Enalapril, pills 20mg, 20pcs

Composition

1 tablet of 20 mg contains: Active ingredient: Enalapril maleate — 20 mg. Auxiliary substances: Lactose monohydrate — 116,400 mg, Magnesium carbonate-120,000 mg, Gelatin-10,700 mg, Crospovidone-10,700 mg, Magnesium stearate-2,200 mg

Composition

.

ACE inhibitor.

Pharmaceutical action:  

An ACE inhibitor is a hypotensive drug, the mechanism of action is associated with a decrease in the formation of angiotensin II from angiotensin I, a decrease in the concentration of which leads to a direct decrease in aldosterone secretion.

At the same time, OPSS, systolic and diastolic blood pressure, post – and preload on the myocardium decreases. Dilates the arteries to a greater extent than the veins, while there is no reflex increase in heart rate.

Reduces the degradation of bradykinin, increases the synthesis of Pg. The hypotensive effect is more pronounced at high plasma renin concentrations than at normal or reduced ones.

Lowering blood pressure within therapeutic limits does not affect cerebral circulation, blood flow in the brain vessels is maintained at a sufficient level and against the background of reduced blood pressure.

Increases coronary and renal blood flow. Prolonged use reduces LV hypertrophy of the myocardium and myofibrils of the resistive artery walls, prevents the progression of CHF and slows down the development of LV dilation.

Improves blood supply to the ischemic myocardium.

Reduces platelet aggregation. Prolongs life expectancy in patients with CHF, slows down the progression of LV dysfunction in patients who have had a myocardial infarction, without clinical manifestations of HF.

It has some diuretic effect. Reduces intraglomerular hypertension, slowing the development of glomerulosclerosis and the risk of CRF.

Enalapril is a “prodrug”: as a result of its hydrolysis, enalaprilate is formed, which inhibits ACE.

The time of onset of the hypotensive effect with oral use is 1 hour, it reaches a maximum in 4-6 hours and persists for up to 24 hours.

In some patients, therapy for several weeks is necessary to achieve optimal blood pressure levels. With CHF, a noticeable clinical effect is observed with long-term treatment-6 months or more.

Indications

Arterial hypertension. In case of chronic heart failure (as part of combination therapy).

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

From the cardiovascular system: excessive decrease in blood pressure, orthostatic collapse, rarely-chest pain, angina pectoris, myocardial infarction (usually associated with a pronounced decrease in blood pressure), arrhythmias (atrial brady or tachycardia, atrial fibrillation), palpitations, thromboembolism of the branches of the pulmonary artery.

From the nervous system: dizziness, fainting, headache, weakness, insomnia, anxiety, confusion, increased fatigue, drowsiness (2-3%), very rarely when used in high doses – nervousness, depression, paresthesia.

From the sensory organs: vestibular disorders, hearing and vision disorders, tinnitus.

From the digestive system: dryness of the oral mucosa, decreased appetite, dyspeptic disorders (nausea, diarrhea or constipation, vomiting, abdominal pain), intestinal obstruction, pancreatitis, liver and biliary dysfunction, hepatitis, jaundice.

From the respiratory system: unproductive” dry ” cough, interstitial pneumonitis, bronchospasm, shortness of breath, rhinorrhea, pharyngitis.

Allergic reactions: skin rash, angioedema of the face, small intestine (very rare), extremities, lips, tongue, glottis and/or larynx, dysphonia, exfoliative dermatitis, multiforme

exudative erythema (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell’s syndrome), pemphigus (pemphigus), pruritus, urticaria, photosensitivity, Ceresit, vasculitis, myositis, arthralgia, arthritis, stomatitis, glossitis.

From the laboratory parameters: hypercreatininemia, increased urea concentration, increased activity of “hepatic” transaminases, hyperbilirubinemia, hyperkalemia, hyponatremia,

decreased Hb and hematocrit, increased ESR, thrombocytopenia, neutropenia, agranulocytosis (in patients with autoimmune diseases), eosinophilia.

From the urinary system: impaired renal function, proteinuria.

Others: alopecia, decreased libido, “hot flashes” of blood to the face. Hypoglycaemia has been reported in patients with diabetes mellitus who have taken insulin and oral hypoglycaemic drugs.

Interaction

Enhances the effect of ethanol, slows down the elimination of Li+.

Weakens the effect of drugs containing theophylline.

The antihypertensive effect is reduced by NSAIDs, including selective COX-2 inhibitors, estrogens; diuretics, other antihypertensive drugs (beta – blockers, methyldopa, nitrates, BMCC, hydralazine, prazosin), drugs for general anesthesia, ethanol are enhanced.

Potassium-sparing diuretics and potassium-containing drugs increase the risk of hyperkalemia. Drugs that cause bone marrow depression increase the risk of neutropenia and/or agranulocytosis.

When ACE inhibitors and gold preparations for parenteral use (sodium aurothiomalate) are used simultaneously, a symptom complex is described, including facial hyperemia, nausea, vomiting, and a decrease in blood pressure.

Concomitant use with insulin and oral hypoglycemic drugs increases the risk of hypoglycemia. Immunosuppressants, allopurinol, cytostatics increase hematotoxicity.

How to take, course of use and dosage

Assign inside regardless of the time of meal. In 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. If prescribed to patients receiving diuretics at the same time, treatment with diuretics should be discontinued 2-3 days before Enalapril is prescribed. If this is not possible, then the initial dose of the drug should be 2.5 mg / day. 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. 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 sessions. 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. 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: a marked decrease in blood pressure up to the development of collapse, myocardial infarction, acute cerebrovascular accident or thromboembolic complications, convulsions, stupor. Treatment: 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: intravenous use of saline solution, plasma substitutes, if necessary — use of angiotensin II, hemodialysis (the rate of elimination of enalaprilat on average is 62 ml/min).

Purpose

Angiotensin-converting enzyme inhibitor

Description

For tablets of 20 mg — round, biconvex tablets of white color with a risk on one side.

Functional features

After oral use,60% of the drug is absorbed.Food intake does not affect the absorption of enalapril. Enalapril binds up to 50% to blood proteins. Enalapril is rapidly metabolized in the liver to form the active metabolite enalaprilate, which is a more active ACE inhibitor than enalapril. The bioavailability of the drug is 40%. The maximum concentration of enalapril in blood plasma is reached in 1 hour, enalaprilat – in 3-4 hours. Enalaprilat easily passes through the histohematic barriers, excluding the blood-brain barrier, and a small amount passes through the placenta and into breast milk. The half-life of enalaprilat is about 11 hours. Enalapril is mainly excreted by the kidneys-60% (20% – in the form of enalapril and 40% – in the form of enalaprilat), through the intestine — 33% (6% — in the form of enalapril and 27% — in the form of enalaprilat). It is removed during hemodialysis (rate-62 ml / min) and peritoneal dialysis.

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. Transient 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. In the presence of renal insufficiency, a decrease in the excretion of the active metabolite may occur, leading to an increase in its concentration in blood plasma. Such 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. 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. At the beginning of treatment, until the end of the dose selection period, it is necessary to refrain from driving vehicles and engaging in potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions, as dizziness is possible, especially after the initial dose of an ACE inhibitor in patients taking diuretics. Before surgery (including dentistry), the surgeon/anesthesiologist should be warned about the use of ACE inhibitors.

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