Pranstad: Non-insulin-dependent type 2 diabetes medicine

2021-06-21 03:58 AM

Pranstad 1 is used as an adjunct to diet and exercise only in the treatment of type 2 (non-insulin-dependent) diabetes mellitus for patients with high blood glucose uncontrolled by diet and exercise.

Producer

Stellapharm J.V.

Ingredient

Each tablet: Repaglinide 1mg.

Describe

Tablets are round, white, one side engraved, the other smooth can be broken in half.

Pharmacodynamic

Pharmacotherapeutic group: Antidiabetic drugs; other hypoglycemic agents, except insulin.

ATC code: A10BX02

Repaglinide lowers blood glucose levels by stimulating insulin secretion from the pancreas. This effect is dependent on islet beta-cell function.

Insulin release is glucose-dependent and decreases when glucose levels are low.

Repaglinide closes ATP-dependent potassium channels in beta cell membranes by binding at specific sites. The closure of the potassium channel causes beta cell depolarization, which leads to the opening of calcium channels. The result of increased calcium influx induces insulin secretion. The ion channel mechanism is highly tissue-selective with a low affinity for cardiac and skeletal muscle.

Pharmacokinetics

Repaglinide is rapidly absorbed from the gastrointestinal tract, with peak plasma concentrations being achieved within 1 hour. The average bioavailability is about 60%.

Repaglinide is highly protein bound to plasma and has a plasma half-life of about 1 hour. Repaglinide is metabolized almost entirely in the liver via the cytochrome P450 isoenzyme system CYP2C8 and CYP3A4. Inactive metabolites are eliminated via bile. In patients with renal impairment (creatinine clearance less than 40 ml/min) or chronic liver disease, plasma repaglinide concentrations are higher and the elimination half-life is longer.

Indications and uses

Pranstad 1 is used as an adjunct to diet and exercise alone in the treatment of type 2 (non-insulin-dependent) diabetes mellitus in patients with high blood glucose not controlled by diet and exercise. mere sex.

Pranstad 1 can be combined with metformin in patients with high blood glucose not adequately controlled by diet, exercise, and monotherapy with metformin, a sulfonylurea, repaglinide, or a thiazolidinedione.

Dosage and Administration

Oral use 15 minutes before each meal, but it can range from 30 minutes before a meal to just before a meal.

Starting dose

For previously treatment-naive patients or with an HbA1C < 8%: A dose of 0.5 mg should be initiated before a meal.

For patients who have been treated with hypoglycemic agents and have HbA1C ≥ 8%: Initial dose is 1-2 mg before meals.

Dose adjustment

Dosage adjustment should be determined by blood glucose response, usually fasting blood glucose.

The pre-meal dose should be doubled to 4 mg until the blood glucose level is satisfactory. Assess response at least one week after each dose adjustment.

The recommended dose range is 0.5 mg to 4 mg. Pranstad 1 can be taken before meals 2, 3, or 4 times/day depending on the patient's meal pattern. The maximum daily dose is 16 mg.

The patient is taking other antidiabetic drugs

Patients can be switched directly from other oral antidiabetic agents to repaglinide. The maximum starting dose for switching to repaglinide is 1 mg before the main meal.

Combination with metformin

The dose of each drug should be adjusted to control blood glucose, each drug should be used at the lowest effective dose.

Special patient group

Patients with severe renal impairment (creatinine clearance 20-40 mL/min) should initiate repaglinide at a dose of 0.5 mg, after which the dose should be adjusted carefully.

There are no clinical studies in children and adolescents < 18 years of age or in patients > 75 years of age. Therefore, it is not recommended for this group of patients.

Overdose

Manifestations Acute overdosage of repaglinide is mainly hypoglycemia.

Symptoms of hypoglycaemia without loss of consciousness or neurotoxicity: Administer glucose immediately and adjust the dose and/or diet. Patients should be closely monitored for at least 24 to 48 hours, as hypoglycemia may recur after apparent clinical recovery. There is no evidence that repaglinide is removed by hemodialysis.

Severe hypoglycemia with coma, convulsions, or neurasthenia rarely occurs, requiring emergency care and immediate hospitalization. If the patient is diagnosed or suspected to be in a hypoglycemic coma, give a rapid intravenous injection of glucose solution (50% concentration). Then continue infusion of a more dilute glucose solution (10% concentration) at a rate that can maintain blood glucose levels above 100 mg/dL.

Contraindications

The patient is hypersensitive to the drug.

Patients with type 1 diabetes.

Diabetic patients complicated by acute or chronic metabolic acidosis, including diabetic ketoacidosis, with or without coma; In this case, insulin must be used.

Use in pregnant and lactating women

Pregnant

There are no studies on the safety of repaglinide in pregnant women, so repaglinide should be used during pregnancy only when clearly needed.

Abnormal blood glucose levels during pregnancy may be associated with an increased incidence of birth defects, and insulin is recommended as an alternative to repaglinide during pregnancy to maintain optimal blood glucose control.

Breastfeeding Women

Because of the potential for repaglinide to cause hypoglycemia and possible bone changes in the nursing infant, the drug should be discontinued or breastfeeding should be discontinued, taking into account the importance of the drug to the mother. If repaglinide is discontinued and the diet is not sufficient to control blood glucose, insulin should be substituted.

Interactive

Drugs that affect liver enzymes

Co-administration of repaglinide with drugs that induce CYP3A4 or CYP2C8 isoenzymes such as troglitazone, rifampin, barbiturates, carmabazepine may theoretically increase the metabolism of repaglinide.

Co-administration of repaglinide with CYP2C8 isoenzyme inhibitors, such as gemfibrozil, trimethoprim, or montelukast, may increase repaglinide plasma concentrations.

Protein-binding drugs

Salicylates or other nonsteroidal anti-inflammatory drugs, sulfonamides, probenecid, chloramphenicol, oral anticoagulants (such as warfarin), monoamine oxidase inhibitors, HMG-CoA reductase inhibitors, beta-adrenergic blockers. When initiating or discontinuing these agents while a patient is receiving repaglinide, the patient should be monitored for signs of hypoglycemia or loss of glycemic control.

Other drugs

Drugs that cause hyperglycemia and may affect blood glucose control in patients with diabetes include Corticosteroids, niacin, thiazide, and other diuretics, oral contraceptives, and sympathomimetics. sympathomimetics, hyperthyroidism, estrogens, phenytoin, phenothiazines, calcium channel blockers, and isoniazid.

Incompatibility

Due to the absence of incompatibility studies, this drug should not be mixed with other medicinal products.

Side effects

Frequent

Metabolism: Hypoglycaemia.

Respiratory: Upper respiratory tract infection, sinusitis, rhinitis, bronchitis.

Gastrointestinal: Nausea, diarrhea.

Musculoskeletal: Joint pain, back pain.

Nervous: Headache.

Less common

Digestion: Constipation, vomiting, dyspepsia.

Other: Paresthesia, chest pain, urinary tract infection, allergies.

Caution

Repaglinide should not be used with NPH-insulin.

All hypoglycemic agents, including repaglinide, have the potential to cause hypoglycemia.

Hepatic impairment may cause elevated blood levels of repaglinide and may impair gluconeogenesis, both of which increase the risk of severe hypoglycemia.

Elderly, debilitated, or malnourished patients and adrenal, hepatic, pituitary, or severe renal impairment are particularly susceptible to the hypoglycemic effect.

Symptoms of hypoglycaemia are difficult to see in the elderly, taking beta-adrenergic blockers. Hypoglycaemia usually occurs when there are not enough calories in the body, after heavy or prolonged physical activity, drinking alcohol, or taking multiple medications to lower blood glucose.

When a patient is stabilized on a diabetes regimen under stress such as fever, trauma, infection, or surgery, loss of glycemic control can occur. At this point, repaglinide should be discontinued and insulin replaced.

Patients should be careful to avoid hypoglycemia while driving. This is especially important in people who have difficulty recognizing the signs of hypoglycaemia or have frequent episodes of hypoglycemia. Driving should be considered in these cases.

Preservation

In sealed packaging, dry place. The temperature should not exceed 30oC.

Presentation and packaging

Tablets: Box of 3 blisters x 10 tablets, box of 6 blisters x 10 tablets.