Active substanceLisinoprilLisinopril
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  • Dosage form: & nbsppills
    Composition:

    In 1 tablet of the drug contains:

    active substance: lisinopril dihydrate (in terms of lisinopril) 5.0 mg or 10.0 mg;

    Excipients: calcium hydrophosphate dihydrate 75.0 mg or 100.0 mg, corn starch 20.0 mg or 25.0 mg,lactose monohydrate (sugar milk) -72.4 mg or 74.4 mg, povidone (polyvinylpyrrolidone, medium-molecular medical) -3.6 mg or 5.0 mg. talc (magnesium hydrosilicate) 2.5 mg or 3.5 mg. calcium stearate - 1.5 mg or 2.1 mg.

    Description:Tablets are white or almost white in color. Tablets with a dosage of 5 mg are round planocylindrical forms, with a dosage of 10 mg are round biconvex forms.
    Pharmacotherapeutic group:Angiotensin-converting enzyme inhibitor (ACE)
    ATX: & nbsp

    C.09.A.A.03   Lisinopril

    C.09.A.A   ACE Inhibitors

    Pharmacodynamics:

    Angiotensin-converting enzyme inhibitor (ACE). reduces the formation of angiotensin II from angiotensin I. Reduction in angiotensin II leads to a direct decrease in the release of aldosterone. Reduces the degradation of bradykinin and increases the synthesis of prostaglandins. Reduces the overall peripheral vascular resistance, arterial pressure (BP), preload, pressure in the pulmonary capillaries, causes an increase in the minute volume of blood and increased tolerance of the myocardium to loads in patients with chronic heart failure. Expands arteries more than veins. Some effects are explained by the effect on the tissue renin-angiotensin-aldosterone system.With prolonged use, myocardial hypertrophy and the walls of arteries of resistive type decrease. Improves the blood supply of the ischemic myocardium. In addition to reducing blood pressure, lisinopril Organika reduces albuminuria.

    ACE inhibitors prolong life expectancy in patients with chronic heart failure, slow the progression of left ventricular dysfunction in patients who underwent myocardial infarction without clinical manifestations of heart failure.

    The onset of action is after 1 hour. The maximum effect is determined after 6-7 hours, duration is 24 hours. With arterial hypertension, the effect is observed in the first days after the start of treatment, stable effect develops after 1 -2 months.

    Pharmacokinetics:

    Absorption -30% (6-60%); bioavailability is 25%. Poorly binds to blood plasma proteins. Permeability through the blood-brain barrier and placental barrier -low. The maximum concentration of Lysinopril Organic in blood plasma is 90 ng / ml. The time required to reach the maximum concentration is 7 hours.

    Metabolism is practically nc exposed and excreted by the kidneys unchanged. The half-life is 12 hours.

    In patients with chronic heart failure, the absorption and clearance of Lysinopril Organic is reduced.

    In patients with renal insufficiency, the concentration of Lysinopril Organic is several times higher than the concentration in the blood plasma in volunteers, with an increase in the time to reach the maximum concentration in the blood plasma and an increase in the half-life.

    In elderly patients, the concentration of the drug in the blood plasma and the area under the curve is 2 times greater than in young patients.

    Indications:Arterial hypertension (in monotherapy or in combination with other antihypertensive agents), chronic heart failure (as part of combination therapy for the treatment of patients taking cardiac glycosides and / or diuretics); early treatment of acute myocardial infarction in combination therapy (within the first 24 hours with stable hemodynamic parameters to maintain these parameters and prevention of left ventricular dysfunction and heart failure); diabetic nephropathy (decreased albuminuria in patients with type 1 diabetes mellitus with normal BP and patients with type 2 diabetes mellitus with arterial hypertension).
    Contraindications:Hypersensitivity to lisinopril Organic or other ACE inhibitors, other components of the drug; angioedema in history, including the use of ACE inhibitors; hereditary edema of Quincke or idiopathic angioedema; hemodialysis or hemofiltration using high-flux membranes (eg AN69®); apheresis of low-density lipoproteins using dextran sulfate; desensitizing therapy for venom of Hymenoptera (bees, wasps); simultaneous use with aliskiren and aliskirenoderzhaschimi drugs in patients with diabetes mellitus and patients with impaired renal function of moderate and / or severe severity (creatinine clearance less than 60 ml / min); lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome; pregnancy, lactation; age to 18 years (efficacy and safety not established).
    Carefully:Impaired renal function; uremia; bilateral stenosis of the renal arteries or stenosis of the artery of a single kidney with progressive azotemia; condition after kidney transplantation; diabetes; hyperkalemia; stenosis of the aortic aorta;hypertrophic obstructive cardiomyopathy; mitral stenosis; primary hyperaldosteronism; arterial hypotension; cerebrovascular diseases (including cerebral circulatory insufficiency); cardiac ischemia; coronary insufficiency; autoimmune systemic diseases of connective tissue (including scleroderma, systemic lupus erythematosus); oppression of bone marrow hematopoiesis; diet with restriction of table salt; hypovolemic conditions (including the results of diarrhea, vomiting); simultaneous use with preparations containing aliskiren, or angiotensin II receptor antagonists (with double blockade of RAAS, there is an increased risk of arterial hypotension, hyperkalemia and renal failure); Older age (over 65 years).
    Pregnancy and lactation:

    When establishing pregnancy, use Lizinopril Organica as soon as possible. Admission of ACE inhibitors in the II and III trimester of pregnancy has an adverse effect on the fetus (there may be a marked decrease in blood pressure, kidney failure, hyperkalemia, hypoplasia of the skull bones, fetal death).Data on the negative effects of the drug on the fetus in case of application during the I trimester are not present. For newborns and infants who have undergone intrauterine exposure to ACE inhibitors, careful monitoring is recommended to timely detect a marked decrease in blood pressure, oliguria, and hyperkalemia.

    Lysinopril Organica penetrates the placenta. There is no data on the isolation of lisinopril Organic in breast milk. If taking Lizinopril Organic is necessary during lactation, then breastfeeding should be discarded.

    Dosing and Administration:

    Inside, once a day in the morning, regardless of food intake, preferably at the same time. With arterial hypertension, patients who do not receive other antihypertensive drugs are administered 5 mg once a day. In the absence of effect, the dose is increased every 2-3 days by 5 mg to an average therapeutic dose of 20-40 mg / day (increasing the dose above 40 mg / day usually does not lead to a further decrease in blood pressure). The usual daily maintenance dose is 20 mg. The maximum daily dose is 40 mg. With insufficient therapeutic effect, it is possible to combine the drug with other antihypertensive drugs.

    If the patient received a preliminary treatment with diuretics, the use of such drugs should be stopped 2-3 days before the Lizinopril Organic drug is started. If the ego is not possible, then the initial dose of Lysinopril Organica should not exceed 5 mg per day. In this case, after taking the first dose, medical supervision is recommended for several hours (maximum effect is achieved after about 6 hours), since a pronounced decrease in blood pressure may occur.

    When renovascular hypertension or other conditions with increased activity of the renin-angiotensin-aldosterone system, it is advisable to prescribe a low initial dose of 5 mg per day under enhanced medical supervision (control of blood pressure, kidney function, potassium content in blood serum). The maintenance dose, continuing strict medical control, should be determined depending on the dynamics of blood pressure. In renal failure due to the fact that lisinopril Organica is excreted by the kidneys, the initial dose should be determined depending on the creatinine clearance (CK). Further, the selection of doses should be made depending on individual reactions with regular monitoring of kidney function, potassium, sodium in the blood serum.The initial dose for CK 30-70 ml / min is 5-10 mg / day, 10-30 ml / min - 5 mg / day. less than 10 ml / min, including patients who are on hemodialysis - 2.5 mg / day.

    With chronic heart failure: the initial dose is 2.5 mg per day, with a gradual increase in 3-5 days to 5-10 mg per day. The maximum daily dose is -20 mg. Early treatment of acute myocardial infarction (as part of combination therapy): in the first 24 hours - 5 mg, then 5 mg every other day, 10 mg after two days and then 10 mg once a day. The course of treatment - at least 6 weeks. At the beginning of treatment or within 3 days after an acute myocardial infarction in patients with low systolic blood pressure (120 mm Hg or lower) a smaller dose of 2.5 mg is prescribed. In the case of a decrease in blood pressure (systolic blood pressure below or equal to 100 mm Hg), the daily dose of 5 mg, if necessary, is reduced to 2.5 mg. In the case of a long pronounced decrease in blood pressure (systolic blood pressure less than 90 mm Hg for more than 1 hour), drug treatment should be discontinued. With diabetic nephropathy (a decrease in albuminuria in patients with type 1 diabetes mellitus with normal arterial pressure and in patients with type 2 diabetes mellitus with arterial hypertension): the initial dose is 10 mg / day. which if necessary is increased to 20 mg / day to achieve the target values ​​of diastolic blood pressure.

    It is possible to use lisinopril in other dosage forms - 2.5 mg tablets or 5 mg tablets with a risk to ensure this dosage regimen.

    Side effects:

    The frequency of adverse reactions is classified according to the recommendations of the World Health Organization (WHO): very often (> 1/10): often (> 1/100. <1/10); infrequently (> 1/1000. <1/100): rarely (> 1/10000, <1/1000): very rarely (<1/10000): the frequency is unknown (the frequency of undesired reactions can not be estimated based on the available data).

    Violations from the blood and lymphatic system: rarely - a decrease in hemoglobin, a decrease in hematocrit; very rarely - oppression of bone marrow function, anemia, thrombocytopenia, leukopenia, neutropenia, agranulocytosis, hemolytic anemia, lymphadenopathy.

    Immune system disorders: infrequently - angioedema (face, lips, tongue, larynx or epiglottis, upper and lower limbs); rarely - a syndrome, including an increase in the rate of erythrocyte sedimentation (ESR). arthralgia and the appearance of anti-nuclear antibodies, urticaria; very rarely - autoimmune diseases, intestinal neurotic edema.

    Disorders from the endocrine system: rarely - the syndrome of impaired secretion of antidiuretic hormone (ADH).

    Disorders from the psyche: infrequently - lability of mood; rarely anorexia; frequency is unknown - depression, confusion).

    Impaired nervous system: often - dizziness, headache; infrequently - paresthesia, sleep disturbance (drowsiness / insomnia); rarely confusion; frequency is unknown-convulsive twitching of the muscles of the extremities and lips.

    Disorders from the side of the organ of vision: rarely - visual impairment.

    Hearing disorders and labyrinthine disturbances: infrequently - vergigo.

    Heart Disease: infrequently - acute myocardial infarction, tachycardia, palpitation; rarely - exacerbation of the severity of symptoms and weighting of the course of CHF, violation of atrioventricular conduction, chest pain.

    Vascular disorders: often - orthostatic hypotension; infrequent, marked decrease in blood pressure; rarely - impaired cerebral circulation in patients with "increased risk" due to a marked decrease in blood pressure, Raynaud's syndrome, vasculitis.

    Disturbances from the respiratory system: often - dry cough; infrequently - rhinitis; very rarely - sinusitis, dyspnea, bronchospasm, allergic alveolitis / eosinophilic pneumonia.

    Disorders from the digestive system: often - nausea, vomiting, diarrhea; rarely dry mouth, dyspepsia, abdominal pain, changes in taste; very rarely - pancreatitis.

    Disorders from the liver and bile ducts: rarely - hepatocellular or cholestatic jaundice, hepatitis.

    Disorders from the kidneys and urinary tract: often - renal dysfunction; rarely uremia, acute renal failure; very rarely - oliguria, anuria; frequency unknown - proteinuria.

    Disorders from the rut and subcutaneous tissues: infrequently - itchy skin. rash; rarely psoriasis; very rarely - pemphigus, toxic epidermal necrolysis (Lyell syndrome), erythema multiforme, Stevens-Johnson syndrome, pseudolymphoma of the skin.

    Disturbances from the musculoskeletal and connective tissue: rarely - myalgia, arthralgia / arthritis.

    Violations of the genitals and breast: infrequently - sexual dysfunction; rarely - gynecomastia.

    Laboratory and instrumental data: infrequently - increased urea concentration in blood plasma, hypercreatininaemia, gipekalemia, increased activity of "hepatic" trane aminases, rarely - hyperbilirubinemia. hyponatremia; very rarely, an increase in ESR, an increase in the titer of antinuclear antibodies, a decrease in glucose concentration.

    General disorders and disorders at the site of administration: rarely - fever, asthenia, fatigue, alopecia, impaired development of the fetus; very rarely-increased sweating.

    Overdose:

    Symptoms: a pronounced decrease in blood pressure, dryness of the oral mucosa, a violation of water electrolyte balance, renal failure, increased respiration, tachycardia, palpitations, bradycardia, vascular collapse, dizziness, anxiety, anxiety, irritability, dry cough, hyperventilation of the lungs, drowsiness , urinary retention, constipation.

    Treatment: symptomatic therapy, intravenous injection of 0.9% sodium chloride solution, if necessary - vasopressor drugs. It is necessary to monitor blood pressure. water-electrolyte balance, urea concentration, creatinine clearance.With a pronounced decrease in blood pressure, it is necessary to move the patient to a horizontal position with the legs elevated upwards. In the case of a stable bradycardia, a temporary pacemaker is required. Hemodialysis is effective. Gastric lavage, application of enterosorbents and laxatives.

    Interaction:

    With the simultaneous use of lisinopril with potassium-sparing diuretics (spironolactone, triamterene, amiloride, eplerenone), potassium preparations, salt substitutes containing potassium, cyclosporine, the risk of hyperkalemia increases, especially in cases of impaired renal function. Therefore, these combinations should be prescribed only with regular monitoring of potassium content in blood plasma and kidney function.

    Simultaneous use of lisinopril with beta-blockers. blockers of "slow" calcium channels, diuretics, tricyclic antidepressants / neuroleptics, other drugs with hypotensive effect increases the severity of hypotensive effect.

    Lizinopril slows the withdrawal of lithium preparations, which can increase the risk of side effects.Therefore, when combined, it is necessary to regularly monitor the lithium content in blood plasma.

    Antacids and colestramine reduce the absorption of lisinopril in the gastrointestinal tract.

    When combined with insulin and hypoglycemic agents for oral administration, the risk of developing hypoglycemia increases.

    When combined with non-steroidal anti-inflammatory drugs (NSAIDs), cycloxygenase-2 inhibitors and acetylsalicylic acid (at a dose of more than 3 g / day), estrogen, sympathomimetics, hypotensive effect of lisinopril decreases.

    NSAIDs and ACE inhibitors increase the level of potassium in the blood plasma and can worsen kidney function. This effect is usually reversible.

    The use of lisinopril in combination with acetylsalicylic acid as an antiplatelet agent, thrombolytic and / or nitrates is not contraindicated.

    With simultaneous application ethanol strengthens the action of lisinopril.

    With simultaneous use of ACE inhibitors and gold preparations for intravenous administration (sodium aurotomy malate) describes a symptom complex, which includes facial flushing, nausea, vomiting, and lowering blood pressure.

    Co-administration with selective serotonin reuptake inhibitors can lead to severe hyponatraemia.

    When combined with allopurinol and aliskirensoderzhaschimi drugs in patients with diabetes mellitus and patients with impaired renal function, moderate and / or severe (creatinine clearance less than 60 mL / min) increases the risk of hyperkalemia, deterioration of renal function and increased incidence of cardiovascular disease and mortality.

    In elderly patients (over 65 years) and patients with impaired renal function concomitant use of ACE inhibitors with sulfamethoxazole / trimethoprim was accompanied by severe hyperkalemia. which is believed to have been caused by a make-up, so lisinopril Use with caution with preparations containing trimethoprim, regularly monitoring the potassium content in the blood plasma.

    Special instructions:

    Symptomatic hypotension.

    Most often, a marked decrease in blood pressure arises with a decrease in the volume of circulating blood (BCC), caused by diuretic therapy, reduction of table salt in food, dialysis, diarrhea, or vomiting.In patients with chronic heart failure with concurrent renal failure or without it, a marked decrease in blood pressure is possible. Under the strict supervision of a physician, use the preparation Lizinopril Organica in patients with coronary heart disease, cerebrovascular insufficiency, in which a sharp decrease in blood pressure can lead to myocardial infarction or stroke. Transient arterial hypotension is not a contraindication for taking the next dose of the drug.

    When using the drug Lysinopril Organica, in some patients with chronic heart failure, but with normal or low blood pressure, there may be a decrease in blood pressure, which is usually not the reason for discontinuing treatment.

    Before the start of treatment with the drug, if possible, should normalize the sodium content and / or make up the BCC, carefully monitor the effect of the initial dose of Lysinopril Organic on the patient.

    In the case of stenosis of the renal arteries (in particular, with bilateral stenosis or in the presence of stenosis of the artery of a single kidney), as well as in case of circulatory failure due to lack of sodium and / or liquid ions,the use of the drug Lizinopril Organica can lead to impaired renal function, acute renal failure, which is usually irreversible even after drug withdrawal.

    In acute myocardial infarction, the use of standard therapy (thrombolytics, acetylsalicylic acid, beta-adrenoblockers) Lysinopril Organic can be used in conjunction with intravenous administration or with the use of therapeutic transdermal systems of nitroglycerin.

    Surgical intervention / general anesthesia: with extensive surgical interventions, as well as using other means of reducing blood pressure, Lysinopril Organica, blocking the formation of angiotensin II, can cause a pronounced unpredictable decrease in blood pressure.

    Angioedema, edema of the face, limbs, lips. tongue, epiglottis and / or larynx was rarely seen in patients treated with ACE inhibitors that may occur at any time of treatment. In this case, treatment with Lysinopril Organic should be stopped as soon as possible and for the patient to establish an observation until the symptoms regress completely.In cases where there was only edema of the face and lips, the condition usually passes without treatment, however, it is possible to prescribe antihistamines. Angioedema with edema of the larynx can be lethal. When the tongue, epiglottis or larynx are swollen, airway obstruction may occur. Therefore, immediately appropriate therapy (0.3-0.5 ml epinephrine (adrenaline) 1: 1000 subcutaneously, administration of glucocorticosteroids, antihistamines) and / or measures to ensure airway patency. Patients who have had an angioneurotic edema in the anamnesis and who were not associated with previous treatment with ACE inhibitors may have a higher risk of developing it during treatment with an inhibitor of AMP. Anaphylactic reaction was noted in patients on hemodialysis using high-flow dialysis membranes (AN69®), which simultaneously take ACE inhibitors. In such cases, one should consider the possibility of using another type of membrane for dialysis or another antihypertensive agent. Possible occurrence of anaphylactic reactions during apheresis of low density lipoproteins with dextran sulfate.

    In some cases, the desensitisation of the venom of Hymenoptera, treatment with ACE inhibitors was accompanied by hypersensitivity reactions. This can be avoided by interrupting the administration of ACE inhibitors.

    In patients of the Negroid race, the risk of developing angioedema is higher. Like other ACE inhibitors, lisinopril It is less effective in reducing blood pressure in patients of the Negroid race. This effect, perhaps, is associated with a marked predominance of low-grade status in patients of the Negroid race with arterial hypertension.

    In rare cases on the background of therapy with ACE inhibitors intestinal edema of the intestine develops. In this case, patients have abdominal pain as an isolated symptom or in combination with nausea and vomiting, in some cases without a previous angioedema and a normal C1-esterase content. The diagnosis is established by means of computed tomography of the abdominal cavity, ultrasound examination or at the time of surgical intervention. Symptoms disappear after stopping the intake of ACE inhibitors. In patients with pain in the abdomen, taking ACE inhibitors.when carrying out a differential diagnosis, it is necessary to take into account the possibility of developing angioedema of the intestine.

    In elderly patients, the same dose leads to a higher concentration of the drug in the blood, therefore special caution is required when determining the dose.

    Cough was used in the use of ACE inhibitors. Cough is dry, prolonged, which disappears after discontinuation of treatment with ACE inhibitors. With a differential diagnosis of cough, one must also consider the cough caused by the use of ACE inhibitors. Based on the results of epidemiological studies, it is assumed that simultaneous administration of ACE inhibitors and insulin, as well as hypoglycemic agents for oral administration may lead to the development of hypoglycemia. The greatest risk of development is observed during the first weeks of combination therapy, as well as in patients with impaired renal function. Patients with diabetes require careful monitoring of glycemia, especially during the first month of therapy with an ACE inhibitor.

    In some cases, hyperkalemia was noted. Risk factors for the development of hyperkalemia include renal failure, diabetes mellitus, intake of potassium preparations, intake of potassium-sparing diuretics (spironolactone. eplerenone, triamterene, amiloride) or other drugs that cause an increase in potassium in the blood (eg, heparin), especially in patients with impaired renal function. During the treatment with the drug, regular monitoring of potassium, glucose, urea, and lipid ions in patients with blood plasma is necessary.

    The use of ACE inhibitors can lead to the development of cholestatic jaundice with progression up to fulminant liver necrosis, therefore it is necessary to stop taking the drug with an increase in the activity of "liver" transaminases and the appearance of symptoms of cholestasis.

    There have been cases of development of neutropenia / agranulocytosis, thrombocytopenia and anemia in patients receiving ACE inhibitors. Such cases are quite rare in patients with normal renal function. Neutropenia and agranulocytosis disappear after the withdrawal of ACE inhibitors. Lisinopril should be used with extreme caution in patients with systemic connective tissue diseases receiving immunosuppressive therapy, treatment with allopurinol or procainamide, especially in patients with impaired renal function. In such patients, in some cases, infectious diseases resistant to antibiotic therapy can develop.In the case of lisinopril in these patients, regular monitoring of blood leukocytes should be carried out.

    If any symptoms of infection (eg, sore throat, fever) appear, the patient should consult a doctor immediately, as they may be a manifestation of neutropenia.

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

    Because the potential risk of agranulocytosis can not be ruled out, periodic monitoring of the blood picture is required.

    Effect on the ability to drive transp. cf. and fur:There is no evidence of the effect of Lysinopril Organic on the ability to drive vehicles and mechanisms, applied in therapeutic doses, but it must be taken into account that there may be dizziness, so care should be taken.
    Form release / dosage:Tablets 5 mg and 10 mg.
    Packaging:

    For 10 tablets in a planar cell packaging made of polyvinylchloride film and aluminum foil printed lacquered.

    2, 3 or 5 contour mesh packages together with instructions for use in a pack of cardboard.

    Storage conditions:

    Store in a dark place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:3 years. Do not use after the expiration date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:LP-000744
    Date of registration:29.09.2011 / 19.10.2016
    Expiration Date:Unlimited
    The owner of the registration certificate:ORGANICS, JSC ORGANICS, JSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp25.02.2018
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