Captopril 50 mg instructions for use. Captopril - indications and instructions for use (how to take tablets), analogues and reviews. At what dosage of the drug does blood pressure normalize? Action when applied under the tongue. central nervous system

1 tablet contains:

active substance: captopril 25 mg or 50 mg;

Excipients: microcrystalline cellulose, milk sugar, corn starch, aerosil, magnesium stearate.

Tablets of white or off-white color with a characteristic odor, biconvex with a score on one side. Light marbling is allowed. In appearance they must comply with the requirements of the Global Fund XI, issue. 2, p. 154.

Absorption is fast, reaches 75% (meal reduces absorption by 30-40%). Bioavailability - 35-40% (first pass effect through the liver). Communication with blood plasma proteins (mainly albumin) - 25-30%. The maximum concentration in blood plasma (114 ng/ml) after oral administration is achieved after 30-90 minutes. It penetrates poorly through the blood-brain barrier and placental barrier (less than 1%). Metabolized in the liver to form captopril disulfide dimer and captopril-cysteine ​​disulfide. Metabolites are pharmacologically inactive.

The half-life is 3 hours. 95% is excreted by the kidneys (40-50% unchanged, the rest in the form of metabolites). Secreted into mother's milk. 4 hours after a single oral dose, the urine contains 38% unchanged captopril and 28% in the form of metabolites, after 6 hours - only in the form of metabolites; in daily urine - 38% unchanged captopril and 62% in the form of metabolites. The half-life for impaired renal function is 3.5-32 hours. Cumulates in chronic renal failure.

Arterial hypertension, including renovascular; chronic heart failure (as part of complex therapy); dysfunction of the left ventricle after myocardial infarction in a clinically stable condition; diabetic nephropathy against the background of type I diabetes mellitus (with albuminuria more than 30 mg/day).

Hypersensitivity to the drug and other ACE inhibitors, angioedema (due to the use of ACE inhibitors, including in history); severe renal or liver dysfunction; hyperkalemia; bilateral renal artery stenosis or stenosis of the artery of a single kidney with progressive azotemia; condition after kidney transplantation; stenosis of the aortic mouth and similar obstructive changes that impede the outflow of blood; pregnancy, lactation period; age up to 18 years.

Severe autoimmune diseases (especially SLE or scleroderma), suppression of bone marrow hematopoiesis (risk of developing neutropenia and agranulocytosis), cerebral ischemia, diabetes mellitus (increased risk of developing hyperkalemia); patients on hemodialysis; sodium-restricted diet; primary hyperaldosteronism; cardiac ischemia; conditions accompanied by a decrease in circulating blood volume (including diarrhea, vomiting); elderly age.

Captopril-STI is prescribed orally 1 hour before meals. The dosage regimen is set individually.

For arterial hypertension, treatment is prescribed with the lowest effective dose of 12.5 mg 2 times a day (rarely with 6.25 mg 2 times a day). Attention should be paid to the tolerability of the first dose within the first hour. If arterial hypotension develops, the patient should be transferred to a horizontal position (such a reaction to the first dose should not serve as an obstacle to further therapy). If necessary, the dose is gradually increased (with an interval of 2-4 weeks) until the optimal effect is achieved. For mild or moderate arterial hypertension, the usual maintenance dose is 25 mg 2 times a day; the maximum dose is 50 mg 3 times a day. The maximum daily dose is 150 mg.

In case of heart failure, it is prescribed together with diuretics and/or in combination with digitalis preparations (to avoid an initial excessive decrease in blood pressure, the diuretic is canceled or the dose is reduced before prescribing Captopril-STI). The initial dose is 6.25 mg or 12.5 mg 3 times a day, if necessary, the dose is increased to 25 mg 3 times a day. The maximum daily dose is 150 mg.

In cases of left ventricular dysfunction after myocardial infarction in patients who are in a clinically stable condition, the use of Captopril-STI can be started within 3 days after myocardial infarction. The initial dose is 6.25 mg/day, then the daily dose can be increased to 37.5 - 75 mg in 2-3 doses (depending on the tolerability of the drug). If necessary, the dose is gradually increased to a maximum daily dose of 150 mg/day.

If arterial hypotension develops, a dose reduction may be required.

Subsequent attempts at a maximum daily dose of 150 mg should be based on patient tolerance to Captopril-STI.

For diabetic nephropathy, Captopril-STI is prescribed in a daily dose of 75-100 mg/day in 2-3 doses. For insulin-dependent diabetes with microalbuminuria (albumin release 30-300 mg per day), the dose of the drug is 50 mg 2 times a day. With a total protein clearance of more than 500 mg per day, the drug is effective at a dose of 25 mg 3 times a day.

With a moderate degree of renal dysfunction (creatinine clearance - at least 30 ml/min./1.73 sq.m.), Captopril-STI can be prescribed at a dose of 75-100 mg/day. With a more pronounced degree of renal dysfunction (creatinine clearance - less than 30 ml/min/1.73 sq. m), the initial dose should be no more than 12.5 mg/day; in the future, if necessary, the dose of Captopril-STI is gradually increased at sufficiently long intervals, but a lower daily dose of the drug is used than in the case of treating arterial hypertension.

If necessary, loop diuretics are additionally prescribed rather than thiazide diuretics.

From the cardiovascular system: tachycardia, decreased blood pressure, orthostatic hypotension, peripheral edema.

From the nervous system: dizziness, headache, feeling of fatigue, asthenia, paresthesia.

From the respiratory system: dry cough, pulmonary edema, bronchospasm.

From the urinary system: proteinuria, deterioration of kidney function (increased levels of urea and creatinine in the blood).

From the side of water-electrolyte metabolism: hyperkalemia, hyponatremia (most often with a salt-free diet and concomitant use of diuretics), proteinuria, increased levels of urea nitrogen and creatinine in the blood, acidosis.

From the digestive system: decreased appetite, impaired taste, dry mouth, stomatitis, nausea, abdominal pain, dyspepsia, constipation or diarrhea, increased activity of liver transaminases, hyperbilirubinemia, signs of hepatocellular damage (hepatitis) and cholestasis (in rare cases); pancreatitis (in isolated cases).

From the hematopoietic organs: neutropenia, anemia, thrombocytopenia, agranulocytosis.

Allergic reactions: skin rash (maculopapular, less often - vesicular or bullous in nature), itching, angioedema, "flushes" of blood to the skin of the face, fever, photosensitivity, serum sickness, lymphadenopathy, in rare cases - the appearance of antinuclear antibodies in the blood.

Others: general weakness.

Symptoms: marked decrease in blood pressure up to collapse, myocardial infarction, acute cerebrovascular accident, thromboembolic complications.

Treatment: place the patient with the lower limbs elevated; take measures aimed at restoring blood pressure (increasing the volume of circulating blood, including intravenous infusion of saline), symptomatic therapy.

Hemodialysis may be used; peritoneal dialysis is not effective.

Captopril increases the concentration of digoxin in the blood plasma by 15-20%.

Increases the bioavailability of propranolol.

Cimetidine, by slowing down metabolism in the liver, increases the concentration of captopril in the blood plasma.

The hypotensive effect is weakened by non-steroidal anti-inflammatory drugs (Na + retention and decreased prostaglandin synthesis).

Combination with thiazide diuretics, vasodilators (), verapamil, beta-blockers, tricyclic antidepressants, ethanol, enhances the hypotensive effect.

Combined use with potassium-sparing diuretics, potassium preparations, cyclosporine, potassium supplements, salt substitutes (contain significant amounts of K +) increases the risk of developing hyperkalemia.

Slows down the elimination of lithium drugs.

When used in combination with procainamide, allopurinol, flecainide, the risk of developing immunosuppressive effects increases.

Probenecid slows down the excretion of captopril in the urine.

Clonidine reduces the severity of the hypotensive effect.

Immunosuppressants (or) increase the risk of developing hematological disorders.

Before starting, as well as regularly during treatment with Captopril-STI, renal function should be monitored. In patients with chronic heart failure, it is used under close medical supervision.

During long-term use of Captopril-STI, approximately 20% of patients experience an increase in serum urea and creatinine by more than 20% compared to the norm or baseline value. In less than 5% of patients, especially with severe nephropathy, treatment discontinuation is required due to an increase in creatinine concentration.

In patients with arterial hypertension, when using Captopril-ST, severe arterial hypotension is observed only in rare cases. The likelihood of developing arterial hypotension increases with fluid and salt deficiency (for example, after intensive treatment with diuretics), in patients with heart failure or on dialysis.

The possibility of a sharp decrease in blood pressure can be minimized by first withdrawing (4-7 days before) the diuretic or increasing sodium chloride intake (about a week before starting treatment), or by prescribing Captopril-STI at the beginning of treatment in small doses (6 ,25-12.5 mg/day).

In the first 3 months of therapy, the number of blood leukocytes is monitored monthly, then once every 3 months; in patients with autoimmune diseases in the first 3 months - every 2 weeks, then every 2 months. If the number of leukocytes is below 4000/μl, a general blood test is indicated; below 1000/μl, the drug is stopped.

In some cases, against the background of the use of ACE inhibitors, incl. Captopril-STI, there is an increase in the concentration of K+ in the blood serum. The risk of developing hyperkalemia when using captopril is increased in patients with renal failure and diabetes mellitus, as well as those taking potassium-sparing diuretics, potassium supplements or other drugs that cause an increase in the concentration of K+ in the blood (for example, heparin). The simultaneous use of potassium-sparing diuretics and potassium supplements should be avoided.

When performing hemodialysis in patients receiving Captopril-STI, the use of high-permeability dialysis membranes (for example, AN 69) should be avoided, since in such cases the risk of developing anaphylactoid reactions increases. If angioedema develops, the drug is discontinued and careful medical observation and symptomatic therapy are carried out.

When taking Captopril-STI, a false-positive reaction may occur in a urine test for acetone.

Prescribe with caution to patients on a low-salt or salt-free diet (increased risk of developing arterial hypotension).

Tablets of 25 and 50 mg.

10 tablets per blister pack (blister) or 20, 30, 40, 50 or 60 tablets per polymer jar or polymer bottle.

2, 3, 4, 5 or 6 blisters or a jar or bottle along with instructions for use are placed in a cardboard box.

In a dry place, protected from light, at a temperature not exceeding 25°C.

Keep out of the reach of children.

Do not use after the expiration date stated on the package.

Active substance: captopril 50 mg; 25 mg.

Antihypertensive drug, 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 plasma renin; a decrease in blood pressure is observed at normal and even reduced concentrations of the hormone, which is due to the effect on the tissue RAAS. Increases coronary and renal blood flow.
Thanks to its vasodilating effect, it reduces roundabout percentage (afterload), wedge pressure in the pulmonary capillaries (preload) and resistance in the pulmonary vessels; increases cardiac output and exercise tolerance. With long-term use, it reduces the severity of left ventricular myocardial hypertrophy, prevents progression and slows down the development of left ventricular dilatation. Helps reduce sodium levels in patients with chronic heart failure. Dilates arteries more than veins. Improves blood supply to ischemic myocardium. Reduces platelet aggregation.
Reduces the tone of the efferent arterioles of the glomeruli of the kidneys, improving intraglomerular hemodynamics, and prevents the development.

Pharmacokinetics. After oral administration, at least 75% is quickly absorbed from the gastrointestinal tract. Simultaneous food intake reduces absorption by 30-40%. Cmax in blood plasma is achieved after 30-90 minutes. Protein binding, mainly albumin, is 25-30%. Excreted in breast milk. Metabolized in the liver to form captopril disulfide dimer and captopril-cysteine ​​disulfide. Metabolites are pharmacologically inactive.
T1/2 is less than 3 hours and increases at (3.5-32 hours). More than 95% is excreted by the kidneys, 40-50% unchanged, the rest in the form of metabolites.
When cumulates.

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

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.

Caution should be used if there is a history of angioedema during therapy with ACE inhibitors, hereditary or idiopathic angioedema, aortic stenosis, cerebrovascular and cardiovascular diseases (including cerebrovascular insufficiency, ischemic heart disease, coronary insufficiency), severe autoimmune connective tissue diseases (including SLE), with suppression of bone marrow hematopoiesis, with diabetes mellitus, bilateral renal artery stenosis, stenosis of the artery of a single kidney, condition after kidney transplantation, renal and/or, on a sodium-restricted diet, conditions accompanied by a decrease in blood volume (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 fluid volume.

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

When taking captopril, a false-positive reaction may occur in a urine test for acetone.

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

Impact on the ability to drive vehicles and operate machinery
Caution is required when driving vehicles or performing other work that requires increased attention, because possible, especially after the initial dose of captopril.

From the central nervous system and peripheral nervous system: dizziness, feeling of fatigue, asthenia,.
From the cardiovascular system: orthostatic hypotension; rarely - .
From the digestive system: loss of appetite, disturbance of taste; rarely - abdominal pain, or increased activity of liver transaminases, hyperbilirubinemia; signs of hepatocellular damage (hepatitis); in some cases -; in isolated cases - .
From the hematopoietic system: rarely - , ; very rarely in patients with autoimmune diseases -.
Metabolism: hyperkalemia, acidosis.
From the urinary system: impaired renal function (increased concentration of urea and creatinine in the blood).
From the respiratory system: dry.
Allergic reactions: ; rarely - Quincke's edema; in some cases - the appearance of antinuclear antibodies in the blood.

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

When used simultaneously 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 potassium retention in the body while 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.

When used simultaneously with loop diuretics or thiazide diuretics, severe arterial 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 developing hypokalemia. Increased risk of developing renal dysfunction.

When used simultaneously with anesthetics, severe arterial hypotension is possible.

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

When used simultaneously with allopurinol, the risk of developing hematological disorders increases; 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 conclusively established whether acetylsalicylic acid reduces the therapeutic effectiveness 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 increased plasma concentrations of digoxin when captopril is administered concomitantly with digoxin. The risk of drug interactions is increased in patients with impaired renal function.

When used simultaneously with indomethacin and ibuprofen, the antihypertensive effect of captopril is reduced, apparently due to 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).

When used simultaneously with insulins, hypoglycemic agents and sulfonylurea derivatives, hypoglycemia may develop due to increased glucose tolerance.

With simultaneous use of ACE inhibitors and interleukin-3, there is a risk of developing arterial hypotension.

When used simultaneously 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 suddenly discontinued in patients receiving captopril, a sharp increase in blood pressure may occur.

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

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

When used simultaneously with orlistat, the effectiveness of captopril may decrease, which can lead to increased blood pressure, hypertensive crisis, and a case of cerebral hemorrhage has been described.

With simultaneous use of ACE inhibitors with pergolide, the antihypertensive effect may be enhanced.

When used simultaneously with probenecid, the renal clearance of captopril is reduced.

When used simultaneously with procainamide, the risk of developing leukopenia may increase.

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

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

When used simultaneously with cyclosporine, there are reports of the development of acute renal failure and oliguria.

It is believed that the effectiveness of antihypertensive drugs may be reduced when used simultaneously with erythropoietins.

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

Use during pregnancy and breastfeeding
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 it during lactation, the issue of stopping breastfeeding should be decided.

Use for liver dysfunction
Use with caution in case of liver failure.

Use for renal impairment
Use with caution in conditions after kidney transplantation or renal failure.
In case of impaired renal function, the daily dose should be reduced.
The simultaneous use of potassium-sparing diuretics and potassium supplements should be avoided in patients with renal failure.

Use in elderly patients
Use with caution in elderly patients.

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

Captopril-STI is an angiotensin-converting enzyme (ACE) inhibitor.

Release form and composition

Dosage form - tablets: biconvex, white or white with a creamy tint, possible slight marbling, characteristic odor, with a score on one side (in a cardboard pack there is 1 polymer jar or bottle containing 60 tablets, or 2, 3, 4, 5 or 6 packages of cellular contours containing 10 tablets each, and instructions for use of Captopril-STI).

Composition of 1 tablet of 25/50 mg:

• active ingredients: captopril – 25/50 mg;
• auxiliary components: talc – 1/2 mg; povidone K-17 – 1.975/3.95 mg; microcrystalline cellulose – 6.97/13.94 mg; corn starch – 7.98/15.96 mg; magnesium stearate – 1/2 mg; lactose monohydrate - to obtain a tablet weighing 100/200 mg.

Pharmacological properties

Pharmacodynamics

Captopril-STI is an ACE inhibitor that reduces the formation of angiotensin II from angiotensin I, which leads to a direct decrease in the release of aldosterone. Against this background, post- and preload on the heart, blood pressure (BP), as well as total peripheral vascular resistance are reduced.

The pharmacological actions of the drug, due to the properties of its active substance (captopril), also include:

• dilation of arteries (to a greater extent than veins);
• increased prostaglandin synthesis and decreased bradykinin degradation;
• increased renal and coronary blood flow;
• reduction in the severity of hypertrophy of the myocardial walls and resistive arteries (with long-term use of the drug);
• improvement of blood supply to ischemic myocardium;
• decreased platelet aggregation;
• decrease in Na + content in heart failure;
• lowering blood pressure without the development of reflex tachycardia (unlike direct vasodilators - minoxidil, hydralazine), leading to a decrease in myocardial oxygen demand.

The hypotensive effect of Captopril-STI does not depend on the activity of plasma renin, and a decrease in blood pressure during its use is observed with normal and even reduced levels of the hormone, which results from the effect on tissue renin-angiotensin systems.

In patients with heart failure, taking angiotensin-converting enzyme inhibitors in an adequate dose does not affect blood pressure.

After oral administration, the maximum decrease in blood pressure is observed after 1–1.5 hours. The duration of the hypotensive effect depends on the dose of Captopril-STI and reaches optimal values ​​over several weeks.

Pharmacokinetics

Absorption of captopril is rapid and reaches 75%, however, when eating food, it decreases by an average of 30–40%. Its bioavailability varies from 35 to 40%, and its binding to plasma proteins, mostly albumin, ranges from 25 to 30%.

After 30–90 minutes after oral administration, the maximum concentration of captopril in the blood plasma is reached - 114 ng per 1 ml. The substance is weak (< 1%) проникает через плацентарный и гематоэнцефалический барьеры. Его метаболизм проходит в печени с образованием фармакологически неактивных метаболитов дисульфидного димера каптоприла и каптоприл-цистеиндисульфида.

The half-life of the drug is 3 hours. 95% of excretion is carried out by the kidneys, with 40 to 50% excreted unchanged, and the remainder in the form of metabolites. The substance is secreted into mother's milk. 4 hours after a single oral dose, the content of unchanged captopril in the urine is 38%, in the form of metabolites - 28%, and after 6 hours it is detected only in the form of metabolites. The content of unchanged captopril in daily urine is 38%, in the form of metabolites – 62%.

In patients with impaired renal function, the half-life of the drug varies from 3.5 to 32 hours. In chronic renal failure, captopril accumulates.

Indications for use

• chronic heart failure (CHF), as part of complex treatment;
• arterial hypertension, including renovascular form;
• diabetic nephropathy in type 1 diabetes mellitus (with albuminuria above 30 mg/day);
• dysfunction of the left ventricle after myocardial infarction in patients with a clinically stable condition.

Contraindications

Absolute:

• angioedema that occurred during therapy with ACE inhibitors, including history;
• severe liver/kidney dysfunction;
• stenosis of the artery of a single kidney or bilateral stenosis of the renal arteries with progressive azotemia;
• stenosis of the aortic mouth and similar obstructive changes that impede the outflow of blood;
• hyperkalemia;
• condition after kidney transplantation;
• pregnancy and breastfeeding;
• age under 18 years;
• individual intolerance to the components of the drug and other ACE inhibitors.

Relative (Captopril-STI tablets are prescribed under medical supervision):

• cardiac ischemia;
• cerebral ischemia;
• inhibition of bone marrow hematopoiesis due to the likelihood of developing agranulocytosis and neutropenia;
• severe autoimmune pathologies (especially scleroderma or systemic lupus erythematosus);
• diabetes mellitus (due to an increased risk of hyperkalemia);
• primary hyperaldosteronism;
• conditions that are accompanied by a decrease in circulating blood volume, including vomiting and diarrhea;
• stay on hemodialysis;
• following a sodium-restricted diet;
• elderly age.

Captopril-STI, instructions for use: method and dosage

Captopril-STI tablets are taken orally 60 minutes before meals. The dosage is determined by the doctor individually.

• arterial hypertension: therapy begins with the minimum effective dose – 12.5 mg 2 times a day; in rare cases (including for elderly patients) – 6.25 mg 2 times a day. During the first hour after administration, it is important to monitor the patient's condition. If arterial hypertension appears, he should be transferred to the supine position. The development of such a reaction to the first dose should not serve as an obstacle to further treatment. If necessary, the dose is gradually increased, with an interval of 14–28 days, until the optimal therapeutic effect is achieved. The usual maintenance dose for mild or moderate arterial hypertension is 25 mg 2 times a day; maximum – 50 mg 3 times a day (150 mg);
• heart failure: initial dose - 6.25 or 12.5 mg 3 times a day, with a possible dose increase to 25 mg 3 times a day (if necessary). The maximum dose is 150 mg per day. Captopril-STI is prescribed in combination with diuretics or digitalis preparations. Before starting to take the drug, in order to avoid an initial excessive decrease in blood pressure, reduce the dose or discontinue the diuretic;
• dysfunction of the left ventricle after myocardial infarction in patients who are in a clinically stable condition: taking tablets can be started as early as 3 days after myocardial infarction at an initial dose of 6.25 mg per day. Further, the daily dose, depending on the tolerability of the drug, can be gradually increased to 37.5–75 mg, divided into 2–3 doses or, if necessary, gradually increased to a maximum of 150 mg per day. A dose reduction may be required in cases of arterial hypotension. Further attempts to prescribe the maximum dose of Captopril-STI (150 mg per day) should be based on the patient's tolerability of the drug;
• diabetic nephropathy: 75 to 100 mg per day, divided into 2 to 3 doses. Patients with insulin-dependent diabetes with microalbuminuria (daily albumin excretion varies from 30 to 300 mg) take 50 mg of Captopril-STI 2 times a day. If the total protein clearance exceeds 500 mg per day, taking the drug at a dose of 25 mg 3 times a day is effective.

In cases of moderate renal dysfunction (creatinine clearance - at least 30 ml per 1 min per 1.37 m2), the drug is taken at 75-100 mg per day. Patients with more severe renal impairment (creatinine clearance< 30 мл в 1 мин на 1,73 м 2) начинают прием Каптоприла-СТИ с 12,5 мг в день (не более). В дальнейшем, при необходимости, через достаточно продолжительный интервал времени, доза может быть повышена, однако при этом она не должна превышать суточную, применяемую для терапии артериальной гипертензии. Дополнительно, если врач посчитает целесообразным, могут назначаться петлевые диуретики, а не диуретики тиазидного ряда.

Side effects

Possible adverse reactions [> 10% – very common; (>1% and< 10%) – часто; (>0.1% and< 1%) – нечасто; (>0.01% and< 0,1%) – редко; < 0,01%, включая отдельные сообщения – очень редко]:

• cardiovascular system: peripheral edema, orthostatic hypotension, decreased blood pressure, tachycardia;
• nervous system: paresthesia, asthenia, feeling of fatigue, headache, dizziness;
• respiratory system: bronchospasm, pulmonary edema, dry cough;
• urinary system: deterioration of kidney function (increased levels of creatinine and urea in the blood), proteinuria;
• water-electrolyte metabolism: acidosis, increased levels of creatinine and urea nitrogen in the blood, proteinuria, hyponatremia (usually observed when following a salt-free diet or during combination therapy with diuretics), hyperkalemia;
• digestive system: hepatitis (signs of hepatocellular damage), hyperbilirubinemia, increased activity of liver transaminases, diarrhea or constipation, dyspepsia, abdominal pain, nausea, stomatitis, dry mouth, impaired taste, decreased appetite; rarely - cholestasis; very rarely - pancreatitis;
• hematopoietic organs: agranulocytosis, thrombocytopenia, anemia, neutropenia;
• allergic reactions: lymphadenopathy, serum sickness, photosensitivity, fever, flushing of the face, angioedema, itching, skin rash (maculopapular, less often bullous or vesicular); rarely - the appearance of antinuclear antibodies in the blood;
• other: general weakness.

Overdose

Main symptoms: thromboembolic complications, pronounced decrease in blood pressure up to collapse, acute cerebrovascular accident, myocardial infarction.

Therapy: the patient is placed in a horizontal position with his legs elevated, measures aimed at restoring blood pressure are applied (increasing the volume of circulating blood, including intravenous administration of saline), and symptomatic treatment is also carried out. Hemodialysis may be prescribed; the use of peritoneal dialysis is not effective.

special instructions

Before starting to take Captopril-STI, as well as regularly during therapy, it is important to monitor kidney function. For CHF, the drug is used under close medical supervision.

In 20% of cases, with long-term treatment with Captopril-STI, there is an increase in serum creatinine and urea, compared with the initial value or norm, by more than 20%. In less than 5% of patients, especially against the background of severe nephropathies, discontinuation of therapy is necessary due to an increase in creatinine levels.

In rare cases, taking pills for arterial hypertension leads to severe arterial hypotension. The likelihood of its development increases with heart failure, salt and fluid deficiency (for example, after intensive diuretic therapy), as well as in patients on dialysis.

The risk of a sharp decrease in blood pressure can be minimized in three ways:

1. Preliminary withdrawal of the diuretic (4–7 days before);
2. Increased intake of sodium chloride (approximately 7 days before starting to take the tablets);
3. Use of the drug in initial doses not exceeding 6.25–12.5 mg per day.

The number of blood leukocytes in the first 3 months of therapy should be monitored monthly, then once every 3 months; for autoimmune pathologies in the first 3 months - every 14 days, then - once every 2 months. If the number of leukocytes< 4000 на 1 мкл назначают общий анализ крови, когда показатель падает ниже 1000 на 1 мкл, терапию отменяют.

Taking ACE inhibitors, including Captopril-STI, in some cases leads to an increase in the concentration of K + in the blood serum. With diabetes mellitus, renal failure, taking potassium-sparing diuretics, medications containing potassium or drugs that increase the concentration of potassium in the blood (for example, heparin), the risk of developing hyperkalemia is increased. In this regard, it is recommended to avoid combined therapy with potassium-sparing diuretics and potassium supplements.

In cases of hemodialysis while taking Captopril-STI, it is important to avoid the use of dialysis membranes with high permeability (for example, AN69), since in such cases the likelihood of developing anaphylactoid reactions increases.

If angioedema occurs, the angiotensin-converting enzyme inhibitor is discontinued, the patient is closely monitored and symptomatic treatment is prescribed.

It should be taken into account that the result of a urine test for acetone while taking captopril may be false positive.

Patients on a low-salt or salt-free diet should take Captopril-STI with caution due to the increased risk of arterial hypotension.

Impact on the ability to drive vehicles and complex mechanisms

Since taking Captopril-STI can lead to the development of dizziness (especially after taking the initial dose), patients are advised to refrain from driving vehicles and performing potentially hazardous activities during the treatment period.

Use during pregnancy and lactation

Captopril-STI is not prescribed during pregnancy/breastfeeding.

Use in childhood

Captopril-STI is not prescribed to patients under 18 years of age.

For impaired renal function

The use of Captopril-STI is contraindicated in patients with severe renal dysfunction, arterial stenosis of a single kidney with progressive azotemia or bilateral renal artery stenosis, as well as in the period after kidney transplantation.

For liver dysfunction

In case of severe liver dysfunction, taking the drug is contraindicated.

Use in old age

Captopril-STI is used in elderly patients under medical supervision.

Drug interactions

Possible interactions of captopril with other substances/drugs:

• digoxin: its concentration in the blood plasma increases by 15–20%;
• propranolol: its bioavailability increases;
• cimetidine: the concentration of captopril in the blood plasma increases by slowing metabolism in the liver;
• non-steroidal anti-inflammatory drugs: the hypotensive effect of the drug is weakened (decreased prostaglandin synthesis and sodium retention);
• ethanol, tricyclic antidepressants, beta-blockers, verapamil, minoxidil (vasodilators), thiazide diuretics: the hypotensive effect of captopril is enhanced;
• lithium preparations: their elimination slows down;
• salt substitutes, potassium supplements, cyclosporine, potassium supplements, potassium-sparing diuretics: the likelihood of hyperkalemia increases;
• flecainide, allopurinol, procainamide: the likelihood of developing an immunosuppressive effect increases;
• probenecid: the excretion of the drug in the urine slows down;
• clonidine: the severity of the hypotensive effect of the drug is reduced;
• cyclophosphamide, azathioprine (immunosuppressants): the risk of hematological disorders increases.

Analogs

Analogues of Captopril-STI are Captopril-FPO, Angiopril-25, Captopril, Blockordil, Captopril Sandoz, Vero-Captopril, Captopril-Ferein, Capoten, Captopril-AKOS, Captopril-UBF, Captopril-Sar, Captopril Welfarm, etc.

Terms and conditions of storage

Store in a place protected from light and moisture, at temperatures up to 25 °C. Keep away from children.

Shelf life – 3 years.