Captopril tablets Sandoz 25mg, No. 40

• Arterial hypertension (including renovascular),

• chronic heart failure (as part of combination therapy),

• dysfunction of the left ventricle after myocardial infarction in clinically stable patients.

• Diabetic nephropathy in type 1 diabetes mellitus (with albuminuria more than 30 mg / day).

When administered orally, 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.

.active substance: captopril - 25 mg

excipients: microcrystalline cellulose; milk sugar; corn starch; magnesium stearic acid

• hypersensitivity to captopril and other ACE inhibitors;

• Quincke's edema (including a history after the use of ACE inhibitors);

• severe renal dysfunction, azotemia, hyperkalemia, bilateral renal artery stenosis or stenosis of a solitary kidney artery with progressive azotemia, condition after kidney transplantation, primary hyperaldosteronism;

• aortic stenosis, mitral stenosis, the presence of other obstructions to the outflow of blood from the left ventricle of the heart;

• severe liver dysfunction;

• arterial hypotension;

• cardiogenic shock;

• pregnancy;

• lactation period;

• children under 18 years of age.

pharmachologic 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 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 antihypertensive effect does not depend on the plasma renin activity, a decrease in blood pressure is noted at normal and even reduced hormone concentration, which is due to the effect on the tissue RAAS. Increases coronary and renal blood flow.

Due to the vasodilating effect, it reduces the OPSS (afterload), the pressure of wedging in the pulmonary capillaries (preload) and resistance in the pulmonary vessels; increases cardiac output 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 reduce sodium in patients with chronic heart failure. Expands arteries more than veins. Improves blood supply to the ischemic myocardium. Reduces platelet aggregation.

Reduces the tone of the efferent arterioles of the renal glomeruli, improving intraglomerular hemodynamics, and prevents the development of diabetic nephropathy

Indications of the active substances of the drug

• Arterial hypertension (including renovascular),

• chronic heart failure (as part of combination therapy),

• dysfunction of the left ventricle after myocardial infarction in clinically stable patients.

• Diabetic nephropathy in type 1 diabetes mellitus (with albuminuria more than 30 mg / day).

Dosage regimen

When administered orally, 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 effect

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

On the part of 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).

Respiratory system: dry cough.

Allergic reactions: skin rash; rarely - Quincke's edema, bronchospasm, serum sickness, lymphadenopathy; in some cases - the appearance of anti-nuclear antibodies in the blood.

Contraindications for use

• Pregnancy,

• lactation period,

• age up to 18 years,

• hypersensitivity to captopril and other ACE inhibitors.

Application 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.

If pregnancy is established, captopril should be discontinued immediately.

Captopril is excreted in breast milk.

If necessary, use during lactation should decide on the termination of breastfeeding.

Application for violations of liver function

It should be used with caution in liver failure.

Application for impaired renal function

It should be used with caution in the condition 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 should be avoided in patients with renal insufficiency.

Application in children

Contraindicated under the age of 18. The use of captopril in children is possible only if other drugs are ineffective.

Use in elderly patients

It should be used with caution in elderly patients.

special instructions

It should be used with caution if there is a history of angioedema during therapy with ACE inhibitors, hereditary or idiopathic angioedema, with aortic stenosis, cerebro- and cardiovascular diseases (including with cerebral circulatory insufficiency, coronary artery disease, coronary insufficiency), severe autoimmune diseases of connective tissue (including SLE, scleroderma), with inhibition of bone marrow hematopoiesis, with diabetes mellitus, hyperkalemia, bilateral renal artery stenosis, stenosis of the artery of a single kidney, condition after kidney transplantation, renal and / or liver failure, in the background diets 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.

The arterial hypotension that occurs during surgery while taking captopril is eliminated by replenishing the volume of fluid.

The simultaneous use of potassium-sparing diuretics and potassium preparations should be avoided, especially in patients with renal failure and diabetes mellitus.

When taking captopril, a false positive reaction may occur when urine is analyzed for acetone.

The use of captopril in children is possible only if other drugs are ineffective.

Influence on the ability to drive vehicles and use mechanisms

Caution is required when driving or performing other work requiring increased attention, as dizziness may occur, especially after the initial dose of captopril.

Drug interactions

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 containing potassium, hyperkalemia may develop (especially in patients with impaired renal function), because ACE inhibitors reduce the content of aldosterone, which leads to a retention of 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 renal dysfunction increases; hyperkalemia is rarely observed.

With simultaneous use with 'loop' diuretics or thiazide diuretics, severe 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 developing hypokalemia. Increased risk of renal dysfunction.

With simultaneous use with drugs for anesthesia, severe arterial hypotension is possible.

With simultaneous use with azathioprine, anemia may develop, which is due to inhibition of the activity of erythropoietin under the influence of ACE inhibitors and azathioprine. Cases of the development of leukopenia have been described, which may be associated with an additive inhibition of bone marrow function.

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

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 definitively 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, by inhibiting COX and prostaglandin synthesis, can cause vasoconstriction, which leads to a decrease in cardiac output and 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 while using captopril with digoxin. The risk of 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 the inhibition of prostaglandin synthesis under the influence of NSAIDs (which are believed to play a role in the development of the hypotensive effect of ACE inhibitors).

With simultaneous use with insulins, hypoglycemic agents, sulfonylurea derivatives, hypoglycemia may develop due to an increase in 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 alpha-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 the case of a 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 has been described.

With the simultaneous use of ACE inhibitors with pergolide, an increase in the antihypertensive effect is possible.

With simultaneous use with probenecid, the renal clearance of captopril decreases.

With simultaneous use with procainamide, an increase in the risk of developing leukopenia is possible.

With simultaneous use 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, 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 when used simultaneously with erythropoietins.