Ç«¬áÓñ¿ß® 7,5

General characteristics. Structure:

1 tablet, coated, contains active agent - a zofenopril of calcium of 7,5 mg.

Excipients: lactoses monohydrate, magnesium stearate, cellulose microcrystallic, starch corn, silicon dioxide colloid.

Cover: gipromelloza, titanium dioxide, macrogoal 400, macrogoal 600.

Pharmacological properties:

Pharmacodynamics. Zofenopril - anti-hypertensive drug, the mechanism of its action is connected with reduction of education from angiotensin I of angiotensin II which decrease in contents leads to direct reduction of allocation of Aldosteronum. At the same time the general peripheric vascular resistance, systolic and diastolic arterial pressure, a post - and preload of a myocardium decreases. Expands arteries more than veins, at the same time reflex increase in the heart rate (HR) is not noted. Reduces degradation of bradikinin, increases prostaglandin synthesis.

The hypotensive effect is more expressed at high concentration of a renin of a blood plasma, than at normal or its reduced concentration. The lowering of arterial pressure (ABP) in therapeutic limits does not exert impact on cerebral circulation, the blood stream in vessels of a brain is supported at the sufficient level and against the background of the reduced ABP. Strengthens a coronary and renal blood stream.

At prolonged use the hypertrophy of a left ventricle of a myocardium and myocytes of walls of arteries of resistive type decreases, prevents progressing of heart failure and slows down development of dilatation of a left ventricle. Improves blood supply of an ischemic myocardium. Reduces aggregation of thrombocytes. Zofenopril of calcium is pro-medicine as active inhibitor is free sulphhydryl connection - зофеноприлат - formed as a result of thioradio hydrolysis.

Time of approach of hypotensive effect at intake - 1 h, reaches a maximum in 4-6 h and remains to 24 h. At some patients therapy for several weeks is necessary for achievement of optimum level of the ABP. At heart failure the noticeable clinical effect is observed at prolonged treatment - 6 months and more.

Pharmacokinetics. Zofenopril of calcium is quickly and completely absorbed in a digestive tract at oral administration and is exposed to almost full transformation in зофеноприлат which maximum concentration in blood is reached in 1,5 hours after reception orally of a drug Zokardis® dose

About 88% of a zofenopril of calcium contact proteins of a blood plasma. Zofenopril is quickly metabolized in a liver with formation of an active metabolite of a zofenoprilat.

The elimination half-life of a zofenoprilat makes 5,5 hours, and its general clearance makes 1300 ml/min. after oral administration of a zofenopril of calcium. It is removed зофеноприлат preferential by kidneys - 69%, through intestines - 26%.

Indications to use:

• Arterial hypertension of soft and moderate severity.
• An acute myocardial infarction with signs or symptoms of heart failure at patients with stable indicators of a hemodynamics and not receiving thrombolytic therapy.

Route of administration and doses:

Ç«¬áÓñ¿ß® 7,5 is appointed inside irrespective of meal time (to, in time or after food), washing down with enough liquid.

At arterial hypertension

Patients with normal renal and hepatic function
 For achievement of the optimum ABP treatment should be begun with 2 pill of the drug Зокардис® 7,5 taken once a day and gradually at insufficient expressiveness of hypotensive effect, to increase a dose at an interval of 4 weeks.

Usually effective dose makes 4 pill of the drug Зокардис® 7,5 taken once a day.

The maximum daily dose makes 8 pill of the drug Зокардис® 7,5 a day, taken once or divided into two doses, everyone on 4 tablets.

Patients with disturbance of water-salt balance

Initial therapy by APF inhibitors demands correction of salt and/or water deficits, the termination of the carried-out therapy by diuretics within 2-3 days prior to reception of APF inhibitor and begins with the dose making 2 tablets of the drug Зокардис® 7,5 once a day. If it is impossible, then it is necessary to begin with the dose making 1 tablet of the drug Зокардис® 7,5 a day.

Patients with disturbance of renal function or being on a hemodialysis

From patients with a weak renal failure (the clearance of creatinine (CC)> of 45 ml/min.) the dose decline is not required. To patients with average and heavy degree of a renal failure (clearance of creatinine <45 ml/min.) it is necessary to appoint 1/2 therapeutic doses once a day.

The initial dose for the patients who are on dialysis makes 1/4 doses, used for patients with normal renal function.

Dosage at elderly patients

Correction is not required from elderly patients with normal KK. At elderly patients with KK <45 ml/min. reception 1/2 day doses is recommended.

Dosage at abnormal liver functions

At patients with slight and average degree of an abnormal liver function the initial dose of the drug Зокардис® 7,5 makes a half of the dose applied at patients with normal function of a liver.

Patients with heavy degree have abnormal liver functions Зокардис® 7,5 should not be applied.

Acute myocardial infarction (as a part of a combination therapy).

Treatment by the drug Зокардис® 7,5 should be begun within 24 hours after emergence of the first symptoms of a myocardial infarction and to continue within 6 weeks.

It is necessary to apply the following scheme of a dosage:

1st and 2nd day            1 таб. Ç«¬áÓñ¿ß® 7,5 each 12 hours,
3rd and 4th day            2 таб. Ç«¬áÓñ¿ß® 7,5 each 12 hours,
from the 5th day and further    4 таб. Ç«¬áÓñ¿ß® 7,5 each 12 hours.

 

In case of excessive decrease in the ABP in an initiation of treatment or during the first 3 days after a myocardial infarction, the initial dose is not increased or cancelled.

After 6 weeks of reception therapy can be stopped at patients without signs of a left ventricular failure or heart failure. For correction of a left ventricular failure or heart failure, and also arterial hypertension treatment can be continued for a long time.

Dosage at elderly patients

Ç«¬áÓñ¿ß® 7,5 it is necessary to apply with care at patients with a myocardial infarction, 75 years are more senior.

Features of use:

The Tranzitorny expressed lowering of arterial pressure is not a contraindication for treatment continuation by drug after stabilization of the ABP. In case of the repeated expressed decrease in the ABP, it is necessary to reduce a dose or to cancel drug.

At development of excessive decrease in the ABP of the patient transfer to horizontal position with a low headboard, if necessary solution of sodium of chloride and plasma substituting drugs enter 0,9%.

Use of high-flowing dialysis membranes increases risk of development of anaphylactic reaction. Correction of the mode of dosing in days, free from dialysis, has to be carried out depending on the ABP level. Before treatment by APF inhibitors control of the ABP, blood indicators (hemoglobin, potassium, creatinine, urea, activity of "hepatic" enzymes), a squirrel in urine is necessary.

It is necessary to watch carefully patients with heavy heart failure, coronary heart disease and diseases of vessels of a brain at which sharp decrease in the ABP can lead to a myocardial infarction, a stroke or a renal failure. Sudden cancellation of treatment does not lead to a syndrome of "cancellation" (sharp raising of the ABP).

Patients with the instruction on development of a Quincke's disease in the anamnesis, have an increased risk of its development at reception of APF inhibitors.

For newborns and babies who were exposed to pre-natal influence of APF inhibitors it is recommended to conduct careful observation for early detection of the expressed decrease in the ABP, an oliguria, a hyperpotassemia and neurologic frustration, possible owing to reduction of a renal and brain blood-groove at decrease in the ABP called by APF inhibitors. At an oliguria maintenance of the ABP and renal perfusion by administration of the corresponding liquids and vasoconstrictors is necessary.

At patients with reduced function of kidneys it is necessary to reduce a single dose or to increase intervals between administrations of drug.

During selection of a therapeutic dose 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 an initial dose of APF inhibitor at the patients accepting diuretic means is possible.

It is necessary to be careful when performing physical exercises at hot weather (risk of development of dehydration and excessive decrease in the ABP because of decrease in volume of the circulating blood). Before surgical intervention (including stomatology) it is necessary to warn the surgeon/anaesthesiologist about use of APF inhibitors.

During treatment it is not recommended to take alcoholic beverages since alcohol strengthens hypotensive effect of drug.

Simultaneous use of hypoglycemic means, increases risk of a hypoglycemia.

Side effects:

From cardiovascular system: excessive decrease in the ABP, an orthostatic collapse, is rare - a retrosternal pain stenocardia, a myocardial infarction (are usually connected with the expressed decrease in the ABP), arrhythmias (atrial bradi-or tachycardia, atrial fibrillation), heartbeat, a thromboembolism of branches of a pulmonary artery, pain in heart, a syncope.

From the central nervous system: dizziness, a headache, weakness, sleeplessness, alarm, a depression, confusion of consciousness, increased fatigue, drowsiness (2-3%), is very rare at use of high doses - nervousness, paresthesias.

From sense bodys: seldom: disturbances of a vestibular mechanism, hearing disorder and sight, sonitus.

From a digestive tract: dryness in a mouth, anorexia, dispepsichesky frustration (nausea, diarrhea or a lock, vomiting, pains in a stomach), intestinal impassability, pancreatitis, an abnormal liver function and a zhelchevydeleniya, hepatitis, jaundice.

From respiratory system: unproductive dry cough, it is very rare: intersticial pneumonitis, bronchospasm, asthma, rhinorrhea, pharyngitis.

Allergic reactions: seldom: skin rash, a Quincke's disease of the person, extremities, lips, language, a glottis and/or throat, a dysphonia, a polymorphic erythema, exfoliative dermatitis, it is very rare: Stephens-Johnson's syndrome, toxic epidermal necrolysis, pemphigus, itch, small tortoiseshell, photosensitization, serositis, vasculitis, miositis, arthralgia, arthritis, stomatitis, glossitis.

From laboratory indicators: hypercreatinemia, increase in content of urea, increase in activity of "hepatic" transaminases, hyperbilirubinemia, hyperpotassemia, hyponatremia. Decrease in a hematocrit and hemoglobin, increase SOE, thrombocytopenia, a neutropenia, an agranulocytosis (at patients with autoimmune diseases), an eosinophilia are noted in certain cases.

From an urinary system: renal failure, proteinuria.

Interaction with other medicines:

Hypotensive effect of APF inhibitors can amplify others
 anti-hypertensive means, diuretics, general anesthetics, febrifugal and sedatives, ethanol.

At co-administration of a zofenopril with non-steroidal anti-inflammatory drugs decrease in hypotensive effect of a zofenopril is possible; with kaliysberegayushchy diuretics - a hyperpotassemia; with lithium salts - lithium removal delay.

Immunodepressants, Allopyrinolum, cytostatics strengthen a gematotoksichnost. Hypoglycemic means - increase risk of a hypoglycemia.

Contraindications:

Hypersensitivity to a zofenopril and other APF inhibitors, existence in the anamnesis of the Quincke's disease connected with treatment by APF inhibitors, a porphyria, the expressed abnormal liver functions, pregnancy, the lactation period, aged up to 18 years (efficiency and safety are not established), a heavy renal failure.

With care it is necessary to apply Зокардис® 7,5 at primary hyper aldosteronism, a bilateral stenosis of renal arteries, a stenosis of an artery of the only kidney, a hyperpotassemia, a state after transplantation of a kidney; an aortal stenosis, a mitral stenosis (with disturbances of a hemodynamics), an idiopathic hypertrophic subaortal stenosis, diseases of connecting fabric, cerebrovascular diseases, a diabetes mellitus, a renal failure (a proteinuria more than 1 g/days), a liver failure, at the patients keeping to a diet with restriction of salt or being on a hemodialysis at a concomitant use with immunodepressants and saluretics, at elderly people (75 years are more senior), psoriasis.

It is necessary to be careful at appointment to patients with the reduced volume of the circulating blood (as a result of therapy by diuretics, at restriction of consumption of table salt, carrying out a hemodialysis, diarrhea and vomiting) - the risk of the sudden and expressed decrease in the ABP after use even of an initial dose of APF inhibitor is increased.

Use at pregnancy and a lactation

The drug Зокардис® 7,5 cannot be used during pregnancy and it is not necessary to apply to women of childbearing age in the absence of effective contraception. As zofenoprit calcium it is allocated in breast milk, drug should not be used to nursing mothers.

Overdose:

Symptoms: the expressed decrease in the ABP up to development of a collapse, a myocardial infarction, an acute disorder of cerebral circulation or tromboembolic episodes, spasms, a stupor.

Treatment: the patient is transferred to horizontal position with a low headboard. In mild cases the gastric lavage and intake of saline solution, in more hard cases - the actions directed to stabilization of the ABP are shown: intravenous administration of 0,9% of solution of sodium of chloride, plasma substitutes, if necessary - administration of angiotensin II, a hemodialysis (enalaprilat removal speed – 62 ml/min.).

Storage conditions:

List B. At a temperature not above 25 °C to store in the place, unavailable to children! Period of validity 3 years. Expiration date of a period of validity is given on a folding cardboard pack. Not to use after the date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets, coated, on 7,5 mg.

On 7 or 14 tablets in the blister from PVC / aluminum foil.

On 1 or 2 blisters together with the application instruction place in a cardboard pack.