Glibenclamide

When ATH:
A10BB01

Characteristic.

Sulfonylurea derivative II generation.

White crystalline powder (or white with kremovatym). Practically insoluble in water, few soluble in alcohol.

Pharmacological action.
Hypoglycemic, hypocholesteremic.

Application.

Diabetes mellitus type 2 if you can not compensate hyperglycemia diet, weight loss, physical activity.

Contraindications.

Hypersensitivity (incl. to sulfanilamides, thiazide diuretics), prekomatosnoe and diabetic coma, Ketoacidosis, extensive burns, surgery and trauma, ileus, gastroparesis; states, accompanied by malabsorption of food, Hypoglycemia (infectious diseases and others.); Hypo- or hyperthyroidism, the liver and kidneys, leukopenia, diabetes mellitus type 1, pregnancy, lactation.

Pregnancy and breast-feeding.

Category actions result in FDA - C. (The study of reproduction in animals has revealed adverse effects on the fetus, and adequate and well-controlled studies in pregnant women have not held, However, the potential benefits, associated with drugs in pregnant, may justify its use, in spite of the possible risk.)

At the time of treatment should stop breastfeeding.

Side effects.

Cardio-vascular system and blood (hematopoiesis, hemostasis): seldom-B19, granulocytopenia, erythropenia, pancytopenia, eozinofilija, leukopenia, agranulocytosis (rarely), in some cases - hypoplastic or hemolytic anemia.

From the nervous system and sensory organs: headache, dizziness, change in taste.

Metabolism: gipoglikemiâ, proteinuria, Late each porphyria.

From the digestive tract: abnormal liver function, cholestasis, dyspepsia.

Allergic reactions: skin rashes (эritema, exfoliative dermatitis).

Other: fever, arthralgia, polyuria, weight gain, photosensitivity.

Cooperation.

Antifungals for systemic effects (azole), ftorkhinolony, tetracikliny, chloramphenicol (It inhibits the metabolism), H₂-blockers, beta-blockers, ACE inhibitors, NSAIDs, MAO inhibitors, clofibrate, bezafibrate, probenecid, paracetamol, ethionamide, anabolic steroid, pentoxifylline, allopurinol, cyclophosphamide, reserpine, sulfonamides, insulin - potentiate hypoglycemia. Barbiturates, fenotiazinы, diazoksid, glucocorticoid and thyroid hormones, Estrogens, progestins, glucagon, adrenomimetic drugs, lithium salt, derivatives of niacin and saluretics - weaken the hypoglycemic effect. Acidifying the urine means (Ammonium chloride, calcium chloride, ascorbic acid in high doses) enhance the effect of (reduce the degree of dissociation and increase the reabsorption). It is synergistic (additive effect) anticoagulants. Rifampicin accelerates and lowers the efficiency of inactivation.

Overdose.

Symptoms: gipoglikemiâ (the sensation of hunger, severe weakness, anxiety, headache, dizziness, Sweating, heartbeat, muscle tremors, swelling of the brain, speech disorder and vision, impairment of consciousness, and hypoglycemic coma, possible death).

Treatment: in mild cases, immediate sugar intake, sweet hot tea, fruit juice, corn syrup, honey; in severe cases - introduction 50% glucose solution (50 ml IV and inside), Continuous / v infusion of 5-10% dextrose, i / m administration of glucagon 1-2 mg, diazoxide inside by 200 mg every 4 or h 30 mg i.v. during 30 m; with cerebral edema - mannitol and dexamethasone; monitoring of blood glucose (every 15 m), pH determination, BUN, creatinine, electrolytes.

Dosing and Administration.

Inside, without chewing, with a little water. The daily dose is individually, depending on the age, the severity of diabetes, the level of hyperglycemia, and is usually 1.25-20 mg (initial dose 2.5-5 mg / day, maximum daily intake - 20-25 mg), which is administered in one, two, less often - three receptions for 30-60 minutes (micronized form for 10-15 minutes) before meals. With little effect possible combination with a biguanide and the insulin.

Precautions.

To prevent hypoglycaemia should strictly observe the regularity of. It is mandatory the use of food within, than 1 h after using the drug. During the selection of a dose during the initial appointment or transfer to others. hypoglycemic agents show regular determination of sugar profile (few times a week). During treatment requires dynamic control of glucose levels (Glycosylated hemoglobin) serum (at least 1 times a 3 Months). It will be appreciated, that the clinical manifestations of hypoglycemia may be masked when taking beta-blockers, klonidina, reserpine, guanethidine. In case of transfer to glibenclamide from insulin in a dose 40 U / day or more - on the first day, a half dose of insulin is prescribed and 5 mg of glibenclamide with a gradual dose adjustment of the latter as needed. Use with caution in elderly patients - start treatment with half doses, which subsequently change by no more than 2,5 mg / day at weekly intervals, in feverish conditions the treatment of glibenclamide required rejection of alcohol (possible disulfiramopodobnyh), prolonged sun exposure and limit consumption of fatty foods. At the beginning of treatment is not recommended activity, requiring increased reaction rate.

Cooperation