Каптоприл-Сар®

General characteristics. Structure:

Active ingredient: 25 mg of captopril.

Excipients: sugar milk (lactose), potato starch, polyvinylpirrolidone low-molecular medical (povidone), sodium lauryl sulfate, magnesium stearate, stearic acid.

Anti-hypertensive cardiological drug.

Pharmacological properties:

Pharmacodynamics. Anti-hypertensive means, APF inhibitor. The mechanism of anti-hypertensive action is connected with competitive inhibition of activity of APF that leads to reduction in the rate of transformation of angiotensin I into angiotensin II (which has the expressed vasoconstrictive effect and stimulates secretion of Aldosteronum in bark of adrenal glands). Besides, captopril, apparently, exerts impact on kinin-kallikrein system, interfering with disintegration of bradikinin. The hypotensive effect does not depend on activity of a renin of plasma, decrease in the ABP is noted at normal and even reduced concentration of hormone that is caused by impact on fabric RAAS. Increases a coronary and renal blood stream.

Thanks to vasodilating action, reduces OPSS (afterload), jamming pressure in pulmonary capillaries (preloading) and resistance in pulmonary vessels; increases the minute volume of heart and tolerance to loading. At prolonged use reduces expressiveness of a hypertrophy of a myocardium of a left ventricle, prevents progressing of heart failure and slows down development of dilatation of a left ventricle. Promotes decrease in content of sodium at patients with chronic heart failure. Expands arteries more than veins. Improves blood supply of an ischemic myocardium. Reduces aggregation of thrombocytes.

Lowers a tone of the taking-out arterioles of balls of kidneys, improving an intraglomerular hemodynamics, interferes with development of a diabetic nephropathy.

Pharmacokinetics. After intake not less than 75% are quickly absorbed from a GIT. The concomitant use of food reduces absorption by 30-40%. Cmax in a blood plasma is reached in 30-90 min. Linkng with proteins, is preferential with albumine, makes 25-30%. It is allocated with breast milk. The dimeasure of captopril and captopril-tsisteindisulfida is metabolized in a liver with education disulfide. Metabolites pharmacological are inactive.

T1/2 makes less than 3 h and increases at a renal failure (3.5-32 h). More than 95% are removed by kidneys, 40-50% in not changed look, other part - in the form of metabolites.

At a chronic renal failure kumulirut.

Indications to use:

- arterial hypertension, including renovascular;

- chronic heart failure (as a part of a combination therapy);

- dysfunctions of a left ventricle after the postponed myocardial infarction at clinically stable state;

- a diabetic nephropathy against the background of a diabetes mellitus of type 1 (at an albuminuria more than 30 mg/days)

Route of administration and doses:

At intake an initial dose - on 6.25-12.5 mg of 2-3 times/days. At insufficient effect the dose is gradually increased to 25-50 mg of 3 times/days. At renal failures the daily dose should be reduced.

The maximum daily dose makes 150 mg.

Features of use:

Use at pregnancy and feeding by a breast. It must be kept in mind that use of captopril in II and III trimesters of pregnancy can cause disturbances of development and death of a fruit. At the established pregnancy captopril should be cancelled immediately. Captopril is emitted with breast milk. In need of use in the period of a lactation it is necessary to resolve an issue of the breastfeeding termination.

With care it is necessary to apply at instructions in the anamnesis on a Quincke's disease against the background of therapy by APF inhibitors, a hereditary or idiopathic Quincke's disease, at an aortal stenosis, tserebro-and cardiovascular diseases (including at insufficiency of cerebral circulation, ischemic heart disease, coronary insufficiency), a serious autoimmune illness of connecting fabric (including hard currency, a scleroderma), at oppression of a marrowy hemopoiesis, at a diabetes mellitus, a hyperpotassemia, a bilateral stenosis of renal arteries, a stenosis of an artery of the only kidney, a state after transplantation of kidneys, a renal and/or liver failure, against the background of a diet with sodium restriction, the states which are followed by decrease in OTsK (including at diarrhea, vomiting), at patients of advanced age.

At patients with chronic heart failure captopril is applied under careful medical control.

The arterial hypotension arising during surgical intervention against the background of reception of captopril is eliminated with completion of volume of liquid.

It is necessary to avoid simultaneous use of kaliysberegayushchy diuretics and drugs of potassium, especially at patients with a renal failure and a diabetes mellitus.

At reception of captopril false positive reaction can be observed in the analysis of urine on acetone.

Use of captopril for children is possible only in case of inefficiency of other drugs.

Influence on ability to driving of motor transport and to control of mechanisms. Care at control of vehicles or performance of other work requiring special attention since dizziness, especially after an initial dose of captopril is possible is necessary.

Side effects:

From TsNS and peripheral nervous system: dizziness, headache, feeling of fatigue, adynamy, paresthesias.

From cardiovascular system: orthostatic hypotension; seldom - tachycardia.

From the alimentary system: nausea, loss of appetite, disturbance of flavoring feelings; seldom - abdominal pains, diarrhea or a lock, increase in activity of hepatic transaminases, a hyperbilirubinemia; signs of hepatocellular damage (hepatitis); in some cases - a cholestasia; in isolated cases - pancreatitis.

From system of a hemopoiesis: seldom - a neutropenia, anemia, thrombocytopenia; very seldom at patients with autoimmune diseases - an agranulocytosis.

From a metabolism: hyperpotassemia, acidosis.

From an urinary system: a proteinuria, a renal failure (increase in concentration of urea and creatinine in blood).

From respiratory system: dry cough.

Allergic reactions: skin rash; seldom - a Quincke's edema, a bronchospasm, a serum disease, a limfoadenopatiya; in some cases - emergence of anti-nuclear antibodies in blood.

Interaction with other medicines:

At simultaneous use with immunodepressants, cytostatics the risk of development of a leukopenia increases.

At simultaneous use with kaliysberegayushchy diuretics (including Spironolactonum, Triamterenum, amiloride), the potassium drugs, substitutes of salt and dietary supplement to food containing potassium development of a hyperpotassemia (especially at patients with renal failures) is possible since APF inhibitors reduce the maintenance of Aldosteronum that leads to a potassium delay in an organism against the background of restriction of removal of potassium or its additional receipt in an organism.

At simultaneous use of APF and NPVS inhibitors the risk of development of renal failures increases; the hyperpotassemia is seldom observed.

At simultaneous use with "loopback" diuretics or thiazide diuretics the expressed arterial hypotension, especially after reception of the first dose of diuretic, apparently, at the expense of a hypovolemia which leads to tranzitorny strengthening of anti-hypertensive effect of captopril is possible. There is a risk of development of a hypopotassemia. Increase in risk of development of renal failures.

At simultaneous use with anesthetics heavy arterial hypotension is possible.

At simultaneous use with Azathioprinum development of anemia is possible that is caused by oppression of activity of erythropoetin under the influence of APF inhibitors and Azathioprinum. Cases of development of a leukopenia are described that can be connected with the additive oppression of function of marrow.

At simultaneous use with Allopyrinolum the risk of development of hematologic disturbances increases; cases of development of heavy hypersensitivity reactions, including Stephens-Johnson's syndrome are described.

At simultaneous use of aluminum of hydroxide, magnesium of hydroxide, magnesium of a carbonate bioavailability of captopril decreases.

Acetylsalicylic acid in high doses can reduce anti-hypertensive effect of captopril. It is not finalized whether acetylsalicylic acid reduces a therapeutic effectiveness of APF inhibitors at patients with an ischemic heart disease and heart failure. The nature of this interaction depends on the course of a disease. Acetylsalicylic acid, inhibiting TsOG and synthesis of prostaglandins, can cause vasoconstriction that leads to reduction of cordial emission and an aggravation of symptoms of the patients with heart failure receiving APF inhibitors.

There are messages on increase in concentration of digoxin in a blood plasma at simultaneous use of captopril with digoxin. The risk of development of medicinal interaction is increased at patients with renal failures.

At simultaneous use with indometacin, an ibuprofen anti-hypertensive effect of captopril, apparently, owing to inhibition under the influence of NPVS of synthesis of prostaglandins decreases (which as believe, play a part in development of hypotensive effect of APF inhibitors).

At simultaneous use with insulin, hypoglycemic means derivative sulphonylurea development of a hypoglycemia due to increase in tolerance to glucose is possible.

At simultaneous use of APF inhibitors and interleykina-3 there is a risk of development of arterial hypotension.

At simultaneous use with interferon alpha 2а or interferon a beta cases of development of a heavy granulocytopenia are described.

Upon transition from reception of a clonidine to captopril anti-hypertensive action of the last develops gradually. In case of sudden cancellation of a clonidine at the patients receiving captopril, perhaps sharp increase in the ABP.

At simultaneous use of lithium of a carbonate the concentration of lithium in blood serum which is followed by intoxication symptoms increases.

At simultaneous use with minoksidily, Sodium nitroprussidum anti-hypertensive action amplifies.

At simultaneous use with orlistaty reduction of efficiency of captopril is possible that can lead to increase in the ABP, hypertensive crisis, the case of a hematencephalon is described.

At simultaneous use of APF inhibitors with pergolidy strengthening of anti-hypertensive effect is possible.

At simultaneous use with probenetsidy the renal clearance of captopril decreases.

At simultaneous use with procaineamide increase in risk of development of a leukopenia is possible.

At simultaneous use with Trimethoprimum there is a risk of development of a hyperpotassemia, especially at patients with renal failures.

At simultaneous use with Chlorpromazinum there is a risk of development of orthostatic hypotension.

At simultaneous use with cyclosporine there are messages on development of an acute renal failure, an oliguria.

Believe that reduction of efficiency of anti-hypertensive means at simultaneous use with erythropoetins is possible.

Contraindications:

Pregnancy, the lactation period, age up to 18 years, hypersensitivity to captopril and other APF inhibitors.

With care it is necessary to apply at a liver failure.

With care it is necessary to apply at a state after transplantation of kidneys, a renal failure.

With care it is necessary to apply at patients of advanced age.

Storage conditions:

Period of validity 2 years. Not to use after the term specified on packaging. List B. In the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets on 25 mg. On 10 tablets in a blister strip packaging from a film of polyvinyl chloride and aluminum foil. 2 or 4 blister strip packagings together with the application instruction place in a pack from a cardboard bandbox