Enalaprilat

General characteristics. Structure:

Active ingredient: 1,25 mg of enalapril in 1 ml of solution.

The drug rendering a hypotensive, vazodilatiruyushchy, cardioprotective and natriuretic effect.

Pharmacological properties:

Pharmacodynamics. Inhibits APF, slows down biosynthesis of the angiotensin II causing vasoconstriction and inducing education and release of Aldosteronum and interferes with destruction of bradikinin and PGE2 (powerful internal vasodilating causes).

Pharmacokinetics. After introduction about 60% are inside soaked up (irrespective of existence of food in a GIT). Cmaxdostigayetsya during 1 h. Is exposed to biotransformation in a liver with formation of an active metabolite — enalaprilat which Cmax is defined by 4 h. Enalaprilat easily passes through gistogematichesky barriers, excepting GEB, gets through a placenta. T1/2 makes 11 h. It is excreted preferential by kidneys (to 40% it is removed in the form of enalaprilat). During 24 h about 90% of the entered quantity eliminirutsya. Decrease in the ABP is shown in 1 h after reception, reaches a maximum to 6 h and continues within 1 days. At some patients therapy for several weeks is necessary for achievement of optimum level of the ABP.

At heart failure long (within 6 months) treatment increases portability of exercise stresses, promotes reduction of the sizes of heart, reduces a lethality. Hypotensive effect of enalapril is caused by reduction of content in blood of angiotensin II and Aldosteronum, increase in concentration of bradikinin and PGE2. Decrease in OPSS is followed by increase in cordial emission without change of ChSS, pressure decline in pulmonary capillaries and unloading of a small circle of blood circulation, the investigation of what is increase in tolerance to exercise stresses and reduction of the sizes of dilatirovanny heart.

Indications to use:

Hypertension, symptomatic arterial hypertension, heart failure, diabetic nephropathy, secondary hyper aldosteronism, Raynaud's disease, scleroderma, complex therapy of a myocardial infarction, angina of exertion, chronic renal failure.

Route of administration and doses:

Inside. An initial dose — 5 mg of 1 times a day, and at patients with pathology of kidneys or accepting diuretic drugs — 2,5 mg of 1 times a day. At good tolerance and need the dose can be increased to 10–40 mg a day once or in two steps.

Features of use:

The initial dose is entered in a hospital at continuous monitoring of the ABP during not less than 3 h. During therapy it is necessary to control periodically concentration of transaminases and an alkaline phosphatase in a vascular bed (at increase in their contents treatment is cancelled).

With care appoint at disturbance of functions of kidneys (selection of a dose has to be carried out under control of concentration of enalapril to blood as the glomerular filtration rate is inversely proportional to its level in plasma).

Use at pregnancy and feeding by a breast. Category of action on a fruit on FDA — C (the I trimester). Category of action on a fruit on FDA — D (II and III trimesters).

Side effects:

Oppression TsNS, a depression, an ataxy, spasms, drowsiness or sleeplessness, peripheral neuropathy, vision disorders, taste, sense of smell, a ring in ears, conjunctivitis, dacryagogue, hypotonia, a myocardial infarction, an acute disorder of cerebral circulation (as a result of hypotonia), disturbance of a heart rhythm (atrial takhi-or bradycardia, a ciliary arrhythmia), orthostatic hypotension, a stenocardia attack, a thromboembolism of branches of a pulmonary artery, a bronchospasm, диспноэ, unproductive cough, an intersticial pneumonitis, bronchitis and other upper respiratory tract infections, a rhinorrhea, stomatitis, a xerostomia, a glossitis, anorexia, dyspepsia, a melena, a lock, pancreatitis, disturbance of functions of a liver (cholestatic hepatitis, a hepatocellular necrosis), dysfunction of kidneys, an oligouriya, infections of urinary tract, a gynecomastia, impotence, a neutropenia, thrombocytopenia, exfoliative dermatitis, a toxic epidermal necrolysis, a pempigus, shingles, alopecia, photodermatitis, allergic reactions (Stephens-Johnson's syndrome, small tortoiseshell, Quincke's edema, acute anaphylaxis, etc.).

Interaction with other medicines:

Effects of enalapril strengthen diuretics, antihypertensives, alcohol, weaken — estrogen, NPVS, sympathomimetics. Kaliysberegayushchy diuretics and kaliysoderzhashchy drugs increase risk of development of a hyperpotassemia.

Contraindications:

Hypersensitivity, pregnancy, feeding by a breast, children's age.

Overdose:

Symptoms: excessive hypotension, development of a myocardial infarction, an acute disorder of cerebral circulation and tromboembolic episodes against the background of sharp decrease in the ABP.

Treatment: in/in administration of isotonic solution of sodium of chloride and symptomatic therapy.

Storage conditions:

To store at a temperature of 15-25 °C, in dry, protected from light and the place, unavailable to children. Period of validity 3 years. Not to use after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Solution for injections of 1,25 mg/ml, on 1 ml in each ampoule. On 5 or on 10 ampoules, together with the application instruction in cardboard packaging.