Active substanceEnalaprilEnalapril
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  • Dosage form: & nbsppills
    Composition:

    1 tablet contains:

    Active substance: enalapril maleate - 5 mg.

    Excipients: lactose monohydrate, gelatin, magnesium hydroxycarbonate, silicon dioxide colloid, sodium carboxymethyl starch, magnesium stearate
    Description:Round slightly biconvex tablets of almost white color with beveled edges and incision for division on one side.
    Pharmacotherapeutic group:Angiotensin-converting enzyme inhibitor
    ATX: & nbsp

    C.09.A.A.02   Enalapril

    Pharmacodynamics:

    Enalapril is an antihypertensive agent from the group of angiotensin-converting enzyme (ACE) inhibitors. Enalapril is about the drug: as a result of its hydrolysis is formed 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 (heart rate) is not noted.

    The antihypertensive effect is more pronounced with high renin activity of the blood plasma than at its normal or reduced level.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 long-term use, myocardial hypertrophy of the left ventricle and myocytes of the walls of arteries of resistive type decrease, prevents the progression of heart failure and slows down the development of dilatation of the left ventricle. Improves the blood supply of the ischemic myocardium.

    Has some diuretic effect.

    Time of onset of hypotensive effect with oral administration -1h, reaches a maximum after 4-6 hours and lasts up to 24 hours. In some patients, in order to achieve the optimal level of blood pressure, therapy is needed for several weeks. With heart failure, a significant clinical effect is observed with long-term treatment - 6 months or more
    Pharmacokinetics:

    After ingestion, 60% of the drug is absorbed. Eating does not affect the absorption of enalapril. Enalalryl is rapidly metabolized in the liver to form an active metabolite, enalaprilate. Connection with blood plasma proteins up to 60%.

    The maximum concentration of enalapril in the blood plasma is achieved after 1 hour, enalaprilata - 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 11h. Displayed enalapril mainly kidneys - 60 % (20% - in the form of enalapril and 40% - in the form of enalaprilata), through the intestine - 33 % (6% in the form of enalapril and 27% in the form of enalaprilate).

    Removed during hemodialysis (the rate of excretion of 62 ml / min) and peritoneal dialysis
    Indications:

    arterial hypertension (including renovascular hypertension); chronic heart failure (as part of combination therapy); prevention of the development of clinically significant heart failure in patients with asymptomatic dysfunction of the left ventricle (as part of combination therapy).

    Contraindications:

    Hypersensitivity to enalapril, other ACE inhibitors or drug components; presence in the anamnesis of an angioedema, associated with the treatment with ACE inhibitors; lactose intolerance, lactase deficiency,Glucose-galactose malabsorption, as well as hereditary or idiopathic angioedema; pregnancy; lactation period; age to 18 years (efficacy and safety not established).

    Carefully:

    Use for primary hyperaldosteronism, bilateral renal artery stenosis, stenosis of the artery to a solitary kidney, 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 greater than 1 g / d.), liver failure, patients a diet with restriction of salt or hemodialysis, while the use of immunosuppressants and saluretikami in the elderly (over 65 years), ENT otion of bone marrow hematopoiesis; Conditions accompanied by a decrease in the volume of circulating blood (BCC) (including diarrhea, vomiting).

    Pregnancy and lactation:

    The use of Berlipril® 5 during pregnancy is contraindicated.

    If pregnancy is confirmed, taking Berlipril® 5 should be stopped immediately.

    ACE inhibitors can cause disease or death of the fetus or newborn when used in pregnant women during the II and III trimesters of pregnancy. The use of ACE inhibitors during these periods was accompanied by a negative impact on the fetus and the newborn, including developed arterial hypotension, renal failure, hyperkalemia and / or hypoplasia of the skull bones in the newborn. Perhaps the development of oligohydramnion, apparently due to a decrease in the function of the kidneys of the fetus. This complication can lead to limb contracture, deformation of the bones of the skull, including its facial part, and lung hypoplasia. When using the drug Berlipril® 5, the patient should be informed of the potential risk to the fetus.

    These undesirable effects on the embryo and fetus do not appear to be the result of the intrauterine effect of ACE inhibitors during the first trimester of pregnancy.

    If it is not possible to cancel Berlipril® 5 during pregnancy,careful monitoring of the newborn is necessary to detect a decrease in blood pressure, oliguria and hyperkalemia.

    Enalapril, which penetrates the placenta, can be removed from the bloodstream of the newborn with peritoneal dialysis; in theory it can be removed by means of exchange blood transfusion.

    Enalapril and enalaprilate are excreted in breast milk in trace amounts, but their safety has not been studied. If you need to use the drug during lactation, breastfeeding should be discontinued.

    Dosing and Administration:

    Berlipril ® 5 is administered orally regardless of the time of ingestion.

    Arterial hypertension

    To ensure the following dosing regimen, it is possible to use enalapril in other dosages: 10 mg and 20 mg.

    The initial dose of the drug is from 5 mg to 20 mg once a day, depending on the severity of arterial hypertension. With mild hypertension, the recommended dose is 5-10 mg. At other degrees of severity of arterial hypertension, the initial dose is 20 mg once a day. The maintenance dose is 1 tablet 20 mg once a day.Dosage is selected individually for each patient, but should not exceed 40 mg per day.

    The maximum daily dose of the drug is 40 mg / day. once or twice. Renovascular hypertension

    Because in patients in this group, blood pressure and renal function may be particularly sensitive to ACE inhibition, therapy should begin with an initial dose of 5 mg per day or less. Then the dose is selected in accordance with the therapeutic response of the patient to the therapy. Usually effective dose is 20 mg per day with daily use.

    In the case of the drug Berlipril ® 5 y patients simultaneously receiving diuretics, treatment with a diuretic should be discontinued 2-3 days before the application of the drug Berlipril®5. If this is not possible, the initial dose of the drug should be 2.5 mg / day. (1/2 tablets of 5 mg each).

    In the case of hyponatremia (the content of sodium ions in the blood serum is less than 130 mmol / l) or the concentration of creatinine in the serum of more than 0.14 mmol / l, the initial dose is 2.5 mg (1/2 tablets 5 mg) once a day.

    The maximum daily dose is 20 mg.

    Chronic Renal Failure

    In chronic renal failure cumulation occurs with a decrease in filtration of less than 10 ml / min. When creatinine clearance (CC) is 80-30 ml / min, the dose is usually 5-10 mg / day, with QC up to 30-10 ml / min - 2.5-5 mg / day, with CC less than 10 ml / min - 1,25-2,5 mg / day. only during dialysis days (enalalil undergoes hemodialysis, dose adjustment on days when hemodialysis is not performed should be performed depending on blood pressure).

    Chronic heart failure and asymptomatic left ventricular dysfunction. In chronic heart failure, the initial dose is 2.5 mg (1/2 tablets of 5 mg) once, while the drug should be administered under close medical supervision to establish the primary effect of the drug on blood pressure. The drug can be used to treat heart failure with severe clinical manifestations, usually in conjunction with diuretics and, when necessary, cardiac glycosides. In the absence of symptomatic arterial hypotension (caused by therapy with Berlipril ® 5) or after appropriate correction, the dose should be gradually increased to the usual maintenance dose of 20 mg, which is applied either singly or divided into 2 divided doses depending on the patient's tolerability .The dose can be selected within 2-4 weeks or in shorter periods if there are residual signs and symptoms of heart failure.

    The duration of treatment depends on the effectiveness of therapy. With too pronounced decrease in blood pressure, the dose of the drug is gradually reduced.

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

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

    Side effects:

    The frequency is classified according to the headings, depending on the occurrence of the case: very often (> 1/10), often (<1 / 10-> 1/100), infrequently (<1 / 100-> 1/1000), rarely (<1 / 1000-> 1/10000), very rarely (<1/10000).

    Violations of the blood and lymphatic system: infrequently: Anemia (including aplastic and hemolytic anemia); rarely: neutropenia, a decrease in hemoglobin and hematocrit, thrombocytopenia, agranulocytosis, suppression of bone marrow function, pancytopenia, enlarged lymph nodes, autoimmune diseases.

    Disorders of metabolism and nutrition: infrequently - hypoglycemia.

    From the side of the central nervous system: often - headache, depression; infrequently - confusion, drowsiness, insomnia, increased excitability, paresthesia, dizziness; rarely - a change in the nature of dreams, sleep disturbances.

    From the side of the organ of vision: Often: violation of accommodation.

    From the side of the cardiovascular system: Often - dizziness; often - marked decrease in blood pressure, syncope, myocardial infarction or cerebral stroke, chest pain, heart rhythm disturbances, angina pectoris, tachycardia; infrequently: orthostatic hypotension, palpitation; rarely - Raynaud's syndrome.

    From the respiratory system: Often - cough; often - dyspnoea; infrequently: rhinorrhea, sore throat and hoarseness, bronchospasm / bronchial asthma; rarely- pulmonary infiltrates, rhinitis, allergic alveolitis / eosinophilic pneumonia.

    From the digestive system: Often - nausea; often - diarrhea, abdominal pain, change in taste perception; infrequently - intestinal obstruction, pancreatitis, vomiting, indigestion, constipation, lack of appetite, irritation of the stomach, dryness of the oral mucosa, peptic ulcer; rarely - stomatitis / aphthous ulcers, glossitis; rarely - angioedema of the intestine.

    From the liver and bile excretory system: rarely - hepatic insufficiency, hepatitis - hepatocellular or cholestatic, including hepatic necrosis, cholestasis (including jaundice).

    From the skin and subcutaneous fat: often - skin rash, hypersensitivity reactions / angioedema: reported angioedema with involvement of the face, limbs, lips, tongue, vocal folds and / or larynx; infrequently: increased sweating, itching, hives, alopecia; rarely - erythema multiforme, Stevens-Johnson syndrome, exfoliative dermatitis, toxic epidermal necrolysis, pemphigus, erythroderma.

    A symptom complex has been reported that may be accompanied by some and / or all of the following side effects: fever, serositis, vasculitis,

    myalgia / myositis, arthralgia / arthritis, an increase in the titer of antinuclear antibodies (ANA), an increase in the rate of erythrocyte sedimentation, eosinophilia, and leukocytosis. There may be a skin rash, photosensitivity or other skin manifestations.

    From the side of the urinary system, infrequently - impaired renal function, renal failure, proteinuria; rarely - oliguria.

    On the part of the reproductive system and mammary glands: infrequently - impotence; rarely - gynecomastia.

    Violations of a general nature: very often - asthenia; often - fatigue; infrequently - muscle cramps, redness of the skin of the face, tinnitus, discomfort, fever.

    Laboratory indicators often - hyperkalaemia, increased serum creatinine concentration; infrequently - increased serum urea concentration, hyponatremia; rarely - Increased activity of "liver" transaminases, hyperbillirubinemia.

    Overdose:

    Symptoms: marked decrease in blood pressure up to the development of collapse, myocardial infarction, acute impairment of cerebral circulation 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 shown, in more severe cases - measures aimed at stabilizing blood pressure: intravenous injection of physiological solution, plasma substitutes, if necessary - the introduction of angiotensin II, hemodialysis (the rate of excretion of enalaprilate is 62 ml / min).

    Interaction:

    With simultaneous use of enalapril with non-steroidal anti-inflammatory drugs (NSAIDs), including selective inhibitors of cyclooxygenase-2 (COX-2 inhibitors), the antihypertensive effect of ACE inhibitors, including enalalil or angiotensin II receptor antagonists, may be reduced.

    Simultaneous reception with potassium-sparing diuretics (spironolactone, triamterene, amiloride) can lead to hyperkalemia.

    A transient increase in serum lithium concentration and its toxic effects was reported while concomitant use with the preparation of Berlipril® 5. The simultaneous use of thiazide series diuretics and ACE inhibitors can lead to an increase in serum lithium concentration and thereby increase the risk of lithium intoxication. Therefore, the combined use of Berlipril® 5 and lithium preparations is not recommended; If this combination is necessary, careful monitoring of the concentration of lithium in the blood serum is necessary.

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

    Simultaneous use with antipyretic and analgesic agents can reduce the effectiveness of the drug.

    Enalapril weakens the effect of drugs containing theophylline.

    The antihypertensive effect of enalapril is enhanced by diuretics, beta-blockers, methyldopa, nitrates, blockers of "slow" calcium channels dihydropyridine series, hydralazine, prazozin.

    Immunosuppressants, allopurinol, cytotoxic drugs increase hematotoxicity. Drugs that cause bone marrow depression, increase the risk of developing neutropenia and / or agranulocytosis.

    The combined use of ACE inhibitors and hypoglycemic agents (insulin, hypoglycemic agents for oral administration) can enhance the hypoglycemic effect of the latter with the risk of developing hypoglycemia. This is most often observed during the first weeks of joint use, as well as in patients with renal insufficiency. In patients with diabetes mellitus receiving hypoglycemic agents for ingestion and insulin, blood glucose control is necessary, especially during the first month of joint use with ACE inhibitors.

    In rare cases, with the joint application of gold preparations for parenteral use (sodium aurotomy malate) and ACE inhibitors (enalapril) describes a symptom complex that includes reddening of the facial skin, nausea, vomiting and arterial hypotension.

    Special instructions:

    Caution should be exercised in appointing patients with reduced BCC (as a result of diuretic therapy, limiting intake of table 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 arterial hypotension is not a contraindication for continuing treatment with the drug after BP stabilization. In the case of a re-expressed decrease in blood pressure, you should reduce the dose or cancel the drug.

    The use of high-flow dialysis membranes increases the risk of developing an anaphylactic reaction. Before and during treatment with ACE inhibitors, periodic monitoring of blood pressure, blood counts (hemoglobin, potassium, creatinine, urea, activity of "liver" transaminases), protein in the urine is necessary.

    It should be carefully monitored for patients with severe chronic heart failure,ischemic heart disease and cerebrovascular diseases, in which a sharp decrease in blood pressure can lead to myocardial infarction, stroke, or renal dysfunction.

    During the period of treatment, it is not recommended to use alcoholic beverages. alcohol increases the hypotensive effect of the drug.

    Before surgery (including dentistry), it is necessary to alert the surgeon / anesthesiologist about the use of Berlipril® 5.

    Sudden abolition of treatment does not lead to the development of the syndrome of "withdrawal" (a sharp rise in blood pressure).

    Effect on the ability to drive transp. cf. and fur:Care must be taken when driving vehicles and practicing potentially dangerous activities that require increased concentration and speed of psychomotor reactions
    Form release / dosage:

    Tablets of 5 mg.

    Packaging:

    10 tablets per contour cell package (blister) made of laminated film (polyamide / aluminum / PVC) and aluminum foil.

    By 2, 3, 5 or 10 blisters together with instructions for use in a cardboard box.

    Storage conditions:

    Store at a temperature not exceeding 25 ° C.

    Keep the medicinal product out of the reach of children!

    Shelf life:

    Do not use after the expiration date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:П N012342 / 01
    Date of registration:01.03.2011
    The owner of the registration certificate:Berlin-Chemie / Menarini Pharma, GmbH Berlin-Chemie / Menarini Pharma, GmbH Germany
    Manufacturer: & nbsp
    Information update date: & nbsp21.10.2015
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