*Capoten*

pharmachologic effect

ACE inhibitor. Reduces the formation of angiotensin II from angiotensin I. A decrease in the content of angiotensin II leads to a direct decrease in the release of aldosterone. At the same time, OPSS, blood pressure, post- and preload on the heart are reduced. Expands arteries more than veins. It causes a decrease in the degradation of bradykinin (one of the effects of ACE) and an increase in the synthesis of Pg. The hypotensive effect does not depend on the activity of plasma renin, a decrease in blood pressure is noted at normal and even reduced concentrations of the hormone, which is due to the effect on the tissue renin-angiotensin systems. Enhances coronary and renal blood flow. With prolonged use, it reduces the severity of myocardial hypertrophy and the walls of the arteries of the resistive type. Improves blood supply to ischemic myocardium. Reduces platelet aggregation. Helps to reduce the content of Na + in patients with CHF. In doses of 50 mg / day, it exhibits angioprotective properties in relation to the vessels of the microvasculature and can slow down the progression of chronic renal failure in diabetic nephroangiopathy. A decrease in blood pressure, unlike direct vasodilators (hydralazine, minoxidil, etc.), is not accompanied by reflex tachycardia and leads to a decrease in myocardial oxygen demand. With HF in an adequate dose does not affect the magnitude of blood pressure. Maximum reduction Blood pressure after oral administration is observed after 60-90 minutes. The duration of the hypotensive effect is dose-dependent and reaches optimal values ​​within a few weeks.

Indications for use

For mild/moderate hypertension, as additional funds in the treatment of thiazide diuretics in patients who do not respond effectively enough to treatment with thiazide drugs alone. Severe hypertension when standard treatment fails.

Capoten is indicated for the treatment of congestive heart failure. The drug should be used together with diuretics and, where necessary, digitalis preparations.

Mode of application

Hypertension

Treatment with Kapoten should be carried out using the smallest effective dose, which should be selected in accordance with the needs of the patient.

Mild/Moderate hypertension

With mild / moderate degree hypertension Kapoten should be used as an adjunct to thiazide diuretic treatment. The initial dose is 12.5 mg twice a day. The usual maintenance dose is 25 mg twice daily, which can be increased in steps over 2-4 weeks until the desired response to treatment is obtained, up to a maximum dose of 50 mg twice daily.

severe hypertension

In severe hypertension, the initial dose is 12.5 mg twice daily. The dose can be increased in stages up to a maximum dose of 50 mg three times a day. Kapoten can be used together with other antihypertensive drugs, however, the dose of such drugs should be selected individually. Usually, you should not exceed the daily dose of Kapoten, equal to 150 mg / day.

Heart failure

Treatment with Capoten should be started under close medical supervision. Capoten should be given when treatment with a diuretic (such as furosemide 40-80 mg or equivalent) fails to relieve symptoms. An initial dose of 6.25 mg or 12.5 mg may minimize the transient pressure drop. The possibility of such an effect can be reduced by canceling or reducing the dose of the diuretic, if possible, before starting treatment with Capoten. The usual maintenance dose is 25 mg two or three times a day, and the dose can be increased in stages, once every two weeks at least, until a satisfactory response is obtained. The usual maximum daily dose is 150 mg. Capoten should be administered in combination with a diuretic and, when necessary, with digitalis.

elderly patients

The dose should be adjusted depending on the change blood pressure and maintained at the minimum level necessary to achieve a sufficient result. Since in elderly patients the function of the kidneys may be limited, and dysfunctions of other organs may also be noted, it is necessary to use a small dose of Kapoten at the beginning of treatment.

Capoten is not recommended for the treatment of mild/moderate hypertension in children. Existing experience with neonates, especially preterm infants; is limited. Since renal function in neonates is not equivalent to that in older children or adults, Capoten should be used when patients are under medical supervision. The initial dose should be 0.3 mg per kg of body weight per day up to a maximum dose of 6 mg/kg of body weight per day in divided doses. The dose should be selected individually, depending on the patient's response to treatment and distributed over 2-3 doses throughout the day.

Patients with impaired renal function

Kapoten is not recommended for use in patients with impaired renal function. When its use is clinically indicated in patients with severe hypertension in the presence of impaired renal function, the dose should possibly be lower to ensure adequate control of blood pressure. The dose can be adjusted to the response of the patient, but sufficient time must elapse between dose changes. In such patients, the loop diuretic is the drug of choice, not the thiazide-type diuretic.

Kapoten is easily excreted from the body by hemodialysis.

Side effects

Neutropenia, anemia, thrombocytopenia.

proteinuria, increased content blood urea, as well as creatinine, increased serum potassium and acidosis.

The cardiovascular system

Hypotension, tachycardia.

Availability side effects on captopril is mainly associated with renal function, since the drug is excreted from the body mainly through the kidneys. The dose should not exceed the value necessary to achieve an adequate result, and it should be reduced in patients with impaired renal function.

Eruptions, usually with itching. As a rule, they are mild, temporary, macular-papular in nature. V rare cases- the nature of the urticaria. In some cases, rashes are associated with fever, and some patients developed angioedema. Itching, flushing, vesicular rash and photosensitivity have been reported.

Gastrointestinal tract

Reversible and usually self-limiting taste disturbance has been reported. Due to loss of taste, weight loss may occur. Aphthous ulcer-like stomatitis has been reported. In some patients, an increase in the activity of liver enzymes has been reported. In rare cases, hepatocellular damage and cholestatic jaundice have been reported. Stomach irritation and abdominal pain may occur.

Hand paresthesias, serum sickness, cough, bronchospasm, and lymphadenopathy have been reported.

Contraindications

History of hypersensitivity to captopril.

Precautionary measures

Patient evaluation should include assessment of renal function prior to initiation of treatment and at appropriate intervals thereafter. Patients with impaired renal function should not usually be treated with captopril. Kapoten should not be used in patients with aortic stenosis or obstructive defects in the outflow tract of blood from the heart.

hypotension

After the first doses of the drug, some patients may experience symptomatic hypotension. In most cases, the symptoms are relieved simply by moving the patient to the supine position. In patients with severe forms of renin-dependent hypertension (for example, renovascular hypertension) or in the presence of severe congestive heart failure receiving large doses diuretic, excessive hypotensive reactions were usually noted within one hour after taking the initial dose of Kapoten. In such patients, discontinuation of diuretic treatment or a marked decrease in the diuretic dose for 4-7 days before starting treatment with Capoten reduces the likelihood of such an effect. If you start treatment with Kapoten with small doses (6.25 mg or 12.5 mg), the duration of the possible hypotensive effect is reduced. In some patients, saline infusion may be beneficial. The development of hypotension after taking the first dose does not remove the need for subsequent dose selection of Kapoten.

Effects on the kidneys

Proteinuria in patients with pre-existing normal function kidneys are rare. When proteinuria is present, it is usually seen in patients with severe hypertension and indications of pre-existing kidney disease. Some of these patients have nephrotic syndrome. In patients with indications of pre-existing kidney disease during the first nine months of treatment, it is recommended to determine the protein in the urine monthly.

Neutropenia/agranulocytosis, thrombocytopenia and anemia have been reported in patients receiving Kapoten. In patients with normal renal function in the absence of other complicating factors, neutropenia is observed in rare cases.

Capoten should not be routinely used in patients with pre-existing impaired renal function, vascular collagenoses, patients treated with immunosuppressive drugs, allopurinol or procainamide, or a combination of these complicating factors, since neutropenia is almost exclusively associated with patients in this group . Some of these patients may develop serious infections, which in some cases do not respond to intensive antibiotic treatment. If Kapoten is used in such patients, it is recommended to count before starting treatment. shaped elements white blood, including the determination of the differential blood count every two weeks during the first three months of treatment with Kapoten and periodically thereafter. During treatment, all patients should be instructed to report any sign of infection, such as sore throat, temperature increase when a differential count of white blood elements is carried out. Capoten and other prescribed drugs should be discontinued if neutropenia (neutrophils less than 1000/mm3) is noted or suspected. In most patients, the number of neutrophils quickly returns to normal after discontinuation of Kapoten.

Surgery/Anesthesiology

In patients undergoing major surgical operations or, under anesthesia with drugs that cause hypotension, captopril will block the formation of angiotenside II caused by compensatory renin secretion. This can lead to hypotension, which can be corrected by volume replacement.

Clinical Chemistry

Kapoten can give false positive test in urine for acetone.

Pregnancy

Capoten has been shown to have a lethal effect on rabbit and sheep fetuses. No toxic effect on the fetus in hamsters and rats was found.

Capoten is contraindicated for use during pregnancy and should not be used in women of childbearing age unless they are protected by effective contraception.

Because captopril is secreted into women's milk, Kapoten should not be used in breastfeeding women.

Interaction with other drugs

Diuretics potentiate the antihypertensive effect of Kapoten. Potassium-sparing diuretics (triamterene, amiloride, and spironolactone) or potassium supplements can lead to a marked increase in serum potassium concentration.

When taken simultaneously with indomethacin, there may be a decrease in the antihypertensive effect. This is probably also noted with the use of other non-steroidal anti-inflammatory drugs.

Capoten has been reported to be synergistic with peripheral vasodilators such as minoxidil. Knowledge of this interaction may help avoid initial hypotensive reactions.

It is assumed that the antihypertensive effect of Kapoten may be slowed down when patients receiving clonidine are transferred to Kapoten.

Neutropenia and/or Stevens-Johnson syndrome have been reported in patients treated with Capoten in combination with allopurinol or procainamide. Although a causal relationship has not been identified, these combinations should be used with caution, especially in patients with impaired renal function.

The use of azathioprine and cyclophosphamide has been associated with blood dyscrasias in patients with kidney failure who simultaneously took Kapoten.

Excretion of Kapoten through the kidneys is reduced in the presence of probenecid.

Overdose

In case of overdose, blood pressure should be monitored and, if hypotension develops, volume replacement is the treatment of choice. Captopril is removed from the body by dialysis.

Release form

Blister packs containing 40 tablets of 25 mg each.

Blister packs containing 40 tablets of 50 mg each.

Storage conditions

Store at room temperature.

Release from pharmacies by prescription.

Synonyms

Captopril (Captopril)

Compound

1-[(2S)-3-mercapto-2-methyl-propionyl]-L-proline.

Attention

Before using the drug Kapoten you should consult your doctor. This instruction provided in free translation and is intended for informational purposes only. For more complete information please refer to the manufacturer's instructions.

Or an angiotensin converting enzyme. Its main action is to lower blood pressure. The drug is also often used along with other drugs in the treatment of heart failure in chronic form. We will consider reviews about Kapoten in this article.

Compound

The only form in which the drug is produced is tablets for oral administration. The active substance is captopril. The drug is available in two dosages, 25 and 50 mg each. active ingredient in one tablet. excipients"Capotena" perform:

1. Lactose.
2. Corn starch.
3. Stearic acid.
4. Cellulose in the form of microcrystals.

Indications

The drug is prescribed to patients with the following pathologies:

1. Arterial hypertension various genesis, including the kidney.
2. Heart failure in a chronic form.
3. A heart attack, the consequence of which was a violation of the functioning of the left ventricle of the heart muscle.
4. Nephropathy, which developed against the background of type 1 diabetes mellitus.

Application

The medication is taken orally. The tablet can be divided into parts depending on the required dose. Do not chew, bite or crush the tablet. Required dosage calculated on an individual basis. Reception begins with the smallest dose - 6.25 mg with a gradual increase to the amount that has the maximum effect. therapeutic effect. The largest allowable daily dosage- 600 mg. The optimal dosage for most patients is 300 mg. Reviews about Kapoten are plentiful.

Contraindications

"Capoten" is a rather potent drug and has a number of absolute contraindications, which include:

Relative contraindications

It is relatively contraindicated to take the remedy under the following conditions:

Side effects

"Capoten" can cause adverse reactions from almost all organs and systems of the human body:

1. Nervous system: dizziness, drowsiness, fatigue, headaches, fainting, confusion, depression, impaired coordination, convulsions, numbness of the limbs, impaired sense of smell and vision.
2. Circulatory system: hypotension, myocardial infarction, angina pectoris, arrhythmia, palpitations, pallor skin, anemia, thromboembolism pulmonary artery, hot flashes, neutropenia, peripheral edema, eosinophilia, thrombocytopenia, agranulocytosis.
3. Respiratory system: bronchospasm, pneumonitis, bronchitis, shortness of breath, unproductive cough, rhinitis.
4. Gastrointestinal tract: stomatitis, glossitis, xerostomia, anorexia, gingival hyperplasia, vomiting, nausea, oral ulcers, dyspepsia, diarrhea, constipation, cholestasis, pancreatitis, hepatocellular type cirrhosis, cholestatic hepatitis. This confirms the "Kapoten" instructions for use and reviews.
5. Reproductive system: polyuria, proteinuria, oliguria, decreased erectile function, impotence, deterioration of kidney function.
6. Skin: rashes, redness, itching, herpes zoster, photodermatitis, erythroderma, toxic epidermal necrolysis, exfoliative dermatitis.
7. Allergies: Quincke's edema, urticaria, anaphylactic shock, Stevens-Johnson syndrome.
8. Composition of the blood: an increase in the level of potassium and sodium in the blood, as well as a decrease in glucose levels. The activity of liver enzymes, the concentration of urea, bilirubin and creatinine increases. There is a decrease in hematocrit and hemoglobin.
9. Joints and muscles: arthralgia, myalgia, chills.

All this is indicated in the instructions. Reviews, the price of "Capoten" will be considered below.

Interaction with other drugs

The possibility of developing leukopenia increases with the simultaneous administration of Kapoten with interferon alfa-2, cytostatics, immunosuppressants and procainamide.

Hyperkalemia can be triggered by the simultaneous administration of the drug with potassium-sparing, diuretic drugs. The same applies to heparin and potassium-containing salt substitutes.

When taken simultaneously with drugs such as Nimesil, Ibuprofen, etc., there may be a violation of the kidneys. Cyclosporine can cause kidney failure. "Capoten" at joint admission with diuretics and anesthetics can provoke hypotension, as they dramatically reduce blood circulation. All this is described in detail in the instructions for use. The price of "Capoten", according to reviews, is slightly overpriced.

Azathioprine can cause leukopenia and anemia. The effectiveness of Kapoten is significantly reduced when taken with magnesium, aluminum and magnesium carbonate hydroxides. The same effect is exerted by erythropoietins and Orlistat. The latter can cause a hypertensive crisis and even cerebral hemorrhage.

Price

The drug costs about 140-150 rubles. It depends on the region and pharmacy chain. If you wish, you can find similar drugs, but they will cost several times cheaper.

Analogues

Below are analogues that are cheaper in price:

hypertension in modern world is not a rare disease. As statistics show, every third inhabitant of the planet has problems with blood pressure with age. When making a diagnosis, it is important to start treatment on time, since the disease often leads to severe complications.

For conservative therapy prescribe drugs that normalize blood pressure. In this respect, it has performed well. medicinal product Kapoten. It is a pronounced ACE inhibitor with a rapid hypotensive effect.

The hood is called ambulance, as it can quickly bring down blood pressure with a sharp increase in it.

Many studies have already been carried out on this drug, which confirmed its positive result in the treatment of hypertension.

The composition of the drug

The package contains white tablets (sometimes they can have a creamy tint) with a specific smell.

The composition of one tablet (25 mg) includes captopril as the main active ingredient. Thanks to him, the effect of the drug comes in about 15 minutes after taking it and the effect lasts up to 7-8 hours.

Of the auxiliary ingredients: starch, cellulose, octadecanoic acid, lactose.

How does it affect pressure

At high pressure Vessels begin to narrow, which is why blood cannot circulate normally. Capoten tablets dilate blood vessels up to normal level, which leads to a decrease in blood pressure and an improvement in well-being.

Also, the advantage of the drug is its instant absorption into the blood. At least 70 percent of the main substance is absorbed and subsequently excreted in the urine.

Capoten usually begins to act a few minutes after ingestion.

The maximum effect of its action can be felt after 60-80 minutes. It is not recommended to drink tablets after meals, as in this case the effect of the drug is dulled.

Who is prescribed the medicine

1. BP indicators are periodically or regularly overestimated;
2. In the presence of heart failure. If such a disease occurs in a chronic form, then the drug can be taken only as aid to improve well-being;
3. Previously had a myocardial infarction;
4. With the development diabetic nephropathy in combination with diabetes.

After long-term use the drug should be periodically boiled kidney function.

At what pressure do you take

Given the vasodilating and hypotensive effect of the drug, it can be used for any hypertension.

With the help of Kapoten, you can normalize the pressure in emergency situations when other medicines are not available. Also, the drug is suitable for use after suffering a hypertensive crisis or other similar complications.

How to take with high blood pressure

So if blood pressure began to rise, it is enough to chew one tablet in the mouth with a dose of 25 mg. Within an hour after taking it, it will drop to twenty percent.

If the indicators remain too high, then after an hour you can take another tablet in this way. In this case, the indicators stabilize to a normal level without taking additional drugs and without calling an ambulance.

Reception at high pressure and crisis

Kapoten can also be used for hypertensive crisis. To do this, put 2 tablets (25 mg each) under the tongue at once and completely dissolve them. The pressure will begin to gradually decrease after ten minutes. It is undesirable to take higher doses without consulting a doctor.

The doctor should calculate the required dosage, taking into account the characteristics of the course of the disease, the usual blood pressure indicators and the body's response to the drug.

Instructions for use for hypertension

It is worth noting that correct reception medication should be before meals. Better in 1 - 1.5 hours, in the amounts that the doctor has established.

If hypertension is diagnosed initial stage, then the drug is enough to take orally one tablet twice a day. If the disease progresses, then it is worth taking two tablets at a time, twice a day.

Download complete instructions on the use of the drug

When arterial hypertension is running form, then you need to start taking half a tablet twice a day and gradually increase the dosage to two tablets three times a day.

Is it possible to drink during pregnancy

Kapoten reduces blood pressure well, but can it be taken during pregnancy? Such tests were simply not carried out. Many doctors point out that in the event of a sudden hypertensive crisis, when other drugs are not at hand, you can drink the minimum dose - half a tablet.

But for course therapy before and after childbirth, it is prohibited. Not recommended as a medicine and in the first months of pregnancy.

Before you decide to take the medicine yourself, you should consult with your doctor and get his approval.

How quickly and for how long does the drug work?

The initial effect is noted already fifteen minutes after taking the drug inside.

The maximum effect occurs in an hour or an hour and a half.

The effect of the drug usually lasts up to 7-8 hours.

• If there is intolerance to its components;
• During pregnancy and lactation;
• Children under the age of majority;
• After operations performed on the kidneys;
• With reduced pressure (hypotension);
• If the patient has liver failure;
• With hyperkalemia;
• Elderly people (only if the doctor approves the drug);
• With diabetes.

Side effects

The medication has some side effects therefore, the medicine should be taken with caution. It is important to observe the required dosage and not increase it without the consent of the doctor.

These negative effects include:

1. Peripheral and pulmonary edema, dizziness;
2. Possible manifestation of tachycardia;
3. General weakness and lethargy;
4. Renal and urinary disorders;
5. Anemia may develop;
6. The manifestation of an allergy to the components of the drug (may be swelling, rash, itching, etc.);
7. Job disruption digestive organs(loss of appetite, abdominal pain, liquid stool or vice versa constipation, etc.)

An overdose of medication can cause negative manifestations in the form of: circulatory disorders of the brain, thrombosis of the veins of the lower extremities, myocardial infarction. In this case, the pressure must be stabilized to normal state via NaCl solution(0.9% intravenously). The patient must take lying position, lower limbs needs to be raised.

The advantage of the drug

There are several main advantages of Kapoten:

• Risk reduction lethal outcome from cardiovascular complications.
• Efficiency and speed. Also, the advantage of the drug is its relatively mild effect on the body. It does not affect the nervous system.
• This medicine and similar drugs do not interfere with the functioning of the kidneys. Therefore, it is allowed to take it even with renal pathologies.
• The price is another advantage of the drug. He is not expensive means, so even people with a limited budget can buy medicine.

Kapoten's analogs

Then you should pay attention to drugs with similar action. Now in pharmacies there are quite a lot of drugs with the same hypotensive effect: Alkadil, Catopil, Captopril, Lisinopril, Vasolapril, etc.

As an alternative medication, patients usually prefer Captopril. It is considered to be absolutely similar to Kapoten's action and helps in cases where other drugs do not give a visible result.

Kapoten (pharmacologically active substance- captopril) - an antihypertensive drug from the American pharmaceutical company"Bristol-Myers Squibb", belonging to the group of angiotensin-converting enzyme inhibitors (ACE inhibitors). This is the first original drug given pharmacological group, who discovered new era in the treatment of hypertension. The mechanism of its antihypertensive action is due to the ability to suppress the activity of ACE, resulting in a decrease in the rate of transition of angiotensin I to angiotensin II. The latter is known to be the most powerful endogenous vasoconstrictor factor that stimulates the release of aldosterone by the adrenal cortex. In addition, it is believed that captopril also affects the kinin-kallikrein system, thereby preventing the breakdown of bradykinin (which has its own negative side in the form of side effects such as cough and angioedema associated with the accumulation of bradykinin). The antihypertensive effect of the drug is not associated with the activity of plasma renin. Thus, a decrease in blood pressure is observed not only at normal, but also at a low concentration of this hormone, which is caused by the effect on the tissue renin-angiotensin-aldosterone system. Due to its vasodilating action, capoten reduces total peripheral and pulmonary vascular resistance, pulmonary artery wedge pressure, increases cardiac output and tolerability. physical activity. With prolonged use, it reduces the severity of left ventricular hypertrophy, prevents the progression of heart failure and inhibits the development of left ventricular dilatation. Reduces sodium levels in patients suffering from chronic heart failure. Increases the lumen of the arteries to a greater extent than the veins. Improves blood supply to areas of the myocardium affected by ischemia. Inhibits aggregation (gluing) of platelets. Reduces the tone of the efferent (carrying out) arterioles of the renal glomeruli, thereby normalizing intraglomerular hemodynamics, inhibits the development of diabetic nephropathy.

After oral administration, at least 2/3 of the active substance is rapidly absorbed into gastrointestinal tract. Simultaneous food intake reduces the absorption properties of capoten by 30-40%. The maximum plasma concentration is established after 30-90 minutes. Getting into systemic circulation, 25-30% of the drug binds to proteins (primarily to albumin). Kapoten is metabolized by microsomal liver enzymes with the formation of pharmacologically active metabolites. The half-life of the drug is less than 3 hours (in case of renal insufficiency, it can increase up to 32 hours, depending on the degree of the disease).

Kapoten is available in tablets. The initial dose of the drug can vary from 6.25 to 12.5 mg 2-3 times a day. In the absence or weakness of the therapeutic response, the dose is progressively increased to 25-50 mg 3 times a day. Persons suffering from kidney disease are prescribed more gentle doses of capoten. The maximum allowable daily dose of the drug is 150 mg. In addition to direct contraindications, there are a number of restrictions under which capoten should be prescribed with extreme caution. For example, this includes angioedema provoked by taking ACE inhibitors, aortic valve stenosis, cerebral circulatory failure, ischemic disease heart disease, diabetes mellitus, hyperkalemia, already mentioned renal or hepatic insufficiency, elderly age. Kapoten is not recommended for use in conjunction with potassium preparations and potassium-sparing diuretics (primarily for patients with diabetes mellitus and renal failure). This is due to an increased risk of hyperkalemia, since ACE inhibitors reduce the concentration of aldosterone, which, in turn, entails a delay in the body of potassium ions. The use of capoten in children is possible only in cases where other drugs have been ineffective.

Pharmacology

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 hypotensive effect does not depend on the activity of plasma renin, a decrease in blood pressure is noted 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.

Due to the vasodilating effect, it reduces OPSS (afterload), wedge pressure 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 levels in patients with chronic heart failure. Expands arteries more than veins. Improves blood supply to ischemic myocardium. Reduces platelet aggregation.

It lowers the tone of the glomerular efferent arterioles of the kidneys, improving intraglomerular hemodynamics, and prevents the development of diabetic nephropathy.

Pharmacokinetics

After oral administration, at least 75% is rapidly absorbed from the gastrointestinal tract. Simultaneous food intake reduces absorption by 30-40%. C max in blood plasma is reached in 30-90 minutes. Protein binding, mainly to albumin, is 25-30%. Stands out from breast milk. It is metabolized in the liver to form a disulfide dimer of captopril and captopril-cysteine ​​disulfide. Metabolites are pharmacologically inactive.

T 1/2 is less than 3 hours and increases with renal failure (3.5-32 hours). More than 95% is excreted by the kidneys, 40-50% is unchanged, the rest is in the form of metabolites.

In chronic renal failure cumulates.

Release form

15 pcs. - cellular contour packings (2) - packs of cardboard.

Dosage

When taken 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.

Interaction

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 ACE inhibitors and NSAIDs increase the risk of developing impaired renal function; rarely observed hyperkalemia.

With simultaneous use 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.

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

With simultaneous use with azathioprine, anemia may develop, which is due to the inhibition of erythropoietin activity under the influence of ACE inhibitors and azathioprine. Cases of the development of leukopenia are described, which may be associated with 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, it can reduce the antihypertensive effect of captopril. It has not been conclusively 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 deterioration in patients with heart failure receiving ACE inhibitors.

There are reports of an increase in the concentration of digoxin in the blood plasma with the simultaneous use of captopril with digoxin. Development risk drug interaction elevated in patients with impaired renal function.

With simultaneous use with indomethacin, ibuprofen, the antihypertensive effect of captopril decreases, 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).

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 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 the event of sudden withdrawal of clonidine in patients receiving captopril, it is possible sharp rise HELL.

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, a decrease in the effectiveness of captopril is possible, which can lead to an increase in blood pressure, hypertensive crisis described a case of cerebral hemorrhage.

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 increased risk of developing leukopenia is possible.

With simultaneous use with trimethoprim, there is a risk of developing hyperkalemia, especially in patients with impaired renal function.

With simultaneous use with chlorpromazine, there is a risk of developing 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 agents when used simultaneously with erythropoietins.

Side effects

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

From the side of cardio-vascular system: orthostatic hypotension; rarely - tachycardia.

From the side digestive system: nausea, loss of 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 hemopoietic system: rarely - neutropenia, anemia, thrombocytopenia; very rare 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).

From the side respiratory system: dry cough.

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

Indications

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

Contraindications

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

Application features

Use 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

Caution should be used when liver failure.

Application for violations of kidney function

Caution should be used in the condition after kidney transplantation, renal failure.

In case of impaired renal function, the daily dose should be reduced.

The concomitant use of potassium-sparing diuretics and potassium preparations should be avoided in patients with renal insufficiency.

Use in children

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

special instructions

Caution should be used when indicating a history of angioedema during therapy with ACE inhibitors, hereditary or idiopathic angioedema, with aortic stenosis, cerebro- and cardiovascular diseases (including in case of insufficiency cerebral circulation, ischemic heart disease, coronary insufficiency), severe autoimmune diseases connective tissue(including SLE, scleroderma), with oppression of bone marrow hematopoiesis, with diabetes mellitus, hyperkalemia, bilateral stenosis renal arteries, stenosis of the artery of a single kidney, condition after kidney transplantation, renal and / or liver failure, against the background of a sodium-restricted diet, 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.

arising during surgical intervention arterial hypotension 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 insufficiency and diabetes mellitus.

When taking captopril, a false positive reaction can be observed in the analysis of urine for acetone.

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

Influence on the ability to drive vehicles and control mechanisms

Caution required when driving vehicles or other work that requires heightened attention, because dizziness is possible, especially after the initial dose of captopril.

Owner registration certificate:
BRISTOL-MYERS SQUIBB AUSTRALIA Pty. Ltd.

Produced:
Chemical-Pharmaceutical Plant AKRIKHIN OAO

ATX code for CAPOTEN

C09AA01 (Captopril)

Analogues of the drug according to ATC codes:

You should consult with your doctor before stopping the use of KAPOTEN. These instructions for use are for informational purposes only. For more information, please refer to the manufacturer's annotation.

Clinical and pharmacological group

01.024 (ACE inhibitor)

Release form, composition and packaging

Tablets from white to white with a creamy sheen color, square with rounded edges, biconvex with a cross-shaped notch on one side and squeezed out the inscription "SQUIBB" and the number "452" - on the other, with a characteristic odor; light marbling is allowed.

Excipients: microcrystalline cellulose, corn starch, stearic acid, lactose.

10 pieces. - blisters (4) - cardboard packs. 14 pcs. - blisters (2) - cardboard packs. 14 pcs. - blisters (4) - packs of cardboard.

pharmachologic effect

ACE inhibitor. Suppresses the formation of angiotensin II and eliminates its vasoconstrictive effect on arterial and venous vessels.

Reduces OPSS, afterload, lowers blood pressure. Reduces preload, reduces pressure in the right atrium and pulmonary circulation.

Reduces the secretion of aldosterone in the adrenal glands.

Pharmacokinetics

Suction

When taken orally, the bioavailability of captopril is 60-70%. Simultaneous food intake slows down the absorption of the drug by 30-40%.

Distribution

Binding to blood proteins is 25-30%.

breeding

T1 / 2 is 2-3 hours. The drug is excreted from the body mainly in the urine, up to 50% unchanged.

CAPOTEN: DOSAGE

Kapoten® is administered orally 1 hour before meals. The dosing regimen is set individually.

With arterial hypertension, the initial dose is 12.5 mg 2 times / day. If necessary, the dose is increased gradually (with an interval of 2-4 weeks) until the optimal effect is achieved. With mild and moderate arterial hypertension, the average therapeutic dose is 25 mg 2 times / day; maximum dose is 50 mg 2 times / day. In severe hypertension, the initial dose is 12.5 mg 2 times / day. The dose is gradually increased to a maximum daily dose of 150 mg (50 mg 3 times / day).

In chronic heart failure, Kapoten® is prescribed in cases where the use of diuretics does not provide an adequate effect. The initial dose is 6.25 mg 3 times / day. If necessary, the dose is increased every 2 weeks. Maintenance dose - 25 mg 2-3 times / day. The maximum daily dose is 150 mg.

In case of left ventricular dysfunction after myocardial infarction in patients who are in a clinically stable state, the use of Kapoten can be started as early as 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) up to a maximum of 150 mg / day.

In diabetic nephropathy, the daily dose is from 75 mg to 100 mg, divided into 2-3 doses. In insulin-dependent diabetes mellitus with microalbuminuria (albumin clearance 30-300 mg / day), the dose of the drug is 50 mg 2 times / day. With a total protein clearance of more than 500 mg / day, the drug is effective at a dose of 25 mg 3 times / day.

Patients with impaired renal function of mild or moderate degree (CC ≥ 30 ml / min / 1.73 m2) Kapoten® is prescribed in daily dose 75-100 mg. At severe violations kidney function (KK

For elderly patients, the dose is selected individually. Treatment is recommended to start with the lowest therapeutic dose of 6.25 mg 2 times / day and, if possible, maintain it at this level.

If necessary, "loop" diuretics are additionally prescribed, and not thiazide diuretics.

Overdose

Symptoms: a sharp decrease in blood pressure.

Treatment: the introduction of isotonic or other plasma-substituting drugs, hemodialysis.

drug interaction

Diuretics, vasodilators (for example, minoxidil) enhance the antihypertensive effect of Kapoten®.

Indomethacin and other NSAIDs may reduce the antihypertensive effect of Kapoten®.

Simultaneous use of Kapoten with potassium-sparing diuretics (triamterene, amiloride and) or potassium preparations can lead to hyperkalemia.

The simultaneous use of lithium salts and Kapoten can lead to an increase in the concentration of lithium in the blood serum.

Against the background of the simultaneous use of Kapoten with allopurinol and procainamide, neutropenia and / or Stevens-Johnson syndrome may be observed.

With the simultaneous use of immunosuppressants (for example, azathioprine and cyclophosphamide) with Kapoten, the risk of developing hematological disorders increases.

Pregnancy and lactation

The drug is contraindicated for use during pregnancy and lactation.

CAPOTEN: SIDE EFFECTS

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

From the respiratory system: dry cough (usually disappearing after discontinuation of the drug), bronchospasm, pulmonary edema.

Allergic reactions: angioedema of the extremities, face, lips, mucous membranes, tongue, pharynx or larynx.

From the side of the central nervous system and peripheral nervous system: headache, dizziness, ataxia, paresthesia, drowsiness, visual disturbances.

From the side of water and electrolyte balance: hyperkalemia, hyponatremia.

From the urinary system: proteinuria, increased levels of urea nitrogen and creatinine in blood plasma, acidosis.

From the hemopoietic system: neutropenia, agranulocytosis, thrombocytopenia, anemia; rarely - a positive test for antibodies to the nuclear antigen.

On the part of the digestive system: taste disturbance, dry mouth, stomatitis, gum hyperplasia, abdominal pain, diarrhea, hepatitis, increased levels of hepatic transaminases in blood plasma, hyperbilirubinemia.

Terms and conditions of storage

List B. The drug should be stored in a dry place, out of the reach of children, at a temperature not exceeding 25°C. Shelf life - 5 years.

Indications

• arterial hypertension,
• including
• renovascular;
• chronic heart failure (as part of combination therapy);
• dysfunction of the left ventricle after myocardial infarction in a clinically stable condition;
• diabetic nephropathy against the background of type 1 diabetes mellitus (with albuminuria> 30 mg / day).

Contraindications

• angioedema (hereditary or associated with the use of ACE inhibitors in history);
• severe renal dysfunction;
• severe liver dysfunction;
• hyperkalemia;
• bilateral stenosis of the renal arteries or stenosis of the artery of a single kidney with progressive azotemia;
• condition after kidney transplantation;
• aortic stenosis and similar obstructive changes,
• obstructing the outflow of blood from the left ventricle;
• pregnancy;
• lactation period (breastfeeding);
• age up to 18 years;
• hypersensitivity to the drug and other ACE inhibitors.

With caution, the drug should be prescribed for severe autoimmune diseases of the connective tissue (including SLE, scleroderma), inhibition of bone marrow hematopoiesis (risk of developing neutropenia and agranulocytosis), cerebral ischemia, diabetes mellitus (increased risk of developing hyperkalemia), patients on hemodialysis, patients on a diet with sodium restriction, with primary hyperaldosteronism, coronary artery disease, conditions accompanied by a decrease in BCC (including vomiting, diarrhea), elderly patients.

special instructions

Before starting, as well as regularly during treatment with Kapoten, kidney function should be monitored. In patients with chronic heart failure, Kapoten® should be used under close medical supervision.

On the background long-term use Kapoten approximately 20% of patients have an increase in serum urea and creatinine by more than 20% compared with the norm or baseline. Less than 5% of patients, especially with severe nephropathies, require discontinuation of treatment due to an increase in creatinine concentration.

In patients with arterial hypertension when using Kapoten, severe arterial hypotension is observed only in rare cases; the likelihood of developing this condition increases with increased loss of fluid and salts (for example, after intensive treatment with diuretics), in patients with heart failure or on dialysis.

Opportunity sharp decline Blood pressure can be minimized with the preliminary cancellation (4-7 days) of the diuretic or an increase in the intake of sodium chloride (approximately a week before the start of administration), or by prescribing Kapoten 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 should be monitored monthly, then - 1 time in 3 months. In patients with autoimmune diseases, the number of leukocytes in the first 3 months of treatment should be monitored every 2 weeks, then every 2 months. If the number of leukocytes is less than 4000 / μl, it is indicated to carry out general analysis blood, if less than 1000 / μl - stop taking the drug.

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

When carrying out hemodialysis in patients receiving Kapoten®, the use of dialysis membranes with high permeability (for example, AN 69) should be avoided, since in such cases the risk of developing anaphylactoid reactions increases.

In case of development angioedema the drug is canceled and careful medical supervision is carried out. If the swelling is localized on the face, special treatment usually not needed (may be used to reduce symptoms) antihistamines); in the event that the edema spreads to the tongue, pharynx or larynx and there is a threat of obstruction respiratory tract, you should immediately enter 0.5 ml of a 0.1% solution of epinephrine (adrenaline).

When taking Kapoten, a false-positive reaction may be observed in the analysis of urine for acetone.

With caution, Kapoten® should be prescribed to patients on a low-salt or salt-free diet, because. in this case, the risk of arterial hypotension increases.

In case of symptomatic arterial hypotension after taking Kapoten, the patient should take a horizontal position with raised legs.

Pediatric use

The safety and efficacy of the drug in children and adolescents under the age of 18 have not been established.

Influence on the ability to drive vehicles and control mechanisms

During the period of treatment, it is necessary to refrain from driving vehicles and engaging in potentially dangerous species activities requiring increased concentration attention and speed of psychomotor reactions, tk. dizziness is possible, especially after taking the initial dose.