Enalapril

General characteristics. Structure:

Active ingredient: 5 mg, 10 mg or 20 mg of enalapril.

Excipients: potato starch, talc, magnesium stearate, lactose monohydrate

Kardilogichesky drug with the expressed hypotensive action.

Pharmacological properties:

Pharmacodynamics. Enalapril in an organism is hydrolyzed with formation of an active metabolite - enalaprilat. Suppresses formation of angiotensin II and eliminates its vasoconstrictive action. Drug gradually reduces the ABP, without causing change of ChSS and IOC. Reduces OPSS, reduces an afterload. Reduces also preloading, reduces pressure in the right auricle and a small circle of blood circulation. Drug reduces a hypertrophy of a left ventricle. Drug reduces a tone of the taking-out arterioles of balls of kidneys, thereby improving an intraglomerular hemodynamics, and interferes with development of a diabetic nephropathy.

The maximum effect develops in 6-8 h and remains during 24 h. The full therapeutic effect is reached in several weeks of treatment.

Indications to use:

Primary arterial hypertension; secondary arterial hypertension at diseases of kidneys (including at a renal failure, a diabetic nephropathy); chronic heart failure (as a part of a combination therapy); asymptomatic dysfunction of a left ventricle (as a part of a combination therapy)

Route of administration and doses:

Tablets should be swallowed entirely, washing down with a small amount of liquid, regardless of meal. Drug should be accepted in one and too time of day. The mode of dosing is set individually depending on a condition of the patient.

At treatment of arterial hypertension drug is appointed in an initial dose 5mg/days. Dose adjustment is carried out depending on the reached clinical effect. Usually supporting daily dose makes from 10-20mg, in exceptional cases – to 40 mg in 1 or 2 receptions. The initial dose for patients who received diuretics makes 2,5mg 1 times/days.

At chronic heart failure the recommended initial dose of drug makes 2,5mg 1 times/days. It is necessary to increase a drug dose gradually before achievement of the maximum clinical effect; on average selection of an optimum dose requires 2 – 4 weeks. The average maintenance dose makes 2,5 – 10mg/days in 1 reception, the maximum maintenance dose – 40mg/days in 2 receptions.

At asymptomatic dysfunction of a left ventricle the recommended initial dose of drug makes 2,5mg 2 times/days; depending on a condition of the patient dose adjustment is possible. The average maintenance dose makes 10 mg of 2 times/days.

At treatment of arterial hypertension at diseases of kidneys the mode of dosing is set depending on expressiveness of renal failures or from KK values. At KK more 30ml/mines the initial dose makes 5mg/days, at KK less 30ml/mines – 2,5mg/days, the dose of drug should be increased gradually, the satisfactory clinical effect will not be reached yet.

Features of use:

It must be kept in mind a possibility of development of arterial hypotension in patients with heavy heart failure, heavy renal failures, and also at the patients with disturbances of the water and electrolytic balance caused by treatment by diuretics, an electrolyte-deficient diet, diarrhea, vomiting or who are on a hemodialysis.

With care, also because of risk of development of arterial hypotension, appoint drug to patients with an ischemic heart disease, a serious cerebrovascular illness, at a stenosis of the mouth of an aorta with disturbances of a hemodynamics or other obstacles to outflow of blood from a left ventricle. If the patient with arterial hypertension received treatment by diuretics, then they, whenever possible, should be cancelled in 2-3 days prior to treatment by enalapril. Otherwise the risk of development of arterial hypotension significantly increases. If cancellation of diuretics is impossible, then enalapril should be applied in the reduced doses.

At chronic heart failure the dose of diuretics needs to be reduced. It is necessary to cancel drug before a research of function of epithelial bodies. With care appoint to the patients who are engaged in potentially dangerous types of activity requiring special attention and speed of psychomotor reactions.

Side effects:

Arterial hypotension, syncope, dizziness, headache, feeling of fatigue, weakness, dry cough, bronchospasm, nausea, dryness in a mouth, diarrhea, increase in activity of transaminases, cholestatic jaundice, skin rash, a Quincke's disease, a photosensitization, anemia, a leukopenia, thrombocytopenia, an agranulocytosis.

Interaction with other medicines:

At co-administration with kaliysberegayushchy diuretics or drugs of potassium development of a hyperpotassemia is possible.

At simultaneous use with diuretics, a beta – adrenoblockers, metildopy, nitrates, blockers of calcium channels, gidralaziny, Prazozinum strengthening of hypotensive action is possible.

At simultaneous use with NPVS (including with acetylsalicylic acid) decrease in effect of enalapril and increase in risk of development of a renal failure is possible.

simultaneous use with ethanol, and also means for the general anesthesia the risk of development of arterial hypotension increases.

Enalapril weakens effect of the drugs containing theophylline.

At simultaneous use with drugs of lithium removal of lithium is slowed down and its action amplifies.

simultaneous use with Cimetidinum the enalapril elimination half-life is extended.

Contraindications:

Quincke's disease in the anamnesis (including connected using APF inhibitors), a porphyria, pregnancy, a lactation, hypersensitivity to enalapril or other components of drug, hypersensitivity to other APF inhibitors, children's age.

Overdose:

Symptoms: arterial hypotension.

Treatment: the patient should give horizontal position with the raised legs. The gastric lavage with further purpose of absorbent carbon is shown. In more hard cases - in/in administration of isotonic solution of sodium of chloride or plasma substitutes. Carrying out a hemodialysis is possible.

Storage conditions:

In the dry, protected from light place at a temperature not above 25 °C. List B. To store in the place, unavailable to children. Period of validity 2 years.

Issue conditions:

Without recipe

Packaging:

On 10, 15 or 20 tablets in a blister strip packaging. On two or three blister strip packagings on 10 tablets in a pack. On two blister strip packagings on 15 tablets a dosage of 5 mg in a pack. On one or two to a blister strip packaging on 20 tablets a dosage of 5 mg in a pack. Packaging for hospitals: 280 blister strip packagings on 10 tablets a dosage of 5 mg or on 20 tablets a dosage of 5 mg or on 10 tablets a dosage of 10 mg in a box.