Active substanceCaptoprilCaptopril
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  • Dosage form: & nbsppills
    Composition:

    1 tablet contains:

    active substance: 50 mg of captopril;

    Excipients: magnesium stearate, microcrystalline cellulose, lactose (milk sugar), corn starch, silicon dioxide colloid (aerosil).

    Description:

    Tablets are white or white with a creamy shade of color, flat-cylindrical with a facet and a risk, with a characteristic smell. A slight "marble" is allowed.

    Pharmacotherapeutic group:Angiotensin-converting enzyme inhibitor (ACE)
    ATX: & nbsp

    C.09.A.A.01   Captopril

    Pharmacodynamics:

    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 angiotensin-converting enzyme) and an increase in prostaglandin synthesis.

    The hypotensive effect does not depend on the plasma renin activity, the decrease in arterial pressure is noted at a normal and even lowered level of the hormone, which is due to the effect on tissue renin-angiotensin 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 chronic heart failure. Reduction of blood pressure in contrast to direct vasodilators (hydralazine, 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 ingestion 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 administration - 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 (T1 / 2) is 3 hours. It is excreted by the kidneys 95% (40-50% unchanged), the rest in the form of metabolites. After 4 hours after a single oral intake, 38% of unchanged captopril and 28% of metabolites are contained in the urine, after 6 hours only in the form of metabolites; in daily urine - 38% of unchanged captopril and 62% - in the form of metabolites. It is secreted with breast milk.

    T1 / 2 with impaired renal function - 3.5-32 hours Cumulates in chronic renal failure.

    Indications:

    Arterial hypertension, incl. Renovascular.

    Chronic heart failure (as part of complex therapy).

    Violation of the function of the left ventricle after a previous myocardial infarction in a clinically stable state.

    Diabetic nephropathy against a type 1 diabetes mellitus (for albuminuria more than 30 mg / day).

    Contraindications:

    Hypersensitivity to the drug and other components of the drug, hereditary or idiopathic edema, angioedema (with the use of other ACE inhibitors, including in the anamnesis), severe renal or hepatic impairment, hyperkalemia, bilateral stenosis of the renal arteries, or stenosis of the artery of a single kidney with progressing azotemia, a condition after kidney transplantation, stenosis of the aortic orifice and similar changes that hinder blood outflow, pregnancy, lactation period, age of 18 years.

    Lactose intolerance, lactase deficiency or glucose-galactose malabsorption.

    Carefully:

    In severe autoimmune diseases (especially systemic lupus erythematosus or scleroderma), oppression of bone marrow hematopoiesis (risk of developing neutropenia and agranulocytosis), cerebral ischemia, diabetes mellitus (increased risk of hyperkalemia), in patients on hemodialysis,diet with sodium restriction, primary hyperaldosteronism, ischemic heart disease, conditions accompanied by a decrease in the volume of circulating blood (including diarrhea, vomiting), in old age. Be wary appoint patients who are on a low-salt or salt-free diet (increased risk of arterial hypotension and hyperkalemia).

    Dosing and Administration:

    Captopril-FPO® is administered orally 1 hour before meals. The dosage regimen is set individually.

    With arterial hypertension treatment is started with the lowest effective dose of 12.5 mg (1/4 tablets 50 mg) 2 times a day (rarely with 6.25 mg 2 times a day). Pay attention to the tolerability of the first dose during the first hour. If in this case the arterial hypotension developed, the patient should be transferred to a horizontal position (such a reaction to the first dose should not serve as an obstacle to furtherher therapy). If necessary, the dose gradually (with an interval of 2-4 weeks) is increased to achieve the optimal effect. With a mild to moderate degree of hypertension, the usual maintenance dose is 25 mg (1/2 tablet of 50 mg) 2 once a day; the maximum dose is 50 mg (1 tablet of 50 mg) 2 times a day. At a severe degree of hypertension, the maximum daily dose is 150 mg (50 mg 3 times a day).

    In elderly patients, the initial dose is 6.25 mg 2 times a day.

    With chronic heart failure prescribe along with diuretics and / or in combination with cardiac glycosides (in order to avoid an initial excessive decrease in blood pressure, prior to the appointment of the drug Captopril-FPO® diuretic is canceled or reduced dose). The initial dose is 6.25 mg or 12.5 mg 3 times a day, if necessary, increase the dose gradually (at intervals of not less than 2 weeks) to 25 mg (1/2 tablets 50 mg) 2-3 times a day . The maximum daily dose is 150 mg.

    With violations of the function of the left ventricle after suffering a myocardial infarction in patients in a clinically stable state, Captopril-FPO® can be prescribed as early as 3 days after myocardial infarction. The initial dose is 6.25 mg / day, then the daily dose can be increased to 75 mg in 2-3 doses (depending on the drug's tolerance). If necessary, the dose is gradually increased to a maximum daily dose of 150 mg / day. With the development of arterial hypotension, a dose reduction may be required.Subsequent attempts to apply a maximum daily dose of 150 mg should be based on the tolerability of patients with the drug Captopril-FPO.

    With diabetic nephropathy appoint a dose of 75-100 mg / day in 2-3 hours. With insulin-dependent diabetes mellitus (type 1) with microalbuminuria (albumin release 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 (1/2 tablets 50 mg) 3 times a day.

    With a moderate degree of impaired renal function (clearance of creatinine KK - not less than 30 ml / min / 1.73 m2) Captopril-FPO® can be given 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; In the future, if necessary, the dose of the drug Kaptopril-FPO® is gradually increased after sufficiently long intervals of time, but use a daily dose of the drug less than in the case of arterial hypertension. If necessary, additionally prescribed "loop" diuretics, and not diuretics thiazide series.

    Side effects:

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

    From the central nervous system: dizziness, headache, general weakness, fatigue, asthenia, paresthesia, drowsiness, visual impairment.

    From the respiratory system: dry cough, pulmonary edema, bronchospasm.

    From the urinary system: impaired renal function.

    From the side of water-electrolyte exchange: hyperkalemia, hyponatremia (most often with salt-free diet and simultaneous intake of diuretics), proteinuria, increased urea nitrogen in the blood, creatinine, acidosis.

    On the part of the organs of hematopoiesis: neutropenia, anemia, thrombocytopenia, agranulocytosis.

    Allergic reactions: angioedema, "hot flashes" of blood to the skin of the face, fever, skin rash (maculopapular, less often vesicular or bullous), skin itching, photosensitivity, bronchospasm, serum sickness, lymphadenopathy, in rare cases - the emergence antinuclear antibodies in the blood.

    Co the sides of the digestive system: a violation of taste, a decrease in appetite, stomatitis, dyspepsia, nausea,abdominal pain, constipation or diarrhea, increased activity of "liver" enzymes, hyperbilirubinemia; hepatitis and cholestasis (rarely); pancreatitis (in isolated cases), gingival hyperplasia, intestinal edema (very rarely).

    Overdose:

    Symptoms: a marked decrease in blood pressure, including collapse, myocardial infarction, acute impairment of cerebral circulation, thromboembolic complications.

    Treatment: gastric lavage, use of activated charcoal, reduction of dose or complete withdrawal of the drug; transfer of the patient to a horizontal position with raised lower limbs; measures aimed at restoring blood pressure (increasing the volume of circulating blood, including intravenous infusion of 0.9% sodium chloride solution).

    Symptomatic therapy: epinephrine (subcutaneously or intravenously), antihistamines, hydrocortisone (intravenously). Hemodialysis is possible; peritoneal dialysis - not effective.

    Interaction:

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

    Increases the bioavailability of propranolol.

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

    The hypotensive effect weakens indomethacin and other non-steroidal anti-inflammatory drugs, incl. selective inhibitors of cyclooxygenase-2 (COX-2) due to a delay in sodium ions and a reduction in the synthesis of prostaglandins, especially against a background of low renin activity, and estrogens (sodium ion retention).

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

    Combined use with potassium-sparing diuretics (eg triamterene, spironolactone, amyloride), potassium preparations, cyclosporine, milk with low salt content (can contain potassium ions up to 60 mmol / l), potassium supplements, salt substitutes (contain significant amounts of potassium) increases the risk of hyperkalemia.

    Slows the excretion of lithium drugs, increasing its concentration in the blood (possibly enhancing the toxic effect of lithium).

    When captopril is prescribed against the background of taking allopurinol or procainamide, the risk of developing Stevens-Johnson syndrome and immunosuppressive action is increased.

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

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

    Insulin and hypoglycemic agents for oral administration - the risk of developing hypoglycemia.
    Special instructions:

    Patients with chronic heart failure are treated under close medical supervision.

    Before the onset, and also regularly during the treatment with the drug Captopril-FPO®, kidney function should be monitored. Against the background of long-term use of the drug Captopril-FPO, approximately 20% of patients have a stable increase in the concentrations of 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 an increase in the serum creatinine concentration.

    In patients with hypertension with the use of the drug Captopril-FPO, expressed arterial hypotension is observed only in rare cases; The likelihood of developing this condition increases with deficiency of fluid and salts (incl.after intensive treatment with diuretics), in patients with chronic heart failure or who are on dialysis.

    The probability of a sharp decrease in blood pressure can be minimized by a preliminary cancellation (for 4-7 days) of a diuretic, or by administration of captopril at the start of treatment in small doses (6.25-12.5 mg / day).

    When therapy in outpatient settings, the patient should be warned about the possible appearance of symptoms of an infection requiring a follow-up medical examination, a clinical and laboratory examination.

    In the first 3 months of therapy, the number of blood leukocytes is monitored monthly, then 4 times in 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. If the first symptoms of a secondary infection occur against a background of myeloid hypoplasia, an extensive blood test should be performed immediately.

    In some cases, against the background of the use of ACE inhibitors, incl. captopril, there is an increase in the concentration of potassium in the blood serum. The risk of developing hyperkalemia with ACE inhibitors is increasedin patients with renal insufficiency and diabetes mellitus, and also 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 is carried out in patients receiving Captopril-FPO®, dialysis membranes with high permeability should be avoided (for example, AN69), because in such cases the risk of anaphylactoid reactions increases.

    In case of development of angioedema, the drug is canceled and careful medical supervision and symptomatic therapy are carried out. With the localization of edema on the face of special treatment is not required (to reduce the severity of symptoms - antihistamines); in case of spread of edema to the tongue, throat or larynx with the threat of airway obstruction, immediately enter epinephrine subcutaneously (0.5 ml at a dilution of 1: 1000).

    When taking the drug Captopril-FPO®, a false positive reaction can be observed when analyzing urine for acetone.

    Caution should be exercised when performing physical exercises or in hot weather (risk of dehydration and excessive blood pressure lowering due to decreased circulating blood volume).

    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 50 mg.

    Packaging:For 10 or 20 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

    By 1, 2, or 4 contour squares, together with instructions for use, are placed in a pack of cardboard.

    Storage conditions:

    In a dry, the dark place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    2 years.

    Do not use after the expiration date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-002408/10
    Date of registration:24.03.2010
    Expiration Date:Unlimited
    The owner of the registration certificate:OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia
    Manufacturer: & nbsp
    Representation: & nbspOBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSCOBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSCRussia
    Information update date: & nbsp07.12.2017
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