Clinical and pharmacological group: & nbsp

ACE Inhibitors

Included in the formulation
  • Dapril®
    pills inwards 
    Medocemi Co., Ltd.     Cyprus
  • Diropress®
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    Sandoz d.     Slovenia
  • Diroton®
    pills inwards 
    GEDEON RICHTER, OJSC     Hungary
  • Irumed®
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  • Lizakard
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  • Lizigamma®
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  • Lisinopril
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  • Lisinopril
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    MEDISORB, CJSC     Russia
  • Lisinopril
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    PRANAFARM, LLC     Russia
  • Lisinopril
    pills inwards 
    ZIO-HEALTH, JSC     Russia
  • Lisinopril
    pills inwards 
  • Lisinopril
    pills inwards 
    NIZHFARM, JSC     Russia
  • Lisinopril
    pills inwards 
    ALSI Pharma, ZAO     Russia
  • Lisinopril
    pills inwards 
    VERTEKS, AO     Russia
  • Lisinopril
    pills inwards 
    NIZHFARM, JSC     Russia
  • Lisinopril
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  • Lisinopril
    pills inwards 
    Alkaloid, JSC     Macedonia
  • Lisinopril
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  • Lisinopril
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    OZONE, LLC     Russia
  • Lisinopril Grindeks
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    GRINDEX, JSC     Latvia
  • Lizinopril Canon
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  • Lysinopril Organica
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    ORGANICS, JSC     Russia
  • Lisinopril-OBL
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  • Lisinopril-Krka
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  • Lizinopril-SZ
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    NORTH STAR, CJSC     Russia
  • Lizinopril-Teva
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  • Lysinate®
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    Aktavis, AO     Iceland
  • Liziprex®
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    IRBITSK HFZ, OJSC     Russia
  • Lizonorm
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    Adifarm, EAD     Bulgaria
  • Lysoryl
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  • Listril®
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  • Liten®
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    Boznalek, AO     Bosnia and Herzegovina
  • Rileys-sanovel
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  • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    ONLS

    АТХ:

    C.09.A.A.03   Lisinopril

    C.09.A.A   ACE Inhibitors

    Pharmacodynamics:

    ACE inhibitor. The mechanism of antihypertensive action is associated with inhibition of ACE activity, which leads to a decrease in the conversion rateangiotensin I in angiotensin II (which has a pronounced vasoconstrictor effect and stimulates the secretion of aldosterone in the adrenal cortex). As a result of the decrease in the formation of angiotensin II, a secondary increase in plasma renin activity occurs due to the elimination of negative feedback during the release of renin and a direct decrease in the secretion of aldosterone. Reducing the secretion of aldosterone can increase the concentration of potassium.

    Reduces the overall peripheral vascular resistance (afterload), wedging pressure in the pulmonary capillaries (preload) and resistance in the pulmonary vessels, increases the minute volume of the heart and tolerance to the load.

    Lizinopril reduces albuminuria. In patients with hyperglycemia contributes to the normalization of the function of the damaged glomerular endothelium. Does not affect the concentration of glucose in the blood in patients with diabetes mellitus and does not lead to an increase in cases of hypoglycemia.

    Pharmacokinetics:

    After oral administration lisinopril slowly and not completely absorbed from the digestive tract. Absorption on the average is 25%, differs high variability - 6-60%. Cmax in plasma is achieved after about 7 hours. Binding to plasma proteins is negligible. It is excreted unchanged in the urine. In patients with normal renal function, the elimination half-life is 12 hours.

    Lizinopril is excreted from the body during hemodialysis.

    Indications:

    Essential and Renovascular Hypertension (in the form of monotherapy or in combination with other antihypertensive drugs).

    Chronic heart failure (as part of combination therapy).

    Acute myocardial infarction (in the first 24 hours with stable hemodynamic parameters to maintain these parameters and prevention of left ventricular dysfunction and heart failure).

    Diabetic nephropathy (to reduce albuminuria in patients with insulin-dependent diabetes mellitus at normal arterial pressure and in patients with non-insulin-dependent diabetes mellitus with hypertension).

    IX.I10-I15.I10   Essential [primary] hypertension

    IX.I30-I52.I50.0   Congestive heart failure

    Contraindications:

    Hypersensitivity to lisinopril or other ACE inhibitors.

    Pregnancy, breast-feeding.

    Carefully:

    Angioedema due to treatment with ACE inhibitors in history, hereditary or idiopathic angioedema, aortic stenosis, cerebrovascular diseases (including cerebral circulatory insufficiency), ischemic heart disease, coronary insufficiency, severe autoimmune systemic connective tissue diseases (including systemic lupus erythematosus , scleroderma), oppression of bone marrow hematopoiesis, diabetes mellitus, hyperkalemia, bilateral stenosis of the renal arteries, stenosis of the artery only kidney condition after kidney transplantation, renal failure, sodium restricted diet revenues, state, accompanied by a decrease in circulating blood volume (including diarrhea, vomiting), advanced age, the age of 18 years (Safety and efficacy have not been studied).

    Pregnancy and lactation:

    Adequate and well-controlled studies in humans and animals have not been conducted. Do not use during pregnancy and lactation.

    FDA Recommendations category C first semester, category D - second term.

    Dosing and Administration:

    Inside, regardless of food intake.With arterial hypertension, patients who do not receive other antihypertensives are prescribed 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 per day (increasing the dose above 40 mg per day does not usually lead to a further decrease in blood pressure). The usual daily maintenance dose is 20 mg. The maximum daily dose is 40 mg.

    The overall effect usually develops in 2-4 weeks from the start of treatment, which should be taken into account when increasing the dose. With insufficient clinical effect, it is possible to combine the drug with other antihypertensive drugs.

    With renovascular hypertension or other conditions with increased activity renin-angiotensin-aldosterone system it is advisable to prescribe a low initial dose of 2.5-5 mg per day, under enhanced medical supervision (control of blood pressure, kidney function, potassium concentration in blood serum). The maintenance dose, continuing strict medical control, should be determined depending on the dynamics of blood pressure.

    With renal insufficiency, due to the fact that lisinopril is released through the kidneys, the initial dose should be determined depending on the creatinine clearance, then, in accordance with the reaction, a maintenance dose should be established in conditions of frequent monitoring of renal function, potassium level, sodium in the blood serum.

    With persistent arterial hypertension long-term maintenance therapy of 10-15 mg per day is indicated.

    In chronic heart failure, the initial dose is 2.5 mg 1 time per day, followed by an increase of 2.5 mg 3-5 days before the usual maintenance daily dose of 5-20 mg. The dose should not exceed 20 mg per day.

    In elderly people, a more pronounced and prolonged hypotensive effect is often observed, which is associated with a decrease in the rate of excretion of lisinopril (it is recommended to start treatment with 2.5 mg per day).

    Acute myocardial infarction (as part of combination therapy). In the first day - inside 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 the first 3 days after acute myocardial infarction, a lower dose of 2.5 mg should be given in patients with low systolic blood pressure (120 mm Hg or lower). In the case of lowering blood pressure (systolic blood pressure less than or equal to 100 mm mercury column) daily dose of 5 mg, if necessary, temporarily reduced to 2.5 mg. In the case of a prolonged, marked decrease in blood pressure (systolic blood pressure Below 90 mm mercury column more than 1 hour) treatment with lisinopril should be discontinued.

    Diabetic nephropathy. In patients with non-insulin-dependent diabetes mellitus, 10 mg of lisinopril is administered once a day. If necessary, it is possible to increase the dose to 20 mg once a day in order to achieve diastolic blood pressure values ​​below 75 mm mercury column in the sitting position. In patients with insulin-dependent diabetes mellitus, the dosage is the same with the aim of achieving values diastolic blood pressure Below 90 mm mercury column in the sitting position.

    Side effects:

    Dry cough.

    Reduced blood pressure.

    Edema of the Quincke.

    Hyperkalemia, proteinuria.

    Headache, unusual fatigue, nausea, diarrhea, skin rash.

    Disturbance of taste, pain in the chest, neutropenia, agranulocytosis, hepatotoxic effect, pancreatitis.

    Overdose:

    Symptoms (occur when taking a single dose of 50 mg): a marked decrease in blood pressure, dryness of the oral mucosa, drowsiness, urinary retention, constipation, anxiety, increased irritability.

    Treatment: there is no specific antidote. Symptomatic therapy. Gastric lavage, application of enterosorbents and laxatives. Intravenous introduction of 0.9% sodium chloride solution was shown. In the case of a sustained bradycardia, the use of an artificial pacemaker is necessary. It is necessary to control blood pressure, water-electrolyte balance. Hemodialysis is effective.

    Interaction:

    With simultaneous use with antihypertensive agents, additive antihypertensive action is possible.

    With simultaneous use with potassium-sparing diuretics (spironolactone, triamterene, amiloride), potassium preparations, substitutes for edible salt containing potassium, the risk of hyperkalemia increases, especially in patients with impaired renal function.

    With the simultaneous use of ACE inhibitors and non-steroidal anti-inflammatory drugs, the risk of developing renal dysfunction increases, and hyperkalemia is rarely observed.

    With simultaneous use with "loop" diuretics, thiazide diuretics intensify antihypertensive effect. The appearance of severe arterial hypotension, especially after the first dose of a diuretic, is apparently due to hypovolemia, which leads to a transient increase in the hypotensive effect of lisinopril. Increased risk of impaired renal function.

    With simultaneous use with indomethacin, the antihypertensive effect of lisinopril decreases, apparently due to inhibition under the influence of non-steroidal anti-inflammatory drugs the synthesis of prostaglandins (which are believed to play a role in the development of the hypotensive effect of ACE inhibitors).

    With simultaneous use with insulin, hypoglycemic agents - derivatives of sulfonylureas, hypoglycemia can be developed by increasing glucose tolerance.

    With simultaneous application with clozapine, the concentration of clozapine in the blood plasma increases.

    With simultaneous application of lithium carbonate, the concentration of lithium in the serum increases, accompanied by symptoms of lithium intoxication.

    A case of the development of severe hyperkalemia in a patient with diabetes mellitus is described with simultaneous application with lovastatin.

    A case of severe arterial hypotension with simultaneous application with pergolide is described.

    With simultaneous use with ethanol, the action of ethanol is enhanced.

    Special instructions:

    ACE inhibitor of medium duration; active substance, not requiring hepatic activation; Do not cumulate.

    For antihypertensive effects comparable to captopril, hydrochlorothiazide, chlorthalidone, amlodipine, rilmenidine, valsartan, but the latter less often causes side effects.

    If inefficacy of lisinopril in a dose of 20 mg is prescribed olmesartan (20-40 mg each).

    Lizinopril helps to reduce left ventricular hypertrophy.

    Reduces the thickness of intima and media in elderly patients with arterial hypertension.

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