Active substanceLisinoprilLisinopril
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  • Dosage form: & nbsptabscesses
    Composition:

    Each tablet contains:

    active substance: lisinopril dihydrate equivalent to 5, 10 or 20 mg of lisinopril;

    Excipients: mannitol, calcium dihydrogen phosphate, iron oxide red, corn starch, pregelatinized starch, magnesium stearate.

    Description:

    Round, bulging pills of pink color.Marble and minor inclusions are possible.

    Pharmacotherapeutic group: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 onset of the effect occurs 2 hours after taking the drug. The maximum effect occurs in 4-6 hours and lasts at least 24 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 lead to an increase in cases of hypoglycemia.

    Pharmacokinetics:

    Bioavailability of the drug when taken orally is about 25-50% of the dose. The intake does not affect the absorption. The maximum concentration in the blood plasma is achieved in 6-7 hours.

    Lizinopril does not bind to plasma proteins, practically does not undergo metabolism in the body and is excreted unchanged in urine, most of it is released during the initial phase (effective 12.6 hours), followed by a terminal, distant phase (about 30 hours).

    Permeability through the blood-brain and placental barrier is low.

    Indications:

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

    - Chronic heart failure (as part of combination therapy to treat patients taking digitalis and / or diuretics).

    - Early treatment of 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 (decrease in albuminuria in insulin-dependent patients with normal BP and insulin-independent patients with arterial hypertension).

    Contraindications:

    Hypersensitivity to the active ingredient - lisinopril and auxiliary components of the tablet, as well as to other ACE inhibitors.

    Angioedema in history, 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 stenosis, hypertrophic obstructive kardiomipatiya, primary hyperaldosteronism, hypotension, cerebrovascular diseases (including cerebrovascular insufficiency), ischemic heart disease, coronary insufficiency, autoimmune disease systemic connective tissues (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.

    In the treatment of hypertension patients who do not receive other antihypertensive drugs, the initial dose is 5 mg once a day. If the effect is insufficient, 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 prior treatment with diuretics, then the use of such drugs should be stopped 2-3 days before the application of Dapril®.If this is not feasible, the initial dose of Dapril® 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.

    With 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 (control of blood pressure, kidney function, potassium concentration in 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 kidney function, potassium level, 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

    2,5

    (including patients receiving hemodialysis treatment)

    With persistent arterial hypertension, prolonged maintenance therapy at a dose of 10-15 mg / day is indicated.

    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, supporting a daily dose of 5-20 mg. The dose should not exceed 20 mg per day.

    In elderly people often more pronounced prolonged hypotensive effect, 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 a dose of 2.5 mg. 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.more than 1 hour), treatment with Dapril® should be stopped.

    Diabetic Nephropathy

    In patients with insulin-dependent diabetes mellitus, 10 mg of lisinopril 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 non-insulin dependent diabetes mellitus, the dosage is the same, in order to achieve diastolic blood pressure values ​​below 90 mm Hg. in the sitting position.

    Side effects:

    In general, Dapril® is well tolerated.

    The most common side effects: dizziness, headache (5-6% of patients), weakness, diarrhea, dry cough (3%), nausea, vomiting, orthostatic hypotension, skin rash, chest pain (1-3%).

    Other side effects:

    From the blood and lymphatic system: less than 0.01% of cases - oppression of bone marrow hematopoiesis, anemia, thrombocytopenia, leukopenia, neutropenia, agranulocytosis, hemolytic anemia, autoimmune diseases, erythrocyte sedimentation rate acceleration (ESR) syndrome; from 0.01% to 0.1% of cases - a decrease in the concentration of hemoglobin and hematocrit.

    From the side of the cardiovascular system: less than 1% - a marked decrease in blood pressure, heart rhythm disturbances, tachycardia, cerebrovascular stroke in patients with an increased risk of the disease, due to a marked decrease in blood pressure, myocardial infarction, orthostatic hypotension

    From the immune system: 0.1% - angioedema (face, lips, tongue, larynx or epiglottis, upper and lower extremities), the appearance of antinuclear antibodies.

    From the central nervous system: less than 1% - increased fatigue, drowsiness, convulsive twitching of muscles, limbs and lips, asthenic syndrome, confused consciousness, mood lability, decreased potency;

    Laboratory indicators: less than 1% - hyperkalemia, azotemia, hyperuricemia, hyperbilirubinemia, increased activity of "hepatic" enzymes, especially in the presence of a history of kidney disease, diabetes and renosvascular hypertension.

    From the skin: from 0,01 to 0,1% of cases - hives, increased sweating, skin itching, alopecia. Less than 0.01% - pemphigus, Stevens-Johnson syndrome.

    From upper and lower respiratory tract disorders: less than 0.01% - bronchospasm, sinusitis, eosinophilic pneumonia; from 0,1 to 1% of cases - rhinitis; from 1,0 to 10% of cases - cough

    Other: myalgia, arthralgia, fever, impaired development of the fetus.

    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 fluids, blood pressure control, 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 the additional administration of a diuretic to the patient, receiving Dapril®, 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 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:

    Symptomatic hypotension

    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 concomitant renal insufficiency or without it, a marked decrease in blood pressure is possible, which is observed in patients with a severe stage of chronic heart failure, as a result of the use of large doses of diuretics, hyponatremia or pronounced impairment of renal function.In such patients, treatment with Dapril® should be started under the strict supervision of the doctor (with care to select the 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.

    Before the treatment with Dapril®, if possible, normalize the sodium concentration and / or replenish the lost volume of the liquid, carefully monitor the effect of the initial dose of the drug on the patient.

    In the case of renal artery stenosis (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 Dapril® can lead to impaired renal function, acute renal failure, which usually turns out to be irreversible after drug discontinuation.

    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, 5 mg, 10 mg and 20 mg.

    Packaging:

    For 10 tablets in PVC / aluminum blister.

    By 3 blisters (tablets of 5 mg and 10 mg) together with instructions for use in a cardboard box.

    2 blisters each (tablets of 20 mg) together with instructions for use in a cardboard pack.

    Storage conditions:

    Store in a dry, dark place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.
    Shelf life:4 years.

    Do not use after the time specified on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:П N012855 / 01
    Date of registration:24.12.2007
    Expiration Date:Unlimited
    The owner of the registration certificate:Medocemi Co., Ltd.Medocemi Co., Ltd. Cyprus
    Manufacturer: & nbsp
    Representation: & nbspMEDOKEMI LTD. MEDOKEMI LTD. Cyprus
    Information update date: & nbsp18.03.2017
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