Enalapril Geksal

General characteristics. Structure:

Tablets on the 5th mg:aktivny substance: enalapril a maleate – 5,0 mg; excipients: Natrii hydrocarbonas, lactoses monohydrate, corn starch, talc, hypro rod, magnesium stearate.
Tablets on the 10th mg:aktivny substance: enalapril a maleate – 10,0 mg; excipients: Natrii hydrocarbonas, lactoses monohydrate, corn starch, talc, magnesium stearate, ferrous oxide red.

Tablets on the 20th mg:aktivny substance: enalapril a maleate – 20,0 mg; excipients: Natrii hydrocarbonas, lactoses monohydrate, corn starch, talc, magnesium stearate, ferrous oxide red, ferrous oxide yellow.

Pharmacological properties:

Pharmacodynamics. APF inhibitor. Pharmacological activity the enalapril metabolite – enalaprilat has. Suppresses formation of angiotensin II and eliminates its vasoconstrictive action. At the same time the general peripheric vascular resistance, the systolic and diastolic arterial pressure (AP), post-and preload of a myocardium goes down.
Expands arteries more than veins, at the same time reflex increase in heart rate is not noted.
Reduces also preloading, reduces pressure in the right auricle in a small circle of blood circulation, reduces a hypertrophy of a left ventricle. Reduces a tone of the taking-out arterioles of balls of kidneys, reducing thereby an intraglomerular hemodynamics and interferes with a diabetic nephropathy. Does not influence metabolism of glucose, lipoproteins and sexual function.
The maximum effect develops in 6-8 hours and remains within 24 hours. The therapeutic effect is reached in several weeks of treatment.

Pharmacokinetics. After intake about 60% of enalapril are absorbed from a GIT. Meal does not influence drug absorption. Linkng with proteins of plasma less than 50%. Is exposed to hydrolysis with formation of the enalaprilat having the expressed pharmacological activity. The maximum concentration in blood serum of enalapril is reached in 1 hour, - is reached enalaprilat in 3-4 hours. In 4 days after the beginning of reception the size of an elimination half-life makes 11 hours. It is removed generally by kidneys – 60% (20% - in the form of enalapril and 40% - in the form of enalaprilat), through intestines – 33% (6% - in the form of enalapril and 27% - in the form of enalaprilat).

Indications to use:

- Arterial hypertension;
- Chronic heart failure (as a part of a combination therapy)
- Dysfunction of a left ventricle.

Route of administration and doses:

Drug can be used irrespective of meal, washing down with enough liquid.
Day doses accept, as a rule, in the morning, however, administration of drug can be divided into 2 times – morning and evening.
At a concomitant use of diuretics strengthening of hypotensive effect is possible.

Arterial hypertension:
The initial dose makes 5 mg in the morning (1 tablet on 5 mg of enalapril of a maleate). If at reception of the specified dose the size of arterial pressure is not normalized, the day dose can be raised to 10 mg. The interval between increase in doses has to make not less than 3 weeks.
The maintenance dose makes, as a rule, 10 mg of enalapril of a maleate.
The maximum daily dose should not exceed 40 mg a day (2 times on 20 mg of enalapril of a maleate).

Chronic heart failure:
The initial dose makes 2,5 mg in the morning. Increase in a dose should be made gradually, depending on a condition of the patient.
The maintenance dose makes, as a rule, 5 – 10 mg (1 - 2 tablets on 5 mg, or 1 tablet on 10 mg of enalapril of a maleate). The maximum daily dose should not exceed 20 mg (2 tablets on 10 mg, or 1 tablet on 20 mg).

Dysfunction of a left ventricle:
The initial dose makes 2,5 mg of enalapril of a maleate 2 times a day, dose adjustment depending on a condition of the patient is possible. The average maintenance dose makes 10 mg 2 times a day.

Patients with a moderate renal failure (clearance of creatinine of 30 - 60 ml/min.) and patients are aged more senior than 65 years:
The initial dose makes 2,5 mg in the morning.
The maintenance dose makes, as a rule, 5 – 10 mg (1 – 2 tablets on 5 mg or 1 tablet on 10 mg) maleate enalapril in day. The maximum daily dose should not exceed 20 mg (2 tablets on 10 mg, or 1 tablet on 20 mg) enalapril.

Patients with the expressed renal failures (clearance of creatinine less than 30 ml/min.) and being on a hemodialysis:
The initial dose makes 2,5 mg of enalapril of a maleate a day.
The patients who are on a hemodialysis have to accept drug after dialysis.
The maintenance dose makes, as a rule, 5 mg (1 tablet on 5 mg) enalapril in day. The maximum daily dose should not exceed 10 mg (1 tablet on 10 mg, or 2 tablets on 5 mg) in day.
Use of drug in the form of monotherapy, or in a combination with other anti-hypertensive means, especially, with diuretics is possible.

Features of use:

It is necessary to be careful at appointment Geksal's Enalapril to patients with the reduced volume of the circulating blood (as a result of therapy by diuretics, at restriction of consumption of table salt, carrying out a hemodialysis, diarrhea and vomiting) – the risk of the sudden and expressed decrease in the ABP after use even of an initial dose of APF inhibitor is increased. Tranzitorny arterial hypotension is not a contraindication for treatment continuation by drug after stabilization of the ABP. In case of repeated decrease in the ABP it is necessary to reduce a dose or to cancel administration of drug.
Cannot apply enalapril the patients who are on dialysis with use of polyacrylonitronew membranes of AN 69 in connection with probability of development of anaphylactic reactions.
Before administration of drug it is necessary to check function of kidneys. Patients with an impaired renal function should reduce a single dose, or to increase intervals between administrations of drug.
Prior to the beginning of and during treatment it is necessary to control the level of arterial pressure and to carry out the analysis of laboratory parameters, especially at loss of salts and/or liquids, an impaired renal function, heavy or renal hypertensia, heart failure and are aged more senior than 65 years.
In case of the previous treatment by diuretics, in particular, at patients with chronic heart failure, the risk of development of orthostatic hypotonia therefore before an initiation of treatment enalapril it is necessary to offset loss of liquids and salts increases.
At some patients with a bilateral stenosis of arteries of kidneys or a stenosis of the only kidney increase in content of urea in blood and creatinine in serum was observed. Changes had reversible character and indicators were returned to norm after the treatment termination.
For newborns and babies who underwent pre-natal influence of APF inhibitors it is recommended to conduct careful observation for early detection of the expressed decrease in the ABP, an oliguria, a hyperpotassemia and neurologic frustration, possible owing to reduction of a renal and brain blood-groove at decrease in the ABP called by APF inhibitors. At an oliguria maintenance of the ABP and renal perfusion by administration of the corresponding liquids and vasoconstrictors is necessary.
At development of a Quincke's disease of the person, extremities, lips or a throat, it is necessary to stop immediately administration of drug and to see a doctor. Emergence of cough which stops after cancellation of administration of drug is possible.
Sudden cancellation of treatment does not lead to a syndrome of "cancellation" (sharp raising of the ABP).
Before a research of functions of epithelial bodies drug should be cancelled.
Before surgical intervention (including stomatology) it is necessary to warn the surgeon/anaesthesiologist about use of APF inhibitors.
Patients should appoint drug with care with a diabetes mellitus because of risk of development of a hyperpotassemia.

Instructions for participants dorozhno - the transport movement:
As a result of treatment by enalapril development of individual reactions which can break ability of the patient to active participation in dorozhno – the transport movement is possible that should be meant also at service of cars and during the work with the devices requiring special attention. These phenomena amplify at increase in a dose and at alcohol intake.

Side effects:

The majority of side effects are temporary and do not demand cancellation of administration of drug.

From outside warmly – vascular system:
At the beginning of therapy seldom: arterial hypotension (including orthostatic), dizziness, weakness, a vision disorder and is very rare – a retrosternal pain, stenocardia, heartbeat, a thromboembolism of branches of a pulmonary artery.

From respiratory system:
Unproductive dry cough, intersticial pneumonitis, bronchospasm, asthma, rhinorrhea, pharyngitis.

From a digestive tract:
Dryness in a mouth, anorexia, dispepsichesky frustration (nausea, diarrhea or a lock, vomiting. Pains in a stomach), intestinal impassability, pancreatitis, an abnormal liver function and a zhelchevyvedeniya, hepatitis, jaundice.

From a nervous system:
In rare instances there can be a headache, dizziness, weakness, increased fatigue, drowsiness, a consciousness oglushennost; extremely seldom (at reception in high doses) – a depression, a sleep disorder, a peripheral neuropathy and paresthesia, muscular spasms, nervousness, a sonitus and a vagueness of sight. These disturbances are temporary and are normalized after cancellation of administration of drug.

From function of kidneys:
Seldom – renal failures, a proteinuria, development of a hyperpotassemia and hyponatremia, and also flavoring changes (the phenomena are temporary and are normalized after cancellation of administration of drug).

From reproductive system:
Very seldom when using in high doses – impotence.

Allergic reactions:
Skin rash, Quincke's disease of the person, extremities, lips, language, glottis and/or throat, dysphonia, exfoliative dermatitis, multiformny exudative erythema (including Stephens-Johnson's syndrome), toxic epidermal necrolysis, pemphigus, skin itch, small tortoiseshell, photosensitization, seroses, vasculitis, miositis, arthralgia, arthritis, stomatitis.

Laboratory indicators:
Decrease in level of hemoglobin, hematocrit and quantity of thrombocytes is possible. Very in rare instances, especially at patients with an impaired renal function, diffusion diseases of connecting fabric, or when performing simultaneous therapy by Allopyrinolum, novokainamidy or immunosuppressors, development of anemia, thrombocytopenia, a neuropathy, increase in concentration of urea, a giperkreatininemiya, an eosinophilia is possible; in isolated cases – increase in activity of "hepatic" transaminases, an agranulocytosis or a pancytopenia.
It is regularly necessary to control sizes of the listed above laboratory parameters prior to the beginning of and during treatment, especially patients have risk groups.

 

Interaction with other medicines:

Allopurinol:umensheny numbers of leukocytes in blood, a leukopenia.

Analgetics, non-steroidal anti-inflammatory drugs (for example, acetylsalicylic acid, indometacin): easing of hypotensive effect of enalapril is possible.

Anti-hypertensive a sredstva:usileniye of hypotensive effect of enalapril, in particular at a concomitant use of diuretics.

Means for anesthesia and narcotic sredstva:usileny lowerings of arterial pressure.

Potassium, kaliysberegayushchy diuretics (especially Spironolactonum, amiloride, Triamterenum), and also other means, for example, heparin: increase in level of potassium in serum.

Boiled a sol:oslableniye of anti-hypertensive effect.

Litiy:povysheniye of lithium level in blood serum (regular control of content of lithium is necessary).

Peroral anti-diabetic means, инсулин:в exceptional cases strengthening of hypoglycemic effect of peroral antihyperglycemic means (for example, sulphonyl – urea / бигуанидин) and insulin is possible. In such cases reduction of a dose of antihyperglycemic means is required.

Novokainamid:umensheny numbers of leukocytes in blood, a leukopenia.

Cytostatics, immunosuppressors, system kortikosteroidy:umensheny numbers of leukocytes in blood, a leukopenia.

Alkogol:usileniye of effect of alcohol.

Contraindications:

Enalapril Geksal cannot be applied at

- hypersensitivity to drug and to other inhibitors of an angiotensin-converting enzyme;
- a Quincke's disease in the anamnesis, including, and against the background of reception of APF inhibitors;
stenosis (unilateral or bilateral) renal arteries;
- diseases of a liver or kidneys;
- pregnancy, feeding by a breast;
- age up to 18 years (efficiency and safety are not established).

Overdose:

Overdose:
Simptomy:vyrazhenny lowering of arterial pressure, up to development of a collapse, a myocardial infarction, an acute disorder of cerebral circulation or tromboembolic episodes, spasms, a stupor.
Lecheniye:bolny is transferred to horizontal position with a low headboard. In mild cases the gastric lavage and intake of saline solution, in more hard cases - the actions directed to stabilization of the ABP are shown: intravenous administration of normal saline solution, plasma substitutes, if necessary – administration of angiotensin II, a hemodialysis (speed of removal of enalaprilat averages 62 ml/min.).

Storage conditions:

At a temperature not above 25 °C in the place, unavailable to children!

Issue conditions:

According to the recipe

Packaging:

Tablets on 5, 10 and 20 mg.
On 10 tablets in the blister from aluminum / aluminum or PVC / aluminum foil.
On 1, 2, 3, 4 or 5 blisters together with the instruction for the consumer in a cardboard pack.