Enalapril

General characteristics. Structure:

Active ingredient: 10 mg of enalapril of a maleate.

Excipients: starch corn, gelatin, methylparaben, calcium phosphate double-base, magnesium stearate, talc, erythrosine of a supr.

Cardiological anti-hypertensive drug.

Pharmacological properties:

Pharmacodynamics. Enalapril – anti-hypertensive drug which mechanism of action is connected with oppression of activity of the angiotensin-converting enzyme leading to reduction of formation of angiotensin-II. Enalapril belongs to "pro-drugs": after its hydrolysis in an organism enalaprilat which inhibits the specified enzyme is formed. Enalapril renders also some diuretic effect.

Along with a lowering of arterial pressure drug reduces before - and an afterload by a myocardium at heart failure, improves blood circulation in a small circle and breath function, lowers resistance in vessels of kidneys that contributes to normalization of blood circulation in them.

Pharmacokinetics. After intake enalapril is quickly and rather fully soaked up from digestive tract. Bioavailability of drug makes 53-74%, linkng with proteins of a blood plasma - 50%. The maximum concentration in blood is reached in 3-4 hours after administration of drug inside.

Duration of action is 12-24 hours. Drug is metabolized in a liver, a part is hydrolyzed in enalaprilat therefore at patients with abnormal liver functions time of the maximum action can increase. Drug is removed by kidneys. The elimination half-life makes about 11 hours.

Indications to use:

Enalapril is appointed at various forms of arterial hypertension, including renovascular hypertensia. Drug is effective at chronic heart failure (as a part of a combination therapy).

Route of administration and doses:

Enalapril is appointed inside irrespective of meal time.

For the patients who are not receiving diuretics - the recommended initial dose of 5 mg a day. Further the dose is selected individually. Usually the dose from 10 to 40 mg a day in one or two receptions is required.

For the patients receiving diuretics - for the purpose of prevention of arterial hypotension, in 1-2 days prior to purpose of therapy diuretic should be cancelled. In case of impossibility of cancellation of diuretic, the recommended initial dose of enalapril of-2,5 mg.

At chronic heart failure it is better to begin treatment with a dose of 2,5 mg of 1 times a day. Constant control of arterial pressure is necessary. Then reception of 2,5 mg 2 times a day within 3-4 days is recommended. Since second week, the dose is increased if necessary to 10 mg of 1 times a day. On 3-4 week the dose is increased to 20 mg in one or two receptions if systolic pressure is not lower than 100 mm of mercury.

Selection of a dose and further treatment can be carried out on an outpatient basis, at the same time it is necessary to estimate the patient's condition not less than 1 time a month (only at selection of a dose survey and control of the doctor is required each 10 days), to carry out control of content of creatinine and electrolytes of blood. Existence of arterial hypotension to 80/60 mm of mercury. against the background of a maintenance therapy in the absence of complaints at the patient is not a reason for drug withdrawal. It is necessary to be careful only at a concomitant use of diuretics (especially loopback and kaliysberegayushchy), and also potassium drugs. At development of arterial hypotension it is necessary to transfer the patient to a bed rest for several days if it does not help, then the patient should enter intravenously 400-800 ml of normal saline solution.

Use of enalapril at the arterial hypertension caused by a nephropathy in patients with a diabetes mellitus. The dosage of drug depends on that, is followed or not a diabetic nephropathy by arterial hypertension. If the diabetic nephropathy proceeds against the background of normal arterial pressure, then use small doses of Enalapril - 2,5 or 5 mg a day. If the nephropathy is followed by arterial hypertension, then doses select as well as at arterial hypertension (as much as possible up to 40 mg a day).

At a renal failure. The usual dosage of drug is recommended for patients at whom the clearance of creatinine is higher than 30 ml/min. (creatinine level in blood not higher than 3 mg/dl). An initial dose - no more than 2,5 mg a day - if clearance of creatinine less than 30 ml/min. Further selection of a dose is carried out individually under control of level of creatinine and electrolytes of blood. For the patients who are on a hemodialysis, the initial dose and a dose in days of dialysis should not exceed 2, 5 mg a day.

Features of use:

Development of arterial hypotension is possible that is not a reason for drug withdrawal, but demands observance of measures of prevention (control of electrolytes of blood, control of arterial pressure, drug dose adjustment).

Development of arterial hypotension during anesthesia at surgeries. Use of Enalapril together with the anesthetics possessing anti-hypertensive action can cause arterial hypotension.

After purpose of enalapril increase in level of an urea nitrogen and serumal creatinine owing to the developed arterial hypotension and secondary renal hypoperfusion is possible.

At purpose of enalapril the previous therapy has to be reconsidered by diuretics and drugs of potassium. In 2 weeks after purpose of enalapril it is necessary to carry out laboratory control: urea nitrogen, creatinine and electrolytes of a blood plasma, and also general analysis of urine. The special attention is deserved by patients at whom chronic heart failure or arterial hypertension are combined with a bilateral stenosis of renal arteries or a stenosis of an artery of the only kidney.

Hyperpotassemia. Enalapril interferes with potassium loss therefore at its use there is no need to use kaliysberegayushchy diuretics and drugs of potassium. Otherwise development of a hyperpotassemia, especially at patients with a renal failure and a diabetes mellitus is possible. Before a research of function of epithelial bodies enalapril should be cancelled.

Side effects:

Enalapril in general is well transferred and in most cases does not cause the side reactions demanding drug withdrawal.

From the central nervous system: in 2-3% of cases – a headache, dizziness, increased fatigue.

From respiratory system: dry cough, asthma. Less than at 2% of patients:

From digestive tract: nausea, diarrhea, it is rare – pancreatitis, a liver failure, dispepsichesky frustration, dryness in a mouth, an abdominal pain.

From cardiovascular system: arterial hypotension, syncope; disturbance of a cordial rhythm, stenocardia is very rare.

Laboratory analyses: a proteinuria, a hyperpotassemia, increase in activity of hepatic transaminases, increase in concentration of bilirubin in blood, a neutropenia, decrease in hemoglobin, a hematocrit and/or leukocytes.

Allergic reactions: skin rashes, separate cases of a Quincke's disease of the person, throat.

Very seldom when using in high doses – sleeplessness, the increased nervous irritability, a depression, disturbance of balance, paresthesia, a sonitus, a hair loss, inflows, a glossitis, impotence; patients with autoimmune diseases have an agranulocytosis.

Interaction with other medicines:

At co-administration of enalapril with non-steroidal anti-inflammatory drugs (NPVS) decrease in hypotensive effect of enalapril is possible; with kaliysberegayushchy diuretics (Spironolactonum, Triamterenum, amiloride) – development of a hyperpotassemia is possible; with lithium salts – lithium removal delay (control of concentration of lithium in a blood plasma is shown).

During treatment it is forbidden to take alcoholic beverages as alcohol strengthens hypotensive effect of drug.

The concomitant use of enalapril with febrifugal and soothing drugs can reduce efficiency of enalapril.

Enalapril weakens effect of the drugs containing theophylline.

Cimetidinum extends effect of enalapril.

Simultaneous use with diuretics, beta adrenoblockers, metildopy, nitrates, blockers of calcium channels, gidralaziny, Prazozinum strengthens hypotensive effect of enalapril.

Contraindications:

Hypersensitivity to enalapril and other inhibitors of an angiotensin-converting enzyme, existence in the anamnesis of the Quincke's disease connected with treatment by APF inhibitors, an aortal stenosis, a mitral stenosis, pregnancy, the lactation period, children's age.

Overdose:

Symptoms: arterial hypotension.

Treatment: It is necessary to put the patient on a back and to raise legs. In mild cases of overdose to the patient appoint inside saline solution. In more serious cases in the conditions of a hospital hold the events directed to stabilization of arterial pressure: intravenous administration of normal saline solution or plasma substitutes. Use of a hemodialysis is possible.

Storage conditions:

List B. In the dry, protected from light place at a temperature not above + 25 °C.
To store in the place, unavailable to children. Period of validity 3 years.

Issue conditions:

According to the recipe

Packaging:

10, 20, 30 or 50 tablets in banks polymeric or cases plastic. 10 tablets in a blister strip packaging from aluminum foil and a film polyvinyl chloride. One bank, a case or 1, 2, 3, 5 or 50 blister strip packagings together with a leaf insert in secondary packaging.