Enalapril pills 10mg 20pcs

Composition

Enalapril 10 mg

Pharmacological action

Pharmacogroup:

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

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

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 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

Caution should be exercised when prescribing to patients with reduced BCC (as a result of diuretic therapy, when limiting 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 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.

With the development of an excessive decrease in blood pressure, the patient is transferred to a horizontal position with a low headboard, if necessary,0.9% NaCl solution and plasma-substituting drugs are administered.

The use of high-flow dialysis membranes (including AN69) increases the risk of anaphylactic reaction. Correction of the dosage regimen on days free from dialysis should be carried out depending on blood pressure.

Before and during treatment with ACE inhibitors, it is necessary to monitor blood pressure, blood parameters (Hb, K+ concentration, creatinine, urea, activity of “liver” enzymes), protein in the urine.

Patients with decompensated CHF, coronary artery 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).

In patients with indication of the development of angioedema in history have an increased risk of its development while receiving ACE inhibitors.

For newborns and children who were exposed in-utero to ACE inhibitors, it is recommended to conduct a careful monitoring for early detection of expressed lower AD, oliguria, hyperkalemia, and neurological disorders, possible due to reduced renal and cerebral blood flow with blood pressure decrease caused by ACE inhibitors. With oliguria, it is necessary to maintain blood pressure and renal perfusion by introducing appropriate fluids and vasoconstrictor drugs.

In patients with reduced renal function, the single dose should be reduced or the intervals between doses should be increased. Enalapril should be discontinued before testing the function of the parathyroid glands.

Caution should be exercised when exercising or in hot weather (risk of dehydration and excessive blood pressure reduction due to BCC reduction).

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

During the treatment period, care should be taken when driving vehicles and doing other activities. potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions (dizziness may occur, especially after taking the initial dose of an ACE inhibitor in patients taking diuretic drugs).

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