Index of drugs

Treatment of hypertension. Treatment of chronic heart failure.

1 tabl powl. contains 0.5 mg, 1 mg, 2.5 mg or 5 mg of cilazapril (and respectively: 62.478 mg, 61.956 mg, 123.39 mg or 120.78 mg lactose).

Cilazapril is a long-acting inhibitor of angiotensin converting enzyme (ACE), inhibiting the activity of the renin-angiotensin-aldosterone system and conversion of inactive angiotensin I to angiotensin II - a substance with potent vasodilator effect. Cilazapril is effective in all degrees of essential hypertension and renal arterial hypertension. It causes lowering systolic and diastolic blood pressure both in the standing and lying position, usually without the orthostatic component. Cilazapril is a biologically inactive substance - after absorption from the gastrointestinal tract it is converted to active cilazaprilat. The bioavailability of cilazaprilat is approximately 60%. C_max in the blood reaches within 2 h after administration. Cilazaprilate is excreted unchanged mainly by the kidneys and its effective T_0,5 is 9 hours.

Hypersensitivity to cilazapril, other ACE inhibitors or to any of the excipients. History of angioneurotic edema associated with treatment with ACE inhibitors. Congenital or idiopathic angioedema. Co-administration with aliskiren in patients with diabetes or renal impairment (GFR <60 ml / min / 1.73 m²). II and III trimester of pregnancy.

The drug should be used with extreme caution in patients with mitral valve stenosis and narrowing of the left ventricle outflow tract, as is the case with aortic valve stenosis or hypertrophic cardiomyopathy. Due to the increased risk of symptomatic hypotension, caution should be exercised in patients with water-electrolyte disturbances (associated with the use of diuretics, salt-restricted diet, dialysis, diarrhea or vomiting), with severe renin-dependent hypertension, with more severe heart failure, treated with high doses of loop diuretics, patients with hyponatraemia or renal dysfunction - these patients should be carefully monitored at the beginning of treatment and during dose escalation; if possible, the diuretic should be discontinued for some time. The above remarks also apply to patients with ischemic heart disease or cerebral circulation disorders, in whom excessive reduction of blood pressure may cause a myocardial infarction or cerebrovascular accident. Transient hypotension is not a contraindication to the administration of further doses of the drug, provided that the blood pressure is increased as a result of replenishing the volume of fluids. If hypotension becomes symptomatic, dose reduction or discontinuation of cilazapril should be considered. In patients undergoing surgery or anesthesia using agents that cause hypotension, cilazapril may inhibit the formation of angiotensin II, secondary to compensated renin - cilazapril should be discontinued one day before the planned surgery; in the event of hypotension due to this mechanism, they can be corrected by increasing the volume of fluids. Take caution when using the drug in patients with renal insufficiency (indicated dose modification) - regularly check the concentration of potassium and creatinine in the blood. It is not recommended for patients with CCr <10 ml / min. In patients with symptomatic heart failure, hypotension following the initial dose of an ACE inhibitor may lead to further deterioration of renal function. In patients with bilateral renal artery stenosis or artery stenosis of the sole active kidney, an increase in urea and creatinine in the blood, usually reversible at the end of treatment, may occur after administration of an ACE inhibitor. this particularly applies to patients with renal failure.If renal arterial hypertension coexists, there is an increased risk of severe hypotension and renal failure - these patients should be started under close medical supervision, small doses and careful dose increase; discontinue diuretic therapy and monitor renal function during the first weeks of treatment with cilazapril. There is no information on the use of cilazapril in people who have recently had a kidney transplant. Due to the risk of hypotension, syncope, hyperkalemia and renal dysfunction (including acute renal failure), dual RAA blocking is not recommended (eg, through the combined use of an ACE inhibitor with an angiotensin II receptor antagonist or aliskiren); if the use of the RAA double block is absolutely necessary, it should only be carried out under the supervision of a specialist, and the vital parameters of the patient, such as kidney function, electrolyte concentration and blood pressure should be closely monitored. At the same time, ACE inhibitors and angiotensin II receptor antagonists should not be used in patients with diabetic nephropathy. Exercise caution in patients at risk of hyperkalaemia, eg in patients with renal insufficiency, uncontrolled diabetes, with the use of potassium supplements, potassium-sparing diuretics or serum potassium-increasing drugs - regularly monitor the level of potassium in the blood. Due to the risk of neutropenia and agranulocytosis, it is recommended to periodically determine the number of leukocytes in patients with connective tissue diseases (collagenases), taking immunopressives, Allopurinol or procainamide, and when these coexist, especially if there have been renal dysfunctions. In patients with diabetes, glycemic monitoring should be carefully monitored during the first month of treatment with an ACE inhibitor. In patients treated with ACE inhibitors who have developed jaundice or increased liver enzymes, ACE inhibitors should be discontinued and appropriate treatment initiated. In patients undergoing dialysis with high permeability, there is a high likelihood of anaphylactoid reactions - consideration should be given to using an antihypertensive agent from another group or other type of dialysis membranes. In patients requiring venom desease desensitization or LDL-apheresis treatment with dextran sulphate, it is recommended to temporarily discontinue ACE inhibitors due to the risk of life-threatening anaphylactoid reactions. In patients with angioedema of the face, limbs, lips, tongue, mucous membranes, glottis and or larynx, cilazapril should be immediately discontinued, appropriate therapy should be instituted and the patient monitored until the signs of edema have completely resolved (fatal angioedema has been observed associated with laryngeal or tongue swelling). Patients with angioneurotic edema independent of taking ACE inhibitors may have an increased risk of edema when taking cilazapril. Angioedema of the gut should be taken into account in the differential diagnosis of abdominal pain in patients treated with ACE inhibitors. The black patients are more likely to have angioedema. In black patients, cilazapril may be less effective. In the differential diagnosis of cough, cough induced by ACE inhibitors should be considered. Due to the lactose content, the drug should not be used in patients with rare hereditary galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.

The drug is contraindicated in pregnancy. ACE inhibitors used during pregnancy cause neonatal oligohydramnios and hypotension and / or anuria. It is not known whether cilazapril is excreted in human milk (it is present in animal milk) - do not use during breast-feeding.

Common: headache, dizziness, paresthesia, visual disturbances, tinnitus, hypotension (including symptomatic hypotension), cough, shortness of breath, nausea, vomiting, abdominal pain, taste disturbances, indigestion, diarrhea, constipation, muscle cramps, rash , pruritus, weakness.Uncommon: mood disorders or sleep disorders, bronchospasm, dry mouth, swelling of the face, limbs, lips, mucous membranes, tongue, glottis and / or larynx; urticaria, renal failure, impotence, excessive sweating. Rare: increase in liver enzymes, increase in bilirubin in the blood. Very rare: confusion, arrhythmia, angina pectoris, myocardial infarction and stroke (probably secondary to worsening of hypotension in high-risk patients), eosinophilic pneumonia, rhinitis, pancreatitis, cytolytic or cholestatic hepatitis, erythema multiforme, acute renal failure, decrease in hemoglobin, hematocrit reduction, thrombocytopenia, leukopenia, neutropenia, agranulocytosis, pancytopenia; hemolytic anemia in patients with G-6-PD deficiency. Increases in urea and creatinine in the blood and / or hyperkalemia (occurring after discontinuation of the drug) may occur, especially in the case of renal failure, severe heart failure and renovascular hypertension.

Orally.Hypertension: the recommended starting dose is 1 mg once a day; The maintenance dose is adjusted individually, usually 2.5-5 mg per day. If the normalization of pressure is not achieved after using the 5 mg dose, a low-dose diuretic (from a different group than potassium-sparing diuretics) may be used at the same time. In patients with hypertension treated with diuretic therapy, the diuretic should be discontinued 2-3 days prior to initiation of treatment with cilazapril. The recommended starting dose of cilazapril in these patients is 0.5 mg once a day. If necessary, the use of a diuretic may be resumed later.Chronic heart failure. The preparation can be used simultaneously with digitalis and / or diuretic glycosides; the recommended starting dose is 0.5 mg once a day, under close medical supervision; the dose should be increased to the lowest maintenance dose of 1 mg per day and further to the usual maintenance dose of 1-2.5 mg daily. The maximum dose is 5 mg per day.Special groups of patients. Patients with renal insufficiency: CCr> 40 ml / min - initial dose of 1 mg once a day, maximal dose 5 mg once a day; CCr 10-40 ml / min - initial dose 0.5 mg once a day, maximal dose 2.5 mg once a day); CCr <10 ml / min - not recommended. In patients undergoing hemodialysis, the preparation should be used on days when the patient is not dialyzed; adjust the dose to the arterial pressure.Elderly patients. Hypertension: initial dose - 0.5-1 mg once a day, maintenance dose determined individually depending on the patient's response and tolerability. Chronic heart failure: initial dose - 0.5 mg, maintenance dose - 1-2.5 mg; in elderly patients with chronic heart failure taking high doses of diuretics, it is mandatory to start treatment with a dose of 0.5 mg per day.Children. The efficacy and safety of cilazapril in children have not been established - use is not recommended.Way of giving. It is taken once a day, always at the same time of the day, regardless of meals.