Active substanceCaptoprilCaptopril
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  • Dosage form: & nbsppills
    Composition:

    1 tablet contains:

    aactive substance: Captopril in terms of 100% substance - 25 mg;

    atExcipients: cellulose microcrystalline - 40 mg, corn starch - 7 mg, stearic acid - 3 mg, lactose - 25 mg.

    Description:Tablets from white to white with a creamy shade of color with a characteristic odor, square with rounded edges, biconvex with a cross-shaped notch on one side and a squeezed word "SQUIBB" and the number "452" - on the other. A slight "marble" is allowed.
    Pharmacotherapeutic group:Angiotensin-converting enzyme inhibitor (ACE inhibitor)
    ATX: & nbsp

    C.09.A.A.01   Captopril

    Pharmacodynamics:

    The drug Kapoten® 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. The maximum hypotensive effect is observed within 60-90 minutes after ingestion. The degree of reduction in blood pressure is the same when the patient is standing and lying down.

    EThe efficacy and safety of captopril in children are not established. The literature describes the limited experience of using captopril in children. Children, especially newborns, may be more prone to developing hemodynamic side effects. There have been cases of the development of excessive, prolonged and unpredictable increase in blood pressure, as well as complications related to it, including oliguria and seizures.

    Pharmacokinetics:

    When ingested quickly absorbed in the gastrointestinal tract, the maximum concentration in the blood plasma is observed about 1 hour after admission. 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%. The half-life period is 2-3 hours. The drug is excreted from the body mainly by the kidneys, up to 50% unchanged, the rest - in the form of metabolites.

    Indications:

    - Ahypertension, including renovascular;

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

    - disturbances in left ventricular function after myocardial infarction with clinically stable condition;

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

    Contraindications:

    - Pincreased sensitivity to captopril, any other component of the drug, or other ACE inhibitors;

    - Angioedema (angioedema) in the anamnesis associated with the administration of ACE inhibitors and hereditary / idiopathic angioedema);

    - severe dysfunction of the liver and / or kidney;

    - refractory 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 orifice and similar changes that hinder the outflow of blood from the left ventricle;

    - simultaneous use with aliskiren and aliskirenoderzhaschimi drugs in patients with diabetes mellitus or impaired renal function (GFR less than 60 ml / min);

    - pregnancy;

    - the period of breastfeeding;

    - age under 18 years (effectiveness and safety not established);

    - lactose intolerance, lactase deficiency and glucose-galactose malabsorption syndrome.

    Carefully:

    - Severe autoimmune diseases of connective tissue (including systemic lupus erythematosus, scleroderma);

    - oppression of bone marrow hematopoiesis (risk of neutropenia and agranulocytosis);

    - ischemia of the brain;

    - Diabetes mellitus (increased risk of hyperkalemia);

    - patients who are on hemodialysis;

    - Diet with restriction of table salt;

    - primary hyperaldosteronism;

    - cardiac ischemia;

    - conditions accompanied by a decrease in the volume of circulating blood (including vomiting, diarrhea);

    - elderly age (dosage correction is required);

    - surgical intervention / general anesthesia, arterial hypotension, use of negroid race in patients, renal and / or liver dysfunction, chronic heart failure,hemodialysis using high-flow membranes (for example, AN69®), desensitizing therapy, low-density lipoprotein apheresis (LDL), simultaneous use of potassium-sparing diuretics, potassium preparations, potassium-containing substitutes and lithium, simultaneous use of immunosuppressants, allopurinol, procainamide (risk of neutropenia, agranulocytosis) .

    Pregnancy and lactation:

    The use of the drug Kapoten® is contraindicated during pregnancy.

    The drug Kapoten® should not be used in the first trimester of pregnancy. Appropriate controlled trials of the use of ACE inhibitors in pregnant women have not been conducted. Available limited data on the effect of the drug in the first trimester of pregnancy suggest that the use of ACE inhibitors does not lead to fetal malformations associated with fetotoxicity. Epidemiological data suggesting a risk of teratogenicity after exposure to ACE inhibitors in the first trimester of pregnancy were not convincing, but some increase in risk can not be ruled out. If the use of an ACE inhibitor is considered necessary, patients planning pregnancy,should be transferred to alternative antihypertensive therapy that has an established safety profile for use during pregnancy.

    It is known that prolonged exposure of ACE inhibitors to the fetus in the II and III trimesters of pregnancy can lead to disruption of its development (decreased kidney function, oligohydramnion, delayed ossification of the bones of the skull) and development of complications in the newborn (such as renal failure, arterial hypotension, hyperkalemia) . If the patient received the Kapoten® preparation during the second and third trimester of pregnancy, it is recommended that an ultrasound be performed to assess the condition of the skull bones and the function of the fetal kidneys.

    The use of ACE inhibitors during pregnancy can cause developmental disorders (including arterial hypotension, neonatal hypoplasia of the skull bones, anuria, reversible or irreversible renal failure) and fetal death. When establishing the fact of pregnancy, the use of Kapoten® should be stopped as soon as possible.

    Approximately 1% of the accepted dose of captopril is found in breast milk.In connection with the risk of developing serious adverse reactions in the child, breastfeeding should be stopped or treatment with Kapoten® taken from the mother during the period of breastfeeding.

    Dosing and Administration:

    Inside, one hour before a meal. The dosage regimen is set individually.

    With arterial hypertension the drug is prescribed in an initial dose of 12.5 mg (1/2 tablets of 25 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 a mild to moderate degree of hypertension, the usual maintenance dose is 25 mg 2 times a day; the maximum dose is 50 mg twice a day. In severe arterial hypertension, the initial dose is 12.5 mg (1/2 tablets of 25 mg) twice a day. The dose is gradually increased to a maximum daily dose of 150 mg (but 50 mg 3 times per day).

    For the treatment of chronic heart failure. In the case of diuretic therapy prior to the appointment of the drug Kapoten®, the presence of a marked decrease in the content of electrolytes and bcc should be avoided. The initial daily dose is 6.25 mg (1/4 tablets of 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 patients who are in a clinically stable state, the use of the drug Kapoten® can begin as early as 3 days after myocardial infarction. The initial dose is 6.25 mg (1/4 tablets of 25 mg) per day, then the daily dose can be increased to 37.5-75 mg for 2-3 doses (depending on the drug's tolerance) up to a maximum of 150 mg in day.

    With diabetic nephropathy the drug Kapoten® is prescribed in a dose of 75-100 mg, divided into 2-3 doses. In type 1 diabetes mellitus with hyperalbuminuria (albumin release 30-300 mg per day) the dose of the drug is 50 mg 2 times a day. With proteinuria more than 500 mg per day, the drug is effective at a dose of 25 mg 3 times a day.

    Patients with impaired renal function at moderate degree of renal dysfunction (creatinine clearance (CK) not less than 30 ml / min / 1.73 m2) the drug Kapoten® 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 (1/2 tablet but 25 mg); further, if necessary, with sufficiently long intervals, the dose of the drug Kapoten® is gradually increased, using a smaller, than usual, daily dose of the drug.

    In old age the dose of the drug is selected individually, it is recommended to start therapy with a dose of 6.25 mg (1/4 tablets of 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:

    The frequency of adverse reactions is understood to be: frequency ≥1 / 100, <1/10, infrequent ≥1 / 1000, <1/100, rarely ≥1 / 10000, <1/1000, very rarely <1/10000.

    From the side of the cardiovascular system:

    infrequent - tachycardia or arrhythmia, angina pectoris, palpitations, orthostatic arterial hypotension, peripheral edema, marked lowering of blood pressure, Raynaud's syndrome, "flushes" of blood to the skin of the face, pallor;

    very rarely - cardiac arrest, cardiogenic shock.

    From the respiratory system:

    often - dry, unproductive cough, shortness of breath;

    very rarely - bronchospasm, eosinophilic pneumonitis, rhinitis, pulmonary edema.

    Allergic reactions:

    often - itchy skin, with or without rashes, rashes on the skin, alopecia;

    infrequently - angioedema of the extremities, face, lips, mucous membranes, tongue, pharynx and larynx;

    rarely - angioedema of the intestine;

    very rarely - urticaria, Stevens-Johnson syndrome, erythema multiforme, photosensitivity, erythroderma, pemphigoid reactions, exfoliative dermatitis, allergic alveolitis, eosinophilic pneumonia.

    From the central nervous system:

    often - drowsiness, dizziness, insomnia;

    infrequently - headache, paresthesia; rarely - ataxia;

    very rarely - confusion, depression, cerebral blood flow disorders, including stroke and syncope, blurred vision.

    From the hematopoiesis:

    Very rarely - neutropenia, agranulocytosis, pancytopenia, lymphadenopathy, eosinophilia, thrombocytopenia, anemia (including aplastic and hemolytic forms), an increase in the titer for antinuclear antibodies, autoimmune diseases.

    From the digestive system:

    often - nausea, vomiting, irritation of the mucous membrane of the stomach, abdominal pain, diarrhea, constipation, taste, dryness of the oral mucosa, indigestion;

    infrequently - anorexia;

    rarely - stomatitis, aphthous stomatitis;

    very rarely - glossitis, stomach ulcer, pancreatitis, gingival hyperplasia, impaired liver function and cholestasis (including jaundice), increased activity of liver enzymes, hepatitis (including rare cases of hepatonecrosis), hyperbilirubinemia.

    From the musculoskeletal system:

    very rarely - myalgia, arthralgia.

    From the urinary system:

    rarely - renal dysfunction (including renal failure), polyuria, oliguria, frequent urination;

    very rarely - nephrotic syndrome.

    On the part of the organs of reproduction:

    very rarely - impotence, gynecomastia.

    Others:

    infrequently - pain in the chest, increased fatigue, a feeling of general malaise, asthenia;

    rarely - hyperthermia.

    Laboratory indicators:

    very rarely - proteinuria, eosinophilia, hyperkalemia, hyponatremia, increased urea nitrogen, bilirubin and creatinine in the blood, a decrease in hematocrit, a decrease in hemoglobin, leukocytes, platelets, hypoglycemia.

    Overdose:

    Symptoms: a sharp decrease in blood pressure, shock, stupor, bradycardia, water-electrolyte balance disorders, renal failure.

    Treatment: gastric lavage, the introduction of adsorbents and sodium sulfate for 30 minutes after administration, the introduction of 0.9% sodium chloride solution or other plasma-substituting solutions (pre-patient to lay, raise your legs and then carry out replenishment activities BCC), hemodialysis. With bradycardia or pronounced vagus reactions - the introduction of atropine. An artificial pacemaker can be considered. Peritoneal dialysis is ineffective for removing captopril from the body.

    Interaction:

    In patients receiving diuretics, the drug Kapoten® can potentiate the hypotensive effect. Such an action is also provided by restriction of reception of table salt (salt-free diets), hemodialysis. Typically, an excessive reduction in blood pressure occurs within 1 hour after taking the first prescribed dose of the drug Kapoten®.

    Vasodilators (eg, nitroglycerin) in combination with the drug Kapoten® should be used at the lowest effective doses because of the risk of excessive blood pressure lowering.

    Caution should be exercised when co-administration of the drug Kapoten® (without or with a diuretic) and ldrugs that affect the sympathetic nervous system (for example, ganglion blockers, alpha-adrenoblockers).

    With the joint application of the drug Kapoten® and indomethacin (and possibly other non-steroidal anti-inflammatory drugs, for example, acetylsalicylic acid) may be reduced hypotensive effect, especially with hypertension, accompanied by low activity of renin. In patients with risk factors (elderly age, hypovolemia, simultaneous use of diuretics, impaired renal function), simultaneous use of non-steroidal anti-inflammatory drugs (including cyclooxygenase-2 inhibitors) and ACE inhibitors (including captopril), can lead to impaired renal function, up to acute renal failure. Usually, kidney dysfunction in such cases is reversible. Periodically monitor renal function in patients taking the drug Kapoten® and non-steroidal anti-inflammatory drugs.

    With therapy with the drug Kapoten® potassium-sparing diuretics (e.g., triamterene, spironolactone, amiloride, eplerenone), potassium preparations, potassium supplements,salt substitutes (contain significant amounts of potassium ions) should be prescribed only with proven hypokalemia, since their use increases the risk of developing hyperkalemia.

    With simultaneous use of ACE inhibitors (especially in combination with diuretics) and lithium preparations it is possible to increase the lithium content in the blood serum, and, consequently, the toxicity of lithium preparations. Periodically determine the content of lithium and serum.

    ACE inhibitors, including captopril, can potentiate a hypoglycemic effect insulin and hypoglycemic agents for oral administration, such as sulfonylureas.

    It is necessary to monitor the concentration of glucose in the blood at the beginning of therapy with the drug Kapoten®, and, if necessary, adjust the dose of the hypoglycemic drug.

    Double blockade of the renin-angiotensin-aldosterone system (RAAS), caused by the simultaneous administration of ACE inhibitors and receptor antagonists for angiotensin II or aliskiren and aliskiren-containing drugs, was associated with an increased incidence of side effects such as hypotension, hyperkalemia, decreased renal function (including acute renal failure).

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

    The use of the drug Kapoten® in patients taking immunosuppressants (e.g., cyclophosphacin or azathioprine), increases the risk of hematological disorders.

    Special instructions:

    Before you start, and also regularly in the process of treatment with the drug Kapoten® kidney function should be monitored. Patients from chronic heart failure under careful medical supervision.

    When taking ACE inhibitors, a characteristic non-productive cough is observed, which stops after the withdrawal of therapy of ingibiACE inhibitors In rare cases, with the intake of ACE inhibitors, there is a syndrome that begins with the appearance of cholestatic jaundice, passing into a lightning hepatonecrosis, sometimes fatal. The mechanism of development of this syndrome is unknown. If a patient receiving ACE inhibitor therapy develops jaundice or a marked increase in the activity of hepatic enzymes, discontinue treatment with ACE inhibitors and establish patient monitoring. In some patients with kidney disease, especially with severe renal artery stenosis, there is an increase in the concentrations of urea nitrogen and creatinine in the blood serum after lowering blood pressure. This increase is usually reversible upon discontinuation of drug therapy Kapoten®. In these cases, a reduction in the dose of the drug may be required Kapoten® and / or cancellation of a diuretic.

    On background of prolonged use of the drug Kapoten® approximately 20% of patientsentThere is an increase in the concentrations of urea and serum creatinine by more than 20% compared with the norm or baseline.

    Less than 5% of patients, especially in severe nephropathies, require discontinuation of treatment due to increased creatinine concentrations.

    It is not recommended to use a double blockade renin-angiotosinaldosterone system (RAAS), caused by the simultaneous administration of inhibitors ACE and angiotensin II receptor antagonists or aliskiren and aliskirecontaining drugs, since hebut associatedwith increased frequency of side effects, such as an arterial hypotension, giperkaliemiI, decreased kidney function (including acute renal failure). If simultaneous application of inhibitors APF and APA II (double blockade of RAAC) it is necessary, the treatment should be carried out under the supervision of the doctor and with the constant monitoring of kidney function, the content of electrolytes in the blood, and blood pressure.

    It is not recommended to use joint inhibitors APF and angiotensin receptor antagonists II in patients with diabetic nephropathy.

    In patients with hypertension with the drug Kapoten® severe arterial hypotension is observed only in rare cases; the probability of developing this condition increases with increased loss of fluid and salts (for example, after intensive treatment with diuretics), in patients with heart failure andland those on dialysis. The possibility of a sharp drop in blood pressure can be minimized by a preliminary cancellation (for 4-7 days) diuretic or increased intake of sodium chloride (about a week before the start of the intake), or by prescribing Kapoten® at the beginning of treatment in small doses (6.25-12.5 mg / day).

    Be wary of patients on a low-salinity or salt-free diet (an increased risk of developing an arterial hypothesistion) and hypercalIemiah. Excessive reduction in blood pressure can be observed in patients during major surgical operations, as well as in the application of means for general anesthesia, which have an antihypertensive effect. In such cases, for the correction of reduced arterialpressure apply the measures nabout an increase in the volume of circulating blood.

    Excessive reduction in blood pressure due to taking antihypertensive drugs may increase the risk of developing myocardial infarction or stroke in patients with coronary heart disease or cerebrovascular disease. When developing arterial hypotension, the patient should take a horizontal position with raised legs. You may need intravenous injection of 0.9% sodium chloride solution.

    Care should be taken when taking ACE inhibitors in patients with mitral / aortic stenosis/ hypertrophic obstructive cardiomyopathy; in the case of cardiogenic shock and hemodynamically significantobstruction reception is not recommended.

    In patients taking ACE inhibitors, there were neutropenia / agranulocytosis, thrombocytopenia and anemia. In patients with normal renal function and in the absence of other disorders neutropenia is rare. With renal failure, simultaneous administration of the drug Kapoten® and allopurinol led to neutropenia.

    A drug Kapoten® It should be used very carefully naqientov with autoimmune diseases of connective tissue, in immunosuppressors, allopurinol and procainamide, especially if there is a previously existing renal dysfunction. Due to the fact that the majority lethal cases of neutropenia against the background of ACE inhibitors developed in thepatients, it is necessary to control the number of leukocytes blood before the beginning of treatment, in the first 3 months - every 2 weeks, then every 2 months.

    All patients should be monitored monthly lof white blood cells in the blood in the first 3 months after initiation of therapy with the drug Kapoten®, then every 2 months. If the number of white blood cells is less than 4000 / μl, a repeated blood test is performed, below 1000 / μL - the drug is stopped while continuing to monitor the patient. Usually restoring the number of neutrophils occurs within 2 weeks after discontinuation of the drug Kapoten®. At 13% cases of neutropeniathe marked a lethal outcome. In almost all cases, lethal outcome was noted in patients with diseases of connective tissue, renal andheart failure, nand the reception background andmmunosuppressorov or a combination of both of these factors.

    When using inhibitors of APThere may be proteinuria, mainly inpatients with impaired renal function, as well asWhen using high doses of drugs. In most cases, proteinuria when taking the drug Kapoten® disappeared or the degree of its severity decreased within 6 months, regardless of whether the drug was stopped or not. Indices of kidney function (concentration of urea nitrogen in the blood and creatinine) in patients with proteinuria almost always were within normal limits. Patients with kidney disease should determine the protein content in the urine before the treatment and periodically during the course of therapy. AT some casesand the background of the use of inhibitors APF, incl. preparation Kapoten®, an increase in the potassium content in serum is observed. The risk of developing hyperkalemia with inhibitors APF is elevated in patients with renal insufficiency and sugar diabet, and also the host fecesiceberggaydiuretics, potassium preparations, or other drugs that cause an increase in the potassium content in the blood (for example,PaRandm). You should avoid the simultaneous use of potassium-sparing diuretics and potassium preparations. In addition, with the use of ACE inhibitors simultaneously with thiazide diureticse no risk of development hypokalemia, so in such cases, regular monitoring of the potassium content in the blood during therapy should be carried out.

    When hemodialysis in patients receiving ACE inhibitors, the use of dialysis membranes with high permeability should be avoided (for example, AN69), because in such cases the risk of developing anaphylactoid reactions. Anaphylactoid reactions were also observed in patients who underwentPof low density (apheresis) proteins with dextran sulfate.One should consider the use of either antihypertensive drugs of another class, or elsetype of dialysis membranes.

    In rare cases, against the background of therapy with ACE inhibitors, life-threatening anaphylactoid reactions in patients undergoing a course of desensitization with the help of venom of Hymenoptera (bees, wasps). In such patients, these reactions were prevented by temporarily discontinuing therapy with an ACE inhibitor. Care should be taken when desensitizing such patients.

    In the case of angioedema, the drug is withdrawn and carefully monitored until the symptoms disappear completely. Angioneurotic edema of the larynx can lead to death. 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;pinephrin (addressonlin) subcutaneously (0.3-0.5 ml in a 1: 1000 dilution). In rare cases, patients after the administration of ACE inhibitors, angioedema of the intestine was noted, accompanied by abdominal paintand (with nausea and vomiting andwhether without them), sometimes - at normal values ​​of activity of C-1-esterase and without a previous edema of the face. Bowel edema should be included in the spectrum of differential diagnosis of patients with complaints of abdominal pain when taking ACE inhibitors.

    In representatives of the Negroid race, cases of angioedema development were noted with greater frequency in comparison with representatives of the European race.

    Patients with diabetes who receive hypoglycemic drugs (hypoglycemic agents for ingestion or insulin) should carefully monitor the level of glycemia, especially during the first month of therapy with ACE inhibitors.

    ACE inhibitors are less effective in representatives of the Negroid than in the patients of the European race, which may be due to the greater prevalence of low renin activity in representatives of the Negroid race.

    PIn the conduct of extensive surgical operations or in the application of agents for general anesthesiaand, possessing the hypothesisMr.In patients receiving ACE inhibitors, an excessive decrease in blood pressure may be noted. And these cases can increase the volume of circulatingthe blood.

    When taking the drug Kapoten® a false positive reaction can be observed when analyzing urine for acetone.

    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. dizziness, especially after taking an initial dose.
    Form release / dosage:Tablets of 25 mg.
    Packaging:

    For 10 or 14 tablets in a contour mesh package.

    4 contour packs of 10 tablets or 2 or 4 contour packs of 14 tablets together with instructions for use are placed in a pack of cardboard.

    Storage conditions:In a dry place, at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    5 years.

    Do not use the drug after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:П N013055 / 01
    Date of registration:07.12.2007 / 05.07.2017
    Expiration Date:Unlimited
    The owner of the registration certificate:AKRIKHIN HFK, JSC AKRIKHIN HFK, JSC Russia
    Manufacturer: & nbsp
    Representation: & nbspAKRIKHIN OJSC AKRIKHIN OJSC Russia
    Information update date: & nbsp03.12.2017
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