DRUG TITLE

Prandin (Repaglinide)

Pharmacological action

Oral hypoglycemic drug. Rapidly lowers blood glucose levels by stimulating the release of insulin from functioning pancreatic β-cells. The mechanism of action is related to the ability to block ATP-dependent channels in the membranes of β-cells by affecting specific receptors, which leads to cell depolarization and opening of calcium channels. As a result, increased calcium influx induces insulin secretion by β-cells.

After taking Prandin (Repaglinide), insulinotropic response to a meal is observed within 30 min, which leads to a decrease in blood glucose levels. There is no increase in insulin concentration between meals. In patients with type 2 diabetes mellitus (insulin-independent), when taking repaglinide in doses from 500 µg to 4 mg, a dose-dependent decrease in blood glucose levels is observed.

Pharmacokinetics

After oral administration, Prandin (Repaglinide) is rapidly absorbed from the gastrointestinal tract, with Cmax reached 1 h after administration, then plasma levels of repaglinide rapidly decrease and become very low after 4 h. There were no clinically significant differences in pharmacokinetic parameters of repaglinide when taken immediately before meals, 15 and 30 minutes before meals or on an empty stomach.

Binding to plasma proteins is more than 90%.

Vd is 30 l (which is consistent with the distribution in the intercellular fluid).

Prandin (Repaglinide) is almost completely biotransformed in the liver to form inactive metabolites. Repaglinide and its metabolites are excreted mainly with bile, less than 8% - with urine (as metabolites), less than 1% - with feces (unchanged). T1/2 is about 1 h.

Contraindications to use

Hypersensitivity to repaglinide; type 1 diabetes mellitus, diabetic ketoacidosis, diabetic precoma and coma; infectious diseases, major surgical interventions and other conditions requiring insulin therapy; severe hepatic impairment; simultaneous use of gemfibrozil; pregnancy, breast-feeding period; age below 18 years and above 75 years.

With caution: with liver function abnormalities of mild to moderate degree, febrile syndrome, chronic renal insufficiency, alcoholism, general seriousness, malnutrition.

Use in pregnancy and lactation

The use of repaglinide in pregnancy is contraindicated. If it is necessary to use during lactation, breastfeeding should be discontinued.

Administration in liver dysfunction

It is contraindicated in severe hepatic dysfunction. Caution should be exercised when mild or moderate hepatic impairment exists.

Administration in impaired renal function

Caution should be exercised when using in chronic renal insufficiency,

Administration in children

Administration in children and adolescents under 18 years old is contraindicated due to lack of sufficient data concerning safety and efficacy of repaglinide in this group of patients.

Use in elderly patients

It is contraindicated in patients over 75 years old due to insufficient data on the safety and efficacy of repaglinide in this group of patients.

Indications for the active substance Prandin (Repaglinide)

Type 2 diabetes mellitus (when diet therapy, weight loss and physical activity are ineffective) in monotherapy or in combination with metformin or thiazolidinedione when satisfactory glycemic control cannot be achieved with repaglinide, metformin or thiazolidinedione monotherapy.

Dosing regimen

Oral. Used as an adjunct to diet and exercise to reduce blood glucose concentrations. The dosage regimen is established individually, selecting the dose in order to optimize glucose levels.

Recommended initial daily dose is 0.5 mg. Average daily dose is 12 mg. Maximum daily dose is 16 mg.