Enapril

Enapril exhibits hypotensive activity.

Indications Enapril

It is used to reduce high blood pressure.

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Release form

The release of the therapeutic substance is realized in tablet form, in the amount of 20 pieces in a box.

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Pharmacodynamics

The complex antihypertensive medication contains 2 active elements that reduce blood pressure values – enalapril with hydrochlorothiazide.

Enalapril is a highly specific competitor-antagonist (inhibits the activity) of the ACE component. Its effect prevents the conversion of angiotensin-1 to angiotensin-2, which contributes to a significant vasoconstrictor effect with a subsequent increase in blood pressure.

At the same time, enalapril reduces the volume of aldosterone produced, due to which its blood values and the angiotensin-2 index decrease. This effect leads to a decrease in blood pressure, systemic resistance of peripheral vessels, pressure within the small blood flow and the right atrium, and in addition, it potentiates the volume of cardiac output.

The effect of enalapril leads to a gradual decrease in systolic and diastolic pressure, a decrease in left ventricular hypertrophy and stabilization of coronary blood flow.

Hydrochlorothiazide is a diuretic that acts by decreasing the reabsorption of ionized sodium and chloride within the proximal tubule. It also inhibits the reabsorption of potassium and bicarbonate.

The diuretic effect develops with alkalosis and acidosis, decreasing with prolonged use of the substance.

The combination of the two above-mentioned components in one drug increases its antihypertensive activity and at the same time reduces tissue swelling and the load on the myocardium.

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Pharmacokinetics

Enalapril is well absorbed inside the gastrointestinal tract (approximately 60%). It undergoes intrahepatic hydrolysis, during which enalaprilat is secreted, which is an active metabolic product. The bioavailability index of the drug is 40%. The plasma Cmax level of the active component is recorded after 1 hour, and its active metabolic product - after 3-4 hours.

Protein synthesis of enalaprilat inside plasma is less than 50%. One third of the administered portion is excreted through the intestine (27% as the enalaprilat component and another 6% as enalapril) and the kidneys (18% as enalaprilat and 61% as enalapril). The half-life of enalaprilat is 11 hours, and the clearance values inside the kidneys are 150±44 ml/minute.

Rapid absorption of hydrochlorothiazide results in the development of a diuretic effect after 1-2 hours. The component passes through the placenta and into breast milk. Elimination of the substance occurs quite quickly; approximately 95% with urine.

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Dosing and administration

The medicine should be taken orally, once a day. The tablets are taken at a time of day convenient for the patient, without reference to food intake. The duration of therapy with the medicine and the size of its daily portions are selected taking into account the severity of the developing pathology.

Usually, to reduce elevated blood pressure, you need to start with taking 1 tablet per day. Then, based on the clinical picture, the dosage can be increased to 2-4 tablets. In this case, the maximum daily dosage is selected for the patient individually, taking into account the general state of health, the severity of hypertension and the presence of concomitant diseases. In addition, it is necessary to monitor kidney function and serum potassium levels.

In case of kidney diseases, dosages are selected taking into account the values of CC. If this indicator exceeds 30 ml/minute, it is necessary to halve the initial portion (to half a tablet), and then gradually increase it, monitoring the work of the kidneys, until the optimal result is obtained.

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Use Enapril during pregnancy

The medication should not be used during pregnancy or breastfeeding.

Contraindications

Main contraindications:

• history of angioedema;
• severe intolerance associated with hydrochlorothiazide, enalapril or additional components of the drug;
• severe liver disease;
• severe form of gout;
• severe kidney diseases (including anuria, diabetic nephropathy, and acute renal failure);
• diabetes mellitus with severe symptoms;
• stenosis affecting the renal arteries or aorta;
• obstructive cardiomyopathy of hypertrophic nature.

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Side effects Enapril

The use of the drug may cause the development of side effects:

• dizziness or headaches;
• severe nausea (which may or may not result in vomiting);
• dry cough;
• dryness of the oral mucosa;
• problems with liver function (increased serum transaminase levels), accompanied by signs of secondary cholestasis;
• muscle weakness, hyponatremia or hypokalemia (with long-term use of the drug);
• increased levels of urea and creatinine, as well as the development of proteinuria (in case of renal pathologies).

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Overdose

Typically, intoxication with the drug is accompanied by a decrease in blood pressure values, manifested by nausea, a feeling of general weakness, pallor, dizziness, hyperhidrosis, disturbances in the level of EBV and headaches.

When the first reliable symptoms of poisoning develop, it is necessary to perform gastric lavage and give the patient adsorbents. It is also necessary to place the victim horizontally, lowering his head. Later, in order to correct the blood volume indicators, it is necessary to administer intravenous (via a dropper) 9% NaCl, and also angiotensin-2 (if necessary).

It is necessary to carry out all measures while simultaneously monitoring the vital values of the patient's general condition, as well as serum urea and potassium levels with creatinine.

In case of hypokalemia, KCl solution and potassium aspartate should be used (no more than 2 g per day). In case of hypochloremic alkalosis, NaCl should be used. In extremely severe conditions, hemodialysis is performed.

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Interactions with other drugs

The combined use of antihypertensive medications, ethanol, barbiturates, as well as narcotic substances and phenothiazine derivatives leads to an increase in antihypertensive activity, which is why it is necessary to constantly monitor blood pressure indicators and, in some cases, reduce the dose of Enapril.

The combined use of the drug with NSAIDs or NaCl leads to a weakening of its antihypertensive properties.

Administration together with GCS causes an imbalance of electrolyte parameters (may lead to hypokalemia). Combination with non-depolarizing muscle relaxants enhances their effect. Combination with pressor amines reduces pressor symptoms.

Taking the medicine together with foxglove potentiates the effect of the latter.

Due to the negative impact of hydrochlorothiazide on lithium excretion processes, it is necessary to exclude the possibility of their combined use, because lithium poisoning may develop as a result.

The combination of the drug and potassium-sparing agents (spironolactone and amiloride with triamterene) may increase plasma potassium levels.

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Storage conditions

Enapril must be stored at temperatures in the range of 15-25°C.

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Shelf life

Enapril can be used within a 36-month period from the date of manufacture of the medicinal substance.

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Application for children

The use of Enapril in pediatrics is prohibited (under 12 years of age).

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Analogues

The analogs of the drug are the medications Accuzide, Lopril, Hartil, Captopril and Enzix with Ampril and Ramipril, and in addition Bisoprolol, Co-Prenessa, Noliprel and Quinard with Lisinopril, etc.

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Reviews

Enapril receives quite a few reviews, because this medicine is sold in pharmacies quite rarely. Based on the characteristics of the active elements of the drug, it has good therapeutic effectiveness, having a positive effect on blood pressure indicators.