Captopril 50 mg tablets 40
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Active substance: captopril 50 mg.
Excipients: lactose monohydrate (milk sugar) - 94 mg, microcrystalline cellulose - 49 mg, corn starch - 5 mg, magnesium stearate - 2 mg.
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 conversion of angiotensin I 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 the activity of renin plasma, a decrease in blood pressure is noted with a normal and even reduced concentration of the hormone, which is due to the effect on tissue RAAS. Increases coronary and renal blood flow.
Due to the vasodilating effect, it reduces OPSS (afterload), jamming pressure in the pulmonary capillaries (preload) and resistance in the pulmonary vessels; increases the minute volume of the heart and exercise tolerance. With prolonged use, it reduces the severity of left ventricular myocardial hypertrophy, prevents the progression of heart failure and slows down the development of left ventricular dilatation. Helps to reduce the sodium content in patients with chronic heart failure. Dilates arteries to a greater extent than veins. Improves blood supply to ischemic myocardium. Reduces platelet aggregation.
Lowers the tone of the glomeruli of the kidneys carrying arterioles, improving intraglomerular hemodynamics, prevents the development of diabetic nephropathy.
After ingestion, at least 75% is rapidly absorbed from the gastrointestinal tract. Simultaneous food intake reduces absorption by 30-40%. C max in the blood plasma is achieved after 30-90 min. Binding to proteins, mainly with albumin, is 25-30%. It is excreted in breast milk. It is metabolized in the liver with the formation of the disulfide dimer captopril and captopril-cysteine disulfide. Metabolites are pharmacologically inactive.
T 1/2 is less than 3 hours and increases with renal failure (3.5-32 hours). More than 95% is excreted by the kidneys, 40-50% unchanged, the rest - in the form of metabolites.
In chronic renal failure, cumulates.
Indications for use
- Arterial hypertension (including renovascular),
- chronic heart failure (as part of combination therapy),
- impaired function of the left ventricle after myocardial infarction in patients,
- who are in a clinically stable condition,
- diabetic nephropathy in type 1 diabetes mellitus (with albuminuria more than 30 mg / day).
- age up to 18 years,
- hypersensitivity to captopril and other ACE inhibitors.
Use in 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. With an established pregnancy, captopril should be canceled immediately.
Captopril is excreted in breast milk. If it is necessary to use during lactation, the issue of discontinuation of thoracic should be resolved. Feeding.
Use in case of impaired liver functionWith caution should be used for liver failure.
Use in renal dysfunction
With caution should be used in conditions after kidney transplantation, renal failure.
In case of impaired renal function, the daily dose should be reduced.
The simultaneous use of potassium-sparing diuretics and potassium preparations in patients with renal insufficiency should be avoided.
Use in childrenContraindicated under the age of 18 years. The use of captopril in children is possible only in case of ineffectiveness of other drugs.
Use in elderly patientsWith caution should be used in elderly patients.
C caution should be used when indicating a history of angioedema against the background of therapy with ACE inhibitors, hereditary or idiopathic angioedema, with aortic stenosis, cerebro- and cardiovascular diseases (including cerebral circulation insufficiency, coronary artery disease, coronary artery failure), severe autoimmune connective tissue diseases (including SLE, scleroderma), with inhibition of bone marrow hematopoiesis, with diabetes mellitus, hyperkalemia, bilateral stenosis of the renal arteries, stenosis of the artery of a single kidney, condition after kidney transplantation, renal renal hematopoiesis and / or liver failure, against the background of a diet with sodium restriction, conditions accompanied by a decrease in BCC (including diarrhea, vomiting), in elderly patients.
In patients with chronic heart failure, captopril is used under close medical supervision.
Arterial hypotension that occurs during surgery while taking captopril is eliminated by replenishing the volume of fluid.
Should be avoided simultaneous use of potassium-sparing diuretics and potassium preparations, especially in patients with renal insufficiency and diabetes mellitus.
When taking captopril, a false-positive reaction may be observed when analyzing urine for acetone.
The use of captopril in children is possible only in case of ineffectiveness of other drugs.
Influence on the ability to drive vehicles and mechanisms
Caution is necessary when driving vehicles or performing other work that requires increased attention, because dizziness is possible, especially after the initial dose of captopril.
With simultaneous use with immunosuppressants, cytostatics, the risk of developing leukopenia increases.
With simultaneous use with potassium-sparing diuretics (including spironolactone, triamterene, amiloride), potassium preparations, salt substitutes and Dietary supplements for food containing potassium may develop hyperkalemia (especially in patients with impaired renal function), because ACE inhibitors reduce the content of aldosterone, which leads to a delay in potassium in the body against the background of limiting the excretion of potassium or its additional intake into the body.
With the simultaneous use of ACE inhibitors and NSAIDs, the risk of developing impaired renal function increases; hyperkalemia is rarely observed.
With simultaneous use with "loop" diuretics or thiazide diuretics, pronounced arterial hypotension is possible, especially after taking the first dose of a diuretic, apparently due to hypovolemia, which leads to a transient increase in the antihypertensive effect of captopril. There is a risk of hypokalemia. Increased risk of developing impaired renal function.
With simultaneous use with anesthesia agents, severe arterial hypotension is possible.
When used simultaneously with azathioprine may develop anemia, which is due to inhibition of the activity of erythropoietin under the influence of ACE inhibitors and azathioprine. Cases of leukopenia development are described, which may be associated with additive inhibition of bone marrow function.
With simultaneous use with allopurinol, the risk of developing hematological disorders increases; cases 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 decreases.
Acetylsalicylic acid in high doses can reduce the antihypertensive effect of captopril. It has not been conclusively established 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 synthesis prostaglandins can cause vasoconstriction, which leads to a decrease in cardiac output and a worsening of the condition of patients with heart failure receiving ACE inhibitors.
There are reports of an increase in the concentration of digoxin in the blood plasma with the simultaneous use of captopril with digoxin. The risk of developing drug interactions is increased in patients with impaired renal function.
With simultaneous use with indomethacin, ibuprofen, the antihypertensive effect of captopril decreases, apparently due to inhibition under the influence of NSAIDs of the synthesis of prostaglandins (which are believed to play a role in the development of the hypotensive effect of ACE inhibitors).
With simultaneous use with insulin, hypoglycemic agents of sulfonylurea derivatives, hypoglycemia may develop by increasing glucose tolerance.
With the simultaneous use of ACE inhibitors and interleukin-3 there is a risk of developing arterial hypotension.
With simultaneous use with interferon alfa-2a or interferon beta, cases of severe granulocytopenia are described.
When switching from taking clonidine to captopril, the antihypertensive effect of the latter develops gradually. In the case of sudden withdrawal of clonidine in patients receiving captopril, a sharp increase in blood pressure is possible.
With the simultaneous use of lithium carbonate, the concentration of lithium in the blood serum increases, accompanied by symptoms of intoxication.
With simultaneous use with minoxidil, sodium nitroprusside, the antihypertensive effect is enhanced.
With simultaneous use with orlistat, it is possible to reduce the effectiveness of captopril, which can lead to an increase in blood pressure, hypertensive crisis, a case of cerebral hemorrhage is described.
With the simultaneous use of ACE inhibitors with pergolide, amplification is possible antihypertensive effect.
With simultaneous use with probenecid, the renal clearance of captopril decreases.
With simultaneous use with procainamide, the risk of developing leukopenia may increase.
With simultaneous use with trimethoprim, there is a risk of developing hyperkalemia, especially in patients with impaired renal function.
With simultaneous use with chlorpromazine, there is a risk of developing orthostatic hypotension.
With simultaneous use with cyclosporine, there are reports of the development of acute renal failure, oliguria.
It is believed that it is possible to reduce the effectiveness of antihypertensive drugs with simultaneous use with erythropoietins.
Dosage and Administration
Captopril is prescribed an hour before meals. The dosage regimen is set individually.
With arterial hypertension: The drug is prescribed in the initial dose of 25 mg 2 times a day. If necessary, the dose is gradually (with an interval of 2-4 weeks) increase until the optimal effect is achieved.
With mild or moderate arterial hypertension, the usual maintenance dose is 25 mg 2 times a day; The maximum dose is 50 mg 2 times a day.
In severe arterial hypertension, the maximum dose is 50 mg 3 times a day. The maximum daily dose is 150 mg.
For the treatment of chronic heart failure, Captopril is prescribed in cases where the use of diuretics does not provide an adequate effect. The average maintenance dose is 25 mg 2-3 times a day. In the future, if necessary, the dose is gradually (with an interval of at least 2 weeks) increased. The maximum dose is 150 mg per day.
Use in patients with impaired renal function Patients with impaired renal function with a moderate degree of impaired renal function (creatinine clearance of at least 30 ml / min / 1.73 m 2 ) Captopril can be prescribed at a dose of 75-100 mg / day. With a more pronounced degree of impaired renal function (creatinine clearance less than 30 ml / min / 1.73 m 2), the initial dose should be no more than 12.5-25 mg / day; in the future, if necessary, with sufficiently long intervals, the dose of Captopril is gradually increased, but a smaller than usual daily dose of the drug is used.
Symptoms: severe arterial hypotension, up to collapse, myocardial infarction, acute cerebral circulation disorder, thromboembolic complications.
Treatment: lay 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. It is possible to use hemodialysis; peritoneal hemodialysis is ineffective.
From the side of the central nervous system and the peripheral nervous system: dizziness, headache, feeling tired, asthenia, paresthesia.
From the cardiovascular system: orthostatic hypotension; rarely - tachycardia.
From the digestive system: nausea, decreased appetite, impaired 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 hematopoietic system: rarely - neutropenia, anemia, thrombocytopenia; very rarely in patients with autoimmune diseases - agranulocytosis.
From the side of metabolism: hyperkalemia, acidosis.
From the urinary system: proteinuria, impaired renal function (increased concentration of urea and creatinine in the blood).
From the respiratory side system: dry cough.
Allergic reactions: skin rash; rarely - Quincke's edema, bronchospasm, serum sickness, lymphadenopathy; in some cases - the appearance of antinuclear antibodies in the blood.
In a dry place, at temperatures below 30°C.
Keep out of reach of children.
- Dosage form
- 50 mg
- Number of tablets
- INN Russian