Active substanceLisinoprilLisinopril
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  • Dosage form: & nbsppills
    Composition:

    Lizinopril 5 mg

    active substances: lisinopril dihydrate 5.445 mg, corresponds to 5 mg of lisinopril anhydride

    Excipients: mannitol 22 mg, calcium phosphate monosodium dihydrate 61.38 mg, corn starch 16.5 mg, pregelatinized starch 3.3 mg, silicon dioxide colloid 0.55 mg, magnesium stearate 0.825 mg.

    Lizinopril 10 mg

    active substances: lisinopril dihydrate 10.89 mg, corresponds to 10 mg of lisinopril anhydride

    Excipients: mannitol 44 mg, calcium phosphate monosodium dihydrate 122.76 mg, corn starch 33 mg, pregelatinized starch 6.6 mg, silicon dioxide colloid 1.1 mg, magnesium stearate 1.65 mg.

    Lisinopril 20 mg

    active substances: lisinopril dihydrate 21.78 mg, corresponds to 20 mg of lisinopril anhydride

    Excipients: mannitol 44 mg, calcium hydrogen phosphate dihydrate 111.87 mg, corn starch 33 mg, pregelatinized starch 6.6 mg, silicon dioxide colloid 1.1 mg, magnesium stearate 1.65 mg.

    Description:

    Tablets 5 mg - white, round, tablets having edges cut inward and risk on one side and marking "5" on the other side

    Tablets 10 mg and 20 mg - white, round, biconvex tablets, having a risk on one side and marking "10" or "20" on the other hand.

    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, 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. 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. 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, clearance of lisinopril clearance is reduced.

    In patients with renal insufficiency, the concentration of lisinopril 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 drugs), chronic heart failure (as part of combination therapy for the treatment of patients taking digitalis and / or diuretics), early treatment of acute myocardial infarction (in the first 24 hours with stable hemodynamic parameters for maintenance of these parameters and prevention of left ventricular dysfunction and heart failure), diabetic nephropathy (decrease in albuminuria in insulin-dependent patients with normal th AD and non-insulin dependent patients with hypertension).
    Contraindications:Hypersensitivity to lisinopril or other ACE inhibitors, angioedema in the anamnesis, including the use of ACE inhibitors, hereditary edema of Quincke, age under 18 years (efficacy 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, renal insufficiency, azotemia, hyperkalemia, aortic aortic stenosis, hypertrophic obstructive cardiomyopathy, primary hyperaldosteronism, arterial hypotension, cerebrovascular diseases (v. 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 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, then the medication should be stopped 2-3 days before Lysigamma is started. If this is not feasible, the initial dose of Lysigamma 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 an 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 concentration in 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, then, in accordance with the reaction, a maintenance dose should be established in conditions of frequent monitoring of kidney function, potassium level, sodium in the blood serum.

    Creatinine clearance ml / min

    Initial dose of mg / day

    30-70

    5-10

    10-30

    2,5-5

    less than 10

    2,5

    (including patients treated with hemodialysis)

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

    In chronic heart failure - begin with 2.5 mg 1 time per 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 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 less than or equal to 100 mm Hg), a daily dose of 5 mg is possible if it is necessary to 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 Lysigamma should be discontinued.

    Diabetic Nephropathy

    In patients with insulin-dependent diabetes mellitus, 10 mg of Lysigamma is applied once a day. The dose may, if necessary, be increased to 20 mg once daily to achieve diastolic blood pressure values ​​below 75 mm Hg. Art. in the sitting position. In patients with insulin-dependent diabetes mellitus, the dosage is the same, in order to achieve diastolic blood pressure values ​​below 90 mm Hg. Art. in the sitting position.

    Side effects:

    Side effects during treatment with lisinopril and other ACE inhibitors were observed with the following frequency:

    Very often (> 1/10, more than 10% of cases), Often (from> 1/100 to <1/10, in 1% to 10% of cases), infrequently (from> 1/1000 to <1/100, in 0.1% -1% of cases), Rarely (from> 1/10000 to <1/1000, in 0.01% to 0.1% of cases), Very rarely (<1/10000, less than 0.01% of cases ), including single messages.

    Organs and Systems

    Adverse Reactions

    Violations of the blood and lymphatic system

    Rarely

    Reduction of hemoglobin concentration, decrease in hematocrit

    Rarely

    Bone marrow depression, anemia, thrombocytopenia, leukopenia, neutropenia, agranulocytosis, hemolytic anemia, lymphadenopathy, autoimmune diseases

    Metabolic disorders

    Rarely

    Hypoglycaemia

    Disorders from the nervous system and mental disorders

    Often

    Dizziness, headache

    Infrequently

    Emotional lability, paresthesia, dizziness, taste disorders, sleep disturbances

    Rarely

    Confusion of consciousness

    Frequency

    unknown

    Symptoms of depression, fainting

    Disorders from the cardiovascular system

    Often

    Orthostatic conditions, including hypotension

    Infrequently

    Myocardial infarction or stroke, it is possible to develop secondary excessive hypotension in high-risk patients, palpitations, tachycardia, Raynaud's syndrome

    Disturbances from the respiratory system, chest and mediastinal organs

    Often

    Cough

    Infrequently

    Rhinitis

    Rarely

    bronchospasm, sinusitis, allergic alveolitis, eosinophilic pneumonia

    Disorders from the gastrointestinal tract

    Often

    Diarrhea, vomiting

    Infrequently

    Nausea, abdominal pain, digestive disorders

    Rarely

    Dryness of the oral mucosa

    Rarely

    Pancreatitis, angioedema, intestinal edema, hepatocellular or cholestatic hepatitis, jaundice and liver failure


    Disturbances from the skin and subcutaneous tissues

    Infrequently

    Allergic reactions (rash, itching), angioedema, facial edema, extremities, lips, tongue, vocal cords and larynx

    Rarely

    Hives, alopecia, psoriasis symptoms

    Rarely

    Increased sweating, pemphigus, toxic epidermal necrolysis, Stevens-Johnson syndrome, erythema polymorph, pseudolymphocytoma of the skin

    Disorders from the kidneys and urinary tract

    Often

    Impaired renal function

    Rarely

    Uremia, acute renal failure

    Rarely

    Oliguria, anuria

    Disorders from the reproductive system and mammary glands

    Infrequently

    Impotence

    Rarely

    Gynecomastia

    Disorders from the endocrine system

    Rarely

    syndrome of impaired secretion of anti diuretic hormone (SIADH)

    General disorders and disorders at the site of administration

    Infrequently

    Feeling tired, asthenia

    Laboratory research

    Infrequently

    Increase in the concentration of urea and creatinine in the serum, increased activity of hepatic enzymes, hyperkalemia

    Rarely

    Increased serum bilirubin concentration, hyponatraemia

    During the treatment with lisinopril, there were reports of symptoms such as fever, vasculitis, myalgia, arthralgia or arthritis, a positive response to antinuclear antibodies (ANA), increased ESR, eosinophilia, leukocytosis, rash, increased photosensitivity or other dermatological manifestations.

    Overdose:

    Symptoms (occur when taking a single dose of 50 mg): a marked decrease in blood pressure; dry mouth, drowsiness, urinary retention, constipation, anxiety, increased irritability.

    Treatment: symptomatic therapy, intravenous fluid administration, control of blood pressure, water-electrolyte balance and normalization of the latter.

    Lizinopril can be removed from the body by hemodialysis.

    Interaction:

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

    Cautiously can be applied together: with diuretics: with additional administration of a diuretic to a patient receiving Lisinopril, as a rule, there is an additive antihypertensive effect - the risk of a pronounced decrease in blood pressure;

    - with other antihypertensive agents (additive effect);

    - with non-steroidal anti-inflammatory drugs (indomethacin and others), estrogens, as well as adrenostimulators - a decrease in the antihypertensive effect of lisinopril;

    - with lithium (liberation of lithium may decrease, therefore, the concentration of lithium in the blood serum should be monitored regularly);

    - with antacids and colestyramine - reduce absorption in the gastrointestinal tract. Alcohol enhances the effect of the drug.

    Lizinopril reduces the excretion of potassium from the body when treated with diuretics.

    Special instructions:

    Most often, a marked decrease in blood pressure occurs with a decrease in fluid volume caused by diuretic therapy, a decrease in 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. 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 Lysigamma should be started under the strict supervision of a doctor (with care to select a dose of the drug and diuretics).

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

    Transient hypotensive reaction is not a contraindication for taking the next dose of the drug.

    When using Lysigamma, 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.

    Prior to treatment, if possible, Lysigamma should normalize the sodium concentration and / or replenish the lost volume of fluid, carefully monitor the effect of the initial dose of Lysigamma 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 circulation due to lack of sodium and / or liquid, the use of Lysigamma can lead to impaired renal function, acute renal failure, which usually is irreversible after drug discontinuation.

    With acute myocardial infarction

    The use of standard therapy (thrombolytics, acetylsalicylic acid, beta-blockers). Lysigamma can be used in conjunction 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 drugs 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 the drug is used in dialysis with a polyacryl-nitrile membrane, anaphylactic shock can 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 lisinopril on the ability to drive vehicles and mechanisms, applied in therapeutic doses, but it must be borne in mind that dizziness may occur, therefore, care must be taken.
    Form release / dosage:Tablets of 5, 10 and 20 mg.
    Packaging:For 10 tablets per blister, 3 blisters per cardboard pack with application instructions for use.
    Storage conditions:Store at a temperature not exceeding + 25 ° C, in a dry place, protected from light, and out of the reach of children.
    Shelf life:

    3 years.

    The drug should not be used after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LS-001739
    Date of registration:19.07.2011
    Expiration Date:Unlimited
    Date of cancellation:2018-01-16
    The owner of the registration certificate:Wörwag Pharma GmbH & Co. KG. KGWörwag Pharma GmbH & Co. KG. KG Germany
    Manufacturer: & nbsp
    Representation: & nbspVEVWAG PHARMA GmbH & Co. KG VEVWAG PHARMA GmbH & Co. KG Germany
    Information update date: & nbsp26.02.2018
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