Instructions for the use of Captopril, description and prices of analogues

Chemical structure and class of the drug

Captopril (Captoprilum) belongs to the group of angiotensin-converting enzyme inhibitors. The name according to the systematic international nomenclature is (S) -1- (3-Mercapto-2-methyl-1-oxopropyl) -L-proline. The registration code of the drug in the anatomical and therapeutic classification is С09АА01.

Release form and dosage

The drug Captopril is available in the form of tablets containing 0.025 g of active ingredient, as well as a number of additional ingredients:

• lactose;
• povidone;
• calcium stearate;
• potato starch;
• colloidal silicon dioxide.

Tablets are packed in blisters of 20 pieces.

How the drug works, is absorbed and excreted

Captopril is the first synthetically produced angiotensin-converting enzyme inhibitor. It has a versatile effect:

• reduces the tone of the renal glomerular efferent arterioles, thereby improving hemodynamics inside the glomeruli, and also reducing the risk of developing diabetic nephropathy;
• reduces the degree of hypertrophy of the muscle layer of the wall of the left ventricle, thereby restraining the development of heart failure;
• acts as a vasodilator, reducing preload, afterload and pressure in the vessels of the lungs;
• under its influence, the minute volume of blood circulation and tolerance to stress increases;
• blocks the conversion of the first form of angiotensin into the second;
• protects the left ventricle from dilatation.

When taken internally, Captopril tablets completely dissolve, the released active substance is rapidly absorbed in the gastric tract by 75% or more. The presence of food in the stomach reduces the bioavailability of the drug by more than a third.

The maximum content of the active substance in the blood plasma is observed 30 to 90 minutes after taking the pill. 25 - 30% Captopril enters into chemical bonds with proteins, more often albumin. He is able to pass the placenta and all histohematogenous barriers, including the BBB.

The active substance is decomposed in hepatocytes. The metabolic products remaining after this, as well as unchanged captopril (up to half of the administered dose), are excreted mainly through the kidneys. The half-life is less than 3 hours, but can be significantly increased in patients suffering from renal failure. During the day, the body leaves 95% of the administered drug.

The most noticeable result in the form of a drop in high blood pressure is observed after one to one and a half hours after taking Captopril inside. The duration of the therapeutic effect depends on the dosage. The most stable decrease in pressure is observed after several weeks of regular intake of the drug.

Indications for use

There are the following indications for the use of Captopril:

• myocardial infarction;
• arterial hypertension;
• heart failure;
• nephropathy associated with type I diabetes mellitus with macroproteinuria.

With regard to heart failure, the use of Captopril produces a positive effect in patients with its chronic form, which developed against the background of a reduced contractile function of the ventricles. The drug is used both in monotherapy and in combination with diuretics, β-blockers and digitalis drugs.

With myocardial infarction, Captopril can be prescribed on the first day of the disease in order to prevent symptomatic circulatory failure. The target group is stable patients with asymptomatic left ventricular dysfunction with an ejection fraction of less than or equal to 40%. The duration of the drug intake is 28 days.

Contraindications

Taking Captopril is unacceptable for the following pathological conditions:

• hypersensitivity to any components that make up the drug, as well as other ACE inhibitors;
• a history of idiopathic or hereditary angioedema after taking any ACE inhibitors;
• hemodynamically significant stenosis of the arteries of both kidneys or the only one;
• glucose-galactose malabsorption syndrome;
• intolerance to galactose;
• lack of lactase;
• porphyria.

The presence of contraindications when taking the drug by pregnant, lactating or women planning to conceive is discussed in the next section.

Pregnancy and breastfeeding

Pregnancy, planning it and breastfeeding the baby are absolute contraindications for prescribing the drug. If women who take Captopril with pressure or other pathologies confirm pregnancy during the course of therapy with this drug, then it should be immediately canceled and replaced with a safe medication.

Side Effects, Overdose and Treatment

It is very important to know how to take Captopril safely so as not to harm yourself. After all, this drug is characterized by numerous side effects from various body systems. In rare cases, death is possible.

Disorders of the cardiovascular system are manifested:

• tides;
• pain in the heart;
• Raynaud's syndrome;
• cardiac arrest;
• pallor of the face;
• cardiogenic shock;
• excessive drop in blood pressure;
• tachycardia: both with maintaining the correct rhythm, and with its violation.

Respiratory manifestations are characteristic:

• rhinitis;
• dyspnea;
• bronchospasm;
• allergic alveolitis;
• eosinophilic pneumonia;
• unproductive dry chest cough that goes away spontaneously a few weeks after you stop taking Captopril.

The digestive tract also does not stand aside:

• vomit;
• diarrhea;
• constipation;
• nausea;
• pancreatitis;
• dry mouth;
• peptic ulcer;
• epigastric pain;
• aphthous stomatitis;
• irritated stomach;
• inflammation of the mucous membrane of the tongue.

The harmful effect on the hepatobiliary system is manifested:

• cholestasis up to jaundice;
• disorder of liver function;
• an increase in the content of bilirubin, biliverdin;
• inflammation of the liver, up to necrotizing hepatitis.

The consequences of treatment with Captopril for the nervous system can be:

• ataxia;
• drowsiness;
• headache;
• loss of consciousness;
• dizziness;
• sensitivity disorders;
• disorders of the taste buds.

The lymphatic and hematopoietic systems are also at gunpoint. The following disorders of their work can be observed:

• neutropenia;
• eosinophilia;
• agranulocytosis;
• lymphadenopathy;
• aplastic anemia;
• hemolytic anemia;
• a drop in platelet production;
• a general decrease in the number of leukocytes;
• in patients suffering from renal pathologies - pancytopenia.

Captopril can negatively affect the immune system, causing autoimmune lesions and / or the appearance of antinuclear antibodies.

The detrimental effect on metabolism is the development of acidosis, anorexia and a drop in blood sugar.

Mental disorders are expressed in depressive states, sleep disorders and confusion.

Eye problems, manifested by blurred vision, may develop.

Side effects on the skin and subcutaneous fat are manifested by the following pathologies:

• itching;
• alopecia;
• dermatitis;
• rashes;
• erythroderma;
• photosensitivity;
• polymorphic erythema;
• pemphigoid reactions;
• angioedema;
• Stevens-Johnson syndrome.

Connective tissue and the musculoskeletal system can respond with joint and muscle pain. Urinary tract - nephrotic syndrome, kidney dysfunction, up to failure, a significant increase or, conversely, a decrease in the daily volume of urine, increased frequency of urination. Reproductive system - gynecomastia and impotence.

General manifestations can also be observed: weakness, fever, fatigue, chest pain.

There may be a change in laboratory parameters:

• growth of ESR;
• leukopenia;
• hyponatremia;
• thrombocytopenia;
• the appearance of protein in the urine;
• an increase in the content of urea;
• drop in hemoglobin and hematocrit;
• an increase in the content of potassium in the blood plasma;
• an increase in the content of liver pigments in plasma.

There may be a pseudopositive reaction to acetone on urinalysis.

In patients of the Negroid race, the usual dosage of Captopril, like other ACE inhibitors, does not bring a pronounced therapeutic effect.

If the drug is prescribed to children, then they should be under constant medical supervision during the entire treatment period due to insufficient knowledge of its safety for this category of patients.

As for driving vehicles and working with dangerous mechanisms, reviews about Captopril indicate a worsening reaction at the beginning of taking the drug, when changing its dosage, and also in the case of drinking alcohol during therapy.

An overdose of a drug is manifested by the following symptoms:

• stupor;
• kidney failure;
• imbalance of electrolytes;
• a decrease in the frequency of heart contractions;
• a pronounced drop in blood pressure, up to shock.

If a person has swallowed an excessive amount of Captopril or its analogue, then it is necessary to provide him with first aid as soon as possible in order to prevent the development of health-threatening and life-threatening complications. You should start with gastric lavage. Then, no later than half an hour after Captopril has entered the body, the instruction requires you to take sodium sulfate and activated carbon or other sorbents.

In the presence of bradycardia and too powerful vagal reactions, atropine is used. In severe cases, it may be necessary to connect a pacemaker.

The most effective way to remove the drug is hemodialysis.

Methods and conditions of use

Both the drug itself and the analogues of Captopril are intended for internal administration, regardless of food intake. However, it should be remembered that the presence of food in the stomach makes the medicine weaker by about a third. The drug is taken regularly, every day, at the same time.

If a dose is missed, it should be taken as early as possible. And if there are several hours left until the next intake, then you should not make up for lost time, it is better to wait and drink the next dose.

As an emergency, it is practiced to dissolve the pill under the tongue.

Arterial hypertension

Long-term therapy of arterial hypertension with the original drug or its substitute should be started by taking 0.0125 - 0.025 g twice a day. After 14 - 28 days, it is recommended to titrate the dose, focusing on the current blood pressure readings. As a rule, we are talking about switching to receiving 0.01 - 0.015 g twice a day.

The drug is prescribed in monotherapy or in combination with other drugs to lower blood pressure, including diuretics. A special regimen of taking Captopril - once a day - is indicated when this drug is combined with thiazide diuretics.

If the patient has an increased activity of the renin-angiotensin-aldosterone system, expressed in arterial hypertension of a renovascular nature, hypovolemia and circulatory failure in the stage of decompensation, treatment according to modern methods begins with the intake of 0.00625 - 0.0125 g of Captopril once a day. Gradually, the patient is transferred under the supervision of a doctor for a two-time appointment. If necessary, the doctor can increase the daily dose to 0.05 - 0.1 g once or twice divided.

Heart failure

For this pathology, the recommended dose of Captopril or its substitute at the beginning of treatment is from 0.00625 to 0.0125 g, divided into 2 - 3 doses per day. In the future, the attending physician titrates the dose to a maintenance level - from 0.075 to 0.150 g per day. This is done with constant monitoring of the patient's response to therapy. The dosage is increased gradually, no more than once every 2 weeks.

Myocardial infarction

With this pathology, two types of treatment are used: short-term and long-term.

Short-term therapy

In order for Captopril to help patients with a heart attack, it should be prescribed no later than within a day from the onset of the disease.

The treatment regimen is shown in the following table:

At the end of the course of treatment, the doctor assesses the patient's condition and decides on further tactics.

Long-term therapy

If, for any reason, treatment with Captopril or similar drugs was not prescribed on the first day, then the next optimal time to start it is considered the interval between III and XVI days of the disease, subject to stable hemodynamics and treatment of residual manifestations of ischemia.

Treatment is carried out in a hospital with constant medical supervision, including the level of blood pressure, until the dose reaches 0.075 g per day.

The starting dose is set at a fairly low level, especially in patients with low or normal blood pressure - 0.00625 g, then a switch to 0.0125 g three times a day follows, then - 0.025 g also 3 times a day. This rate of increase is maintained provided that there are no side effects.

In order for pharmacological cardioprotection to become truly effective in the long-term treatment of myocardial infarction, the dose of Captopril should be from 0.075 to 0.150 g per day, divided into two or three doses.

If the patient has symptomatic hypotension or heart failure, then in order to achieve such dosages of the drug, it is possible to reduce the intake of other vasodilators and / or diuretics.

Captopril in the treatment of myocardial infarction can be combined with thrombolytics, aspirin and β-blockers.

Diabetic nephropathy

With the development of this pathology in patients suffering from type I diabetes mellitus, doctors recommend taking Captopril at 0.075 - 0.100 g per day in two doses. If necessary, it is supplemented with other prescription drugs to lower blood pressure.

Patients with impaired renal function

Since the excretion of the drug occurs through the kidneys, then with their functional disorders, you can act in two ways:

• reduce the dosage of the drug;
• to increase the time interval from one reception to another.

In order for Captopril not to accumulate in the body, its dosage should be selected based on the following table:

If you need to carry out therapy with diuretics, it is better to prescribe loop, rather than thiazide diuretics.

Children

Unfortunately, for this category of patients, not enough studies have been carried out to find out how safe and effective Captopril is, therefore this drug is used in children strictly under medical supervision.

Treatment should be started with a dosage of 0.3 mg / kg of the child's weight and 0.15 g / kg for patients in special groups:

• babies;
• newborns;
• premature newborns;
• children suffering from kidney failure.

As a rule, for children, the daily dose is divided into three doses with an individual selection of the interval between them, based on the effect of the drug.

Aged people

Old people often suffer from functional disorders of the excretory and other systems of the body, therefore, treatment begins with 0.00625 g twice a day. Dose titration is performed based on the dynamics of blood pressure. The goal is to select the minimum dosage that will achieve a persistent hypotensive effect. And due to the extremely low level of income of citizens of retirement age, the price of Captopril is also important, because small doses also mean low costs for buying a medicine in a pharmacy.

Captopril preparations

Since Captopril has established itself as a reliable, relatively inexpensive and effective drug, it is not surprising that its production was opened in almost all corners of the world and under various brands. Most popular generics:

1. Kapoten
2. Captopril Sandoz.
3. Captopril STI.
4. Captopril Akos.
5. Captopril FPO.

According to the reviews of patients and medical personnel, Captopril Sandoz from the pharmaceutical company Sandoz d.d., Slovenia is recognized as one of the most effective generics. According to studies carried out by the authoritative organization Doctors of the Russian Federation, this drug received an overall rating of 8.5 out of 10 possible, its effectiveness was rated at 4.5 out of 5, and safety - 4 out of 5.

The release form and packaging of Captopril Sandoz are shown in the following table:

The next generic product of Captopril is Capoten, a drug from the Russian manufacturer, the chemical and pharmaceutical plant AKRIKHIN JSC.

According to research by the Doctors of the Russian Federation, this drug received an overall rating of 8.15 out of 10 possible, its effectiveness was rated at 4.38 out of 5, and safety - at 3.77 out of 5.

Packaging and cost of Kapoten are shown in the table:

Another popular generic is Captopril STI from the Russian pharmaceutical company AVVA-RUS OJSC (Russia). A distinctive feature of the drug is the doubled concentration of the active substance in each tablet. This fact should be taken into account when purchasing Captopril STI.

Forms of drug release and prices are shown in the table:

The next generic Captopril is Captopril AKOS. It is produced at the Russian pharmaceutical company Sintez. The nomenclature of drug release forms includes tablets of two types, containing 0.025 and 0.050 g each.

As for the packaging of the drug and prices for it, information about this is indicated in the following table:

Generic Captopril FPO is produced by the Russian pharmaceutical company CJSC FP Obolenskoye. The drug is available in the form of tablets with 0.025 g of active ingredient, packaged in contoured cell packs of 10 pieces, nested in cardboard boxes of four. Their cost in pharmacies is 139.99 rubles.