Composition
1 tablet 5 mg contains:
Active ingredient: Â
Enalapril maleate — 5 mg.
Auxiliary substances: Â
Lactose monohydrate — 106,000 mg,
Magnesium carbonate — 71.645 mg,
Gelatin-7,800 mg,
Crospovidone — 7,800 mg,
Magnesium stearate — 1,755 mg
Pharmacological action
Enalapril is an angiotensin-converting enzyme inhibitor. Enalapril has a dilating effect on the arteries and to a lesser extent on the veins.
The hypotensive effect of Enalapril is more pronounced with an increased concentration of renin in the blood plasma. The use of Enalapril improves renal and coronary blood flow.
Long-term use of Enalapril reduces left ventricular hypertrophy and prevents the development of chronic heart failure.
Enalapril has a stimulating effect on the blood supply to the myocardium. Reduces platelet aggregation.
Enalapril is indicated for slowing the development of left ventricular dysfunction in patients who have had a myocardial infarction.
According to the reviews received, Enalapril has some diuretic effect.
Enalapril is a “prodrug” that hydrolyzes to form enalaprilate, which in turn inhibits the angiotensin-converting enzyme.
The antihypertensive effect occurs 1 hour after taking Enalapril and lasts for 24 hours.
Some patients need therapy for several weeks to achieve optimal blood pressure readings.
Patients with chronic heart failure require at least 6 months of treatment to achieve a noticeable clinical effect.
Indications
prevention of coronary ischemia; arterial hypertension; patients with left ventricular dysfunction of the myocardium.
Use during pregnancy and lactation
It is contraindicated for use during pregnancy.
If you are pregnant, enalapril should be discontinued immediately.
Enalapril is excreted in breast milk.
If it is necessary to use it during lactation, the question of stopping breastfeeding should be decided.
Contraindications
Hypersensitivity to enalapril and other ACE inhibitors, a history of angioedema associated with treatment with ACE inhibitors, porphyria, pregnancy, lactation, age up to 18 years (efficacy and safety have not been established). Use with caution in primary hyperaldosteronism, bilateral renal artery stenosis, stenosis of the artery of a single kidney, hyperkalemia, condition after kidney transplantation; aortic stenosis, mitral stenosis (with hemodynamic disorders), idiopathic hypertrophic subaortic stenosis, systemic connective tissue diseases, coronary heart disease, cerebrovascular diseases, diabetes mellitus, renal failure (proteinuria — more than 1 g/kg). day), hepatic insufficiency, in patients following a salt-restricted diet or undergoing hemodialysis, while taking immunosuppressants and saluretics, in the elderly (over 65 years of age).
Side effects
Orthostatic collapse, rarely – palpitations, chest pain, pulmonary embolism, arrhythmias (atrial fibrillation, atrial Bradi – or tachycardia), angina, myocardial infarction;
fainting, dizziness, weakness, headache, paresthesia, insomnia, depression, anxiety, confusion, drowsiness (2-3%), fatigue,
rarely in excess of the dosage – depression, nervousness; dry mouth, impaired function of the bile, dyspeptic disorders (diarrhea or constipation, nausea, vomiting), intestinal obstruction,
pain in the abdomen, pancreatitis, jaundice, hepatitis; pharyngitis, rhinorrhea, shortness of breath, bronchospasm, interstitial pneumonitis, non-productive cough; glossitis, stomatitis, arthritis, arthralgia, myositis, vasculitis, and Ceresit,
photosensitivity, urticaria, pruritus, epidermal necrolysis, pemphigus (pemphigus), multiforme exudative erythema, exfoliative dermatitis, dysphonia, angioneurotic edema, skin rash face;Â
eosinophilia, agranulocytosis, thrombocytopenia, neutropenia, increased ESR, decreased Hb and hematocrit, hyponatremia, hyperkalemia, increased transaminase activity, hypercreatininemia, hyperbilirubinemia, increased urea concentration, proteinuria; decreased libido, alopecia.
Interaction
Concomitant use of Enalapril with nonsteroidal anti-inflammatory drugs (NSAIDs) may reduce the hypotensive effect.
Potassium-sparing diuretics (spironolactone, triamterene, amiloride) can lead to hyperkalemia.
With lithium salts – to slow down the excretion of lithium (control of the concentration of lithium in blood plasma is shown).
Concomitant use with antipyretics and painkillers may reduce the effectiveness of enalapril. Enalapril weakens the effect of drugs containing theophylline.
Antihypertensive effect of enalapril is enhanced by diuretics, beta-blockers, 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.
How to take, course of use and dosage
Assign inside regardless of the time of meal. For monotherapy of arterial hypertension: the initial dose is 5 mg once a day.
In the absence of a clinical effect, the dose is increased by 5 mg after 1-2 weeks. After taking the initial dose, patients should be under medical supervision for 2 hours and an additional 1 hour until
blood pressure stabilizes. If necessary and sufficiently well tolerated, the dose can be increased to 40 mg / day in 2 divided doses. After 2-3 weeks, they switch to a maintenance dose of 10-40 mg / day, divided into 1-2 doses.
With 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 to patients receiving diuretics at the same time, treatment with a diuretic should be discontinued 2-3 days before the appointment of Enalapril.
If this is not possible, then the initial dose of the drug should be 2.5 mg / day.
Use in patients with hyponatremia: in patients with hyponatremia (serum sodium ion concentration less than 130 mmol / l) or serum creatinine concentration more than 0.14 mmol/L, the initial dose is 2.5 mg once a day.
For 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 2.5-5 mg every 3-4 days in accordance with the clinical response to the maximum tolerated doses, depending on the values of blood pressure, but not higher than 40 mg/day once or in 2 doses.
Use in patients with low systolic blood pressure (less than 110 mm Hg): therapy should begin with a dose of 1.25 mg / day. Dose selection should be carried out within 2-4 weeks or in a shorter time frame.
The average maintenance dose is 5-20 mg / day in 1-2 doses.
Use in elderly patients: Â
elderly people often have a more pronounced antihypertensive effect and prolongation of the drug’s action time, which is associated with a decrease in the rate of elimination of enalapril, so the recommended initial dose for the elderly is 1.25 mg.
Use in patients with impaired renal function: Â
in chronic renal failure, accumulation occurs when filtration decreases to less than 10 ml/min.
With a creatinine clearance of 80-30 ml / min, the dose is usually 5-10 mg / day, with a creatinine clearance of up to 30-10 ml / min-2.5-5 mg / day, with a creatinine clearance of less than 10 ml/min – 1.25-2.5 mg/day only on dialysis days.
The duration of treatment depends on the effectiveness of the therapy.
If the blood pressure is too pronounced, the dose of the drug is gradually reduced.
The drug is used both in monotherapy and in combination with other antihypertensive agents.
Overdose
Symptoms: Â
marked decrease in blood pressure up to the development of collapse, myocardial infarction, acute cerebrovascular accident or thromboembolic complications, convulsions, stupor.
Treatment: Â
the patient is placed in a horizontal position with a low headboard. In mild cases, gastric lavage and ingestion of saline solution are indicated, in more severe cases-measures aimed at stabilizing blood pressure: Â
intravenous use of saline, plasma substitutes, if necessary – the introduction of angiotensin II, hemodialysis (the rate of elimination of enalaprilat on average is 62 ml / min).
Special instructions
Caution should be exercised when prescribing Enalapril to patients with reduced circulating blood volume (as a result of diuretic therapy, with limited salt intake,
hemodialysis, diarrhea and vomiting) – the risk of sudden and pronounced decrease in blood pressure after even the initial dose of an ACE inhibitor is increased.
Transistor arterial hypotension is not a contraindication for continuing treatment with the drug after blood pressure stabilization.
In case of repeated pronounced decrease in blood pressure, 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 dosage regimen on dialysis-free days should be made depending on the blood pressure level. Before and during treatment with ACE inhibitors, periodic monitoring of blood pressure, blood parameters (hemoglobin, potassium, creatinine, urea, activity of “liver” enzymes), protein in the urine is necessary.
Patients with severe heart failure, ischemic heart disease, and vascular diseases of the brain should be carefully monitored if a sharp decrease in blood pressure can lead to myocardial infarction, stroke, or impaired renal function.
Sudden discontinuation of treatment does not lead to a “withdrawal” syndrome (a sharp rise in blood pressure). Newborns and children who have been exposed to ACE inhibitors in utero should be
carefully monitored for the timely detection of a marked decrease in blood pressure, oliguria, hyperkalemia, and neurological disorders that may result from a decrease in renal and cerebral blood flow with a decrease in blood pressure caused by ACE inhibitors.
With oliguria, it is necessary to maintain blood pressure and renal perfusion by introducing appropriate fluids and vasoconstrictors.
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 during Enalapril treatment.
Patients with severe autoimmune diseases, such as systemic lupus erythematosus or scleroderma, have an increased risk of developing neutropenia or agranulocytosis while taking Enalapril.
Caution is recommended when prescribing Enalapril for the treatment of chronic heart failure in patients receiving cardiac glycosides and / or diuretics.
Before studying the functions of the parathyroid glands, the drug should be discontinued. Alcohol increases the hypotensive effect of the drug. Before surgery (including dentistry), the surgeon/anesthesiologist should be warned about the use of ACE inhibitors.
Use in patients with impaired renal function: in the presence of renal insufficiency, it is possible to reduce the excretion of the active metabolite, leading to an increase in its concentration in blood plasma.
Other patients may need to be prescribed lower doses of the drug. In patients with arterial hypertension and unilateral or bilateral renal artery stenosis, an increase in serum urea and creatinine may occur.
In such patients, renal function should be monitored during the first few weeks of therapy. It may be necessary to reduce the dosage of the drug.
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.
Effects on ability to drive vehicles and operate machinery: at the beginning of treatment until the end of the titration, it is necessary to refrain from driving and transport activities potentially
hazardous activities, require high concentration and psychomotor speed, reactions as dizziness, especially after the initial dose of ACE inhibitor in patients taking diuretics.
Form of production
Tablets are white in color, round, biconvex, with a risk on one side.
Storage conditions
Store in a dry place, at a temperature of 15 to 25 C.
Keep out of the reach of children.
Shelf
life is 3 years. Do not use after the expiration date.
Active ingredient
Enalapril
Conditions of release from pharmacies
By prescription
Dosage form
Tablets
Purpose
For adults as directed by your doctor
Indications
Heart Failure, Hypertension
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