Enalapril (tablets 0,005, 0,01, 0,02)
Enalapril
International nonproprietary name
Enalapril.
Enalapril.
Pharmacotherapeutic group
Inhibitors of angiotensin-transforming enzyme.
Composition
1 tablet contains 5 mg, 10 mg or 20 mg of enalapril maleate.
Pharmacological action
Pharmacodynamics
Enalapril is an inhibitor of angiotensin-transforming enzyme.
It inhibits formation of angiotensin II and eliminates its vasoconstrictive action, increases cardiac output, reduces vascular resistance, pressure in lesser circulation. Promotes increase of potassium level in blood serum.
Decrease of arterial pressure is revealed in 1 hour after intake, reaches a maximum in 6 hours and proceeds within 1 day. The long-term (within 6 months) treatment at cardiac insufficiency increases tolerability of exercise stresses, promotes decrease of heart sizes, reduces a lethality.
Pharmakokinetics
About 60 % of the preparation is absorbed after intake of the administrated dose (irrespective of food intake). The maximal concentration in blood is reached within 1 hour. Enalapril is subject to biotransformation with formation of active metabolite – enalaprilate, which maximal concentration in blood is reached in 4 hours. Enalaprilate easily passes through histohematogenous barriers, except for hematoencephalic barrier, passes through a placenta. The period of half-elimination --Т1/2-- is 11 hours. 90 % from the untaken dose is eliminated within 24 hours. It is excreted mainly by kidneys (up to 40 % is eliminated in a form of enalaprilate).
Indications
Arterial hypertensia, including renovascular, chronic heart failure.
Dosage and method of administration
Preparation is administrated per orally. A regimen of dosage is individual. The initial dose is 2,5-5 mg 1 time a day. An average dose is 10-20 mg a day in two steps. The maximal recommended dose is 40 mg a day (in rare cases - up to 80 mg a day).
Special indications
During therapy it is necessary to periodically control the concentration of transaminases and alkaline phosphatase in bloodstream (the treatment should be withdrawn at their content increase).
Side effects
The majority of by-effects has temporary character and does not require the preparation withdrawn. The giddiness, nausea, headache, undue fatiguability, dry cough are possible. There can be palpitation, orthostatic hypotension, pains in the region of heart. From gastrointestinal tract - abdominal pain, diarrhea; failure of liver and kidneys function; hyperpotassemia, rising of level of hepatic transaminases, bilirubin; muscular cramps. Very seldom at the maximal dosage there can be sleep disorders, skin eruption, nervousness, depression, imbalance, paresthesia, tinnitus, an visionobscurity.
Contraindications
Angioneurotic edema in the anamnesis. Pregnancy, lactation, children's age. Hypersensitivity to enalapril and other АПФinhibitors.
Safety measures
It is necessary to administrate enalapril with extra care in patients with the lowered function of kidneys and liver; simultaneously with immunodepressants; at bilaterial stenosis of renal arteries.
Interactions with other preparations
At combined intake with NSAID the decrease of their effect is possible, at administration with potassium-sparing diuretics the risk of hyperpotassemia development, with lithium salts – slowing-down of lithium elimination. Enalapril strengthens an alcohol action.
Overdosage
Signs:hypotension, myocardial infarction development, acute disturbance of cerebral circulation and tromboembolic episodes on background of sharp decrease of arterial pressure.
Treatment:intravenous introduction of sodium chloride isotonic solution and symptomatic therapy.
The form of release
5 mg, 10 mg and 20 mg tablets. 10 tablets in a blister; 3 blisters in a pack.
The preparation "Enalapril" is made in cooperation with “ CTS Chemical Industries Ltd. ” company, Israel.
