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

1 tablet contains the active substance: enalapril maleate - 10 mg; auxiliary substances: lactose monohydrate (sugar milk) - 116.2 mg, corn starch - 25.8 mg, talc (magnesium hydrosilicate) - 3.2 mg, silicon dioxide colloid (aerosil) - 3.2 mg, magnesium stearate - 1 , 6 mg.

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

Pharmacotherapeutic group:inhibitor of angiotensin-converting enzyme (ACE).

ATX: & nbsp

C.09.A.A.02 Enalapril

Pharmacodynamics:

Enalapril is an antihypertensive drug whose mechanism of action is associated with inhibition of the activity of the angiotensin converting enzyme, leading to a decrease in the formation of angiotensin-P.

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

Expands arteries more than veins, with a reflex increase in heart rate is not noted.

The hypotensive effect is more pronounced with a high plasma renin level than at a normal or reduced level of plasma.Decrease in blood pressure within the therapeutic limits does not affect cerebral circulation, blood flow in the vessels of the brain is maintained at a sufficient level and against a background of low blood pressure. Strengthens coronary and renal blood flow.

With prolonged use, hypertrophy of the left ventricle of the myocardium and myocytes of the walls of arteries of the resistive type decreases, prevents the progression of the cardiac deficiency and slows the development of dilatation of the left ventricle. Improves blood supply of ischemic myocardium. Reduces the aggregation of platelets.

Has some diuretic effect.

The time of the onset of an antihypertensive effect with ingestion is 1h, reaches a maximum after 4-6 hours and lasts up to 24 hours. Some patients need therapy for several weeks to achieve the optimal level of blood pressure. With heart failure, a noticeable clinical effect is observed with prolonged use - 6 months or more.

Pharmacokinetics:

After ingestion, about 60% of enalapril is absorbed. Eating does not affect absorption. In the liver it is metabolized with the formation of the active metabolite enalaprilata, which is a more active ACE inhibitor than enalapril. The connection with the proteins of the blood plasma enalaprilata - 50 - 60%. The maximum concentration of enalaprilat in the blood serum is observed after 3-4 hours, enalapril after 1 hour. Stable concentrations in blood serum - after 4 days. Enalaprilat easily passes through the histohematological barriers, excluding the blood-brain barrier, a small amount penetrates through the placenta and into breast milk.

The half-life of enalaprilat is 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 enalaprilata).

It is removed during hemodialysis (rate 62 ml / min) and peritoneal dialysis.

Indications:

The drug is used in the treatment of arterial hypertension, chronic heart failure and asymptomatic left ventricular dysfunction (as part of a combination therapy).

Contraindications:

Hypersensitivity to enalapril, other components of the drug or other ACE inhibitors, pregnancy, lactation period, porphyria.

The drug should not be used in patients with angioedema in a history associated with the previous use of ACE inhibitors (an allergic reaction with a sharp swelling of the lips, face, neck and, possibly, hands and feet,accompanied by choking and hoarseness), patients who have ever observed angioedema, age 18 years (effectiveness and safety have been established).

Carefully:

Enalapril should be used with caution in patients with bilateral renal artery stenosis or stenosis of the artery to a solitary kidney.

Be wary of primary hyperaldosteronism, hyperkalemia, condition after kidney transplantation; aortic stenosis, mitral stenosis (with impaired hemodynamics), idiopathic hypertrophic subaortic stenosis, systemic connective tissue diseases, ischemic heart diseases, cerebrovascular diseases, diabetes, renal disease (proteinuria - more than 1 g / day), liver failure, patients complying diet with restriction of salt or hemodialysis, while admission to immunosuppressants and saluretikami in the elderly (over 65 years), inhibition of bone marrow to ovetvoreniya, state, accompanied by a decrease in blood volume (including diarrhea, vomiting).

Pregnancy and lactation:

During pregnancy and lactation it is not possible to prescribe a drug. If pregnancy occurs during the treatment with Enalapril, tell your doctor as soon as possible. He will prescribe another antihypertensive treatment.

Dosing and Administration:

Tablets should be swallowed whole, washed down with a small amount of liquid. Tablets can be taken before, during or after a meal. You should get used to taking the drug regularly and at the same time. If the patient misses the drug, it should be taken as soon as possible, but not if the dose remains several hours before the next dose is taken. In this case, you should only take the next dose and not take the missed dose. Doses should never be doubled. Treatment with Enalapril requires regular medical examinations, especially at the beginning of treatment and / or when determining the most appropriate dose of the drug. The frequency of medical examinations is determined by the attending physician.

The dose of the drug is always adjusted depending on the patient's condition.

Treatment of arterial hypertension: the recommended initial dose is 5 mg once a day.After taking the initial dose, patients should be under medical supervision for 2 hours and an additional 1 hour until the blood pressure stabilizes. Correction of the dose depends on the achievement of therapeutic effect (lowering blood pressure) and in the absence of a clinical effect increase after 1-2 weeks by 5 mg. Usually the maintenance dose is from 10 to 20 mg, if necessary and with a fairly good tolerability, the dose can be increased to 40 mg per day.

The maximum daily dose is 40 mg.

At higher doses, separation into 2 divided doses is advisable.

The initial dose for patients who could not interrupt the use of diuretics before the start of Enalapril treatment is 2.5 mg as a single dose.

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

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

Treatment of chronic heart failure: the recommended initial dose is 2.5 mg once daily. The dose of Enalapril should be increased gradually until the maximum clinical effect is achieved, usually after 2-4 weeks. The usual maintenance dose is 2.5 mg to 10 mg as a single dose; the maximum maintenance dose is 20 mg twice a day.

Treatment of asymptomatic left ventricular dysfunction: the recommended initial dose is 2.5 mg twice daily; some dosage adjustment depends on the tolerance of the drug to the patient. Usually the maintenance dose is 10 mg twice a day.

Treatment of arterial hypertension in diseases of the kidneys: dose of enalapril is determined depending on renal function and / or clearance parameters of creatinine. For patients with creatinine clearance greater than 0.5 ml / s (30 ml / min.), The initial dose is 5 mg per day; for patients with creatinine clearance less than 0.5 ml / s (30 ml / min) the initial dose is 2.5 mg per day and gradually increases to achieve a clinical effect.

Patients on hemodialysis: for patients on the day of hemodialysis 2.5 mg; the rest of the days the doctor adjusts the dose in accordance with the indices of blood pressure.

Treatment with Enalapril - for a long time, usually throughout life, if circumstances do not arise that require its cancellation.

Side effects:

The side effects observed during the treatment with Enalapril are usually mild, transient and do not require drug withdrawal:

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

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

From the sense organs: violation of the vestibular apparatus, hearing and vision impairment, 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, interstitial pneumonitis, bronchospasm / asthma, dyspnea, rhinorrhea, pharyngitis, sore throat, hoarseness.

Allergic reactions: skin rash, angioedema, swelling of the face, extremities, lips, tongue, glottis and / or larynx, dysphonia, polymorphic erythema, exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis, pemphigus, pruritus, urticaria, photosensitivity, serositis, vasculitis, myositis, arthralgia, arthritis, stomatitis, glossitis, increased sweating.

From the laboratory indicators: hypercreatininemia, increased urea levels, increased activity of "hepatic" transaminases, hyperbilirubinemia, hyperkalemia, hyponatremia, decreased hemoglobin and hematocrit concentration, increased erythrocyte sedimentation rate (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, decreased potency.

A complex symptom complex has been reported that may include all or some of the following symptoms: fever, serositis, vasculitis, myalgia / myositis, arthralgia / arthritis, positive antinuclear antibody test, increased ESR, eosinophilia and leukocytosis.

If the patient notes or suspects the presence of side effects associated with the use of the drug, he should inform the doctor about it.

Overdose:

If the patient has taken too many tablets at one time, the doctor should be called immediately.

Symptoms of overdose: excessive reduction in blood pressure up to the development of collapse, myocardial infarction, acute disorders of cerebral circulation or thromboembolic complications, convulsions, stupor.

Treatment: the patient is transferred to a horizontal position with a low headboard.

In mild cases shown gastric lavage and intake of brine, in more severe cases - measures aimed at stabilizing the blood pressure, in / in a physiological saline solution, plasma expanders, if necessary - in / administration of angiotensin II, hemodialysis (elimination rate enalaprilat - 62 ml / min).

Interaction:

The patient should refrain from taking alcoholic beverages, because ethanol increases the decrease in blood pressure with enalapril.

Simultaneous use of enalapril and diuretics or other antihypertensive drugs increases the effectiveness of these drugs. Interaction with drugs used to treat heart failure (cardiac glycosides) has no clinical significance.

Before surgery, tell the doctor that the patient is taking enalapril, since there is a risk of developing arterial hypotension in general anesthesia.

Simultaneous use of enalapril and non-steroidal anti-inflammatory drugs or acetylsalicylic acid (aspirin) can reduce the effectiveness of enalapril and increase the risk of impaired renal function.

Simultaneous use of certain diuretics (spironolactone, amiloride or triamterene) and / or the addition of tablets containing potassium may cause an increase in potassium levels in the blood serum (hyperkalemia). Enalapril weakens the effect of funds containing theophylline. Simultaneous use of lithium drugs can enhance the side effect of lithium.

Preparations containing cimetidine, prolong the action of enalapril. If the patient is already taking the above drugs or is advised to take any of them, he should tell the doctor that he is taking Enalapril.

Drugs that cause bone marrow depression increase: the risk of developing neutropenia and / or agranulocytosis.

Immunosuppressants, allopurinol, cytotoxic drugs increase hematoxicity.

Special instructions:

Arterial hypotension (a sharp decrease in blood pressure) can be observed (even a few hours after the first dose) in patients with severe heart failure or severe renal dysfunction, as well as in patients with water-electrolyte balance disorders caused by treatment with diuretics, salt-free diet, diarrhea, vomiting, or on hemodialysis. The pronounced decrease in blood pressure is usually manifested in the form of nausea, frequent heart rate (heart rate) and fainting. In the case of development of arterial hypotension, the patient should take a horizontal position, with a low head and call a doctor.Arterial hypotension and its severe consequences are rare and transient. Transient arterial hypotension is not a contraindication to further treatment with the drug. Once BP is stabilized, the patient normally tolerates the administration of subsequent doses of the drug. Arterial hypotension can be avoided by interrupting treatment with diuretics and refusing a salt-free diet before starting treatment with Enalapril, if possible. If

relapses of arterial hypotension occur, accompanied by such symptoms as nausea, frequent heart rate and fainting, you should consult a doctor. It is necessary to monitor the function of the kidneys before treatment and during the treatment of Enalapril.

During the treatment with Enalapril, potassium levels in the blood serum may be raised, especially in patients with chronic renal failure, diabetes mellitus, while prescribing potassium-sparing diuretics (such as spironolactone, amiloride and triamterene) or tablets containing potassium. Therefore, while taking Enalapril and these drugs, you should strictly follow the doctor's instructions.If the patient experiences muscle weakness or irregular heartbeat during this treatment, tell the doctor immediately.

Allergic reactions can develop due to the use of certain types of filter membranes used for hemodialysis or other types of blood filtration (apheresis). If the doctor plans such treatment, it should be warned about the simultaneous treatment with Enalapril.

During the treatment of allergies (desensitization) to aspen or bee venom, hypersensitivity reactions may occur.

If the doctor plans such treatment, it should be warned about the simultaneous treatment with Enalapril.

Before the study of parathyroid function Enalapril should be canceled. Caution should be exercised when performing physical exercises or in hot weather (risk of dehydration and excessive blood pressure lowering due to decreased circulating blood volume).

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

The effectiveness and safety of the drug in the treatment of children is not established, so it should not be prescribed to children.

Effect on the ability to drive transp. cf. and fur:

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased concentration and speed of psychomotor reactions (possibly dizziness, especially after taking the initial dose of an ACE inhibitor in patients taking diuretic medicines).

Form release / dosage:

Tablets 10 mg.

Packaging:For 10 tablets in a planar cell package. For 2, 3, 5 contour packs together with the instruction for use are placed in a pack of cardboard

Storage conditions:

In the dark place at a temperature ofnot higher than 25 ° C. Keep out of the reach of children.

Shelf life:

2 years.

The drug should not be used after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N000706 / 01

Date of registration:20.03.2008

The owner of the registration certificate:ORGANICS, JSC ORGANICS, JSC Russia

Manufacturer: & nbsp

ORGANICS, JSC Russia

Information update date: & nbsp23.10.2015

Illustrated instructions

Instructions

Enalapril (Enalapril)