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Active ingredients
Captopril
Release form
Pills
Composition
Captopril 25 mg. Additional substances: microcrystalline cellulose - 40 mg, corn starch - 7 mg, stearic acid - 3 mg, lactose monohydrate - 25 mg.
Pharmacological effect
ACE inhibitor. Suppresses the formation of angiotensin II and eliminates its vasoconstrictor effect on arterial and venous vessels. Reduces the round neck, afterload, lowers blood pressure. Reduces preload, reduces pressure in the right atrium and the pulmonary circulation. Reduces the release 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 in the position of the patient standing and lying. The efficacy and safety of captopril in children have not been established. The literature describes limited experience with captopril in children. Children, especially newborns, may be more likely to develop hemodynamic side effects. There have been cases of excessive, prolonged and unpredictable increases in blood pressure, as well as associated complications, including oliguria and seizures.
Pharmacokinetics
Absorption When ingested, it is rapidly absorbed from the gastrointestinal tract. Cmax in plasma is reached approximately 1 hour after administration. Bioavailability of captopril is 60-70%. Simultaneous food intake slows down the absorption of the drug by 30-40%. Distribution Binding to blood proteins is 25-30%. Excretion of T1 / 2 is 2-3 hours. The drug is excreted from the body mainly in the urine, up to 50% in unchanged form, the rest - as metabolites.
Indications
- arterial hypertension, incl. Renovascular - chronic heart failure (as part of combination therapy) - left ventricular function dysfunction after myocardial infarction in a clinically stable condition - diabetic nephropathy associated with type 1 diabetes (with albuminuria> 30 mg / day).
Contraindications
- angioedema (angioedema) in history, associated with the use of ACE inhibitors; - hereditary / idiopathic angioedema; - severe renal dysfunction; - severe liver dysfunction; - refractory hyperkalemia; progressive azotemia; - condition after kidney transplantation; - aortic stenosis and similar obstructive changes,impeding the outflow of blood from the left ventricle; - simultaneous use with aliskiren and aliskiren-containing drugs in patients with diabetes or renal dysfunction (GFR less than 60 ml / min); - lactose intolerance, lactase deficiency and glucose-galactose malabsorption syndrome; - pregnancy; - lactation period (breastfeeding); - age up to 18 years (efficacy and safety have not been established); - hypersensitivity to the components of the drug and other ACE inhibitors. With caution, you should prescribe the drug when severe s autoimmune diseases of the connective tissue (including SLE, scleroderma); oppression of bone marrow hematopoiesis (risk of developing neutropenia and agranulocytosis); cerebral ischemia; diabetes mellitus (increased risk of hyperkalemia); primary hyperaldosteronism; CHD; conditions accompanied by a decrease in BCC (including vomiting, diarrhea); hypotension; impaired renal and / or liver function; chronic heart failure; performing surgery / general anesthesia; patients on hemodialysis; patients on a sodium restricted diet; when conducting hemodialysis using high-strength membranes (for example, AN69), desensitizing therapy, LDL apheresis; simultaneous use of potassium-sparing diuretics, potassium preparations, potassium-containing substitutes, lithium preparations, immunosuppressants, allopurinol, procainamide (risk of developing neutropenia, agranulocytosis); elderly patients (dose adjustment required); Negroid patients.
Precautionary measures
During treatment, psoriasis may worsen. During pheochromocytoma, propranolol can only be used after taking an alpha blocker. After a long course of treatment, propranolol should be discontinued gradually, under the supervision of a physician. during anesthesia, you must stop taking propranolol or find a remedy for anesthesia with minimal negative inotropic effects. Influence on ability to drive motor transport and control mechanisms of patients whose activities require increased attention,the question of the use of propranolol on an outpatient basis should be resolved only after evaluating the individual response of the patient.
Use during pregnancy and lactation
Use of the drug Capoten is contraindicated in pregnancy. The drug Capoten should not be used in the first trimester of pregnancy. Appropriate controlled studies of the use of ACE inhibitors in pregnant women have not been conducted. The limited data available on the effects of the drug in the first trimester of pregnancy indicate that the use of ACE inhibitors does not lead to fetal developmental defects associated with fetotoxicity. Epidemiological data indicating the risk of teratogenicity after exposure to ACE inhibitors in the first trimester of pregnancy were not convincing, but a slight increase in risk cannot be ruled out. If the use of an ACE inhibitor is considered necessary, patients planning a pregnancy should be transferred to alternative antihypertensive therapy, which has an established safety profile for use in pregnancy. (decrease in kidney function, oligohydramnion, slowing down ossification of the skull bones) and the development of complications in the newborn (such as kidney failure, arterial ipotenziya, hyperkalemia). If the patient received Capoten in the II and III trimesters of pregnancy, it is recommended to conduct an ultrasound to assess the state of the bones of the skull and kidney function of the fetus. 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 the drug Capoten should be stopped as soon as possible. Approximately 1% of the dose of captopril found in breast milk. In connection with the risk of serious adverse reactions in the child, breastfeeding should be stopped or therapy with the drug Capoten in the mother should be discontinued for the period of breastfeeding.
Dosage and administration
The drug is taken orally for 1 hour before meals.The dosage regimen is set individually. In case of arterial hypertension, the initial dose is 12.5 mg (1/2 tab. 25 mg) 2 times / day. If necessary, increase the dose gradually (with an interval of 2-4 weeks) until the optimum effect is achieved. In mild and moderate arterial hypertension, the maintenance dose is 25 mg 2 times / day; the maximum dose is 50 mg 2 times / day. In severe hypertension, the initial dose is 12.5 mg (1/2 tab. 25 mg) 2 times / day. The dose is gradually increased to a maximum daily dose of 150 mg (50 mg 3 times / day). In chronic heart failure, the initial daily dose is 6.25 mg (1/4 tab. 25 mg) 3 times / day. If necessary, increase the dose gradually (at intervals of at least 2 weeks). Maintenance dose is 25 mg 2-3 times / day. The maximum daily dose is 150 mg. If before the administration of the drug Capoten, diuretic therapy was performed, it is necessary to exclude the presence of a pronounced decrease in the content of electrolytes and bcc. The initial dose is 6.25 mg / day (1/4 tab. 25 mg), then the daily dose can be increased to 37.5-75 mg in 2-3 doses (depending on the tolerance of the drug) up to the maximum - 150 mg / day. In diabetic Nephropathy drug prescribed in a dose of 75-100 mg, divided into 2-3 doses. In type 1 diabetes mellitus with microalbuminuria (albumin clearance 30-300 mg / day), the dose of the drug is 50 mg 2 times / day. When proteinuria is more than 500 mg / day, the drug is effective at a dose of 25 mg 3 times / day. Patients with impaired renal function of moderate degree (CC ≥ 30 ml / min / 1.73 m2) Capoten is prescribed in a dose of 75-100 mg / day. For severe impaired renal function (CC <30 ml / min / 1.73 m2), the initial dose is not more than 12.5 mg / day (1/2 tab. 25 mg). In the future, if necessary, the dose is gradually increased (with sufficiently large intervals), but use a smaller than usual daily dose of the drug. For elderly patients, the dose is adjusted individually. It is recommended to begin treatment with a dose of 6.25 mg (1/4 tab. 25 mg) 2 times / day and, if possible, maintain it at this level. If necessary, loop diuretics are additionally prescribed, and not the thiazide diuretics.
Side effects
Determination of the frequency of adverse reactions: often (≥1 / 100, <1/10); infrequently (≥1 / 1000, <1/100), rarely (≥1 / 10 000, <1/1000), very rarely (<1/10 000). From the cardiovascular system: infrequently - tachycardia or arrhythmia, angina pectoris, palpitations, orthostatic hypotension, excessive reduction of blood pressure, Raynaud's syndrome, flushing of the skin of the face, pallor; very rarely - cardiac arrest, cardiogenic shock. On the part of the respiratory system: often - dry non-productive cough, shortness of breath; very rarely - bronchospasm, eosinophilic pneumonitis, rhinitis, pulmonary edema. On the skin and subcutaneous tissues: often - pruritus, with or without rashes, rash on the skin, alopecia. Allergic reactions: infrequent - angioedema of the extremities, face, lips, mucous membranes, tongue, pharynx and larynx; rarely, angioedema; very rarely - urticaria, Stevens-Johnson syndrome, erythema multiforme, photosensitivity, erythroderma, pemphigoid reactions, exfoliative dermatitis, allergic alveolitis, eosinophilic pneumonia. From the nervous system: often - drowsiness, dizziness, insomnia; infrequently - headache, paresthesia; rarely - ataxia; very rarely - confusion, depression, disorders of cerebral circulation, including stroke and syncope, blurred vision. From the blood system: very rarely - neutropenia, agranulocytosis, pancytopenia, lymphadenopathy, eosinophilia, thrombocytopenia, anemia (including aplastic and hemolytic forms),) side of the immune system: very rarely - increased titer of antinuclear antibodies, autoimmune diseases. From the alimentary system: often - nausea, vomiting, irritation of the gastric mucosa, pain in the abdominal area lethargy, diarrhea, constipation, disturbance of taste, dryness of the oral mucosa, dyspepsia; infrequently - anorexia; rarely - stomatitis, aphthous stomatitis; very rarely - glossitis, gastric ulcer, pancreatitis, gum 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 - impaired renal function (including renal failure),polyuria, oliguria, frequent urination; very rarely - nephrotic syndrome. From the reproductive system: very rarely - impotence, gynecomastia. Others: infrequently - peripheral edema, chest pain, fatigue, general malaise, asthenia; rarely - hyperthermia. Laboratory parameters: very rarely - proteinuria, eosinophilia, hyperkalemia, hyponatremia, elevated nitrogen content of urea, bilirubin and creatinine in the blood, decreased hematocrit, decreased hemoglobin, white blood cells, platelets, hypoglycemia.
Overdose
Symptoms: a sharp decrease in blood pressure, shock, stupor, bradycardia, impaired water and electrolyte balance, renal failure. Treatment: gastric lavage, the introduction of adsorbents and sodium sulfate for 30 minutes after taking the drug, the introduction of 0.9% sodium chloride solution or other plasma-substituting drugs ( pre-patient should be transferred to a horizontal position with a low head, then carry out activities to fill the BCC), hemodialysis. For bradycardia or severe vagal reactions, atropine is administered. The use of an artificial pacemaker may be considered. Peritoneal dialysis is ineffective for removing captopril from the body.
Interaction with other drugs
In patients taking diuretics, Capoten may potentiate the hypotensive effect. A similar restriction on the use of table salt (salt-free diets) and hemodialysis also have a similar effect. Usually, an excessive decrease in blood pressure occurs within the first hour after taking the first prescribed dose of Capoten. Vasodilators (for example, nitroglycerin) in combination with Capoten should be used in the lowest effective doses because of the risk of an excessive decrease in blood pressure. Care should be taken when using the drug Capoten ( with or without diuretic) and drugs that affect the sympathetic nervous system (for example, ganglioblokatory, alpha-blockers). When used together Capoten and indomethacin (and, possibly, other NSAIDs, for example, acetylsalicylic acid), there may be a decrease in the hypotensive effect, especially in hypertension, accompanied by low renin activity.In patients with risk factors (advanced age, hypovolemia, simultaneous use of diuretics, impaired kidney function), simultaneous use of NSAIDs (including COX-2 inhibitors) and ACE inhibitors (including captopril) can lead to deterioration of renal function, up to acute renal failure. Kidney damage is usually reversible in such cases. Kidney function should be periodically checked in patients taking Capoten and NPVS. When therapy is administered with Capoten, potassium-saving diuretics (for example, triamterene, spironolactone, amiloride), potassium preparations, potassium supplements, salt substitutes (contain significant amounts of potassium ions) should be prescribed only when proven hypokalemia, because their use increases the risk of hyperkalemia. With the simultaneous use of ACE inhibitors (especially in combination with diuretics) and lithium preparations, an increase in the lithium content in the blood serum, and, consequently, the toxicity of lithium preparations is possible. Serum lithium levels should be determined periodically. If insulin and hypoglycemic agents for oral administration are used at the same time, such as sulfonylurea derivatives, with ACE inhibitors, including Capoten, an excessive decrease in blood glucose concentration is possible. It is necessary to control the concentration of glucose in the blood at the start of therapy with Capoten and, if necessary, adjust the dose of the hypoglycemic drug. arterial hypotension, hyperkalemia, reduced kidney function (including acute renal failure). Use of the drug K potentials in patients receiving allopurinol or procainamide, increases the risk of neutropenia and / or syndrome Stevens-Dzhonsona.Primenenie Capoten drug in patients receiving immunosuppressive agents (eg azathioprine or tsiklofosfatsin), increases the risk of hematological disorders.
special instructions
Before starting, as well as regularly in the process of treatment with the drug Capoten should monitor renal function.In patients with chronic heart failure, Capoten should be used under close medical supervision. When using ACE inhibitors, a characteristic nonproductive cough is observed, which stops after discontinuation of therapy with ACE inhibitors. In rare cases, when ACE inhibitors are used, sometimes fatal. The mechanism of development of this syndrome is unknown. If jaundice develops in a patient receiving treatment with ACE inhibitors, or there is a marked increase in liver enzyme activity, discontinue treatment with ACE inhibitors and monitor the patient. serum creatinine after blood pressure reduction. This increase is usually reversible after discontinuation of therapy with Kapoten. In these cases, it may be necessary to reduce the dose of the drug Capoten and / or cancel the diuretic. Against the background of long-term use of the drug Capoten, an increase in the concentration of urea and serum creatinine by more than 20% is observed in approximately 20% of patients compared to normal or baseline. Less than 5% of patients, especially with severe nephropathies, require discontinuation of treatment due to an increase in creatinine concentration. It is not recommended to use a double blockade of RAAS caused by the simultaneous use of ACE inhibitors and angiotensin II or aliskiren receptor antagonists and aliskiren-containing drugs, since it was associated with elevated the incidence of side effects such as hypotension, hyperkalemia, reduced kidney function (including acute renal failure). If simultaneous use of ACE inhibitors and angiotensin II receptor antagonists (double blockade of RAAS) is necessary, treatment should be carried out under the supervision of a physician and with the ongoing monitoring of kidney function, blood electrolytes, and AD. angiotensin II in patients with diabetic nephropathy. In patients with arterial hypertension when using the drugCapoten severe arterial hypotension is observed only in rare cases; the likelihood of developing this condition increases with increased loss of fluid and salt (for example, after intensive diuretic treatment), in patients with heart failure or being on dialysis. The possibility of a sharp decrease in blood pressure can be minimized with prior cancellation (4-7 days) of a diuretic or an increase in sodium chloride intake (about a week before the start of treatment), or by administering the drug Capoten at the beginning of treatment at low doses (6.25-12.5 mg / day). With caution, the drug is prescribed to patients on a low sodium or salt-free diet (an increased risk of developing hypotension and hyperkalemia). An excessive decrease in blood pressure may occur in patients during major surgical procedures. eractions, as well as the use of anesthetics with hypotensive effect. In such cases, measures to increase BCC are used to correct reduced blood pressure. Excessive blood pressure reduction due to the use of antihypertensive drugs may increase the risk of myocardial infarction or stroke in patients with IHD or vascular diseases of the brain. With the development of arterial hypotension patient should be transferred to a horizontal position with a low head. May require i.v. administration of a 0.9% sodium chloride solution. Care should be taken when using ACE inhibitors in patients with mitral / aortic stenosis / hypertrophic obstructive cardiomyopathy; in the case of cardiogenic shock and hemodynamically significant obstruction, the use of the drug is not recommended. Patients taking ACE inhibitors had neutropenia / agranulocytosis, thrombocytopenia and anemia. In patients with normal renal function and in the absence of other disorders, neutropenia is rare. In renal insufficiency, simultaneous use of the drug Capoten and allopurinol resulted in neutropenia. The drug Capoten should be used very carefully in patients with autoimmune diseases of the connective tissue, in receiving immunosuppressants, allopurinol and procainamide, especially in the presence of previously existing kidney function disorders.Due to the fact that the majority of lethal cases of neutropenia against the background of the use of ACE inhibitors developed in these patients, they should be monitored for the number of blood leukocytes before starting treatment, for the first 3 months every 2 weeks, then every 2 months. All patients should monthly monitor the number of leukocytes in the blood in the first 3 months after the start of therapy with the drug Capoten, then every 2 months. If the number of leukocytes is below 4000 / μl, repeated blood count is shown, below 1000 / μl - the drug is stopped, continuing to monitor the patient. Usually, the number of neutrophils is restored within 2 weeks after discontinuation of the drug Capoten. In 13% of cases of neutropenia, death was noted. In almost all cases, the death of neutropenia was noted in patients with connective tissue diseases, renal or heart failure, while receiving immunosuppressants or a combination of both of these factors. When using ACE inhibitors, proteinuria can occur, mainly in patients with impaired renal function, and when using the drug in high doses. In most cases, proteinuria with the use of the drug Capoten disappeared or its severity decreased within 6 months, regardless of whether the drug was stopped or not. Indicators of kidney function (blood urea nitrogen and creatinine) in patients with proteinuria were almost always within the normal range. In patients with kidney disease, the urine protein content should be determined before starting treatment and periodically throughout the course of therapy. In some cases, against the background of the use of ACE inhibitors, incl. drug Capoten, there is an increase in the content of potassium in the serum. The risk of developing hyperkalemia with the use of ACE inhibitors is increased in patients with renal insufficiency and diabetes mellitus, as well as receiving potassium-saving diuretics, potassium preparations or other drugs that cause an increase in the content of potassium in the blood (for example, heparin). The simultaneous use of potassium-sparing diuretics and potassium preparations should be avoided. In addition, when using ACE inhibitors simultaneously with thiazide diuretics, the risk of hypokalemia is not excluded,therefore, in such cases, regular potassium in the blood should be monitored during therapy. When performing hemodialysis in patients receiving ACE inhibitors, the use of high-permeability dialysis membranes (for example, AN69) should be avoided, since in such cases the risk of anaphylactoid reactions is increased. Anaphylactoid reactions were also observed in patients undergoing an apheresis procedure for LDL using dextran sulfate. Consideration should be given to the use of either antihypertensive drugs of another class or another type of dialysis membranes. In rare cases, during therapy with ACE inhibitors, life-threatening anaphylactoid reactions were noted in patients undergoing desensitization with hymenoptera (bees, wasps). In these patients, these reactions were prevented by temporarily discontinuing therapy with an ACE inhibitor. Special care should be taken in case of desensitization of such patients. In case of development of angioedema, the drug is canceled and careful medical monitoring is carried out until the symptoms disappear. Angioedema of the larynx can be fatal. If the edema is localized on the face, special treatment is usually not required (antihistamines can be used to reduce the severity of symptoms); If the edema spreads to the tongue, pharynx or larynx and there is a threat of airway obstruction, epinephrine (adrenaline) should be immediately administered (0.3-0.5 ml at a dilution of 1: 1000). In rare cases, patients after taking ACE inhibitors had angioedema of the intestines, which was accompanied by abdominal pain (with nausea and vomiting or without them), sometimes with normal values of C-1-esterase activity and without prior edema of the face. Intestinal edema should be included in the range of differential diagnosis of patients with complaints of abdominal pain when using ACE inhibitors. In representatives of the Negroid race, cases of angioedema edema were observed with a higher frequency compared with Caucasians. ACE inhibitors are less effective in representatives of the Negro race than in Caucasians,which may be associated with a higher prevalence of low renin activity in the Negroid race. Patients with diabetes who are receiving hypoglycemic drugs (hypoglycemic agents for ingestion or insulin) should carefully control the glycemia level, especially during the first month of treatment with ACE inhibitors. extensive surgeries or when using general anesthesia drugs that have hypotensive effects in patients taking ACE inhibitors, sya an excessive fall in blood pressure. In these cases, it is possible to increase the BCC. When using the drug Capoten, a false positive reaction may be observed when analyzing urine on acetone. Effect on the ability to drive vehicles and control mechanisms psychomotor reactions, because dizziness may occur, especially after taking the initial dose.