Enap (enalapril maleate) ampoules 1.25 mg/ml. 1ml. №5

Description

Enap ampoules  Storage
active substance: enalaprilat;

1 ml solution for injection contains 1.25 mg enalaprilat;

Enap ampoules Excipients: benzyl alcohol, sodium chloride, sodium hydroxide, water for injections.

Enap ampoules Dosage form
Solution for injection.

Main physical and chemical properties: clear colorless solution without visible mechanical impurities.

Pharmacotherapeutic group
Agents acting on the renin-angiotensin system. Angiotensin-converting enzyme inhibitors.

ATX code C09A A02.

Pharmacological properties

Pharmacodynamics.

Mechanism of action

Enalaprilat inhibits the angiotensin-converting enzyme that catalyzes the conversion of angiotensin I to angiotensin II. Inhibition of angiotensin-converting enzyme leads to a decrease in the concentration of angiotensin II, an increase in plasma renin activity and a decrease in aldosterone secretion.

Pharmacodynamic effect

The antihypertensive effect and hemodynamic effects of enalaprilat in patients with high blood pressure are the result of dilation of resistant blood vessels and a decrease in total peripheral resistance, which gradually lowers blood pressure. Systolic and diastolic pressure and pressure in the main pulmonary artery decrease, coronary circulation increases, heart index and stroke volume increase (at constant heart rate).

After intravenous injection, the effect of the drug occurs in 5-15 minutes, the maximum effect – in 1-4 hours, and its effect lasts for about 6 hours.

Enalaprilat does not affect the metabolism of glucose, lipoproteins, uric acid and cholesterol. The drug can be prescribed to patients with diabetes, chronic obstructive pulmonary disease, angina, congestive heart failure.

Pharmacokinetics.

Absorption

After oral administration, enalaprilat is poorly absorbed and almost inactive, so it should only be administered intravenously.

Distribution

Following intravenous injection, the drug is rapidly distributed in most tissues of the body with the highest concentrations in the lungs, kidneys and blood vessels. The half-life is 4 hours. 50 to 60% of enalaprilat is bound to serum proteins.

Metabolism

Enalaprilat is not metabolized; 100% of enalaprilat is excreted in the urine.

Breeding

Enalaprilat is excreted mainly by the kidneys, via glomerular filtration and tubular secretion. Excretion occurs in several stages due to strong binding to the serum angiotensin-converting enzyme. The half-life at the initial stage is approximately 11 hours, and at the last – 35 hours.

Renal dysfunction

Exposure to enalapril and enalaprilat is increased in patients with renal insufficiency. Output slows down; therefore, dose adjustment should be performed according to renal function.

Enalaprilat can be removed from the general circulation by hemodialysis. The clearance of enalaprilat during dialysis is 1.03 ml / s (62 ml / min).

Indication
Hypertension, hypertensive crisis.
Enalaprilat is indicated for the treatment of hypertension in cases where oral treatment is not possible.

Contraindication

Hypersensitivity to enalapril, enalaprilat, other angiotensin-converting enzyme (ACE) inhibitors or to any of the ingredients.
History of angioneurotic edema associated with prior treatment with angiotensin-converting enzyme inhibitors.
Hereditary or idiopathic angioneurotic edema.
Pregnant women or women planning to become pregnant (see section “Use during pregnancy or breast-feeding”).
Enap® should not be used with aliskiren-containing products in patients with diabetes mellitus or renal impairment (GFR <60 ml / min / 1.73 m2) (see section “Interaction with other medicinal products and other forms of interaction”). .