Captopril, pills 50mg, 40pcs

Composition

of 1 tab. – captopril 50 mg

Pharmacological action

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 vasoconstrictive 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 plasma renin, a decrease in blood pressure is noted at normal or even reduced concentrations of the hormone, which is due to the effect on the tissue RAAS. Increases coronary and renal blood flow.

Due to its vasodilating action, 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 load tolerance. With prolonged use, it reduces the severity of left ventricular hypertrophy, prevents the progression of heart failure and slows down the development of left ventricular dilation. Helps to reduce the sodium content in patients with chronic heart failure. Dilates the arteries to a greater extent than the veins. Improves blood supply to the ischemic myocardium. Reduces platelet aggregation.

Lowers the tone of the glomerular arterioles of the kidneys, improving intra-glomerular hemodynamics, prevents the development of diabetic nephropathy.

Indications

Arterial hypertension (including renovascular hypertension), chronic heart failure (as part of combination therapy), left ventricular dysfunction after myocardial infarction in patients who are in a clinically stable condition. Diabetic nephropathy in type 1 diabetes mellitus (with albuminuria greater than 30 mg / day).

Use during pregnancy and lactation

It should be borne in mind that the use of captopril in the second and third trimesters of pregnancy can cause developmental disorders and fetal death. If pregnancy is established, captopril should be discontinued immediately. Captopril is excreted in breast milk. If it is necessary to use during lactation, the question of stopping breastfeeding should be decided.

Contraindications

Pregnancy, lactation, age up to 18 years, hypersensitivity to captopril and other ACE inhibitors.

Side effects

From the central nervous system and peripheral nervous system:  dizziness, headache, fatigue, asthenia, paresthesia.

From the cardiovascular system:  orthostatic hypotension; rarely tachycardia.

From the digestive system:  nausea, decreased appetite, impaired taste sensations; 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).

Respiratory system disorders:  dry cough.

Allergic reactions:  skin rash; rarely-angioedema, bronchospasm, serum sickness, lymphadenopathy; in some cases-the appearance of antinuclear antibodies in the blood.

Interaction

When used concomitantly with immunosuppressants, cytostatics, the risk of developing leukopenia increases.

When used concomitantly with potassium-sparing diuretics (including spironolactone, triamterene, amiloride), potassium preparations, salt substitutes and dietary supplements containing potassium, hyperkalemia may develop (especially in patients with impaired renal function), since ACE inhibitors reduce the content of aldosterone, which leads to potassium retention in the body against the background of limiting the excretion of potassium or its additional intake into the body.

Concomitant use of ACE inhibitors and NSAIDs increases the risk of developing impaired renal function; hyperkalemia is rarely observed.

When used concomitantly with loop diuretics or thiazide diuretics, severe hypotension is possible, especially after taking the first dose of the 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.

When used concomitantly with anaesthetic agents, severe hypotension is possible.

When used concomitantly with azathioprine, anemia may develop, which is due to inhibition of erythropoietin activity under the influence of ACE inhibitors and azathioprine. Cases of leukopenia are described, which may be associated with additive suppression of bone marrow function.

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

With the simultaneous use of aluminum hydroxide, magnesium hydroxide, magnesium carbonate, the bioavailability of captopril decreases.

Acetylsalicylic acid in high doses may reduce the antihypertensive effect of captopril. It has not been definitively established whether acetylsalicylic acid reduces the therapeutic efficacy of ACE inhibitors in patients with CHD and heart failure. The nature of this interaction depends on the course of the disease. Acetylsalicylic acid, by inhibiting COX and prostaglandin synthesis, 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 increased plasma digoxin concentrations when captopril is co-administered with digoxin. The risk of drug interactions is increased in patients with impaired renal function.

When used concomitantly with Indometacin, ibuprofen, the antihypertensive effect of captopril decreases, apparently due to the inhibition of prostaglandin synthesis under the influence of NSAIDs (which are believed to play a role in the development of the antihypertensive effect of ACE inhibitors).

When used concomitantly with insulins, hypoglycemic agents and sulfonylureas, hypoglycemia may develop due to increased glucose tolerance.

Concomitant use of ACE inhibitors and interleukin-3 increases the risk of hypotension.

When used concomitantly with Interferon alfa-2a or interferon beta, cases of severe granulocytopenia have been described.

When switching from taking clonidine to captopril, the antihypertensive effect of the latter develops gradually. In case of sudden withdrawal of clonidine in patients receiving captopril, a sharp increase in blood pressure may occur.

Concomitant use of lithium carbonate increases the concentration of lithium in the blood serum, accompanied by symptoms of intoxication.

When used concomitantly with minoxidil, sodium nitroprusside, the antihypertensive effect is enhanced.

When used concomitantly with orlistat, the effectiveness of captopril may decrease, which may lead to an increase in blood pressure, a hypertensive crisis, and a case of brain hemorrhage is described.

When ACE inhibitors are co-administered with pergolide, the antihypertensive effect may be enhanced.

When used concomitantly with probenecid, the renal clearance of captopril decreases.

Concomitant use with procainamide may increase the risk of developing leukopenia.

When used concomitantly with trimethoprim, there is a risk of hyperkalemia, especially in patients with impaired renal function.

When used concomitantly with chlorpromazine, there is a risk of developing orthostatic hypotension.

When used concomitantly with cyclosporine, acute renal failure and oliguria have been reported.

It is believed that it is possible to reduce the effectiveness of antihypertensive drugs when used simultaneously with erythropoietins.

How to take it, course of administration and dosage

When taken orally, the initial dose is 6.25-12.5 mg 2-3 times a day.

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

The maximum daily dose is 150 mg.

Overdose

Symptoms of overdose: a sharp drop in blood pressure. Recommended treatment: intravenous administration of a plasma-substituting solution (for example,0.9% sodium chloride solution), hemodialysis.

Special instructions

C caution should be used when referring to a history of angioedema during therapy with ACE inhibitors, hereditary or idiopathic angioedema, with aortic stenosis, Cerebro – and cardiovascular diseases (including the cerebrovascular insufficiency, coronary artery disease, coronary insufficiency), severe autoimmune connective tissue diseases (including SLE, scleroderma), when the oppression of bone marrow hematopoiesis, diabetes mellitus, hyperkalemia, bilateral renal artery stenosis, stenosis of the artery to a solitary kidney, condition after kidney transplantation, renal and/or hepatic insufficiency on the background of a diet with restriction of sodium, state, accompanied by a decrease in BCC (including diarrhea, vomiting), in patients of advanced age. 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. Concomitant use of potassium-sparing diuretics and potassium supplements should be avoided, especially in patients with renal insufficiency and diabetes mellitus. When taking captopril, a false positive reaction may occur in the urine test for acetone. The use of captopril in children is possible only if other drugs are ineffective. Effects on the ability to drive motor vehicles and operate mechanisms: Caution is required when driving vehicles or performing other work that requires increased attention, as dizziness may occur, especially after the initial dose of captopril. In case of renal insufficiency, caution should be used in the condition after kidney transplantation, renal failure. In case of impaired renal function, the daily dose should be reduced. Concomitant use of potassium-sparing diuretics and potassium supplements should be avoided in patients with renal insufficiency. When liver function is impaired, caution should be used in patients with hepatic insufficiency. The elderly should be used with caution in elderly patients.

Form of production

Tablets

Storage conditions

Keep out of reach of children in a dry place at temperatures up to 30 °C.

Shelf

life is 3 years.

Active ingredient

Captopril

Conditions of release from pharmacies

By prescription

Dosage form

Tablets