Enzix Duo Forte, Tablet Set 2.5mg+20 mg 45 pcs

ENZIX DUO FORTE contains two separate drugs in one package: the angiotensin-converting enzyme (ACE) inhibitor ENALAPRIL and the diuretic INDAPAMID.

Enalapril

Antihypertensive drug, its mechanism of action is related to the reduction of angiotensin I angiotensin II, the reduction of which leads to a direct reduction of aldosterone release.

This decreases total peripheral vascular resistance, systolic and diastolic blood pressure (BP), post- and preload on myocardium.

It dilates arteries more than veins and there is no reflexive increase of heart rate.

Hypotensive effect is more expressed at high level of plasma renin than at normal or reduced level.

Decrease in BP within therapeutic limits does not affect cerebral blood flow, blood flow in the brain vessels is maintained at a sufficient level even at reduced blood pressure.

It increases coronary and renal blood flow. Long-term use reduces left ventricular myocardial hypertrophy and myocyte walls of resistant arteries, prevents the progression of heart failure and slows the development of left ventricular dilatation.

Improves blood supply to ischemic myocardium.

Reduces platelet aggregation. It has some diuretic effect. Enalapril is a “prodrug”: as a result of its hydrolysis enalaprilat is formed which inhibits angiotensin-converting enzyme (ACE).

Time of onset of hypotensive effect when taken orally is 1 hour, it reaches a maximum after 4-6 hours and lasts up to 24 hours.

Indapamide

Hypotensive agent, thiazide-like diuretic of moderate potency and long duration of action, benzamide derivative.

Reduces arterial smooth muscle tone, reduces total peripheral vascular resistance. It has moderate saluretic and diuretic effects associated with blockade of reabsorption

of sodium, chloride, hydrogen and, to a lesser extent, potassium ions in proximal tubules and cortical segment of the distal tubule of the nephron.

Vasodilator effects and reduction of total peripheral vascular resistance are based on the following mechanisms: reduction of reactivity of the vascular wall to noradrenaline and angiotensin II;

increased synthesis of prostaglandins, having vasodilator activity; inhibition of calcium current in vascular smooth muscle cells. Contributes to the reduction of left ventricular hypertrophy.

In therapeutic doses has no effect on lipid and carbohydrate metabolism (including in patients with concomitant diabetes).

Antihypertensive effect is developed at the end of the first/beginning of the second week if the drug is constantly used and maintained for 24 hours after single use.

Simultaneous use of Enalapril and Indapamide leads to enhancement of antihypertensive effect of Enalapril.

Pharmacokinetics

Enalapril

After oral administration about 60% is absorbed from the gastrointestinal tract. Simultaneous intake of food does not affect the absorption of enalapril. Blood plasma protein binding for enalaprilat is 50-60%.

Enalapril is rapidly and completely hydrolyzed in the liver to form an active metabolite – enalaprilat, which is a more active ACE inhibitor than enalapril. The bioavailability of the drug is 40%.

Maximum concentration of enalapril in blood plasma is reached after 1-2 hours, enalaprilat – after 3-4 hours.

Enalaprilat easily passes through the histohematic barriers, excluding the blood-brain barrier, a small amount passes through the placenta and into the breast milk.

The elimination half-life of enalaprilat is about 11 hours. Enalapril is mainly excreted through the kidneys 60% (20% as enalapril and 40% as enalaprilate), through the intestine 33% (6% as enalapril and 27% as enalaprilate).

Elimination by hemodialysis (rate 62 ml/min.) and peritoneal dialysis.

Indapamide

After oral administration, it is rapidly and completely absorbed from the gastrointestinal tract; bioavailability is high (93%). Food intake slightly slows down the absorption rate, but does not affect the completeness of absorption.

Maximal concentration in plasma is reached 1-2 hours after oral administration. The equilibrium concentration is reached after 7 days of regular use.

Half-life period is on the average 14-18 hours, the blood plasma protein binding is 79%. It also binds with elastin of vascular smooth muscle.

It has high volume of distribution, passes through histohematic barriers (including placental), penetrates into breast milk.

Metabolized in liver. The kidneys excrete 60 – 80% as metabolites (about 5% is excreted unchanged), through the intestines – 20%.

In patients with renal insufficiency pharmacokinetics is not changed. It does not cumulate.

Indications

Arterial hypertension.

Active ingredient

Composition

How to take, the dosage

Interaction

Special Instructions

Contraindications

Side effects

Overdose

Pregnancy use

The drug is contraindicated for use during pregnancy and lactation. If it is necessary to use Enzix during lactation, breastfeeding should be stopped.

In newborns and infants who have had intrauterine exposure to ACE inhibitors should be closely monitored for early detection of marked BP decrease, oliguria,

Hyperkalemia and neurologic disorders that may develop due to decreased renal and cerebral blood flow with ACE inhibitor-induced BP decrease.

In oliguria, BP and renal perfusion should be maintained by administration of appropriate fluids and vasoconstrictors.

Similarities