Captopril, tablets 50 mg 40 pcs.

An 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 marked vasoconstrictor effect and stimulates aldosterone secretion in the adrenal cortex). In addition, captopril appears to affect the kinin-callikrein system by inhibiting the breakdown of bradykinin. Hypotensive effect does not depend on the activity of plasma renin, BP reduction is noted at normal and even reduced concentration of the hormone, which is due to the effect on tissue RAAS. It increases coronary and renal blood flow.

Owing to the vasodilator effect, it decreases ROS (post-load), congestion pressure in the pulmonary capillaries (preload) and resistance in the pulmonary vessels; it increases cardiac minute volume and exercise tolerance. With long-term use, it reduces the severity of left ventricular myocardial hypertrophy, prevents the progression of heart failure and slows the development of left ventricular dilatation. Helps reduce sodium in patients with chronic heart failure. Dilates arteries more than veins. Improves blood supply to ischemic myocardium. Reduces platelet aggregation.

Lowering tone of the renal tubular arterioles, improving intra-column hemodynamics, prevents the development of diabetic nephropathy.

Indications

Active ingredient

Composition

How to take, the dosage

In case of oral administration, the initial dose is 6.25-12.5 mg 2-3 times a day.

In case of insufficient effect the dose is gradually increased to 25-50 mg 3 times per day. In case of impaired renal function, the daily dose should be reduced.

The maximum daily dose is 150 mg.

Interaction

In concomitant use with immunosuppressants, cytostatics the risk of leukopenia increases.

Concomitant use with potassium-saving diuretics (including spironolactone, triamterene, amiloride), potassium preparations, salt substitutes and food supplements containing potassium may lead to hyperkalemia (especially in patients with renal impairment).Because ACE inhibitors decrease the content of aldosterone, which leads to potassium retention in the body against the background of potassium excretion restriction or its additional intake.

The simultaneous use of ACE inhibitors and NSAIDs increases the risk of renal dysfunction; hyperkalemia is rare.

Concomitant use with “loop” diuretics or thiazide diuretics may cause significant arterial hypotension, particularly after the first dose of diuretics, probably due to hypovolemia, which leads to transient enhancement of antihypertensive effect of captopril. There is a risk of hypokalemia. There is an increased risk of developing renal function abnormalities.

Serious arterial hypotension is possible when used concomitantly with anesthetics.

In concomitant use with azathioprine anemia may occur due to inhibition of erythropoietin activity caused by ACE inhibitors and azathioprine. There have been described cases of leukopenia, which may be associated with additive suppression of bone marrow function.

Concomitant use with allopurinol increases the risk of hematologic disorders; there have been described cases of severe hypersensitivity reactions, including Stevens-Johnson syndrome.

The co-administration of aluminum hydroxide, magnesium hydroxide, magnesium carbonate decreases the bioavailability of captopril.

Acetylsalicylic acid in high doses may decrease the antihypertensive effect of captopril. Whether acetylsalicylic acid reduces the therapeutic efficacy of ACE inhibitors in patients with CHD and heart failure has not been definitively established. The nature of this interaction depends on the course of the disease. Acetylsalicylic acid, by inhibiting COX and prostaglandin synthesis, may cause vasoconstriction, which leads to decreased cardiac output and deterioration in patients with heart failure receiving ACE inhibitors.

There have been reports of increased plasma concentrations of digoxin when concomitant use of captopril with digoxin. The risk of drug interaction is increased in patients with impaired renal function.

Concomitant use with indomethacin, ibuprofen decreases antihypertensive effect of captopril, probably due to inhibition by NSAIDs of prostaglandin synthesis (which is believed to play a role in development of hypotensive effect of ACE inhibitors).

In concomitant use with insulin and hypoglycemic agents with sulfonylurea derivatives, hypoglycemia may develop due to increased glucose tolerance.

In concomitant use of ACE inhibitors and interleukin-3, there is a risk of arterial hypotension.

In concomitant use with interferon alpha-2a or interferon beta, cases of severe granulocytopenia have been described.

When switching from clonidine to captopril, the antihypertensive effect of the latter develops gradually. If clonidine is abruptly withdrawn, patients receiving captopril may experience a sharp increase in BP.

Concomitant use of lithium carbonate increases serum lithium concentration accompanied by intoxication symptoms.

Concomitant use with minoxidil, sodium nitroprusside increases the antihypertensive effect.

Concomitant use with orlistat may decrease the effectiveness of captopril, which may lead to increased BP, hypertensive crisis, a case of cerebral hemorrhage has been described.

The simultaneous use of ACE inhibitors with pergolide may increase the antihypertensive effect.

Concomitant use with probenecid decreases renal clearance of captopril.

Concomitant use with procainamide may increase the risk of leukopenia.

Concomitant use with trimethoprim poses a risk of hyperkalemia, especially in patients with renal impairment.

Concomitant use with chlorpromazine causes a risk of orthostatic hypotension.

In concomitant use with cyclosporine there have been reports of acute renal failure and oliguria.

It is believed that there may be a decrease in the effectiveness of antihypertensive agents when used concomitantly with erythropoietins.

Special Instructions

Contraindications

Side effects

CNS and peripheral nervous system disorders: dizziness, headache, fatigue, asthenia, paresthesias.

Cardiovascular system: orthostatic hypotension; rarely – tachycardia.

The digestive system: nausea, decreased appetite, impaired sense of taste; rarely – abdominal pain, diarrhea or constipation, increased liver transaminase activity, hyperbilirubinemia; signs of hepatocellular damage (hepatitis); in rare cases – cholestasis; in single cases – pancreatitis.

Hematopoietic system: rare – neutropenia, anemia, thrombocytopenia; very rare in patients with autoimmune diseases – agranulocytosis.

Mechanical disorders: hyperkalemia and acidosis.

Urinary system disorders: proteinuria, renal dysfunction (increased concentration of urea and creatinine in blood).

Respiratory system disorders: dry cough.

Allergic reactions: skin rash; rarely – Quincke’s edema, bronchospasm, serum sickness, lymphoadenopathy; in some cases – appearance of antinuclear antibodies in blood.

Overdose

Pregnancy use

Similarities