Enap

Enap is an antihypertensive drug that contains the element enalapril, which suppresses the activity of ACE, resulting in a decrease in the production of angiotensin-2.

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Indications Enapa

It is used in the following conditions:

• primary hypertension;
• complex therapy for CHF;
• prevention of the development of severe heart failure in people who have been diagnosed with left ventricular dysfunction without symptoms (complex treatment course);
• to reduce the incidence of myocardial infarctions;
• to reduce the frequency of hospitalizations in people with unstable angina.

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Release form

The drug is produced in tablets with different volumes of the active substance - 2.5, 5, and also 10 and 20 mg. There are 10 such tablets inside the blister pack. There are 2, 3 or 6 packs in the box.

Pharmacodynamics

The component enalapril is a derivative of amino acids (such as L-proline and L-alanine). After oral administration of the drug, the component is hydrolyzed, turning into enalaprilat, which slows down the action of ACE. The activity of the component leads to a decrease in the production of angiotensin-2 from angiotensin-1. Due to a decrease in its plasma values, there is an increase in the activity of plasma renin and a decrease in the production of aldosterone.

Because ACE is similar to kininase-2, enalapril is able to block the processes of bradykinin destruction (a peptide with vasopressor properties). It has not yet been finally determined what therapeutic result this effect of enalapril leads to.

The hypotensive effect of the component is based on the suppression of RAAS activity, which is extremely important in regulating blood pressure values. However, in individuals with increased blood pressure and low renin levels, the hypotensive effect of enalapril is also recorded.

The use of the drug reduces the level of blood pressure, regardless of the position of the patient's body. No significant increase in the heart rate is noted.

Symptomatic orthostatic collapse occurs only occasionally. In some cases, several weeks of treatment are required to achieve a significant reduction in blood pressure. Abrupt discontinuation of Enap did not result in an increase in blood pressure.

In individuals with primary hypertension, in the case of a decrease in blood pressure, a weakening of peripheral vascular resistance and an increase in cardiac output values are observed. However, no noticeable change in heart rate is recorded. Blood circulation inside the kidneys increases, and the glomerular filtration rate does not change. However, this indicator increases in individuals with a low filtration rate.

In patients with nephropathy, whether diabetic or non-diabetic, enalapril resulted in a reduction in proteinuria or albuminuria and a decrease in renal excretion of IgG.

In patients treated for CHF, at the stage of therapy using CG and diuretics, and at the same time with the introduction of enalapril, there is a decrease in cardiac output or blood pressure with total peripheral vascular resistance, as well as heart rate (usually in patients with CHF this indicator is elevated).

There is a decrease in capillary congestion inside the lungs. Long-term use of the drug increases tolerance to physical activity and reduces the severity of heart failure symptoms. In patients with moderate or mild CHF, the drug slows the progression of the disease and reduces the rate of development of left ventricular dilatation.

In patients with left ventricular dysfunction, LS reduces the risk of developing symptoms of the most common ischemic outcomes (reduction in the number of cases of myocardial infarction together with the number of hospitalizations associated with angina).

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Pharmacokinetics

A pronounced ACE inhibitory effect is usually recorded after 2-4 hours from the moment of oral administration of the drug. The hypotensive effect often develops after 60 minutes from the moment of oral administration of the substance, and Cmax values occur after 4-6 hours. The duration of the effect is determined by the size of the therapeutic portion. When using the dosages recommended by the doctor, the hypotensive and hemodynamic effect is maintained for at least 24 hours.

The active substance taken is rapidly absorbed, with an absorption rate of approximately 60%. Peak blood levels of the substance are observed 60 minutes after administration; food intake does not affect the absorption rate. The drug undergoes active hydrolysis, which forms enalaprilat, which slows down the activity of ACE. Cmax values of enalaprilat are recorded 3-4 hours after oral administration. After repeated administration, the half-life of enalapril is 11 hours.

The substance does not undergo any significant transformation within the body, except for transformation into enalaprilat.

Excretion occurs mainly via the kidneys. In the urine, 40% of enalaprilat is found, as well as 20% of enalapril in an unchanged state.

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Dosing and administration

The medication should be taken orally, without reference to food intake. It is necessary to take the medicine at the same time of day, with a small amount of any liquid.

To reduce elevated blood pressure, the drug is initially prescribed in a dose of 5-20 mg, once a day (a more precise dosage is determined by the severity of the disorder). In mild hypertension, 5 or 10 mg of the substance should be taken per day.

In individuals with a marked increase in RAAS activity, the blood pressure level may drop sharply. In such cases, it is necessary to use small medicinal doses - 5 mg per day. Therapy is carried out under medical supervision.

Before using Enap, it is necessary to take into account that in case of previous therapy with diuretic drugs (in large doses), dehydration may develop and the likelihood of a drop in blood pressure may increase already at the beginning of the treatment course. In this case, a maximum of 5 mg of the drug per day should be taken. The use of diuretic drugs should be discontinued 2-34 days before starting to use the medication. During therapy, it is necessary to monitor kidney function and determine blood potassium levels.

The maintenance dosage is 20 mg, taken once a day. If necessary, the daily dose can be increased to 40 mg. Dosage sizes are generally selected individually.

During the treatment of CHF or left ventricular dysfunction, it is necessary to initially use 2.5 mg of the drug per day. When treating CHF, combined use with CG, diuretics and β-blockers is sometimes prescribed.

Having corrected the elevated blood pressure values, the dose can be gradually increased by 2.5-5 mg at 3-4 day intervals until it is brought to the maintenance level of 20 mg per day. The maximum permissible daily dosage is 40 mg.

Since the therapy may significantly reduce blood pressure and cause renal failure, kidney function and blood pressure values must be closely monitored during the treatment cycle. If the blood pressure drops sharply after taking the first dose, there is no need to stop taking the medicine.

People with kidney disease should increase the intervals between doses of the drug or reduce its dosage.

Elderly patients should take an initial dose of 1.25 mg because they have a slower excretion of enalapril.

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Use Enapa during pregnancy

It is prohibited to prescribe Enap during pregnancy, because there is a possibility of teratogenic effects. If pregnancy is diagnosed, it is necessary to immediately stop using the drug.

When using ACE inhibitors in pregnant women, it is necessary to undergo ultrasound examination periodically to assess the parameters of amniotic fluid. In addition, ultrasound of the kidneys and cranial bones of the fetus is performed.

The active ingredient Enap is found in breast milk, so breastfeeding should be discontinued during the treatment period.

Contraindications

Among the contraindications:

• the presence of intolerance in the patient to the component enalapril, as well as other elements of the drug;
• history of Quincke's edema that appeared during therapy with ACE inhibitors;
• Quincke's edema of idiopathic or hereditary nature;
• porphyria;
• use in combination with aliskiren in people with kidney disease or diabetes mellitus;
• glucose-galactose malabsorption, hypolactasia and lactase deficiency (because the drug contains lactose).

The medication should be used with caution in the following cases:

• stenosis associated with the arteries inside the kidneys;
• hyperkalemia;
• persons who have undergone a kidney transplant;
• Conn's syndrome;
• decreased BCC values;
• obstructive cardiomyopathy of the hypertrophic type;
• stenosis of the aortic or mitral valve;
• diabetes mellitus;
• IHD;
• general connective tissue lesions;
• suppression of hematopoietic processes;
• cerebrovascular pathologies;
• renal failure.

Caution is also required when used by individuals on a dietary regimen with reduced salt intake, as well as by individuals taking immunosuppressants or diuretics, and by those undergoing hemodialysis sessions.

People over 65 years of age should consult a doctor before taking this medication.

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Side effects Enapa

Therapy may be accompanied by the development of the following side effects:

• disorders of hematopoiesis: thrombocytopenia, neutro- or pancytopenia, anemia, and in addition agranulocytosis, lymphadenopathy, autoimmune diseases, decreased hemoglobin and hematocrit values and suppression of hematopoiesis;
• metabolic disorders: hypoglycemia;
• problems with the functioning of the nervous system: headaches, paresthesia, vertigo, depression, insomnia, disturbances of consciousness, a feeling of strong excitability or drowsiness and sleep disorders;
• lesions affecting the function of the cardiovascular system: a sharp drop in blood pressure, dizziness, angina, chest pain, heart rhythm disorders, myocardial infarction or stroke, palpitations and Raynaud's disease;
• signs related to the senses: tinnitus, changes in taste and blurred vision;
• digestive disorders: nausea, abdominal pain, constipation, vomiting, bloating, diarrhea, intestinal obstruction, as well as dyspepsia, pancreatitis, dry mouth and anorexia. In addition, stomatitis, peptic ulcer, glossitis, liver dysfunction and bile secretion, as well as aphthous ulcers, liver necrosis, hepatitis and cholestasis;
• respiratory problems: sore throat, dyspnea, cough, hoarseness, bronchial spasm, rhinorrhea, runny nose, eosinophilic pneumonia and alveolitis of allergic origin;
• epidermal lesions: Quincke's edema, itching, symptoms of intolerance, rashes, hyperhidrosis, urticaria, erythroderma, as well as alopecia, erythema multiforme, pemphigus, TEN and exfoliative dermatitis;
• disorders of the urogenital system: proteinuria, oliguria, renal failure, gynecomastia, renal dysfunction and impotence;
• musculoskeletal dysfunction: muscle cramps;
• laboratory test findings: hyponatremia or hyperkalemia, elevated serum creatinine, blood urea levels, liver enzyme activity, and blood bilirubin levels;
• other symptoms: myalgia, Parhon syndrome, leukocytosis, fever, vasculitis, and in addition myositis, serositis, increased ESR, arthritis and signs of photosensitivity.

Overdose

In case of intoxication, after about 6 hours, a strong drop in blood pressure values is observed. Collapse and disorder of EBV indices are possible, as well as renal failure, hyperventilation, convulsions, bradycardia with strong heartbeat, tachycardia and dizziness.

In case of overdose, it is necessary to place the victim horizontally, so that the head is at the level of the body. In case of mild poisoning, gastric lavage is performed and the patient is given activated carbon. In case of severe disorders, 0.9% NaCl is administered intravenously, and in addition, catecholamines or plasma substitutes can be used intravenously.

Excretion of enalaprilat can be accomplished by hemodialysis at a rate of 62 ml/minute.

People with bradycardia are given a pacemaker. In case of poisoning, serum electrolyte values and creatinine levels should be closely monitored.

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Interactions with other drugs

In case of double blockade of RAAS activity (when combining ACE inhibitors with angiotensin-2 terminal antagonists or aliskiren), the probability of a drop in blood pressure increases. If such a combination of drugs is necessary, it is necessary to closely monitor the values of EBV, renal function and blood pressure indicators.

The drug should not be combined with aliskiren in people with kidney disease or diabetics.

ACE inhibitors reduce the loss of potassium under the influence of diuretics. The use of enalapril together with potassium-containing substitutes or potassium-sparing diuretics may lead to the development of hyperkalemia. With this combination, it is necessary to monitor the serum potassium values.

Following previous treatment with diuretics, the volume of circulating blood may decrease and the risk of a decrease in blood pressure may increase when using enalapril. This effect can be reduced by discontinuing the use of diuretics, increasing the daily volume of salt and water, and reducing the dose of enalapril.

Combination of Enap with methyldopa, nitroglycerin, α- and β-adrenergic blockers, ganglionic blocking drugs, CCBs or other nitrates can additionally lower blood pressure.

Use with lithium agents results in a temporary increase in lithium levels, as well as lithium poisoning. Administration of thiazide diuretics may increase serum lithium levels. Such combinations are best avoided, and if such a combination is needed, it is important to closely monitor serum lithium levels.

Administration of drugs together with certain anesthetics, antipsychotics or tricyclics may further reduce blood pressure values.

Combined use with NSAIDs may reduce the hypotensive activity of the drug. Weakening of renal function is possible (especially in people with kidney pathologies). Such an effect is treatable.

Combined use with insulin and antidiabetic drugs may enhance antidiabetic activity and increase the likelihood of hypoglycemia.

The hypotensive properties of Enap are potentiated by the use of ethyl alcohol.

Sympathomimetics reduce the hypotensive activity of ACE inhibitors.

Enalapril weakens the effect of medications containing the component theophylline.

The introduction of cytostatics, immunosuppressants or allopurinol together with the drug increases the risk of leukopenia. In people with renal dysfunction, the use of ACE inhibitors with allopurinol increases the likelihood of allergy.

Cyclosporine increases the risk of developing hyperkalemia.

The bioavailability of ACE inhibitors is reduced when administered with antacids.

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Storage conditions

Enap should be stored in a place closed to small children. Temperature marks – no more than 25°C.

Shelf life

Enap can be used within 36 months from the date of production of the drug.

Application for children

The medication is not used in pediatrics (under 18 years of age).

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Analogues

Analogues of the therapeutic element are the drugs Renipril, Enap R, Ednit and Bagopril with Invoril, as well as Berlipril, Enalapril with Vazolapril, etc.

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Reviews

Enap receives mostly positive reviews from doctors. It is believed that with the correct use of the drug, the patient's quality of life improves significantly. But it should be taken into account that the drug often causes side effects. Patients' comments often note the development of a dry cough, etc. It is necessary to remember that if the condition begins to worsen, you should immediately consult a doctor to change the dose of the drug or prescribe another drug.