Enalapril: indications for use, instructions, side effects and contraindications

Hypertension is one of the leading causes of death from cardiac diseases in almost all countries.

Regular intake of the antihypertensive drug Enalapril in a therapeutic dosage several times reduces the risk of complications from the cardiovascular system and sudden death outcome.

An important role is played not only by the effectiveness of the drug itself, but also by its general effect on the psychoemotional state of the patient.

Angiotensin-converting enzyme (ACE) inhibitors, which include Enalapril, rarely cause side complications and practically do not have a significant effect on the patient's usual image life.

How does the drug fight high blood pressure?

The name of the protein compounds angiotensins comes from the Greek words angeon - vessel and tensio - tension. They are formed from β-globulin angiotensinogen, which is in the plasma part of the blood. Under the influence of renin, which is produced in kidney cells, angiotensinogen is converted into angiotensin I. However, it also has no effect on vascular tone.

But under the influence of another enzyme formed in the lung tissue, angiotensin-converting or angiotensin-converting (ACE - kinase II), angiotensin I passes into angiotensin II. It is one of the strongest endogenous (internal) factors that affect the tone of the vascular wall, and as a result, the level of systolic and diastolic blood pressure (BP).

ACE inhibitors also stimulate the synthesis of vasodilating bradykinin, inhibit the hypertensive activity of corticotropic and luteinizing hormones. Thanks to this, Enalapril has the following effect on the human body:

• Inhibition of the synthesis and secretion of aldosterone, a hormone of the adrenal cortex that causes fluid and ion retention sodium in the body, and potassium ions necessary for the normal functioning of the myocardium are intensively excreted from urine.
• Weakening of reabsorption in the renal tubules and a decrease in the production of antidiuretic hormone (arginine-vasopressin), which manifests itself in an additional mild diuretic effect.
• Long-term maintenance of the hypotensive effect by reducing the concentration of another vasoconstrictor factor, endothelin I.
• Influence on the vascular endothelium, which is especially important in old age, since during aging, deposits of collagen, elastin and calcium are formed on the walls of the arteries. Endothelial dysfunction is the first stage in the development of atherosclerosis, which begins even before the onset of atherosclerotic plaque formation. Enalapril increases the synthesis of nitric oxide and improves blood rheology, which, in turn, restores blood flow in the arteries.
• Reducing the energy requirements of the myocardium, due to which the rhythm of muscle contraction is normalized tissues, this feature of this drug explains its widespread use in such pathologies, how ischemic disease (Ischemic heart disease), chronic heart failure, angina pectoris.
• Improving the "work" of the left ventricle, which primarily suffers in myocardial infarction, compliance the doctor's recommendations regarding the dosage and duration of treatment reduces the pathological increase in the mass of the left ventricle of the heart.

In addition to acting on the cardiovascular system, Enalapril also has a protective effect on the kidneys. The fact is that in the pathogenesis of renal failure, the activation of the renin-angiotensin-aldosterone system is of great importance.

The enzymes, proteins and other substances produced by it lead to collagen deposits and disruption of the functioning of the tubular system of the excretory organs. Knowing this mechanism, doctors prescribe Enalapril not only for nephropathies, but also for the treatment of renovascular hypertension, which is caused by a narrowing of the renal artery.

According to the pharmacological classification of ACE inhibitors, Enalapril belongs to class IIa prodrugs. It does not act on the body "directly", but undergoes hydrolysis processes and is transformed into an active metabolite, enalaprilat, which directly affects the angiotensin-converting enzyme. And if Enalapril is prescribed in the form of tablets for the long-term treatment of hypertension, then a 0.125% solution of enalaprilat (in pharmacies you can buy Enap for injection) is used for relief hypertensive crises.

The drug is rapidly, but not completely (approximately 60%), absorbed in the gastrointestinal tract, regardless of food intake. The bioavailability of Enalapril is about 40%. The antihypertensive effect of the drug begins with the achievement of its maximum concentration in the blood, through 1-4 hours after ingestion, the half-life and, accordingly, the action - up to 11 hours. More than half of the drug (up to 60%) is excreted by the kidneys in the form of enalaprilat and unchanged enalapril, part through the intestines.

Enalapril: indications for use, form of release, restrictions on use

Enalapril is produced by various domestic and foreign pharmaceutical corporations, sometimes the name the company is reflected in the trade name of the drug, for example, Enalapril Ajio manufactured by Ajio Pharmaceuticals, India.

The medicine is sold in packs of 20, 30 or 50 white tablets with 5, 10 or 20 mg of active ingredient. They can be biconvex or even with a horizontal line dividing the pill into two equal parts.

The chemical composition of Enalapril contains several amino acid residues. According to its physical properties, the active substance is a white crystal-like powder, which practically does not dissolve in any solution, with the exception of alcohol.

Therefore, for the formation of tablets, auxiliary substances are added to it, such as lactose, magnesium compounds, gelatin, crospovidone.

Indications for the use of Enalapril are the following diseases:

• hypertension of various etiology and severity of the course;
• congestive heart failure;
• heart attack (only in combination with a number of other medicines);
• diabetic nephropathy (kidney pathology in diabetes mellitus);
• secondary hyperaldosteronism (an increase in the level of the adrenal cortex hormone aldosterone against the background of pathological activation of the renin - angiotensin - aldosterone system);
• Raynaud's disease (circulatory disorders in the small arteries and arterioles of the upper and lower extremities);
• scleroderma (a systemic disease accompanied by an excessive accumulation of collagen in almost all tissues);
• prevention of complications, angina attacks, heart attacks in patients with an increase in the mass of the left ventricle of the heart.

In the foreign medical literature there is information that in patients with indications for the use of Enalapril, the frequency of symptoms of acute cardiac hypoxia decreased, attacks of pain in the chest area, visits to a cardiologist for a worsening of the general condition, in comparison with other patients who do not have this drug prescribed.

But you will have to look for another way to stabilize blood pressure in the presence of contraindications for the appointment of Enalapril.

These include:

• hypersensitivity, and not only to Enalapril, but also to other drugs from the class of angiotensin-converting enzyme inhibitors;
• if a person previously had Quincke's edema, including of unexplained etiology;
• pathological reaction to lactose;
• early and adolescence (up to 18 years).

For the drug Enalapril, indications for use require constant medical supervision in cases where there is:

• renal failure;
• narrowing of the lumen of the renal arteries or artery of only one "working" kidney;
• liver pathology;
• violation of blood flow in the blood vessels that feed the heart;
• rehabilitation period after kidney transplant surgery;
• systemic connective tissue pathologies;
• disorders of blood flow in the vessels of the brain.

Correction of the dose of Enalapril is necessary in the elderly (after 65-70 years old), with endocrine disorders, an increase in the concentration of potassium in the blood, hyponatremia, in combination with other medicines intended for the treatment of coronary heart disease. To eliminate the risk of overdose, before prescribing the drug, check the condition of the patient's liver and kidneys.

Enalapril: instruction, dosage features

The drug in the form of ampoules is not available, therefore it is taken in the form of tablets, regardless of food and time of day.

The instruction for Enalapril provides for various treatment regimens depending on the underlying disease:

• With arterial hypertension (including renovascular "renal" type of pathology). The initial daily amount is 5 mg per day. During 1-2 for weeks the doctor monitors the patient's condition and gradually increases the dosage. Usually it is up 10-20 mg, divided into two doses throughout the day.
• With congestive chronic heart failure. Therapy begins with 2.5 mg per day, gradually (by 2.5-5 mg twice a week) this amount is brought to 15-20 mg per day (it is also possible to divide into two doses).

When treating with this drug, the following nuances must be taken into account:

• the daily amount of the drug Enalapril, the instruction does not recommend exceeding 40 mg (with renovascular hypertension - 20 mg). With a too pronounced decrease in blood pressure, it is reduced until the patient's condition is normalized;
• in patients over 65 years of age, the dosage is 1.25 mg per day;
• if the level of sodium ions in the blood is below normal (or the level of creatinine is above 0.14 mmol / l), the recommended daily amount of Enalapril in accordance with the instructions is 2.5 mg;
• in chronic renal failure with a reduced level of filtration, accumulation begins, in other words, the accumulation of Enalapril, which requires dosage adjustment;
• before you start taking the medicine, follow 2-3 the day should stop the use of diuretics;
• patients with low systolic blood pressure (less than 110 mm Hg) treatment should start with 1.25 mg per day, and the average maintenance amount of medication usually does not exceed 20 mg.

The drug Enalapril instruction allows you to use it both independently and in combination with other antihypertensive drugs. Usually the medicine is combined with diuretics. At the same time, a persistent antihypertensive effect is obtained against the background of a lower dosage of medications, which also reduces the risk of side complications.

So, in one of the studies, when taking 2.5 mg of the diuretic indapamide, the symptoms of hypertension were arrested in the amount of enalapril 15.5 mg. Currently, studies are underway on the effect of co-administration of ACE inhibitors and mildronate on improvement of the state of the vascular wall, which is important in the treatment of coronary heart disease in the background atherosclerosis.

The antihypertensive effect of the combination of Enalapril with diuretics, calcium antagonists led to the creation of combination drugs, these are:

• Enap N and Enap HL, containing 10 mg of enalapril and 25 mg or 12.5 mg of the diuretic hydrochlorothiazide, respectively;
• Co-Renitek, 20 mg enalapril and 12.5 mg hydrochlorothiazide;
• Coripren, 10 mg of enalapril and calcium antagonist medicinidipine;
• Enzix Duo Forte is a set of 20 mg enalapril tablets and 2.5 mg indapamide tablets;
• Renipril, in composition, is a complete analogue of the drug Enap HL;
• Berlipril Plus, the dosage of active substances coincides with the medicine Enap N.

The method of using these drugs is not much different from the instructions for Enalapril. They are also taken once a day, usually 1 tablet. It is also worth paying attention to other names of this ACE inhibitor. These are Enalapril Hexal, Enalapril Akti, Enalapril FPO.

These preparations contain only Enalapril and are used in the same dosage as described above.

As indicated in the instructions, the use of Enalapril during pregnancy is contraindicated. This is due to the fact that the drug easily passes through the placenta and enters the fetal bloodstream, which can lead to irreversible pathologies. Therefore, with an unplanned conception against the background of treatment with Enalapril, doctors warn a woman about possible complications.

Also, the medicine is not recommended to be combined with breastfeeding, since the active component of the drug passes into milk and lasts for a day. It is clear that given the medication regimen, safe lactation is not possible.

Treatment with Enalapril lasts more than one month, and during this period, patients often need other drugs. However, not all medications are combined with ACE inhibitors.

• Antihypertensive drugs. There is a mutual reinforcement of the action, which requires a reduction in dosage.
• Loop diuretics. One of the side effects of Enalapril is an increase in the level of potassium in the blood, this is especially often observed with concomitant renal failure, diabetes. Certain diuretics (Spironolactone or Triamterene) remove excess potassium from the body.
• Drugs to lower blood sugar. Enalapril enhances their action, which is fraught with the risk of hypoglycemia. This combination requires a blood glucose test for the first four weeks of treatment.
• Medicines containing lithium. ACE inhibitors delay the excretion of lithium by the kidneys, which leads to an increase in their concentration in the body.
• Medicines affecting the functioning of the central nervous system (antidepressants, drugs for general anesthesia, antipsychotics). There is a possibility that your blood pressure drops too much.
• Sympathomimetics (Isoprenaline, Izadrin, Astmopent), non-steroidal anti-inflammatory drugs (NSAIDs) reduce the hypotensive effect of Enalapril.
• Cytostatics and other immunosuppressants when combined with ACE inhibitors can cause a strong decrease in the level of leukocytes in the blood.
• Antacids, affect the degree of absorption of Enalapril from the digestive tract.

Other drugs do not significantly affect the use of Enalapril in the dosage according to the instructions. In the course of treatment, regular monitoring of clinical indicators of general and biochemical blood tests is necessary. In home therapy, the patient is asked to independently measure blood pressure twice a day and record these indicators in a special journal.

Enalapril: side effects, symptoms of overdose, prices and possible analogues

Reviews of doctors, patients and many years of clinical studies have shown that side effects against the background of Enalapril are rare, and in most cases the drug is well tolerated.

But about 5-10% patients experience the following complications:

• dizziness, headache;
• depression, increased fatigue;
• excessive decrease in blood pressure, orthostatic hypotension, arrhythmia;
• chest pain;
• nausea, diarrhea, soreness in the epigastrium, a perverse perception of taste;
• skin rash, allergic edema of the face, tongue, extremities;
• cough;
• dry mouth.

The rare side effects of Enalapril include:

• disorders of the hematopoietic system;
• hypoglycemia;
• sleep disturbances, nightmares;
• fainting;
• tinnitus, blurred vision;
• dysfunction of the liver;
• spasm of the biliary tract;
• disorders of urination;
• deterioration of sexual function in men;
• excessive sweating.

In addition, there is evidence of an increase in diseases of the upper and lower respiratory tract, organs of the genitourinary system while taking the drug. Also, many patients complained of exacerbation of herpes infection. But to date, the exact relationship between these manifestations in the drug Enalapril, the side effects of which are described in the instructions, has not been established.

Symptoms of a drug overdose develop progressively after about 5-6 hours. At first, a person complains of a decrease in blood pressure, bradycardia, weakness up to collapse. Without medical care, myocardial infarction, renal failure and death can occur.

Such consequences can be avoided if, after an overdose of Enalapril, rinse the patient's stomach, give an adsorbent. Hemolysis is also effective. Patients with bradycardia need a cardiac pacemaker.

The price of the domestic drug Enalapril ranges from 11 rubles for 20 tablets of 10 mg to 25 rubles for the same number of pills, but 20 mg each. Foreign counterparts are several times more expensive. However, in some cases, this overpayment is justified. Frankly speaking, in European countries the requirements for the production of medicines are much stricter than in our country. In addition, almost all foreign pharmaceutical companies present on the domestic market meet generally accepted international quality standards.

Therefore, a cardiologist can advise such analogs of this ACE inhibitor:

• Berlipril;
• Renipril;
• Rintek;
• Gemiton;
• Enalapril HEXAL;
• Enarenal;
• Enap.

Depending on the prescribed treatment regimen, the therapist may also prescribe Diursan - a German-made drug that is often used today to treat hypertension.

The method of using the listed analogs is the same, since the dosage of the active ingredient, that is, pure enalapril, is calculated to achieve a therapeutic effect. Sometimes your doctor will recommend another ACE inhibitor medicine, Lisinopril. According to clinical studies that compared the effectiveness of drugs under the same conditions, the effect of Lisinopril is no different from Enalapril.

These drugs equally had a persistent hypotensive effect, reduced the risk of sudden cardiac death and improved the general condition of patients. Therefore, Enalapril, an overdose of which is impossible if the instructions for use are followed, are advised for all categories of patients, both young and elderly.