Enapril

Enapril demonstrates hypotensive activity.

Indications Enapril

It is used to reduce elevated blood pressure.

[1], [2]

Release form

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

[3], [4], [5], [6],

Pharmacodynamics

Comprehensive antihypertensive medication contains in its composition 2 active elements that reduce the values of blood pressure - enalapril with hydrochlorothiazide.

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

At the same time, enalapril reduces the volume of aldosterone produced, which causes its blood values and angiotensin-2 to decrease. This effect leads to a decrease in blood pressure, systemic resistance of peripheral vessels, pressure inside the small blood flow and the right atrium, and in addition it potentiates the amount 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 reducing the reabsorption of ionized sodium elements with chlorine inside the proximal tubule. At the same time, it inhibits the reabsorption of potassium with bicarbonates.

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

The combination of the two components in the composition of one drug increases its antihypertensive activity and at the same time reduces tissue swelling and stress on the myocardium.

[7], [8], [9], [10], [11]

Pharmacokinetics

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

Protein synthesis enalaprilat inside the plasma is less than 50%. The injected portion is excreted by one third through the intestines (by 27% in the form of the enalaprilat component and another 6% in the form of enalapril), as well as the kidneys (by 18% as enalaprilat, and 61% as enalapril). The half-life of enalaprilat is 11 hours, and the clearance value within the kidneys is 150 ± 44 ml / minute.

The rapid absorption of hydrochlorothiazide leads to the development of a diuretic effect after 1-2 hours. The component passes through the placenta and into breast milk. The elimination of the substance is quite fast; approximately 95% with urine.

[12], [13], [14],

Dosing and administration

Take the drug should be orally, 1-fold per day. Use pills at the right time for the patient, without reference to food intake. The duration of drug therapy and the size of its daily rations are selected, taking into account the severity of the developing pathology.

Usually, to reduce elevated blood pressure, you need to start by taking the 1st pill per day. Further, based on the clinical picture, the size of the dosage can be increased to 2-4 tablets. In this case, the maximum daily dosage is selected by the patient personally, taking into account the general state of his health, the severity of hypertension and the presence of concomitant diseases. In addition, you need to monitor the work of the kidneys and indicators of potassium inside the serum.

When kidney disease dosage is selected, taking into account the values of QC. If this figure exceeds 30 ml / minute, it is necessary to halve the initial portion (up to half a pill), and then gradually increase it, tracking the work of the kidneys until the optimal result is obtained.

[21], [22]

Use Enapril during pregnancy

To use the drug during pregnancy or breastfeeding is impossible.

Contraindications

Main contraindications:

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

[15], [16], [17], [18], [19]

Side effects Enapril

The use of the drug may cause the development of adverse events:

• dizziness or headaches;
• severe nausea (which leads to vomiting or not);
• dry cough;
• dryness of the oral mucosa;
• problems with the liver (increased values of transaminases within the serum), accompanied by signs of cholestasis of a secondary nature;
• muscle weakness, hyponatremia or hypokalemia (with prolonged use of the drug);
• increased levels of urea and creatinine, as well as the development of proteinuria (with renal pathologies).

[20]

Overdose

Usually, with drug intoxication, there is a decrease in blood pressure values, manifested by nausea, a feeling of general weakness, pallor, dizziness, hyperhidrosis, EBV level disorders and headaches.

When the first significant symptoms of poisoning develop, it is necessary to perform a gastric lavage and give the patient adsorbents. You also need to position the victim horizontally, his head down. Later, in order to correct the indicators of blood volume, it is necessary to administer intravenously (via an IV) the introduction of 9% NaCl, and besides this angiotensin-2 (if required).

It is necessary to carry out all activities, simultaneously tracking the vital values of the patient’s general state, and in addition, serum indicators of urea and potassium with creatinine.

In hypokalemia, you should use a solution of KCl and potassium asparaginate (in the daily portion not more than 2 g). In the case of hypochloremic alkalosis, NaCl should be used. In extremely difficult conditions, hemodialysis is performed.

[23], [24], [25], [26], [27], [28], [29],

Interactions with other drugs

The combined use of antihypertensive drugs, ethanol, barbiturates, as well as drugs and derivatives of phenothiazine leads to an increase in antihypertensive activity, due to which it is necessary to constantly monitor blood pressure and, in some cases, lower the portion of Enapril.

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

Introduction together with GCS causes an imbalance in electrolyte indices (may lead to hypokalemia). Combination with non-depolarizing muscle relaxants enhances their effect. The combination with amines of the pressure character reduces the pressure of symptomatology.

Taking the medicine with digitalis means potentiates the influence of the latter.

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

The combination of the drug and means of potassium-sparing character (spironolactone and amiloride with triamterene) can increase the values of potassium inside the plasma.

[30], [31], [32]

Storage conditions

Enapril is required to be kept at temperature values in the range of 15-25 ° С.

[33], [34], [35], [36], [37]

Shelf life

Enapril can be used within a 36-month period from the time the drug was manufactured.

[38], [39]

Application for children

Appointment of Enapril in pediatrics is prohibited (up to 12 years of age).

[40], [41]

Analogs

Analogues of the drug are medicines Akkuzid, Lopril, Hartil, Kaptopres and Enziks with Ampril and Ramipril, and besides this Bisoprolol, Co-Prenessa, Noliprel and Quinard with Lisinopril and so on.

[42], [43], [44], [45], [46], [47], [48], [49]

Reviews

Enapril receives quite a few reviews, because it sells this medicine in pharmacies rarely. If we proceed from the characteristics of the active elements of the drug, it has good therapeutic efficacy, having a positive impact on the blood pressure indicators.