Enap, tablets 20 mg 60 pcs

An antihypertensive drug, ACE inhibitor. The mechanism of action is associated with inhibition of ACE activity, which leads to reduction of angiotensin II formation.

Enalapril is a derivative of two amino acids: L-alanine and L-proline. After absorption, enalapril taken orally is hydrolyzed to enalarylate, which inhibits ACE. Its mechanism of action is related to reduction of angiotensin I and angiotensin II formation, decrease of which in plasma leads to increase of plasma renin activity (due to elimination of negative feedback on renin production) and reduction of aldosterone secretion. Since ACE is identical with the enzyme kininase II, enalapril can also block the degradation of bradykinin, a peptide with a potent vasopressor effect. The significance of this effect in the mechanism of action of enalapril has not been definitively established.

The antihypertensive effect of enalapril is primarily associated with inhibition of RAAS activity, which plays an important role in BP regulation. Despite this fact, enalapril has antihypertensive effect even in patients with arterial hypertension and low concentration of renin.

Enalapril decreases BP regardless of body position (both lying and standing) without a significant increase in HR. Symptomatic orthostatic hypotension is rare. In some patients, it may take several weeks of therapy to achieve optimal BP reduction. Abrupt withdrawal of enalapril has not been accompanied by a rise in BP.

Effective inhibition of ACE activity usually occurs 2-4 hours after a single oral administration of enalapril. Time of onset of antihypertensive action when taken orally is usually 1 h and reaches a maximum of 4-6 h. Duration of action depends on the dose. When used in recommended doses, the antihypertensive effect and hemodynamic effects are maintained for at least 24 h.

In patients with essential hypertension, a decrease in BP is accompanied by a decrease in PPS and an increase in cardiac output, while HR does not change or changes slightly. Renal blood flow increases, but glomerular filtration rate does not change. However, in patients with a baseline low glomerular filtration rate, it usually increased.

In patients with diabetic/nondiabetic nephropathy, albuminuria/proteinuria and renal IgG excretion decreased with enalapril.

In patients with chronic heart failure (CHF) on therapy with cardiac glycosides and diuretics
administration of enalapril is accompanied by a decrease in PPS and BP, an increase in cardiac output, with a decrease in HR (usually in patients with chronic heart failure HR is increased). Pulmonary capillary congestion pressure also decreases. With long-term use, 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 down the development of left ventricular dilatation. At left ventricular dysfunction enalapril decreases risk of development of major ischemic outcomes (including frequency of myocardial infarction and number of hospitalizations for unstable angina).

Indications

Active ingredient

Composition

Active ingredient:

Enalapril maleate 20 mg.

Auxiliary substances:

Lactose monohydrate,

hydroxypropylcellulose,

corn starch,

sodium bicarbonate,

talc,

magnesium stearate.

How to take, the dosage

The drug Enap is administered orally, regardless of the time of meals. The initial dose of Enap is 10-20 mg per day (once daily).

Thereafter, the dose is adjusted individually for each patient – usually 20 mg once a day.

The maximum daily dose should not exceed 40 mg.

In cases of heart failure, the dose is prescribed starting at 2.5 mg, then gradually increasing to 10 to 20 mg (in one to two doses).

Intravenous solution.

Enap is administered at a dose of 1.25 mg (1 mL) every 6 hours, including patients who have previously taken oral enalapril. Treatment should only be given as an inpatient.

The drug is given by IV infusion slowly (over 5 min) or by drop infusion diluted in 20-50 ml of 5% dextrose (glucose) solution or 0.9% sodium chloride solution.

If therapeutic effect is not satisfactory 1 h after administration, the drug in a dose of 1.25 mg (1 ml) may be repeated and after 6 h the treatment may be continued according to the usual schedule (1.25 mg every 6 h).

In patients taking diuretics, the initial dose of the drug is reduced to 0.625 mg (0.5 ml). If the therapeutic effect is unsatisfactory 1 h after administration, the same dose may be administered again, and after 6 h, treatment is continued with the full dose (1.25 mg every 6 h).

In mild to moderate chronic renal failure with CK > 30 mL/min (serum creatinine less than 265.2 µmol/L), the dose of Enap P is 1.25 mg (1 ml) every 6 h, which means no dose adjustment is required.

If CK < 30 mL/min (serum creatinine greater than 265.2 μmol/L), the starting dose is 0.625 mg (0.5 mL) followed by 1 h monitoring to detect excessive BP reduction.

If there is no effect after 1 h, the 0.625 mg dose is repeated and treatment is continued at a dose of 1.25 mg every 6 h. For patients on hemodialysis, the dose of Enap P is 0.625 mg (0.5 mL) every 6 h for 48 h.

Interaction

The patient should refrain from drinking alcoholic beverages because ethanol increases the reduction of blood pressure (BP) with enalapril.

The concomitant use of enalapril and diuretics or other hypotensive agents increases the effectiveness of these drugs.

The interaction with drugs used to treat heart failure (cardiac glycosides) is not clinically relevant.

Before surgery, the physician should be told that the patient is taking enalapril because of the risk of arterial hypotension during general anesthesia.

The concomitant use of enalapril and nonsteroidal anti-inflammatory drugs (NSAIDs) or acetylsalicylic acid (aspirin) as well as estrogen may decrease the effectiveness of enalapril and increase the risk of renal dysfunction.

The concomitant use of some diuretics (spironolactone, amiloride or triamterene) and/or additional administration of tablets containing potassium may cause increased serum potassium levels (hyperkalemia).

Drugs that cause bone marrow suppression increase the risk of neutropenia and/or agranulocytosis.

Immunosuppressants, allopurinol, cytostatics increase hematotoxicity.

Enalapril weakens the effect of agents containing theophylline.
Simultaneous use of lithium drugs may increase the side effects of lithium.

The concomitant use of Enap with cimetidine increases the half-life (T 1/2) of Enap. If a patient is already taking the above drugs or is advised to take any of them, they should tell their physician that they are taking Enap.

Special Instructions

With caution use Enap in motorists. When concomitant use with diuretics, beta-blockers the effect of Enap is increased, and with nonsteroidal anti-inflammatory drugs the effect is reduced.

Hypotension (rapid decrease in blood pressure) may be observed (even several hours after the first dose) in patients with severe heart failure or significant renal dysfunction as well as in patients with electrolyte-water balance disorders due to diuretic treatment, salt-free diet, diarrhea, vomiting or patients on hemodialysis. A marked decrease in blood pressure (BP) is usually manifested by nausea, increased heart rate (HR) and fainting.

In the case of arterial hypotension, the patient should be in a horizontal, low-headed position and a doctor should be called.

Contraindications

Side effects

Overdose

If a patient has taken too many pills in one sitting, a doctor should be called immediately.

Symptoms: excessive decrease in blood pressure (BP) up to the development of collapse, myocardial infarction, acute stroke or thromboembolic complications, convulsions, stupor.

Treatment: the patient is transferred to a horizontal position with a low headboard. In mild cases gastric lavage and oral administration of saline solution are indicated, in more severe cases – measures aimed at stabilization of arterial pressure (BP), IV administration of saline solution, plasma substitutes, if necessary – IV administration of angiotensin II, hemodialysis (elimination rate of enalaprilat – 62 ml/min).

Similarities