Enalapril, 20 mg tablets 20 pcs.

Enalapril is an ACE inhibitor. It is a prodrug, from which the active metabolite enalaprilat is formed in the body. It is believed that the mechanism of antihypertensive action is associated with competitive inhibition of ACE activity, which leads to a decrease in the rate of conversion of angiotensin I to angiotensin II, which is a powerful vasoconstrictor.

The decrease in angiotensin II concentration results in a secondary increase in plasma renin activity by eliminating the negative feedback of renin release and a direct decrease in aldosterone secretion. In addition, enalaprilat appears to influence the kinin-callicrein system by inhibiting the breakdown of bradykinin.

With its vasodilator effect, it decreases RPO (postload), congestion pressure in the pulmonary capillaries (preload) and resistance in the pulmonary vessels; it increases cardiac minute volume and exercise tolerance.

Indications

Active ingredient

Composition

Lactose monohydrate;

Magnesium carbonate;

p> gelatin;

crospovidone;

magnesium stearate.

How to take, the dosage

Prescribe orally regardless of the time of meals.

In monotherapy of arterial hypertension, the initial dose is 5 mg once daily. If there is no clinical effect, the dose is increased by 5 mg after 1-2 weeks. After the initial dose, patients should be under medical supervision for 2 hours and an additional 1 hour until BP stabilizes. If necessary and tolerated well enough, the dose can be increased to 40 mg/day in 2 doses. After 2-3 weeks, switch to a maintenance dose of 10-40 mg/day divided into 1-2 doses. In moderate arterial hypertension, the average daily dose is about 10 mg.

The maximum daily dose of the drug is 40 mg/day.

If patients are prescribed concomitantly receiving diuretics, the diuretic treatment should be stopped 2-3 days before prescribing Enalapril. If this is not possible, the starting dose of the drug should be 2.5 mg/day.

Patients with hyponatremia (serum sodium ion concentration less than 130 mmol/L) or serum creatinine concentration greater than 0.14 mmol/L should be started with 2.5 mg once daily.

In renovascular hypertension, the initial dose is 2.5-5 mg/day. The maximum daily dose is 20 mg.

In chronic heart failure, the initial dose is 2.5 mg once, then the dose is increased by 2.5 to 5 mg every 3-4 days according to clinical response to maximum tolerated doses depending on BP values, but not more than 40 mg/day once or in 2 doses. In patients with low systolic blood pressure (less than 110 mmHg) therapy should be started with 1.25 mg/day. The dose should be adjusted for 2-4 weeks or for shorter periods. The average maintenance dose is 5-20 mg/day in 1-2 doses.

The elderly are more likely to have a more pronounced hypotensive effect and a longer duration of action of the drug due to a decreased elimination rate of enalapril, so the recommended starting dose for the elderly is 1.25 mg.

In chronic renal failure, cumulation occurs when filtration is less than 10 mL/min. With a CK of 80-30 mL/min, the dose is usually 5-10 mg/day, 2.5-5 mg/day with a CK of up to 30-10 mL/min, and 1.25-2.5 mg/day on dialysis days only with a CK of less than 10 mL/min.

The duration of treatment depends on the effectiveness of therapy. If BP decreases too significantly, the dose of the drug is gradually reduced.

The drug is used both in monotherapy and in combination with other antihypertensive agents.

Interaction

Concomitant administration of Enalapril with NSAIDs may decrease the hypotensive effect; with potassium-saving diuretics (spironolactone, triamterene, amiloride) may lead to hyperkalemia; with lithium salts – to delay lithium excretion (plasma lithium concentration control is indicated).

Simultaneous use with antipyretics and analgesics may decrease the effectiveness of enalapril.

Enalapril weakens the effect of drugs containing theophylline.

Enalapril hypotensive effects are enhanced by diuretics, beta-adrenoblockers, methyldopa, nitrates, slow calcium channel blockers, hydralazine, prazosin.

Immunosuppressants, allopurinol, cytostatics increase hematotoxicity.

The drugs causing bone marrow suppression increase the risk of neutropenia and/or agranulocytosis.

Special Instructions

Caution should be exercised when prescribing Enalapril in patients with decreased blood pressure (as a result of diuretic therapy, restriction of table salt intake, hemodialysis, diarrhea and vomiting) – the risk of a sudden and pronounced BP decrease after using even the initial dose of ACE inhibitor is increased. Transient arterial hypotension is not a contraindication for continuation of treatment with the drug after BP stabilization. In case of repeated pronounced BP decrease, the dose should be reduced or the drug should be discontinued.

The use of highly permeable dialysis membranes increases the risk of anaphylactic reaction. Adjustment of the dosing regimen on days free of dialysis should be made depending on the BP level.

Before and during treatment with ACE inhibitors, periodic monitoring of BP, blood parameters (hemoglobin, potassium, creatinine, urea, liver enzyme activity), urine protein is necessary.

Patients with severe heart failure, coronary heart disease, or cerebrovascular disease in whom a sharp decrease in BP may result in myocardial infarction, stroke, or impaired renal function should be closely monitored.

The abrupt withdrawal of treatment does not result in “withdrawal” syndrome (a rapid rise in BP).

In newborns and infants who have had intrauterine exposure to ACE inhibitors should be closely monitored for the timely detection of marked BP decline, oliguria, hyperkalemia, and neurologic impairment that may result from decreased renal and cerebral blood flow with ACE inhibitor-induced BP decline. In oliguria, it is necessary to maintain BP and renal perfusion by administration of appropriate fluids and vasoconstrictors. In the presence of renal failure, excretion of the active metabolite may be reduced, resulting in increased plasma concentrations. These patients may require prescribing lower doses of the drug.

In patients with arterial hypertension and unilateral or bilateral renal artery stenosis, serum urea and creatinine may increase.

In such patients, renal function should be monitored during the first few weeks of therapy. Dose reduction of the drug may be necessary.

The risk/benefit ratio should be considered when prescribing Enalapril to patients with coronary and cerebrovascular insufficiency due to the risk of increased ischemia with excessive arterial hypotension.

The drug should be administered with caution in patients with diabetes mellitus due to the risk of hyperkalemia.

Patients with a history of angioedema may have an increased risk of developing angioedema with Enalapril treatment.

Patients with severe autoimmune diseases, such as systemic lupus erythematosus or scleroderma, have an increased risk of neutropenia or agranulocytosis with Enalapril.

We recommend caution when prescribing Enalapril for therapy of chronic heart failure in patients treated with cardiac glycosides and/or diuretics.

The drug should be discontinued before parathyroid function tests. Alcohol increases the hypotensive effect of the drug.

Before surgical procedures (including dentistry), the surgeon/anesthesiologist should be warned about the use of ACE inhibitors.

Impact on driving and operating machinery.

At the beginning of treatment, until the end of the dose adjustment period, it is necessary to refrain from driving and engaging in potentially dangerous activities requiring increased concentration and rapid psychomotor reactions, as dizziness is possible, especially after the initial dose of ACE inhibitor in patients taking diuretics.

Contraindications

Main:

Side effects

Enalapril is generally well tolerated and in most cases does not cause adverse events requiring drug withdrawal.

Cardiovascular system disorders: excessive BP decrease, orthostatic collapse, rarely – chest pain, angina pectoris, myocardial infarction (usually associated with a pronounced BP decrease), very rarely – arrhythmias (atrial brady or tachycardia, atrial fibrillation), palpitation, pulmonary artery thromboembolism.

Nervous system disorders: dizziness, headache, weakness, insomnia, anxiety, confusion, increased fatigue, somnolence (2-3%), very rarely with high doses – nervousness, depression, paresthesia.

Sensory system disorders: vestibular system disorders, hearing and vision disorders, tinnitus.

Gastrointestinal tract: dry mouth, anorexia, dyspeptic disorders (nausea, diarrhea or constipation, vomiting, abdominal pain), intestinal obstruction, pancreatitis, liver function and biliary excretion disorders, hepatitis, jaundice.

Respiratory system: non-productive dry cough, interstitial pneumonitis, bronchospasm, dyspnea, rhinorrhea, pharyngitis.

Allergic reactions: skin rash, pruritus, urticaria, angioneurotic edema, extremely rare – dysphonia, erythema polymorphic, exfoliative dermatitis, Stephen-Johnson syndrome, toxic epidermal necrolysis, pemphigus, photosensitization, serositis, vasculitis, myositis, arthralgia, arthritis, stomatitis, glossitis.

In laboratory parameters: hypercreatininemia, increased urea, increased liver enzymes activity, hyperbilirubinemia, hyperkalinemia, hyponatremia. In some cases decrease of hematocrit level, increase of sedimentation rate, thrombocytopenia, neutropenia, agranulocytosis (in patients with autoimmune diseases), eosinophilia are noted.

Urinary system disorders: impaired renal function, proteinuria.

Others: alopecia, decreased libido, hot flashes.

Overdose

Symptoms: marked BP decrease up to the development of collapse, myocardial infarction, acute cerebral circulation disorder or thromboembolic complications, convulsions, stupor.

Treatment: the patient is transferred to a horizontal position with a low headboard. In mild cases gastric lavage and oral administration of saline solution are indicated, in more severe cases – measures aimed at BP stabilization: intravenous infusion of saline solution, plasma substitutes, angiotensin II administration, hemodialysis, if necessary (elimination rate of enalaprilat averages 62 ml/min).

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