Characteristic
Oral hypoglycemic agent.
White or almost white powder. Molecular weight 452.6.
Pharmacology
It blocks ATP-dependent potassium channels in the membranes of functionally active beta-cells of the pancreatic islet apparatus, causes their depolarization and the opening of calcium channels, inducing insulin incretion. An insulinotropic response develops within 30 minutes after application and is accompanied by a decrease in blood glucose levels during meals (insulin concentration between meals does not increase).
In experiments in vivo and on animals, no mutagenic, teratogenic, carcinogenic effects and effects on fertility were detected.
Rapidly and completely absorbed from the gastrointestinal tract. Cmax is achieved after 1 hour and is 9.8; 18.3; 26 and 65.8 ng / ml after taking doses of 0.5; one; 2 and 4 mg, respectively; when taken with food, Cmax may decrease by 20%. Plasma levels rapidly decrease within 4 hours. Absolute bioavailability is 56%, plasma protein binding is very high (more than 98%), volume of distribution is 31 l (after intravenous administration to healthy volunteers). Almost completely biotransformed in the liver (oxidation and binding to glucuronic acid), forming inactive metabolites. T1 / 2 from the blood – 1 hour. It is excreted within 4-6 hours, mainly with bile through the gastrointestinal tract (90%) and with urine (less than 8%).Contraindications
Hypersensitivity, type 1 diabetes mellitus, diabetic ketoacidosis, diabetic precoma and coma, severe liver and / or kidney dysfunction; conditions requiring insulin therapy (including infectious diseases, major surgical interventions), pregnancy, breastfeeding.
Application restrictions
Feverish syndrome, alcoholism, chronic renal failure. It should not be prescribed to children and adolescents under 18 years of age, as well as to patients over 75 years of age (safety and efficacy in patients of these age categories have not been determined).
Use during pregnancy and lactation
Contraindicated in pregnancy.
The FDA fetal category is C.
At the time of treatment should stop breastfeeding.
Side effects of Repaglinide
Hypoglycemia, dyspepsia (nausea, abdominal pain; very rarely – diarrhea or constipation, vomiting), allergic reactions (skin rash, itching, urticaria); in some cases – liver dysfunction (transient increase in liver transaminase activity) and visual impairment (associated with fluctuations in glycemia levels).Interaction
Beta-blockers, ACE inhibitors, chloramphenicol, indirect anticoagulants (coumarin derivatives), NSAIDs, probenecid, salicylates, MAO inhibitors, sulfonamides, alcohol, anabolic steroids – enhance the effect. Calcium channel blockers, corticosteroids, diuretics (especially thiazides), isoniazid, high doses of nicotinic acid, estrogens, incl. as part of oral contraceptives, phenothiazines, phenytoin, sympathomimetics, thyroid hormones – weaken the effect.
Dosage and administration
Inside, 15-30 minutes before meals (usually 3 times a day before the main meals). The dose is selected individually. The initial dose is 0.5 mg. Dose increases are carried out no earlier than 1-2 weeks after the start of treatment, focusing on the level of glycemia. The maximum single dose is 4 mg, the daily dose is 16 mg. If the patient has been taking another oral hypoglycemic agent, or if the glycated hemoglobin level is greater than or equal to 8%, the recommended starting dose is 1 mg.
Buy Repaglinid
Price Repaglinid
Цена Репаглинид
Купить Репаглинид
Acheter Repaglinid
Prix Repaglinid
Comprar Repaglinid
Precio Repaglinid
