Enalapril, tablets 5 mg 20 pcs

Enalapril is an angiotensin-converting enzyme inhibitor. Enalapril has a dilating effect on arteries and to a lesser extent on veins.

Enalapril has a more pronounced hypotensive effect when plasma renin concentrations are elevated. The use of Enalapril improves renal and coronary blood flow.

Long-term use of Enalapril reduces left ventricular myocardial hypertrophy and prevents development of chronic heart failure.

Enalapril has a stimulating effect on myocardial blood flow. It reduces platelet aggregation.

Enalapril is indicated to slow the development of left ventricular dysfunction in patients who have had a myocardial infarction.

Enalapril has been reported to have some diuretic effect.

Enalapril is a “prodrug” that by hydrolysis forms enalaprilate, which in turn inhibits the angiotensin-converting enzyme.

Hypotensive effect occurs 1 hour after taking Enalapril and lasts for 24 hours.

Some patients require therapy for several weeks to achieve optimal blood pressure readings.

Patients with chronic heart failure require a course of at least 6 months of treatment for a noticeable clinical effect.

Indications

Prevention of coronary ischemia; arterial hypertension; patients with left ventricular myocardial dysfunction.

Active ingredient

Composition

1 tablet 5 mg contains:

The active ingredient:

Enalapril maleate – 5 mg.

Associates:

Lactose monohydrate – 106.000 mg,

Magnesium carbonate – 71.645 mg,

Gelatin – 7,800 mg,

Crospovidone – 7,800 mg,

Magnesium stearate – 1,755 mg.

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 sufficiently well tolerated, the dose can be increased to 40 mg/day in 2 doses. After 2-3. weeks, a maintenance dose of 10-40 mg/day divided into 1-2 doses is switched to.

In moderate arterial hypertension, the average daily dose is about 10 mg. The maximum daily dose of the drug is 40 mg/day.

Use in patients receiving diuretics: If prescribed in patients receiving diuretics at the same time, 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: In patients with hyponatremia (serum sodium ion concentration less than 130 mmol/L) or serum creatinine concentration greater than 0.14 mmol/L the starting dose is 2.5 mg once daily.

In renovascular hypertension: 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 2.5-5 mg every 3-4 days according to clinical response to the maximum tolerated dose depending on BP values, but not more than 40 mg/day once or in 2 doses.

Use in patients with low systolic blood pressure (less than 110 mmHg): therapy should be started with a dose of 1.25 mg/day. The dose should be adjusted within 2-4 weeks or at shorter intervals.

The average maintenance dose is 5-20 mg/day in 1-2 doses.

The use in elderly patients:

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

The use in patients with impaired renal function:

In chronic renal failure, cumulation occurs when filtration is less than 10 ml/min.

In patients with a creatinine clearance (CK) of 80-30 mL/min, the dose is usually 5-10 mg/day, with CK up to 30-10 mL/min -2.5-5 mg/day, and with CK less than 10 mL/min, 1.25-2.5 mg/day on dialysis days only.

The duration of treatment depends on the effectiveness of therapy.

If BP decreases too markedly, the drug dose is gradually reduced.

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

Interaction

The simultaneous administration of Enalapril with nonsteroidal anti-inflammatory drugs (NSAIDs) may reduce the hypotensive effect.

With potassium-saving diuretics (spironolactone, triamterene, amiloride) may lead to hyperkalemia.

With lithium salts – slowing of lithium excretion (monitoring of plasma lithium concentrations 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. Drugs that cause bone marrow suppression increase the risk of neutropenia and/or agranulocytosis.

Special Instructions

Patients with reduced circulating blood volume (as a result of diuretic therapy, restriction of table salt intake, hemodialysis, diarrhea and vomiting) should be cautioned when prescribing Enalapril – the risk of a sudden and marked BP decrease after even an initial dose of ACE inhibitor is increased.

Transient arterial hypotension is not a contraindication to continue treatment with the drug after BP stabilization.

In case of repeated marked BP decrease, the dose should be reduced or the drug should be discontinued. Use of high permeability dialysis membranes increases the risk of anaphylactic reaction.

The dosing regimen on days free of dialysis should be adjusted depending on the BP level. Before and during treatment with ACE inhibitors, periodic monitoring of BP, blood parameters (hemoglobin, potassium, creatinine, urea, activity of “liver” enzymes), urine protein is necessary.

Patients with severe heart failure, coronary heart disease, and cerebrovascular disease in whom a rapid decrease of BP may result in myocardial infarction, stroke, or renal impairment should be closely monitored.

The abrupt withdrawal of treatment does not lead to “withdrawal” syndrome (a sharp rise in BP). Newborns and infants who have had intrauterine exposure to ACE inhibitors should be closely monitored for early detection of significant decreases in BP, oliguria, hyperkalemia, and neurologic impairment due to decreased renal and cerebral blood flow with ACE inhibitor-induced BP reduction.

In oliguria, it is necessary to maintain BP and renal perfusion by administration of appropriate fluids and vasoconstrictors.

The drug should be used with caution in patients with diabetes because of the risk of hyperkalemia.

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

Patients with significant 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 intervention (including dentistry), the surgeon/anesthesiologist should be warned about the use of ACE inhibitors.

Patients with impaired renal function: In the presence of renal failure, the excretion of the active metabolite may be reduced, resulting in increased plasma concentrations. Such 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.

Impact on driving and operating machinery: at the start of treatment and before completion of the dose adjustment period, patients taking diuretics should refrain from driving and engaging in potentially dangerous activities requiring increased concentration and rapid psychomotor reactions since dizziness is possible, especially after the initial dose of ACE inhibitor.

Contraindications

Side effects

Orthostatic collapse, rarely – palpitation, chest pain, pulmonary embolism, arrhythmias (atrial fibrillation, atrial brady or tachycardia), angina pectoris, myocardial infarction; fainting, dizziness, weakness, headache, paresthesia, insomnia, depression, anxiety, confusion, drowsiness (2-3%), fatigue, very rare in overdose – depression, nervousness; dry mouth, poor bile secretion function, dyspeptic disorders (diarrhea or constipation, nausea, vomiting), intestinal obstruction, abdominal pain, pancreatitis, jaundice, hepatitis; pharyngitis, rhinorrhea, shortness of breath, bronchospasm, interstitial pneumonitis, non-productive cough; glossitis, stomatitis, arthritis, arthralgia, myositis, vasculitis, serositis, photosensitization, urticaria, skin itching, epidermal necrolysis, pemphigus, erythema multiforme, exfoliative dermatitis, dysphonia, angioneurotic edema, facial skin rash; eosinophilia, agranulocytosis, thrombocytopenia, neutropenia, increased sedimentation, decreased Hb and hematocrit, hyponatremia, hyperkalemia, increased transaminase activity, hypercreatininemia, hyperbilirubinemia, increased concentration of urea, proteinuria; decreased libido, alopecia.

Overdose

Symptoms:

The pronounced decrease in BP up to the development of collapse, myocardial infarction, acute cerebral circulation disorder or thromboembolic complications, seizures, 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 stabilization of BP:

Intravenous administration of saline solution, plasma substitutes, if necessary – angiotensin II infusion, hemodialysis (elimination rate of enalaprilat is on average 62 ml/min).

Pregnancy use

It is contraindicated in pregnancy.

Enalapril should be stopped immediately if pregnancy occurs.

Enalapril is excreted with breast milk.

If its use is necessary during lactation, discontinuation of breastfeeding should be considered.

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