Enalapril - instructions for use, dose, side effects, contraindications

active substance: Enalapril Mapeat in terms of 100% of the substance - 10 mg Excipients: sugar milk (lactose) - 183.08 mg, potato starch - 17.62 mg, talc - 4.60 mg, calcium stearate - 2.20 mg, hydroxypropyl cellulose Klucel (giprolose) - 2.50 mg.

Description:Tablets of white with a yellowish hue of color of flat-cylindrical shape with a facet.

Pharmacotherapeutic group:Angiotensin-converting enzyme (ACE) inhibitor.

ATX: & nbsp

C.09.A.A.02 Enalapril

Pharmacodynamics:

Enalapril is an antihypertensive drug, the mechanism of its action is primarily associated with a decrease in the activity of angiotensin-converting enzyme (ACE), which leads to a decrease in the formation of angiotensin II, which causes the narrowing of blood vessels. At the same time, the formation of kinins and prostacyclin, which have a vasodilating action, is activated.

Enalapril refers to "prodrugs": after hydrolysis an active enalaprilate, which has this action. Enalapril has also a certain diuretic effect associated with moderate inhibition of aldosterone synthesis.

Along with a decrease in blood pressure, the drug reduces pre- and postnagruzku on the myocardium in heart failure,improves circulation in the small circle and the function of breathing, lowers the resistance in the vessels of the kidneys, which contributes to the normalization of renal circulation.

Pharmacokinetics:

After ingestion, 60% of the drug is absorbed. Eating does not affect the absorption of enalapril.

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

The maximum concentration of enalapril in the blood plasma is achieved after 1 hour, enalaprilata after 3-4 hours. Enalaprilat easily passes through the histohematological barriers, excluding the blood-brain barrier, a small amount penetrates the placenta and into the breast milk.

The half-life of enalaprilat is about 11 hours. Displayed enalapril mainly through the kidneys - 60% (20% - in the form of enalapril and 40% - in the form of enalaprilata), intestines - 33% (6% - enalapril and 27% - enalaprilata). It is removed during hemodialysis (rate 62 ml / min) and peritoneal dialysis.

Indications:

- arterial hypertension;

chronic heart failure (as part of combination therapy).

Contraindications:

- increased sensitivity to enalapril and other angiotensin converting enzyme (ACE) inhibitors;

- angioedema in history, associated with treatment with ACE inhibitors;

- pregnancy;

- lactation period;

- age to 18 years (efficacy and safety not studied).

Carefully:

Stenosis of the aortic or other obstructions to outflow of blood from the left ventricle of the heart; bilateral stenosis of the renal arteries, stenosis of the artery of a single kidney, condition after kidney transplantation, hyperkalemia, primary hyperaldosteronism; kidney failure; ischemic heart disease, cerebrovascular diseases, severe autoimmune diseases of connective tissue (including systemic lupus erythematosus, scleroderma), oppression of bone marrow hematopoiesis; liver failure; diabetes; diet with sodium restriction; conditions, accompanied by a decrease in the volume of circulating blood (including diarrhea, vomiting), porphyria.

Pregnancy and lactation:

A drug Enalapril contraindicated in pregnancy.If pregnancy occurs during the treatment with Enalapril, immediately discontinue the drug. If it is necessary to use Enalapril during lactation, breastfeeding should be stopped.

Dosing and Administration:

To fully ensure the following dosing regimen Enalapril It is possible to use this drug of the same manufacturer in other doses of 5 mg and 20 mg.

Enalapril is administered orally regardless of food intake.

With monotherapy of arterial hypertension, the initial dose of Enalapril is 5 mg 1 time per day. If there is no clinical effect, after 1-2 weeks the dose is increased by 5 mg. 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 a fairly good tolerability dose can be increased to 40 mg per day for 1-2 doses. After 2-3 weeks pass to maintaining a dose equal to 10-40 mg per 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.

In the case of enalapril administration to a patient taking diuretics at the same time, diuretic treatment should be stopped 2-3 days before enalapril is started. If this is not possible, the initial dose of the drug should be 2.5 mg per day.

Patients with hyponatremia (concentration of sodium ions in the blood serum of less than 130 mmol / l) or with an increase in serum creatinine concentration greater than 0.14 mmol / l are prescribed Enalapril in an initial dose of 2.5 mg once a day.

With Renovascular hypertension, the initial dose is 2.5-5 mg per day. The maximum daily dose is 20 mg.

In chronic heart failure, the initial dose of Enalapril is 2.5 mg once, then the dose is increased by 2.5-5 mg every 3-4 days according to the clinical response to the maximum tolerated dose, depending on the blood pressure, but not above 40 mg per day once or in 2 divided doses. In patients with low systolic blood pressure (less than 110 mm Hg), therapy should be started at a dose of 1.25 mg per day. Selection of the dose should be carried out within 2-4 weeks or if necessary and the opportunity in a shorter time.The average maintenance dose is 5-20 mg per day for 1-2 doses.

In elderly people, more pronounced hypotensive effect and lengthening of the action time of Enalapril are more likely, which is associated with a decrease in the rate of excretion of the drug, so the recommended initial dose for elderly patients is 1.25 mg.

In chronic renal failure cumulation of the drug occurs with a decrease in filtration less 10 ml / min. With the clearance of creatinine (CC) 80-30 ml / min dose of enalapril should be 5-10 mg per day, with a decrease in QC up to 30-10 ml / min - 2,5-5 mg per day, less than 10 ml / min -1,25-2,5 mg per day only in days Dialysis The duration of treatment depends on the effectiveness of therapy. When the blood pressure is too marked, the dose of Enalapril is gradually reduced.

The drug is used in both monotherapy and in combination with other antihypertensive agents.

Side effects:

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

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

From the sense organs: disturbances of the vestibular apparatus, hearing and vision impairment, tinnitus.

From the side of the digestive tract: dry mouth, decline appetite, dyspeptic disorders (nausea, diarrhea or constipation, vomiting, abdominal pain), intestinal obstruction, pancreatitis, impaired liver function and biliary tractleading ways, hepatitis, jaundice.

From the respiratory system: unproductive "dry" cough, interstitial pneumonitis, bronchospasm, dyspnea, rhinorrhea, pharyngitis.

Allergic reactions: skin rash, angioedema, facial edema, extremities, lips, tongue, glottis and / or throat, dysphonia, polymorphic exudative erythema (including Stevens-Johnson syndrome), exfoliative dermatitis, toxic epidermal necrolysis (Lyell's syndrome), pemphigus (pemphigus) , itching, hives, photosensitivity, serositis, vasculitis, myositis, arthralgia, arthritis, stomatitis, glossitis.

From the laboratory indicators: hypercreatininaemia, increased urea levels, increased activity of "hepatic" transaminases, hyperbilirubinemia, hyperkalemia, hyponatremia. In some cases there is a decrease in hematocrit and hemoglobin content, increased ESR, thrombocytopenia, neutropenia, agranulocytosis (in patients with autoimmune diseases), eosinophilia.

From the urinary system: a violation of kidney function, proteinuria. Other: alopecia, decreased libido, "hot flashes".

Overdose:

Symptoms: marked reduction in blood pressure until the development of collapse, myocardial infarction, acute cerebrovascular accident or thromboembolic complications, convulsions, stupor.

Treatment: patient is transferred to a horizontal position with a low headboard. In mild cases, gastric lavage and ingestion of saline are indicated. In more severe cases, measures aimed at stabilizing blood pressure are recommended: intravenous injection of physiological solution, plasma substitutes, and if necessary - angiotensin II, hemodialysis (the rate of excretion of enalaprilate is 62 ml / min).

Interaction:

Reduction of the hypotensive effect of Enalapril with simultaneous administration with non-steroidal anti-inflammatory drugs (NSAIDs). Use of the drug in conjunction with potassium-sparing diuretics (spironolactone, triamterene, amiloride) can lead to hyperkalemia, with lithium salts - to slow down lithium removal (control of lithium concentration in blood plasma is shown).

Enalapril weakens the effect of drugs containing theophylline.

The hypotensive effect of Enalapril is enhanced by diuretics, beta-blockers, methyldopa, nitrates, blockers of "slow" calcium channels, hydralazine, prazozin, ethanol.

Immunosuppressants, allopurinol, cytostatics that cause bone marrow suppression, increase the risk of developing neutropenia and / or agranulocytosis up to a fatal outcome.

Special instructions:

Care should be taken when prescribing patients with reduced circulating blood volume (as a result of diuretic therapy, limiting intake of salt, hemodialysis, diarrhea and vomiting) - the risk of a sudden and pronounced decrease in blood pressure after applying even an initial dose of an ACE inhibitor is increased.Transient hypotension is not a contraindication for continuing treatment with the drug after stabilizing blood pressure. In the case of a repeated decrease in arterial pressure should reduce the dose or cancel the drug.

With the development of excessive reduction in blood pressure, the patient is transferred to a horizontal position with a low headboard, if necessary, physiological saline and plasma-substituting drugs are administered.

The use of high-flow dialysis membranes increases the risk of developing an anaphylactic reaction. Correction of the dosing regimen on days free from dialysis should be carried out depending on the level of arterial pressure.

Before and after treatment with ACE inhibitors, control of blood pressure, blood counts (hemoglobin, potassium, creatinine, urea, activity of "liver" enzymes), protein in the urine is necessary.

It should be carefully monitored for patients with severe heart failure, coronary heart disease and cerebrovascular diseases, in which a sharp drop in blood pressure can lead to myocardial infarction, stroke, or renal dysfunction.Sudden withdrawal of treatment does not lead to the syndrome of "withdrawal" (a sharp rise in blood pressure).

Patients with an indication of angioedema development in the anamnesis have an increased risk of developing edema with ACE inhibitors.

For newborns and infants who have been exposed to the intrauterine effect of ACE inhibitors, careful monitoring is recommended to detect the pronounced decrease in arterial pressure, oliguria, hyperkalemia and neurological disorders that are possible due to a decrease in renal and cerebral blood flow while lowering the arterial pressure caused by ACE inhibitors. In oliguria, maintenance of arterial pressure and renal perfusion is necessary by the introduction of appropriate fluids and vasoconstrictors.

In patients with reduced renal function, a single dose should be reduced or intervals between doses should be increased.

Before the study of the function of the parathyroid glands Enalalryl should be discarded.

During the period of treatment it is not recommended to drink alcoholic beverages, since alcohol enhances the hypotensive effect of the drug.

During the treatment period it is necessary to refrain from driving motor vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions, since dizziness is possible, especially after the initial dose of an ACE inhibitor in patients taking diuretic drugs

Care should be taken when performing physical exercises or hot weather (the risk of dehydration and excessive decrease in blood pressure due to a decrease in the volume of circulating blood).

Before surgery (including dentistry), it is necessary to alert the surgeon and anesthesiologist about the use of ACE inhibitors.

Form release / dosage:

Tablets 10 mg.

Packaging:

For 10 tablets in a planar cell packaging made of polyvinylchloride film and aluminum foil printed lacquered. 2 contour squares with instructions for use in a pack of cardboard.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 of the year.

He Use at the expiration date indicated on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N000742 / 01

Date of registration:28.10.2011

The owner of the registration certificate:VALENTA PHARM, PAO VALENTA PHARM, PAO Russia

Manufacturer: & nbsp

VALENTA PHARMACEUTICS, JSC Russia

Information update date: & nbsp19.10.2015

Illustrated instructions

Instructions

Enalapril (Enalapril)