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Active ingredients
Glikvidon
Release form
Pills
Composition
1 tablet contains: Glikvidon 30 mg. Auxiliary substances: lactose monohydrate - 134.6 mg, dried corn starch - 70 mg, soluble corn starch - 5 mg, magnesium stearate - 0.4 mg.
Pharmacological effect
Hypoglycemic drug for oral use, a derivative of sulfonylurea II generation. It has pancreatic and extra-pancreatic effects. Stimulates insulin secretion, potentiating the glucose-mediated pathway of insulin formation. In animal studies, it has been shown that Glurenorm reduces insulin resistance in the liver and adipose tissue by increasing insulin receptors, as well as stimulating the insulin-mediated post-receptor mechanism. The hypoglycemic effect develops 60-90 minutes after ingestion, the maximum effect occurs after 2-3 h and lasts about 8-10 hours
Pharmacokinetics
Absorption After ingestion of a single dose of glycvidone (15 mg or 30 mg), the drug is rapidly and almost completely (80-95%) absorbed from the gastrointestinal tract, reaching a plasma concentration of 0.65 mcg / ml (range 0.12-2.14 mcg / ml). The average time to reach the Cmax drug in plasma is 2 hours and 15 minutes (range: 1.25–4.75 hours). The AUC0-∞ value is 5.1 mcg × h / ml (range: 1.5-10.1 mcg × h / ml). There are no differences in pharmacokinetic parameters in patients with diabetes and in healthy individuals. The distribution of Glycvidon has a high affinity for plasma proteins (> 99 %). There is no data on the possible passage of glycvidone or its metabolites through the BBB or the placenta. There are no data on the possibility of glycvidone penetration into breast milk. MetabolismGlycvidon is completely metabolized by the liver, mainly by hydroxylation and demethylation. Glycvidone metabolites do not have or have poorly expressed pharmacological activity compared with the original substance. ExcretionThe main part of the metabolites is excreted through the intestine. Only a small part of the metabolites is excreted by the kidneys. Studies have shown that after oral administration, about 86% of the isotope-labeled drug (14C) is excreted through the intestine. Regardless of the dose and route of administration, about 5% (as metabolites) of the amount of the drug administered is excreted by the kidneys.The level of elimination of Glurenorm by the kidneys remains minimal even with regular administration. T1 / 2 is 1.2 hours (in the range of 0.4-3.0 hours), the final T1 / 2 is approximately 8 hours (in the range of 5.7-9.4 hours). Pharmacokinetics in particular In clinical cases, elderly patients and middle-aged patients have similar pharmacokinetic indicators. Most of the drug is excreted through the intestines. There is evidence that the drug metabolism does not change in patients with liver failure. Glycvidon excretion by the kidneys is insignificant; the drug does not accumulate in patients with impaired renal function.
Indications
- diabetes mellitus type 2 in patients of middle and old age (with the ineffectiveness of diet therapy).
Contraindications
- type 1 diabetes; - diabetic acidosis, ketoacidosis, precoma and coma; - condition after resection of the pancreas; - acute intermittent porphyria; - severe hepatic failure; - some acute conditions (for example, infectious diseases or large surgical operations); - rare hereditary diseases such as galactosemia, lactase deficiency, lactose intolerance, glucose-galactose malabsorption; - pregnancy; - lactation period (breastfeeding period); - age up to 18 years (due to insufficiency of nnyh on efficacy and safety in this age group); - hypersensitivity to sulfonamides.
Precautionary measures
With caution, febrile syndrome; - thyroid disease (with impaired function); - deficiency of glucose-6-phosphate dehydrogenase; - alcoholism.
Use during pregnancy and lactation
There are no data on the use of glycvidon in women during pregnancy and breastfeeding. It is not known whether glykvidon or its metabolites penetrate into breast milk. In pregnant women with diabetes mellitus, careful monitoring of plasma glucose concentration is necessary. Reception of oral antidiabetic agents in pregnant women does not provide adequate control of the level of carbohydrate metabolism. Therefore, the use of the drug Glyurenorm during pregnancy and lactation is contraindicated. In case of pregnancy or when planning pregnancy during the use of the drug Glyurenorm, the drug should be canceled and switch to insulin.
Dosage and administration
The drug is used inside. You must comply with the recommendations of the doctor regarding the dose of the drug and diet. You should not stop taking the drug without consulting a doctor. The initial dose of Glurenorm is usually 1/2 tab. (15 mg) at breakfast. The drug must be taken at the beginning of a meal. After taking Glyurenorm, food intake should not be missed. If taking 1/2 tab. (15 mg) does not lead to adequate improvement, after consultation with the doctor, the dose should be gradually increased. If the daily dose of Glurenorm does not exceed 2 tab. (60 mg), it can be prescribed in 1 dose, during breakfast. When a higher dose is prescribed, the best effect can be achieved when taking a daily dose, divided into 2-3 doses. In this case, the highest dose should be taken at breakfast. Increasing the dose of more than 4 tab. (120 mg) / day usually does not lead to a further increase in efficacy. The maximum daily dose is 4 tab. (120 mg).
Side effects
From the hemopoietic system: thrombocytopenia, leukopenia, agranulocytosis. Metabolism: hypoglycemia. Nervous system: headache, dizziness, drowsiness, paresthesia, fatigue. angina, extrasystole, cardiovascular insufficiency, hypotension. On the part of the digestive system: loss of appetite, nausea, vomiting, constipation, diarrhea, discomfort in the abdomen, dry mouth, cholestasis. skin and subcutaneous tissue hormones: rash, pruritus, urticaria, Stevens-Johnson syndrome, photosensitization reaction. Others: chest pain.
Overdose
An overdose of sulfonylurea derivatives can lead to hypoglycemia. Symptoms: tachycardia, increased sweating, hunger, heartbeat, tremor, headache, insomnia, irritability, impaired speech and vision, motor restlessness and loss of consciousness. glucose (dextrose) or foods rich in carbohydrates. In severe hypoglycemia (loss of consciousness, coma), dextrose is administered IV. After the restoration of consciousness, the intake of easily digestible carbohydrates (in order to avoid the repeated development of hypoglycemia).
Interaction with other drugs
It is possible to increase the level of hypoglycemia with the simultaneous use of a , insulin and oral hypoglycemic agents. Beta-blockers, sympatholytics (including clonidine), reserpine and guanethidine may increase l hypoglycemic effect and at the same time to mask the symptoms of hypoglycemic. and phenytoin can also reduce the hypoglycemic effect of glycvidone. The potentiation or weakening of the hypoglycemic effect of glycvidone was isano when taking histamine H2 receptor blockers (cimetidine, ranitidine) and ethanol.
special instructions
Patients with diabetes should strictly follow the recommendations of the doctor. Especially careful control is needed when selecting a dose or when switching from another hypoglycemic drug. Oral hypoglycemic agents should not replace a therapeutic diet that allows you to control the patient's body weight. Skipping meals or non-compliance with the doctor's recommendations can significantly reduce the concentration of glucose in the blood and lead to loss of consciousness. When taking a pill before a meal, and not as recommended, at the beginning of a meal, the effect of the drug on the concentration of glucose in the blood is more pronounced, which increases the risk of hypoglycemia. If symptoms of hypoglycemia appear, you should immediately take food that contains sugar. In the case of conserved hypoglycemic state immediately seek vrachu.Fizicheskaya load can enhance hypoglycemic deystvie.Alkogol or stress may enhance or decrease the hypoglycemic effect derivatives sulfonilmocheviny.Primenenie sulfonylureas in patients suffering from deficiency of glucose-6-phosphate dehydrogenase deficiency can lead to hemolytic anemia. SinceGlurenorm is a sulfonylurea derivative, care must be taken when using the drug in patients with glucose-6-phosphate dehydrogenase deficiency and, if possible, it is necessary to make a decision to change the drug. One tablet of Glurenorm contains 134.6 mg of lactose (538.4 mg of lactose in the maximum daily dose). Patients with rare hereditary diseases, such as galactosemia, lactase deficiency, glucose-galactose malabsorption, should not take Glurenorm. Glycvidon is a short-acting sulfonylurea derivative and is therefore used in patients with diabetes mellitus type 2 with an increased risk of hypoglycemia, for example, in elderly patients and patients with impaired renal function. Because the glycvidon is not excreted by the kidneys only slightly, Glurenorm can be used in patients with renal impairment and diabetic nephropus iey. However, the treatment of patients with severe renal insufficiency should be carried out under close medical supervision. There is evidence that the use of glycvidone in patients with type 2 diabetes with concomitant liver disease is effective and safe. Only the elimination of inactive metabolites in such patients is somewhat delayed. However, prescribing the drug is not recommended for patients with diabetes mellitus and the concomitant severe abnormal liver function. During clinical studies, it was found that the use of Glyurenorm for 18 and 30 months did not lead to an increase in body weight, even cases of weight loss by 1-2 kg In comparative studies with other sulfonylurea derivatives, it was proved that patients taking Glurenorm for more than a year have no significant changes in body weight. Effect on the ability to drive vehicles and control mechanisms There is no data on the effect of the drug on the ability to drive vehicles and mechanisms. However, patients should be warned about such manifestations of hypoglycemia as drowsiness, dizziness, accommodation disturbance that may occur while taking the drug. Care must be taken when driving vehicles and machinery.In hypoglycemic conditions, the control of vehicles and machinery should be avoided.