$5.00
Manufacturer: Ukraine
Treatment of arterial hypertension; treatment of clinically expressed heart failure; prevention of clinically expressed heart failure in patients with asymptomatic left ventricular dysfunction (ejection fraction ≤ 35 %).
Description
Enalapril-TEVA 5 mg. Composition
active substance: enalapril maleate;
1 tablet contains 5 mg of enalapril maleate;
Enalapril-TEVA 5 mg. excipients: lactose, corn starch, talc, sodium bicarbonate, hydroxypropyl cellulose, magnesium stearate.
Enalapril-TEVA 5 mg. Dosage form
Pills.
Basic physical and chemical properties: white, round, biconvex snap tab with a notch on one side.
Pharmacotherapeutic group
ACE inhibitors, monocomponent. ATX code С09А А02.
Pharmacodynamics
Enalapril maleate is a salt of maleic acid of enalapril, a derivative of two amino acids – L-alanine and L-proline. ACE (ACE) is a peptidyl dipeptidase that catalyzes the conversion of angiotensin I to the vasopressor substance angiotensin II. After absorption, enalapril is hydrolyzed to enalaprilat, which inhibits ACE. Suppression of ACE leads to a decrease in angiotensin II in plasma, as a result of which renin activity in plasma increases (due to the elimination of the negative feedback of renin release) and aldosterone secretion decreases.
ACE is identical to kininase II. Thus, enalapril can also block the breakdown of bradykinin, a potent vasodepressor peptide. However, the significance of this phenomenon for the therapeutic effect of enalapril remains unclear.
The mechanism through which enalapril lowers blood pressure is primarily associated with inhibition of the activity of the renin-angiotensin-aldosterone system. Enalapril may exhibit an antihypertensive effect even in patients with low-grade hypertension.
The use of enalapril in patients with arterial hypertension leads to a decrease in blood pressure in patients in horizontal and vertical positions without a significant increase in heart rate.
Symptomatic postural hypotension is rare. In some patients, achieving optimal blood pressure reduction may require several weeks of therapy. Abrupt discontinuation of enalapril was NOT associated with a rapid increase in blood pressure.
Pharmacokinetics
Absorption
Enalapril is rapidly absorbed from the gastrointestinal tract, the maximum plasma concentration is reached within 1 hour. Absorption volume is approximately 60%, absorption is not affected by food intake. Once absorbed, enalapril is rapidly and extensively hydrolyzed to enalaprilat, a potent ACE inhibitor. The maximum concentration of enalaprilat in the blood serum is reached 4 hours after taking a dose of enalapril. The half-life of enalaprilat after repeated administration of enalapril is 11 hours.
Distribution
Within the entire range of therapeutic concentrations, 60% of enalaprilat binds to blood plasma proteins.
Metabolism
After absorption, enalapril is rapidly hydrolyzed to form the active substance enalaprilat, a potent ACE inhibitor.
Output
Enalaprilat is excreted by the kidneys. The main components in the urine are enalaprilat, which accounts for approximately 40% of the dose, and unchanged enalapril (approximately 20%).
Impaired renal function
In patients with renal insufficiency, the exposure of enalapril and enalaprilat is increased. In patients with mild to moderate renal impairment (creatinine clearance 40-60 ml / min), the AUC of enalaprilat in a stable state was approximately 2 times higher than in patients with normal renal function after administration of 5 mg once a day. In severe renal failure (CC ≤ 30 ml / min), AUC increased approximately 8 times. At this level of renal failure, the effective half-life of enalaprilat increases, and the time to reach a stable state increases (see “Dosage and Administration”).
Enalaprilat can be removed from the general circulation using hemodialysis. The clearance of enalaprilat during dialysis is 62 ml / min.
Indications
Treatment of arterial hypertension.
Treatment of clinically significant heart failure.
Prevention of clinically significant heart failure in patients with asymptomatic left ventricular dysfunction (ejection fraction <35%).
Contraindications
Hypersensitivity to enalapril, to any excipient of the drug or other ACE inhibitors.
A history of angioedema associated with previous treatment with ACE inhibitors.
Pregnancy or planning pregnancy (see section “Use during pregnancy or lactation”).
Hereditary or idiopathic angioedema.
Simultaneous use of enalapril with drugs containing aliskiren in patients with diabetes mellitus or with impaired renal function (glomerular filtration rate <60 ml / min / 1.73 m2).
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