Glibenclamide stimulates insulin secretion by lowering the threshold for glucose stimulation of pancreatic beta cells, increases sensitivity to insulin and its degree of binding to target cells that increases insulin release, enhances the action of insulin absorption muscle glucose and liver, inhibits lipolysis in adipose tissue . Effective second stage insulin secretion. Has hypolipidemic effect, reduces the thrombogenic properties of blood. Andriol side effects in micronized form is a high-tech, specially milled form glibenclamide, which allows the drug will be absorbed from the gastrointestinal tract.Due to earlier attainment of maximum glibenclamide plasma concentration, hypoglycemic effect substantially corresponds in time to lift the glucose concentration in the blood plasma after a meal that makes the effect of the drug softer and more physiological. The duration of the hypoglycemic action of glibenclamide envy dose and can last up to 24 hours . Pharmacokinetics When administered glibenclamide is rapidly and almost completely absorbed. Simultaneous food intake does not significantly affect the absorption of glibenclamide. Full release of micronized active agent occurs within 5 minutes. Time to maximum concentration -. 1-2 hours Connection with the plasma protein is 98%. Glibenclamide is completely metabolized in the liver with the formation of two inactive metabolites, one of which is excreted by the kidneys, the other – the bile. The half-life following oral administration -. 2-5 hours in patients with impaired liver function the elimination of the active substance from the plasma is slowed down. In patients with renal insufficiency – compensatory increases the excretion of metabolites in the bile. When creatinine clearance ≥ 30 ml / min, the total elimination of remains unchanged, in severe renal insufficiency glibenclamide possible accumulation in the body.
Type 2 diabetes as monotherapy or in combination therapy with other oral hypoglycemic agents other than sulfonylurea derivatives and Glinides.
– Hypersensitivity to glibenclamide and / or other components of the drug;
– hypersensitivity to cross-reactions may occur other sulfonylureas, sulfonamides, diuretic (diuretic) means of containing in the molecule a sulfonamide group, and probenecid, that is to.. ;
– type 1 diabetes,
– diabetic ketoacidosis, diabetic precoma and coma;
– state after pancreatic resection;
– severe hepatic insufficiency,
– severe renal insufficiency (creatinine clearance <30 mL / min);
– decompensation of carbohydrate metabolism in infectious diseases, burns, trauma or after major surgery, when shown holding insulin;
– ileus, gastroparesis;
– hereditary lactose intolerance, lactase deficiency or malabsorption syndrome of glucose and lactose.
– deficiency of glucose-6-phosphate dehydrogenase;
– pregnancy and lactation
– children under 18 years (effectiveness and safety have been studied).
– thyroid disease (with impaired function);
– feverish syndrome
– cerebral atherosclerosis;
– hypofunction of the anterior pituitary and adrenal cortex;
– chronic alcoholism; acute alcohol intoxication;
– state, accompanied by malabsorption of food and the development of hypoglycemia;
– older age (over 70 years) due to the risk of hypoglycemia.
Pregnancy and lactation
Use of the drug Manin ® 1.75 during pregnancy and lactation is contraindicated. When pregnancy occurs the drug should be discontinued.
Dosage and administration
The dose depends on the age, severity of diabetes, blood glucose fasting and 2 hours after a meal.
The initial dose of the drug5 is 1-2 tablets (1.75 mg – 3.5 mg) 1 time per day. If the initial dose does not result in the achievement of adequate metabolic control, dose should be phased increase under medical supervision. Increasing the dose should be made at intervals of a few days up to one week, until the desired therapeutic dose, which must not exceed the maximum.
The drug should be taken before meals, with liquid squeezed small amount of liquid. Daily dose is up to 2 tablets should be taken one time a day – in the morning just before breakfast. Higher doses are divided into a morning and an evening reception in the ratio of 2:. 1
If you forget one dose, the next dose should be taken at the usual time, while not allowed to take a higher dose.
Elderly, debilitated patients or patients with reduced power, as well as suffering from severely impaired renal or hepatic function starting and maintenance dose should be reduced due to the risk of hypoglycemia.
Translation from other hypoglycemic agents:
Go with other hypoglycemic drugs to the should be initiated under the supervision of a physician with 1-2 tablets of the per day (1.75 mg – 3.5 mg), gradually increasing the dose to the desired therapeutic.
Possible side effects when using the are listed below in descending frequency of occurrence: often (> 1/100, <1/10), uncommon (> 1/1000, <1/100), rarely (> 1 / 10,000, <1/1000), very rare (<1/10000), including isolated reports. Violations of the metabolism and nutrition: Common: hypoglycemia (hunger, hyperthermia, tachycardia, drowsiness, weakness, skin moisture, violation coordination of movements, tremor, general anxiety, anxiety, headache, transient neurological disorders (eg, visual disturbances and speech, the appearance of paresis or paralysis or changed perception of sensation); weight gain; disorders of the gastrointestinal tract: Uncommon: nausea , a feeling of heaviness in the stomach, belching, vomiting, abdominal pain, diarrhea, “metallic” taste in the mouth; Violation of the liver and biliary tract: Very andriol side effects rare: a temporary increase in activity of “liver” enzymes – intrahepatic cholestasis, hepatitis, by the Violations immune system: Uncommon: pruritus, urticaria, purpura, petechiae, increased photosensitivity. Very rare: generalized allergic reactions, accompanied by skin rash, arthralgia, fever, jaundice and proteinuria; allergic vasculitis; anaphylactic shock. Violations of the blood and lymphatic system: Rare: thrombocytopenia Very rare: leucopenia, erythropenia, agranulocytosis; in a few cases: pancytopenia, hemolytic anemia. Others: Very rare: blurred vision, and accommodation disorders, increased diuresis, transient proteinuria, hyponatremia, “precipitates a effect” (disulfiramopodobnyh reaction) when taking alcohol (the most frequent signs of effects: nausea, vomiting, abdominal pain, feeling the heat of the skin of the face and upper body, tachycardia, dizziness, headache). Cross allergic to probenecid, sulfonylureas, sulfonamides, diuretics (diuretic) products containing in the molecule a sulfonamide group.
Overdose Symptoms: hypoglycemia (hunger, hyperthermia, tachycardia, drowsiness, weakness, moisture skin, incoordination, tremors, generalized anxiety, anxiety, headache, transient neurological disorders (eg, visual disturbances and speech manifestation of paresis or paralysis or altered perception of sensations) with the progression of hypoglycemia may lose the patient self-control and awareness, the development of hypoglycemic coma.. Treatment: hypoglycemia mild to be taken into a piece of sugar, food or drinks high in sugar (jam, honey, a glass of sweet tea). In unconsciousness must enter intravenous glucose (40 ml -. 80 ml 40% dextrose (glucose), then 5-10% dextrose infusion solution can then enter additional glucagon 1 mg intravenously (subcutaneously or intramuscularly) If the patient does not come to consciousness. that this measure can be repeated, it may require more intensive therapy.
Interaction with other drugs
Increased hypoglycemic effect of the drug is possible at the same time taking with angiotensin converting enzyme inhibitors, anabolic agents and male sex hormones, other oral hypoglycemic agents (eg, acarbose, biguanides) and insulin azapropazone, nonsteroidal anti-inflammatory drugs ( NSAIDs), beta blockers, quinolone derivatives, chloramphenicol, clofibrate and its analogs, derivatives of coumarin, disopyramide, fenfluramine, antifungal drugs (miconazole, fluconazole), fluoxetine, monoamine oxidase inhibitors, p-aminosalicylic acid, pentoxifylline (in large doses administered parenterally) perhexiline, pyrazolone derivatives, phosphamide (e.g., cyclophosphamide, ifosfamide, trofosfamide), probenecid, salicylates, sulfonamides, and tetracyclines tritokvalinom.
Acidifying urine agents (ammonium chloride or calcium chloride) enhance the effect of the andriol side effects by reducing its degree of dissociation and increasing its reabsorption.
The hypoglycemic effect of the can be reduced while the use of barbiturates, isoniazid, diazoxide, glyukortikosteroidami, glucagon, nicotinate (in high doses), phenytoin, phenothiazines, rifampin, thiazide diuretics, acetazolamide, . oral contraceptives and estrogens, iodine-containing drugs thyroid hormones, sympathomimetic agents, blockers “slow” calcium channels, lithium salts
antagonists H 2 receptors may attenuate the one hand, and on the other – to enhance the hypoglycemic effect of the. Pentamidine in rare cases can cause severe decrease or increase in blood glucose levels.
It may intensify or weaken the action of coumarin derivatives.
In addition to increasing hypoglycemic effect of beta-blockers, clonidine, guanethidine and reserpine, and drugs with a central mechanism of action, could weaken the sense of harbingers of the symptoms of hypoglycemia.
During treatment with Manin ® 1.75 must be complied with a doctor’s recommendation to comply with diet and self-blood glucose concentrations.
Prolonged abstinence from food, insufficient supply the body with carbohydrates, intense exercise, diarrhea or vomiting are the risk of hypoglycemia.
Simultaneous medications that have effects on the central nervous system, lowers blood pressure (including beta-blockers), as well as autonomic neuropathy may mask the symptoms of hypoglycemia.
in elderly patients, the risk of hypoglycemia is somewhat higher, so the need for a more careful selection of dose and regular monitoring of the glucose concentration in the blood of fasting and after meals, especially at the beginning of treatment.
Alcohol can provoke the development of hypoglycemia, as well as the development of “precipitates a ‘effect (nausea, vomiting, abdominal pain, feeling of facial skin hot and upper body, tachycardia, dizziness, headache), so you should abstain from drinking alcohol during treatment with.
Large surgery and trauma, extensive burns, infections with fever syndrome may require the cancellation of oral hypoglycemic drugs and insulin destination.
during treatment, not recommended for prolonged exposure to the sun.
Effects on ability to drive vehicles and management mechanisms
During treatment must be careful when driving and other potentially hazardous activities that require concentration and speed of psychomotor reactions. propionaat