Active substanceCaptoprilCaptopril
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  • Dosage form: & nbsppills
    Composition:

    1 tablet contains:

    active substance: captopril 25 mg;

    Excipients: Milk sugar (lactose), potato starch, polyvinylpyrrolidone, low molecular weight Medical (povidone), sodium lauryl sulfate, magnesium stearate, stearic acid.

    Description:

    Tablets of white or almost white color of flat-cylindrical form, with a facet, with a characteristic smell. Light marble is allowed.

    Pharmacotherapeutic group:Angiotensin converting enzyme inhibitor
    ATX: & nbsp

    C.09.A.A.01   Captopril

    Pharmacodynamics:

    Captopril-Sar® is an inhibitor of the angiotensin converting enzyme (ACE). Suppresses the formation of angiotensin II and eliminates its vasoconstrictive effect on arterial and venous vessels. Reduces the overall peripheral vascular resistance, reduces afterload, lowers blood pressure.Reduces preload, reduces pressure in the right atrium and a small circle of circulation. Reduces the secretion of aldosterone in the adrenal glands.

    Pharmacokinetics:

    When administered, the bioavailability of captopril is 60-70%. Simultaneous food intake slows the absorption of the drug by 30-40%. Communication with plasma proteins is 25-30%. Metabolised in the liver. More than 95% of captopril is excreted by the kidneys, 40-50% of which is unchanged, the rest is in the form of metabolites. The half-life period is 2-3 hours. The drug is excreted from the body mainly by the kidneys, up to 50% at unchanged form.

    Indications:- Arterial hypertension, including renovascular;

    - chronic heart failure (as part of combination therapy);

    violations of left ventricular function after a myocardial infarction with a clinically stable condition;

    - Diabetic nephropathy against the background of type 1 diabetes mellitus (for albuminuria more than 30 mg / day).

    Contraindications:

    Hypersensitivity to captopril or other ACE inhibitors; angioedema (history of therapy with ACE inhibitors or hereditary); severe violations of the liver and / or kidney function; hyperkalemia; bilateral stenosis of the renal arteries,stenosis of the artery of a single kidney with progressive azotemia, condition after kidney transplantation, stenosis of the aortic aorta and similar changes impeding the outflow of blood from the left ventricle, pregnancy, lactation, age under 18 years (efficacy and safety not established).

    Carefully:

    Severe autoimmune diseases of connective tissue (including systemic lupus erythematosus, scleroderma), oppression of bone marrow hematopoiesis (risk of neutropenia and agranulocytosis), cerebral ischemia, diabetes (increased risk of hyperkalemia), patients undergoing hemodialysis, a diet with sodium restriction, primary hyperaldosteronism, ischemic heart disease, conditions accompanied by a decrease in the volume of circulating blood (including vomiting, diarrhea), and advanced age (dose adjustment is required).

    Dosing and Administration:

    Captopril-Sar® is administered orally an hour before meals. The dosage regimen is set individually.

    When titrating the dose of the drug captopril according to the declared indications, it is necessary to use captopril in dosage form: tablets of 12.5 mg.

    With arterial hypertension Captopril is prescribed in an initial dose of 12.5 mg twice a day. If necessary, the dose gradually (with an interval of 2-4 weeks) is increased to achieve the optimal effect. With mild and moderate arterial hypertension, the usual maintenance dose is 25 mg twice a day; the maximum dose is 50 mg twice a day. With severe arterial hypertension, the initial dose is 12.5 mg 2 times a day. The dose is gradually increased to a maximum daily dose of 150 mg (50 mg 3 times per day).

    For the treatment of chronic heart failure Captopril is prescribed in cases where the use of diuretics does not provide an adequate effect. The initial daily dose is 6.25 mg 3 times a day. In the future, if necessary, the dose gradually (at intervals of not less than 2 weeks) is increased. The average maintenance dose is 25 mg 2-3 times a day, and the maximum - 150 mg per day.

    In cases of violations of left ventricular function after a previous myocardial infarction in patients in a clinically stable state, the use of captopril can begin as early as 3 days after myocardial infarction. The initial dose is 6.25 mg per day,then the daily dose can be increased to 37.5-75 mg for 2-3 doses (depending on the tolerability of captopril) up to a maximum of 150 mg per day.

    With diabetic nephropathy Captopril-Sar® is prescribed in a dose of 75-100 mg, divided into 2-3 doses. With insulin-dependent diabetes with microalbuminuria (release of albumin 30-300 mg per day), the dose of the drug is 50 mg 2 times a day. With a total protein clearance of more than 500 mg per day, the drug is effective at a dose of 25 mg 3 times per day.

    Patients with impaired renal function with a moderate degree of renal impairment (creatinine clearance (CK) of at least 30 ml / min / 1.73 m2) Captopril-Sar® can be administered at a dose of 75-100 mg / day. With a more pronounced degree of renal dysfunction (CC less than 30 ml / min / 1.73 m2) the initial dose should not exceed 12.5 mg / day; further, if necessary, with sufficiently long intervals, the dose of Captopril-Sar® is gradually increased, but a smaller, than usual, daily dose of the drug is used.

    In old age dose captopril is selected individually, therapy is recommended to start with a dose of 6.25 mg 2 times a day and, if possible, maintain it at this level.

    If necessary, additionally prescribed loop diuretics, and not diuretics thiazide series.

    Side effects:

    From the side of the cardiovascular system: orthostatic hypotension, tachycardia, peripheral edema, lowering of blood pressure.

    From the respiratory system: dry cough, usually occurring after withdrawal of the drug, bronchospasm, pulmonary edema.

    Allergic reactions: angioedema of the extremities, face, lips, mucous membranes, tongue, pharynx and larynx.

    From the central nervous system: headache, dizziness, ataxia, paresthesia, drowsiness, visual impairment.

    From the side of water-electrolyte exchange: hyperkalaemia, hyponatremia, proteinuria, increased urea nitrogen and creatinine in the blood, acidosis.

    On the part of the organs of hematopoiesis: neutropenia, agranulocytosis, thrombocytopenia, anemia, a positive test for antibodies to a nuclear antigen (rarely).

    From the digestive system: a taste disorder, dry mouth, stomatitis, increased activity of liver enzymes, abdominal pain, diarrhea, hepatitis, hyperbilirubinemia.
    Overdose:

    Symptoms: a sharp drop in blood pressure.

    Treatment: the introduction of a 0.9% solution of sodium chloride or other plasma-substituting solutions, hemodialysis.

    Interaction:

    Diuretics and vasodilators (for example, minoxidil) potentiate the hypotensive effect of Captopril-Sar®.

    With the joint use of Captopril-Sar® with estrogens and indomethacin (and, possibly, with other non-steroidal anti-inflammatory drugs), hypotensive action may decrease.

    Simultaneous use with potassium-sparing diuretics (for example, triamterene, spironolactone, amiloride), potassium preparations, potassium supplements, salt substitutes (contain significant amounts of potassium) increases the risk of hyperkalemia.

    With the simultaneous use of lithium salts, it is possible to increase the concentration of lithium in the blood serum.

    The use of captopril-Sar® in patients taking allopurinol or procainamide, increases the risk of developing neutropenia and / or Stevens-Johnson syndrome.

    The use of captopril-Sar® in patients taking immunosuppressants (for example, cyclophosphamide or azathioprine), increases the risk of hematological disorders.

    Special instructions:

    Before starting, and also regularly during the treatment of Captopril-Sar®, kidney function should be monitored.Patients with chronic heart failure are treated under close medical supervision.

    Against a background of prolonged use of Captopril-Sar®, an increase in urea and serum creatinine is observed in approximately 20% of patients compared with the norm or baseline in approximately 20% of patients. Less than 5% of patients, especially in severe nephropathies, require discontinuation of treatment due to increased creatinine concentrations.

    In patients with arterial hypertension with the use of Captopril-Sar®, severe arterial hypotension is observed only in rare cases; the likelihood of developing this condition increases with increased loss of fluid and salts (eg, after intensive treatment with diuretics), in patients with heart failure or who are on dialysis.

    The possibility of a sharp drop in blood pressure can be minimized if the diuretic is preliminarily canceled (for 4-7 days) or if the intake of sodium chloride is increased (approximately one week before the start of the intake) or by administering Captopril-Sar® at the start of treatment in small doses (6 , 25-12.5 mg / day).

    In the first 3 months of therapy, the number of blood leukocytes is monitored monthly, then - once every 3 months; in patients with autoimmune diseases in the first 3 months - every 2 weeks, then every 2 months. If the number of white blood cells is lower 4000 / μl, a general blood test is performed, below 1000 / μL - the drug is stopped.

    In some cases, in the background of the use of ACE inhibitors, including captopril-Sar®, an increase in the concentration of potassium in the blood serum is observed. The risk of hyperkalemia in the use of ACE inhibitors is increased in patients with renal insufficiency and diabetes mellitus, as well as taking potassium-sparing diuretics, potassium preparations or other drugs that cause an increase in the concentration of potassium in the blood (for example, heparin). You should avoid the simultaneous use of potassium-sparing diuretics and potassium preparations.

    When hemodialysis in patients receiving Captopril-Sar®, the use of dialysis membranes with high permeability should be avoided (for example, AN69), because in such cases the risk of anaphylactoid reactions increases.

    In the case of angioedema, the drug is withdrawn and carefully monitored.If the edema is localized on the face, special treatment is usually not required (to reduce the severity of symptoms can be used antihistamines); if the swelling spreads to the tongue, throat or larynx and there is a threat of development of airway obstruction, you should immediately enter epinephrine (epinephrine) subcutaneously (0.5 ml in a dilution of 1: 1000).

    When taking Captopril-Sar®, a false positive reaction may occur when analyzing urine for acetone.

    Be wary appoint patients who are on a low-salt or salt-free diet (increased risk of hypotension) and hyperkalemia.

    In case of symptomatic arterial hypotension after taking Captopril-Sar®, the patient should take a horizontal position with raised legs.
    Effect on the ability to drive transp. cf. and fur:During the period of treatment it is necessary to refrain from driving motor vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions. possibly dizziness, especially after taking the initial dose.
    Form release / dosage:

    Tablets of 25 mg.

    Packaging:10 tablets per contour cell packaging made of polyvinylchloride film and aluminum foil.

    2 or 4 contour mesh packages together with the instruction for use are placed in a pack of cardboard box.

    Storage conditions:

    In dry, sheltered 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 after the time specified on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-001788/07
    Date of registration:30.07.2007 / 28.09.2015
    Expiration Date:Unlimited
    The owner of the registration certificate:BIOCHEMIST, OJSC BIOCHEMIST, OJSC Russia
    Manufacturer: & nbsp
    Representation: & nbspBIOCHEMICAL JSC BIOCHEMICAL JSC Russia
    Information update date: & nbsp07.12.2017
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