Nateglinide - instructions for use, dose, side effects, contraindications

Clinical and pharmacological group: & nbsp

Hypoglycemic synthetic and other agents

Included in the formulation

Starlix

pills inwards

Novartis Pharma AG Switzerland

АТХ:

A.10.B.X.03 Nateglinide

Pharmacodynamics:

Restores early secretion of insulin, which leads to a decrease in postprandial glucose concentration in the blood and glycated hemoglobin (HbA1c).

Under the influence of nateglinide taken before meals, the early (or first) phase of insulin secretion is restored. The mechanism of this phenomenon is the rapid and reversible interaction of nateglinide with K⁺ATP-dependent channels of pancreatic β-cells. The selectivity of nateglinide in relation to K⁺ATP-dependent channels of β-cells of the pancreas are 300 times greater than those for the channels of the heart and blood vessels.

Nateglinide, unlike other oral hypoglycemic agents, causes pronounced insulin secretion within the first 15 minutes after ingestion, thereby smoothing postprandial fluctuations ("peaks") of blood glucose concentration. In the next 3-4 hours, insulin levels return to baseline, thus avoiding the development of postprandial hyperinsulinemia, which can lead to delayed hypoglycemia.

The secretion of insulin by β-cells of the pancreas caused by nateglinide depends on the level of glucose concentration in the blood, that is, as the concentration of glucose decreases, the secretion of insulin decreases.Conversely, simultaneous intake of food or infusion of glucose solution leads to a marked increase in the secretion of insulin.

Pharmacokinetics:

Nateglinide is rapidly absorbed and stimulates the secretion of insulin in the pancreas for 20 minutes after oral administration. A rapid rise in plasma insulin concentration with a peak level of about 1 hour after admission and a decrease to baseline after 4 hours after admission is observed when nateglinide is administered 3 times daily before meals.

Indications:

As a monotherapy for lowering blood glucose levels in patients with diabetes mellitus type 2 (insulin-independent diabetes), in which glycemic levels are not controlled by diet and exercise and which have not been treated for a long time with other hypoglycemic agents.

Nateglinide is also indicated for therapy in combination with metformin in patients with inadequate glycemic control against metformin (substitute metformin nateglinide is not recommended).

ICD-10

XV.O20-O29.O24.1 An earlier insulin-dependent diabetes mellitus

IV.E10-E14.E11.9 Non-insulin-dependent diabetes mellitus without complications

IV.E10-E14.E11.8 Non-insulin-dependent diabetes mellitus with unspecified complications

IV.E10-E14.E11.7 Non-insulin-dependent diabetes mellitus with multiple complications

IV.E10-E14.E11.6 Non-insulin-dependent diabetes mellitus with other specified complications

IV.E10-E14.E11.5 Non-insulin-dependent diabetes mellitus with peripheral circulatory disorders

IV.E10-E14.E11.4 Non-insulin-dependent diabetes mellitus with neurological complications

IV.E10-E14.E11.3 Non-insulin-dependent diabetes mellitus with eye damage

IV.E10-E14.E11.2 Non-insulin-dependent diabetes mellitus with kidney damage

IV.E10-E14.E11.1 Non-insulin-dependent diabetes mellitus with ketoacidosis

IV.E10-E14.E11.0 Non-insulin-dependent diabetes mellitus with coma

IV.E10-E14.E11 Non-insulin-dependent diabetes mellitus

Contraindications:

Hypersensitivity, diabetes type 1, diabetic ketoacidosis (in this case, insulin treatment is indicated). Children under 18 years of age, pregnancy, breast-feeding.

Carefully:Elderly age, renal and hepatic insufficiency.

Pregnancy and lactation:

FDA recommendation category C.

Contraindicated in pregnancy and lactation.

Dosing and Administration:

At monotherapy - on 120-180 mg 3 times a day. When carrying out combined therapy - 60-120 mg 3 times a day.

Side effects:

Perhaps: the symptoms presumably indicative of the development of hypoglycemia - increased sweating, tremor, dizziness, increased appetite, palpitations, nausea, weakness, malaise (usually these phenomena were poorly expressed and easily stopped by the intake of carbohydrates).

Rarely: increased activity of liver enzymes in the blood (usually mild and transient), rash, itching, urticaria.

Laboratory disorders. There was an increase in the average concentration of uric acid in patients who received nateglinide monotherapy or a combination of nateglinide with metformin, monotherapy with metformin, or monotherapy with glyburide. The comparative difference with placebo was 0.017, 0.026, 0.017 and 0.011 mmol / L, respectively. The clinical significance of this phenomenon is unknown.

Hypoglycemia was relatively rare in all treatment regimens in clinical trials. Only 0.3% of patients nateglinide was canceled due to hypoglycemia. GIT symptoms, especially diarrhea and nausea, were no less frequent in patients who received a combination of nateglinide and metformin than patients who received only metformin.

Overdose:

Not described.

Interaction:

The risk of developing hypoglycemia with nateglinide (as well as other hypoglycemic drugs) is higher in elderly patients with a reduced body weight, with adrenal or pituitary insufficiency. Reducing the concentration of glucose in the blood can be triggered by taking alcohol, increased physical exertion, as well as the simultaneous intake of another hypoglycemic drug.

Simultaneous reception of beta-blockers can mask manifestations of hypoglycemia.

Special instructions:

Patients working with mechanisms and driving vehicles should take special precautions to prevent hypoglycemia.

Instructions

Nateglinide (Nateglinidum)