Enalapril pills 5mg 20pcs

Composition

1 tablet contains:

Active ingredient:

Enalapril maleate – 5 mg.

Excipients:

Microcrystalline cellulose-73 mg;

Pre-gelatinized corn starch-30 mg;

Talcum powder – 3 mg.

Colloidal silicon dioxide – 1 mg;

Magnesium stearate – 1 mg

Pharmacological action

of the pharmaceutical group:

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.

Pharmacokinetics:

After oral use, absorption is 60%. Food intake does not affect absorption. In the liver, it is metabolized to form the active metabolite enalaprilate, which is a more effective ACE inhibitor than enalapril. Binding to plasma proteins of enalaprilat is 50-60%. TCmax enalapril – 1 hour, enalaprilat – 3-4 hours.

Enalaprilat easily passes through the histohematic barriers, excluding the BBB, a small amount penetrates through the placenta and into breast milk.

T1 / 2 enalaprilat – 11 hours It 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.

Indications

• Arterial hypertension (symptomatic, renovascular, including scleroderma, etc. ), CHF I-III st. ;

• Prevention of coronary ischemia in patients with LV dysfunction, asymptomatic LV dysfunction.

Contraindications

• Hypersensitivity to enalapril or other ACE inhibitors;

• Pregnancy and lactation.

With caution:

• A history of angioedema associated with ACE inhibitor therapy, hereditary or idiopathic angioedema;

• Aortic stenosis;

• Cerebrovascular diseases (including cerebrovascular insufficiency);

• IHD;

• Coronary insufficiency;

• Severe autoimmune systemic connective tissue diseases (including SLE, scleroderma);

• Inhibition of bone marrow hematopoiesis;

• Diabetes mellitus;

• Hyperkalemia;

• Bilateral renal artery stenosis;

• Stenosis of the artery of a single kidney;

• Condition after kidney transplantation;

• Renal and / or hepatic insufficiency;

• Diet with Na+restriction;

• Conditions accompanied by a decrease in BCC (including diarrhea, vomiting),

• Elderly, under 18 years of age (safety and efficacy have not been studied).

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, erythema multiforme (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell’s syndrome), pemphigus (pemphigus), pruritus, urticaria, photosensitization, serositis, 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

When used concomitantly with immunosuppressants, cytostatics, the risk of developing leukopenia increases.

With the simultaneous use of potassium-sparing diuretics (including spironolactone, triamterene, amiloride), potassium preparations, salt substitutes and dietary supplements containing potassium, hyperkalemia may develop (especially in patients with impaired renal function), because ACE inhibitors reduce the content of aldosterone, which leads to potassium retention in the body against the background of limiting the excretion of potassium or its additional intake into the body.

With the simultaneous use of opioid analgesics and anesthesia, the antihypertensive effect of enalapril increases.

With the simultaneous use of “loop” diuretics, thiazide diuretics, the antihypertensive effect increases. There is a risk of hypokalemia. Increased risk of impaired renal function.

When used concomitantly with azathioprine, anemia may develop, which is due to inhibition of erythropoietin activity under the influence of ACE inhibitors and azathioprine.

A case of anaphylactic reaction and myocardial infarction with allopurinol in a patient receiving enalapril is described.

Acetylsalicylic acid in high doses may reduce the antihypertensive effect of enalapril.

It has not been definitively established whether acetylsalicylic acid reduces the therapeutic efficacy of ACE inhibitors in patients with CHD and heart failure. The nature of this interaction depends on the course of the disease.

Acetylsalicylic acid, by inhibiting COX and prostaglandin synthesis, can cause vasoconstriction, which leads to a decrease in cardiac output and a worsening of the condition of patients with heart failure receiving ACE inhibitors.

With the simultaneous use of beta-blockers, methyldopa, nitrates, calcium channel blockers, hydralazine, prazosin, it is possible to increase the antihypertensive effect.

When used concomitantly with NSAIDs (including indomethacin), the antihypertensive effect of enalapril decreases, apparently due to the inhibition of prostaglandin synthesis under the influence of NSAIDs (which are believed to play a role in the development of the antihypertensive effect of ACE inhibitors). There is an increased risk of developing impaired renal function; hyperkalemia is rarely observed.

With the simultaneous use of insulin, hypoglycemic agents and sulfonylureas, hypoglycemia may develop.

Concomitant use of ACE inhibitors and interleukin-3 increases the risk of hypotension.

Syncope has been reported with concomitant use with clozapine.

When used concomitantly with clomipramine, an increase in the effect of clomipramine and the development of toxic effects have been reported.

Hyperkalaemia has been reported with co-trimoxazole concomitantly.

When used concomitantly with lithium carbonate, the concentration of lithium in the blood serum increases, which is accompanied by symptoms of lithium intoxication.

When used concomitantly with orlistat, the antihypertensive effect of enalapril decreases, which can lead to a significant increase in blood pressure, the development of a hypertensive crisis.

It is believed that when used concomitantly with procainamide, the risk of developing leukopenia may increase.

When used concomitantly with enalapril, the effect of drugs containing theophylline decreases.

There are reports of acute renal failure in patients after kidney transplantation when used concomitantly with cyclosporine.

When used concomitantly with cimetidine, the T1/2 of enalapril increases and its concentration in blood plasma increases.

It is believed that it is possible to reduce the effectiveness of antihypertensive drugs when used simultaneously with erythropoietins.

Concomitant use with ethanol increases the risk of hypotension.

How to take, course of use and dosage

Inside, regardless of food intake.

For monotherapy of arterial hypertension, the initial dose is 5 mg once a day. In the absence of an 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 blood pressure stabilizes. If necessary and sufficiently well tolerated, the dose can be increased to 40 mg/day in 1-2 doses. After 2-3 weeks, they switch to a maintenance dose of 10-40 mg / day, divided into 1-2 doses. With moderate hypertension, the average daily dose is about 10 mg. The maximum daily dose of the drug is 40 mg. 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, the initial dose of enalapril should be 2.5 mg / day.

In patients with hyponatremia (serum Na+ 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.

Renovascular hypertension: the initial dose is 2.5-5 mg / day. The maximum daily dose is 20 mg.

In severe hypertension, intravenous use is possible (see Enalaprilat), which is performed only in a hospital setting.

With CHF, 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 blood pressure), but not higher than 40 mg/day, once, or in 2 doses. In patients with low systolic blood pressure (less than 110 mmHg), therapy should begin with a dose of 1.25 mg. Dose selection should be carried out within 2-4 weeks or in a shorter period of time. The average maintenance dose is 5-20 mg / day in 1-2 doses. In the elderly, a more pronounced hypotensive effect and prolongation of the drug’s action time are more often observed, 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 case of asymptomatic LV dysfunction-2.5 mg 2 times a day. The dose is adjusted for tolerability up to 20 mg / day, divided into 2 doses.

In CRF, 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, a creatinine clearance of 30-10 ml / min is 2.5-5 mg/day, and less than 10 ml / min is 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.

Overdose

Symptoms: excessive 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 serious cases-measures aimed at stabilizing blood pressure: intravenous use of 0.9% NaCl solution, plasma substitutes, if necessary – intravenous use of angiotensin II, hemodialysis (the rate of elimination of enalaprilat is 62 ml/min).

Special instructions

Use with extreme caution in patients with autoimmune diseases, diabetes mellitus, impaired liver function, severe aortic stenosis, subaortic muscle stenosis of unknown origin, hypertrophic cardiomyopathy, with loss of fluid and salts. Prior treatment with saluretics, in particular in patients with chronic heart failure, increases the risk of orthostatic hypotension, so before starting treatment with enalapril, it is necessary to compensate for the loss of fluid and salts.

With long-term treatment with enalapril, it is necessary to periodically monitor the picture of peripheral blood. Sudden discontinuation of enalapril does not cause a sharp increase in blood pressure.

During surgical interventions during treatment with enalapril, hypotension may develop, which should be corrected by the introduction of a sufficient amount of fluid.

Enalapril should be discontinued prior to parathyroid function testing.

Influence on the ability to drive motor vehicles and manage mechanisms

Caution is required when driving vehicles or performing other work that requires increased attention, as dizziness may occur, especially after taking the initial dose of enalapril.

Form of production

Pills.

Active ingredient

Enalapril

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults, For adults as prescribed by a doctor

Indications

Hypertension, Heart Failure