Repaglinide - instructions for use, analogs, reviews and release forms (tablets of 0.5 mg, 1 mg and 2 mg) of the drug for the treatment of non-insulin-dependent diabetes mellitus in adults, children and pregnancy. Composition and alcohol

In this article, you can read the instructions for using the drug Repaglinide. There are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Repaglinide in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Repaglinide in the presence of existing structural analogs. Use for the treatment of non-insulin-dependent diabetes mellitus type 2 in adults, children, as well as during pregnancy and lactation. The composition of the drug and its interaction with alcohol.

Repaglinide - oral hypoglycemic agent. Rapidly reduces blood glucose levels by stimulating the release of insulin from the functioning beta cells of the pancreas. The mechanism of action is associated with the ability to block adenosine triphosphate (ATP) dependent channels in the membranes of beta cells by acting on specific receptors, which leads to depolarization of cells and the opening of calcium channels. As a result, an increased influx of calcium induces insulin secretion by beta cells.

After taking Repaglinide, an insulinotropic response to food intake is observed for 30 minutes, which leads to a decrease in blood glucose. During periods between meals there is no increase in insulin concentration. In patients with type 2 diabetes mellitus (insulin-independent), when taking Repaglinide in doses from 500 mcg to 4 mg, a dose-dependent decrease in blood glucose is noted.

Composition

Repaglinide + auxiliary substances.

Pharmacokinetics

After ingestion, repaglinide is rapidly absorbed from the gastrointestinal tract (GIT), with the maximum concentration in the blood being reached 1 hour after admission, then the level of repaglinide in the plasma decreases rapidly and after 4 hours becomes very low.There were no clinically significant differences in the pharmacokinetic parameters of repaglinide when taken directly before meals, 15 and 30 minutes before meals or on an empty stomach. Binding to plasma proteins is more than 90%. Repaglinide is almost completely biotransformed in the liver with the formation of inactive metabolites. Repaglinide and its metabolites are excreted mainly with bile, less than 8% with urine (in the form of metabolites), less than 1% with feces (unchanged).

Indications

• non-insulin-dependent diabetes mellitus (type 2 diabetes mellitus).

Forms of release

Tablets 0.5 mg, 1 mg and 2 mg.

Instructions for use and dosing regimen

The dosage regimen is set individually, choosing the dose in order to optimize the glucose level.

The recommended initial dose is 500 μg. Increase in the dose should be carried out no earlier than in 1-2 weeks of continuous intake, depending on the laboratory parameters of carbohydrate metabolism.

Maximum doses: single dose - 4 mg, daily - 16 mg.

After applying another hypoglycemic drug, the recommended initial dose is 1 mg.

Take before each main meal.The optimal time for taking the drug is 15 minutes before a meal, but you can take it 30 minutes before meals or just before meals.

Side effect

• influence on carbohydrate metabolism - hypoglycemic conditions (pallor, increased sweating, palpitations, sleep disorders, tremor);
• fluctuations in blood glucose levels can cause temporary visual impairment, especially at the beginning of treatment (noted in a small number of patients and did not require drug withdrawal);
• stomach ache;
• diarrhea, constipation;
• nausea, vomiting;
• increased activity of hepatic enzymes;
• allergic reactions: itching, erythema, urticaria.

Contraindications

• type 1 diabetes mellitus (insulin-dependent);
• diabetic ketoacidosis (including with coma);
• severe renal dysfunction;
• severe violations of liver function;
• concomitant treatment with drugs inhibiting or inducing CYP3A4;
• pregnancy (including planned) and lactation (breastfeeding);
• hypersensitivity to repaglinide.

Application in pregnancy and lactation

The use of repaglinide during pregnancy and during lactation is contraindicated.

In experimental studies, it has been established that there is no teratogenic effect, but when used in high doses in rats at the last stage of pregnancy, embryotoxicity was observed, a developmental disorder of the limbs in the fetus.

Repaglinide is excreted in breast milk.

Use in children

Application in childhood is not described.

special instructions

With liver or kidney disease, extensive surgery, after a recent illness or infection, a decrease in the effectiveness of Repaglinide is possible.

Use with caution in patients with kidney disease.

In weakened patients or in low-nutrition patients, Repaglinide should be taken at the minimum initial and maintenance doses. To prevent hypoglycemic reactions in this category of patients, the dose should be selected with caution.

The resulting hypoglycemic conditions are usually moderate to severe reactions and are easily stopped by the intake of carbohydrates. In severe conditions, there may be a need for intravenous glucose. The likelihood of such reactions depends on the dose, nutrition, intensity of physical activity, stress.

It should be borne in mind that beta-adrenoblockers can mask the symptoms of hypoglycemia.

During the treatment period, patients should refrain from drinking alcohol, since ethanol can enhance and prolong the hypoglycemic effect of Repaglinide.

Impact on the ability to drive vehicles and manage mechanisms

Against the background of the use of Repaglinide should evaluate the appropriateness of driving a car or practicing other potentially dangerous activities.

Drug Interactions

Strengthening the hypoglycemic effect of Repaglinide is possible with the simultaneous use of monoamine oxidase (MAO) inhibitors, nonselective beta adrenoblockers, angiotensin converting enzyme (ACE) inhibitors, salicylates, nonsteroidal anti-inflammatory drugs (NSAIDs), octreotide, anabolic steroids, ethanol.

Reducing the hypoglycemic effect of Repaglinide is possible with the simultaneous use of hormonal contraceptives for oral administration, thiazide diuretics, glucocorticosteroids (GCS), danazol, thyroid hormones, sympathomimetics (when prescribing or canceling these drugs, you need to carefully monitor the state of carbohydrate metabolism).

With the simultaneous use of repaglinide with drugs that are mainly derived from bile, the potential for interaction between them should be considered.

In connection with available data on the metabolism of repaglinide with CYP3A4 isoenzyme, possible interaction with CYP3A4 inhibitors (ketoconazole, intraconazole, erythromycin, fluconazole, mibefradil) should be considered, leading to an increase in plasma repaglinide level. Inductors CYP3A4 (including rifampicin, phenytoin) can reduce the concentration of repaglinide in plasma. Since the degree of induction is not established, the simultaneous use of repaglinide with these drugs is contraindicated.

Analogues of the drug Repaglinide

Structural analogs for the active substance:

• Diaglinide;
• Iglynide;
• Novonorm.

Analogues of the drug Repaglinide on the pharmacological group (hypoglycemic synthetic and other agents):

• Avandia;
• Adebit;
• Acarbose;
• Antidiab;
• Arfazetine;
• Astroson;
• Bagomet;
• Bethanase;
• Bukarban;
• Victoria;
• Vildagliptin;
• Vipidia;
• Galvus;
• Hillemal;
• Glybenez;
• Glibenclamide;
• Gliclazide;
• Glicon;
• Glimepiride;
• Gliminfor;
• Gliiformin;
• Glucophage;
• Guarem;
• Diabeton;
• Diameter;
• Diastabol;
• Iglynide;
• Kselevia;
• Lysumia;
• Maninil;
• Metformin;
• Minidiab;
• Movoglecken;
• Nateglinide;
• OngliSa;
• Pioglar;
• Pioglit;
• Reclild;
• Rosiglitazone;
• Saxenda;
• Satex;
• Siofor;
• Sofamet;
• Statiglyn;
• Tragenta;
• Trulisiti;
• Formethine;
• Formin;
• Forsiga;
• Chloropropamide;
• Blueberries are ordinary shoots;
• Euglucon;
• Yuglin;
• Januvia;
• Yasitara.

Review of the endocrinologist

Repaglinide drug I receive some of the patients suffering from type 2 diabetes. Single and daily doses to each patient I select individually and adjust them, constantly monitoring the level of glucose in the blood. It is very good that many people with diabetes have their own personal glucometers, which makes it easier to assess the dynamics of glycemia during dose selection and further during treatment. Repaglinide tolerance is good. I do not remember that one of the patients taking it constantly complained of more or less pronounced side effects.

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