Captopril-AKOS

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Captopril-AKOS: instructions for use and reviews

1. Release form and composition
2. Pharmacological properties
3. Indications for use
4. Contraindications
5. Method of application and dosage
6. Side effects
7. Overdose
8. Special instructions
9. Application during pregnancy and lactation
10. Use in childhood
11. In case of impaired renal function
12. For violations of liver function
13. Use in the elderly
14. Drug interactions
15. Analogs
16. Terms and conditions of storage
17. Terms of dispensing from pharmacies
18. Reviews
19. Price in pharmacies

Latin name: Captopril-AKOS

ATX code: C09AA01

Active ingredient: captopril (Captopril)

Producer: Sintez, JSC (Russia)

Description and photo updated: 30.11.2018

Prices in pharmacies: from 11 rubles.

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Captopril-AKOS is an angiotensin-converting enzyme (ACE) inhibitor, an antihypertensive drug.

Release form and composition

The drug is available in the form of tablets: flat-cylindrical, with a beveled, almost white or white color, have a characteristic odor, slight marbling is allowed, a dividing risk is applied on tablets at a dosage of 50 mg (dosage 25 mg: 10 or 25 pieces in blisters in blisters, in a cardboard box 1, 2, 3 or 4 packages; dosage 50 mg: 10 or 20 pcs. in blisters, in a cardboard box 1, 2, 3, 4 or 5 packs; 10, 20, 30, 40, 50, 60, 80 or 100 pcs. In polymer cans, in a cardboard box 1 can; each pack also contains instructions for the use of Captopril-AKOS).

1 tablet contains:

active substance: captopril (in terms of dry weight) - 25 or 50 mg;
auxiliary components: dosage 25 mg - corn starch, milk sugar, magnesium stearate, talc; dosage of 50 mg - lactose monohydrate (milk sugar), colloidal silicon dioxide (aerosil), microcrystalline cellulose, crospovidone (Kollidon CL-M, Kollidon CL), magnesium stearate, talc.

Pharmacological properties

Pharmacodynamics

Captopril-AKOS is an antihypertensive drug, the mechanism of action of which is due to the properties of the active substance - captopril. Captopril is a first generation ACE inhibitor containing an SH group (sulfhydryl group). By inhibiting ACE, it reduces the conversion of angiotensin I to angiotensin II and eliminates its vasoconstrictor effect on venous and arterial vessels. A decrease in the level of angiotensin II contributes to a secondary increase in the activity of blood plasma renin, causing a direct decrease in the secretion of aldosterone by the adrenal cortex. This leads to a decrease in total peripheral vascular resistance (OPSS) and arterial pressure (BP), resistance in the pulmonary vessels, and a decrease in pre- and afterload on the heart. The minute volume of the heart increases, exercise tolerance.

Under the influence of captopril, arteries are dilated to a greater extent than veins. Also, taking Captopril-AKOS leads to an increase in prostaglandin synthesis and a decrease in the degradation of bradykinin.

The hypotensive effect of captopril does not depend on the blood plasma renin activity. Its effect on the tissue renin-angiotensin-aldosterone system (RAAS) causes a decrease in blood pressure with normal and decreased hormone activity.

Captopril enhances coronary and renal blood flow, improves blood supply to the ischemic myocardium. Its long-term use causes a decrease in the severity of hypertrophy of the myocardium and the walls of resistive arteries, prevents the progression of heart failure, and inhibits the development of left ventricular dilatation.

Taking Captopril-AKOS leads to a decrease in platelet aggregation, in heart failure - to a decrease in the content of sodium ions.

By reducing the tone of the efferent arterioles of the glomeruli of the kidneys, it helps to improve intraglomerular hemodynamics and prevents the appearance of diabetic nephropathy.

At a daily dose of 50 mg, captopril exhibits angioprotective properties against the vessels of the microvasculature. In patients with diabetic nephroangiopathy, it can slow the progression of chronic renal failure.

Unlike direct vasodilators, such as hydralazine and minoxidil, a decrease in blood pressure while taking Captopril-AKOS is not accompanied by reflex tachycardia and helps to reduce myocardial oxygen demand. Adequate doses of captopril in patients with heart failure do not affect blood pressure.

After oral administration, the maximum decrease in blood pressure occurs in 1-1.5 hours. The duration of the antihypertensive effect depends on the dose taken; it reaches optimal values after a few weeks of therapy.

You can not make a sharp cancellation of captopril, this can lead to a significant increase in blood pressure.

Pharmacokinetics

After oral administration, there is a rapid absorption of approximately 75% of the dose of Captopril-AKOS. Simultaneous food intake reduces the absorption of captopril by 30-40%. During the initial passage through the liver, 35–40% of the active substance is biotransformed. The maximum concentration (C _max) in blood plasma is reached within 0.5–1.5 hours and is 114 ng / ml.

Plasma protein binding - 25-30% (mainly with albumin).

It overcomes the blood-brain and placental barriers in a small amount (less than 1%). Up to 0.002% of the dose taken is secreted with breast milk.

Captopril is metabolized in the liver with the formation of pharmacologically inactive metabolites - captopril disulfide dimer and captopril-cysteine sulfide.

The half-life (T _1/2) of captopril is approximately 2–3 hours. About 95% of the dose taken is excreted through the kidneys during the first 24 hours (including 40-50% unchanged).

In chronic renal failure, the drug cumulates, T _1/2 can be from 3.5 to 32 hours. Patients with impaired renal function should reduce a single dose and / or increase the interval between taking Captopril-AKOS.

Indications for use

arterial hypertension (including renovascular hypertension);
chronic heart failure - as part of complex therapy;
impaired left ventricular function after myocardial infarction in clinically stable patients;
diabetic nephropathy in type 1 diabetes mellitus (albuminuria more than 30 mg / day).

Contraindications

Absolute:

severe renal dysfunction, bilateral renal artery stenosis, stenosis of a single kidney with progressive azotemia, refractory hyperkalemia, primary hyperaldosteronism, condition after kidney transplantation;
severe liver dysfunction;
simultaneous use of aliskiren and aliskiren-containing agents in patients with type 2 diabetes mellitus or patients with impaired renal function with creatinine clearance (CC) less than 60 ml / min;
lactose intolerance, glucose-galactose malabsorption syndrome or lactase deficiency;
period of pregnancy;
breast-feeding;
age up to 18 years;
hereditary and / or idiopathic angioedema in the presence of previous therapy with ACE inhibitors (including history);
hypersensitivity to other ACE inhibitors, including history;
individual intolerance to the components of the drug.

With caution, Captopril-AKOS tablets should be prescribed for hypertrophic obstructive cardiomyopathy, ischemic heart disease, mitral stenosis, aortic stenosis, and similar changes that impede the outflow of blood from the left ventricle of the heart; with renovascular hypertension, chronic renal failure, systemic lupus erythematosus, scleroderma or other connective tissue diseases; in case of inhibition of bone marrow hematopoiesis, cerebrovascular pathologies, diabetes mellitus, hyperkalemia, liver dysfunction, adherence to a diet with limited salt, hemodialysis, diarrhea, vomiting or other conditions that cause a decrease in the volume of circulating blood; during surgery or general anesthesia,conducting hemodialysis using high-flow membranes (including polyacrylonitrile high-flow membranes AN69), concomitant desensitizing therapy, apheresis of low density lipoproteins (LDL); in combination with potassium-sparing diuretics, potassium preparations, potassium-containing salt substitutes, lithium preparations; patients of the black race, in old age.

Captopril-AKOS, instructions for use: method and dosage

Captopril-AKOS tablets are taken orally 1 hour before meals.

The dose selection is made individually.

To select a dose at the initial stage of therapy, it is necessary to use captopril tablets from other manufacturers, 12.5 mg with a dividing line or 25 mg with a cruciform line.

Recommended dosage:

arterial hypertension: initial dose - 12.5 mg 2 times a day. During the first hour after taking the first dose, careful monitoring of the patient's condition is necessary for the tolerance of Captopril-AKOS. With the development of arterial hypotension, the patient should take a horizontal position with raised legs. This reaction to the first dose is not a reason to discontinue therapy. In the absence of a sufficient clinical effect, the dose is gradually increased, observing the interval of 14-28 days, until the optimal effect is achieved. The maintenance dose for mild to moderate arterial hypertension is usually 25 mg 2 times a day, the maximum daily dose is 100 mg (50 mg 2 times a day). The maximum daily dose for severe arterial hypertension is 150 mg (50 mg 3 times a day);
chronic heart failure (as part of combination therapy with diuretics and / or cardiac glycosides; before the appointment of captopril, the diuretic intake is canceled or its dose is reduced to avoid an excessive decrease in blood pressure): the initial dose is 6.25 mg 3 times a day. If necessary, to achieve the desired effect, the dose is increased gradually, observing an interval of at least 14 days. The maintenance dose is usually 25 mg 2-3 times a day, the maximum daily dose is 150 mg (50 mg 3 times a day). To achieve a stable effect of Captopril-AKOS in the event of symptomatic arterial hypotension, the dose of simultaneously prescribed diuretics and / or other vasodilators can be reduced;
dysfunction of the left ventricle after myocardial infarction: if the patient is clinically stable, the drug can be taken 3 days after myocardial infarction. The initial dose is 6.25 mg once a day. If necessary, the daily dose is gradually increased, taking into account the tolerance of Captopril-AKOS, up to 75 mg, dividing it into 2-3 doses. The maximum daily dose is 150 mg (50 mg 3 times a day). With the development of arterial hypotension, the dose can be reduced, but with subsequent attempts to use 150 mg of captopril per day, the tolerance of the drug should be taken into account;
diabetic nephropathy: 75-100 mg per day, divided into 2-3 doses. The dose of Captopril-AKOS for insulin-dependent diabetes (type 1) with microalbuminuria (release of albumin 30-300 mg per day) should be 50 mg 2 times a day, with a total protein clearance of more than 500 mg per day - 25 mg 3 times a day …

With a moderate degree of renal dysfunction (CC 30 ml / min and above), Captopril-AKOS can be prescribed in a daily dose of 75-100 mg.

In case of severe renal dysfunction (CC less than 30 ml / min), the initial daily dose should not exceed 12.5 mg. If necessary, the dose can be gradually increased, observing sufficiently long time intervals, but the maintenance dose should be less than the usual dose used to treat hypertension.

Perhaps the additional appointment of "loop" diuretics, but not thiazide diuretics.

Correction of the dosage regimen in case of impaired renal function should be carried out taking into account the patient's CC indicator in the following accordance:

CC 40 ml / min: initial daily dose - 25-50 mg, maximum daily dose - 150 mg;
CC 21-40 ml / min: initial daily dose - 25 mg, maximum daily dose - 100 mg;
CC 10–20 ml / min: initial daily dose - 12.5 mg, maximum daily dose - 75 mg;
CC less than 10 ml / min: the initial daily dose is 6.25 mg, the maximum daily dose is 37.5 mg.

The initial dose for elderly patients is 6.25 mg 2 times a day. This dosing regimen prevents renal dysfunction, therefore it is considered optimal for a maintenance dose. It is recommended to adjust the dose of Captopril-AKOS taking into account the patient's therapeutic response regularly, keeping it at the lowest effective level.

Side effects

Undesirable disorders from systems and organs (according to the frequency of their development are classified as follows: very often - ≥ 1/10, often - ≥ 1/100 and <1/10, infrequently - ≥ 1/1000 and <1/100, rarely - ≥ 1/10 000 and <1/1000, very rarely - <1/10 000, the frequency has not been established - it is not possible to determine the frequency from the available data):

from the respiratory system: often - cough (dry, unproductive), shortness of breath; very rarely - rhinitis, bronchospasm, eosinophilic pneumonia, allergic alveolitis, pulmonary edema;
from the central nervous system: often - sleep disturbances, taste disturbances, drowsiness, dizziness; rarely - paresthesia, headache, asthenia; very rarely - cerebrovascular disorders (including fainting, impaired consciousness, stroke), depression;
on the part of the cardiovascular system: infrequently - flushing of the face, orthostatic hypotension, palpitations, tachycardia (tachyarrhythmia), angina pectoris, pallor, peripheral edema, Raynaud's syndrome; very rarely - cardiac arrest, cardiogenic shock;
from the genitourinary system: rarely - an increase in the frequency of urination, impaired renal function, polyuria, oliguria, acute renal failure; very rarely - sexual dysfunction, gynecomastia, nephrotic syndrome;
from the side of metabolism: rarely - anorexia; very rarely - hypoglycemia, hyperkalemia;
on the part of the musculoskeletal system: very rarely - arthralgia, myalgia;
from the digestive system: often - dryness of the oral mucosa, abdominal pain, nausea, vomiting, constipation, diarrhea; rarely - stomatitis, aphthous ulcers on the surface of the tongue and the mucous membrane of the cheeks, gingival hyperplasia; very rarely - pancreatitis, glossitis, peptic ulcer, angioedema of the intestinal mucosa, abnormal liver function, jaundice, hepatitis (including hepatonecrosis), cholestasis, increased serum bilirubin levels, increased activity of "hepatic" transaminases;
on the part of the hematopoietic organs: very rarely - thrombocytopenia, pancytopenia, neutropenia, agranulocytosis, anemia (including aplastic and hemolytic anemia), lymphadenopathy, increased titer for antinuclear antibodies and / or autoimmune diseases, eosinophilia;
dermatological reactions: often - itching with and without rashes, maculopapular skin rash, baldness; rarely - a skin rash of a bullous or vesicular nature; very rarely - exfoliative dermatitis, urticaria, erythema multiforme, photosensitivity, pemphigoid reactions, erythroderma, Stevens-Johnson syndrome;
from the senses: very rarely - impaired visual acuity;
laboratory indicators: very rarely - hyperkalemia, proteinuria, eosinophilia, an increase in the concentration of urea nitrogen and creatinine in the blood plasma, hyponatremia, hypoglycemia, acidosis, a decrease in the level of hemoglobin and hematocrit, a decrease in the number of leukocytes, platelets, an increase in the erythrocyte sedimentation rate;
others: infrequently - weakness, fatigue, chest pain; very rarely - fever; frequency not established - a complex of symptoms, including nausea, vomiting, flushing of the skin of the face and lowering blood pressure.

Overdose

Symptoms: a pronounced decrease in blood pressure (including shock, stupor, collapse), acute renal failure, disturbances in water and electrolyte balance, bradycardia, myocardial infarction, thromboembolic complications, acute cerebrovascular accident.

Treatment: during the first 0.5 hours after taking Captopril-AKOS - gastric lavage or artificial vomiting, administration of sodium sulfate and adsorbents. It is necessary to give the patient's body a horizontal position, raising his legs, and take immediate measures to restore blood pressure, replenish the circulating blood volume, including intravenous (IV) administration of 0.9% sodium chloride solution. If necessary, appoint subcutaneous or intravenous administration of epinephrine (adrenaline), antihistamines, intravenous administration of hydrocortisone. For severe vagal reactions or bradycardia, atropine is recommended. Hemodialysis is shown.

It should be borne in mind that peritoneal hemodialysis is ineffective in this case.

special instructions

When prescribing Captopril-AKOS, one should take into account the blood pressure and the state of the patient's renal function and regularly monitor their indicators during the use of the drug. Patients with chronic heart failure should be treated under close medical supervision.

Severe arterial hypotension on the background of the use of the drug in patients with arterial hypertension occurs in rare cases. To reduce the risk of a sharp drop in blood pressure, it is recommended to start taking with low (6.25–12.5 mg) doses of Captopril-AKOS. Diuretics should be discontinued 4-7 days before taking the first dose of captopril, if necessary, replenish the circulating blood volume.

It should be borne in mind that severe hypotension in violation of cerebral circulation and cardiovascular diseases increases the risk of developing myocardial infarction or stroke.

With the suppression of bone marrow hematopoiesis, taking captopril increases the risk of neutropenia and agranulocytosis.

The use of Captopril-AKOS should be accompanied by regular monitoring of the number of leukocytes in the blood, which is carried out once every 30 days during the first 90 days of therapy, then once every 90 days. This is due to the fact that while taking ACE inhibitors, anemia, thrombocytopenia, neutropenia, or agranulocytosis may occur.

Taking ACE inhibitors in patients with bilateral stenosis of the arteries of a single kidney significantly increases the risk of arterial hypertension and renal failure. In such patients, even a moderate change in serum creatinine concentration can cause functional impairment of the kidneys, therefore, treatment should be started with low doses and under close medical supervision, monitoring renal function.

If patients have kidney disease, the protein content in urine should be determined before starting and regularly throughout the entire course of therapy.

The use of Captopril-AKOS increases the risk of an increase in serum potassium and the development of hyperkalemia in patients with renal insufficiency, diabetes mellitus, as well as in patients simultaneously taking potassium preparations, potassium-sparing diuretics and other drugs that cause an increase in the blood potassium content. The risk of hypotension and hyperkalemia increases with a low-salt or salt-free diet.

With concomitant immunosuppressive therapy with allopurinol or procainamide in patients with connective tissue diseases, especially with impaired renal function, a blood test should be performed every 14 days during the first 90 days, then once every 60 days. If the leukocyte count is below 4 x 10 ⁹ per 1 liter, a general blood test is performed, below 1 x 10 ⁹ per 1 liter - the drug is canceled. In case of signs of infectious diseases, including a sore throat or fever, a clinical blood test with a leukocyte count is required.

It should be borne in mind that taking Captopril-AKOS against the background of desensitizing therapy with Hymenoptera venom and similar agents increases the risk of developing anaphylactoid reactions.

In case of an increase in the activity of hepatic transaminases or the appearance of symptoms of jaundice, treatment with captopril should be immediately canceled.

In blacks, ACE inhibitors, including Captopril-AKOS, exhibit a less pronounced antihypertensive effect.

Performing a urine acetone test in patients taking the drug may give a false positive result.

Influence on the ability to drive vehicles and complex mechanisms

During the period of treatment with captopril, it is necessary to avoid performing potentially hazardous activities, including driving vehicles, especially after taking the initial dose of Captopril-AKOS.

Application during pregnancy and lactation

The use of Captopril-AKOS during gestation and breastfeeding is contraindicated.

Women of childbearing age planning pregnancy should avoid the use of ACE inhibitors (including captopril). They should be advised of alternative antihypertensive therapy.

If conception occurred during the period of taking Captopril-AKOS, its immediate cancellation and regular monitoring of fetal development are required. The use of captopril in the first trimester of pregnancy potentially increases the risk of developing birth defects in the fetus. Long-term use of the drug in the II and III trimesters is toxic to the fetus and leads to a delay in ossification of the skull bones, decreased renal function, oligohydramnios [it is recommended to assess the state of the skull bones and fetal kidney function by ultrasound examination (US)].

In newborns whose mothers have been taking captopril for a long time in the II and III trimesters of pregnancy, the development of neonatal renal failure, hyperkalemia, hypotension is possible.

Pediatric use

The use of Captopril-AKOS in patients under the age of 18 is contraindicated due to the lack of information on the effectiveness and safety of therapy.

With impaired renal function

The use of Captopril-AKOS for the treatment of patients with severe renal impairment such as bilateral renal artery stenosis, stenosis of a single kidney with progressive azotemia, refractory hyperkalemia, primary hyperaldosteronism, condition after kidney transplantation is contraindicated.

Care should be taken to prescribe captopril to patients with chronic renal failure.

With a moderate degree of renal dysfunction (CC 30 ml / min and above), Captopril-AKOS can be prescribed in a daily dose of 75-100 mg.

Perhaps the additional appointment of "loop" diuretics, but not thiazide diuretics.

Correction of the dosage regimen in case of impaired renal function should be carried out taking into account the patient's CC indicator in the following accordance:

CC 40 ml / min: initial daily dose - 25-50 mg, maximum daily dose - 150 mg;
CC 21-40 ml / min: initial daily dose - 25 mg, maximum daily dose - 100 mg;
CC 10–20 ml / min: initial daily dose - 12.5 mg, maximum daily dose - 75 mg;
CC less than 10 ml / min: the initial daily dose is 6.25 mg, the maximum daily dose is 37.5 mg.

For violations of liver function

The use of Captopril-AKOS is contraindicated in severe liver dysfunction.

The drug should be prescribed with caution to patients with impaired liver function.

Use in the elderly

With caution, Captopril-AKOS should be prescribed to elderly patients.

Drug interactions

angiotensin II receptor antagonists (ARA II), aliskiren and other drugs that affect the RAAS: increase the risk of a pronounced decrease in blood pressure, impaired renal function (including acute renal failure), hyperkalemia. In this regard, if it is necessary to prescribe other drugs that affect the RAAS, blood pressure, renal function indicators, and the content of blood plasma electrolytes should be carefully monitored. In case of severe renal impairment and type 2 diabetes mellitus, the combination with aliskiren should be avoided;
potassium-sparing diuretics (amiloride, triamterene, spironolactone, eplerenone), potassium supplements, potassium supplements, salt substitutes: increase the risk of hyperkalemia; it is necessary to control the plasma potassium content;
diuretics (thiazide and "loop"): high doses increase the likelihood of arterial hypotension;
diuretics, muscle relaxants, aldesleukin, alprostadil, cardiotonics, alpha ₁ -adrenergic blockers, beta-blockers, central alpha ₂ -adrenomimetics, slow calcium channel blockers, nitrates, minoxidil, vasodilators: potentiate the hypotensive effect of Captopril-AKOS;
hypnotics, antipsychotics, anxiolytics, antidepressants: enhance the antihypertensive effect of captopril;
nonsteroidal anti-inflammatory drugs (NSAIDs), including indomethacin, selective inhibitors of cyclooxygenase-2, estrogens: with prolonged use, they reduce the effectiveness of captopril. In addition, the combination of NSAIDs and ACE inhibitors may have an additive effect on an increase in serum potassium concentration against the background of a simultaneous decrease in renal function (including acute renal failure), especially in patients with a history of renal impairment, elderly patients, or with a reduced volume of circulating blood;
means of general anesthesia: a pronounced decrease in blood pressure is possible during major operations, especially if the means of general anesthesia have an antihypertensive effect;
lithium preparations: lithium excretion slows down and its concentration in the blood increases;
allopurinol, procainamide: the risk of developing neutropenia and / or Stevens-Johnson syndrome increases;
glucocorticosteroids, epoetin, estrogens and combined oral contraceptives, naloxone, carbenoxolone: weaken the action of Captopril-AKOS;
gold preparations: intravenous administration of sodium aurothiomalate can cause a complex of symptoms in the patient, including a decrease in blood pressure, hyperemia of the facial skin, nausea, vomiting;
sympathomimetics: may reduce the clinical effect of captopril;
oral hypoglycemic agents, insulin: increase the risk of hypoglycemia;
antacids: slow down the absorption of captopril in the gastrointestinal tract;
ethanol: enhances the hypotensive effect of Captopril-AKOS;
probenecid: helps to reduce the renal clearance of captopril, which leads to an increase in its concentration in the blood serum;
azathioprine, cyclophosphamide: increase the likelihood of developing hematological disorders;
propranolol: its bioavailability is increased;
cimetidine: helps to increase the concentration of the active substance in the blood plasma;
clonidine: reduces the severity of the antihypertensive effect.

Analogs

The analogues of Captopril-AKOS are: Captopril, Captopril-Ferein, Captopril-FPO, Captopril-UBF, Captopril Velpharm, Capoten, Katopil, Epsitron, Alkadil, Angiopril-25, Blockordil, Vero-Captopril, Captopril-STI and others.

Terms and conditions of storage

Keep out of the reach of children.

Store at temperatures up to 25 ° C in a dark place.

The shelf life is 5 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews of Captopril-AKOS

Reviews of Captopril-AKOS are positive. Patients note the high efficiency and fast action of the drug. The advantages include low cost.

Price for Captopril-AKOS in pharmacies

The price of Captopril-AKOS for a package containing 20 tablets at a dose of 25 mg can be from 11 rubles, 40 tablets at a dose of 25 mg - from 17 rubles.

Captopril-AKOS: prices in online pharmacies

Drug name

Price

Pharmacy

Captopril-AKOS 25 mg tablets 20 pcs.

RUB 11

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Captopril-AKOS 25 mg tablets 40 pcs.

RUB 18

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Captopril-AKOS 50 mg tablets 20 pcs.

32 RUB

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Captopril-AKOS 50mg tablets 20 pcs.

RUB 40

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Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!