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Description
Enap pills - an antihypertensive drug, an ACE inhibitor. The mechanism of action is associated with inhibition of ACE activity, which leads to a decrease in the formation of angiotensin II.
Active ingredients
Enalapril
Release form
Pills
Pharmacological effect
Antihypertensive agent, the mechanism of action of which is associated with inhibition of the activity of angiotensin-converting enzyme, leading to a decrease in the formation of angiotensin II. Enalapril is a derivative of two amino acids: L-alanine and L-proline. After absorption, enalapril, ingested, is hydrolyzed to enalaprilat, which inhibits ACE. Its mechanism of action is associated with a decrease in the formation of angiotensin I from angiotensin II, a decrease in plasma levels of which leads to an increase in plasma renin activity (by eliminating a negative reaction to renin production) and a decrease in aldosterone secretion. Because ACE is identical to the enzyme kininase II, enalapril can also block the destruction of bradykinin, a peptide that has a powerful vasopressor effect. The significance of this effect in the mechanism of action of enalapril is not finally established. The antihypertensive effect of enalapril is associated primarily with the suppression of the activity of the renin-angiotensin-aldosterone system (RAAS), which plays an important role in the regulation of blood pressure (BP). Despite this, enalapril has an antihypertensive effect even in patients with arterial hypertension and low renin concentrations. Against the background of the use of enalapril, the level of blood pressure decreases regardless of the position of the body (both in the “lying” and “standing” positions) without a significant increase in heart rate (HR). Symptomatic orthostatic hypotension rarely develops. In some patients, achieving an optimal reduction in blood pressure may require several weeks of therapy. Abrupt cancellation of enalapril was not accompanied by a rise in blood pressure. Effective inhibition of ACE activity usually occurs 2-4 hours after a single dose of enalapril inside. The time of onset of the antihypertensive effect is usually when ingested - 1 hour, reaches a maximum - after 4-6 hours. The duration of action depends on the dose.When using the recommended doses, the antihypertensive effect and hemodynamic effects are maintained for at least 24 hours. In patients with essential hypertension, a decrease in blood pressure is accompanied by a decrease in peripheral vascular resistance and an increase in cardiac output, while the heart rate does not change or changes slightly. The renal blood flow increases, but the glomerular filtration rate does not change. However, in patients with initially low glomerular filtration rate, its level usually increased. In patients with diabetic / non-diabetic nephropathy, albuminuria / proteinuria and kidney excretion of IgG decreased with enalapril. In patients with chronic heart failure (CHF) during therapy with cardiac glycosides and diuretics, enalapril is accompanied by a decrease in total peripheral vascular resistance and blood pressure, an increase in cardiac output, and a decrease in heart rate (usually in patients with CHF, heart rate is increased). The pressure of the pulmonary capillaries is also reduced. With long-term use, enalapril increases exercise tolerance and reduces the severity of heart failure as assessed by NYHA criteria. Enalapril in patients with mild and moderate degrees of heart failure slows its progression, as well as slows the development of left ventricular dilatation. When 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).
Pharmacokinetics
Suction. After oral administration, enalapril is rapidly absorbed, the degree of absorption of enalapril is approximately 60%. The maximum concentration (Сmax) of enalapril in the serum is observed within 1 hour after ingestion. Food intake does not affect absorption. Enalapril is rapidly and actively hydrolyzed to form enalaprilat, a powerful ACE inhibitor. Сmax enalaprilat observed 3-4 hours after ingestion. The elimination half-life (T1 / 2) of enalapril with repeated use is 11 hours. In patients with normal renal function, plasma plasma levels of enalaprilat were reached on the 4th day of therapy. Distribution.The link with plasma proteins enalaprilat in the range of therapeutic doses is 60%. Biotransformation (metabolism.) In addition to turning into enalaprilat, enalapril does not undergo significant biotransformation. Inference. Enalaprilat is mainly excreted by the kidneys. Enalaprilat (about 40% of the dose) and unchanged enalapril (about 20%) are mainly detected in the urine.
Indications
Essential hypertension, chronic heart failure (as part of combination therapy), prevention of development of clinically severe heart failure in patients with asymptomatic left ventricular dysfunction (as part of combination therapy), prevention 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.
Dosage and administration
The drug is taken orally, regardless of the meal, preferably at the same time of day. Tablets should be taken with a small amount of liquid. Arterial hypertension. The initial dose is 5 to 20 mg 1 time per day, depending on the severity of arterial hypertension. In mild arterial hypertension, the recommended initial dose is 5-10 mg / day. In patients with marked activation of the RAAS (for example, with renovascular hypertension, electrolyte loss and / or dehydration, decompensation of heart failure or severe arterial hypertension), an excessive decrease in blood pressure in start of treatment. In such situations, it is recommended to begin therapy with a low initial dose of 5 mg / day or less, under the supervision of a physician. Prior therapy with high doses of diuretics can lead to dehydration and an increased risk of arterial hypotension at the beginning of therapy with Enap, the recommended initial dose is 5 mg per day Treatment with diuretics should be stopped for 2-3 days before the start of the drug Enap. Care should be taken when using the drug Enap, monitor kidney function and the content of potassium in the blood serum. Usually the maintenance dose is 20 mg 1 time / day. The dose is chosen individually, if necessary, can be increased to a maximum daily dose of 40 mg. Chronic heart failure and dysfunction of the left ventricle. The initial dose is 2.5 mg 1 time / day, and the treatment should be started under the close supervision of a physician. The preparation Enap for the treatment of heart failure can be applied simultaneously on diuretics and / or beta-blockers,if necessary, with cardiac glycosides. In the absence of symptomatic hypotension at the beginning of therapy or after its correction, the dose should be increased gradually (by 2.5-5 mg every 3-4 days) to the usual maintenance dose of 20 mg / day, which is prescribed either once or in 2 doses, in depending on the tolerability of the drug. Dose selection is carried out within 2-4 weeks (for details, see the instructions).