Chloropropamide (Chlorpropamidum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Hypoglycemic synthetic and other agents

Included in the formulation
АТХ:

A.10.B.B.02   Chloropropamide

Pharmacodynamics:

The sulfonylurea derivative of the first generation, by reducing the threshold of stimulation of pancreatic β-cells by glucose stimulates insulin secretion, increases its release and the degree of binding to target cells. The hypoglycemic effect depends on the number of functioning β-cells.

Has hypolipidemic and antidiuretic effect.

Pharmacokinetics:

After oral administration, an empty stomach is absorbed up to 96% in the gastrointestinal tract. The maximum concentration in the blood plasma is achieved in 2-4 hours. The connection with plasma proteins is 98%.

Therapeutic effect develops 1 hour after taking and continues for 24 hours. Metabolism in the liver.

The half-life is 36 hours. Elimination by the kidneys, up to 30% unchanged.

Indications:

It is used for the treatment of diabetes mellitus II type in the absence of the effect of diet therapy. Used for diabetes insipidus, as well as for the treatment of diabetic microangiopathy in the initial stage.

ICD-10

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

IV.E20-E35.E23.2   Non-diabetes mellitus

IX.I70-I79.I79.2 *   Peripheral angiopathy in diseases classified elsewhere

Contraindications:

Diabetes I type (insulin-dependent), coma, ketoacidosis, individual intolerance, children under 18 years of age.

Carefully:

Concomitant diseases of the endocrine system affecting carbohydrate metabolism: adenohypophysis and adrenocortical insufficiency, dysfunction of the thyroid gland.

Pregnancy and lactation:

Recommendations for FDA - Category C. Contraindicated in pregnancy and lactation.

Dosing and Administration:

Inside for half an hour before meals to 0.25 g once a day in the morning. It is possible to increase the dose to 0.5 g before the normalization of glycemia.

The highest daily dose: 0.5 g.

The highest single dose: 0.5 g.

Side effects:

Central and peripheral nervous system: insomnia, paresthesia, emotional lability, impaired sensibility, paresis.

Hemopoietic system: pancytopenia, agranulocytosis, eosinophilia, hemolytic and aplastic anemia.

Respiratory system: dyspnoea.

The cardiovascular system: tachycardia, arterial hypotension.

Digestive system: loss of appetite, constipation, cholestatic jaundice.

Sense organs: impaired vision.

Musculoskeletal system: symptoms of lactic acidosis - cramps of the calf muscles.

Dermatological reactions: photosensitivity, late porphyria.

Allergic reactions.

Overdose:

Development of hypoglycemia.

Treatment: sugar inside, with loss of consciousness - intravenous injection of 40% dextrose solution.

Interaction:

Increase the concentration of the drug in the blood plasma inhibitors of the isoenzyme 3A4 cytochrome P450: ketoconazole, ciclosporin, erythromycin.

Reduced glycemic control while applying the drug to the thiazide diuretics, calcium channel blockers slow, lithium preparations, glucocorticoids, isoniazid, sympathomimetics, nicotinic acid, phenytoin, phenothiazines, thyroid hormones.

With simultaneous application with furosemide, a dose reduction is necessary.

With simultaneous use with drugs that inhibit bone marrow hematopoiesis, the risk of myelosuppression increases.

The use of alcohol (especially on an empty stomach) during treatment increases the concentration of lactic acid in the blood plasma and increases the risk of hypoglycemia.

Special instructions:

During pregnancy and lactation, the drug is canceled, the treatment of diabetes continues with injections of insulin.

Instructions
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