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Active ingredients
Captopril
Release form
Pills
Composition
1 tablet contains: Active ingredient: captopril 50 mg.
Pharmacological effect
Antihypertensive agent, ACE inhibitor. The mechanism of antihypertensive action is associated with competitive inhibition of ACE activity, which leads to a decrease in the rate of angiotensin I conversion to angiotensin II (which has a pronounced vasoconstrictor effect and stimulates the secretion of aldosterone in the adrenal cortex). In addition, captopril appears to have an effect on the kinin-kallikrein system, preventing the breakdown of bradykinin. The hypotensive effect does not depend on plasma renin activity, a decrease in blood pressure is noted during normal and even reduced hormone concentrations, which is due to exposure to tissue RAAS. Increases coronary and renal blood flow. Due to the vasodilating effect, it reduces the round neck (afterload), the wedging pressure in the pulmonary capillaries (preload) and the resistance in the pulmonary vessels; increases heart volume and load tolerance. With prolonged use reduces the severity of left ventricular myocardial hypertrophy, prevents the progression of heart failure and slows down the development of left ventricular dilatation. Helps reduce sodium in patients with chronic heart failure. Expands arteries to a greater extent than veins. Improves blood supply to ischemic myocardium. It reduces platelet aggregation. It lowers the tone of the outgoing arteriole of the glomerular kidney, improves intraglomerular hemodynamics, and prevents the development of diabetic nephropathy.
Pharmacokinetics
After ingestion, at least 75% is rapidly absorbed from the gastrointestinal tract. Simultaneous food intake reduces absorption by 30-40%. Cmax in plasma is reached in 30-90 minutes. Binding to proteins, mainly albumin, is 25-30%. It is excreted in breast milk. Metabolized in the liver with the formation of disulfide dimer captopril and captopril-cysteine disulfide. Metabolites are pharmacologically inactive. T1 / 2 is less than 3 hours and increases in renal failure (3.5-32 hours). More than 95% is excreted by the kidneys, 40-50% unchanged, and the rest in the form of metabolites. In chronic renal failure, it accumulates.
Indications
Arterial hypertension (includingrenovascular), chronic heart failure (as part of combination therapy), left ventricular dysfunction after myocardial infarction in patients in a clinically stable state. Diabetic nephropathy with type 1 diabetes mellitus (with albuminuria more than 30 mg / day).
Contraindications
Pregnancy, lactation, age up to 18 years, hypersensitivity to captopril and other ACE inhibitors.
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. The impact on the ability to drive vehicles and control mechanisms of patients whose activities require increased attention, the question of the use of propranolol on an outpatient basis should be addressed only after evaluating the individual response of the patient.
Use during pregnancy and lactation
It should be borne in mind that the use of captopril in the II and III trimesters of pregnancy can cause developmental disorders and fetal death. When a pregnancy is established, captopril should be canceled immediately. Captopril is excreted in breast milk. If necessary, use during lactation should decide on the termination of breastfeeding.
Dosage and administration
When ingestion, the initial dose is 6.25-12.5 mg 2-3 times / day. With insufficient effect, the dose is gradually increased to 25-50 mg 3 times / day. In case of impaired renal function, the daily dose should be reduced. The maximum daily dose is 150 mg.
Side effects
From the side of the central nervous system and peripheral nervous system: dizziness, headache, fatigue, asthenia, paresthesia. From the side of the cardiovascular system: orthostatic hypotension; rarely - tachycardia. From the digestive system: nausea, loss of appetite, a violation of taste; rarely - abdominal pain, diarrhea or constipation,increased activity of hepatic transaminases, hyperbilirubinemia; signs of hepatocellular damage (hepatitis); in some cases - cholestasis; in isolated cases - pancreatitis. From the side of the hematopoietic system: rarely - neutropenia, anemia, thrombocytopenia; very rarely in patients with autoimmune diseases - agranulocytosis. On the side of metabolism: hyperkalemia, acidosis. On the urinary system: proteinuria, impaired kidney function (increased concentration of urea and creatinine in the blood). On the part of the respiratory system: dry cough.Allergic reactions: skin rash; rarely - angioedema, bronchospasm, serum sickness, lymphadenopathy; in some cases, the appearance of anti-nuclear antibodies in the blood.
Overdose
Symptoms: severe hypotension, up to collapse, myocardial infarction, acute violation of cerebral circulation, thromboembolic complications. Treatment: put the patient with elevated lower limbs; measures aimed at restoring blood pressure (increasing the volume of circulating blood, including intravenous infusion of isotonic sodium chloride solution), symptomatic therapy. Perhaps the use of hemodialysis; peritoneal hemodialysis is ineffective.
Interaction with other drugs
With simultaneous use with immunosuppressants, cytostatics, the risk of developing leukopenia increases. When used simultaneously with potassium-saving diuretics (including spironolactone, triamterene, amiloride), potassium preparations, salt substitutes and dietary supplements for food containing potassium, hyperkalemia may develop (especially patients with impaired renal function), because ACE inhibitors reduce the content of aldosterone, which leads to a delay of potassium in the body against the background of limiting the excretion of potassium or its additional intake in the body. With the simultaneous use of ACE inhibitors and NSAIDs, the risk of developing renal dysfunction increases; hyperkalemia is rarely observed. In case of simultaneous use with loop diuretics or thiazide diuretics, severe hypotension is possible, especially after taking the first dose of diuretic, apparently due to hypovolemia, which leads to a transient enhancement of the antihypertensive action of captopril. There is a risk of hypokalemia.Increased risk of developing renal dysfunction. If used concurrently with anesthetics, severe hypotension is possible. If used simultaneously with azathioprine, anemia may develop due to the suppression of erythropoietin activity under the influence of ACE inhibitors and azathioprine. Cases of the development of leukopenia are described, which may be associated with additive inhibition of bone marrow function. When used simultaneously with allopurinol, the risk of hematological disorders increases; Cases of the development of severe hypersensitivity reactions, including Stevens-Johnson syndrome, are described. With the simultaneous use of aluminum hydroxide, magnesium hydroxide, magnesium carbonate, the bioavailability of captopril is reduced. Acetylsalicylic acid in high doses can reduce the antihypertensive effect of captopril. It has not been finally determined whether acetylsalicylic acid reduces the therapeutic efficacy of ACE inhibitors in patients with coronary artery disease and heart failure. The nature of this interaction depends on the course of the disease. Acetylsalicylic acid, inhibiting COX and prostaglandin synthesis, can cause vasoconstriction, which leads to a decrease in cardiac output and a deterioration of patients with heart failure receiving ACE inhibitors. There are reports of an increase in the concentration of digoxin in the blood plasma while using captopril with digoxin. The risk of drug interaction is increased in patients with impaired renal function. When used simultaneously with indomethacin and ibuprofen, the antihypertensive effect of captopril decreases, apparently due to inhibition of prostaglandin synthesis under the influence of NSAIDs (which are thought to play a role in the development of the hypotensive effect of ACE inhibitors ). With simultaneous use with insulins, hypoglycemic agents of sulfonylurea, hypoglycemia may develop due to increased and glucose tolerance. With simultaneous use of ACE inhibitors and interleukin-3, there is a risk of arterial hypotension. Simultaneous use with interferon alpha-2a or interferon beta describes cases of severe granulocytopenia. The transition from clonidine to captopril develops the antihypertensive effect of the latter gradually.In the case of sudden withdrawal of clonidine in patients receiving captopril, a dramatic increase in blood pressure is possible. With simultaneous use of lithium carbonate, the concentration of lithium in the blood serum increases, accompanied by symptoms of intoxication. If used simultaneously with minoxidil, sodium nitroprusside, the antihypertensive effect is enhanced. a decrease in the effectiveness of captopril, which can lead to an increase in blood pressure, hypertensive crisis, described a case of hemorrhage in the brain. In case of simultaneous use with probenecid, renal clearance of captopril is reduced. Simultaneous use with procainamide may increase the risk of developing leukopenia. If used simultaneously with trimethoprim, there is a risk of hyperkalemia, especially in patients with impaired renal function. With simultaneous use with chlorpromazine, there is a risk of orthostatic hypotension. With simultaneous use with cyclosporine has been reported on the development of acute renal failure, oligurii.Polagayut that may decrease the effectiveness of antihypertensive drugs while the use of erythropoietin.
special instructions
C caution should be used for indications of a history of angioedema during therapy with ACE inhibitors, hereditary or idiopathic angioedema, with aortic stenosis, cerebro and cardiovascular diseases (including cerebrovascular insufficiency, coronary insufficiency, etc.). autoimmune diseases of the connective tissue (including SLE, scleroderma), in the suppression of bone marrow hematopoiesis, in diabetes mellitus, hyperkalemia, bilateral renal artery stenosis, Nose artery of the only kidney, condition after kidney transplantation, renal and / or liver failure, on the background of a sodium-restricted diet, conditions accompanied by decreased BCC (including with diarrhea, vomiting) in elderly patients. In patients with chronic heart failure, captopril is used under close medical supervision. Arterial hypotension that arises during surgery and captopril is eliminated by filling up the volume of fluid. Simultaneous administration should be avoided. eneniya potassium-sparing diuretics and drugsespecially in patients with renal insufficiency and diabetes mellitus. When taking captopril, a false positive reaction may be observed in the analysis of urine for acetone. Use of captopril in children is possible only if other drugs are ineffective. Impact on the ability to drive vehicles and control mechanisms. Care should be taken when driving or performing other work requiring increased attention, since dizziness is possible, especially after the initial dose of captopril.