Index of drugs

Treatment of hypertension. Treatment of chronic heart failure.

1 tabl contains 0.5 mg, 1 mg, 2.5 mg or 5 mg of cilazapril. The preparation contains lactose.

A long-acting ACE inhibitor (an enzyme that catalyzes the conversion of angiotensin I to angiotensin II). It inhibits the renin-angiotensin-aldosterone system (RAA) and the conversion of inactive angiotensin I to angiotensin II, which strongly constricts blood vessels. In hypertensive patients, it causes lowering of systolic and diastolic pressure in a sitting and standing position, usually without an orthostatic component. It does not cause reflex tachycardia. The onset of antihypertensive effect occurs within 1 h after dosing, maximum effect is observed after 3-7 h, and the effect of one dose is usually maintained for 24 h. In patients with heart failure, inhibiting the activity of the RAA system, cilazapril improves hemodynamic conditions in overloaded heart by reducing vascular resistance and pulmonary capillary wedge pressure in patients already treated with diuretics and / or digitalis. In addition, these people significantly increase exercise capacity, and thus improve the quality of life. The haemodynamic and clinical effects of the drug are rapid and persist during treatment. Cilazapril is well absorbed from the gastrointestinal tract and is rapidly metabolised to the active metabolite - cilazaprilat. The bioavailability of cilazaprilat following oral administration of cilazapril is approximately 60%; C_max cilazaprilate is achieved within 2 hours. Cylazaprilat is excreted unchanged mainly by the kidneys and its effective T_0,5 is 9 hours.

Hypersensitivity to cilazapril, other ACE inhibitors or other components of the preparation. History of angioneurotic edema associated with prior use of ACE inhibitors. Congenital or idiopathic angioedema. II and III trimester of pregnancy.

The safety and efficacy of cilazapril in children has not been established - use is not recommended. Particularly cautiously use in patients with highly stimulated renin-angiotensin-aldosterone system, due to the risk of significant hypotension and renal impairment (medical supervision is necessary, and the treatment should start with a small dose, very carefully increased) - this applies to . patients with renovascular hypertension (with renal artery stenosis) or other causes that cause renal failure, hyponatraemia, dehydrated or previously treated with vasodilators, with severe heart failure. If possible, the diuretic should be temporarily discontinued. If renal failure occurs, treatment should be discontinued. Similar caution should be exercised in patients with angina or cerebrovascular disease in whom hypotension can cause myocardial or cerebral ischemia. Due to the risk of hypotension, caution should be exercised in patients with obstructive cardiac diseases (eg with aortic valve stenosis or mitral valve or hypertrophic cardiomyopathy with left ventricular tract stenosis) and in patients undergoing major surgery or under general anesthesia with drugs causing hypotension (hypotension can be compensated by increasing the intravascular volume). In patients receiving ACE inhibitors who have developed jaundice or who have a marked increase in liver enzymes, cilazapril should be discontinued. Particularly with caution and in a very small dose, use in patients with liver cirrhosis (without ascites), due to the risk of hypotension. Cilazapril is not recommended for patients with ascites. Because of the risk of neutropenia, caution should be exercised in patients with kidney disease in the course of collagenosis and in patients receiving immunosuppressive agents, especially if they have kidney problems.Concomitant use of ACE inhibitors and potassium-sparing diuretics, potassium or potassium-containing compounds may lead to hyperkalemia, especially in patients with impaired renal function - if such combination therapy is necessary, cilazapril should be used at reduced doses and closely monitored for potassium in the blood and kidney function. Exercise caution in patients with diabetes mellitus, especially if they have renal dysfunction. ACE inhibitors are less effective as antihypertensive agents in black patients. The risk of angioneurotic edema seems to be higher in black patients compared to patients of other breeds. Patients with a history of angioneurotic edema not related to the use of ACE inhibitors may be at higher risk of angioedema. Anaphylactoid reactions may occur in patients receiving ACE inhibitors and dialyzed using high-flow dialysis membranes, eg AN69 (use a different type of membrane or antihypertensive agent from another group) during LDL apheresis with dextran sulphate (discontinue treatment with ACE inhibitor before each apheresis) or in patients undergoing desensitisation, e.g. Hymenoptera venom (ACE inhibitors should be temporarily discontinued and should not be replaced with a beta blocker). Due to the lactose content, the preparation should not be used in patients with galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.

The use of the preparation in the first trimester of pregnancy is not recommended (there is a risk of teratogenic effect). Use in the second and third trimester of pregnancy is contraindicated. Cilazapril used in the second and third trimester of pregnancy is toxic to fetal development (deterioration of renal function, oligohydramnios, delayed ossification of the skull) and newborn (renal failure, hypotension, hyperkalemia) - when exposure to the drug occurred from the second trimester of pregnancy, it is recommended an ultrasound examination of the fetus skull and kidneys; children whose mothers took the drug during pregnancy should be closely monitored for hypotension. The drug is not recommended during breast-feeding.

Common: headache, dizziness, hypotension (including orthostatic), cough, nausea, diarrhea, vomiting, rash, fatigue. Uncommon: mood changes, fainting, sleep disturbances, myocardial infarction or cerebrovascular accident (secondary to significant lowering of blood pressure in high-risk patients), palpitations, tachycardia, Raynaud's fears, rhinitis, chest pain, pain abdominal distress, dyspepsia, digestive disorders, bloom, pruritus, impotence, weakness, moderate elevation of urea and creatinine (transient after discontinuation of treatment, most often seen in patients with renal artery stenosis, renovascular hypertension), hyperkalemia (usually transient). Rare: depression, paresthesia, confusion, dyspnoea, dyspnoea, sinusitis, bronchitis, allergic alveolitis (eosinophilic pneumonia), bronchospasm, dry mouth, angioneurotic edema (face, limbs, lips, tongue, epiglottis) , larynx), urticaria, alopecia, psoriasis, muscle pain, joint pain, kidney damage, uremia, proteinuria in patients with glomerulonephritis, increased bilirubin, increased levels of liver enzymes (transaminases, alkaline phosphatase, GGT), hyponatremia. Very rare: decreases in hemoglobin or hematocrit, myelosuppression, thrombocytopenia, leukopenia, neutropenia, agranulocytosis, haemolytic anemia, generalized enlargement of the lymph nodes, autoimmune diseases, hypoglycaemia, neuropathy, vasculitis, pancreatitis, enterocolitis, cytolytic or cholestatic hepatitis with or without necrosis (in exceptional cases, severe forms), jaundice, hepatic failure, hyperhidrosis, pemphigus, toxic epidermal necrolysis, Stevens-Johnson syndrome, erythema multiforme, acute renal failure, oliguria, anuria, gynecomastia.When ACE inhibitors have been used, a complex syndrome has been reported including one or more of the following: fever, vasculitis, myalgia, arthritis pain and inflammation, positive antinuclear antibody (ANA), accelerated OB, eosinophilia and leukocytosis, rash, photosensitivity or other dermatological symptoms.

Orally. Adults.Hypertension: initial dose 1 mg once a day; The maintenance dose is adjusted individually, usually 2.5-5 mg once a day. In patients with high activity of the renin-angiotensin-aldosterone system (especially in patients with hyponatremia and / or hypovolaemia, heart failure or severe hypertension), the recommended starting dose is 0.5 mg once a day and the treatment should be started under the supervision of a physician. Patients with hypertension taking concomitant diuretic at the same time: starting dose of 0.5 mg once a day, the diuretic should be discontinued 2-3 days before the start of cilazapril; if necessary, you can resume its administration later.Chronic heart failure: starting dose of 0.5 mg once a day for a week, treatment should be started under close medical supervision; if the dose is well tolerated, it may be increased weekly to 1 mg or 2.5 mg; the maximum daily dose is 5 mg.Special groups of patients. In patients with renal impairment, the dose depends on creatinine clearance:> 40 ml / min - initial dose of 1 mg once a day, maximum dose of 5 mg once a day; 10-40 ml / min - initial dose 0.5 mg once a day, maximal dose 2.5 mg once a day; <10 ml / min - not recommended. In patients with renovascular hypertension, treatment should be started under close medical supervision and small doses should be carefully increased; during the first weeks of treatment with the preparation discontinue the use of diuretics and monitor renal function. In patients with cirrhosis (without ascites) the dose is 0.5 mg daily, blood pressure should be carefully monitored. In the elderly, the recommended starting dose for the treatment of hypertension is 0.5-1 mg once a day; in the treatment of chronic heart failure 0.5 mg once a day.
The preparation should be taken once a day, at the same time of the day, regardless of the meal.