Diabeton MR tablets 60mg №30
Description for Diabeton MR tablets 60mg №30
Pharmacodynamics. Gliclazide - oral hypoglycemic agents, sulfonylureas, which differs from other similar compounds by the presence of a heterocyclic ring which contains nitrogen and has the endocyclic bond. Gliclazide lowers blood glucose by stimulating insulin secretion, β-cells of islets of Langerhans of the pancreas.
Increased postprandial insulin and C-peptide secretion is maintained even after 2 years of treatment. Gliclazide exhibits also gemovaskulyarnye properties.
Impact on insulinosekretsiyu. In patients with type II diabetes gliclazide restores I and phase II insulinosekretsii in response to glucose intake. Increase of insulin takes place in accordance with the food or glucose load.
Gemovaskulyarnye properties. Gliclazide reduces the risk of mikrotrombozov vessels through two mechanisms implemented during the development of diabetes complications:
partially inhibits adhesion and aggregation of platelets, reduces the number of markers of platelet activation (β-tromboglobulin, thromboxane B2);
affect the fibrinolytic activity of vascular endothelial (increases the activity of tissue plasminogen activator).
Pharmacokinetics. Gliclazide concentration in blood plasma increased progressively during the first 6 hours after admission, and then reaches a constant level (plateau), which is held 6-12 hours after application.
A single dose daily dose diabeton MR 60 mg provides effective concentration of gliclazide in plasma for 24 h. The individual variations are minor.
Gliclazide completely absorbed in the gastrointestinal tract. Food intake did not affect the rate and extent of absorption.
Observed linear relationship between the adopted dose of the drug to 120 mg and a concentration in blood plasma. Binding of gliclazide with the proteins of blood plasma is approximately 95%.
Gliclazide is metabolized primarily in the liver and excreted in the urine, less than 1% of the active substance is excreted in the urine in unchanged form. Active metabolites in plasma are absent.
Half-life of gliclazide is approximately 12-20 hours
The volume of distribution is approximately 30 liters.
diabetes mellitus type II (insulin-dependent) for inability to control blood glucose levels only by diet, exercise or weight loss.
for oral administration. Assigned only to adults. The daily dose ranges from 1 / 2 to 2 tablets per day (30-120 mg / day). The daily dose taken odinokratno during breakfast. Half a tablet or tablet (s) should be swallowed whole (do not crush or chew).
If the patient has forgotten to take pills, do not increase the dose the next day.
Like all hypoglycemic funds needed individual titration diabeton MR 60 mg depending on individual patient response to treatment (blood glucose and glycated hemoglobin HbAlc).
The initial dose and titration. The recommended starting dose is 30 mg (1 / 2 tablet per day). With effective control of blood glucose can continue treatment at this dose.
If necessary, increase the level of glycemic control daily dose can be increased to 60 mg (1 tablet), 90 mg (1.5 tablets) or 120 mg (2 tablets) once during breakfast. Increasing the dose recommended gradually at intervals of 1 month, except in cases where no marked decrease in blood glucose levels within 2 weeks of treatment. In such circumstances, the dose may be increased after 2 weeks of treatment.
Average daily dose is 1 tablet once a day during lunch for most patients from the very beginning of treatment.
The maximum recommended daily dose - 120 mg (2 tablets).
One tablet to modified release drug diabeton MR 60 mg equivalent to two tablets with modified release drug diabeton MR 30 mg.
Modified release tablet of the drug diabeton MR 60 mg can be shared, which allows to use the drug at a dose of 30 mg (1 / 2 tablets) and 90 mg (1.5 tablets).
Moving a patient with treatment preparation containing 80 mg of gliclazide, an appointment diabeton MR 60 mg modified release tablets: 1 tablet containing gliclazide 80 mg, equivalent to 1 / 2 tablets diabeton MR 60 mg. Need to carefully monitor blood counts during the transition to diabeton MR 60 mg.
Moving a patient with treatment with other oral hypoglycemic agents on diabeton MR 60 mg: diabeton MR 60 mg may be appointed instead of the other oral hypoglycemic agents. It must take into account the dosage and half-life of the latter. The transition period is generally not needed. You should begin with a dose of 30 mg followed by dose adjustment (see initial dose and titration).
In the transition from glucose-lowering drugs sulfonylurea with a longer half-life than diabeton MR 60 mg treatment interruption for several days may be needed to prevent the additive effect of two drugs and the development of hypoglycemia. Treatment with diabeton MR 60 mg starting dose of 30 mg / d (1 / 2 tablets), followed by dose adjustment in compliance with the rules that were described earlier (see above).
The simultaneous use of other antidiabetic drugs: diabeton MR 60 mg can be used in combination with biguanides, inhibitors of α-glucosidase and insulin. In the event that was not achieved adequate control of blood glucose in patients taking diabeton MR 60 mg can be started simultaneously with insulin therapy under close medical supervision.
For elderly patients (over 65) dosing regimen of the drug diabeton MR 60 mg is the same as for patients below the age of 65 years.
For patients with renal insufficiency mild to moderate severity dosing regimen of the drug diabeton MR 60 mg is the same as for patients with normal renal function, but the patient should be monitored carefully.
For patients belonging to the risk of development of hypoglycemia (see SPECIAL PRECAUTIONS and INTERACTIONS), the minimum recommended starting dose - 30 mg / day.
For patients with severe vascular disease (CHD, severe pathology of coronary arteries, diffuse vascular lesions), a minimum initial dose - 30 mg / day.
• Hypersensitivity to gliclazide, other sulfonylureas;
• sulfonamides or any component of the drug;
• insulin-dependent diabetes mellitus type I;
• diabetic precoma and coma, ketoacidosis;
• severe hepatic or severe liver or kidney failure;
• Simultaneous treatment miconazole;
• During pregnancy and lactation;
• Children's age.
based on the experiences of gliclazide and other derivatives sulfanimocheviny, you may experience side effects stated below.
Hypoglycemia. As with other sulfonylurea drugs, taking gliclazide may cause hypoglycemia due to irregular meals, especially if the meal is skipped.
The emergence of hypoglycemia may be accompanied by characteristic symptoms, such as: headache, heavy sensation of hunger, nausea, vomiting, weakness, sleep disturbance, anxiety, impaired concentration and reaction, depression, confusion, impaired vision and speech, aphasia, tremor, paresis, violation sensitivity, dizziness, tiredness, loss of self-control, delirium, seizures, shallow breathing, bradycardia, drowsiness and loss of consciousness that can lead to coma with a fatal outcome.
In addition, there may be such symptoms adrenergic kontrregulyatsii as excessive sweating, clammy skin, feeling of anxiety, tachycardia, hypertension, heart feeling, angina, arrhythmia.
Usually the symptoms of hypoglycemia disappear after carbohydrate intake (sugar). However, artificial sugar (saharozamenitali) ineffective. Experience of using other drugs sulfonylurea indicates that the state of hypoglycemia may occur repeatedly, even if the first aid measures are effective.
If an episode of hypoglycemia, severe or prolonged, the patient needs emergency care or hospitalization, even if his condition temporarily controlled by the Admission of sugar.
Other side effects
From the gastrointestinal tract: abdominal pain, nausea, vomiting, dyspepsia, diarrhea and constipation. Compliance with recommendations for the drug during a breakfast will help avoid or minimize the occurrence of these manifestations.
Rarely observed following side effects:
Skin and subcutaneous tissue: rash, itching, urticaria, erythema, rash makropapuleznaya, buleznaya rash.
From the blood system (are rare): anemia, thrombocytopenia, leukopenia, granulocytopenia. Typically, these effects disappear after discontinuation of treatment.
From the hepatobiliary system: improving liver enzymes (ALT, AST, ALP), hepatitis (isolated cases). In case of jaundice, drug treatment should be discontinued.
Mentioned side effects usually disappear after discontinuation of the drug.
On the part of the vision: temporary impairment may occur, especially early in treatment, due to changes in blood glucose levels.
Violations that may occur when using any drug sulfonylurea: erythropenia cases, agranulocytosis, hemolytic anemia, pancytopenia, and allergic vasculitis. In the application of sulfonylurea drugs have also been described increase of liver enzymes, and even abnormal liver function (eg with cholestasis and jaundice) and hepatitis, the manifestations of which decreased after discontinuation of these drugs or in rare cases lead to life-threatening liver failure
Hypoglycemia. Using the drug sulfonylurea hypoglycemia may occur (see ADVERSE REACTIONS). This drug should be given only to patients who are able to eat regularly (including breakfast). It is important to regularly take carbohydrates, because the increased risk of hypoglycemia occurs when meals are late, or if an inadequate amount of this food is low in carbohydrates.
Factors povyshayutschie risk of hypoglycemia:
• the patient refuses or fails to implement the recommendations of a physician (especially elderly patients);
• inadequate, irregular meals, periods of fasting and diet changes;
• an imbalance between physical exercise and consumption of carbohydrates;
• renal failure;
• severe hepatic impairment;
• overdose of drugs;
• Certain disorders of the endocrine system: impaired function of the thyroid gland, and adrenal insufficiency gipopituitrizm;
• simultaneous use of certain medicines (see Interactions).
Renal and hepatic impairment: pharmacokinetics and / or pharmacodynamics of gliclazide may vary in patients with hepatic and severe renal insufficiency. Hypoglycemic episodes in these patients may be prolonged, therefore, need appropriate treatment.
Deterioration of glycemic control in patients receiving hypoglycemic medications may be caused by infection, fever, trauma or surgery. In some cases it may be that the appointment of insulin.
Hypoglycemic efficacy of any oral glucose-lowering means, including gliclazide, can change over time. This may be due to progression of disease severity or in connection with a decrease in response to treatment. This phenomenon is known as secondary failure, which differs from the primary disease, when drugs are ineffective from the start of treatment. Before making a conclusion about the development of secondary failure in a patient, you must validate compliance with the dose and the patient's diet.
Laboratory indicators: to evaluate the control of blood glucose levels recommended by determining the level of glycated hemoglobin (or level of fasting blood glucose).
Patients with G6 FDG-failure application sulfonylurea drugs can cause hemolytic anemia. Such patients gliclazide should be used with caution and to consider the appointment of alternative therapy.
The composition of the drug is lactose, so patients with congenital intolerance galactose malabsorption syndrome, glucose and galactose lactase deficiency Lappa is not recommended to assign the drug.
Children. Gliclazide is not recommended to be used in children because of the lack of studies in this patient
Use during pregnancy and lactation. Experience in use of the drug diabeton MR 60 mg in pregnancy is missing. When planning or when a pregnant woman needs to be translated from oral hypoglycemic agents to insulin.
Diabeton MR 60 mg is contraindicated during breastfeeding because of the possibility of occurrence of hypoglycemia in the child.
Ability to influence the reaction rate in the management of transport or working with other mechanisms. Patients should be aware of the symptoms of hypoglycemia, and be able to recognize them and when they occur to be careful while driving and working with different mechanisms, especially at the beginning of treatment.
In applying the drug, co-administration which can cause hypo-or hyperglycemia, it is necessary to warn patients about the need for careful monitoring of blood glucose during treatment. May be necessary correction doses hypoglycemic agents during and after treatment with these drugs.
Drugs, co-administration which may increase the risk of hypoglycemia:
Contraindicated for concurrent use of:
miconazole (for systemic use, the gel to oral) increases hypoglycemic effect with the possible development of symptoms of hypoglycemia and even a development of coma.
Not recommended by the simultaneous application of:
phenylbutazone (for systemic use) increases the hypoglycemic effect of sulfonylurea derivatives (replacing their relationship to plasma proteins and / or reduces their excretion);
Alcohol increases the risk of hypoglycemic reactions (due to the inhibition of compensatory reactions), which can lead to hypoglycemic coma. You should avoid alcohol and drugs containing alcohol.