Active substanceLisinoprilLisinopril
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  • Dosage form: & nbsppills
    Composition:

    Ingredients

    Amount in tablet, mg

    2.5 mg

    5.0 mg

    10.0 mg

    20.0 mg

    Active substance:





    Lisinopril

    2,76*

    5,520*

    11,040*

    22,080*

    Excipients:





    corn starch

    86,0

    86,330

    82,685

    80,670

    calcium phosphate dibasic anhydrous

    39,97

    36,875

    35,0

    26,0

    dye yellow sunset FSF

    -

    0,0250

    -

    -

    quinoline yellow dye

    -

    -

    0,025

    -

    diamond blue

    0,020

    -

    -

    -

    talcum pure

    2,50

    2,50

    2,50

    2,50

    Silica colloidal dioxide

    0,50

    0,50

    0,50

    0,50

    sodium starch glycolate

    7,0

    7,0

    7,0

    7,0

    magnesium stearate

    1,25

    1,25

    1,25

    1,25

    * - quantities of lisinopril dihydrate corresponding to the content of lisinopril, including 1.5% excess, consumed during processing of the preparation are indicated.
    Description:

    Lizinopril 2.5 mg. From white to almost white, round, biconvex tablets.

    Lizinopril 5.0 mg. Pinkish-beige, round, flat with chamfer tablets, having a risk on one side.

    Lizinopril 10.0 mg. Yellow, round, flat with a chamfer, having a risk on one side.

    Lizinopril 20.0 mg. From white to almost white, round, flat with a chamfer tablet, having a risk on one side.

    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, blood pressure (BP),preload, pressure in the pulmonary capillaries, causes an increase in the minute volume of blood and an increase in myocardial tolerance 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. 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, stored for 24 hours. The duration of action also depends on the size of the dose. 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. 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:

    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%. 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.

    Lizinopril is not biotransformed in the body, it is excreted by the kidneys unchanged. The half-life is 12 hours.

    In patients with chronic heart failure, absorption and clearance of lisinopril are reduced, bioavailability is 16%.

    Impaired renal function leads to an increase in AUC (area under the curve "plasma concentration-time") and half-life of lisinopril, but these changes become clinically significant only when the glomerular filtration rate decreases below 30 ml / min.

    In patients with liver cirrhosis, bioavailability is reduced by 30%, and clearance by 50%.

    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 drugs);

    - 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 (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 type 1 diabetes mellitus with normal blood pressure and patients with type 2 diabetes mellitus with arterial hypertension).

    Contraindications:Hypersensitivity to lisinopril or other ACE inhibitors, angioedema in the history, including the use of ACE inhibitors, idiopathic angioedema, hereditary edema of Quincke, age under 18 years (efficacy and safety not established).
    Carefully:Expressed human kidney, bilateral renal artery stenosis or artery stenosis only kidneys with progressive azotemia, condition after kidney transplantation, renal insufficiency, azotemia, hyperkalemia, aortic stenosis, hypertrophic obstructive kardiomipatiya, primary hyperaldosteronism, hypotension, cerebrovascular disease (ie. h. cerebral circulatory insufficiency), ischemic heart disease, coronary insufficiency, autoimmune systemic diseases will connect (including scleroderma, systemic lupus erythematosus); oppression of bone marrow hematopoiesis; diet with restriction of table salt; 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. Lisinopril penetrates the placental barrier. Admission of ACE inhibitors in the II and III trimesters 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 Lizakard 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.

    During the treatment with Lizakard, breastfeeding should be abolished (there is no data on the penetration of lisinopril into breast milk).

    Dosing and Administration:

    Inside, once a day in the morning, regardless of food intake, preferably at the same time.

    With 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 therapeutic 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, simultaneous use of the drug with other antihypertensive drugs is possible.

    If the patient received prior treatment with diuretics, the use of such drugs should be stopped 2-3 days before the Lizakard preparation is started. If this is not feasible, the initial dose of Lizakard 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 chronic heart failure - begin with 2.5 mg 1 time per day, followed by an increase in the dose of no more than 10 mg with an interval of at least 2 weeks. The dose should not exceed 20 mg per day.

    In elderly people, 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 begin treatment with 2.5 mg / day). Acute myocardial infarction (as part of combination therapy): on the first day - 5 mg orally, then 5 mg every other 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 blood pressure (120 mm Hg.or lower), a smaller dose of 2.5 mg should be given. In the case of a decrease in blood pressure (systolic blood pressure is below or equal to 100 mm Hg), a daily dose of 5 mg can, if necessary, temporarily reduce to 2.5 mg. 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 Lizakard should be stopped.

    Diabetic nephropathy: in patients with type 1 diabetes mellitus, 10 mg of Lizakard is administered once a 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 type 2 diabetes mellitus, the dosage is the same, in order to achieve diastolic blood pressure values ​​below 90 mmHg. in the "sitting" position.

    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, renal function, serum potassium concentration). The maintenance dose, continuing strict medical control, should be determined depending on the dynamics of blood pressure.

    In patients with renal insufficiency and patients on hemodialysis, the initial dose is set depending on the level of creatinine clearance less than 10, including patients on hemodialysis. The maintenance dose is determined depending on blood pressure (under the control of kidney function, the level of potassium and sodium in the blood).

    Creatinine clearance ml / min

    Initial dose of mg / day

    30-70

    5-10

    10-30

    2,5-5

    Less than 10

    2,5

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

    Side effects:

    The incidence of side effects is classified according to the recommendations of the World Health Organization: very often - not less than 10%; often - not less than 1%, but less than 10%; infrequently - not less than 0,1%, but less than 1%; rarely - not less than 0.01%, but less than 0.1%; very rarely - less than 0.01%; often - is unknown.

    From the cardiovascular system: often - marked decrease in blood pressure, orthostatic hypotension; infrequently - acute myocardial infarction or stroke, tachycardia, palpitations, Raynaud's syndrome.

    From the central nervous system: often - dizziness, headache; infrequently - lability of mood, paresthesia, sleep disturbance, asthenia; rarely confusion, impaired vision; the frequency is unknown - depression, fainting.

    From the hemopoietic system and lymphatic system: rare-reduction of hemoglobin, hematocrit; Very rarely - leukopenia, neutropenia, agranulocytosis, thrombocytopenia, hemolytic anemia, lymphadenopathy, autoimmune diseases, oppression of bone marrow hematopoiesis, eosinophilia and leukocytosis.

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

    From the digestive system: often - diarrhea, vomiting; infrequently-dissipation, changes in taste, abdominal pain; rarely dryness of the oral mucosa; Very rarely - pancreatitis, jaundice (hepatocellular or cholestatic), hepatitis, hepatic insufficiency, intestinal edema.

    From the skin: infrequently - skin itching, rash, angioedema, swelling of the face, limbs, lips, tongue, larynx; rarely-urticaria, alopecia, psoriasis; very rarely - increased sweating, pemphigus, toxic epidermal necrolysis (Lyell's syndrome), erythema multiforme, Stevens-Johnson syndrome, vasculitis, exanthema, photosensitivity reactions.

    From the urinary system: often - renal dysfunction; rarely uremia, acute renal failure; very rarely anuria, oliguria.

    On the part of the reproductive system: infrequently - impotence, rarely - ginekomastia.

    From the side of metabolism: very rarely - hypoglycemia.

    From the endocrine system: rarely - the syndrome of impaired secretion of antidiuretic hormone.

    From the laboratory indicators: infrequently - increased urea concentration in the blood, hypercreatininaemia, hyperkalemia, increased activity of "liver" transaminases; rarely - hyperbilirubinemia; hyponatremia; very rarely - an increase in ESR, a positive test for antinuclear antibodies.

    Other: very rarely - fever, myalgia, myositis, arthralgia, arthritis, serositis.

    With the simultaneous administration of ACE inhibitors and intravenous sodium aurotomyalate, a symptom complex including facial flushing, nausea, vomiting and arterial hypotension is described.

    Overdose:

    Symptoms: marked decrease in blood pressure; dry mouth, drowsiness, urinary retention, constipation, anxiety, increased irritability, disturbance of water-electrolyte balance,renal failure, rapid breathing, tachycardia, palpitations, bradycardia, dizziness, anxiety, cough.

    Treatment: symptomatic therapy, gastric lavage, intake of adsorbents, intravenous injection of 0.9% sodium chloride solution and other plasma-substituting solutions; if necessary - vasopressor drugs, control of blood pressure, water-electrolyte balance and normalization of the latter. Lisinopril can be removed from the body by hemodialysis. It is possible to develop anaphylactoid reactions during hemodialysis using high-flow membranes.

    Interaction:

    Special care is required when using the drug simultaneously with potassium-sparing diuretics (spironolactone, triamterene, amiloride, eplerenone), potassium preparations, potassium-containing substitutes for table salt - increases the risk of hyperkalemia, especially in patients with impaired renal function. Therefore, they can be jointly administered only on the basis of an individual decision of the attending physician with regular monitoring of potassium level in the blood serum and kidney function.

    It is recommended to use with caution at the same time as:

    - non-steroidal anti-inflammatory drugs (NSAIDs) (including selective inhibitors of cyclooxygenase-2 (COX-2)), estrogen, adrenostimulants reduce hypotensive effect of lisinopril;

    - lithium - lithium release may decrease, therefore, the concentration of lithium in serum should be monitored regularly;

    - antacids and colestyramine - reduce absorption in the gastrointestinal tract;

    - NSAIDs with ACE inhibitors and angiotensin II receptor antagonists - the possibility of hypokalemia and renal insufficiency. Allopurinol, cytostatics, immunosuppressants, glucocorticosteroids (GCS), procainamide when used together with lisinopril may cause leukopenia.

    Joint use of the drug Lizakard with beta-blockers, slow calcium channel blockers (BCCC), diuretics, tricyclic antidepressants / neuroleptics and other antihypertensive drugs increases the severity of hypotensive action.

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

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

    Ethanol enhances the action of the drug Lizakard.

    Special instructions:

    Most often, a marked decrease in blood pressure occurs with a decrease in fluid volume caused by diuretic therapy, a decrease in table salt in the diet, dialysis, diarrhea, or vomiting. In patients with chronic heart failure with simultaneous renal failure or without it, the development of symptomatic arterial hypotension is possible.

    It is more often detected in patients with a severe stage of chronic heart failure, as a result of the use of large doses of diuretics, hyponatremia or impaired renal function. In such patients, treatment with Lizakard should be started under the strict supervision of a doctor (with care to select the dose of the drug and diuretics).

    Similar rules should be adhered to when appointing patients with coronary heart disease, cerebrovascular insufficiency, in which a sharp decrease in blood pressure can lead to myocardial infarction or stroke.

    Transient decrease in blood pressure is not a contraindication for taking the next dose of the drug.

    When using the drug Lizakard, 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 starting treatment with Lizakard, if possible, normalize the sodium concentration and / or replace lost fluid, carefully monitor the effect of the initial dose of the drug on the patient.

    In the case of stenosis of the renal artery (especially with bilateral stenosis, or in the presence of stenosis of the artery of a single kidney), as well as inadequate blood circulation due to lack of sodium and / or liquid, the use of lisinopril can lead to impaired renal function, acute renal failure, irreversible after drug discontinuation.

    The drug Lizakard can be used together with intravenous administration or with the use of therapeutic transdermal systems of nitroglycerin.

    ACE inhibitors can be used together with beta-blockers, thrombolytic agents and antiplatelet agents, including acetylsalicylic acid in doses no more than 300 mg / day.

    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. Anaphylactic shock can develop in hemodialysis patients using high-flow dialysis membranes (AN69®) that take ACE inhibitors, so either a different type of dialysis membrane or other antihypertensive agents is recommended.

    Sometimes anaphylactic reactions developed in patients taking ACE inhibitors when desiccating the venom of Hymenoptera (eg, wasps or bees). These reactions were avoided in the same patients by temporarily stopping the administration of ACE inhibitors, but after an inadvertent re-use of the drug, the reactions were restored.

    Very rarely, ACE inhibitors were associated with a syndrome that begins with cholestatic jaundice and progresses rapidly to liver necrosis and (sometimes) death. The mechanism of this syndrome is not established. Patients who have developed jaundice with lisinopril or have a significant increase in hepatic enzymes should be withdrawn and appropriate medical care should be provided.

    After the application of ACE inhibitors, a cough may appear. Usually, cough is unproductive and stops after the treatment is canceled. Cough caused by ACE inhibitors should be considered in the differential diagnosis of cough as one of the possible options.

    In patients with diabetes mellitus, taking oral antidiabetics or insulin, it is necessary to carry out constant glycemic control during the first month of therapy with ACE inhibitors.

    In apheresis with dextrin sulfate, the use of ACE inhibitors can lead to anaphylactic reactions that can threaten life. Before prescribing the drug should carefully assess the risk / benefit ratio in the following cases: anaphylactoid reactions,angioedema in history; severe violations of the liver and kidneys, including bilateral stenosis of the renal arteries or stenosis of the renal artery of a single kidney, a condition after a kidney transplant; stenosis of the aortic or mitral valve, or other obstructive changes that hinder the flow of blood from the heart; collagenoses; oppression of bone marrow function; cerebrovascular insufficiency, hypotension; gout; hypercalcemia or a high risk of its development (diabetes mellitus, concurrent use with potassium-sparing diuretics); hyponatremia or restriction of sodium in the diet, hyperuricemia.

    With special care (in a hospital), the drug is prescribed to patients with malignant hypertension or hypertension of renal origin, in conditions accompanied by a decrease in BCC. The drug should be treated under regular medical supervision. In acute myocardial infarction with ST segment elevation, treatment with lisinopril should be started within the first 24 hours after the onset of symptoms, provided there is no arterial hypotension, hypovolemia, renal insufficiency,In patients with clinical signs of heart failure, with a reduced fraction of left ventricular ejection, hypertension, diabetes mellitus lisinopril is the drug of choice. During therapy with the drug, regular monitoring of blood pressure, kidney function, hemogram parameters, body weight, as well as protein and potassium levels in blood plasma, urea and creatinine, and diet compliance are necessary. Angioneurotic edema of the face, extremities, lips, tongue, larynx in patients taking ACE inhibitors is very rare, with patients with angioedema edema of any etiology in history. Angioedema of the larynx can be fatal and requires urgent therapy. If swelling occurs only on the face and lips, it usually passes by itself. Anti-histamines have a positive effect. If the edema in the area of ​​the tongue, throat or larynx is localized and the threat of the development of airway obstruction should be immediately introduced sc: epinephrine rp 1: 1000 (0.3-0.5 ml) or 0.1 ml iv. When used simultaneously with anesthetics that have an antihypertensive effect, during surgery lisinopril can block the formation of angiotensin II, increasing (secondary) renin activity of blood plasma, which can be eliminated by increasing the BCC. Before surgery (including dental surgery), the surgeon / anesthesiologist should be alerted to the use of lisinopril by the patient. During treatment it is recommended to refrain from drinking alcoholic beverages because of the risk of increasing the antihypertensive effect. Care should be taken with physical exertion, especially in hot weather, because of the risk of developing dehydration and increasing antihypertensive effect as a result of a decrease in bcc.

    Effect on the ability to drive transp. cf. and fur:There is no evidence of the effect of Lizakard preparation, applied in therapeutic doses, on the ability to drive vehicles and mechanisms, but it must be taken into account that dizziness may occur, so caution should be exercised.
    Form release / dosage:Tablets of 2.5 mg, 5 mg, 10 mg and 20 mg.
    Packaging:

    By 5, 7, 10 or 14 tablets in a blister of PVC / aluminum foil.

    For 1, 2, 3, 4, 5 or 10 blisters are placed in a cardboard pack together with instructions for use.

    Storage conditions:

    In a dry 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.

    Terms of leave from pharmacies:On prescription
    Registration number:LS-001761
    Date of registration:30.11.2011
    Expiration Date:Unlimited
    The owner of the registration certificate:Shraya Life Senses Pvt. Ltd.Shraya Life Senses Pvt. Ltd. India
    Manufacturer: & nbsp
    Representation: & nbspSHREYA LIFE SENENSIZ Pvt.Ltd. SHREYA LIFE SENENSIZ Pvt.Ltd. India
    Information update date: & nbsp26.02.2018
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