Cilazapril - instructions for use, dose, side effects, contraindications

Clinical and pharmacological group: & nbsp

ACE Inhibitors

Included in the formulation

Incibice®

pills inwards

Hoffmann-La Roche Ltd. Switzerland

АТХ:

C.09.A.A.08 Cilazapril

Pharmacodynamics:

ACE inhibitor. It is a prodrug, from which an active metabolite of cilazaprilate is formed in the body. The mechanism of antihypertensive action is associated with inhibition of ACE activity, which leads to a decrease in the rate of conversion of angiotensin I into angiotensin II (which has a pronounced vasoconstrictive effect and stimulates the secretion of aldosterone in the adrenal cortex). As a result of the decrease in the formation of angiotensin II, a secondary increase in plasma renin activity occurs due to the elimination of negative feedback during the release of renin and a direct decrease in the secretion of aldosterone.

Reduces the total peripheral resistance of the vessels (afterload), wedging pressure in the pulmonary capillaries (preload) and resistance in the pulmonary vessels, increases the minute volume of the heart and tolerance to the load.

Pharmacokinetics:

Prodrug. Absorption - 57% (14% - during meals). Absorption is less than 57%. Biotransformation to cisalapril in the liver. The half-life is11-12 hours (for cisalaprylate - 9 hours). Elimination by the kidneys in the form of cisalaprilat (slowed by chronic renal failure). Cisalapril and cisalaprilate are partially removed during hemodialysis.

Indications:

Arterial hypertension (including renovascular), chronic heart failure (as part of combination therapy with digitalis and / or diuretics).

ICD-10

IX.I10-I15.I15 Secondary Hypertension

IX.I10-I15.I10 Essential [primary] hypertension

IX.I30-I52.I50.9 Heart failure, unspecified

Contraindications:

Hypersensitivity (including other ACE inhibitors), angioedema, history, pregnancy, breast-feeding.

Carefully:

Aortic stenosis, children's age (safety and efficacy not determined).

In diseases and conditions accompanied by a decrease in the content of fluid and salts (including vomiting, diarrhea, low salt diet, previous long-term use of saluretics in patients with chronic heart failure), appropriate correction should be made before starting cilazapril.

Patients with angina and cerebrovascular disease require a doctor's supervision, especially at the beginning of the use of cilazapril, because excessive arterial hypotension can cause myocardial infarction or acute impairment of cerebral circulation.

In patients with severe impairment of liver function, hypotension is possible.

When used simultaneously with potassium-sparing diuretics, potassium-containing preparations and dietary supplements, and salt substitutes, careful monitoring of kidney function and potassium levels in the blood is required.

During surgical interventions during the treatment with cilazapril, it is possible to develop arterial hypotension, which should be corrected by the introduction of a sufficient amount of fluid.

Pregnancy and lactation:

Category of recommendations for FDA is not defined. Contraindicated in pregnancy, promotes fetal hypertrophy. For the duration of treatment, breastfeeding should be discontinued.

Dosing and Administration:

Inside, regardless of food intake, once, at the same time of day.

With arterial hypertension, the initial dose of 1-1.25 mg once a day, supporting - 2.5-5 mg per day.

With Renovascular hypertension, the initial dose of 0.5 mg per day is a single dose.

In chronic heart failure, the initial dose is 0.5 mg (under careful medical supervision) with a gradual increase depending on the tolerability and efficacy of the drug and the patient's condition to the lowest maintenance dose of 1 mg per day and further to a maintenance 1-2.5 mg in day. The maximum daily dose is 5 mg once a day.

In case of impaired renal function, in patients with chronic heart failure and concomitant renal dysfunction, the dosing regimen depends on the creatinine clearance: when creatinine clearance is more than 40 ml / min - 1 mg 1 time per day (maximum dose 5 mg per day), 10- 40 ml / min - 0.5 mg once a day (maximum dose - 2.5 mg per day), less than 10 ml / min - 0.25-0.5 mg 1 or 2 times a week, depending on the dynamics HELL.

With cirrhosis of the liver in the initial dose of 0.25-0.5 mg once a day. In elderly patients in the initial dose of 0.5-1.25 mg per day.

Side effects:

From the side CNS: there may be a headache, dizziness, a feeling of fatigue.

From the side respiratory system: a dry, excruciating cough is possible.

From the side digestive system: nausea and digestive disorders are possible; rarely - pancreatitis.

From the side of cardio-vascular system: Arterial hypotension is possible.

From the side urinary system: rarely - increased urea nitrogen and / or increased creatinine (most likely in patients with impaired renal function).

Allergic reactions: rarely - anaphylactoid reactions, angioedema.

Overdose:

Symptoms: possibly the development of hypotension.

Treatment: carrying out measures to increase the volume of circulating blood. Partially removed from the body during hemodialysis.

Interaction:

Potentiates the hypoglycemic effect of oral antidiabetic drugs.

Simultaneous administration of potassium-sparing diuretics can lead to hyperkalemia (especially in patients with renal insufficiency).

With the simultaneous use of antihypertensive drugs, additive antihypertensive action is possible.

With the simultaneous use of hypoglycemic drugs, the risk of developing hypoglycemia increases.

With the simultaneous use of immunosuppressants, cytostatics, allopurinol, the risk of developing leukopenia increases.

With the simultaneous use of potassium-sparing diuretics (including spironolactone, triamterene, amiloride), potassium preparations, salt substitutes and dietary supplements containing potassium, hyperkalaemia may develop (especially in patients with impaired renal function), since ACE inhibitors reduce aldosterone, which leads to a delay in potassium in the body against the background of limiting the excretion of potassium or its additional intake into the body.

With simultaneous use with NSAIDs, a decrease in the antihypertensive effect of cilazapril is possible.

With the simultaneous use of lithium carbonate, it is possible to disrupt the excretion of lithium from the body.

With simultaneous use with procainamide, there may be an increased risk of developing leukopenia.

Special instructions:

Treatment is carried out under regular medical supervision. If acute arterial hypotension occurs, the patient should be given a horizontal position, and if necessary, carry out measures to increase the volume of circulating blood. After compensating the volume of circulating blood, treatment can be continued. If hypotension persists, reduce the dose or cancel the drug. In patients receiving diuretics, to reduce the risk of symptomatic hypotension diuretic should be canceled 2-3 days before the start of treatment. During treatment, hemodialysis should be avoided through high-performance membranes of polyacrylonitrile metal allyl sulfate (for example, AN69), hemofiltration or LDL-apheresis, since anaphylaxis, anaphylactoid reactions and life-threatening shock are possible.

In patients undergoing hyposensitization using aspen or bee venom against the background of treatment with ACE inhibitors, anaphylactic reactions may occur (therapy should be discontinued before the beginning of hyposensitization).

Care should be taken to conduct surgical interventions using anesthetics that have hypotensive effects.

Patients whose activities are associated with the need for concentration of attention and increased speed of psychomotor reactions should take into account that cilazapril may cause dizziness, especially at the beginning of therapy.

Instructions

Cilazapril (Cilazaprilum)