Index of drugs

Arterial hypertension (as monotherapy or combination therapy), primary hypertension associated with renal failure, secondary renal hypertension, congestive heart failure (in combination therapy).

1 tabl contains 12.5 mg, 25 mg or 50 mg of captopril.

The drug from the first group of drugs that inhibits the activity of the enzyme converting angiotensin I to angiotensin II. It binds to this enzyme at 5 active sites, in which the SH group binds to Zn contained in the enzyme. This combination is easily oxidized which is the cause of the short action of captopril. Initially, the SH group was thought to be responsible for many of the adverse effects of captopril, it is now known that its presence may have beneficial clinical significance due to binding of free radicals, which is particularly desirable in coronary disease, stress states and cardiac arrhythmia with reperfusion, while side effects are the right dose selection has been reduced. The drug lowers blood pressure - the hypotensive effect depends primarily on the decrease in the concentration of angiotensin II, lowering the concentration of aldosterone. Lowering aldosterone results in a slight increase in potassium in the blood while losing sodium and water. The long-term hypotensive effect also depends on the inhibition of kinin degradation (angiotensin I converting enzyme I is identical to bradykinin inactivating kininase II) and the increase in prostaglandin dilatation (PGE₂). Captopril reduces systemic and pulmonary vascular resistance without altering or increasing cardiac output. It does not reduce renal flow. In patients with congestive heart failure due to reduction of peripheral vascular resistance (afterload) and reduction of preload, there is a long-term haemodynamic improvement and improvement of exercise tolerance. It counteracts the overgrowth and proliferation of smooth muscle in vessels as well as hypertrophy and remodeling of the myocardium. It has anti-atherosclerosis. Increases local blood flow in the limbs, improves the cerebral blood flow. It improves carbohydrate tolerance, has a beneficial effect on the lipid metabolism. It is well and quickly absorbed from the gastrointestinal tract. The bioavailability is 49-76%, the presence of food reduces absorption. The clinical effect occurs about 15 minutes after administration of the drug, reaches a maximum between 60-90 min and persists for 4-6 h. Maximum concentration in the blood reaches after 1 h, 25-30% of the drug is bound to plasma proteins. 75% of the drug is excreted in the urine, of which 50% in the unchanged form, and the rest associated with endogenous thiol compounds, e.g. captopril-cysteine ​​(this binding is reversible). T_0,5 is about 2 hours. The drug can be eliminated by hemodialysis or peritoneal dialysis.

Hypersensitivity to captopril or other ACE-converting enzymes, bilateral renal artery stenosis or narrowing of the artery of the sole kidney (captopril abolishes glomerular flow regulation, reduces glomerular filtration in ischemic kidney), kidney transplantation, primary hyperaldosteronism; pregnancy, breastfeeding. Caution use: in renal failure (requires dose reduction); narrowing of the mitral and aortic valve, hypertrophic cardiomyopathy, in patients over 65 years of age, with severe heart failure, in connective tissue diseases, severe electrolyte disturbances, in patients with chronic lung disease, bronchial asthma, hepatic failure, with a dry cough in the past; simultaneously treated with medications that lower the body's defense (eg corticoids, cytostatics, antimetabolites), Allopurinol, procainamide or lithium preparations. Do not use in patients dialysed with high permeability dialyzers with a polyacrylonitrile and polysulfone membrane.

At the doses used, side effects occur in only 2.2% of the treated patients.Captopril can cause: dry tiring cough, angioneurotic edema, sudden decrease in blood pressure (in about 2.5% of treated patients), especially in patients with high-sodium hypertension remaining on a low-sodium diet or receiving diuretics; skin rashes (about 6.0%) maculopapular, urticaria, reversible pemphigoid-like lesions, redness of the skin, pruritus, photosensitivity, angioedema; taste disorders (in about 3.1%) - (reversible - disappear about 2-3 months after discontinuation of the drug); mouth infection; dry mouth; loss of appetite; vomiting; constipation; symptoms of stomach irritation; abdominal pain (about 1.6%); changes in the morphological image of the blood (neutropenia - about 0.04%, agranulocytosis, hemolytic and aplastic anemia, thrombocytopenia, pancytopenia). There may also be symptoms from o.u.n.n .: headache (in about 2.9%), nausea, depression, fatigue (in about 2.7%), insomnia, paresthesia in the upper limbs. In individual cases, pancreatitis, gastrointestinal obstruction, impaired hepatic function (jaundice congestion, hepatitis), increased blood transaminases, proteinuria, transient elevation of urea and creatinine in the blood (approximately 0.6%) may occur. potassium levels and decrease in blood sodium, tachycardia, arrhythmias (tachycardia), ischemic heart pain, bronchospasm, impotence (about 1.1%). Side effects are more common in patients with renal failure. In patients dialyzed with dialysers with polyacrylonitrile and polysulfone membranes, allergic reactions may occur during dialysis.

Adults: in the treatment of hypertension: initial dose of 12.5 mg 2 times a day, increased after about 10 days to a maintenance dose of 25 mg 2 times a day; if necessary, the dose can be gradually increased at intervals of 2-4 weeks to a maximum of 150 mg / day. For the treatment of heart failure: initially 6.25 mg or 12.5 mg 2-3 times a day (the use of small initial doses shortens the duration of transient hypotension), after 10-14 days the dose can be increased, usually up to 25 mg 3-4 times a day . Children: premature babies 0.01-0.15 mg / kg every 12 h (ie up to 0.3 mg / kg / day); newborns and infants up to 6 months: 0.01-0.25 mg / kg every 12 h (ie up to 0.5 mg / kg / day); infants over 6 months: 0.25-0.5 mg / kg m.c. every 8 h (ie 0.75-1.5 mg / kg / day); older children: 1.3-3.0 mg / kg / day in 3 doses; children who should be expected to have an increased antihypertensive reaction (eg treated with diuretics), the starting dose is 0.15 mg / kg / day. The manufacturer notes: the dose above 3 mg / kg / day may be used exceptionally, only under strict medical supervision. According to data from specialist literature, the dose of 6 mg / kg / day should not be exceeded. Take orally at least 1 hour before a meal.