Капотен®

General characteristics. Structure:

Active ingredient: 25 mg of captopril.

Excipients: cellulose microcrystallic, starch corn, stearic acid, lactose.

Pharmacological properties:

Pharmacodynamics. Kapoten is inhibitor the angiotensin — the turning enzyme (ATE). Suppresses formation of angiotensin II and eliminates its vasoconstrictive action on arterial and venous vessels. Reduces the general peripheric vascular resistance, reduces an afterload, reduces arterial pressure. Reduces preloading, reduces pressure in the right auricle and a small circle of blood circulation. Reduces allocation of Aldosteronum in adrenal glands.

Pharmacokinetics. At intake bioavailability of captopril makes 60-70%. The concomitant use of food slows down absorption of drug for 30-40%. Communication with proteins of a blood plasma makes 25-30%. Elimination half-life 2-3 hours. Drug is removed from an organism preferential by kidneys, to 50% in an invariable look.

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:

Kapoten appoint inside for an hour to food. The mode of dosing is set individually.

At arterial hypertension drug 2 times a day appoint in an initial dose 12,5 mg. If necessary the dose gradually (with an interval of 2-4 weeks) is increased before achievement of optimum effect. At soft and moderate arterial hypertension the usual maintenance dose makes 25 mg 2 times a day; the maximum dose — 50 mg 2 times a day. At heavy arterial hypertension the initial dose makes 12,5 mg 2 times a day. A dose gradually increase to the maximum daily dose 150 mg (on 50 mg 3 times a day).

For treatment of chronic heart failure Kapoten appoint when use of diuretics does not provide adequate effect. The initial daily dose makes 6,25 mg 3 times a day. Further, if necessary, the dose gradually (bucketed not less than 2 weeks) is increased. The average maintenance dose makes 25 mg 2-3 times a day, and maximum — 150 mg a day.

At dysfunctions of a left ventricle after the postponed myocardial infarction at the patients who are in clinically stable state, Kapoten's use can be begun in 3 days after a myocardial infarction. The initial dose makes 6,25 mg a day, then the daily dose can be increased to 37,5 - 75 mg for 2-3 receptions (depending on portability of drug) up to maximum — 150 mg a day.

At a diabetic nephropathy Kapoten appoint in the dose 75-100 mg divided into 2-3 receptions. At insulin-dependent diabetes with a microalbuminuria (release of albumine of 30-300 mg a day) the dose of drug makes 50 mg 2 times a day. At the general clearance of protein more than 500 mg a day drug is effective in a dose of 25 mg 3 times a day.

Patients with a renal failure at moderate degree of a renal failure (the clearance of creatinine (CC) not less than 30 ml/min. / 1,73 sq.m) Kapoten can appoint 75-100 mg/days in a dose. At more expressed degree of renal failures (KK less than 30 ml/min. / 1,73 sq.m) the initial dose has to make no more than 12,5 mg/days; further, if necessary, with rather long intervals Kapoten's dose is gradually raised, but use smaller, than usually, a daily dose of drug.

At advanced age the dose of drug is selected individually, therapy 2 times a day are recommended to begin with a dose 6,25 mg and whenever possible to support her at this level.

If necessary in addition appoint loopback diuretics, but not diuretics of a thiazide row.

Features of use:

Before the beginning, and also regularly in the course of treatment by Kapoten it is necessary to control function of kidneys. At patients with chronic heart failure apply under careful medical control.

Against the background of prolonged use of Kapoten approximately at 20% of patients increase in urea and creatinine of blood serum more than for 20%, in comparison with norm or a reference value is observed. Less than at 5% of patients, especially at heavy nefropatiya, the termination of treatment because of growth of concentration of creatinine is required.

At patients with arterial hypertension at Kapoten's use the expressed arterial hypotension is observed only in rare instances; the probability of development of this state increases at the increased loss of liquid and salts (for example, after intensive treatment by diuretics), at patients with heart failure or being on dialysis.

The possibility of a sharp lowering of arterial pressure can be minimized at preliminary cancellation (in 4-7 days) diuretic or increase in intake of sodium of chloride (approximately in a week prior to reception), or by Kapoten's appointment in an initiation of treatment in small doses (6,25-12,5 mg/days).

In the first 3 months of therapy monthly control number of leukocytes of blood, further — 1 time in 3 months; at patients with autoimmune diseases in the first 3 months — in each 2 weeks, then — each 2 months. If the number of leukocytes are lower 4000/mkl, performing the general blood test is shown, below 1000/mkl — administration of drug is stopped.

In certain cases against the background of use of APF inhibitors, including Kapotena, is observed increase in potassium concentration in blood serum. The risk of development of a hyperpotassemia at use of APF inhibitors is increased at the patients with a renal failure and a diabetes mellitus and also accepting the kaliysberegayushchy diuretics, drugs of potassium or other drugs causing increase in potassium concentration in blood (for example, heparin). It is necessary to avoid simultaneous use of kaliysberegayushchy diuretics and drugs of potassium.

When carrying out a hemodialysis at the patients receiving Kapoten it is necessary to avoid use of dialysis membranes with high-permeability (for example, AN69) as in such cases the risk of development of anaphylactoid reactions increases.

In case of development of a Quincke's disease drug is cancelled and carry out careful medical observation. If hypostasis is localized on a face, special treatment usually is not required (for reduction of expressiveness of symptoms antihistaminic drugs can be used); if hypostasis extends to language, a throat or a throat and there is a threat of development of obstruction of respiratory tracts, it is necessary to enter immediately Epinephrinum (adrenaline) subcutaneously (0,5 ml in cultivation 1:1000).

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

During treatment it is necessary to abstain from driving of motor transport and occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions since dizziness, especially after reception of an initial dose is possible.

Side effects:

From cardiovascular system: orthostatic hypotension, tachycardia, peripheral hypostases, lowering of arterial pressure.

From respiratory system: the dry cough which is usually passing after drug withdrawal, a bronchospasm, a fluid lungs.

Allergic reactions: Quincke's disease of extremities, persons, lips, mucous membranes, language, throat and throat.

From the central nervous system: headache, dizziness, ataxy, paresthesias, drowsiness, vision disorders.

From water and electrolytic exchange: a hyperpotassemia, a hyponatremia, a proteinuria, the increased maintenance of an urea nitrogen and creatinine in blood, acidosis.

From bodies of a hemopoiesis: a neutropenia, an agranulocytosis, thrombocytopenia, anemia, positive test for antibodies to nuclear antigen (seldom).

From the alimentary system: taste disturbance, dryness in a mouth, stomatitis, a hyperplasia of gums, increase in activity of enzymes of a liver, an abdominal pain, diarrhea, hepatitis, a hyperbilirubinemia.

Interaction with other medicines:

Diuretic means and vazodilatator (for example, minoksidit) exponentiate hypotensive action of Kapoten.

At combined use of Kapoten with indometacin (and, perhaps, with other non-steroidal anti-inflammatory drugs) it can be noted decrease in hypotensive action.

Simultaneous use with kaliysberegayushchy diuretics (for example, Triamterenum, Spironolactonum, amiloride), potassium drugs, potassium additives, salt substitutes (contain significant amounts of K+) increases risk of development of a hyperpotassemia.

At simultaneous use of salts of lithium increase in concentration of lithium in blood serum is possible.

Kapoten's use for the patients accepting Allopyrinolum or procaineamide increases risk of development of a neutropenia and/or Stephens-Johnson's syndrome. Kapoten's use for the patients accepting immunodepressants (for example, циклофосфацин or Azathioprinum), increases risk of development of hematologic disturbances.

Contraindications:

Hypersensitivity to captopril or other APF inhibitors; a Quincke's disease (in the anamnesis against the background of therapy by APF inhibitors or hereditary); the expressed abnormal liver functions and/or kidneys; hyperpotassemia; a bilateral stenosis of renal arteries, a stenosis of an artery of the only kidney with the progressing azotemia, a state after transplantation of kidneys, the stenosis of the mouth of an aorta and similar changes complicating outflow of blood from a left ventricle, pregnancy, the lactation period, age up to 18 years (efficiency and safety are not established).

With care appoint the patient who is on a low-salt or electrolyte-deficient diet (the increased risk of development of hypotension) and a hyperpotassemia. In case of emergence after Kapoten's reception symptomatic arterial hypotension to the patient should accept horizontal position with the raised legs.

Overdose:

Symptoms: sharp lowering of arterial pressure.

Treatment: administration of isotonic solution of sodium of chloride or other plasma substituting solutions, hemodialysis.

Storage conditions:

List B. In the dry place, at a temperature not above 25 °C. To store in the place, unavailable to children. Not to use drug after expiration date of a period of validity. A period of validity - 5 years.

Issue conditions:

According to the recipe

Packaging:

Tablets of 25 mg. On 10 or 14 tablets in a blister strip packaging. 4 planimetric cell packagings on 10 tablets or 2 or 4 blister strip packagings on 14 tablets together with the application instruction place in a pack from a cardboard.