Enalapril, 20 mg tablets, 20 pcs.
€1.00
Out of stock
(E-mail when Stock is available)
Pharmacological action – hypotensive, vasodilatory, cardioprotective, natriuretic.
ACE inhibitor, a prodrug from which the active metabolite enalaprilat is formed in the body. It is believed that the mechanism of antihypertensive action is associated with competitive inhibition of ACE activity, which reduces the rate of conversion of angiotensin I into angiotensin II (which has a marked vasoconstrictor effect and stimulates the secretion of aldosterone in the adrenal cortex).
The decrease in angiotensin II concentration results in a secondary increase in plasma renin activity by eliminating the negative feedback of renin release and directly reducing aldosterone secretion. In addition, enalaprilat appears to influence the kinin-callicrein system by inhibiting the breakdown of bradykinin.
Due to its vasodilator effect, it reduces total peripheral vascular resistance (postload), congestion pressure in the pulmonary capillaries (preload) and pulmonary vascular resistance; it increases cardiac minute volume and exercise tolerance.
In patients with chronic heart failure, long-term use of enalapril increases exercise tolerance and reduces the severity of heart failure (evaluated according to NYHA criteria). Enalapril in patients with mild to moderate heart failure slows its progression and also slows development of left ventricular dilatation.
In left ventricular dysfunction, enalapril reduces the risk of major ischemic outcomes (including the incidence of myocardial infarction and the number of hospitalizations for unstable angina).
When taken orally, approximately 60% is absorbed from the GI tract. Simultaneous intake of food has no effect on absorption. It is metabolized in the liver by hydrolysis to form enalaprilat, due to the pharmacological activity of which the hypotensive effect is realized. Binding of enalaprilat with plasma proteins is 50-60%.
The elimination half-life of enalaprilat is 11 h and is prolonged in renal insufficiency. After oral administration, 60% of the dose is excreted by the kidneys (20% as enalapril, 40% as enalaprilat), 33% is excreted through the intestine (6% as enalapril, 27% as enalaprilat). After intravenous administration of enalaprilat 100% is excreted unchanged by the kidneys.
Indications
Active ingredient
Composition
How to take, the dosage
In case of oral administration, the initial dose is 2.5-5 mg once a day. The average dose is 10-20 mg per day in two doses.
In intravenous administration, 1.25 mg every 6 hours. For excessive hypotension in patients with sodium deficiency and dehydration due to previous therapy with diuretics, patients receiving diuretics, as well as in case of renal insufficiency, the initial dose of 625 mg is administered. If clinical response is inadequate, this dose may be repeated after 1 hour and treatment may be continued at a dose of 1.25 mg every 6 hours.
The maximum daily dose when given orally is 80 mg.
Interaction
Concomitant use with immunosuppressants, cytostatics increases the risk of leukopenia.
. In concomitant use of potassium-saving diuretics (including spironolactone, triamterene, amiloride), potassium preparations, salt substitutes, and dietary supplements containing potassium, hyperkalemia may develop (especially in patients with impaired renal function) since ACE inhibitors decrease aldosterone content, which leads to potassium retention in the body against restricted potassium excretion or its additional intake.
The simultaneous use of opioid analgesics and drugs for anesthesia increases the antihypertensive effect of enalapril.
The simultaneous use of “loop” or thiazide diuretics increases the antihypertensive effect. There is a risk of hypokalemia. Increased risk of impaired renal function.
In concomitant use with azathioprine anemia may occur due to inhibition of erythropoietin activity caused by ACE inhibitors and azathioprine.
Acetylsalicylic acid in high doses may decrease the antihypertensive effect of enalapril.
It has not been definitively established whether acetylsalicylic acid reduces the therapeutic efficacy of ACE inhibitors in patients with CHF and heart failure. The nature of this interaction depends on the course of the disease.
Acetylsalicylic acid, by inhibiting cyclooxygenase and prostaglandin synthesis, may cause vasoconstriction, which leads to decreased cardiac output and deterioration in patients with heart failure receiving ACE inhibitors.
The simultaneous use of beta-adrenoblockers, methyldopa, nitrates, calcium channel blockers, hydralazine, prazosin may increase the antihypertensive effect.
Concomitant use with NSAIDs (including indomethacin) decreases antihypertensive effect of enalapril, probably due to inhibition of prostaglandin synthesis under NSAID influence (which is believed to play a role in development of hypotensive effect of ACE inhibitors). There is an increased risk of renal dysfunction; hyperkalemia is rarely observed.
The simultaneous use of insulin and hypoglycemic agents of sulfonylurea derivatives may lead to hypoglycemia.
The simultaneous use of ACE inhibitors and interleukin-3 may lead to a risk of hypotension.
In concomitant use with clozapine, there have been reports of syncope.
In concomitant use with clomipramine there have been reports of increased effects of clomipramine and development of toxic effects.
In concomitant use with co-trimoxazole cases of hyperkalemia have been described.
Concomitant use with lithium carbonate leads to increased serum lithium concentration accompanied by symptoms of lithium intoxication.
Concomitant use with orlistat decreases the antihypertensive effect of enalapril, which can lead to a significant increase in BP, development of hypertensive crisis.
It is believed that concomitant use with procainamide may increase the risk of leukopenia.
Concomitant use with enalapril decreases the effect of drugs containing theophylline.
There have been reports of acute renal failure in patients after kidney transplantation when concomitant use with cyclosporine.
Concomitant use with cimetidine prolongs the elimination half-life of enalapril and increases its plasma concentrations.
It is believed that the effectiveness of antihypertensive agents may be reduced when used concomitantly with erythropoietins.
Concomitant use with ethanol increases the risk of arterial hypotension.
Special Instructions
In long-term treatment with enalapril, peripheral blood counts should be monitored periodically. Sudden discontinuation of enalapril does not cause a sudden increase in BP.
In surgical interventions during enalapril treatment, arterial hypotension may occur, which should be corrected by administration of sufficient fluids.
Enalapril should be stopped before parathyroid function tests.
Caution should be exercised when driving motor vehicles or performing other work requiring increased attention, as dizziness is possible, especially after taking the initial dose of enalapril.
Contraindications
An history of angioedema, bilateral renal artery stenosis or renal artery stenosis of the single kidney, hyperkalemia, porphyria, concomitant use with aliskiren in patients with diabetes or impaired renal function (creatinine clearance < 60 ml/min), pregnancy, lactation (breastfeeding), childhood and adolescence under 18 years of age, hypersensitivity to enalapril and other ACE inhibitors.
Particular caution is used in patients with autoimmune diseases, diabetes mellitus, impaired liver function, severe aortic stenosis, subaortic muscle stenosis of unclear genesis, hypertrophic cardiomyopathy, loss of fluid and salts.
In prior saluretic treatment, particularly in patients with chronic heart failure, the risk of orthostatic hypotension increases, so fluid and salt loss should be compensated before starting enalapril treatment.
Side effects
CNS and peripheral nervous system disorders: dizziness, headache, fatigue, increased fatigue; very rarely with high doses – sleep disorders, nervousness, depression, balance disorders, paresthesias, tinnitus.
Cardiovascular system disorders: orthostatic hypotension, fainting, palpitations, heart pain; very rare with high doses – hot flashes.
The digestive system: nausea; rarely – dry mouth, abdominal pain, vomiting, diarrhea, constipation, liver disorders, increased liver transaminases activity, increased blood bilirubin concentration, hepatitis, pancreatitis; very rare in high doses – glossitis.
The hematopoietic system: rarely – neutropenia; in patients with autoimmune diseases – agranulocytosis.
Urinary system disorders: rare – renal dysfunction, proteinuria.
Respiratory system disorders: dry cough.
Reproductive system disorders: very rare when used in high doses – impotence.
Dermatological reactions: very rare in high doses – hair loss.
Allergic reactions: rarely – skin rash, Quincke’s edema.
Others: rarely – hyperkalemia, muscle cramps.
Overdose
Symptoms: excessive hypotension, development of myocardial infarction, acute impairment of cerebral circulation and thromboembolic complications against the background of rapid BP decrease.
Treatment: intravenous sodium chloride isotonic solution and symptomatic therapy.
Similarities
Weight | 0.016 kg |
---|---|
Shelf life | 3 years |
Conditions of storage | In a dry, light-protected place at a temperature not exceeding 25 °C |
Manufacturer | Ozon, Russia |
Medication form | pills |
Brand | Ozon |
Other forms…
Related products
Buy Enalapril, 20 mg tablets, 20 pcs. with delivery to USA, UK, Europe and over 120 other countries.