose occur gradually, which reduces the risk of gipoglikemicakih states. Increases sensitivity insulinovykh receptors to insulino in peripheral tissues and cause vnepankreaticalkie effects. Increases disposal of glucose in the liver and muscles, stimulates education in glycogen (reduces glucose output from the liver). Provides gipolipidemicescoe, antidiureticescoe act lowers trombogenne properties of blood, prevents Aritmi.actie develops in 2 h after administration reaches its peak in 7-8 hours and lasts 8 to 12 hours (for mikronizirovannah of up to 24 h). Quickly and almost completely absorbed from the digestive tract. C_max after a single reception achieved in 1-2 hours Associated with the plasma protein by 99%. The distribution of 10 litres. Hardly crosses the placental barrier. T_1/2 - 4-11 hours The liver completely transformed into two inactive metabolita (are approximately equal amount), one of whom is excreted in the urine, and the second appears to jelchew through blood.

Indications

Diabetes mellitus type 2, with no compensation io diet, a decrease in body mass index, physical activity.

Pregnancy and lactation

Contraindicated. At the time of treatment should stop breastfeeding.

Contraindications

Гиперчувствительност ь (incl. to sulfanilamidnam drugs, tiazidnam dioretikam) diabeticescoe prekomatosnoe and coma, ketoacidosis, extensive burns, surgery and trauma, intestinal occlusion, paresis stomach; of violating food intake, development gipoglikemii (infectious diseases, etc.); hypothesis or Ray, the liver and kidneys, lakopenia, diabetes mellitus type 1, pregnancy, breast-feeding.

Side-Effects

From the circulatory system and blood (blood, gemostaz) : rarely thrombocytopenia, granulozitopenia, eritrotsitopenia, pancitopenia, eozinofilia, leikozitopenia, agranulozitos (very rarely), in some cases, or gipoplastical Hemolytic Anemia.so the nervous system and sensory organs : headache, dizziness, change in the taste of Oshchutmeni.so metabolism : hypoglycaemia, proteinurija, Later skin Porfiria.so part of the stomach : the liver, holetaz, �испепсия.Аллергическ ие reactions : skin skin (erythema, exfoliativei dermatitis). Other : fever, artralgia, poliuria, increased body mass index, photosensitization.

Patient interaction

Antifungal means systemic action (azolov derivative), ftorhinolona, tetratziklin, chloramphenicol (oppressing metabolism), H_2-blokatora, beta-adrenoblokatora, ACE inhibitors, NPVS, MAO inhibitors, klofibrat, bezafibrat, probenecid, paracetamol, ethionamide, 25.06.1997, pentoksifillin, allopurinol, cyclophosphamide, rezerpin, sulfanilamida, insulin-potenziruut gipoglikemia. Barbiturates, fenotiazina, diazoxid, glukokortikoidnye and tireoidnye hormones, estrogena, gestagena, glukagon, adrenomimeticalkie preparations lithium salts, derivatives nicotinic acid and saluretiki-weakened gipoglikemiceski effect. Acidifying the urine (ammonium chloride, calcium chloride, ascorbic acid in high doses), the increase (decrease the degree of dissociation and increase reabsorbqiyu). Is sinergistom (additive effect), the proximity anticoagulants. Rifampicin inachtiwatia accelerates and reduces efficiency.

Overdosing

Symptoms : hypoglycaemia (feeling hunger, sudden weakness, anxiety, headache, dizziness, sweating, rapid heartbeat, muscle drugs, brain swelling, speech disorder, and the violation of consciousness and coma gipoglikemical possible death). Treatment : In light cases, the immediate admission of sugar, sweet hot tea, fruit juice, corn syrup, honey; in the most severe cases, a 50% glucose solution (50 ml / and in the interior), in continuous / cefuroxim in 5-10% solution dekstrozy in / m glukagona a 1-2 mg, diazoxid inside of 200 mg every 4 h or 30 mg in / for a period of 30 minutes; oteke with brain-mannit and dexamethasone; monitoring the fast (every 15 min), the pH, urea nitrogen, creatinine, electrolytes.

Precautions

To prevent gipoglikemicakih states should strictly observe regular admission. The two food consumption no later than one hour after using the drug. Between dose selection in the primary assignment or transfer with other hypoglycemic drugs regularly shown the sugar profile (several times a week). The treatment requires dynamic monitoring of the level of glucose (haemoglobin glikozilirovannogo) in the serum (at least once in three months). It should be borne in mind that the clinical manifestations gipoglikemii may be masked in the admission beta-adrenoblokatorov, clonidine, rezerpina, guanetidina. In the case of transfer to glibenclamide with insulin dose of 40 U / day or more, on the first day shall half dose of insulin and 5 mg glibenklamida to the gradual adjustment of the last dose, as required. To apply caution in elderly patients are starting treatment with polovinnah doses, which would change by no more than 2.5 mg / day with weekly intervals, and aggressive states in the treatment required glibenklamidom Not taking alcohol (disulfiramopodobnaya possible), a prolonged stay in the sun and to restrict smoking fatty foods. Early treatment is not recommended activities requiring high speed response.

Dosing and Administration

The inside is not liquid, squeezed small amounts of water. Daily dose adjusted individually, depending on age, severity of diabetes, the io, and usually 1,25-20 mg (initial dose of 2.5-5 mg / day, the maximum daily 25-mg), which appointed one, two, at three reception for 30-60 minutes (mikronizirovanne forms for 10-15 min) to food. If the effect can be combined with biguanidami and insulin.

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