Enalapril-FPO, pills 10mg 20pcs

Composition

1 tablet contains the Active ingredient-enalapril maleate 5 mg,10 mg.

Auxiliary substances:

corn starch,

lactose (milk sugar),

microcrystalline cellulose,

colloidal silicon dioxide (aerosil A-300),

calcium stearate.

Pharmacological action

Pharmacotherapy group:

Angiotensin converting enzyme (ACE)

Inhibitor Pharmacodynamics :

 Enalapril is an antihypertensive drug from the group of ACE inhibitors. Enalapril is a “prodrug”: as a result of its hydrolysis, enalaprilate is formed, which inhibits ACE. The mechanism of its action is associated with a decrease in the formation of angiotensin II from angiotensin I, a decrease in the content of which leads to a direct decrease in the release of aldosterone. This reduces the total peripheral vascular resistance, systolic and diastolic blood pressure( BP), post-and preload on the myocardium.

Dilates the arteries to a greater extent than the veins, while there is no reflex increase in heart rate.

The hypotensive effect is more pronounced with a high level of plasma renin than with a normal or reduced level. 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.

With prolonged use, hypertrophy of the left ventricle of the myocardium and myocytes of the walls of resistive arteries decreases, prevents the progression of heart failure and slows down the development of left ventricular dilation. Improves blood supply to the ischemic myocardium. Reduces platelet aggregation.

It has some diuretic effect.

The time of onset of the hypotensive effect when taken orally is 1 hour, 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 heart failure, a noticeable clinical effect is observed with long-term treatment-6 months or more.

Pharmacokinetics:

After oral use,60% of the drug is absorbed. Food intake does not affect the absorption of enalapril.

Enalapril binds up to 50% to plasma proteins. Enalapril is rapidly metabolized in the liver to form the active metabolite enalaprilate, which is a more active ACE inhibitor than enalapril. Bioavailability of the drug is 40%.

The maximum concentration of enalapril in blood plasma is reached after 1 hour, enalaprilat-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.

Indications

-arterial hypertension;

– 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, as well as hereditary or idiopathic angioedema, pregnancy, lactation, age up to 18 years (efficacy and safety have not been established).

Use with caution in primary hyperaldosteronism, bilateral renal artery stenosis, single kidney artery stenosis, hyperkalemia, post-kidney transplantation condition; 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/min). day), liver failure, in patients who follow a diet with salt restriction or are on hemodialysis, while taking immunosuppressants and saluretics, in the elderly (older than 65 years), suppression of bone marrow hematopoiesis; conditions accompanied by a decrease in the volume of circulating blood (including diarrhea, vomiting).

Side effects

Enalapril-FPO® is generally well tolerated and in most cases does not cause side effects that require discontinuation of the drug.

From the cardiovascular system: excessive decrease in blood pressure, orthostatic collapse, rarely-chest pain, angina pectoris, myocardial infarction or stroke (usually associated with a pronounced decrease in blood pressure), extremely rare arrhythmias (atrial brady or tachycardia, atrial fibrillation), palpitations, pulmonary embolism, Raynaud’s syndrome.

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

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

From the digestive system: dry mouth, anorexia, dyspeptic disorders (nausea, diarrhea or constipation, vomiting, abdominal pain), intestinal obstruction, pancreatitis, liver and biliary dysfunction, hepatitis (hepatocellular or cholestatic), jaundice.

From the respiratory system: unproductive dry cough, sore throat, hoarseness of voice, pulmonary infiltrates, interstitial pneumonitis, bronchospasm, shortness of breath, rhinorrhea, pharyngitis.

Allergic reactions: skin rash, pruritus, urticaria, angioedema, extremely rare dysphonia, erythema multiforme, exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis, pemphigus, photosensitization, serositis, vasculitis, myositis, arthralgia, arthritis, stomatitis, glossitis, intestinal edema (very rare).

From the laboratory parameters: hypercreatininemia, increased urea content, increased activity of “liver” enzymes, hyperbilirubinemia, hyperkalemia, hyponatremia, hypoglycemia in patients suffering from diabetes mellitus, receiving hypoglycemic agents for oral use or insulin. In some cases, a decrease in the concentration of hemoglobin and hematocrit, an increase in ESR, thrombocytopenia, neutropenia, agranulocytosis (in patients with autoimmune diseases), and eosinophilia are noted.

From the urinary system: impaired renal function, rarely proteinuria.

Others: alopecia, decreased libido, impotence, hot flashes.

Interaction

Concomitant use of enalapril with nonsteroidal anti-inflammatory drugs (NSAIDs), including selective cyclooxygenase-2 inhibitors (COX-2 inhibitors) may reduce the hypotensive effect of enalapril; with potassium-sparing diuretics (spironolactone, triamterene, amiloride) may lead to hyperkalemia; with lithium salts-to slow the excretion of lithium (monitoring of lithium concentration in blood plasma is indicated).

In some patients with impaired renal function and taking NSAIDs, including COX-2 inhibitors, concomitant use of ACE inhibitors may lead to further deterioration of renal function. These changes are reversible.

Concomitant use with antipyretics and painkillers may reduce the effectiveness of the drug.

Enalapril weakens the effect of drugs containing theophylline.

The hypotensive effect of enalapril is enhanced by diuretics, beta-blockers, methyldopa, nitrates, dihydropyridine slow calcium channel blockers, hydralazine, and prazosin.

Immunosuppressants, allopurinol, cytostatics increase hematotoxicity. Drugs that cause bone marrow suppression increase the risk of neutropenia and / or agranulocytosis.

The combined use of ACE inhibitors and hypoglycemic agents (insulin, hypoglycemic agents for oral use) may increase the hypoglycemic effect of the latter with the risk of hypoglycemia. This is most often observed during the first weeks of co-use, as well as in patients with renal insufficiency. In patients with diabetes mellitus receiving oral hypoglycemic agents and insulin, blood glucose monitoring is necessary, especially during the first month of co-use with ACE inhibitors.

ACE inhibitors reduce the excretion of lithium by the kidneys, and increase the risk of lithium intoxication. If it is necessary to prescribe lithium salts, it is necessary to monitor the level of lithium in the blood serum.

A symptom complex that includes facial flushing, nausea, vomiting, and hypotension has been described in rare cases with the combined use of parenteral gold preparations (sodium aurothiomalate) and ACE inhibitors (enalapril).

How to take it, course of use and dosage

Assign inside regardless of the time of meal. To ensure the following dosage regimen, enalapril may be used at a dose of 2.5 mg.

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 steps. 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 concomitant diuretics, diuretic treatment should be discontinued 2-3 days before Enalapril-FPO®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 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. 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 patients often have a more pronounced hypotensive 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 is 62 ml/min).

Special instructions

Caution should be exercised when prescribing 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 stabilization of blood pressure (BP). In case of repeated pronounced decrease in blood pressure, the dose should be reduced or the drug should be discontinued.

The use of high-strength 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 chronic 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 the development of “rebound” 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 occur due to 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.

Before examining the functions of the parathyroid glands, it should be canceled.

Alcohol increases the hypotensive effect of the drug.

At the beginning of treatment, until the end of the dose adjustment period, it is necessary to refrain from driving vehicles and engaging in potentially dangerous activities that require increased concentration and speed of psychomotor reactions, since 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.

Form of production

Tablets are white or white with a yellowish tinge of color, flat-cylindrical, with a chamfer.

Storage conditions

At a temperature not exceeding 25 °C, keep out of the reach of children!

Shelf

life is 3 years.

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