Captopril

Captopril – inhibitor of an angiotensin-converting enzyme (APF).

Form of release and structure

Dosage form – tablets (on 10 pieces in a blister strip packaging, in a cardboard pack of 1, 2, 3, 4, 5 or 10 packagings).

Active agent – captopril, in 1 tablet – 25 or 50 mg.

Indications to use

Use of Captopril is shown at arterial hypertension (including renovascular) and as a part of a combination therapy of chronic heart failure.

Contraindications

• Quincke's disease (including in the anamnesis after reception of other APF inhibitors) or hereditary;
• Cardiogenic shock;
• Arterial hypotension;
• Mitral stenosis, stenosis of the mouth of an aorta, other disturbances of outflow of blood from a left ventricle of heart;
• The expressed renal failures, hyperpotassemia, azotemia, stenosis of the only kidney with the progressing azotemia, a bilateral stenosis of renal arteries, primary hyper aldosteronism, a state after transplantation of a kidney;
• The expressed abnormal liver functions;
• Age up to 18 years;
• Period of pregnancy and breastfeeding;
• Hypersensitivity to captopril and other APF inhibitors.

With care patients should appoint drug with a serious autoimmune illness (among them a scleroderma, a system lupus erythematosus); at ischemia of a brain, coronary heart disease, oppression of marrowy blood circulation (risk of development of an agranulocytosis and neutropenia), a diabetes mellitus (a high probability of development of a hyperpotassemia), the states which are followed by decrease in volume of the circulating blood including vomiting and diarrhea; the patient keeping to a diet with the sodium restriction which is on a hemodialysis and also to patients of advanced age.

Route of administration and dosage

Pill is taken inside in 1 hour prior to food.

The doctor appoints a daily dose individually on the basis of clinical indications.

The recommended dosing mode:

• Chronic heart failure (at a combination therapy), in case of lack of adequate effect of use of diuretics: an initial dose on 6,25 mg 2-3 times a day. The dose is brought to average supporting – on 25 mg 2-3 times a day gradually, with an interval 2 and more than a week. In need of further increase in a dose, increase is made 1 time in 2 weeks;
• Arterial hypertension: an initial dose on 25 mg 2 times a day. At insufficiency of therapeutic effect 1 time in 2-4 weeks is recommended to increase a dose gradually. A maintenance dose for a moderate form of arterial hypertension – on 25 mg 2 times a day, but no more than 50 mg; for a severe form – on 50 mg 3 times a day.

The maximum daily dose – 150 mg.

It is recommended to appoint a daily drug dosing for patients with renal failures: at moderate degree (the clearance of creatinine (CC) is not lower than 30 ml/min. / 1,73 ^{of sq.m}) – 75-100 mg, at the expressed disturbance (KK is lower than 30 ml/min. / 1,73 ^{of sq.m}) – an initial dose of 12,5-25 mg a day. If necessary increase is made for a long time, but drug is always used in a daily dose less than usual.

For patients of advanced age the dose is selected strictly individually, treatment is recommended to begin with 6,25 mg 2 times a day and to try to support a dose at such level.

In need of additional reception of diuretics, appoint diuretic of a loopback, but not thiazide row.

Side effects

Use of Captopril can cause side effects:

• From cardiovascular system: essential lowering of arterial pressure, orthostatic hypotension, peripheral hypostases, tachycardia;
• From digestive tract, a pancreas, liver: dryness in a mouth, disturbance of flavoring feelings, a loss of appetite, nausea, stomatitis; seldom – abdominal pains, diarrhea, a hyperbilirubinemia, increase in activity of liver enzymes, hepatitis;
• From an urinary system: a renal failure (growth of level of concentration of creatinine and urea in blood), a proteinuria;
• From a nervous system: drowsiness, dizziness, feeling of fatigue, headache, paresthesias, ataxy, adynamy, vision disorder;
• From system of a hemopoiesis: seldom – anemia, a neutropenia, an agranulocytosis, thrombocytopenia;
• From respiratory system: bronchospasm, dry cough (passing), fluid lungs;
• Laboratory indicators: a hyponatremia, a hyperpotassemia, acidosis, at patients with a diabetes mellitus – a hypoglycemia (against the background of use of peroral hypoglycemic means and insulin);
• Dermatological reactions: the increased photosensitivity, an itch, skin rash, usually – makulopapulezny, is more rare – violent or vesicular;
• Allergic and immunopathological reactions: a Quincke's disease of mucous membranes of a mouth, language, a throat and throat, lips, the person and extremities, it is very rare – intestinal hypostasis; a lymphadenopathy, a serum disease, in rare instances – existence of antinuclear antibodies in blood;
• Others: paresthesias.

Special instructions

At appointment and regularly in the course of administration of drug it is necessary to carry out control of function of kidneys.

Treatment of patients with chronic heart failure should be carried out under careful medical observation.

With care, especially against the background of renal failures, Captopril is appointed in combination with immunodepressants (including cyclophosphamide, Azathioprinum), Allopyrinolum or procaineamide sick with a system vasculitis or diffusion pathologies of connecting fabric. Not to allow serious complications, prior to use, within the first 3 months (1 times in 2 weeks) and periodically during the entire period of use of drug it is necessary to control a pattern of peripheral blood.

At patients with a disease of kidneys in the anamnesis captopril increases probability of development of a proteinuria therefore at this category of patients follows within the first 9 months (1 times in 4 weeks) to control the level of protein content in urine and if it exceeds norm, it is necessary to resolve an issue of drug withdrawal.

The risk of development of renal failures exists at patients with a stenosis of renal arteries, at increase in level of creatinine or urea in blood it is necessary to lower a dose of drug or to cancel it.

Not to allow development of anaphylactoid reactions in the patients accepting Captopril for carrying out a hemodialysis it is recommended not to use dialysis membranes with high-permeability (including AN69).

The risk of development of arterial hypotension from use of drug can be reduced if prior to treatment (in 4-7 days) it is essential to lower a dose or to stop use of diuretics.

When developing symptomatic arterial hypotension against the background of administration of drug the patient is recommended to accept horizontal position and to raise legs.

At the expressed arterial hypotension the patient needs to enter isotonic solution of sodium chloride intravenously.

At development of a Quincke's disease it is necessary to cancel drug and to see urgently a doctor. For hypostasis with localization on a face, usually, special treatment is not required, except as reception of antihistaminic drugs for decrease in expressiveness of symptoms. If there is a threat of development of obstruction of respiratory tracts (a paraglossa, drinks or throats) it is necessary to enter subcutaneously 0,5 ml of Epinephrinum (adrenaline) into proportions 1:1000.

Use of Captopril can cause dizziness, especially in an initiation of treatment therefore patients are recommended to abstain from control of vehicles and mechanisms, and also potentially dangerous types of activity demanding concentration of attention and high speed of psychomotor reactions.

Medicinal interaction

Hypotensive activity of captopril is exponentiated by vazodilatator (minoksidit) also diuretic means.

Decrease in hypotensive effect of drug is promoted by a combination to a clonidine, estrogen, indometacin and other non-steroidal anti-inflammatory drugs.

At simultaneous use of Captopril:

• Kaliysberegayushchy diuretics and drugs of potassium can lead to a hyperpotassemia;
• Gold drugs (sodium ауротиомалат) and inhibitors of an angiotensin-converting enzyme cause the complex of symptoms including nausea, vomiting, a hyperemia of the person, lowering of arterial pressure;
• Procaineamide and Allopyrinolum promote risk of development of a syndrome of Stephens-Johnson and/or a neutropenia;
• Salts of lithium increase the content of lithium in blood serum;
• Tsiklofosfatsin, Azathioprinum and other immunodepressants increase probability of hematologic disturbances;
• Insulin and hypoglycemic peroral means increase risk of development of a hypoglycemia.

Terms and storage conditions

To store in unavailable to children, the dry place at a temperature up to 30 °C.

Period of validity – 3 years.