Expiration date: 03/2025
Composition and form of issue:
Zocardis, 7, 5
Tablets, film-coated 1 tab.
zofenopril calcium 7, 5 mg
(equivalent to 7, 2 mg of zofenopril)
excipients: lactose monohydrate magnesium stearate microcrystalline starch, corn silicon dioxide highly dispersed
in a blister 7 or 14 PCs. in a pack of cardboard 1 or 2 blisters.
Zocardis 30
Tablets, film-coated 1 tab.
zofenopril calcium 30 mg
(equivalent to 28, 7 mg of zofenopril)
excipients: lactose monohydrate magnesium stearate microcrystalline starch, corn silicon dioxide highly dispersed
in a blister 7 or 14 PCs. in a pack of cardboard 1 or 2 blisters.
Description of dosage form:
Zocardis 7, 5: white round tablets, film-coated, slightly convex on both sides.
Zocardis 30: white oval tablets coated with a bilateral notch for the division.
Characteristic:
ACE inhibitor.
Pharmacological action:
The mechanism of action is associated with a decrease in the formation of angiotensin II from angiotensin I, a decrease in the content of which leads to a direct decrease in the release of aldosterone. Lowers OPS, sad and dad, post-and preload on myocardium. Dilates the arteries to a greater extent than the veins while reflex increase in heart rate is not observed. Reduces the degradation of bradykinin, increases the synthesis of PG.
Pharmacokinetics:
Zofenopril, calcium is rapidly and completely absorbed in the gastrointestinal tract and almost completely metabolized in the liver to form the active metabolite zofenoprilat, Cmax whose blood is achieved through 1, 5 after reception Nocardia.
Approximately 88% of zofenopril calcium binds to plasma proteins.
T1/2 zofenoprilat — 5, 5 h, its total clearance is 1300 ml/min after an oral dose of zofenopril of calcium. Excreted zofenoprilat mainly kidneys-69%, through the intestine-26%.
Description of pharmacological action:
The hypotensive effect is more pronounced at a high concentration of plasma renin than at normal or reduced concentration. Lowering blood PRESSURE in the therapeutic range has no effect on cerebral circulation, blood flow in the vessels of the brain is maintained at a sufficient level and on the background of low blood PRESSURE. Increases coronary and renal blood flow.
With long - term use, the hypertrophy of the left ventricle of the myocardium and the myocyte walls of the arteries of the resistive type decreases, prevents the progression of heart failure and slows the development of left ventricular dilation. Improves blood supply to ischemic myocardium. Lowers platelet aggregation.
Calcium zophenopril is a prodrug, since the active inhibitor is a free sulfhydryl compound — zophenoprilate, formed as a result of thioester hydrolysis.
Hypotensive effect when administered occurs after 1 h, reaches a maximum of 4-6 h and lasts up to 24 h. some patients need therapy for several weeks to achieve the optimal level of blood PRESSURE. With heart failure, a noticeable clinical effect is observed with long — term treatment-6 months or more.
Indications:
Arterial hypertension of mild and moderate severity.
Acute myocardial infarction with symptoms of heart failure in patients with stable hemodynamic parameters and not receiving thrombolytic therapy.
Contraindications:
Hypersensitivity to zofenopril and other ACE inhibitors, the presence of a history of angioedema associated with the treatment of ACE inhibitors, porphyria, severe hepatic impairment, severe renal failure, pregnancy, breastfeeding, age up to 18 years (efficacy and safety have not been established).
With caution — primary aldosteronism, bilateral renal artery stenosis, single kidney artery stenosis, hyperkalemia, post-kidney transplantation condition, aortic stenosis, mitral stenosis (with hemodynamic disorders), idiopathic hypertrophic subaortic stenosis, connective tissue diseases, cerebrovascular diseases, diabetes, renal failure (proteinuria more than 1 g/day), hepatic insufficiency, in patients on a diet with restriction of salt or hemodialysis, concomitant administration with immunosuppressants and saluretics, in the elderly (over 75 years), psoriasis, in patients with reduced BCC (as a result of diuretic therapy, with limited salt intake, hemodialysis, diarrhea and vomiting) — increased risk of sudden and pronounced decrease in blood PRESSURE after the application of even the initial dose of ACE inhibitor.
Use during pregnancy and breast-feeding:
Contraindicated during pregnancy and breastfeeding (because of zofenopril calcium is excreted in breast milk). Do not use in women of childbearing age in the absence of effective contraception.
Side effect:
From the cardiovascular system: excessive lowering of blood PRESSURE, orthostatic collapse rarely-chest pain, angina, myocardial infarction (usually associated with a marked decrease in blood PRESSURE), arrhythmia (atrial Brady or tachycardia, atrial flicker), heartbeat, thromboembolism of the branches of the pulmonary artery, pain in the heart, fainting.
CNS: dizziness, headache, weakness, insomnia, anxiety, depression, confusion, fatigue, drowsiness (2-3%), very rarely when using high doses — nervousness, paresthesia.
From the senses: rarely-violations of the vestibular apparatus, hearing and vision disorders, tinnitus.
From the digestive tract: dry mouth, anorexia, dyspeptic disorders (nausea, diarrhea or constipation, vomiting, abdominal pain) is very rare — intestinal obstruction, pancreatitis, impaired liver and bile secretion, hepatitis, jaundice.
From the respiratory system: unproductive dry cough is very rare-interstitial pneumonitis, bronchospasm, shortness of breath, rhinorrhea, pharyngitis.
From the urinary system: impaired renal function, proteinuria.
Allergic reactions: rarely — skin rash, angioedema of the face, limbs, lips, tongue, glottis and/or larynx, dysphonia, polymorphic erythema, exfoliative dermatitis very rarely — Stevens-Johnson syndrome, toxic epidermal necrolysis, pemphigus, itching, urticaria, photosensitization, serositis, vasculitis, myositis, arthralgia, arthritis, stomatitis, glossit.
Laboratory parameters: hypercreatinemia, increased urea content, increased activity of hepatic transaminases, hyperbilirubinemia, hyperkalemia, hyponatremia. There are in some cases a decrease in hematocrit and hemoglobin, increased ESR, thrombocytopenia, neutropenia, agranulocytosis (in patients with autoimmune diseases), eosinophilia.
Drug interaction:
Hypotensive effect of ACE inhibitors can be enhanced by other antihypertensive agents, diuretics, General anesthetics, antipyretic and painkillers, ethanol. While the appointment of zofenopril NSAIDs may decrease the hypotensive effect of zofenopril, potassium-sparing diuretics is hyperkalemia with lithium salts slowing down the excretion of lithium. Immunosuppressants, allopurinol, cytostatics increase hematotoxicity. While taking with hypoglycemic agents increases the risk of hypoglycemia.
Dosage and administration:
Inside, regardless of the time of meal (before, during or after a meal), with a sufficient amount of liquid.
Zocardis, 7, 5
Arterial hypertension
Patients with normal renal and hepatic function. To achieve optimal blood PRESSURE treatment begins with 2 tables. 1 once a day with insufficient severity of the hypotensive effect, the dose is gradually increased with an interval of 4 weeks.
Usual effective dose is 4 tab. 1 time per day.
The maximum daily dose - 8 table., taken once or in 2 admission (4 table.).
Patients with impaired water-salt balance. Initial therapy with ACE inhibitors requires adjustment of salt and / or water deficits, discontinuation of diuretic therapy for 2-3 days before the start of ACE inhibitor and begins with a dose of 2 tables. Zocardis, 7, 5 1 times a day. If this is not possible, treatment begins with 1 table. Zocardis, 7, 5 1 times a day.
Patients with impaired renal function or on hemodialysis. Patients with mild renal impairment (creatinine Cl more than 45 ml/min) do not require dose reduction. Patients with moderate to severe renal impairment (creatinine Cl less than 45 ml / min) are prescribed 1/2 therapeutic dose once a day.
The initial dose for patients on hemodialysis is 1/4 the dose used for patients with normal kidney function.
Patients with impaired liver function. In patients with mild and moderate liver dysfunction initial dose is half the dose used in patients with normal liver function.
In patients with severe violations of the liver, Zocardis 7, 5 should not apply.
Elderly patient. Elderly patients with normal creatinine clearance do not require dose adjustment. In elderly patients With CL creatinine less than 45 ml/min recommended 1/2 daily dose.
Acute myocardial infarction (as part of combination therapy)
Treatment begins within 24 hours after the first symptoms of myocardial infarction and continues for 6 weeks.
The following dosage regimen should be used:
1st and 2nd day: 1 table. Zocardis, 7, 5 every 12 hours,
Day 3 and 4: table 2. Zocardis, 7, 5 every 12 hours,
from day 5 onwards: table 4. Zocardis 7, 5 every 12 hours.
In case of excessive lowering of blood PRESSURE at the beginning of treatment or within the first 3 days after myocardial infarction, the initial dose is not increased or the drug is canceled.
After 6 weeks of treatment may be discontinued in patients without signs of left ventricular failure or heart failure.
For the correction of left ventricular failure or heart failure, as well as hypertension, treatment can be continued for a long time.
Elderly patient. Zocardis, 7, 5 should be used with caution in patients with myocardial infarction older than 75 years.
Zocardis 30
Arterial hypertension
Patients with normal renal and hepatic function. To achieve optimal blood PRESSURE treatment begins with 1/2 table. 1 once a day with insufficient severity of the hypotensive effect, the dose is gradually increased with an interval of 4 weeks.
Usually effective dose - 1 table. 1 time per day.
The maximum daily dose - 2 tables., taken once or in 2 admission (1 table.).
Patients with impaired water-salt balance. Initial therapy with ACE inhibitors requires adjustment of salt and / or water deficits, discontinuation of diuretic therapy for 2-3 days before the start of ACE inhibitor and begins with a dose of 1/2 table. Zocardis 30, 1 time per day. If this is not possible, treatment begins with 1/4 table. Zocardis 30, 1 time per day.
Patients with impaired renal function or on hemodialysis. Patients with mild renal impairment (creatinine Cl more than 45 ml/min) do not require dose reduction. Patients with moderate to severe renal impairment (creatinine Cl less than 45 ml / min) are prescribed 1/2 therapeutic dose once a day.
The initial dose for patients on hemodialysis is 1/4 the dose used for patients with normal kidney function.
Patients with impaired liver function. In patients with mild and moderate liver dysfunction initial dose is half the dose used in patients with normal liver function.
In patients with severe violations of the liver, Zocardis 30 need not apply.
Elderly patient. Elderly patients with normal creatinine clearance do not require dose adjustment. In elderly patients With CL creatinine less than 45 ml/min recommended 1/2 daily dose.
Acute myocardial infarction (as part of combination therapy)
Treatment begins within 24 hours after the first symptoms of myocardial infarction and continues for 6 weeks.
The following dosage regimen should be used:
1st and 2nd day: 1/4 table. Zocardis 30 every 12 hours,
Day 3 and 4: 1/2 table. Zocardis 30 every 12 hours,
from the 5th day onwards: 1 table. Zocardis 30 every 12 hours
In case of excessive lowering of blood PRESSURE at the beginning of treatment or within the first 3 days after myocardial infarction, the initial dose is not increased or the drug is canceled.
After 6 weeks of treatment may be discontinued in patients without signs of left ventricular failure or heart failure.
For the correction of left ventricular failure or heart failure, as well as hypertension, treatment can be continued for a long time.
Elderly patient. Zocardis 30 should be used with caution in patients with myocardial infarction older than 75 years.
Special instruction:
Transient marked decrease in blood PRESSURE is not a contraindication to continue treatment with the drug after stabilization of blood PRESSURE. In the case of a re-expressed decrease in blood PRESSURE should reduce the dose or cancel the drug.
With the development of excessive lowering of blood PRESSURE, the patient is transferred to a horizontal position with a low headboard, if necessary, 0, 9% sodium chloride solution and plasma-substituting drugs are administered.
The use of high-flow dialysis membranes increases the risk of anaphylactic reaction. Correction dosing regimen in days free of dialysis, should be carried out depending on the level of blood PRESSURE. Before and after treatment with ACE inhibitors necessary to control blood PRESSURE, blood counts (hemoglobin, potassium, creatinine, urea), the activity of liver enzymes, protein in the urine.
It should be carefully monitored for patients with severe heart failure, coronary artery disease and cerebrovascular disease, in which a sharp decrease in blood PRESSURE can lead to myocardial infarction, stroke or renal dysfunction. Sudden cancellation of treatment does not lead to the syndrome of "cancellation" (a sharp rise in blood PRESSURE).
In patients with an indication of the development of angioedema in the anamnesis there is an increased risk of its development when taking ACE inhibitors.
For newborns and infants who have been exposed to intrauterine ACE inhibitors, it is recommended to conduct careful monitoring for the timely detection of a marked decrease in blood PRESSURE, oliguria, hyperkalemia and neurological disorders, possible due to a decrease in renal and cerebral blood flow with a decrease in blood PRESSURE caused by ACE inhibitors. If oliguria is necessary to maintenance of blood pressure and renal perfusion through the introduction of appropriate fluids and vasoconstrictor.
In patients with reduced renal function should reduce the single dose or increase the intervals between doses.
During the selection of the therapeutic dose, it is necessary to refrain from driving vehicles and engaging in potentially dangerous activities that require increased concentration and speed of psychomotor reactions, because dizziness is possible, especially after the initial dose of the ACE inhibitor in patients taking diuretics.
Caution should be exercised when exercising in hot weather (risk of dehydration and excessive lowering of blood PRESSURE due to lowering BCC). Before surgery (including dentistry) it is necessary to warn the surgeon/anesthesiologist about the use of ACE inhibitors.
During treatment, it is not recommended to drink alcoholic beverages, because alcohol increases the hypotensive effect of the drug.
