Description
Latin name
Zocardis
Release form
Coated tablets.
Packing
28 pcs.
Pharmacological action
Pharmacodynamics
ACE inhibitor, antihypertensive drug. The mechanism of action is associated with a decrease in the formation of angiotensin II from angiotensin I. A decrease in the content of angiotensin II leads to a direct decrease in the release of aldosterone, while OPSS, systolic and diastolic blood pressure, post- and myocardial preload are reduced. Expands arteries to a greater extent than veins, while a reflex increase in heart rate is not observed. Reduces the degradation of bradykinin, increases the synthesis of prostaglandin.
The antihypertensive effect is more pronounced with a high concentration of plasma renin than with a normal or reduced concentration. The decrease in blood pressure in the therapeutic range does not affect cerebral circulation, blood flow in the vessels of the brain is maintained at a sufficient level and against a background of decreased blood pressure. Enhances coronary and renal blood flow.
With prolonged use, hypertrophy of the left ventricle of the myocardium and myocytes of the walls of the arteries of the resistive type, prevents the progression of heart failure and slows down the development of dilatation of the left ventricle. Improves blood supply to the ischemic myocardium.
Reduces platelet aggregation. Zofenopril is a prodrug, because free sulfhydryl compound (zofenoprilat), resulting from thioether hydrolysis, has activity.
After oral administration, the hypotensive effect develops after 1 hour, reaches a maximum after 4-6 hours and lasts up to 24 hours. In some cases, therapy is needed for several weeks to achieve an optimal decrease in blood pressure. In heart failure, a noticeable clinical effect is observed with prolonged treatment (6 months or more).
Pharmacokinetics
Absorption and distribution of
After oral administration, zofenopril is rapidly and completely absorbed from the gastrointestinal tract and undergoes almost complete conversion to zofenoprilat.
Cmax of zofenoprilat in blood plasma is achieved 1.5 hours after taking Zokardis. Plasma protein binding for zofenopril is 88%.
Metabolism and excretion
Zofenopril is rapidly metabolized in the liver to form the active metabolite of zofenopril. T1 / 2 of zofenoprilat is 5.5 hours, the total clearance is 1300 ml / min. Zofenoprilat is excreted mainly by the kidneys – 69%, through the intestines – 26%.
Indications
Mild to moderate arterial hypertension.
Acute myocardial infarction with symptoms of heart failure in patients with stable hemodynamics and not receiving thrombolytic therapy.
Contraindications
Hypersensitivity to zofenopril and other ACE inhibitors
angioedema associated with the use of ACE inhibitors, a history of
porphyria
severe liver dysfunction
pregnancy and lactation (breastfeeding)
age under 18 years (efficacy and safety have not been established)
severe renal failure.
Zocardis ® should be used with caution: in case of primary hyperaldosteronism, bilateral renal artery stenosis, stenosis of a single kidney artery, hyperkalemia, condition after kidney transplantation, aortic stenosis, mitral stenosis (with hemodynamic impairment), idiopathic hypertrophic cerebral cortical disease, diseases, diabetes mellitus, renal failure (proteinuria more than 1 g / day), liver failure, with simultaneous use immunosuppressants, in the elderly (over 75 years) with psoriasis.
Caution must be exercised when prescribing the drug to patients with reduced BCC (as a result of diuretic therapy, while restricting salt intake, hemodialysis, diarrhea and vomiting), because increased risk of a sudden and pronounced decrease in blood pressure after the use of an ACE inhibitor, even at the initial dose.
Use during pregnancy and lactation
Zocardi ® is contraindicated in pregnancy and lactation (breastfeeding).
When using the drug, women of childbearing age should use reliable methods of contraception.
Zofenopril calcium is excreted in breast milk.
Composition
1 tablet contains:
Active ingredients:
zofenopril 30 mg.
Excipients:
lactose monohydrate,
magnesium stearate,
microcrystalline cellulose,
corn starch,
silicon dioxide colloidal.
Composition of the shell:
hypromellose,
titanium dioxide,
macrogol 400,
macrogol 600.
Dosage and administration
Tablets are taken orally, regardless of the meal (before, during or after a meal), drinking plenty of fluids.
Arterial hypertension
Patients with normal liver and kidney function
Adults should begin with a dose of 15 mg to achieve optimal blood pressure (2 tablets, 7.5 mg or 1/2 tab. 30 mg) 1 time / day and gradually, with insufficient severity of the hypotensive effect, increase the dose with an interval of 4 weeks.
The average dose is 30 mg 1 time / day (4 tablets of 7.5 mg or 1 tablet of 30 mg).
The maximum daily dose is 60 mg (8 tablets of 7.5 mg or 2 tablets of 30 mg). Multiplicity of admission is 1-2 times / day.
Patients with impaired water-electrolyte balance
Before prescribing ACE inhibitors, correction of water-electrolyte metabolism and cancellation of diuretic therapy 2 3 days before starting an ACE inhibitor are required. In this case, the initial dose of Zocardis is 15 mg / day. If the abolition of diuretics and normalization of the water-electrolyte balance is not possible, then the initial dose of Zokardis should be 7.5 mg / day.
Patients with impaired renal function or undergoing hemodialysis
Zocardis dose adjustment is required. With CC> 45 ml / min, dose adjustment is not performed, with CC <45 ml / min, the dose should be reduced to 1/2 the average therapeutic dose 1 time / day. The starting dose for dialysis patients is 1/4 of the dose used for patients with normal renal function. Elderly patients With normal renal function, dosage adjustment in the elderly is not required. Elderly patients with CC <45 ml / min are recommended 1/2 of the average therapeutic dose. Patients with impaired liver function In patients with mild to moderate hepatic insufficiency, the initial dose of Zokardis ® is 1/2 the dose used in patients with normal liver function. Patients with severe hepatic impairment Zokardis ® is not prescribed. Acute myocardial infarction Treatment with Zokardis ® is started within 24 hours after the onset of the first symptoms of myocardial infarction and continues for 6 weeks, with the following regimen applied: Time period 1 and 2 days 7.5 mg every 12 hours (dosing regimen). Time period 3rd and 4th day, 15 mg every 12 hours (dosing regimen). Time period from the 5th day onwards to 30 mg every 12 hours (dosing regimen). With an excessive decrease in blood pressure at the beginning of treatment or during the first 3 days after myocardial infarction, the initial dose is not increased or the drug is canceled. After 6 weeks of treatment, therapy may be discontinued in patients with no evidence of left ventricular failure or heart failure. For the correction of left ventricular failure or heart failure, as well as arterial hypertension, treatment can be continued for a long time. Dosage in elderly patients with acute myocardial infarction Zokardis ® should be used with caution in patients with myocardial infarction older than 75 years. Side effects of the From the cardiovascular system: excessive decrease in blood pressure, orthostatic collapse rarely – pain behind the sternum, angina pectoris, myocardial infarction (usually associated with a pronounced decrease in blood pressure), arrhythmias (atrial brady or tachycardia, atrial fibrillation, , thromboembolism of the branches of the pulmonary artery, pain in the heart, fainting. From the side of the central nervous system and peripheral nervous system: dizziness, headache, weakness, insomnia, anxiety, depression, confusion, increased fatigue, drowsiness (2-3%) is very rare (when used in high doses) – nervousness, paresthesia. On the part of the sensory organs: rarely – disturbances in the vestibular apparatus, impaired hearing and vision, tinnitus. From the digestive system: dry mouth, anorexia, dyspeptic disorders (nausea, diarrhea or constipation, vomiting, abdominal pain), increased activity of hepatic transaminases, hyperbilirubinemia, intestinal obstruction, pancreatitis, impaired liver function, disorders of the biliary tract, hepatitis, jaundice. From the respiratory system: unproductive dry cough is very rare – interstitial pneumonitis, bronchospasm, shortness of breath, rhinorrhea, pharyngitis. From the hemopoietic system: in some cases, thrombocytopenia, neutropenia, agranulocytosis (in patients with autoimmune diseases), eosinophilia. From the urinary system: increased creatinine and urea, impaired renal function, proteinuria. On the part of laboratory parameters: hypercreatinemia, increased urinary levels, increased activity of AST, ALT, hyperbilirubinemia, hyperkalemia, hyponatremia, in some cases, a decrease in hematocrit and a decrease in hemoglobin, increased ESR, thrombocytopenia, neutropenia, agranulocytosis (in patients with autoimmune diseases), eosinophilia. Allergic reactions: rarely – skin rash, angioedema (face, limbs, lips, tongue, glottis and / or larynx), dysphonia, polymorphic erythema, exfoliative dermatitis very rarely – Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell syndrome) , pemphigus, itching, urticaria, photosensitivity, serositis, vasculitis, myositis, arthralgia, arthritis, stomatitis, glossitis. Drug Interaction When used jointly, the antihypertensive effect of ACE inhibitors may be enhanced by other antihypertensive agents, diuretics, general anesthesia agents, antipyretics, ethanol. When administered with NSAIDs, the antihypertensive effect of zofenopril may be reduced. Hyperkalemia may occur when co-administered with potassium-sparing diuretics. When used simultaneously with lithium salts, there is a slowdown in lithium removal. When used together with immunosuppressants, allopurinol, cytostatics enhance the hematotoxicity of zofenopril. When administered with hypoglycemic agents, the risk of hypoglycemia increases. overdose Symptoms: marked decrease in blood pressure (until collapse, myocardial infarction, acute cerebral circulation or thromboembolic complications), convulsions, stupor. Treatment: the patient is transferred to a horizontal position with a low head. In mild cases – gastric lavage and intake of saline solution, in more severe cases – measures aimed at stabilizing blood pressure (in / in the introduction of 0.9% sodium chloride solution, plasma substitutes) if necessary – the introduction of angiotensin II, hemodialysis. Storage conditions Keep out of the reach of children at a temperature not exceeding 30 ° C. Expiration 3 years. Deystvuyuschee substances zofenopril dosage form dosage form tablets Berlin-Chemie / Menarini Germany
