Capoten is a drug that has been called the “gold standard” for more than 30 years drug treatment hypertension and heart disease. Although after its implementation in clinical practice(in 1981) more than safe means with similar mechanism actions, Kapoten stands out for the speed of attack therapeutic effect. So patients and doctors are in no hurry to “jump ship” from modern drug therapy This is already an obsolete medicine.

Yes, capoten tablets are less well tolerated than their analogues and create a load on the liver, but they are more effective as an ambulance in case of sharp increase blood pressure. And if, when taking capoten, the dosage does not exceed that recommended by the instructions, then the tolerability of the drug is comparable to more modern representatives of the pharmacogroup (enalapril, lisinopril, noliprel forte).

Composition and release form of the drug

For capoten, the release forms are not varied. If more modern competitors of the drug are already available in capsule form, then the only dosage form Capoten tablets remain.

The active component of capoten is called Captoprilum in Latin. The content of this substance in each capoten tablet is 25 mg. Tablets containing not 25, but 50 mg are also available active substance. The composition of the drug described in the instructions for capoten also includes microcrystalline cellulose, starch, stearic acid, lactose. But these components of the drug therapeutic role don't play. They are needed only so that the medicine takes the form of a tablet.

The pharmaceutical company Akrikhin is producing the drug in Russia. However, the tablets were developed by the global biopharmaceutical company Bristol-Myers Squibb, whose office is located in New York. In 1990, to produce a domestic hood, manufacturers entered into an agreement with Bristol-Myers Squibb. In the late 90s of the XX century, together with this company Russian manufacturer launched licensed production of the drug. To protect the drug from counterfeiting, the manufacturer labels capoten: the tablet is supplied brand name“SQUIBB” and the numbers 452. The tablets are also distinguished by their unusual square shape with rounded edges.

Capoten is produced in blister packs and bottles. Depending on the doctor’s recommendations, the patient can choose the desired volume of the package, which contains 10 to 60 tablets. In the packaging design, the manufacturer prudently indicates the concentration active substance in a prominent place: immediately below the name there is a line “25 mg tablets” or “50 mg tablets”. This means that the composition of each tablet includes, respectively, 25 or 50 mg of captopril - the active ingredient that determines all the therapeutic effects of the drug capoten.

How does Kapoten work?

The target of the drug is angiotensin-converting enzyme (ACE).

The enzyme is designed to catalyze the reaction of converting angiotensin I into angiotensin II.

Angiotensin I is a small protein molecule. Only 10 amino acids form the composition of this molecule. The substance circulates in the blood serum without exerting any biological effects until it encounters the active site of ACE. The enzyme slightly changes the composition of angiotensin I by splitting off a couple of amino acids. However, this small change dramatically changes the behavior of the original molecules. Angiotensin II released from ACE is already an active hormone. It affects blood vessels, causing them to narrow, and stimulates the synthesis of another hormone in the adrenal cortex - aldosterone, which retains sodium and water in the body. All these processes lead to increased blood pressure.

ACE is an angiotensin-converting enzyme that converts a hormone called angiotensin-I into the hormone angiotensin-II.

After clarification this mechanism To regulate blood pressure, researchers began to look for a prescription drug that would inhibit (inhibit) ACE activity. In the 70s of the 20th century, the first such substance was synthesized, which was called captopril. And in the early 80s it was approved for the treatment of patients suffering from arterial hypertension. Capoten became the first drug of the pharmacological group ACE inhibitors containing captopril.

After this, dozens more ACE inhibitors were synthesized, the composition of which was made safer. However, along with increased safety, these drugs are also characterized by lower effectiveness. Capoten not only inhibits ACE, but at the same time directly neutralizes potentially dangerous free radicals. The developers of the drug found that this capoten effect, which is not typical for other ACE inhibitors, is due to the presence of a sulfhydryl group in the active substance of the drug.

The composition of the molecules of more modern representatives of this pharmacogroup contains a carboxyl part instead of a sulfhydryl part. All of these drugs increase enzyme activity antioxidant protection. However, only capoten has a complex effect on a number of parts of the free radical fighting system, including stimulating the production of nitric oxide, which protects cells from oxidative stress.

Functionality

Therefore, in cases where it is necessary to prevent, for example, damage to the myocardium by free radicals during stress, preference is given to capoten: the medicine is capable of:

• increase coronary blood flow;
• eliminate endothelial dysfunction;
• prevent the development of nitrate tolerance;
• increase the magnesium content inside cardiomyocytes;
• slow down development;
• stimulate the activity of the parasympathetic system.

Thus, capoten has a more pronounced cardioprotective effect than other representatives of the pharmacological group.

Among additional effects noted to be antidiabetogenic. Of course, the drug does not contain insulin, but capoten improves the binding of insulin produced by the body to receptors on the surface of cells.

For what diseases is Capoten prescribed?

The annotation for the drug Capoten states that this medication reduces blood pressure and increases the performance of the heart muscle. Indeed, the drug has found its main use in the treatment of various forms of hypertension, chronic heart failure, and left ventricular systolic dysfunction.

The manufacturer also lists myocardium (especially during secondary prevention) and diabetic nephropathy as indications for use.

Clinical studies have shown that the drug is more effective than other representatives of its pharmacological group in reducing the risk of developing chronic heart failure and recurrent myocardial infarction. This is due to the fact that the active substance of the drug most actively affects ACE, localized in myocardial cells, as well as a direct antioxidant effect.

Kapoten: instructions for use (official)

Contraindications to the use of Capoten

In the instructions for using capoten, the description of contraindications traditionally includes a clause about intolerance (hypersensitivity) to its components. In addition, the manufacturer does not recommend using the tablets if:

• the patient has impaired liver and kidney function;
• during pregnancy and in case of breastfeeding;
• if stenoses are diagnosed renal arteries or the aorta.

If the patient’s complex drug therapy includes diuretics, adrenergic blockers, immunosuppressants and some other drugs, the effect of the drug may be enhanced or weakened, as well as unplanned hematological effects.

How to take Capoten?

The description recommends the sale of this medication by prescription. The recipe contains recommendations, among which individually selected dosage is of primary importance. For capoten, the dosage is usually in the range of 50–150 mg per day. In typical cases, when prescribing capoten, the prescription contains a recommendation to take it 2 or 3 times a day. This dosage of Capoten is sufficient for effective blood pressure control throughout the day. However, if the composition of drug therapy is not limited to capoten, the standard dosage may be changed. For example, when a patient is prescribed diuretics, the dosage may be reduced.

After purchasing a box of Capoten, Capoten Forte or other ACE inhibitors in tablet form, you should not immediately start with the whole tablet. On initial stage course of treatment, a standard 25 mg tablet will have to be crushed before drinking. For example, for hypertension, only half of a 25 mg tablet is cut off; These halves are taken twice a day. Unfortunately, the manufacturer did not provide tablets with an active substance concentration of less than 25 mg for such cases. After 2–4 weeks, the dose can be adjusted to what is appropriate for most patients: 25 mg twice daily.

If hypertension has severe forms, it is advisable to purchase tablets containing not 25, but 50 mg. They are taken three times a day so that the total dose does not exceed 150 mg.

Video: Treatment of hypertension without drugs (Sytin)

The medicine capoten is widely used for various states associated with a persistent, long-term increase in blood pressure. instructions for use of capoten recommend using it when various forms essential, true and portal hypertension, ischemic chronic illness heart to prevent the risk of myocardial infarction, temporary or retrograde nephropathy with the development of acute renal failure syndrome.

The drug capoten is available in the form of tablets with a dosage of 25 mg. The main active ingredient captopril is supplemented auxiliary components, which are necessary to form the tablet shape. Other components that enhance the effect of captoril are not used in this medicine.

pharmachologic effect

As a standard, capoten is recommended for oral administration with a small amount of liquid. After this, the bioavailability of the active substance in the blood appears within 40 minutes. 60 minutes after administration, the maximum concentration is already observed in the blood. With a sharp increase in blood pressure and the risk of developing hypertensive crisis you need to take capoten under the tongue. In this case, the bioavailability of the active substance is recorded after 5 - 10 minutes, depending on the metabolism of the individual. The drug is excreted by the kidneys within 3 hours from the moment the absorption into the blood begins.

The pharmacological effect is based on the ability of captopril to counteract the synthesis of angiotensin II. This substance narrows the lumen of all blood vessels almost instantly after release into the blood. A small amount of excess adrenaline is sufficient to produce it. Due to the expansion and stabilization of vessel walls circulatory system on the background long-term use the following happens:

• blood flow to the structures of the brain increases, which has a beneficial effect on the brain centers for regulating the humoral activity of the human body;
• dilatation (expansion) of the ventricles and atria is prevented, due to which the contractility of the heart muscle is restored;
• the phenomena of vascular and heart failure are reduced.

Indications

The drug kapoten has rather limited indications for use. This is specialized medicine, which can provide therapeutic effect only when the activity of the cardiovascular system is impaired. For portal hypertension, this substance is used in complex therapy. IN pure form it does not always sufficiently help reduce pressure in the portal and portal veins.

Main indications for use include:

• hypertension - stages 2 - 3;
• excretory arterial hypertension 2 stages;
• cardiovascular acute and chronic failure;
• elimination of defective functioning of the left ventricle in patients who have undergone acute heart attack myocardium;
• nephropathy due to diabetic damage to the renal collateral vessels;
• hepatopathy against the background of liver cirrhosis with portal hypertension in the decompensated stage.

How to take capoten in tablets - dosages
Hypertension 1st degree	1/2 tablet 2 times a day.
Hypertension 2-3 degrees	1 tablet 2 times a day.
Hypertensive crisis and the risk of its development against the background of a sharp increase in blood pressure	2 tablets under the tongue at 30-minute intervals. After resorption of the first tablet, monitoring of blood pressure levels is necessary.
Heart and vascular failure	6.25 mg 3 times a day. If necessary, the dosage is gradually increased.
Myocardial infarction in the acute stage	The drug may be taken 72 hours after the first ischemic attack. 6.25 mg 3 times a day with a gradual increase in a single dosage to 25 mg.
Renal dysfunction in insulin-dependent diabetes mellitus	25 mg 3 times a day for a long time.

For other forms of diseases, the dosage is determined individually by the attending physician. In some cases, combination therapy in combination with diuretics and other antihypertensive drugs is indicated. Optimal control scheme hypertension and related conditions can only be developed under the supervision of your doctor. You should not use drugs in this group on your own without monitoring blood counts and an electrocardiogram.

Contraindications and side effects

Capoten tablets are contraindicated during pregnancy and breastfeeding. Other risk factors for taking the drug include:

• severe intolerance to captopril;
• narrowing of the mouth at the entrance to the aorta;
• stenosis of other large blood arteries;
• azotemia and severe hypoglycemia.

Side effects may manifest themselves in the cardiovascular system in the form of increased heart rate, sharp decline blood pressure, increased shortness of breath. IN in rare cases bronchospasm appears with laryngeal edema, skin rash and activity disorders digestive tract. Eliminate everything side effects It is possible to completely discontinue the drug and replace it with an analogue with a less pronounced pharmacological effect.

INSTRUCTIONS
By medical use drug

Kapoten

(CAPOTEN(R))

General characteristics:

International name: captopril (1-[(2S)-3-mercapto-2-methyl-propionyl]-L-proline);

Dosage form: square tablets with rounded corners, biconvex, white or almost white with a cross-shaped notch on one side and engraving "SQIBB" and "452" on the other, with a slight smell of sulfide;

Compound:1 tablet contains 25 mg captopril;

microcrystalline cellulose, corn starch, lactose, stearic acid.

Release form. Pills.

Pharmacotherapeutic group.

ACE inhibitors (ACE). ATS code C 09A A 01.

Pharmacodynamics.

Capoten suppresses the activity of ACE, as a result of which angiotensin-I is not converted into angiotensin-II, a substance with a strong vasoconstrictor effect. Capoten reduces the secretion of aldosterone in the adrenal cortex, while reducing sodium and water retention in the body. Capoten inhibits the process of destruction of bradykinin and helps to increase the content of prostaglandin E2, as well as nitric oxide, which causes a vasodilator effect. Thanks to these effects, increased arterial pressure, OPSS decreases, pressure in the right atrium and in the pulmonary circulation decreases, cardiac output increases.

Pharmacokinetics.

When taking the drug "capoten" orally, the maximum concentration in the blood is reached after 1 hour. Availability of food in gastrointestinal tract reduces absorption by approximately 30 - 40%; to avoid this, capoten should be taken 1 hour before meals. On average, the minimum absorption of capoten is approximately 75%. Within 24 hours, more than 95% of the absorbed dose is excreted in the urine, 40% to 50% of captopril is excreted unchanged, and the rest is excreted as dimers of captopril disulfide and captopril disulfide-cysteine.

From 25% to 30% of circulating captopril is bound to plasma proteins. The half-life from the blood is about 3 hours. In patients with renal failure There may be a delay in the administration of captopril. Biotransformation of the drug occurs in the liver, the drug passes through histohematic barriers including the BBB and placenta. In women during lactation, captopril penetrates into breast milk. Removed by hemodialysis.

Indications.

Arterial hypertension.

Chronic heart failure.

Myocardial infarction with impaired left ventricular function (ejection fraction<= 40%).

Diabetic nephropathy.

Application.

Arterial hypertension.

Capoten should be used in the lowest effective dose, selected individually for each patient.

Mild to moderate arterial hypertension.

The initial dose is 12.5 mg 2 times a day. The usual maintenance dose is 25 mg 2 times a day, and it can be increased gradually at intervals of 2 to 4 weeks to achieve satisfactory treatment results, most often this is 50 mg 2 times a day.

Severe arterial hypertension.

In severe hypertension, when standard therapy is ineffective or unacceptable due to adverse reactions, the initial dose of the drug "capoten" is 12.5 mg 2 times a day. The dose can be increased in stages to 50 mg 3 times a day. It is advisable to use Capoten together with other antihypertensive drugs, however, the dose of these drugs should be selected individually.

For most patients, a stable therapeutic effect can be obtained without exceeding a daily dose of 150 mg, but the maximum permissible daily dose of the drug "capoten" is 450 mg.

Heart failure.

Treatment with the drug "Capoten" must be started under conditions of careful medical supervision. At an initial dose of 6.25 mg 3 times a day, the effect of transient hypotension can be maximally reduced. The usual maintenance dose is 25 mg 2 or 3 times a day, and the dose can be increased in stages at least every two weeks until satisfactory results are obtained. The maximum daily dose is 150 mg.

Myocardial infarction.

Treatment can begin as early as 3 days after myocardial infarction. After the initial dose of 6.25 mg 3 times a day, the dose of the drug should be gradually increased over the next few weeks to 25 mg 3 times a day, if necessary, the dose can be gradually increased to a maximum daily dose of 150 mg (50 mg 3 times a day). in a day).

If symptomatic hypotension occurs, the dose should be reduced.

Capoten can be prescribed to patients receiving treatment with other drugs in the period after myocardial infarction, in particular thrombolytic drugs, aspirin and beta-blockers.

Diabetic nephropathy.

The recommended daily dose of the drug is from 75 to 100 mg in 2 to 3 doses. For insulin-dependent diabetes with microalbuminuria (albumin excretion 30-300 mg per day), the dose of the drug is 50 mg 2 times a day. If the total protein clearance is more than 500 mg per day, the drug is prescribed at a dose of 25 mg 3 times a day.

If it is necessary to further reduce blood pressure, in addition to Capoten, other antihypertensive drugs can be prescribed: diuretics, beta-blockers, centrally acting drugs or vasodilators.

Patients with impaired renal function.

Capoten in a daily dose of 75 to 100 mg per day in several doses was well tolerated by patients with diabetic nephropathy and mild/moderate renal dysfunction (creative new clearance of at least 30 ml/x./1.73 m2).

Accordingly, in patients with severe renal impairment (creative new clearance less than 30 ml/x./1.73 m2), the initial dose should not exceed 6.25 mg 2 times a day. In the future, the dose is selected depending on the results of treatment, but with large time intervals between dose changes, usually every 1 to 2 weeks, but not more than 75 mg per day.

Elderly patients.

The dose should be adjusted depending on the decrease in blood pressure and maintained at the minimum level necessary to achieve the expected result. Since renal dysfunction and dysfunction of other organs are more common in elderly patients, a small dose of the drug should be used at the beginning of treatment.

Children.

The safety and effectiveness of the drug "capoten" in children have not been sufficiently studied.

Side effect.

The cardiovascular system.

Short-term arterial hypotension is possible (“first dose effect”). In most cases, the attack stops if the patient takes a supine position. The development of hypotension after taking the first dose is not a contraindication for further use of the drug "Capoten".

In patients with severe forms of renin-dependent hypertension (eg, renovascular hypertension) or with severe congestive heart failure receiving large doses of a diuretic, excessive hypotensive reactions were usually observed within one hour after taking the initial dose of Capoten. Discontinuation of diuretic treatment or a significant reduction in the dose of diuretic 4-7 days before starting treatment with this drug reduces the likelihood of developing arterial hypotension. If you start treatment with small doses (6.25 mg or 12.5 mg), the duration of the possible hypotensive effect is reduced. In some patients, infusion of saline solution can lead to a positive effect. In patients using capoten, there were several cases of hypotension, which developed against the background of acute hypovolemia due to vomiting and diarrhea.

Respiratory system.

A dry cough is possible, rarely - bronchospasm.

Kidneys.

Proteinuria and an increase in blood urea nitrogen and creatinine may occur.

Allergic reactions.

Possible skin rashes, redness of the facial skin, rarely - angio-neurotic edema of the face, eyelashes, tongue, peripheral edema.

Blood system.

Neutropenia, anemia, agranulocytosis, and platelet swelling have been reported. Nironeutropenia was rarely observed in patients with normal function.

Water and electrolyte disturbances.

Hyperkalemia (most likely in renal failure), hyponatremia (more often observed in patients on a salt-free diet while taking diuretics), acidosis.

Gastrointestinal tract.

Reversible disturbances in the sense of taste are possible, which disappear on their own, and dry mouth. Stomatitis resembling aphthous ulcers. Sometimes there was an increase in the activity of liver enzymes. Gastric irritation and abdominal pain may occur.

There are rare cases of the development of cholestatic jaundice, as well as hepatonecrosis in individuals taking ACE inhibitors; the mechanism of development of these phenomena has not yet been studied.

There are isolated reports of the development of pancreatitis among patients treated with ACE inhibitors.

Central nervous system.

Possible headache, dizziness, ataxia, paresthesia, drowsiness.

Contraindications.

A history of hypersensitivity to captopril or a case of angioedema while taking other ACE inhibitors.

Bilateral renal artery stenosis or stenosis of the artery of a single kidney with progressive azotemia.

Pregnancy and lactation.

Overdose.

Symptoms: severe arterial hypotension, bradycardia, water and electrolyte imbalance.

Treatment:measures aimed at increasing the level of AT by increasing the volume of blood volume (intravenous administration of saline and plasma substitutes. The drug is removed from the body by hemodialysis

Features of application.

The patient's examination should include assessment of renal function before initiation and course of treatment.

Capoten should not be prescribed to patients with aortic stenosis or in the presence of other obstructive phenomena in the path of blood outflow from the heart.

Since capoten reduces the production of aldosterone in the body, serum potassium concentration usually remains unchanged in patients receiving diuretics. Therefore, you should not regularly use potassium-sparing diuretics or inject potassium. In patients with severe renal impairment, a marked increase in serum potassium concentrations may be observed.

Capoten can cause a false-positive reaction in a urine test for acetone.

Capoten should not be prescribed to patients with renovascular hypertension after kidney transplantation.

Capoten should not be prescribed to patients with autoimmune diseases accompanied by hematopoietic disorders (neutropenia, thrombocytopenia).

In patients receiving capoten who are planning to undergo surgery with general anesthesia, the possibility of developing arterial hypertension under the influence of anesthetics should be considered, which can be corrected by the introduction of an additional volume of fluid (plasma substitutes).

Capoten should not be prescribed to patients with severe manifestations of liver failure.

When using the drug "capoten", you should remember that there is cross-hypersensitivity between drugs in the ACE inhibitor group.

During treatment with the drug "Capoten" you should avoid drinking alcohol.

Caution must be exercised when driving vehicles, as well as when performing work that requires increased attention, since dizziness is possible, mainly after taking the first dose.

Interaction with other drugs.

Diuretics, vasodilators, ganglion blockers, adrenoblockers enhance the hypotensive effect of the drug "capoten".
Drugs that increase serum potassium concentrations, potassium-sparing diuretics (triamterene, amiloride and spironolactone) or potassium administration may lead to a marked increase in serum potassium concentrations.

Indomethacin and other non-steroidal antihypertensive drugs may reduce the hypotensive effect of the drug "capoten".

Clonidine may enhance the antihypertensive effects of the drug "capoten".

Allopurinol and procainamide in combination with the drug "capoten" can cause neutropenia and / or Stevens-Johnson syndrome, the causal relationship is unclear.

Immunosuppressants (azathioprine and cyclophosphamide) taken simultaneously with the drug "Capoten" increases the risk of developing hematological disorders.

Probenecid. The excretion of the drug "capoten" by the kidneys is reduced in the presence of probenecid.

Lithium. The simultaneous use of lithium salts and ACE inhibitors may lead to an increase in serum lithium concentrations.

Anesthesia drugs, when used simultaneously with the drug "capoten", can enhance the hypotensive effect.

Ethanol, when used simultaneously with the drug "capoten", can enhance the hypotensive effect.

Antacids reduce the bioavailability of the drug "capoten".

Storage conditions.

Keep out of the reach of children.

Store at a temperature of 15-25 ° C.

Shelf life - 3 years.

Article publication date: 05/02/2017

Article updated date: 12/18/2018

From this article you will learn all the important information about Capoten tablets: what and how they help. For what diseases are they prescribed, what symptoms do they help relieve.

Capoten is an angiotensin-converting enzyme inhibitor (). Its main effect is to reduce blood pressure.

The drug has side effects and contraindications, so take it only as prescribed by your treating cardiologist or therapist.

These tablets are prescribed to patients suffering from the following diseases:

Capoten for hypertension

The tablets help to significantly reduce blood pressure through two mechanisms:

1. Do not allow blood vessels to narrow. The drug blocks the enzyme that converts angiotensin 1 into angiotensin 2. Angiotensin 2 is a substance that constricts blood vessels, which increases blood pressure. Since blocking the angiotensin-converting enzyme does not produce the same amount of angiotensin 2, blood pressure does not increase.
2. . This effect is achieved by increasing the level of bradykinin, prostaglandin E 2 and nitric oxide in the blood - bioactive substances that reduce vascular tone and dilate them.

Mechanism of action of ACE inhibitors

Thanks to this mechanism of action, Capoten not only prevents pressure from rising, but also reduces it if it has already risen.

This drug is especially effective for hypertension caused by kidney disease. With kidney pathologies, their production of renin increases, a substance that, when combined with angiotensin produced by the liver, forms angiotensin 1. And angiotensin 1 is converted into angiotensin 2 under the action of angiotensin-converting enzyme. Angiotensin 2 causes an increase in blood pressure; renin, angiotensin and angiotensin 1 themselves do not have this effect. Capoten, by blocking angiotensin-converting enzyme, prevents an increase in the level of angiotensin 2.

However, this does not help much with kidney disease itself. This medication only eliminates hypertension caused by kidney disease and, by reducing pressure, relieves excessive stress on the kidneys. If you stop taking the pills, high blood pressure will make itself felt again. To completely get rid of nephrogenic hypertension, it is necessary to treat the underlying kidney disease, and take an ACE inhibitor as an addition to the main therapy - as a symptomatic treatment of high blood pressure.

Capoten for chronic heart failure

How and why the drug helps with chronic heart failure:

• Lower blood pressure if it is elevated (the mechanism of this effect is described in the previous section).
• Relieve swelling. Capoten reduces the level of the adrenal hormone aldosterone, thereby reducing sodium retention and, accordingly, water retention in the body.
• Reduce shortness of breath and warn. Thanks to a decrease in pressure in the small (pulmonary) circle.
• . Due to the dilation of blood vessels and an increase in the volume of blood emitted by the heart.

Dilated and spasmodic artery

Kapoten after a heart attack

It is used not in the acute phase of the disease, but when the patient is already in a stable condition. Typically, the drug can be taken 3 days after a heart attack.

Tablets are needed to prevent heart failure caused by necrosis of a portion of the myocardium. They improve blood circulation, prevent blood stagnation in the small and large circles, as well as edema, and increase the ejection fraction of the left ventricle.

Kapoten also prevents a recurrent heart attack, as it dilates blood vessels, including coronary ones, and normalizes blood supply to the heart muscle.

Capoten for diabetic nephropathy

Diabetic nephropathy is damage to the blood vessels of the kidneys that occurs against the background of diabetes.

For this pathology, the drug is prescribed to improve blood circulation in the kidneys by relieving vascular spasm. And also to lower blood pressure, increased due to kidney damage.

Taking an ACE inhibitor for diabetic nephropathy significantly improves the prognosis: it reduces the risk of needing hemodialysis or a kidney transplant.

Captopril, the active substance of Capoten, is one of the most well-known medications that lower blood pressure. Among the ACE inhibitors, it was the first to be obtained, and it was its great medicinal effectiveness that prompted the development of the synthesis of similar drugs.

Release form and composition

Kapoten supplied to the market in tablet form. The shape and appearance of the tablets vary depending on the manufacturer. Tablets by 25 or 50 mg, usually white, biconvex, possibly embossed on the sides. Cross-shaped bevels (if present) help to separate the tablet into two equal halves weighing 12.5 mg ( 25 mg) or into four parts weighing 6, 25 mg(12.5 mg). As a rule, one package contains from 28 to 56 tablets.

Main substance: captopril 25 mg or 50 mg.

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

How does Kapoten work?

In the human body, there are special systems that regulate the narrowing or dilation of blood vessels using the hormones they release. One of the main systems responsible for contraction is the renin-angiotensin-aldosterone system (RAAS). It regulates the balance of fluids, electrolytes, blood pressure and blood volume. It happens something like this: the liver produces the protein angiotensinogen, which, under the influence of renin produced by the kidneys under certain conditions, is converted into angiotensin I. This substance in itself has no effect on the body; it is needed only as a “raw material” for a real worker - angiotensin II. And it already constricts the blood vessels, causing an increase in pressure.

The transition of angiotensin from the first form to the second is caused by the angiotensin-converting enzyme, ACE. Therefore, when developing blood pressure-lowering drugs, scientists have long tried to find drugs that would inhibit the production of ACE and thereby prevent the appearance of angiotensin II in the body, until at the end of the last century the first ACE inhibitor, captopril, was obtained from the venom of a Brazilian snake. The new drug turned out to be so effective that it served as the basis for the synthesis of new similar drugs. Currently, there are more than 100 types of ACE inhibitors. As practice has shown, ACE inhibitors have proven to be as effective (if not more) as traditional medications for the treatment of arterial hypertension - diuretics and beta blockers.

In addition, ACE inhibitors have many beneficial properties. They are metabolically neutral, which is especially important for patients with concomitant diseases (for example, diabetes). More Kapoten has a cardioprojector and nephroprotective effect, and when taking ACE inhibitors, the risk of recurrent stroke and cardiovascular complications is reduced.

Pharmacokinetics

The degree of absorption of captopril is approximately 75%. Peak concentration is reached 60-90 minutes after taking the medicine. The presence of food in the gastrointestinal tract reduces the level of drug absorption by approximately 30-40%.
The half-life is approximately 2 hours; more than 95% is excreted through the kidneys within 24 hours. Patients with diseases of the urinary system, especially with increased levels of urea and creatinine, should inform their doctor in advance.

Research has shown that Kapoten does not cross the blood-brain barrier.

Indications for use of Capoten

Hypertension. A decrease in blood pressure occurs 60-90 minutes after taking Capoten. The duration of action depends on the dose. The decrease in pressure can be progressive, so it may take several weeks to achieve the maximum therapeutic effect.

Heart failure. Kapoten prescribed for the treatment of chronic heart failure, characterized by a decrease in ventricular systolic function. The drug can be prescribed in conjunction with diuretics and, if necessary, beta blockers.

Myocardial infarction. Stable patients can take Kapoten during the first 24 hours after a heart attack.

Long-term prevention of heart failure symptoms. Kapoten shown for use in clinically stable patients with asymptomatic left ventricular dysfunction.

Diabetic nephropathy type I. Kapoten may be used to treat macroproteinurial diabetic nephropathy in patients with type I diabetes.

How to use Capoten

The dosage of the drug is calculated based on the individual profile of the patient and his blood pressure. The maximum daily dose is 150 mg. Kapoten can take both during, before and after meals - the time of meal does not affect its effectiveness. Taken orally.

Hypertension. The recommended starting dose of Capoten for hypertension is 1-2 tablets 25 mg per day in two divided doses. To achieve the required pressure levels, the dose can be gradually increased (with an interval between changes of at least two weeks) up to 100-150 mg per day in two doses. Capoten is indicated for use both alone and with other blood pressure-lowering agents. Captopril works especially well in combination with thiazide diuretics (in this case Capoten can be taken once a day).

In patients with hypovolemia, renovascular hypertension and cardiac decompensation it is preferable to start with a single dose of 6, 25 mg(quarter tablet) or 12.5 mg (half tablet). Taking Capoten in such patients should be under close medical supervision. The dose is gradually increased to 50 mg (once or twice a day) and, if necessary, up to 100 mg per day (once or twice a day).

Heart failure. Treatment of heart failure with Capoten should be under constant medical supervision. Usually start taking a quarter or half a tablet (6, 25 mg or 12.5 mg). If the patient tolerates the treatment well, the dose can be gradually increased to 150 mg per day (in two doses). The interval between dosage changes should be at least two weeks.

In patients with stable hemodynamics Kapoten shown for use as soon as possible after the first signs of a heart attack appear. In the first 24 hours after a heart attack, the dose starts at 6. 25 mg(quarter tablet), after two hours 12.5 mg, and after twelve hours the dose is increased to 25 mg. The next day they accept drug for 50 g twice daily for four weeks, provided there are no adverse hemodynamic reactions. Four weeks after the heart attack, your doctor will need to create a new treatment plan.

If treatment does not start within the first 24 hours, then Kapoten begin to take between 3 and 16 days after a heart attack, provided that the patient has stable hemodynamics. In this case, treatment begins in a hospital, under strict medical supervision; Particular attention should be paid to blood pressure indicators. The initial dose should be low - usually start with 6.25 mg, then 12.5 mg 3 times a day for two days, and if hemodynamic responses are normal, the dose is increased to 75 mg per day (according to 25 mg 3 times a day). The recommended dose for effective heart protection in this case is 75-150 mg per day in two to three doses.

If necessary, the dose of Capoten is adjusted depending on the condition. Also Kapoten may be used in combination with other treatments for myocardial infarction such as beta blockers, acetylsalicylic acid and thrombolytic agents.

Nephropathy in type I diabetes. In such patients, the recommended daily dose of Capoten is from 75 to 100 mg per day (in three to four doses). If it is necessary to further reduce blood pressure, the patient may be prescribed additional antihypertensive drugs.

Patients with kidney failure. Since captopril is excreted from the body mainly through the kidneys, the dosage and time of taking the drug in such patients is adjusted taking into account the disease - usually either the dose is reduced or the interval between doses of the drug is increased. If concurrent diuretic therapy is required, patients with renal failure are advised to take a loop diuretic rather than a thiazide diuretic, such as furosemide. The dose of the drug is calculated depending on creatinine clearance; for example, if the clearance is more than 40, then taking Capoten starts with 25-50 mg, the maximum dose is 150 mg. If the clearance is low, less than 10, then the initial dose is 6.25 mg, and the maximum is 37.5 mg.

Capoten for the elderly. One general rule when determining the dosage of blood pressure lowering medications in older adults is to start with a lower dose (6.25 mg), since these patients may have reduced kidney function.

Kapoten for children. Captopril should only be used in children under close medical supervision. The initial dose is about 0.3 mg per kg of the child's weight. If the patient suffers from renal dysfunction or is a newborn or infant under one year of age, the initial dose should be only 0.15 mg captopril per kg of the child's weight. As a rule, children are given Kapoten three times a day, and, of course, the dosage should be calculated individually depending on the patient's response to treatment.

Contraindications

Allergic reactions. If the patient or his relatives have experienced allergic reactions after taking drug, use Capoten is not recommended.

Increased individual sensitivity to captopril (or any other ACE inhibitor) or other substances contained in the tablets.

Kidney failure. Can not use Kapoten for the treatment of patients with aortic stenosis or bilateral renal artery stenosis at one functioning point.

Kidney failure caused by diabetes. For such patients it is not recommended to use Kapoten with aliskiren-containing drugs.

Kapoten during pregnancy and breastfeeding

Pregnancy. Kapoten during pregnancy It is prohibited to take it, as the product has a toxic effect on the fetus. If the patient does not plan to become pregnant and uses reliable methods of contraception, use Kapoten Can. If pregnancy is planned, Kapoten it is recommended to replace with alternative antihypertensive treatments that can be used during pregnancy. If pregnancy occurs, treatment with Capoten should be stopped immediately and, if necessary, alternative therapy should be started.

Lactation. Although the amount of captopril excreted in breast milk is negligible, its use is not recommended when breastfeeding premature newborns in the first few weeks after birth. Hypothetically, there may be a risk of cardiovascular and renal side effects in the child. Clinical studies of the effects of Capoten on newborn infants have not been conducted. If the child is older, taking Capoten while breastfeeding is possible if the benefits of using the drug exceed its harm to the mother and child. In any case, the condition of both mother and child should be constantly monitored.

Side effects

Frequency of side effects: very often (from 1/10 to 1/100); common (from 1/100 to 1/100), rare (from 1/1000 to 1/10000) and very rare (1 case in 10,000 people or more).

	Often	Often	Rarely	Very rarely
Circulatory system				Neutropenia, agranulocytosis, pacytopenia (especially in patients with renal dysfunction), anemia, thrombocytopenia, lymphadenopathy
Digestive system		Decreased appetite
Metabolism				Hyperkalemia, hyponatremia, hypoglycemia
Mental disorders	Insomnia			Depression
Nervous system	Dizziness	Headache, pins and needles sensation, tingling (paresthesia)	Drowsiness	Fainting
Vision			Blurred vision
Heart		Tachycardia, arrhythmia, angina pectoris, palpitations		Cardiac arrest, cardiogenic shock
Vessels		Hypotension, skin redness, pallor, orthostatic hypotension
Respiratory system	Dry cough, shortness of breath			Bronchospasm, rhinitis, alveolitis, allergic pneumonia
Gastrointestinal tract	Nausea, vomiting, abdominal pain, diarrhea, constipation, dry mouth, peptic ulcer, dyspepsia		Stomatitis, angioedema of the small intestine	Pancreatitis
Liver				Abnormal liver function, cholestasis, jaundice, hepatitis, hepatic necrosis, increased blood bilirubin levels, increased transaminase levels
Leather	Itching with or without rash	Angioedema		Urticaria, erythema multiforme, photosensitivity, exfoliating dermatitis
Bones, muscles, connective tissue			Myalgia, arthralgia
Urinary system			Renal failure, kidney failure, polyuria, oliguria	Nephrotic syndrome
Reproductive system			Erectile dysfunction, gynecomastia
General disorders		Chest pain, fatigue, asthenia		Pyrexia

Not all side effects that Capoten may cause are listed here; Their presence is largely due to the individual reaction of the body. If a person thinks that after taking Capoten, undesirable effects occur for him, he should inform his doctor about this.

special instructions

Low pressure. Hypotension most often occurs in patients whose blood sodium volume is reduced due to diuretics, salt restriction due to diet, diarrhea, vomiting, or after hemodialysis. Before taking captopril and other ACE inhibitors, it is recommended to compensate for the lack of sodium, as well as prescribe a lower initial dose.

If the patient's low blood pressure is due to heart failure, a lower initial dose is recommended. This is true for the first or second week after the start of treatment; then you can go to the usual dosage. Increasing the dosage of Capoten or a diuretic for such patients should be carried out under the supervision of a physician.

These precautions are because excessively lowering blood pressure in patients with cardiovascular or cerebrovascular disease may increase the risk of myocardial infarction or stroke. If the pressure is very low, the patient should be in a supine position; A saline drip may be required.

Capoten should be used with extreme caution for infants.(especially newborns); they may be more susceptible to adverse pressure changes. The following complications may occur: unpredictable and prolonged decrease in pressure, oliguria, convulsions.

Renovascular hypertension. Patients with bilateral renal artery stenosis or arterial stenosis of one functioning kidney have an increased risk of hypotension and renal failure. Therapy with Capoten in such patients is carried out under close medical supervision; the patient is prescribed a reduced dose of the drug, and the condition of his kidneys must be constantly monitored.

Kidney failure. If creatinine clearance is less than 40 ml/min, then the initial dose of Capoten is calculated based on this indicator. Regular monitoring of potassium and creatinine levels is part of routine medical practice for these patients.

Allergic reactions. Patients taking Capoten may experience various allergic reactions, including Quincke's edema. This can happen any time after starting treatment with drug. Application Capoten in such cases should be stopped immediately, and the patient’s allergy symptoms should be relieved. If allergic reactions are limited to swelling of the face and lips, Kapoten can be taken (best in combination with antihistamines). If the swelling affects the tongue, throat or larynx and airway obstruction is possible, the patient is hospitalized and accept measures to eliminate symptoms.

Patients who have had any allergic reactions in the past (even if they are not caused by ACE inhibitors) are at increased risk of allergies with Capoten.

Also, sometimes after taking Capoten, the patient may begin to complain of abdominal pain, nausea, and vomiting. These symptoms can also be caused by an allergy to ACE inhibitors or substances included in Capoten tablets.

Cough. Sometimes, after taking ACE inhibitors, the patient may experience a cough. It continues during the course of treatment with Capoten and stops on its own after its discontinuation.

Liver failure. In rare cases, taking ACE inhibitors, which include Capoten, causes cholestatic jaundice in the patient, which can lead to liver necrosis and even death. Why this happens is still unclear. Therefore, patients undergoing treatment with ACE inhibitors should be closely monitored; if there is a suspicion of the development of jaundice or an increase in the level of liver enzymes is observed, taking Capoten and other ACE inhibitors should be stopped immediately.

Hyperkalemia. The risk of developing hyperkalemia is increased in patients with renal failure, diabetes mellitus, and in those who use potassium-sparing diuretics, regularly take potassium supplements, and eat potassium-containing salt substitutes. Also at risk are patients taking medications that can cause an increase in potassium levels in the blood (for example, heparin). Therefore, when prescribing Capoten, the use of such substances or medications should be stopped, and if this is not possible, it is recommended to constantly monitor the level of potassium in the blood.

Aortic and mitral valve stenosis, obstructive hypertropic cardiomyopathy, cardiogenic shock. In patients with obstruction of the valves and left ventricular outflow tract, ACE inhibitors should be used with caution. If the patient has cardiogenic shock and hemodynamically significant obstruction. Capoten is not prescribed.

Neutropenia or agranulocytosis. Cases of neutropenia or agranulocytosis, thrombocytopenia and anemia have been reported in patients taking ACE inhibitors, including Capoten. If the patient's renal function is normal, neutropenia is rare. Capoten should be used with extreme caution in patients taking immunosuppressive drugs, allopurinol, procainamide; You should be especially careful if the patient has impaired renal function. Some of these patients suffered from serious infections that did not respond to intensive antibiotic therapy.

If the use of Capoten is necessary for such patients, it is recommended that regular white blood cell counts be performed every two weeks for the first three months after starting treatment with Capoten. Patients should be warned to report any signs of infection (eg, sore throat, fever) to their doctor. If the patient is suspected of neutropenia, taking Capoten should be stopped immediately. In most patients, neutrophils are normal after captopril treatment is discontinued.

Proteinuria. If the patient has impaired renal function or is prescribed high doses of ACE inhibitors (more than 150 mg per day), there is a risk of proteinuria. In most cases, it goes away on its own within six months, regardless of whether Capoten was continued or not. In patients with renal failure, urine protein should be assessed regularly before starting treatment and from time to time after stopping it.

Patients who have undergone surgery or are undergoing treatment with anesthetic drugs. Since anesthetic medications have the property of lowering blood pressure, the dosage of Capoten should be calculated taking this factor into account.

Diabetes. During the first month after starting treatment with ACE inhibitors (including Capoten), blood sugar levels should be monitored in patients who have previously taken antidiabetic agents or insulin.

Heart failure. With long-term treatment with Capoten, patients' creatinine levels rise 20% above normal or baseline levels. Less than 5% of patients (usually those with severe renal impairment) required discontinuation of treatment due to a gradual increase in creatinine.

Risk of hypokalemia. If ACE inhibitors are used in combination with a thiazide diuretic, hypokalemia may develop. Therefore, the patient's blood potassium levels should be constantly monitored.

Lactose. Capoten contains lactose, so its use is not recommended for patients with rare metabolic diseases in which there is lactose intolerance.

Double blockade of the RAAS. There is evidence that the simultaneous use of ACE inhibitors (including Capoten) and aliskiren receptor blockers increases the risk of hypotension, hyperkalemia and decreased renal function (including acute renal failure). Therefore, double blockade of the RAAS using these agents is not recommended. If therapy with a double blockade is absolutely necessary, this should only occur with constant special monitoring and monitoring of renal function, blood electrolytes and blood pressure.

Drug overdose

Symptoms of overdose are severe arterial hypotension, shock, stupor, bradycardia, and renal failure. If an overdose of Capoten occurs within half an hour after administration, it can be combated by inducing vomiting, gastric lavage, and taking adsorbents. If the pressure begins to decrease, medical means are used, including the use of a pacemaker. Captopril can also be removed from the body of an adult using hemodialysis.

Interaction of Capoten with other drugs

Potassium-sparing diuretics or potassium supplements. Such diuretics, dietary supplements, or potassium substitutes can cause a significant increase in potassium in the blood. If these drugs must be used because of severe hypokalemia, they should be used with caution and potassium levels should be monitored regularly.

Thiazide or loop diuretics. If the patient was taking thiazide diuretics before starting Capoten therapy, there is a risk of hypotension. Symptoms of low blood pressure can be reduced by stopping thiazide diuretics or reducing the dose of Capoten. When testing the combined action of Capoten with loop diuretics, such as furosemide, no side effects were found.

Other blood pressure lowering agents. The combined use of these drugs with Capoten may increase its hypotensive effects. Treatment with vasodilators should be carried out with caution.

Alpha blockers. If Capoten is taken together with alpha blockers, there is a risk of developing orthostatic hypotension.

Drugs used to treat acute myocardial infarction. Capoten can be used in conjunction with acetylsalicylic acid, thrombolytics and beta blockers in patients with myocardial infarction.

Lithium-containing drugs. There is information about a reversible increase in the concentration of lithium in the blood when taking lithium drugs simultaneously with ACE inhibitors, including Capoten, which can cause poisoning. Taking thiazide diuretics can also increase the level of lithium toxicity. Therefore, it is not recommended to use Capoten with lithium-containing drugs. If this seems necessary to the doctor, it is necessary to carefully monitor the level of lithium in the blood.

Tricyclic antidepressants and antipsychotics. ACE inhibitors, including Capoten, may enhance the effect of these drugs. As a result, postural hypotension may occur.

Immunosuppressive agents, allopurinol, procainamide, cytostatic. Their combined use with Capoten may lead to an increased risk of leukopenia, especially if the recommended dose is exceeded.

Nonsteroidal anti-inflammatory drugs. If these drugs are used with ACE inhibitors, blood potassium levels may increase and kidney function may decrease. Both effects are reversible. In rare cases, acute renal failure may occur, especially in patients whose kidney function is already impaired (for example, the elderly or those suffering from dehydration).

Sympathomimetics. Concomitant use of sympathomimetics with ACE inhibitors may reduce the antihypertensive effect of the latter; Patients should be monitored closely.

Antidiabetic drugs. AFP inhibitors, including Capoten, may enhance the blood sugar-lowering effect when used with insulin and oral diabetic medications. This happens very rarely; in such cases, it may be necessary to reduce the dose of the antidiabetic agent.

Clinical biochemistry. Capoten can cause a false-positive urine test for acetone.

The effect of Kapoten on the ability to drive a car

During the first time after starting to take Capoten, as well as if there is a change in dosage, the patient's ability to drive a car and perform activities requiring a high level of concentration may be reduced. It is recommended to refrain from this type of activity until the patient feels better.

Interaction of Kapoten with alcohol

Depends on the patient's individual reaction.

Terms of sale

On prescription.

Storage conditions

Capoten should be stored at room temperature (from 15° to 25°), away from direct sunlight and at low humidity, out of the reach of children and pets. It is recommended to store the drug in its original packaging to protect it from moisture.

Best before date

Kapoten price

The price of the drug depends on the manufacturer, the pricing policy of the pharmacy and the number of tablets in the package. As a rule, the range is from 160 to 300 rubles.

Kapoten's analogs

Drugs whose main active ingredient is captopril: Captopril, Captopril Sandoz, Captopril-STI.

Other ACE inhibitors that act similarly to captopril (with some differences):

Drugs whose active substance must undergo metabolic transformation in the liver to act (therefore they have a longer-lasting effect compared to Capoten): enalapril, ramipril, perindopril, benazepril, Renitek, trandolapril.

ACE inhibitors combined with diuretics: capozide.

It should be added that although the main effects of ACE inhibitors are similar, they differ in chemical composition and have different routes of elimination, duration of action and therefore different dosages. Therefore, you should not change one medicine from the group of ACE inhibitors to another on your own without first consulting your doctor.