Active substanceLisinoprilLisinopril
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  • Dosage form: & nbsppills
    Composition:For one tablet:


    2.5 mg

    5 mg




    10 mg

    20 mg

    Active substance:

    Lizinopril dihydrate (in terms of lisinopril)

    0.0025 grams


    0.0050 grams

    0.0100 g

    0.0200 grams

    Excipients:

    Mannitol

    0.0400 g


    0.0400 g

    0.0400 g

    0.0800 grams

    Corn starch

    0.0670 g


    0.0645 g

    0.0595 g

    0.1190 g

    Calcium hydrogen phosphate dihydrate

    0.0400 g

    0.0400 g

    0.0400 g

    0,0800 g

    Povidone

    0.0060 grams

    0.0060 grams

    0.0060 grams

    0.0120 g

    Croscarmellose sodium

    0.0030 grams

    0.0030 grams

    0.0030 grams

    0.0060 grams

    Magnesium stearate

    0.0015 grams

    0.0015 grams

    0.0015 grams

    0.0030 grams

    Weight of a tablet

    0.16 g

    0.16 g

    0.16 g

    0,32 g

    Description:Tablets are white or almost white in a flat-cylindrical form, with a dosage of 2.5 mg, 5 mg, 10 mg - with a bevel, a dosage of 20 mg - with a facet and a risk. Light marble is allowed.
    Pharmacotherapeutic group:Angiotensin-converting enzyme (ACE) inhibitor
    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. 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 tissue renin-angiotensin systems. With prolonged use reduces hypertrophy of the myocardium and the walls of arteries of resistive type. 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 develops after 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 h. 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, there is no pronounced increase in blood pressure.

    In addition to reducing blood pressure lisinopril reduces albuminuria. In patients with hyperglycemia contributes to the normalization of the function of the damaged glomerular endothelium.

    Lizinopril 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 taking the drug, about 25% of lisinopril is absorbed from the gastrointestinal tract. Eating does not affect the absorption of the drug.Absorption is on average 30%, bioavailability is 29%.

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

    Metabolism. Lisinopril 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.

    In patients with renal insufficiency, the concentration of lisinopril is several times higher than the concentration in the blood plasma than 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.

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

    Indications:

    - Arterial hypertension (in monotherapy or in combination with other antihypertensive agents);

    -Hronicheskaya heart failure (in a combination therapy for the treatment of patients receiving digitalis preparations and / or diuretics);

    Early Bird treatment of acute myocardial infarction (within 24 hours with stable haemodynamics to maintain these parameters and prevent left ventricular dysfunction and heart failure);

    -Diabeticheskaya nephropathy (albuminuria decline in patients with insulin-dependent diabetes mellitus and normal blood pressure in patients with non-insulin dependent diabetes mellitus and arterial hypertension).

    Contraindications:Hypersensitivity to lizinoprilu or other ACE inhibitors, angioneurotic edema history, including the use of ACE inhibitors; hereditary angioedema or idiopathic edema, age 18 years (effectiveness and safety have been established).
    Carefully:Expressed human kidney function, bilateral renal artery stenosis or artery stenosis only kidneys with progressive azotemia, condition after kidney transplantation, azotemia, hyperkalemia, aortic stenosis, hypertrophic obstructive cardiomyopathy, primary hyperaldosteronism, hypotension, cerebrovascular disease (includingcerebral circulatory insufficiency), ischemic heart disease, coronary insufficiency, autoimmune systemic connective tissue diseases (including scleroderma, systemic lupus erythematosus); oppression of bone marrow hematopoiesis; diet with sodium restriction; hypovolemic conditions (including as a result of diarrhea, vomiting); elderly age.
    Pregnancy and lactation:

    The use of lisinopril during pregnancy is contraindicated. When establishing a pregnancy, the drug should be stopped as soon as possible. ACE inhibitors in the II and III trimester of pregnancy has adverse effects on the fetus (expressed may decrease blood pressure, renal failure, hyperkalemia, skull hypoplasia, intrauterine 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 penetration of lisinopril into breast milk.For the period of treatment the drug should be abolished breastfeeding.

    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 / 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 clinical effect, it is possible to combine the drug with other antihypertensive drugs.

    If the patient received a preliminary treatment with diuretics, the use of these drugs should be stopped 2-3 days before the start of the use of lisinopril. If this is not feasible, then the initial dose of the drug Lisinopril 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 2.5-5 mg per day, under enhanced medical supervision (blood pressure control, kidney function, potassium ion 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 is released through the kidneys, 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 ions, sodium in the blood serum.

    Creatinine clearance, ml / min

    Initial dose, mg / day

    30-70

    5-10

    10-30

    2,5-5

    Less than 10

    (including patients on hemodialysis)

    2,5

    With persistent arterial hypertension, prolonged maintenance therapy of 10-15 mg / day is shown.

    With chronic heart failure - begin with 2.5 mg once a day, followed by an increase in the dose of 2.5 mg 3-5 days before the usual, maintaining a daily dose of 5-20 mg.The daily dose should not exceed 20 mg.

    In elderly patients, a more pronounced 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 at a dose of 2.5 mg / day).

    Acute myocardial infarction (as part of combination therapy)

    On the first day - 5 mg orally, then 5 mg after 1 day, 10 mg after two days and then 10 mg once a day. In patients with acute myocardial infarction, the drug should be applied for at least 6 weeks.

    At the beginning of treatment or within the first 3 days after an acute myocardial infarction in patients with low systolic BP (120 mm Hg or lower), a smaller dose of 2.5 mg should be given. In the case of a marked decrease in blood pressure (systolic blood pressure is less than or equal to 100 mm Hg), a daily dose of 5 mg can be reduced to 2.5 mg if necessary. In the case of a long pronounced decrease in blood pressure (systolic blood pressure below 90 mm Hg for more than 1 hour), treatment with the drug should be discontinued.

    Diabetic Nephropathy

    In patients with non-insulin-dependent diabetes mellitus, 10 mg of the drug Lisinopril 1 time per day. The dose may, if necessary, be increased to 20 mg once a day in order to achieve diastolic blood pressure values ​​below 75 mmHg. in the "sitting" position.

    In patients with insulin-dependent diabetes mellitus, the dose is the same: to achieve diastolic blood pressure values ​​below 90 mm Hg. in the "sitting" position.

    Side effects:

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

    Most often: dizziness, headache, fatigue, dry cough, nausea, diarrhea.

    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 limbs and lips, rarely - asthenic syndrome.

    On the part of the hematopoiesis system: rarely - leukopenia, neutropenia, agranulocytosis, thrombocytopenia, with prolonged treatment - anemia (decrease in the concentration of hemoglobin, hematocrit, erythrocytopenia).

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

    Laboratory indicators: often - hyperkalemia, hyponatremia, sometimes - hyperbilirubinemia, increased activity of "hepatic" enzymes, hypercreatininemia, increased urea and creatinine concentration in blood serum.

    From the digestive system: rarely - dryness of the oral mucosa, dyspepsia, changes in taste, anorexia, abdominal pain, pancreatitis, hepatocellular case, cholestatic jaundice, hepatitis.

    From the skin: rarely - urticaria, increased sweating, itching, alopecia, photosensitization.

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

    Allergic reactions: rarely angioedema, swelling of the face, extremities, lips, tongue, epiglottis and / or larynx, skin rashes, itching, fever, positive test results for antinuclear antibodies, increased erythrocyte sedimentation rate (ESR), eosinophilia, leukocytosis. In very rare cases - intestinal angioedema.

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

    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. Gastric lavage, application of enterosorbents and laxatives. Intravenous introduction of 0.9% sodium chloride solution was shown. 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 jointly administered only with regular monitoring of serum potassium and kidney function.

    The combined use of lisinopril with beta-blockers, slow calcium channel blockers (BCCI), diuretics, tricyclics, antidepressants / antipsychotics 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 lithium content 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, adrenostimulants reduce the hypotensive effect of lisinopril.

    With simultaneous use of ACE inhibitors and preparations of gold (sodium aurotomy malate) describes a symptom complex, which includes flushing of the facial skin, nausea, vomiting and a decrease in 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 occurs with a decrease in the volume of circulating blood (BCC), caused by diuretic therapy, a decrease in salt in the diet, 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 physician, Lisinopril patients with ischemic heart disease, cerebrovascular insufficiency, in whom a sharp decrease in blood pressure can lead to myocardial infarction or to a stroke. Transient arterial hypotension is not a contraindication for taking the next dose of the drug.

    When using lisinopril, 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 content of sodium ions and / or replenish the BCC, carefully monitor the effect of the initial dose of lisinopril on the patient.

    In the case of stenosis of the renal arteries (especially with bilateral stenosis, or in the presence of stenosis of the artery of a single kidney), as well as inadequate circulation due to lack of sodium and / or liquid ions, the use of lisinopril can lead to impaired renal function,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). Lisinopril it is possible to use together with intravenous administration or with the use of therapeutic transdermal systems of nitroglycerin.

    Surgery / general anesthesia

    With extensive surgical interventions, as well as with the use of other means that cause a decrease in blood pressure, lisinopril, blocking the formation of angiotensin II, can cause a pronounced unpredictable decrease in blood pressure.

    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 using the drug in dialysis conditions using high-flow membranes (including AN 69), anaphylactic shock may occur, therefore, it is recommended that either a different type of membrane for dialysis or the appointment of other antihypertensive agents.

    Effect on the ability to drive transp. cf. and fur:There is no data on the effect of lisinopril 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 of 2.5 mg, 5 mg, 10 mg and 20 mg.
    Packaging:

    10 tablets in a planar cell package.

    20 tablets of 20 mg or 30 tablets of 2.5 mg or 5 mg, or 10 mg in cans of light-protective glass such as BTS or in a can of BV type.

    Each jar or 1, 2 or 3 contour squares, together with instructions for use, are placed in a pack of cardboard.

    Storage conditions:In a dry, protected from light place at a temperature of no higher than 25 ° C. In a place inaccessible to children.
    Shelf life:

    2 years.

    Do not use the medicine after the expiry date indicated on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-001299/10
    Date of registration:24.02.2010 / 27.11.2017
    Expiration Date:Unlimited
    The owner of the registration certificate:Promomed Rus, Open CompanyPromomed Rus, Open Company Russia
    Manufacturer: & nbsp
    Information update date: & nbsp25.02.2018
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