Zocardis 30, pills 30mg, 28pcs

Composition

Active ingredients:

zofenopril calcium 30 mg.

Auxiliary substances:

lactose monohydrate,

magnesium stearate,

microcrystalline cellulose,

corn starch,

colloidal silicon dioxide.

Shell composition:

hypromellose,

titanium dioxide,

macrogol 400,

macrogol 600.

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 the OPSS, systolic and diastolic blood pressure, post – and preload on the myocardium decreases. Dilates the arteries to a greater extent than the veins, while there is no reflex increase in heart rate. Reduces the degradation of bradykinin, increases the synthesis of prostaglandin.

The hypotensive effect is more pronounced at high plasma renin concentrations than at normal or reduced renin concentrations. Lowering blood pressure in the therapeutic range does not affect cerebral circulation, blood flow in the brain vessels is maintained at a sufficient level and against the background of reduced blood pressure. Increases coronary and renal blood flow.

With prolonged use, hypertrophy of the left ventricle of the myocardium and myocytes of the walls of resistive arteries decreases, prevents the progression of heart failure and slows down the development of left ventricular dilation. Improves blood supply to the ischemic myocardium. Reduces platelet aggregation. Zofenopril is a prodrug, because the free sulfhydryl compound (zofenoprilat) formed as a result of thioester hydrolysis has activity.

After oral use, the hypotensive effect develops in 1 hour, reaches a maximum in 4-6 hours and persists for up to 24 hours. In some cases, therapy for several weeks is necessary to achieve optimal blood pressure reduction. In heart failure, a noticeable clinical effect is observed with long-term treatment (6 months or more).

Pharmacokinetics

Suction and distribution

After oral use, zofenopril calcium is rapidly and completely absorbed from the gastrointestinal tract and undergoes almost complete conversion to zofenoprilat.

Cmax of zofenoprilat in blood plasma is reached 1.5 hours after taking Zocardis. The binding to plasma proteins for zofenopril is 88%.

Metabolism and elimination

Zofenopril is rapidly metabolized in the liver to form the active metabolite zofenoprilat. T1 / 2 of zofenoprilat is 5.5 hours, total clearance is 1300 ml/min. Zofenoprilat is mainly excreted 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 hemodynamic parameters and who did not receive thrombolytic therapy.

Use during pregnancy and lactation

Zocardi ® c is contraindicated for use during 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.

Contraindications

• Hypersensitivity to zofenopril and other ACE inhibitors;
• a history of angioedema associated with the use of ACE inhibitors;
• porphyria;
• severe liver function disorders;
• pregnancy and lactation (breastfeeding);
• age up to 18 years (efficacy and safety have not been established);
• severe renal failure.

Zocardis® should be used with caution: in primary hyperaldosteronism, bilateral renal artery stenosis, stenosis of the artery of a single kidney, hyperkalemia, post-kidney transplantation, aortic stenosis, mitral stenosis (with hemodynamic disorders), idiopathic hypertrophic subaortic stenosis, connective tissue diseases, cerebrovascular diseases, diabetes mellitus, renal failure (proteinuria more than 1 g/min). day), hepatic insufficiency, with simultaneous use with immunosuppressants, in the elderly (over 75 years), with psoriasis.

Caution should be exercised when prescribing the drug to patients with reduced BCC (as a result of diuretic therapy, with limited salt intake, hemodialysis, diarrhea and vomiting), because the risk of sudden and pronounced decrease in blood pressure after the use of an ACE inhibitor, even at the initial dose, is increased.

Side effects

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), palpitations, pulmonary embolism, pain in the heart, syncope.

From the central nervous system and peripheral nervous system: dizziness, headache, weakness, insomnia, anxiety, depression, confusion, increased fatigue, drowsiness (2-3%); very rarely (when used in high doses) – nervousness, paresthesia.

From the sensory organs: rarely-disorders of the vestibular apparatus, hearing and vision disorders, 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, liver function disorders, biliary tract disorders, hepatitis, jaundice.

From the respiratory system: unproductive dry cough; very rarely – interstitial pneumonitis, bronchospasm, shortness of breath, rhinorrhea, pharyngitis.

From the hematopoietic system: in some cases, thrombocytopenia, neutropenia, agranulocytosis (in patients with autoimmune diseases), eosinophilia.

From the urinary system: increased creatinine and urea levels, impaired renal function, proteinuria.

From the laboratory parameters: hypercreatinemia, increased urea levels, increased AST, ALT activity, hyperbilirubinemia, hyperkalemia, hyponatremia, in some cases a decrease in hematocrit and a decrease in hemoglobin, an increase in ESR, thrombocytopenia, neutropenia, agranulocytosis (in patients with autoimmune diseases), eosinophilia.

Allergic reactions: rarely – skin rash, angioedema (face, extremities, lips, tongue, glottis and/or larynx), dysphonia, erythema polymorphic, exfoliative dermatitis; very rarely – Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell’s syndrome), pemphigus, pruritus, urticaria, photosensitization, serositis, vasculitis, myositis, arthralgia, arthritis, stomatitis, glossitis.

Interaction

When used together, the antihypertensive effect of ACE inhibitors can be enhanced by other antihypertensive agents, diuretics, general anesthesia, analgesics-antipyretics, and ethanol.

Concomitant use with NSAIDs may reduce the hypotensive effect of zofenopril.

Hyperkalemia may occur when co-administered with potassium-sparing diuretics.

When administered concomitantly with lithium salts, there is a slowdown in the excretion of lithium.

When used together, immunosuppressants, allopurinol, cytostatics increase the hematotoxicity of zofenopril.

Concomitant use with hypoglycemic agents increases the risk of hypoglycemia.

How to take, course of use and dosage

Tablets are taken orally regardless of food intake (before, during or after a meal), washed down with a sufficient amount of liquid.

Arterial hypertension

Patients with normal liver and kidney function

For adults, to achieve an optimal blood pressure level, therapy should begin with a dose of 15 mg (2 tablets of 7.5 mg or 1/2 tablets of 30 mg) 1 time / day and gradually, if the hypotensive effect is insufficient, increase the dose at intervals 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). The frequency of use is 1-2 times / day.

Patients with impaired water-electrolyte balance

Before prescribing ACE inhibitors, correction of water-electrolyte metabolism and discontinuation of diuretic therapy is required 2-3 days before the start of ACE inhibitor use. In this case, the initial dose of Zocardis is 15 mg / day. If the withdrawal of diuretics and normalization of water-electrolyte balance is not possible, then the initial dose of Zocardis should be 7.5 mg / day.

Patients with impaired renal function or undergoing hemodialysis

Zocardis dose adjustment is necessary. If creatinine clearance > 45 ml / min, no dose adjustment is performed, if creatinine clearance >

The initial dose for patients on dialysis is 1/4 of the dose used for patients with normal renal function.

Elderly patients

With normal renal function, no dosage adjustment is required in the elderly. Elderly patients with CC

Patients with impaired liver function

In patients with mild to moderate hepatic insufficiency, the initial dose of Zocardis® is 1/2 of the dose used in patients with normal liver function.

Patients with severe hepatic impairment

Zocardis® is not prescribed.

Acute myocardial infarction

Treatment with Zocardis® begins within 24 hours after the first symptoms of myocardial infarction appear and continues for 6 weeks, using the following scheme::

• The time period of the 1st and 2nd days is 7.5 mg every 12 hours (dosage regimen).
• Time period 3 and 4 days,15 mg every 12 hours (dosage regimen).
• The time period from day 5 onwards is 30 mg every 12 hours (dosage regimen).

If there is an excessive decrease in blood pressure at the beginning of treatment or during the first 3 days after a myocardial infarction, the initial dose is not increased or the drug is discontinued.

After 6 weeks of treatment, therapy may be discontinued in patients without signs of left ventricular failure or heart failure. To correct 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

Zocardis® should be used with caution in patients with myocardial infarction over 75 years of age.

Overdose

Symptoms: a marked decrease in blood pressure (up to the development of collapse, myocardial infarction, acute cerebrovascular accident or thromboembolic complications), convulsions, stupor.

Treatment: the patient is placed in a horizontal position with a low headboard. In mild cases-gastric lavage and ingestion of saline solution, in more severe cases-measures aimed at stabilizing blood pressure (iv use of 0.9% sodium chloride solution, plasma substitutes); if necessary – use of angiotensin II, hemodialysis.

Special instructions

A transient marked decrease in blood pressure is not a contraindication for continuing treatment with the drug after blood pressure stabilization. In case of repeated pronounced decrease in blood pressure, the dose should be reduced or the drug should be discontinued.

With the development of an excessive decrease in blood pressure, the patient is transferred to a horizontal position with a low headboard, if necessary,0.9% sodium chloride solution and plasma substitutes are administered.

The use of high-flow dialysis membranes increases the risk of anaphylactic reactions. Adjustment of the dosage regimen on dialysis-free days should be made depending on the blood pressure level. Before and after treatment with ACE inhibitors, it is necessary to monitor blood pressure, blood parameters (hemoglobin, potassium, creatinine, urea, AST, ALT), and protein levels in the urine.

Patients with severe heart failure, coronary artery disease, and vascular diseases of the brain should be carefully monitored if a sharp decrease in blood pressure can lead to myocardial infarction, stroke, or impaired renal function. Sudden discontinuation of treatment does not lead to a “withdrawal” syndrome (a sharp rise in blood pressure).

Patients with a history of angioedema have an increased risk of developing angioedema when taking ACE inhibitors.

In patients with reduced renal function, the single dose should be reduced or the intervals between doses should be increased. The patient should be warned about the need to exercise carefully when exercising in hot weather (the risk of dehydration and excessive decrease in blood pressure due to a decrease in BCC).

Before carrying out surgical procedures (including dental) should alert the surgeon/anesthesiologist on the use of ACE inhibitors.

For newborns and children who were subjected to in-utero exposure to ACE inhibitors, it is recommended to conduct a careful monitoring for early detection of expressed lower AD, oliguria, hyperkalemia, and neurological disorders, possible due to reduced renal and cerebral blood flow with blood pressure decrease caused by ACE inhibitors. With oliguria, it is necessary to maintain blood pressure and renal perfusion by introducing appropriate fluids and vasoconstrictors.

During the use of the drug, it is not recommended to drink alcoholic beverages, because alcohol increases the hypotensive effect of the drug.

Concomitant use of hypoglycemic agents increases the risk of hypoglycemia.

Influence on the ability to drive vehicles and other mechanisms that require increased concentration of attention

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 of attention and speed of psychomotor reactions, since dizziness is possible (especially after taking the initial dose of an ACE inhibitor in patients taking diuretics).

Form of production

Tablets

Storage conditions

At a temperature not exceeding 30 °C

Shelf life

3 years

Active ingredient

Zofenopril

Conditions of release from pharmacies

By prescription

Dosage form

Tablets