2010/06/14

Glibenclamide

The international name:
Glibenclamide (Glibenclamide)

Group Affiliation:
Hypoglycemic medium for oral administration of sulfonylureas II generation

Description of the active substance (INN):
Glibenclamide

Dosage form:
Tablets

Mode of action:
Oral hypoglycemic means sulfonylurea derivative II generation. Has pancreatic and vnepankreaticheskim effects. It stimulates insulin secretion by lowering the threshold for glucose stimulation of beta-pancreatic cells, increases insulin sensitivity and the degree of its binding to target cells, increases the release of insulin, increases the effect of insulin on glucose uptake of muscle and liver, inhibits lipolysis in adipose tissue. Effective in the second stage of insulin secretion. Has hypolipidemic effect, reduces the thrombogenic properties of blood. Hypoglycemic effect develops in 2 hours and lasts for 12 hours

Indications:
Diabetes mellitus type 2 (in ineffectiveness of diet). Combination therapy with insulin to control the level of daily glycemia.

Contraindications:
Hypersensitivity, diabetes mellitus type 1 (also in childhood and adolescence), diabetic ketoacidosis, diabetic precoma and coma, hyperosmolar coma, microangiopathy, hepatic and / or renal failure, extensive burns, trauma, major surgery, intestinal obstruction , gastric paresis, state, accompanied by malabsorption of food and the development of hypoglycemia (infectious diseases), leukopenia, pregnancy, laktatsii.C caution. Feverish syndrome, alcoholism, adrenal insufficiency, thyroid disease (hypothyroidism or hyperthyroidism).

Adverse effects:
Hypoglycemia (for violation of the dosing and inadequate diet), weight gain, fever, arthralgia, proteinuria, allergic reactions (skin rash, itching), dyspepsia (nausea, diarrhea, feeling of heaviness in the epigastric), neurological disorders (paresis, violations of sensitivity) , hemodyscrasia (atrophic or hemolytic anemia, leukopenia, agranulocytosis, pancytopenia, eosinophilia, thrombocytopenia), abnormal liver function (cholestasis), late cutaneous porphyria, changes in taste, polyuria, photosensitivity, headache, fatigue, weakness, dizziness. Overdosage . Symptoms: hypoglycemia (hunger, increased sweating, severe weakness, palpitations, tremor, anxiety, headache, dizziness, insomnia, irritability, depression, edema, speech and vision, impaired consciousness), hypoglycemic coma. Treatment: if the patient is in consciousness, to take sugar by mouth, with loss of consciousness - in / to enter dextrose (IV bolus - 50% dextrose, then infusion of 10% solution), 2.1 mg of glucagon n / a, i / m or i / c, diazoxide 30 mg / in 30 min, control of glucose concentration every 15 min, and determination of pH, urea nitrogen, creatinine, electrolytes in the blood. After recovery of consciousness is necessary to give the patient foods rich in carbohydrate (to avoid a recurrence of hypoglycemia). When cerebral edema - mannitol and dexamethasone.

Dosage and administration:
The magnitude of the dose depends on age, severity of diabetes, blood glucose, fasting and 2 hours after meals. Average daily dose ranges from 2.5 to 15 mg. Multiplicity of reception - 1-3 times a day for 20-30 minutes before eating. Doses over 15 mg / day did not increase the severity of hypoglycemic effect. The initial dose in elderly patients - 1 mg / day. When replacing hypoglycemic drugs with a similar type of glibenclamide appointed by the scheme given above, but prior to the drug immediately overturned. In the transition from biguanide initial daily dose - 2.5 mg, if necessary daily dose is increased every 5-6 days to 2.5 mg to achieve compensation. In the absence of compensation for 4-6 weeks is necessary to decide on the conduct of combined therapy.

Cautions:
Should regularly monitor blood glucose, fasting and after meals, the daily curve of glucose in the blood and urine. In the case of surgery or decompensated diabetes need to take into account the possibility of using insulin. Should warn patients about the increased risk of hypoglycemia in cases receiving ethanol ( including the possible development of disulfiramopodobnyh reactions: abdominal pain, nausea, vomiting, headache) NSAID during starvation. During the treatment is not recommended long stay in the sun. Need dosage adjustment in physically and emotionally straining, change in diet. Clinical manifestations of hypoglycemia may be masked when taking beta-blockers, clonidine, reserpine, guanetidina. During the period of treatment must be careful when driving and occupation of other potentially hazardous activities that require high concentration and quickness of psychomotor reactions.

Interaction:
ACE inhibitors (captopril, enalapril), blockers of H2-histamine receptors (cimetidine), antifungal drugs (miconazole, fluconazole), NSAIDs (fenilbutazon, azapropazon, oxyphenbutazone), fibrates (clofibrate, bezafibrate), tuberculosis (Ethionamide), salicylates, anticoagulants cumarine series, anabolic steroids, beta-blockers, MAO inhibitors, long-acting sulfonamides, cyclophosphamide, biguanide, chloramphenicol, fenfluramin, acarbose, fluoxetine, guanetidin, pentoxifylline, tetracycline, theophylline, tubular secretion blockers, reserpine, bromocriptine, dizopiramid, pyridoxine, insulin, enhance the effects of allopurinol. diminish the effects of barbiturates, GCS adrenostimulyatorov (epinephrine, clonidine), antiepileptic drugs (phenytoin), BCCI, carbonic anhydrase inhibitors (acetazolamide), thiazide diuretics, chlortalidone, furosemide, triamterene, asparaginase, Baclofen, danazol, diazoxide, isoniazid, morphine ritodrin, salbutamol, terbutaline, glucagon, rifampin, thyroid hormones, salt, Li +, in high doses - nicotinic acid, chlorpromazine, oral contraceptives and estrogens. Acidifying urine drugs (ammonium chloride, CaCl2, ascorbic acid in large doses) increases the effects of by reducing the degree of dissociation and increase the reabsorption of glibenclamide. drugs, which suppress bone marrow hemopoiesis, increased the risk myelosuppression.