Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..
ACE inhibitor. It is a prodrug, from which an 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 leads to a decrease in the rate of conversion of angiotensin I to angiotensin II (which has a pronounced vasoconstrictive effect and stimulates the secretion of aldosterone in the adrenal cortex).
As a result of a decrease in angiotensin II concentration, a secondary increase in plasma renin activity occurs due to elimination of negative feedback during the release of renin and a direct decrease in aldosterone secretion. In addition, enalaprilat, apparently, has an effect on the kinin-kallikrein system, preventing the breakdown of bradykinin.
Due to vasodilator effect, reduces OPSS (afterload), wedging pressure in the pulmonary capillaries (preload) and resistance in the pulmonary vessels; increases the minute volume of the heart and tolerance to the load.
In patients with chronic heart failure with prolonged use, enalapril increases exercise tolerance and reduces the severity of heart failure (assessed by NYHA criteria).Enalapril in patients with mild to moderate heart failure slows its progression, and also slows the development of dilatation of the left ventricle. With left ventricular dysfunction, enalapril reduces the risk of developing major ischemic outcomes (including the incidence of myocardial infarction and the number of hospitalizations for unstable angina).
When ingested, about 60% is absorbed from the digestive tract. Simultaneous food intake does not affect suction. Metabolised in the liver by hydrolysis with the formation of enalaprilata, due to the pharmacological activity of which the hypotensive effect is realized. The binding of enalaprilat to plasma proteins is 50-60%.
T 1/2 enalaprilata is 11 hours and increases with renal failure. After ingestion, 60% of the dose is excreted by the kidneys (20% in the form of enalapril, 40% in the form of enalaprilat), 33% is excreted through the intestine (6% in the form of enalapril, 27% in the form of enalaprilate). After intravenous administration of enalaprilate, 100% is excreted by the kidneys unchanged.
Arterial hypertension (including renovascular), chronic heart failure (as part of combination therapy).
Chronic heart failure (as part of combination therapy).
Prevention of the development of clinically significant heart failure in patients with asymptomatic left ventricular dysfunction (as part of combination therapy).
Prophylaxis of coronary ischemia in patients with left ventricular dysfunction in order to reduce the incidence of myocardial infarction and reduce the frequency of hospitalizations for unstable angina.
When administered orally, the initial dose is 2.5-5 mg 1 time / day. The average dose is 10-20 mg / day in 2 divided doses.
With intravenous administration - 1.25 mg every 6 hours. To detect excessive hypotension, patients with a sodium deficiency and dehydration caused by previous therapy with diuretics, patients receiving diuretics, as well as with renal failure, receive an initial dose of 625 mg. With an inadequate clinical response, this dose can be repeated after 1 hour and continue treatment at a dose of 1.25 mg every 6 hours.
The maximum daily intake for oral administration is 80 mg.
From the central nervous system and peripheral nervous system: dizziness, headache, fatigue, increased fatigue; very rarely when used in high doses - sleep disorders, nervousness, depression, imbalance, paresthesia, tinnitus.
From the cardiovascular system: orthostatic hypotension, syncope, palpitation, pain in the heart; very rarely when used in high doses - hot flashes.
On the part of the digestive system: nausea; rarely dry mouth, abdominal pain, vomiting, diarrhea, constipation, impaired liver function, increased activity of hepatic transaminases, increased bilirubin concentration in the blood, hepatitis, pancreatitis; very rarely when used in high doses - glossitis.
From the hemopoietic system: rarely - neutropenia; in patients with autoimmune diseases - agranulocytosis.
From the urinary system: rarely - violations of kidney function, proteinuria.
From the respiratory system: dry cough.
From the side of the reproductive system: very rarely when used in high doses - impotence.
Dermatological reactions: very rarely when used in high doses - hair loss.
Allergic reactions: rarely - skin rash, angioedema.
Other: rarely - hyperkalemia, muscle cramps.
An angioneurotic edema in the anamnesis, bilateral renal artery stenosis or renal artery stenosis of the only kidney, hyperkalemia, porphyria, concomitant use with aliskiren in patients with diabetes mellitus or renal dysfunction (QC <60 ml / min), pregnancy, lactation (breastfeeding) , children and adolescents under 18 years of age, increased sensitivity to enalapril and other ACE inhibitors.
PREGNANCY AND LACTATION
Contraindicated in pregnancy. If pregnancy occurs, enalapril should be discontinued immediately.
Enalapril is excreted in breast milk. If it is necessary to use it during lactation, the question of stopping breastfeeding should be resolved.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With special care apply in patients with impaired liver function.
APPLICATION FOR CHILDREN
The safety and efficacy of enalapril in children have not been established.
With special care apply in patients with autoimmune diseases, diabetes mellitus, impaired liver function, severe aortic stenosis, subaortic muscular stenosis of unknown origin, hypertrophic cardiomyopathy, loss of fluid and salts. In the case of prior treatment with saluretic, in particular in patients with chronic heart failure, the risk of orthostatic hypotension increases, so before starting treatment with enalapril it is necessary to compensate for the loss of fluid and salts.
With long-term treatment with enalapril, you need to periodically monitor the picture of peripheral blood. The sudden discontinuation of enalapril does not cause a sharp increase in blood pressure.
During surgical interventions during the treatment with enalapril, it is possible to develop arterial hypotension, which should be corrected by the introduction of a sufficient amount of fluid.
Before the study of parathyroid function, enalapril should be discontinued.
Impact on the ability to drive vehicles and manage mechanisms
Care must be taken when driving vehicles or doing other work that requires increased attention, because possibly dizziness, especially after taking the initial dose of enalapril.
With simultaneous use with immunosuppressants, cytostatics increases the risk of developing leukopenia.
With the simultaneous use of potassium-sparing diuretics (including spironolactone, triamterene, amiloride), potassium preparations, salt substitutes and dietary supplements containing potassium, it is possible to develop hyperkalemia (especially in patients with impaired renal function) because ACE inhibitors reduce the content of aldosterone, which leads to a delay in potassium in the body against the background of the limitation of the excretion of potassium or its additional intake into the body.
With the simultaneous use of opioid analgesics and anesthesia, the antihypertensive effect of enalapril is enhanced.
With the simultaneous use of "loop" diuretics, thiazide diuretics, the antihypertensive effect is enhanced. There is a risk of hypokalemia. Increased risk of impaired renal function.
With simultaneous use with azathioprine, the development of anemia is possible, which is due to the inhibition of erythropoietin activity under the influence of ACE inhibitors and azathioprine.
A case of development of anaphylactic reaction and myocardial infarction with allopurinol in a patient receiving enalapril is described.
Acetylsalicylic acid in high doses can reduce the antihypertensive effect of enalapril.
Finally, it is not established whether acetylsalicylic acid reduces the therapeutic efficacy of ACE inhibitors in patients with ischemic heart disease and heart failure.The nature of this interaction depends on the course of the disease.
Acetylsalicylic acid, by inhibiting COX and the synthesis of prostaglandins, can cause vasoconstriction, which leads to a reduction in cardiac output and worsening of patients with heart failure receiving ACE inhibitors.
With the simultaneous use of beta-blockers, methyldopa, nitrates, calcium channel blockers, hydralazine, prazosin, an increase in antihypertensive effect is possible.
With simultaneous use with NSAIDs (including indomethacin), the antihypertensive effect of enalapril decreases, apparently due to inhibition of the synthesis of prostaglandins under the influence of NSAIDs (which are believed to play a role in the development of the antihypertensive effect of ACE inhibitors). Increased risk of renal dysfunction; rarely observed hyperkalemia.
With the simultaneous use of insulin, hypoglycemic agents of sulfonylureas, hypoglycemia may develop.
With the simultaneous use of ACE inhibitors and interleukin-3, there is a risk of developing arterial hypotension.
With simultaneous application with clozapine there are reports of the development of syncope.
With simultaneous use with clomipramine, the effect of clomipramine and the development of toxic effects are reported.
With simultaneous application with co-trimoxazole, cases of hyperkalemia development are described.
When lithium is applied simultaneously with carbonate, the concentration of lithium in the serum increases, which is accompanied by symptoms of lithium intoxication.
With simultaneous use with orlistat reduces the antihypertensive effect of enalapril, which can lead to a significant increase in blood pressure, the development of hypertensive crisis.
It is believed that with simultaneous use with procainamide, there may be an increased risk of developing leukopenia.
With simultaneous use with enalapril, the effect of drugs containing theophylline is reduced.
There are reports of the development of acute renal failure in patients after kidney transplantation with simultaneous application with cyclosporine.
With simultaneous application with cimetidine, T 1/2 enalapril increases and its concentration in the blood plasma increases.
It is believed that it is possible to reduce the effectiveness of antihypertensive agents when used simultaneously with erythropoietins.
With simultaneous use with ethanol, the risk of developing arterial hypotension increases.