Table. 20 mg, № 30
|enalapril maleate||20 mg|
Other ingredients: lactose monohydrate, basic magnesium carbonate, sodium starch glycolate type A, gelatin, silica fine anhydrous, magnesium stearate, brown iron oxide (E172).
Pharmacodynamics. Enalapril maleate - maleate salt and enalapril. Enalapril Hydrolysis occurs in the liver, forming an active metabolite - enalaprilat, which is an inhibitor of ACE. Inhibition of ACE results in a reduction in the formation of tissues and plasma angiotensin II blood, decrease in aldosterone secretion and increase the activity of renin in blood plasma. The consequence of ACE inhibition is to increase the activity of the kallikrein-kinin system, bradykinin accumulation and as a result - activation of the prostaglandin system. Enalapril maleate in patients with hypertension causes reduction in blood pressure without a compensatory increase in heart rate, decrease in peripheral vascular resistance. In patients with heart failure, enalapril maleate leads to a decrease in peripheral vascular resistance, resulting in a decrease in afterload on the heart. In the treatment of enalapril maleate is an increase in the IOC, and stroke index improving exercise tolerance, decrease of left ventricular hypertrophy, improvement intraglomerular renal blood flow. On the metabolism of glucose and lipoprotein enalapril maleate is not affected.
Pharmacokinetics. Following oral administration in the gastrointestinal tract is absorbed to 60% of the dose. Simultaneous food intake does not affect the absorption of enalaprilat. C max in the blood plasma is achieved in about 4 hours. The effective period polunakopleniya enalaprilat after repeated oral administration is 11 hours. Effective inhibition of ACE activity occurs within 2-4 hours after a single dose of enalapril maleate. Starting antihypertensive action noted after 1 hour, and the maximum effect - in 4-6 hours after ingestion. The duration of action is dose-dependent, however, when using the drug at the recommended doses of the antihypertensive and hemodynamic effects persist for at least 24 hours. In volunteers with normal renal function equilibrium concentration is achieved approximately at the 4th day after the start of the drug. The range of therapeutic dosages of binding to plasma proteins does not exceed 60%. Other metabolites other than enalaprilat unknown. The drug is released mainly by the kidneys. The main components in urine are enalaprilat (40% of the dose) and unmodified enalapril maleate (about 20%).
AG; with existing heart failure symptoms, prevention of heart failure in asymptomatic patients with left ventricular dysfunction (ejection fraction of ≤35%).
food intake does not affect the absorption of enalapril maleate. Dose selected individually depending on the patient's condition and the effect of the drug on blood pressure.
AG. Berlipril initial dose is 5-20 mg, depending on the degree of hypertension and the condition of the patient; multiplicity of reception - 1 time per day. In mild hypertension initial dose is 5-10 mg (prescribe drugs Berlipril Berlipril 5 or 10). Patients with significant activation of the renin-angiotensin-aldosterone system (such as renal hypertension, electrolytic imbalance, cardiac decompensation or severe hypertension) in the treatment process may be a significant reduction in blood pressure, in such a case requires continuous observation of the patient and reducing the initial dose to ≤5 mg . At the beginning of the application of enalapril maleate, in the case of prior diuretic therapy in high doses, can develop as a consequence of hypovolemia and - hypotension. These patients are recommended to start treatment at a dose of ≤5 mg and possibly cancel the diuretic 2-3 days before starting therapy. It is also recommended to monitor renal function and potassium levels in the blood plasma. Usual maintenance daily dose is 20 mg of enalapril maleate, the maximum - 40 mg / day.
Heart failure / asymptomatic left ventricular dysfunction. When treating patients with heart failure and asymptomatic left ventricular dysfunction Berlipril administered in addition to diuretic, or digitalis preparations β-adrenoceptor blockers. Starting dose - 2.5 mg. To determine the degree of influence of the drug on blood pressure treatment should start under close medical supervision. If at the beginning of treatment does not occur symptomatic hypotension or it is transient, dose should be gradually increased until the support (20 mg), which the patient receives singly or as tolerated in 2 hours. This dose titration is recommended in the first 2-4 weeks of therapy.
The recommended dose titration Berlipril in the treatment of patients with heart failure and asymptomatic left ventricular dysfunction.
|1st||Day 1-3-th||2.5 mg / day 1 reception|
|Day 4-7-th||5 mg / day in 2 doses|
|2nd||10 mg / day in 1 or 2 doses|
|3rd and 4th||20 mg / day in 1 or 2 doses|
Before and after the start of therapy with Berlipril should conduct a thorough monitoring of blood pressure and renal function, as there have been reports about the development of hypotension and rarely - renal failure. Prior to initiating therapy dose diuretic treatment for patients, reduce as far as possible. Hypotensive reaction Berliprilom early treatment does not mean that it will occur during prolonged treatment, and it does not exclude further applications. Monitoring the level of potassium should be regularly carried out in the kidney and blood plasma.
Dosing with impaired renal function.
|Creatinine clearance, ml / min||initial dosing|
|> 30 <80||5-10 mg|
|> 10, ≤30||2.5 mg|
|≤10||2.5 mg per day of dialysis|
It should increase the intervals between doses of enalapril maleate and / or reduce the dose. Enalapril dialyzed. In the days free from dialysis, the dose depends on the degree of reduction in blood pressure.
Use in elderly patients. The dose should be adjusted depending on the state of renal function.
Use in children. Children under the age of 6 years the dose should be adjusted individually depending on their condition and the degree of blood pressure lowering. For patients with a body weight of 20-50 kg initial dose of 2.5 mg, the maximum daily - 20 mg; for patients with a body weight ≥50 kg initial dose of - 5 mg, the maximum daily - 40 mg. Berlipril not recommended for use in children with glomerular filtration <30 ml / min / 1.73 m2 due to lack of data.
Hypersensitivity to enalapril maleate to other ACE inhibitors or to any component of the formulation.
A history of angioneurotic edema, which evolved from the use of ACE inhibitors. Hereditary angioedema or idiopathic. During pregnancy and breastfeeding.
patients with a deficit of liquid in the body (due to the use of diuretics, diarrhea, vomiting) enalapril maleate should occur under medical supervision in order to prevent the development of hypotension. Particular caution is needed when it is used in patients with mitral stenosis and blood, with hypertrophic cardiomyopathy. The preparation is not used in the shock which is accompanied by circulatory failure, and hemodynamic significant obstacle in the left ventricle remote tract. There have been reports of kidney failure in the application development enalapril maleate in patients with severe heart failure, which was reversible in its early diagnosis and treatment. Enalapril maleate to patients with bilateral renal artery stenosis or stenosis of the artery only functioning kidney is particularly dangerous due to the possible decrease in blood pressure and renal failure, which can often manifest only mild serum creatinine. Treatment of such patients should begin with low doses carefully titrated dose and monitor renal function. Enalapril maleate is not recommended in patients who have recently had a kidney transplant, due to a lack of application experience. Enalapril maleate override in case of patients with jaundice or significant increase in liver enzymes due to a possible development of fulminant hepatic cholestasis and necrosis, sometimes with fatal consequences. Care must be taken assigning enalapril maleate in patients with connective tissue, while the use of immunosuppressive agents, allopurinol, procainamide due to the possible development of neutropenia / agranulocytosis, thrombocytopenia and anemia. In hemodialysis using high-flux-membranes, e.g. AN 69, and simultaneous use of the enalapril of the risk of anaphylactic reactions, however such combinations should be avoided. If there is a need for specific therapy lipidoafereza or insect stings, you should temporarily halt the use of enalapril and transfer the patient to another drug. In patients with diabetes, both an oral antihyperglycemic agents and enalapril maleate, careful monitoring of blood glucose levels. In applying enalapril maleate may cause dry cough, which disappears after cancellation. Before preparing for surgery the anesthetist should be informed that the patient uses enalapril maleate. During treatment with enalapril may develop hyperkalemia, especially in patients with cardiac and / or renal failure, so you should periodically monitor the level of potassium in the blood. Berlipril drug contains lactose, therefore it should not be used in patients with hereditary galactose intolerance, lactase deficiency in the body, or malabsorption of glucose-galactose.
Use during pregnancy and lactation. Enalapril maleate should not be used in the I trimester of pregnancy and during lactation. If you are planning a pregnancy or diagnosed, it should be as soon as possible to switch to treatment with alternative drugs. In the II and III trimester of enalapril maleate is contraindicated due to its toxic effect on the fetus (worsening renal function oligogidramniya, delayed ossification of bones of the skull) and infants (renal failure, hypotension, hyperkalaemia). If the mother has applied enalapril maleate in the II and III trimester of pregnancy, the fetal ultrasound are recommended to check your kidney function and the skull, and infants should be carefully monitored to detect hypotension, oliguria and hyperkalemia.
Children. Due to the lack of sufficient information on the efficacy and safety of the drug Berlipril in chronic heart failure and left ventricular dysfunction, asymptomatic, the drug is only recommended for children with hypertension. This also applies to infants and children with an indicator of glomerular filtration <30 ml / min / 1.73 m2. For more information regarding the dosing of the drug in children, see
Ability to influence the reaction rate when driving or operating machinery. Dizziness, weakness. Given the possibility of such reactions, should refrain from driving vehicles or working with other mechanisms.
at a temperature of not higher than 30 ° C.