Каптоприл-Ферейн®

General characteristics. Structure:

Active ingredient: 25 mg of captopril in 1 tablet.

Excipients: lactose (sugar milk), starch corn, кросповидон (Kollidon TsL), stearic acid, cellulose microcrystallic.

Pharmacological properties:

Pharmacodynamics. Captopril - Fereyn® is inhibitor of the angiotensin-converting enzyme (ACE). Suppresses formation of angiotensin II and eliminates its vasoconstrictive deystyovy 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. Absorption - bystry, reaches 75% (meal lowers by 30-40%), bioavailability - 60-70%. Communication with proteins of plasma (it is preferential with albumine) - 25-30%. Time necessary for achievement of the maximum concentration (114 ng/ml) at oral administration - 30-90 min. Through a blood-brain barrier and a placental barrier gets badly (less than 1%). The dimeasure of captopril and captopril-tsisteindisulfida is metabolized in a liver with education disulfide.

Metabolites pharmacological are inactive. An elimination half-life - 2-3 hours. Other part in the form of metabolites is removed by kidneys of 95% (40-50% in an invariable look). Cosecretes with maternal milk. It is removed preferential by kidneys (to 50% in an invariable look). An elimination half-life at a chronic renal failure - 3,5 - 32 hours. Kumuliruyet at a chronic renal failure.

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:

Captopril - Fereyn® appoint inside for an hour to food. Dosing mode устанавливает­ся individually. At titration of a dose of drug captopril according to the declared indications it is necessary to use captopril in a dosage form: tablets on 12,5 mg.

At arterial hypertension Captopril - Fereyn® appoint in an initial dose 12,5 mg 2 times a day. If necessary the dose gradually (with an interval of 2-4 weeks) is uvelichiyovat 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 soyostavlyat 12,5 mg 2 times a day. The dose is gradually increased to the maximum daily dose. 150 mg (on 50 mg Zraza in days).

For treatment of chronic heart failure captopril is appointed when use of diuretics does not provide adequate effect. The initial daily dose makes 6,25 mg 3 times a day. Further if necessary, a dose postepenyono (bucketed not less than 2 weeks) increase. The average maintenance dose soyostavlyat 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, use of captopril 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 captopril) up to maximum - 150 mg a day.

At a diabetic nephropathy Captopril - Fereyn® appoint in a dose 75-100 mg, razdeyolenny to 2-3 receptions. At achrestic 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 extent of dysfunction по­чек (the clearance of creatinine (CC) not less than 30 ml/min. / 1,73 sq.m) Captopril - Fereyn® 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 the drug dose is gradually raised, but use smaller, than usually, a daily dose.

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 it is regular, in the course of treatment by drug it is necessary to kontroliroyovat function of kidneys. At patients with chronic heart failure apply under careful medical control.

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

At patients with arterial hypertension at use of Kaptoprila-Fereyn® vyrayozhenny arterial hypotension is observed only in rare instances; the probability a razviyotiya 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 purpose of Kaptoprila-Fereyn® 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 inhibitors of an angiotensin-converting enzyme, including Kaptoprila-Fereyn®, increase in potassium concentration in blood serum is observed. The risk of development of a hyperpotassemia at use of inhibitors of an angiotensin-converting enzyme is increased at the patients with a renal failure and sayokharny diabetes and also accepting the kaliysberegayushchy diuretics, drugs of potassium or other drugs causing increase in potassium concentration in blood (for example, ге­парин). It is necessary to avoid simultaneous use of kaliysberegayushchy diuretics and drugs of potassium.

When carrying out a hemodialysis at the patients receiving Kaptopril-Fereyn® 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 tshchayotelny 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 nemedyolenno necessary to enter Epinephrinum (adrenaline) subcutaneously (0,5 ml in cultivation 1:1000).

At administration of drug false positive reaction can be observed in the analysis of a moyocha on acetone.

During treatment it is necessary to abstain from driving of motor transport and occupations poyotentsialno the 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.

Influence on ability to manage vehicles and mechanisms. During treatment it is necessary to abstain from driving of motor transport and occupations poyotentsialno the 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, peyoriferichesky 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 обо­лочек, language, throat and throat.

From the central nervous system: headache, dizziness, ataxy, payoresteziya, 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, an aneyomiya, positive test for antibodies to nuclear antigen (seldom).

From the alimentary system: taste disturbance, dryness in a mouth, stomatitis, poyovysheny activities of enzymes of a liver, an abdominal pain, diarrhea, hepatitis, a hyperbilirubinemia.

Interaction with other medicines:

Diuretic means and vazodilatator (for example, minoksidit) exponentiate gipoyotenzivny effect of drug.

At combined use with estrogen and indometacin (and, perhaps, with other neyosteroidny antiinflammatory drugs) decrease in gipoyotenzivny action can be noted.

Simultaneous use with kaliysberegayushchy diuretics (for example, Triamterenum, Spironolactonum, amiloride), potassium drugs, potassium additives, salt substitutes (contain significant amounts of potassium) increases risk of development of a hyperpotassemia. At simultaneous use of salts of lithium increase in concentration of lithium in blood serum is possible.

Use of drug for the patients accepting Allopyrinolum or procaineamide poyovyshat risk of development of a neutropenia and/or Stephens-Johnson's syndrome.

Use of drug for the patients accepting immunodepressants (for example, cyclophosphamide or Azathioprinum), increases risk of development of hematologic disturbances.

Contraindications:

Hypersensitivity to captopril or other inhibitors of an angiotensin-converting enzyme; a Quincke's disease (in the anamnesis against the background of therapy by ingibiyotor of an angiotensin-converting enzyme or hereditary); the expressed naruyosheniye of function of a liver and/or kidneys; hyperpotassemia; a bilateral stenosis of renal arteyoriya, 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 (the effektivyonost and safety are not established).

With care. A serious autoimmune illness of connecting fabric (including a system lupus erythematosus, a scleroderma), oppression of a marrowy hemopoiesis (risk of development of a neutropenia and agranulocytosis), brain ischemia, sugar diayobt (the risk of development of a hyperpotassemia), the patients who are on a hemodialysis, a diet with sodium restriction, primary hyper aldosteronism, coronary heart disease, states which are followed by decrease in volume of the circulating blood is increased (including vomiting, diarrhea), advanced age (correction of doses is required).

With care drug is appointed the patient who is on a low-salt or bessoyolevy diet (the increased risk of development of hypotension) and a hyperpotassemia.

Overdose:

Symptoms: sharp lowering of arterial pressure.

Treatment: the patient should accept horizontal position with the raised legs; introduction of 0,9% of solution of sodium of chloride or other plasma substituting rastvoyor, hemodialysis.

Storage conditions:

In the dry, protected from light place, at a temperature not above 25 °C. In the place, unavailable to children. A period of validity - 2 years. Not to use after the term specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets on 25 mg. Packaging: 40 or 50 tablets in banks for medicines of orange glass with a triangular nimbus. 40 or 50 tablets in banks for medicines polymeric with screw gorloviyony and the screwed covers. 10 or 20 tablets in a blister strip packaging from a film of polyvinyl chloride and aluminum foil or a packing material. Each can, 1, 2, 3, 4 or 5 blister strip packagings together with the application instruction - in a pack from a cardboard.