The instruction for medical use of medicine
the Trade name Enalapril
the International unlicensed
name Enalapril Dosage Form of the Tablet of 5 mg and 10 mg
of SostavOdn a tablet soderzhitaktivny substance – enalapril a maleate of 5 mg or 10 mg, excipients: lactoses monohydrate, povidone, potato starch, talc, magnesium stearate.
OpisanieTabletki color, white with a yellowish shade, ploskotsilindrichesky, with a facet
Pharmacotherapeutic the gruppapreparata influencing a system renin-angiotensin. Angiotensin — the Converting Enzyme (ACE) inhibitors. AKF inhibitors. EnalaprilKod ATKH S09aa02
Pharmacological to a svoystvaPharmakodinamikaPosla of intake is absorbed about 60% of drug, food does not influence enalapril absorption. After reception in a dose of 10 mg time of achievement of the maximum concentration in blood plasma – 1 h, and its level – 200-400 ng/ml. After absorption is exposed to presistemny metabolism in a liver with formation of active enalaprilat. Enalaprilat easily passes through gistogematichesky barriers (excepting a blood-brain barrier), gets through a placenta and it is found in fruit fabrics. The period of semi-elimination of enalapril is 2 h. After use in a dose of 20 mg the maximum concentration of enalaprilat in blood plasma makes 70-100 ng/ml and is reached in 3-4 h. Therapeutic concentration of enalaprilat in blood plasma makes 10-100 ng/ml. Contacts proteins of plasma for 50%. Elimination half-life of enalaprilat makes 8-11 h Eliminiruyetsya with urine of 60% of the accepted dose (20% in the form of enalapril and 40% in the form of enalaprilat) and through intestines – 33% (6% in the form of enalapril and 27% in the form of enalaprilat). During 24 h about 90% of the accepted dose eliminirutsya. In heavy chronic kidney disease (clearance of creatine less than 30 ml/min.) elimination of enalaprilat slows down, and its level increases in plasma by 13 times, cumulation of drug arises at clearance of creatine less than 10 ml/min. Is removed at a hemodialysis and peritoneal dialysis. PharmakodinamikaEnalapril has hypotensive, vasodilating and cardioprotective effect. Enalapril inhibits activity of angiotensin-converting enzyme (APF). As a result education angiotensin II decreases, secretion of Aldosteronum is stimulated. Interferes with disintegration of bradykinin and strengthens its vasodilating action on bradikininovy receptors of B2 type. As a result of use of enalapril in blood plasma the level of vasoconstrictive hormones decreases, the level of bradykinin, E2 prostaglandin and prostacyclin, the endothelial relaxing factor and atrial natriuretic peptide increases. Enalapril causes expansion of arterial vessels and reduces arterial blood pressure. At administration of enalapril the hypotensive effect develops in 1 h after reception, reaches a maximum to 6 h and about 24 h remain. At persons with an excess weight for achievement of the optimum AD stable level the intake of enalapril within several weeks can be required. Enalapril slows down development of a hypertrophy and fibrosis of a wall of arterial vessels. Thanks to vasodilating action, enalapril reduces the general peripheric resistance of vessels (an afterload by a myocardium), jamming pressure in pulmonary capillaries (preload of a myocardium), resistance in pulmonary vessels, increases warm emission. At prolonged use reduces expressiveness of a hypertrophy of a myocardium, prevents progressing of heart failure and slows down development of dilatation of a left ventricle (cardioprotective action).
Indications – arterial hypertension – chronic heart failure (as a part of combination therapy) – dysfunction of a left ventricle after the postponed myocardial infarction – asymptomatic dysfunction of a left ventricle
Apply the Route of administration and doses inside irrespective of meal. At patients with high activity system renin-angiotensin-aldosteronovoy (for example, renovascular hypertensia, deficiency of salts and/or dehydration, a decompensation of warm activity or a severe form of arterial hypertension) can be observed a sharp lowering of arterial pressure after reception of the first dose. In this connection, the first dose is accepted better before going to bed in a prone position. In arterial hypertension the adult appoint in an initial dose 5 mg once a day. In the absence of effect in 1-2 weeks the dose is increased by 5 mg. At good tolerance the dose can be increased up to 20 mg/days in 1 reception. In 2-3 weeks after intake of enalapril in the maximum dose pass to maintenance therapy in a dose 10 – 20 mg/days. The maximum daily maintenance dose of enalapril makes 40 mg/days (in 2 receptions). In case of use of diuretics, treatment by diuretics should be stopped in 2-3 days prior to prescribing of enalapril, or to begin intake of enalapril with a dose of 2.5 mg/days, slowly increasing a dose by 2.5 mg/week before achievement of optimum effect. At concentration of Na + in blood serum less than 130 mmol/l or creatinine level in blood serum more than 0.14 mmol/l an initial dose of enalapril – 2.5 mg/days. In renovascular and renal hypertensia the initial dose of 2.5-5 mg once a day supporting – 10 mg of 1 times a day. The maximum daily dose of 20 mg in 2 receptions. In chronic heart failure an initial dose of 2.5 mg once with gradual increase on 2.5-5 mg each 3-4 days to the most transferable (depending on the ABP level), but no more than 20 mg/days. Average maintenance dose of 5-20 mg/days. The next increase in a dose carry out more than 90 mm Hg at stable maintaining systolic arterial blood pressure. At patients with low systolic pressure (less than 110 mm Hg.) and also at elderly treatment begin 1.25 mg/days with a dose. At asymptomatic dysfunction of a left ventricle apply 2.5 mg 2 times a day. The dose is increased by 2.5 mg every week to optimum transferable, but by no more than 20 mg/days in 2 receptions. At patients with a renal failure the initial dose of enalapril at the clearance of creatinine (CC) of 80-30 ml/min. makes 5-10 mg/days, at KK of 30-10 ml/min. – 2.5-5 mg/days, at KK less than 10 ml/min. – 1.25-2.5 mg/days only in days of dialysis. Duration of treatment depends on expressiveness of effect of drug, in excessive hypotension the dose of enalapril needs to be reduced.
Side effects – a lowering of arterial pressure, orthostatic hypotension, an acute disorder of cerebral circulation, a myocardial infarction (burglarizing syndrome) – disturbances of a heart rhythm (atrial tachycardia or bradycardia, an atrial fibrillation) – a pulmonary embolism – a vasculitis, Reynaud’s syndrome – dizziness, a headache, weakness, increased fatigue, insomnia or drowsiness, unusual dreams, uneasiness, a depression, paresthesias, confusion of consciousness – a hearing disorder and sight, sonitus, conjunctivitis, dacryagogue – anorexia, disturbance of taste, stomatitis, xerostomia, a glossitis, nausea, vomiting, dyspepsia, a meteorism, an abdominal pain, a constipation, diarrhea, pancreatitis, increase in activity of transaminases, – a liver failure, a cholestasia, hepatitis (hepatocellular or cholestatic, including gepatonekroz) bronchospasm/asthma, short wind, thorax pain, an interstitial pneumonitis, bronchitis, dry cough, pharyngitis, hoarseness of a voice, rhinitis, a rhinorrhea – a mnogoformny exudative erythema (Stephens-Johnson’s syndrome), a small tortoiseshell, a Quincke’s disease of Quincke, an acute anaphylaxis, a serum disease, a toxic epidermal necrolysis (Lyell’s disease), exfoliative dermatitis – erubescence of the person, rash, an itching, a pempigus, an alopecia, a photodermatitis, the increased sweating – a lymphadenopathy, autoimmune diseases – a miositis, an arthralgia, arthritis, muscular spasms – a proteinuria, an oliguria, a renal failure (increase in level of creatinine and urea) – a hyperpotassemia – anemia (including aplastic and hemolytic), a neutropenia, thrombocytopenia, a pancytopenia, an agranulocytosis (the risk is higher at patients with system collagenoses), an eosinophilia, a leukocytosis, increase in SOE, a hyperbilirubinemia, increase in activity of enzymes of a liver, positive test for antinuclear antibodies, increase in level of urea in blood, a hyponatremia, a hypoglycemia – decrease a libido, impotence, a gynecomastia – fervescence, a fever – a syndrome of inadequate secretion of antidiuretic hormone
of the Contraindication – hypersensitivity to enalapril, components of drug or other APF inhibitors (a Quincke’s disease at intake of APF inhibitors), an idiopathic Quincke’s disease in the anamnesis – a porphyria – primary giperaldosteronizm-a hyperpotassemia (more than 6 mmol/l) – a stenosis of the mouth of an aorta or a hypertrophic cardiomyopathy with low emission – a leukopenia or thrombocytopenia – a bilateral stenosis of renal arteries or a stenosis of an artery of the only kidney – hereditary intolerance of fructose, deficiency of Lapp-lactases enzyme, glucose galactose malabsorption pregnancy and the period of a lactation – children’s and teenage age up to 18 years
Medicinal vzaimodeystviyapriy food does not influence enalapril absorption. At simultaneous use of enalapril and kaliysberegayushchy diuretics (Spironolactonum, Triamterenum, amiloride) or drugs of potassium development of a hyperpotassemia is possible. At simultaneous use of enalapril with diuretics, beta blockers, metildopy, nitrates, blockers of calcium channels, gidralaziny, Prazozinum strengthening of hypotensive action is possible. At simultaneous use with non-steroidal anti-inflammatory drugs (including with acetylsalicylic acid) decrease in effect of enalapril and increase in risk of developing a renal failure is possible. Enalapril weakens effect of the drugs containing theophylline. At simultaneous use of enalapril and drugs of lithium the removal of lithium slows down and its action amplifies (control of concentration of lithium in blood plasma is shown). At simultaneous use of enalapril and Cimetidinum the elimination half-life of enalapril is extended. Simultaneous use of APF inhibitors and anti-diabetic drugs (insulin, oral hypoglycemic means) can cause decrease in level of glucose in blood that is followed by risk of development of a hypoglycemia. Such effect is more often observed for the first weeks of the combined treatment and also at patients with renal failures.Sympathomimetics can weaken antihypertensive effect of APF inhibitors. It was seldom reported about emergence of nitritoidny reactions (face reddening, nausea, vomiting and arterial hypotension) at patients who receive drug treatment of gold in injections (sodium aurotiomalat) and at the same time APF inhibitors, including enalapril. Simultaneous use of other hypotensive drugs or vazodilatator can enhance hypotensive effect of enalapril. Alcohol enhances hypotensive effect of APF inhibitors.
Special an ukazaniyaispolzovaniye at older persons. At persons 60 years perhaps development of heavy orthostatic hypotensive reactions are more senior, they are recommended to accept the first dose of enalapril in the evening before going to bed in a prone position. Care when using. It is not recommended to appoint drug after transplantation of a kidney, at patients with a left ventricular stenosis or a stenosis of an aorta, cardiogenic shock and hemodynamically caused obstruction. At some patients without visible disease of kidneys the increase in levels of urea and creatinine in blood was observed if enalapril was applied along with diuretic. In such cases the dose decline of enalapril and/or cancellation of diuretic can be necessary. In this situation the existence at the patient of a renal artery stenosis is not excluded. The risk of developing of arterial hypotension and renal failure increases at patients with a bilateral renal artery stenosis or a stenosis of an artery of the only functioning kidney if they receive treatment by APF inhibitors. Deterioration in function of kidneys can arise already at minor changes of level of creatinine in blood serum. At such patients the treatment should be begun under constant observation of the doctor, with low doses, carefully carrying out selection of a dose and controlling function of kidneys. Seldom use of APF inhibitors was followed by development of a cholestatic syndrome with jaundice or hepatitis, progressing to fulminantny necrosis of a liver. The mechanism of this syndrome is not studied, when developing jaundice or the significant increase in activity of enzymes of a liver it is necessary to cancel APF inhibitor and to appoint the corresponding treatment. Patients with a Quincke’s disease in the anamnesis which is not connected with use of APF inhibitors have a bigger risk of developing of a Quincke’s disease during APF inhibitor use. It was reported about development of a Quincke’s disease of the face, extremities, lips, language, a glottis and/or throat. These reactions can arise during any period of treatment. Even when only the paraglossa is observed (without respiratory distress), long observation of a condition of the patient as prescribing only of antihistaminic drugs and corticosteroids can be insufficiently is necessary.
Developing of cough at use of APF inhibitors is possible. As a rule, cough unproductive, resistant also disappears after the therapy termination. At the patients of negroid race accepting APF inhibitors, enalapril is less effective in a lowering of arterial pressure, in comparison with patients of other races. Patients with the diabetes receiving treatment by anti-diabetic drugs for oral administration or insulin and which begin to apply APF inhibitor should report about need to carry out constant control of development of a hypoglycemia, especially for the first month of the combined treatment. At patients to whom carry out extensive surgical intervention or anesthesia with use of the means leading to development of arterial hypotension enalapril can block formation of angiotensin ІІ owing to compensatory release of renin. If there is arterial hypotension which is explained by the similar mechanism, it can be adjusted by increase in volume of the circulating blood. At some patients receiving treatment by APF inhibitors, including enalapril, the increase in levels of potassium in blood serum was observed. Risk factors of development of a hyperpotassemia include: a renal failure, age (70 years), diabetes, intercurrent diseases (especially a condition of dehydration, a sharp decompensation of warm activity are more senior), a metabolic acidosis and simultaneous use of kaliysokhranyayushchy diuretics. The hyperpotassemia can be the cause heavy, sometimes fatal, of arrhythmia. When using enalapril (especially at persons with autoimmune diseases and system collagenoses) it is necessary to control systematically number of leukocytes in blood. In the first 3 months of treatment it is recommended to control each 2 weeks, further – every 2 month. At appearance of fever of not clear genesis and decrease in level of leukocytes of peripheral blood less than 1×109 in liter the intake of enalapril is immediately stopped. At increase in level of potassium over 6 mmol/l, increase in creatinine more than 50% of an initial indicator (265 µmol/l), proteinurias more than 1 g/days – intake of enalapril should be stopped immediately. It is not necessary to appoint enalapril during a hemodialysis with use of membranes from the poliakrilonitritmetallilsulfat (for example, AN69), haemo filtrations and LPNP-afereza, performing desensitization by apitoxin drugs since at the same time risk of development of anaphylactic reactions increases. Influence on laboratory indicators. Distortion of results of a laboratory research of function of epithelial bodies is possible. It is recommended to stop intake of enalapril in 1-2 days prior to carrying out a research. Emergence of positive reaction to antibodies to nuclear antigen is possible. Pregnancy and the period laktatsiipreparat is not appointed at pregnancy as APF inhibitors can cause diseases or death of a fruit or the newborn, including arterial hypotension, a renal failure, a hyperpotassemia, a hypoplasia of a skull of the newborn, development of an oligogidramnion (contracture of extremities, deformation of facial bones of a skull, a hypoplasia of lungs) is also possible. Drug in trace concentration is emitted with breast milk. In need of its use in the period of a lactation, breastfeeding needs to be stopped. The feature of influence of medicine on ability to run the vehicle and others potentially dangerous mekhanizmamiv the period of use of drug should refrain, whenever possible, from any activity connected with driving and potentially dangerous mechanisms in connection with possible development of such side effects as dizziness.
PeredozirovkaSimptoma: arterial hypotension. Intake of enalapril in a dose of 300-400 mg leads to emergence of level of drug in blood by 100-200 times exceeding therapeutic. Development of acute arterial hypotension up to collapse is characteristic, disturbances of cerebral circulation, a myocardial infarction, a thrombembolia or a Quincke’s disease, also development of a stupor and spasms is possible. Treatment: drug withdrawal, gastric lavage using activated carbon, prescribing of salt laxatives, transfer of the patient to horizontal position with the raised legs, completion of volume of the circulating blood isotonic solution of sodium chloride and plasma substituting solutions, the supporting and symptomatic therapy. In hard cases carry out a hemodialysis.
A form of release and upakovkapo 10 tablets in blister strip packaging from a film of polyvinylchloride and flexible packing on the basis of the aluminum foil or printing aluminum foil varnished. On the 2nd blister strip packagings together with the instruction for medical use in the state and Russian languages place in a pack from cardboard.
To Store storage conditions in the dry, protected from light place, at a temperature not over 25 ºС. To store out of children’s reach!
To 2 godena to use a period of storage after expiry date.
Prescription status According to the prescription
ProizvoditelOtkrytyy joint-stock company “Borisovsky Plant of Medications”, Republic of Belarus, the Minsk Region, Borisov, st. Chapayeva, 64/27, ph. / fax 8-(10375177) 744280.
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to Develop the Address of the organization accepting in the territory of the Republic of Kazakhstan claims from consumers on quality of products (goods) “Borisovsky Plant of Medications” Open joint stock company, Republic of Belarus, Minsk Region, Borisov, Chapayev St., 64/27, ph. / fax 8-(10375177) 744280, the e-mail address of firstname.lastname@example.org
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