Active substanceLisinoprilLisinopril
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  • Dosage form: & nbsppills
    Composition:

    Tablets 5 mg:

    Active substance: lisinopril dihydrate (5.444 mg) in terms of lisinopril (anhydrous) 5 mg;

    Excipients: mannitol, sodium dihydrogen phosphate (anhydrous), starch, magnesium stearate;

    Tablets 10 mg:

    Active substance: lisinopril dihydrate (10,900 mg) in terms of lisinopril (anhydrous) 10 mg;

    Excipients: mannitol, sodium dihydrogen phosphate (anhydrous), starch, magnesium stearate, talc.

    Description:

    Tablets 5 mg: Round flat white tablets with a risk on one side and bevel.

    Tablets 10 mg: Round flat white tablets with chamfer, marked "10", stamping, on one side and crosswise on the other side.

    Pharmacotherapeutic group:Angiotensin-converting enzyme inhibitor (ACE)
    ATX: & nbsp

    C.09.A.A.03   Lisinopril

    C.09.A.A   ACE Inhibitors

    Pharmacodynamics:

    The ACE inhibitor reduces the formation of angiotensin II from angiotensin I. Reducing angiotensin II leads to a direct decrease in the release of aldosterone. Reduces the degradation of bradykinin and increases the synthesis of prostaglandins. , Decreases total peripheral vascular resistance (TPR), blood pressure (BP), preload, the pressure in the pulmonary capillaries, causes an increase in cardiac output and increase tolerance to myocardial stress 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.

    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 antihypertensive effect begins in about 6 hours and persists for 24 hours. The duration of the effect also depends on the size of the dose. The beginning of the action is after 1 hour. The maximum effect is determined in 6-7 hours. With arterial hypertension, the effect is observed in the first days after the start of treatment, stable action develops after 1-2 months. With a sharp withdrawal of the drug, no pronounced increase in blood pressure was observed.

    In addition to reducing blood pressure lisinopril reduces albuminuria. Lisinopril does not affect the concentration of glucose in the blood in patients with diabetes mellitus and does not increase the incidence of hypoglycemia.

    Pharmacokinetics:

    Suction. After oral administration lisinopril absorbed from the gastrointestinal tract (GIT) on average by 25%, but the absorption can vary from 6 to 60%.Bioavailability is 25%: Food intake does not affect the absorption of lisinopril.

    Distribution. Almost does not bind to blood plasma proteins. The maximum concentration in the blood plasma of 90 ng / ml is reached after 7 hours. Permeability through the blood-brain and placental barrier is low.

    Metabolism. Lizinopril is not biotransformed in the body.

    Excretion. It is excreted by the kidneys unchanged. The half-life is 12 hours.

    Pharmacokinetics in selected patient groups. In patients with chronic heart failure, the absorption and clearance of lisinopril are reduced, bioavailability is 16%.

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

    Indications:

    Arterial hypertension (in monotherapy or in combination with other antihypertensive drugs).

    Chronic heart failure (as part of combination therapy to treat 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).

    Contraindications:

    Hypersensitivity to lisinopril or other ACE inhibitors. Angioedema in history, including with the use of ACE inhibitors. Hereditary edema Quincke or idiopathic angioedema.

    Pregnancy and lactation.

    Age to 18 years (effectiveness and safety not established).

    Carefully:Severe renal dysfunction, bilateral renal artery stenosis or arterial stenosis of a single kidney with progressive azotemia, condition after kidney transplantation, azotemia, hyperkalemia, aortic aortic stenosis, hypertrophic obstructive cardiomyopathy, primary hyperaldosteronism, arterial hypotension, cerebrovascular diseases (including cerebral circulatory insufficiency ), ischemic heart disease, coronary insufficiency, autoimmune systemic connective tissue diseases (including chi le scleroderma,systemic lupus erythematosus); oppression of bone marrow hematopoiesis; diet with restriction of table salt; hypovolemic conditions (including as a result of diarrhea, vomiting); old age, hemodialysis using high-permeability dialysis membranes with high permeability (AN69®).
    Pregnancy and lactation:

    The use of Listril® during pregnancy is contraindicated.

    When establishing a pregnancy, taking Listril® should be stopped 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, renal 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.

    Lizinopril penetrates the placenta. There is no data on the isolation of lisinopril in breast milk.If taking Listril® is necessary during lactation, 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 antihypertensives use 5 mg each (1 tablet of 5 mg or 1/2 tablet of 10 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.

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

    If the patient received prior treatment with diuretics, the use of such drugs should be discontinued 2-3 days before Listril® is used. If this is not possible, the initial dose of Listril® 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 there may be a pronounced decrease in blood pressure.

    In the case of renovascular hypertension or other conditions with increased activity of the renin-angiotensin-aldosterone system, it is also advisable to prescribe a low initial dose of 5 mg per day (1 tablet of 5 mg or 1/2 tablet of 10 mg) under enhanced medical supervision (blood pressure control, function kidneys, potassium content in the blood serum). The maintenance dose, continuing strict medical control, should be determined depending on the dynamics of blood pressure.

    With renal failure due to the fact that lisinopril the initial dose should be determined depending on the creatinine clearance. Further, the selection of doses should be made depending on individual reactions with regular monitoring of kidney function, potassium, sodium in the blood serum.

    Creatinine clearance ml / min

    Initial dose of mg / day

    30-70

    5-10

    10-30

    5

    (including patients who are on hemodialysis).

    With persistent arterial hypertension, prolonged maintenance therapy of 1-15 mg / day is shown.

    In chronic heart failure: the initial dose of 2.5 mg ((1/2 tablets of 5 mg or 1/4 tablets of 10 mg) per day, with a gradual increase in 3-5 days to 5-10 mg per day. daily dose of 20 mg.

    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.

    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.

    Side effects:

    The frequency of occurrence, side effects is characterized as often (≥ 1%), rarely (<1%).

    The most common side effects: dizziness, headache, fatigue, diarrhea, dry cough, nausea.

    From the cardiovascular system: often - marked decrease in blood pressure, orthostatic hypotension; rarely - chest pain, tachycardia, bradycardia, aggravation of symptoms of chronic heart failure, violation of atrioventricular conduction, myocardial infarction.

    From the central nervous system: often - paresthesia, lability of mood, confusion, drowsiness, convulsive twitching of the muscles of the extremities and lips, rarely asthenic syndrome.

    From the hematopoiesis: rarely - leukopenia, neutropenia, agranulocytosis, thrombocytopenia, with long-term treatment - anemia (reduction of hemoglobin, hematocrit, erythropenia).

    From the respiratory system: rarely shortness of breath, bronchospasm.

    From the digestive system: rarely dryness of the oral mucosa, anorexia, dyspepsia, taste changes, abdominal pain, pancreatitis, jaundice (hepatocellular or cholestatic), hepatitis.

    From the skin: rarely - urticaria, pruritus, increased sweating, alopecia, photosensitivity.

    From the genitourinary system: rarely - a violation of kidney function, oliguria, anuria, acute renal failure, uremia, proteinuria, decreased potency.

    Laboratory indicators: often - hyperkalemia, hyponatremia; rarely - hyperbilirubinemia, increased activity of "hepatic" transaminases, hypercreatininaemia, increased concentrations of urea and creatinine.

    Allergic reactions: rarely angioedema, swelling of the face, limbs, lips, tongue, epiglottis and / or larynx, skin rashes, itchy skin, fever, false positive antinuclear antibody test results, increased erythrocyte sedimentation rate (ESR), eosinophilia, leukocytosis.In rare cases, there is an intestinal angioedema.

    Other: rarely - arthralgia / arthritis, vasculitis, myalgia.

    Overdose:

    Symptoms (occur when taking a single dose of 50 mg): 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 monitor blood pressure, indicators of water-electrolyte balance. Hemodialysis is effective.

    Interaction:

    With the simultaneous use of the drug with potassium-sparing diuretics (spironolactone, triamterene, amiloride), potassium preparations, salt substitutes containing potassium, cyclosporine, increases the risk of hyperkalemia, especially with impaired renal function, so they can be used together only with regular monitoring of potassium ions in the blood serum and kidney function.

    The combined use of lisinopril, with beta-blockers, slow calcium channel blockers (BCCI), diuretics, tricyclic antidepressants / neuroleptics and other antihypertensive drugs increases the severity of hypotensive action.

    Lizinopril slows down the excretion of lithium preparations. Therefore, when combined, it is necessary to regularly monitor the concentration of lithium in the blood serum.

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

    When combined with insulin and hypoglycemic agents for oral administration, there is a risk of developing hypoglycemia.

    Non-steroidal anti-inflammatory drugs (NSAIDs) (including selective inhibitors of cyclooxygenase-2 (COX-2)), estrogens, adrenomimetics reduce the hypotensive effect of lisinopril.

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

    When combined with selective serotonin reuptake inhibitors, it can lead to severe hyponatraemia.

    Joint application with allopurinol, procainamide, cytostatics can lead to leukopenia.

    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 simultaneous renal insufficiency or without it, a marked decrease in blood pressure is possible.

    Under the strict supervision of a doctor, Listril should be used in patients with coronary heart disease, cerebrovascular insufficiency, in which a sharp decrease in blood pressure may lead to myocardial infarction or to a stroke. Transient arterial hypotension is not a contraindication for taking the next dose of the drug.

    When Listril® is used, 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 a reason for stopping 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 Listril® on the patient.

    In the case of renal artery stenosis (especially when bilateral stenosis or in the presence of artery stenosis single kidney) and circulatory failure due to lack of ions of sodium and / or liquid, use Listril® drug can lead to renal failure, acute renal failure, which is usually irreversible even after drug withdrawal.

    With acute myocardial infarction

    The use of standard therapy (thrombolytics, acetylsalicylic acid, beta-blockers). Listril® may be used in conjunction with intravenous or using therapeutic transdermal nitroglycerin systems.

    Surgery / general anesthesia

    With extensive surgical procedures, as well as the use of other means, causing a decrease in blood pressure, Listril® by blocking the formation of angiotensin, II, can cause unpredictable pronounced decrease in BP.

    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.Because the potential risk of agranulocytosis can not be ruled out, periodic monitoring of the blood picture is required. When the drug is used in dialysis with polyacrylate-nitrile membranes, anaphylactic shock may occur, so either a different type of dialysis membrane or other antihypertensive agents is recommended.

    Effect on the ability to drive transp. cf. and fur:There is no data on the effect of Listril® on the ability to drive vehicles and mechanisms, applied in therapeutic doses, but it must be borne in mind that at the beginning of treatment it is possible to develop arterial hypotension, which can affect the ability to drive vehicles and work with potentially dangerous mechanisms, and there may be dizziness and drowsiness, so be careful.
    Form release / dosage:Tablets of 5 and 10 mg.
    Packaging:10 tablets in Al / Al. blister. 3 blisters in together with instructions for use in a cardboard pack.
    Storage conditions:

    Store at a temperature of no higher than 30 C in a place protected from moisture.

    Keep out of the reach of children.

    Shelf life:

    3 years.

    The drug should not be used after the expiry date indicated on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:П N012046 / 01
    Date of registration:24.02.2011
    Expiration Date:Unlimited
    The owner of the registration certificate:Torrent Pharmaceuticals Co., Ltd.Torrent Pharmaceuticals Co., Ltd. India
    Manufacturer: & nbsp
    Representation: & nbspTORRENT PHARMACEUTICALS LTD. TORRENT PHARMACEUTICALS LTD. India
    Information update date: & nbsp11.04.2018
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