Hypertension. Symptomatic heart failure. Prevention of symptomatic heart failure in patients with left ventricular dysfunction (with ejection fraction ≤35%). Diabetic nephropathy (with microalbuminuria).
Composition:
1 tabl contains 5 mg, 10 mg or 20 mg of Enalapril maleate.
Action:
Enalapril is converted in the liver to enalaprilat, which is an angiotensin-converting enzyme inhibitor - an enzyme that catalyzes the conversion of angiotensin I to angiotensin II in tissues and tissues, and the degradation of bradykinin, which causes blood vessels to widen. Enalapril also reduces the secretion of aldosterone. In hypertensive patients, enalapril causes hypotension in the supine and standing position without compensatory increase in cardiac function. In patients with heart failure, enalapril causes a reduction in peripheral resistance, blood pressure, and increased cardiac output at reduced heart rate. It absorbs quickly after oral administration. Bioavailability is 60% (the presence of food does not affect the absorption of the drug). The maximum concentration in the blood reaches about 1 hour after administration, and the active metabolite (enalaprilat) - after about 3-4 hours. The drug is excreted mainly in the urine, in 40% as enalaprilat, the rest in the unaltered state. T0,5 is about 11 hours.
Contraindications:
Hypersensitivity to Enalapril, other ACE inhibitors or other components of the preparation. Angioneurotic edema after the use of ACE inhibitors. Idiopathic or congenital angioneurotic edema. II and III trimester of pregnancy. Concomitant use with aliskiren in patients with diabetes mellitus or renal impairment (glomerular filtration rate, GFR <60 ml / min / 1.73 m2).
Precautions:
Particularly cautiously use in patients with bilateral renal artery stenosis or renal artery stenosis of the only functioning kidney (under strict medical supervision, monitoring renal function). Particularly cautiously use in patients with hypovolaemia (caused, inter alia, by diuretics, a diet of sodium, dialysis, diarrhea or vomiting), severe heart failure, treated with high doses of thiazide diuretics, hyponatraemia or impaired renal function, ischemic heart disease or cerebral vessels, with aortic or mitral valve stenosis, with narrowing of the left ventricle outflow pathway (do not use in patients with cardiogenic shock or with haemodynamically significant stenosis). Particularly cautiously use with collagenoses, during immunosuppressive therapy, treatment with Allopurinol or procainamide, especially with co-existing renal dysfunction (regular leukocyte counts should be checked). Caution Use in patients with impaired renal function, diabetes mellitus, patients undergoing major surgery or under general anesthesia with hypotensive agents. Due to the risk of anaphylactoid reactions in dialysis patients, membranes with high permeability should not be used; in patients undergoing apheresis treatment with dextran sulphate, ACE inhibitors should be temporarily discontinued. In patients taking ACE inhibitors during desensitisation (eg Hymenoptera venom), anaphylactoid reactions have been observed. In black patients, the risk of angioneurotic edema is greater and the response to enalapril may be weaker. 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 is not recommended in children for indications other than hypertension. Due to the lack of data, the preparation is not recommended for neonates, children and adolescents with a glomerular filtration rate <30 ml / min / 1.73 m2 and in patients after recent kidney transplantation. The concomitant use of ACE inhibitors, angiotensin II receptor antagonists or aliskiren increases the risk of hypotension, hyperkalaemia and renal dysfunction (including acute renal failure) - therefore, dual blocking of the RAA system is not recommended by concomitant use of ACE inhibitors, angiotensin II receptor antagonists or aliskiren. If the use of a dual RAA blockade 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.In patients with diabetic nephropathy, ACE inhibitors and angiotensin II receptor antagonists should not be used concurrently.
Pregnancy and lactation:
ACE inhibitors are not recommended during the first trimester of pregnancy and breast-feeding. In the second and third trimester, the use of ACE inhibitors is contraindicated. The use of ACE inhibitors in the second and third trimester of pregnancy is toxic to the fetus (renal dysfunction, oligohydramnios, delayed ossification of the skull) and the newborn (renal failure, hypotension, hyperkalemia).
Side effects:
Very common (≥1 / 10): blurred vision, dizziness, cough, nausea, asthenia. Common (≥1 / 100, <1/10): headache, depression, hypotension (including orthostatic hypotension), syncope, myocardial infarction or cerebrovascular episode, chest pain, arrhythmia, angina pectoris, tachycardia, shortness of breath , diarrhea, abdominal pain, taste disorder, rash, hypersensitivity reactions (including angioneurotic edema), fatigue, hyperkalemia, increase in blood creatinine. Uncommon (≥1 / 1000, <1/100): anemia (including aplastic and hemolytic anemia), hypoglycemia, confusion, drowsiness or insomnia, nervousness, paresthesia, dizziness, palpitations, watery runny nose, sore throat, hoarseness, bronchial spasm, asthma, intestinal obstruction, pancreatitis, vomiting, dyspepsia, constipation, loss of appetite, gastric irritation, dry mouth, peptic ulcer, excessive sweating, pruritus, urticaria, alopecia, renal dysfunction, renal failure, proteinuria, impotence, muscle cramps, sudden redness of the skin, tinnitus, malaise, fever, increased urea, hyponatremia. Rare (≥1 / 10,000, <1/1000): sleep disorders, Raynaud's phenomenon, pulmonary infiltrates, eosinophilic pneumonia, stomatitis, inflammation of the tongue, increased liver enzymes, increased bilirubin, neutropenia, decreased hemoglobin and hematocrit values in the blood, thrombocytopenia, agranulocytosis, bone marrow suppression, pancytopenia, enlarged lymph nodes, autoimmune diseases, liver failure, parenchymal or cholestatic hepatitis, hepatitis with necrosis, progressive fulminant hepatic necrosis (sometimes fatal), cholestasis ( including jaundice), oliguria, gynecomastia, erythema multiforme, Stevens-Johnson syndrome, exfoliative dermatitis, toxic epidermal necrolysis, pemphigus, erythroderma. Very rare (<1 / 10,000): angioneurotic bowel edema. A complex set of symptoms has been reported that may include one or more symptoms such as fever, serositis, vasculitis, myalgia, arthritis pain and inflammation, positive anti-nuclear antibody titres, increased ESR, eosinophilia, leukocytosis, photosensitivity or other symptoms skin.
Dosage:
Orally, individually.Hypertension. Adults. In mild hypertension, the recommended starting dose is 5-10 mg. In patients with excessive activity of the renin-angiotensin-aldosterone system (eg in renovascular hypertension, in patients with dehydration and / or salt deficiency, in decompensated heart failure or in severe hypertension) and in patients previously treated with high doses of antiretroviral agents Diuretics, treatment should be started under close medical supervision from a dose of 5 mg or less. If possible, discontinue the diuretic for 2-3 days before enalapril treatment, during treatment should check the level of potassium in the blood and renal function. The usual maintenance dose is 20 mg per day. The maximum daily dose is 40 mg. In children about the month 20-50 kg initial dose is 2.5 mg once a day, about the month > 50 kg - 5 mg once a day. If necessary, the dose can be increased in children by month. 20-50 kg to 20 mg daily, in children at > 50 kg to 40 mg.Heart failure, asymptomatic dysfunction of the left ventricle. Adults. It is used in combination with diuretics and, if necessary, with digitalis glycosides or β-blockers. Treatment should be started under close medical supervision. If no symptomatic hypotension develops at the beginning of treatment of heart failure or occurs but is manageable, the dose should be gradually increased: 1-3 days of treatment 2.5 mg per day in 1 dose, 4-7 days of treatment 5 mg per day in 2 doses; in 2 weekstreatment with 10 mg daily in 1-2 doses, in 3 and 4 weeks of treatment with 20 mg daily in 1-2 doses. The optimal therapeutic dose should be achieved within 2-4 weeks of treatment. A maximum dose of 40 mg should be given in 2 doses. In patients using diuretics, if possible, reduce the dose before starting treatment. The occurrence of hypotension after the first dose, does not prejudge that it occurs in the long-term use of the preparation and does not require discontinuation of treatment, should control the level of potassium in the blood and renal function. In patients with renal insufficiency, the interval between consecutive doses should be increased: creatinine clearance 31-80 ml / min - initial dose is 5-10 mg per day; creatinine clearance 11-30 ml / min - initial dose is 2.5 mg per day; creatinine clearance ≤10 ml / min - the initial dose is 2.5 mg on the dialysis day, the dose of the drug on dialysis days should be adjusted to the current blood pressure (enalaprilate is removed from the circulation during dialysis).Diabetic nephropathy (with microalbuminuria). The usual starting dose is 2.5-5 mg, then the dose should be gradually increased until the optimal reduction of albuminuria is achieved, so as not to reduce the pressure below 120/70 mmHg.
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