Active substanceCaptoprilCaptopril
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  • Dosage form: & nbsppills
    Composition:

    1 the tablet contains:

    active substance: captopril 25 mg or 50 mg;

    Excipients: granulate Ludipress (lactose monohydrate, povidone, crospovidone), magnesium stearate or lactose monohydrate, povidone, crospovidone, magnesium stearate.

    Description:

    Tablets of white color flat-cylindrical with a facet and a risk (Captopril 25 mg) or with a crosswise risk (Captopril 50 mg), with a characteristic odor. A slight unevenness of the surface is permissible.

    Pharmacotherapeutic group:Angiotensin converting enzyme inhibitor
    ATX: & nbsp

    C.09.A.A.01   Captopril

    Pharmacodynamics:

    Captopril is an inhibitor of the angiotensin-converting enzyme (ACE). Reduces the formation of angiotensin II from angiotensin I. Reduction in angiotensin II leads to a direct reduction in the release of aldosterone. This reduces the overall peripheral vascular resistance, blood pressure, post- and preload on the heart. Expands arteries more than veins.It causes a decrease in the degradation of bradykinin (one of the effects of ACE) and an increase in the synthesis of prostaglandin.

    The hypotensive effect does not depend on the plasma renin activity, the decrease in blood pressure is noted at a normal and even lowered level of the hormone, which is due to the effect on tissue renin-angiotensive systems. Strengthens coronary and renal blood flow.

    With prolonged use reduces the severity of myocardial hypertrophy and the walls of arteries of resistive type. Improves the blood supply of the ischemic myocardium. Reduces the aggregation of platelets. Helps reduce sodium ions in patients with heart failure.

    Reduction of blood pressure (AD), in contrast to direct vasodilators (hydrazine, minoxidil, etc.) is not accompanied by reflex tachycardia and leads to a decrease in myocardial oxygen demand. With heart failure in an adequate dose does not affect the value of blood pressure.

    The maximum decrease in blood pressure after oral administration is observed after 60-90 minutes. The duration of the hypotensive effect is dose-dependent and reaches optimal values ​​within a few weeks.

    Pharmacokinetics:

    Absorption - fast, reaches 75% (food intake decreases by 30-40%), bioavailability - 35-40% (the effect of "first pass" through the liver). Connection with blood plasma proteins (mainly with albumins) - 25-30%; the maximum concentration in the blood plasma (114 ng / ml) with oral intake - 30-90 min. Through the blood-brain barrier and placental barrier penetrates poorly (less than 1%).

    Metabolized in the liver with the formation of disulfide dimer captopril and captopril-cysteine ​​disulfide. Metabolites are pharmacologically inactive.

    The half-life is 3 hours; is excreted by the kidneys 95% (40-50% unchanged), the rest in the form of metabolites. It is secreted with mother's milk. After 4 hours after a single oral intake, 38% of unchanged captopril and 28% of metabolites are contained in the urine, in 6 hours only in the form of metabolites; in daily urine - 38% of unchanged captopril and 6% - in the form of metabolites.

    The half-life period for impaired renal function is 3.5-32 hours. Cumulates in chronic renal failure.
    Indications:

    Arterial hypertension, including renovascular; chronic heart failure (as part of a combinedtherapy); violations of left ventricular function after a myocardial infarction with a clinically stable condition; Diabetic nephropathy on 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 on hemodialysis, a diet with restriction of sodium, primary hyperaldosteronism,ischemic heart disease, conditions accompanied by a decrease in the volume of circulating blood (including vomiting, diarrhea), advanced age (dose adjustment is required).

    Pregnancy and lactation:

    The drug is contraindicated in pregnancy and during the period of feeding.

    At the onset of pregnancy, the drug should be stopped immediately.
    Dosing and Administration:

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

    With arterial hypertension. Captopril appoint an initial dose of 12.5 mg 2 times 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 appoint in those cases when 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.

    When violations of left ventricular function after a heart attack myocardiumand 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 prescribe 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 can be prescribed in 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 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, loop diuretics are prescribed, and not thiazide diuretics.

    Side effects:

    From the cardiovascular system: orthostatic hypotension, tachycardia, peripheral edema, lowering 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.

    From the 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:

    Increases the concentration of digoxin in the blood plasma by 15-20%.

    Increases the bioavailability of propranolol.

    Cimetidine, by slowing the metabolism in the liver, increases the concentration of captopril in the blood plasma.

    Combination with thiazide diuretics, vasodilators (minoxidil), verapamil, beta-adrenoblockers, tricyclic antidepressants, ethanol enhances the hypotensive effect of Captopril.

    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 joint use of captopril with estrogens and indomethacin (and, possibly, with other nonsteroidal anti-inflammatory drugs), hypotensive effect may decrease.

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

    Clonidine reduces the severity of the hypotensive effect of captopril.

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

    The use of captopril 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 with captopril, kidney function should be monitored. Patients with chronic heart failure are treated under close medical supervision.

    Against the background of prolonged use of Captopril, approximately 20% of patients have an increase in urea and serum creatinine by more than 20% compared to the norm or the baseline value.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, 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 by first canceling (for 4-7 days) a diuretic or increasing the intake of sodium chloride (about a week before the start of the intake), or by the appointment of Captopril at the beginning 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 less than 4000 / mm3, a general blood test is performed, below 1000 / mkl - the drug is stopped.

    In some cases, in the background of the use of ACE inhibitors, including captopril, there is an increase in the concentration of potassium in the blood serum.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 potassium concentration in the blood (for example, heparin). You should avoid the simultaneous use of potassium-sparing diuretics and potassium preparations.

    When conducting hemodialysis in patients receiving Captopril, 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, a false positive reaction can be observed 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, 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 and 50 mg.

    Packaging:For 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

    2 contour mesh packs 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.

    Keep out of the reach of children.

    Shelf life:

    3 of the year.

    Do not use after expiry date.

    Terms of leave from pharmacies:On prescription
    Registration number:P N001920 / 01
    Date of registration:09.11.2007
    Expiration Date:Unlimited
    The owner of the registration certificate:FARMAKOR PRODUCTION, LTD. FARMAKOR PRODUCTION, LTD. Russia
    Manufacturer: & nbsp
    Representation: & nbspFARMAKOR PRODUCTION LLC FARMAKOR PRODUCTION LLC Russia
    Information update date: & nbsp06.12.2017
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