Instructions and indications for the use of the drug carvedilol. Carvedilol-mic Carvedilol single and daily dose

Carvedilol is a drug prescribed for patients with cardiac pathology.

What is the composition and form of release of Carvedilol?

The drug is produced in flat-cylindrical white tablets, they are marked with a risk and a chamfer, the active substance is carvedilol at a dose of 12.5 and 25 milligrams. Auxiliary compounds of the cardiological agent: lactose, polyvidone K25, in addition, crospovidone, sucrose, methylcellulose, and croscarmellose sodium.

Tablets are sealed in contour packs of ten or thirty pieces, which are packed in cardboard boxes. Prescription drug Carvedilol for sale. The shelf life of the drug is three years, after this time it is contraindicated to use it, it must be disposed of.

What is the action of Carvedilol?

The drug Karvedilol blocks alpha one, beta one and beta two adrenoreceptors, normalizes hemodynamic parameters. It has a vasodilating (dilates blood vessels) effect, in addition, antianginal (relieves pain in the heart) and antiarrhythmic effect, as well as an antioxidant effect.

After taking the tablets inside, the active substance carvedilol is almost completely absorbed from the digestive tract. Bioavailability reaches 25%. An hour later, the maximum plasma concentration occurs. Food intake may somewhat slow down the absorption of the active compound, while not affecting bioavailability. Protein binding almost 98%. Excreted with bile.

What are the indications for Carvedilol?

Carvedilol is prescribed for arterial hypertension, with stable angina pectoris, and also as part of a combined treatment for chronic heart failure.

What are the contraindications for Carvedilol?

Among the contraindications are the following conditions:

Heart failure of acute origin and decompensated chronic;
Severe hepatic pathology;
Severe bradycardia;
AV block;
Pregnancy;
With cardiogenic shock;
arterial hypotension;
Hypersensitivity to drug substances;
Breast-feeding;
Until the age of eighteen, no medication is prescribed.

With caution, Carvedilol is prescribed for pheochromocytoma, hypoglycemia, with Prinzmetal's angina, with psoriasis, with depression, thyrotoxicosis, with myasthenia gravis, as well as with occlusive pathology of peripheral vessels.

What is the use and dosage of Carvedilol?

The amount of the drug Carvedilol taken is determined by the attending specialist, according to the identified pathology, the dosing regimen of the drug is determined. With arterial hypertension in the first fourteen days, the initial dose is 12.5 mg, the tablet is taken once a day.

Then the amount of the drug is increased to 25 milligrams, if necessary, then the dose can be increased again after two weeks. With the abolition of the drug Carvedilol, the dosage is reduced gradually over two weeks. Tablets are taken after a meal, washed down with the necessary amount of water.

Overdose from Carvedilol

In case of an overdose of Carvedilol, the instructions for use warn that hypotension, bradycardia will develop, respiratory disorders, heart failure will join, in more severe situations, even cardiac arrest is not excluded.

If a little time has passed immediately after the poisoning, then you can proceed to gastric lavage, for this you should provoke vomiting. Then the patient is given the necessary symptomatic treatment with possible hospitalization in a hospital.

What are the side effects of Carvedilol?

The drug causes the following negative reactions: headache, bradycardia, paresthesias, dizziness, syncopal conditions are possible, muscle weakness, sleep disturbance, orthostatic hypotension, depression, angina pectoris, in addition, dry mouth, AV blockade, nausea, are noted progression of heart failure, as well as abdominal pain.

Other negative effects on the drug: diarrhea, constipation, leukopenia, vomiting, thrombocytopenia, edema, allergic reactions, impaired renal function, flu-like syndrome, decreased tearing, and so on.

special instructions

With caution, Carvedilol is prescribed to persons with bronchospastic syndrome, emphysema, and also with chronic bronchitis. At the beginning of treatment, a sharp decrease in pressure cannot be ruled out, and orthostatic reactions, dizziness up to syncope (fainting) may develop.

During treatment, it is contraindicated to drink alcohol. The drug may reduce the production of tear fluid. It is worth noting that the dose of the drug should be reduced or it should be canceled gradually, otherwise a sharp deterioration in the condition can be provoked.

How to replace Carvedilol, what analogues?

The drug Cardivas, Carvetrend, Carvedilol-Teva, Coriol, Acridilol, Carvedigamma, Carvenal, Carvedilol Stada, Credex, Carvedilol, Carvedilol-OBL, Recardium, Carvedilol Hexal, Talliton, in addition, Bagodilol, Dilatrend, Carvidil, Carvedilol Zentiva, Carvedilol- Pharmaplant, Vedikardol, Carvedilol Obolenskoe, Carvedilol Canon, Carvedilol Sandoz, and Atram are analogues.

Conclusion

A specialist should prescribe cardiological drugs; it is contraindicated to use pills of his own conviction.

Name:

Carvedilol (Carvedilolum)

Pharmacological
action:

Carvedilol - non-selective beta-adrenergic blocker.
It is also a selective alpha receptor blocker.
It has no intrinsic sympathomimetic activity.
Reduces the total precardiac load due to selective blocking of alpha-adrenergic receptors. Due to non-selective blockade of beta-adrenergic receptors, suppression of the renin-angiotensin system of the kidneys (decrease in plasma renin activity), a decrease in blood pressure, heart rate and cardiac output are observed.
By blocking alpha receptors, carvedilol dilates peripheral vessels, thereby reducing vascular resistance.
The combination of vasodilation and blockade of beta receptors is accompanied by the following effects: in patients with coronary heart disease - prevention of myocardial ischemia, pain syndrome; in patients with arterial hypertension - lowering blood pressure; in patients with circulatory failure and left ventricular dysfunction - improved hemodynamics, a decrease in the size of the left ventricle and an increase in the ejection fraction from it.
The drug has no effect on lipid metabolism.

Bioavailability of carvedilol is 25%.
Cmax is observed after ingestion after 60 minutes.
The drug is distinguished by a linear relationship between the concentration in the blood and the dose taken. Bioavailability is independent of food intake.
Carvedilol is a highly lipophilic substance. Approximately 98-99% of it binds to blood proteins.
The half-life is 6-10 hours.
The primary passage through the liver is 60-75%.
The volume of distribution in the body is 2 l / kg.
Plasma clearance - 590 ml / min.
Metabolism of carvedilol passes in the liver due to glucuronidation and oxidation of the phenol ring. After hydroxylation and dimethylation of the aromatic ring, 3 metabolites are formed, which have beta-blocking properties.
At the preclinical stage, it was revealed that the metabolite 4'-hydroxy-phenol has a 13-fold higher activity than carvedilol.

The content of metabolites in the blood is about 10 times less than the concentration of carvedilol.
The other two metabolites (hydroxycarbazole) have pronounced adrenoblocking and antioxidant effects.
The antioxidant effect of metabolites is 30-80 times greater than that of carvedilol. Elimination of the drug is carried out with bile (then - with feces).
A small part in the form is eliminated by the kidneys.
In elderly patients there is a higher concentration of the drug (50% higher). The bioavailability of carvedilol in patients with liver cirrhosis is 4 times greater, and its concentration in the blood is 5 times greater than in healthy individuals.
Some patients with hypertension and renal insufficiency(creatinine clearance less than ≤20 ml / min), there is an increase in the content of the drug in the blood by 40-55% compared with patients with unchanged renal function.

Indications for
application:

Arterial hypertension (in monotherapy and in combination with diuretics);
- chronic heart failure (as part of combination therapy);
- IHD: stable angina.

Mode of application:

Carvedilol is taken inside regardless of food intake.
If the patient has cardiovascular insufficiency, it is recommended to use the drug during meals (to increase absorption, which reduces the risk of developing orthostatic hypotension).
With arterial hypertension
The recommended mode of application is 1-2 r / day.
For adults, the initial dose is 12.5 mg / day for the first 1-2 days.
Maintenance dosage is 25 mg/day. If necessary, you can gradually increase the dosage at intervals of 14 days (not less!) Up to the recommended maximum dose of 50 mg / day.
For elderly patients, the initial recommended dose is 12.5 mg / day (once). This dose is sometimes sufficient for further administration.
With arterial hypertension, the maximum allowable dosage is not more than 50 mg / day.

For stable angina
During the first 1-2 days for adults, the recommended dosage is 25 mg / day, divided into 2 doses.
Maintenance dosage - 50 mg / day (25 mg per dose).
The maximum recommended dose is 100 mg/day (in 2 divided doses).
For elderly patients, the initial recommended dosage is 12.5 mg / day once for the first 1-2 days.
Then transfer the patient to a maintenance dose of 50 mg / day (divided into 2 doses).
This dose is the maximum for patients in this category.

Chronic cardiovascular insufficiency
Carvedilol is indicated as an adjunct to conventional treatment with angiotensin-converting factor inhibitors, diuretics, digitalis and vasodilators.
To take the drug requires a stable condition of the patient over the past 4 weeks before switching to treatment with cardvedilol.
Other important conditions for prescribing the drug are heart rate not more than 50 beats per minute, systolic blood pressure more than 85 mm Hg.
The starting dose is 6.25 mg once a day.
In case of good tolerance, the dose can be gradually increased with an interval of 14 days (at least!) According to the scheme: 6.25 mg 2 times a day - 12.5 mg 2 r / s - 25 mg 2 r / day.
The maximum recommended dose is 50 mg / day (divided into 2 doses) for patients weighing ≤ 85 kg and 100 mg / day (divided into 2 doses) for patients weighing ≥ 85 kg (excluding cases of severe cardiovascular insufficiency).
It is necessary to increase the dosage under close medical supervision.

There may be some worsening of signs of cardiovascular insufficiency at the beginning of therapy (especially in patients who use high doses of diuretics and (or) with severe cardiovascular insufficiency).
In these cases, drug withdrawal is not required, it is only necessary to refrain from increasing the dosage of carvedilol.
During treatment with carvedilol, the general condition of the patient should be monitored by a general practitioner (or cardiologist).
Before increasing the dosage of the drug, an additional examination of the patient is necessary, which includes the determination of hepatic functions, body weight, heart rate, heart rate and blood pressure.

If signs of decompensation develop, fluid retention requires symptomatic therapy (increase in the dosage of diuretics).
In this case, you should refrain from increasing the dosage of carvedilol (at least until the general condition of the patient becomes stable).
Sometimes a reduction in the dose of carvedilol or even a temporary cessation of treatment is required (in these cases, it is possible to titrate the dose of the drug).
If treatment with carvedilol is interrupted o, then it is necessary to start taking the drug again with a minimum dose (6.25 mg once a day), this dose can be gradually increased according to the above rules.
Carvedidol in pediatrics (for patients under 18 years of age) is not prescribed, since there is not enough information about the safety and efficacy of the drug in this age group of people.
It is important to remember that when carvedilol is taken by elderly patients, constant medical supervision is necessary, since these patients are more sensitive to carvedilol.
To cancel the drug a gradual decrease in dose over 7-14 days is necessary.

Side effects:

Hematopoietic system: thrombocytopenia (mild degree).
Metabolism: peripheral edema, hypercholesterolemia, fluid retention, hypervolemia, hyperglycemia. Hyperglycemia is more common in patients with diabetes mellitus.
central nervous system: syncope, sleep disturbances, paresthesia, headache, depression, dizziness.
Organ of vision: visual disturbances, reduced lacrimation, eye irritation.
urinary system: peripheral edema, urination disorder, renal failure.
Gastrointestinal tract: nausea, constipation, dry mouth, abdominal pain, diarrhea, vomiting, elevated transaminases.
reproductive system: swelling of the genitals, impotence.

The cardiovascular system: bradycardia, impaired peripheral circulation, orthostatic hypotension.
Musculoskeletal system: Pain in limbs.
Respiratory system: dryness of the nasal mucosa, shortness of breath (obstructive syndrome) in patients with COPD.
Skin and subcutaneous tissue: urticaria, allergic exanthema, itching, lichen planus-like reaction, psoriasis. If the patient has psoriasis, the skin symptoms may worsen.
Other: swelling at the injection site, general weakness.
Rare: angina pectoris, atrioventricular blockade, exacerbation of signs of peripheral vascular disease (Raynaud's syndrome, intermittent claudication, etc.).
Carvedilol may cause latent diabetes mellitus, worsening of the course of diabetes mellitus, insufficient control over the content of glucose in the blood serum.
When carvedilol is titrated, a decrease in myocardial contractility is possible (rarely).

Contraindications:

Acute and decompensated chronic heart failure requiring intravenous administration of inotropic agents;
- severe liver failure;
- AV block II-III stage;
- severe bradycardia (less than 50 bpm);
- syndrome of weakness of the sinus node;
- arterial hypotension (systolic blood pressure less than 85 mm Hg);
- cardiogenic shock;
- bronchial asthma;
- chronic obstructive pulmonary disease;
- age up to 18 years (efficacy and safety have not been established);
- hypersensitivity to carvedilol or other components of the drug.
Carefully: bronchospastic syndrome, chronic bronchitis, pulmonary emphysema, Prinzmetal's angina, thyrotoxicosis, peripheral vascular occlusive disease, pheochromocytoma, psoriasis, renal failure, AV block I degree, extensive surgery and general anesthesia, diabetes mellitus, hypoglycemia, depression, myasthenia gravis.
Carvedilol Not recommended

Therapy should be long-term and should not be stopped abruptly., especially in patients with coronary heart disease, as this can lead to a worsening of the course of the underlying disease.
If necessary, reducing the dose of the drug should be gradual, over 1-2 weeks.
At the beginning of therapy with carvedilol or with an increase in the dose of the drug in patients, especially the elderly, there may be an excessive decrease in blood pressure, mainly when standing up.
Dose adjustment is required.
In patients with chronic heart failure, when choosing a dose, an increase in symptoms of heart failure and the appearance of edema are possible.
In this case, the dose of carvedilol should not be increased, it is recommended to prescribe large doses of diuretics until the patient's condition stabilizes.
It is recommended to constantly monitor the electrocardiogram and blood pressure while prescribing carvedilol and slow calcium channel blockers, phenylalkylamine derivatives (verapamil) and benzodiazepine (diltiazem), as well as class I antiarrhythmic drugs.

Recommended control kidney function in patients with chronic renal failure, arterial hypotension and chronic heart failure.
In the case of surgery using general anesthesia, the anesthesiologist should be warned about previous therapy with carvedilol.
Carvedilol does not affect the concentration of glucose in the blood and does not cause changes in the glucose tolerance test in patients with non-insulin-dependent diabetes mellitus.
During treatment, avoid the use of ethanol.
Patients with pheochromocytoma should be given alpha-blockers before starting therapy.
Patients wearing contact lenses should be aware that the drug may cause a decrease in lacrimation.
Influence on the ability to drive vehicles and control mechanisms
It is not recommended to drive a car at the beginning of therapy and when increasing the dose of carvedilol. You should refrain from other activities associated with the need for a high concentration of attention and quick psychomotor reactions.

Interaction
other medicinal
by other means:

Calcium antagonists and antiarrhythmics.
Cases of bradycardia and hypotension have been observed while taking carvedilol with amiodarone, diltiazem and/or verapamil.
It is necessary to monitor blood pressure and electrocardiographic study in these patients.
The synergistic effect of carvedilol and calcium antagonists can cause disturbances in atrioventricular conduction of the heart with the development of decompensation.
Careful medical monitoring is required for patients who take class I antiarrhythmic drugs or amiodarone concomitantly with carvedilol.
There are reports of cases of ventricular fibrillation, bradycardia and cardiac arrest at the beginning of carvedilol therapy in patients taking amiodarone.
If an antiarrhythmic drug is administered parenterally, cardiovascular failure may occur (class Ia or class Ic antiarrhythmic drugs).

Cases of bradycardia when the drug is combined with guanethidine, reserpine, methyldopa, guanfacine or monooxygenase inhibitors (except group B monooxygenase inhibitors).
In such cases, monitoring of the heart rate is necessary.
It is not recommended to use carvedilol and dihydropyridines at the same time (risk of severe hypotension, cardiovascular insufficiency).
Nitrates provoke the development of hypotension when combined with carvedilol.
When the drug is combined with digoxin, an increase in the equilibrium concentrations of digoxin and digitoxin is observed (by 16 and 13%, respectively).
If this combination is used, it is necessary to determine the content of digoxin in the blood at the beginning of treatment and at the end of the selection of the maintenance dose.
Carvedilol enhances the antihypertensive effect of drugs of other pharmacological groups(phenothiazines, barbiturates, tricyclic antidepressants, α1 receptor antagonists, alcohol, vasodilators).

When carvedilol is combined with cyclosporine, it is necessary to study the concentration of the latter in the blood, since its content may increase.
Hypoglycemic agents (including insulin).
Carvedilol may reverse signs of hypoglycemia, and antidiabetic agents and insulin may be potentiated by carvedilol, so regular monitoring of serum glucose levels is necessary in these patients.
If the patient is taking clonidine-carvedilol combination, and he needs to cancel both drugs, then carvedilol is first canceled, and then the dosage of clonidine is gradually reduced.
If necessary, inhalation anesthesia should be aware of the negative hypotensive and inotropic interactions of anesthetics with carvedilol.
The effectiveness of carvedilol is reduced when combined with drugs that retain fluid and sodium in the body (anti-inflammatory painkillers, corticosteroids, estrogens).

Patients taking barbiturates, cimetidine, fluoxetine, ketoconazole, haloperidol, erythromycin, verapamil, or rifampicin (drugs that induce or inhibit cytochrome P450 enzymes) should be under medical supervision, as carvedilol concentrations may increase (if inhibitors are used) or decrease (if inductors are used).
The combination with ergotamine has a significant vasoconstrictive effect.
When combined with neuromuscular blockers there is an increase in the blocking of neuromuscular transmission.
The risk of severe bradycardia and hypertension increases with the combination of carvedilol with sympathomimetics (beta-, alpha-agonists).

Pregnancy:

Carvedilol Not recommended during pregnancy and lactation.
In an animal experiment, the teratogenic effect of the drug was not confirmed, however, clinical studies to study the safety of taking this category of patients are not enough.
Carvedilol can reduce placental blood flow, which provokes premature birth or uterine death of the fetus.
Bradycardia, hypoglycemia, pulmonary insufficiency, cardiorespiratory complications and hypothermia may occur when taking carvedilol during pregnancy in a fetus or newborn.
Carvedilol is prescribed during pregnancy only when the expected benefit of the drug outweighs the potential risks to the newborn (fetus).
If carvedilol is taken by a pregnant woman, it should be discontinued 2-3 days before the due date.
If this is not observed, the newborn should be observed for the first 2-3 days of life.
The drug is lipophilic, animal experiments have shown the ability of the molecule and its metabolites to penetrate into breast milk.
If the drug is taken by a nursing woman, breastfeeding is stopped.

Overdose:

Symptoms: Exceeding the dose of carvedilol can provoke bradycardia, severe hypotension, heart failure, loss of consciousness, vomiting, cardiac arrest, respiratory failure, bronchospasm, convulsions and cardiogenic shock.

Treatment: in the treatment it is necessary to monitor the main vital signs.
Patients with an overdose should, if necessary, be in an intensive care unit.
Supportive care: for the prevention of severe bradycardia - atropine 0.5–2 mg intravenously, to support the cardiovascular system: glucagon (first intravenous bolus 1–10 mg, then intravenous infusion 2–5 mg / hour).
Sympathomimetic drugs are prescribed (isoprenaline, dobutamine or epinephrine - the dose depends on the patient's body weight).
With bradycardia refractory to drug therapy - electrical stimulation of the heart.
For the relief of bronchospasm - beta-sympathomimetics in the form of intravenous infusion or inhalation, intravenous aminophylline is also effective.
For the relief of convulsive syndrome - slowly intravenous diazepam.
Since carvedilol is rapidly bound to blood proteins, hemodialysis is ineffective.
In case of severe overdose symptoms, maintenance treatment is carried out for a long time, since the redistribution and elimination of the drug will be slow.
The duration of therapy depends on the patient's condition (until the condition is stable).

Release form:

Carvedillot tablets 6.25 mg, 12.5 mg and 25 mg white to white with a creamy tint, flat-cylindrical, with a chamfer; light marbling is allowed in 10, 20, 30 or 60 pieces.
Tablets Carvedillot Zentiva 6.25 mg, 12.5 mg and 25 mg brownish-yellow color, interspersed, with a risk for dividing on one side and engraved with the number "12" - on the other, 15 or 30 pcs.
Canon Carvedillot Tablets 6.25 mg, 12.5 mg and 25 mg are flat-cylindrical, with a chamfer and a risk, white or almost white, slight marbling is allowed at 7, 10, 14, 20, 21, 28, 30, 35, 40, 50, 56, 60, 70 , 80, 81, 90 or 100 pcs.

Carvedillot Sandoz tablets 3.125 mg, 6.25 mg, 12.5 mg, 25 mg and 50 mg yellow, round, biconvex, scored on both sides and on the sides and marked "C2" on one side.
Carvedillot Stada tablets 12.5 mg and 25 mg pinkish-beige, round, biconvex, with a risk on both sides and on the sides and with the inscription "C3" on one side, 30 pcs.
Carvedillot-Teva tablets 3.125 mg, 6.25 mg, 12.5 mg and 25 mg white or almost white, round, biconvex, engraved with "CA3" on one side, 28 or 30 pcs.

Storage conditions:

Store in a dry, dark place at a temperature not exceeding 25°C.
Keep out of the reach of children.
Shelf life - 2 years.

1 tablet of Carvedilol contains:
- active substance: carvedilol - 12.5 mg;
- Excipients: microcrystalline cellulose, lactose (milk sugar), crospovidone (plasdon XL10), sodium stearyl fumarate.

Carvedilol: instructions for use and reviews

Latin name: Carvedilol

ATX Code: C07AG02

Active substance: carvedilol (carvedilol)

Producer: FP Teva (Israel), Active Component, Ozon LLC, VERTEX (Russia), G. Amphray Laboratories (India), Moechs Catalana S. A. (Spain), Polpharma (Poland)

Description and photo update: 13.08.2019

Carvedilol is an alpha- and beta-blocker without internal sympathomimetic activity with antianginal, vasodilating and antiarrhythmic action.

Release form and composition

Dosage form - tablets: flat-cylindrical, white, with a chamfer and a separating risk (in a blister pack: 10 pcs., 3 packs in a carton pack, 30 pcs., 1 pack in a carton pack).

The active substance is carvedilol, in 1 tablet - 12.5 or 25 mg.

Auxiliary components: sucrose, methylcellulose, polyvidone K25, lactose, crospovidone, croscarmellose sodium.

Pharmacological properties

Pharmacodynamics

Carvedilol is a blocker of alpha 1 -, beta 1 - and beta 2 -adrenergic receptors, which is a racemic mixture of R (+) and S (-) stereoisomers. Each of them is characterized by identical antioxidant and α-adrenergic blocking properties. The beta-adrenergic blocking effect of carvedilol is not selective and is explained by the presence of a levorotatory S (-) stereoisomer in its composition.

Carvedilol does not have its own sympathomimetic activity and has membrane stabilizing properties.

The vasodilating effect is due mainly to the blockade of alpha 1-adrenergic receptors. Thanks to him, there is a decrease in total peripheral vascular resistance (OPSS). Vasodilation, combined with blockade of beta-adrenergic receptors, leads to the fact that in patients with arterial hypertension, blood pressure decreases without an increase in peripheral vascular resistance, and there is no slowdown in peripheral blood flow (unlike beta-blockers). The heart rate decreases slightly. In patients with coronary heart disease, carvedilol has an antianginal effect, and also reduces pre- and afterload on the cardiovascular system and does not have a pronounced effect on the concentration of magnesium, sodium and potassium ions and lipid metabolism in blood plasma.

In patients with heart failure and / or left ventricular dysfunction, carvedilol normalizes the size of the left ventricle, improves ejection fraction and favorably affects hemodynamic parameters. Also, the drug has an antioxidant effect, which consists in the elimination of free oxygen radicals.

Carvedilol reduces the number of cases with a fatal outcome and reduces the frequency of hospitalizations, eliminates unpleasant symptoms and improves the functioning of the left ventricle in patients with chronic heart failure of non-ischemic and ischemic etiology. The therapeutic effects of carvedilol are dose-dependent.

Pharmacokinetics

Carvedilol is rapidly absorbed from the gastrointestinal tract when taken orally. This compound is highly lipophilic. Its maximum blood level is recorded approximately 1 hour after ingestion. The elimination half-life is on average 6-10 hours. Carvedilol binds to plasma proteins by 95-99%. The bioavailability of the drug is 24-28%. The absolute bioavailability of carvedilol reaches approximately 25%: 15% for the S-form and 30% for the R-form. When taking the drug during meals, a significant change in this indicator is not observed.

Most carvedilol is metabolized primarily in the liver via conjugation and oxidation to certain metabolites. The substance is involved in metabolic processes during the "primary passage" through the liver. The metabolism of carvedilol, which is carried out through oxidation, is stereoselective. R(+)-isomer is metabolized mainly by CYP1A2 and CYP2D6 isoenzymes. In the case of the S (-) isomer, the CYP2D9 isoenzyme is predominantly involved in metabolic processes and, to a lesser extent, the CYP2D6 isoenzyme. Also, the metabolism of carvedilol is carried out with the help of other cytochrome P 450 isoenzymes: CYP2C19, CYP2E1 and CYP3A4. Due to hydroxylation and demethylation of the phenol ring, 3 metabolites are formed, characterized by vasodilating properties, which are less pronounced than those of carvedilol itself. Metabolites have a pronounced adrenoblocking and antioxidant effect. Excretion of carvedilol is carried out mainly with bile through the intestines and partly with urine in the form of metabolites.

With kidney dysfunction, the pharmacokinetic parameters of the drug do not change significantly. The pharmacokinetics of carvedilol remains almost the same regardless of the age of the patient (no statistically significant effect of this parameter was found).

In patients with cirrhosis of the liver, the bioavailability of carvedilol is increased by 80% due to a decrease in the intensity of metabolism during the "primary passage" through the liver. In severe liver dysfunction, the use of carvedilol is not recommended.

Carvedilol crosses the placental barrier and is determined in breast milk, and is practically not excreted from the blood plasma during a dialysis session.

Indications for use

• stable angina;
• Chronic heart failure (combination therapy);
• Arterial hypertension.

Contraindications

• Severe bradycardia (heart rate less than 50 beats per minute);
• Sick sinus syndrome (SSS);
• Chronic heart failure in the stage of decompensation;
• Atrioventricular blockade (AV-blockade) II and III degree (except for patients with an artificial pacemaker);
• Acute heart failure;
• Arterial hypotension (systolic blood pressure (BP) below 85 mm Hg);
• Cardiogenic shock;
• severe liver failure;
• Age up to 18 years;
• The period of pregnancy and breastfeeding;
• Hypersensitivity to the components of the drug.

According to the instructions, Carvedilol should be used with caution in AV block I degree, Prinzmetal's angina, peripheral vascular occlusive diseases, thyrotoxicosis, pheochromocytoma, renal failure, psoriasis, bronchospastic syndrome, pulmonary emphysema, chronic bronchitis, general anesthesia during extensive surgical operations, myasthenia gravis , hypoglycemia, diabetes, depression.

Instructions for use Carvedilol: method and dosage

Tablets are taken orally, after meals, with a small amount of water.

The doctor prescribes the dose of the drug individually, taking into account clinical indications.

• Stable angina: initial dose - 12.5 mg 2 times a day. With good tolerance and insufficient efficacy, the first dose increase can be carried out after 7-14 days of therapy by 12.5 mg, the second increase after 14 days without changing the frequency of administration. The daily dose of the drug should be no more than 50 mg and taken 2 times a day;
• Chronic heart failure: initial dose (first 2 weeks) - 3.125 mg 2 times a day. The selection of the dose must be made strictly individually, under the supervision of the attending physician. In patients with good tolerability of Carvedilol, the dose is increased by a factor of 1 every 2 weeks and adjusted to 25 mg 2 times a day for 6 weeks. An increase is recommended to be made up to the maximum tolerated dose by the patient, for patients with a body weight of up to 85 kg, the target daily dose is 50 mg, more than 85 kg - 75-100 mg;
• Arterial hypertension: the first 7-14 days - 12.5 mg per day. The multiplicity of reception can be 1 time (in the morning after breakfast) or 2 times a day, dividing the daily dose in half. Then the daily dose is increased to 25 mg, it should be taken according to the already established scheme. The last dose increase is made after 14 days.

If the drug is interrupted for a period of more than 2 weeks, then treatment should be resumed from the initial dose according to the recommended scheme.

For elderly patients (over 70 years old), the drug is prescribed in a daily dose of not more than 25 mg with a frequency of administration 2 times a day.

Cancellation of the drug is carried out by a gradual (1-2 weeks) reduction in the dose taken.

In case of missing the next dose, the tablet should be taken as soon as remembered, but the dose should not be doubled at the next dose.

Side effects

The use of Carvedilol can cause undesirable effects:

• From the side of the cardiovascular system: angina pectoris, bradycardia, AV blockade, orthostatic hypotension; rarely - progression of heart failure, intermittent claudication, peripheral circulatory disorders;
• From the nervous system: muscle weakness (more often at the beginning of treatment), headache, dizziness, sleep disturbances, syncope, paresthesia, depression;
• From the digestive system: nausea, dry mouth, vomiting, diarrhea or constipation, abdominal pain, increased activity of liver enzymes;
• From the urinary system: edema, severe renal dysfunction;
• From the hemopoietic system: leukopenia, thrombocytopenia;
• Allergic reactions: sneezing, skin reactions (itching, exanthema, rash, urticaria), exacerbation of psoriasis, bronchospasm, nasal congestion, shortness of breath (in predisposed patients);
• Other: pain in the extremities, flu-like syndrome, weight gain, decreased tearing.

Overdose

Symptoms of an overdose of Carvedilol include heart failure, bradycardia, a marked decrease in blood pressure, cardiogenic shock, and cardiac arrest. Vomiting, bronchospasm, respiratory disorders, clouded consciousness and generalized convulsions are sometimes observed. In this case, it is recommended to carry out correction and constant monitoring of vital signs. If necessary, hospitalization in the intensive care unit is required.

It is also acceptable to carry out such activities as the introduction of sympathomimetics [epinephrine (adrenaline), dobutamine] in various doses depending on the body's response to maintenance therapy and body weight, the appointment of atropine intravenously (0.5-2 mg each) with severe symptoms of bradycardia and glucagon (1-10 mg intravenously by bolus, then 2-5 mg every hour as long-term infusion therapy) to maintain the functioning of cardiovascular activity. You can also lay the patient on his back and raise his legs.

If hypotension is the main clinical sign of overdose, norepinephrine (norepinephrine) should be administered. However, continuous monitoring of circulatory characteristics is very important during treatment.

If the resistance of bradycardia to medical procedures is established, the use of an artificial pacemaker is indicated. With bronchospasm, beta-agonists are prescribed in the form of an aerosol (with proven inefficiency, the drug is administered intravenously) or aminophylline intravenously. With convulsions, diazepam should be slowly injected intravenously.

Since in case of a severe overdose, accompanied by a state of shock, prolongation of the half-life of carvedilol and the removal of this substance from the depot are sometimes noted, it is recommended to continue maintenance therapy for a sufficiently long period of time.

special instructions

Do not use the drug to treat patients with low blood pressure.

At the beginning of the application and with increasing doses, orthostatic reactions and a sharp decrease in blood pressure are possible. In patients with heart failure, especially the elderly, when using combination therapy or while taking diuretics, there are severe dizziness up to fainting.

Treatment of patients with coronary heart disease, renal insufficiency, arterial hypotension, peripheral vascular disease, heart failure should be carried out under regular monitoring of renal function, with a deterioration in laboratory parameters, Carvedilol should be discontinued.

In patients with psoriasis, peripheral vascular disease, a history of anaphylactic reactions, the effect of the drug can lead to a worsening of the condition, with Prinzmetal's angina - provoke the appearance of retrosternal pain. The use of the drug reduces sensitivity in allergic tests.

Against the background of taking the drug with caution, it is recommended to carry out general anesthesia with drugs with a negative inotropic effect, such as cyclopropane, ether, trichlorethylene. The patient should inform the doctor about taking Carvedilol. Before planned extensive surgical operations, a gradual withdrawal of the drug should be carried out.

The drug tends to mask the symptoms of hyperglycemia and thyrotoxicosis. Treatment of patients with diabetes mellitus is recommended to be accompanied by regular monitoring of blood glucose levels, if necessary, adjust hypoglycemic therapy.

Special care should be taken when prescribing the drug to patients with severe metabolic acidosis.

Treatment of patients with pheochromocytoma begins with the appointment of alpha-blockers, and then switched to the use of the drug.

During the period of treatment, alcohol is contraindicated.

When discontinuing the combination therapy of carvedilol and clonidine, carvedilol should be phased out first, and only a few days later, a reduction in the dose of clonidine should be started.

At the beginning of treatment and with increasing doses, the drug can cause dizziness and an excessive decrease in blood pressure, therefore, during the period of its use, it is recommended to refrain from all potentially hazardous activities, the implementation of which depends on the high speed of psychomotor reactions and increased attention.

Use during pregnancy and lactation

Information on the use of Carvedilol during pregnancy is currently insufficient. Beta-blockers reduce placental blood flow, adversely affect the development of the embryo and can provoke hypoglycemia, bradycardia and arterial hypotension. There is no sufficient experience in prescribing Carvedilol to pregnant women in clinical practice. Therefore, the drug is contraindicated for use in this category of patients, except in cases of extreme necessity, when the probable benefit of treatment for the mother outweighs the potential risk to the fetus.

Animal experiments have proven that carvedilol and its metabolites pass into breast milk. There are no data on the penetration of these substances into human breast milk, therefore, when prescribing the drug during lactation, breastfeeding should be stopped.

drug interaction

While taking the drug, it is impossible to prescribe intravenous administration of diltiazem and verapamil because of the risk of a strong decrease in blood pressure and a decrease in heart rate.

The action of carvedilol enhances the combination with antianginal, antihypertensive, some antiarrhythmic drugs, anesthetics, other beta-blockers (including in the form of eye drops), cardiac glycosides, monoamine oxidase inhibitors, sympatholytics (reserpine).

With the simultaneous use of Carvedilol:

• Phenobarbital, rifampicin and other inducers of hepatic enzymes can reduce the concentration of carvedilol in the blood plasma;
• Ergot alkaloids impair peripheral circulation;
• Cimetidine and other liver enzyme inhibitors may increase the plasma concentration of carvedilol;
• Digoxin increases its concentration in blood plasma.

The drug can enhance the effect of hypoglycemic agents and mask the development of hypoglycemia.

Analogues

Analogues of Karvedilol are: Atram, Alotendin, Anaprilin, Amlodak-AO, Aodak-AO, Dilatrend, Vedikardol, Karvetrend, Carvidex, Karvedigamma, Karvedilol Obolenskoye, Karvedilol-KV, Carvedilol Geksal, Karvedilol-Lugal, Carvedilol Zentiva, Carvedilol Sandoz, Kardivas, Carvidil, Credex, Coriol, Talliton.

Terms and conditions of storage

Store in a dry, dark place at temperatures up to 25 °C. Keep away from children.

Shelf life - 3 years.

Carvedilol is a B-blocker. But this drug is different from most of the other members of this group, which are most often used to treat cardiovascular diseases.

It blocks, in addition to B2-adrenergic receptors, also B1- and alpha1-adrenergic receptors. Due to this, the drug has additional therapeutic effects, but there are also more adverse reactions because of this.

In this article, we will look at why doctors prescribe Carvedilol, including instructions for use, analogues and prices for this drug in pharmacies. Real REVIEWS of people who have already used Carvedilol can be read in the comments.

Composition and form of release

Carvedilol is available as film-coated tablets of 12.5 mg and 25 mg. They have a flat-cylindrical shape, white. Produced in a blister - 30 tablets.

• The composition of this drug includes carvedilol, which is the active substance, as well as a number of excipients.

Clinical and pharmacological group: beta1-, beta2-blocker. Alpha1-blocker.

Indications for use

What does the drug help? Indications for the appointment of Carvedilol are:

• arterial hypertension (usually together with other medicines for pressure);
• stable angina;
• chronic heart failure (NYHA stage II-III), together with other drugs - diuretics, digoxin or ACE inhibitors.

pharmachologic effect

Carvedilol is a non-selective beta-adrenergic blocker. It is also a selective alpha receptor blocker. It has no intrinsic sympathomimetic activity. Reduces the total precardiac load due to selective blocking of alpha-adrenergic receptors.

Due to non-selective blockade of beta-adrenergic receptors, suppression of the renin-angiotensin system of the kidneys (decrease in plasma renin activity), a decrease in blood pressure, heart rate and cardiac output are observed. By blocking alpha receptors, carvedilol dilates peripheral vessels, thereby reducing vascular resistance.

The combination of vasodilation and blockade of beta receptors is accompanied by the following effects: in patients with coronary heart disease - prevention of myocardial ischemia, pain syndrome; in patients with arterial hypertension - lowering blood pressure; in patients with circulatory failure and left ventricular dysfunction - improved hemodynamics, a decrease in the size of the left ventricle and an increase in the ejection fraction from it. The drug has no effect on lipid metabolism.

Carvedilol is rapidly and extensively absorbed after oral administration with a bioavailability of approximately 25% - 35%. The bioavailability of the active substance is not affected by food intake, but may slow down its absorption. Plasma protein binding is almost absolute 98-99%. Clearance - from 6 to 10 hours. The drug is excreted from the body mainly with bile.

Instructions for use

According to the instructions for use, Carvedilol tablets are taken orally, after meals, with a small amount of water. The doctor prescribes the dose of the drug individually, taking into account clinical indications.

• With arterial hypertension during the first 7-14 days, the recommended initial dose is 12.5 mg / day (1 tab.) In the morning after breakfast. The dose can be divided into 2 doses of 6.25 mg Carvedilol (1/2 tab. 12.5 mg). Further, the drug is prescribed at a dose of 25 mg (1 tab. 25 mg) in 1 dose in the morning, or divided into 2 doses of 12.5 mg (1 tab. 12.5 mg). If necessary, after 14 days it is possible to increase the dose again.
• Stable angina: initial dose - 12.5 mg 2 times a day. With good tolerance and insufficient efficacy, the first dose increase can be carried out after 7-14 days of therapy by 12.5 mg, the second increase after 14 days without changing the frequency of administration. The daily dose of the drug should be no more than 50 mg and taken 2 times a day;
• In chronic heart failure, the dose is selected individually, under the close supervision of a physician. The recommended starting dose is 3.125 mg 2 times / day for 2 weeks. With good tolerance, the dose is increased at intervals of at least 2 weeks to 6.25 mg 2 times / day, then 12.5 mg 2 times / day and then up to 25 mg 2 times / day. The dose should be increased to the maximum that is well tolerated by the patient. In patients weighing less than 85 kg, the target dose is 50 mg/day; in patients weighing over 85 kg, the target dose is 75-100 mg/day. If treatment is interrupted for more than 2 weeks, then its resumption begins with a dose of 3.125 mg 2 times / day, followed by an increase in dose.

In case of missing the next dose, the tablet should be taken as soon as remembered, but the dose should not be doubled at the next dose. If the drug is interrupted for a period of more than 2 weeks, then treatment should be resumed from the initial dose according to the recommended scheme.

• Cancellation of the drug is carried out by a gradual (1-2 weeks) reduction in the dose taken.

For elderly patients (over 70 years old), the drug is prescribed in a daily dose of not more than 25 mg with a frequency of administration 2 times a day.

Contraindications

Contraindications to the use of Carvedilol:

1. Pregnancy;
2. lactation period;
3. Age less than 18 years.
4. Individual intolerance to the components;
5. Bronchial asthma;
6. Renal, liver failure;
7. Decompensated heart failure;
8. Severe bradycardia;
9. Atrioventricular block;
10. Acute cardiac disorders.

According to the instructions, Carvedilol requires careful use in the presence of:

1. Hormonally active tumor of the adrenal glands;
2. kidney problems;
3. Psoriasis;
4. diabetes mellitus;
5. Hyperthyroidism;
6. depressive states;
7. advanced age;
8. Chronic obstructive pneumonia;
9. Damage to the vessels of the lower extremities.

It is impossible to take Carvedilol without a doctor's prescription, and treatment should be carried out under constant monitoring of renal, hepatic parameters, blood sugar and insulin levels.

Side effects

Carvedilol can cause such side effects from organs and systems:

• Nervous system - headache, weakness, dizziness, sleep disturbances, depression, syncope, paresthesia;
• The impact on the cardiovascular system is manifested by a significant decrease in the frequency of heart contractions, a violation in the conduction system of the myocardium (AV blockade), a decrease in pressure, pain in the heart area, angina attacks, an increase in heart failure, an increase in the symptoms of Raynaud's syndrome, a deterioration in blood circulation in the periphery, the appearance edema.
• Hematopoietic system - leukopenia, thrombocytopenia;
• Changes in the digestive system: nausea, sometimes vomiting, frequent loose stools or constipation, dry mouth, abdominal pain, increased blood levels of liver enzymes (transaminases).
• Urinary system - severe impairment of renal function, edema;
• Allergies can be manifested by the occurrence of hives, itching and various rashes.

Other side effects are flu-like syndrome, pain in the extremities, decreased tearing, weight gain.

Analogues Karvedilol

Structural analogues for the active substance:

• Acridilol;
• Bagodilol;
• Vedicardol;
• Dilatrend;
• Karvedigamma;
• Carvenal;
• Carvetrend;
• Carvidil;
• Cardivas;
• Coriol;
• Credex;
• Recardium;
• Talliton.

Attention: the use of analogues must be agreed with the attending physician.

Instructions for use

Attention! The information is provided for informational purposes only. This manual should not be used as a guide to self-medication. The need for appointment, methods and doses of the drug are determined solely by the attending physician.

general characteristics

Compound.

Active substance: carvedilol;

1 tablet contains 12.5 or 25 mg of carvedilol;

Excipients: lactose monohydrate, sucrose, povidone, crospovidone, colloidal anhydrous silicon dioxide, magnesium stearate.

Dosage form. Pills.

Basic physical and chemical properties. Tablets are round, biconvex, scored, white or almost white.

Pharmacotherapeutic group

Drugs affecting the cardiovascular system. Combined blockers (Blockers- drugs that, interacting with receptors, inhibit the action of an agonist) alpha and beta adrenoreceptors. ATC code С07А G02.

Pharmacological properties

Pharmacodynamics.

Antihypertensive, vasodilator, antianginal (Antianginal- drugs that improve blood supply to the myocardium by expanding the coronary arteries) means. Non-selective alpha 1 -, beta 1 - and beta 2 -blocker, without internal sympathomimetic activity. The vasodilating effect is mainly due to blockade (Blockade- slowing down or interruption of the conduction of electrical impulses in any part of the conduction system of the heart or myocardium) alpha 1 -adrenergic receptors. By blocking beta-adrenergic receptors, it reduces the activity of renin- angiotensin (Angiotensin is a peptide hormone produced in human blood. Regulates blood pressure and water-salt metabolism of the body, stimulates the secretion of aldosterone, prostaglandins and other hormones)-aldosterone system, renin activity plasma (Plasma- the liquid part of the blood, which contains formed elements (erythrocytes, leukocytes, platelets). Various diseases (rheumatism, diabetes mellitus, etc.) are diagnosed by changes in the composition of blood plasma. Medicines are prepared from blood plasma at the same time, it decreases without delaying the removal of fluid. Reduces blood pressure, total peripheral vascular resistance, pre- and afterload(or afterload) - the load on the heart caused by resistance to blood flow in the arterial system. Thus, afterload is a pressure load that increases, for example, with arterial hypertension) on the heart, moderately reduces heart rate without affecting renal blood flow and kidney function. The combination of vasodilating action and beta-adrenergic blocking properties contributes to the fact that in patients arterial hypertension (Arterial hypertension- a disease characterized by an increase in blood pressure of more than 140/90 mm Hg. Art.) lowering blood pressure is not accompanied by a simultaneous increase in peripheral vascular resistance, as when taking other beta blockers (Beta blockers- substances that bind to beta-adrenergic receptors and stimulate them. Substances that bind to receptors and have intrinsic activity are called agonists). It has membrane stabilizing properties.

Is powerful antioxidant (Antioxidants- substances that slow down or prevent the oxidation of organic compounds; protect cells from damage caused by free radicals), eliminating free radicals (Radical- a group of atoms, usually unchanged, passing from one compound to another and incapable of long-term existence in a free state \; in chemical formulas is often set off in round or square brackets) oxygen. Does not affect lipid metabolism, in particular the ratio lipoproteins (Lipoproteins- complex proteins, which are a complex of lipids with proteins. They are contained mainly in biological membranes and participate in the transport of substances through them. Determination of the content of lipoproteins in the blood is of diagnostic value) high / low density, and the content of potassium, sodium and magnesium ions in the blood.

The antihypertensive effect develops 2-3 hours after a single dose and lasts for 24 hours. With prolonged treatment, the maximum effect develops after 3-4 weeks. In patients ischemic heart disease (Cardiac ischemia- a chronic pathological process, which is caused by insufficient blood supply to the myocardium. Most cases (97-98%) are the result of atherosclerosis of the coronary arteries of the heart. The main clinical forms are angina pectoris, myocardial infarction and coronarogenic (atherosclerotic) cardiosclerosis) has anti-ischemic and antianginal effect. In patients with dysfunction of the left ventricle (Ventricles- 1) Cavities in the central nervous system: 4 in the brain and 1 in the spinal cord. Filled with cerebrospinal fluid. 2) Departments of the human heart) and / or circulatory insufficiency has a beneficial effect on hemodynamic parameters, increasing the ejection fraction of the left ventricle and reducing its size, reduces the end systolic and end diastolic volumes, as well as peripheral and pulmonary resistance, increases tolerance (Tolerance- decrease in response to repeated administration of a substance, addiction of the body, as a result of which a larger and larger dose is required to achieve the effect inherent in the substance. There is also a distinction between reverse tolerance - a special condition in which a smaller dose is required to achieve a given effect, and cross-tolerance - when taking one substance increases tolerance to taking other substances (usually from the same group or class). Tachyphylaxis is called the rapid (literally after the first use) development of tolerance to taking a medicinal substance. Also, the immunological state of the body, in which it is not able to synthesize antibodies in response to the introduction of a certain antigen while maintaining immune reactivity to other antigens. The problem of tolerance matters in organ and tissue transplantation) to physical activity. Ejection fraction and cardiac index do not change with normal heart function. The effect of carvedilol is more pronounced in patients with tachycardia (Tachycardia- an increase in heart rate to 100 or more beats per minute. Occurs with physical and nervous stress, diseases of the cardiovascular and nervous systems, diseases of the endocrine glands, etc.)(heart rate more than 82 beats / min) and low ejection fraction (less than 23%).

Pharmacokinetics.

Rapidly and almost completely absorbed from the gastrointestinal tract. The maximum concentration in the blood is reached after about 1 hour. Bioavailability (Bioavailability- an indicator of the degree and rate of entry into the blood of a medicinal substance from the total dose administered) is 25% due to the effect of "first pass through the liver" (60-75%). Eating does not affect the bioavailability and the level of maximum concentration, but lengthens the time to reach it. Contacts proteins (Squirrels- natural high-molecular organic compounds. Proteins play an extremely important role: they are the basis of the life process, participate in the construction of cells and tissues, are biocatalysts (enzymes), hormones, respiratory pigments (hemoglobins), protective substances (immunoglobulins), etc.) plasma by 98–99%. Intensively metabolized mainly in the liver due to the connection with glucuronic acid. As a result of demethylation and hydroxylation, three metabolites are formed with a pronounced beta-blocking and antioxidant effect. The volume of distribution is about 2 l / kg and increases with impaired liver function. Passes through the placental barrier, excreted in breast milk. Half-life (Half-life(T1 / 2, a synonym for the half-life) - the period of time during which the concentration of drugs in the blood plasma decreases by 50% of the initial level. Information about this pharmacokinetic indicator is necessary to prevent the creation of a toxic or, conversely, ineffective level (concentration) of drugs in the blood when determining the intervals between injections) carvedilol - 6-10 hours, plasma clearance (Clearance(purification, purification) - a pharmacokinetic parameter that reflects the rate of purification of blood plasma from the drug and is denoted by the symbol C1)- about 590 ml/min. Excreted mainly from bile (Bile- a secret produced by the glandular cells of the liver. Contains water, bile salts, pigments, cholesterol, enzymes. Promotes the breakdown and absorption of fats, enhances peristalsis. The human liver secretes up to 2 liters of bile per day. Preparations of bile and bile acids are used as choleretic agents (allohol, decholine, etc.)), a small part of the dose is excreted as metabolites by the kidneys.

In case of impaired liver function, the volume of distribution increases by 80%. With cirrhosis of the liver, bioavailability increases by 4 times, and the maximum concentration in blood plasma - by 5 times. In elderly patients, the plasma concentration of carvedilol is 50% higher than in young patients. Renal dysfunction is not accompanied cumulation (Cumulation- accumulation of a medicinal substance in the body, usually accompanied by an increase in the effect and often leading to the manifestation of a side or toxic effect) carvedilol. It is practically not excreted during hemodialysis.

Indications for use

Arterial hypertension (as monotherapy and in combination with other antihypertensive agents), stable angina pectoris (angina pectoris- a syndrome caused by myocardial ischemia and characterized by the episodic appearance of a feeling of discomfort or pressure in the precordial region, which in typical cases occur during exercise and disappear after its cessation or administration of nitroglycerin under the tongue (angina pectoris)), chronic (Chronic- a long, ongoing, protracted process, occurring either constantly or with periodic improvements in condition) heart failure (NYHA stages I-III) in combination with diuretics (Diuretics- medicinal substances that increase the excretion of urine by the kidneys and thereby contribute to the removal of excess water and sodium chloride from the body), digoxin and inhibitors (Inhibitors- chemicals that inhibit the activity of enzymes. Used to treat metabolic disorders) angiotensin converting enzyme.

Contraindications

Increased individual sensitivity to the components of the drug, arterial hypotension, decompensated heart failure, severe bradycardia (Bradycardia- a decrease in the number of heartbeats to 60 beats per minute or less (absolute bradycardia) or a lag in the increase in heart rate from an increase in body temperature)(less than 50 beats / min), atrioventricular block (Atrioventricular block- slowing down or interrupting the conduction of electrical impulses through the atrioventricular node) II and III degree (with the exception of patients with an artificial pacemaker), sick sinus syndrome, cardiogenic shock (Cardiogenic shock- one of the most formidable complications in the acute period of myocardial infarction, which is characterized by impaired hemodynamics and vital functions of the body), chronic obstructive pulmonary disease, bronchial asthma, severe liver dysfunction, metabolic acidosis (Acidosis- a shift in the acid-base balance of the body towards an increase in acidity (decrease in pH)). Pregnancy, breastfeeding period, children's age (up to 18 years).

Dosage and administration

Assign adults regardless of the meal. The dose and duration of treatment is determined individually by the doctor depending on the disease, tolerability and effectiveness. therapy (Therapy- 1. The field of medicine that studies internal diseases, one of the oldest and main medical specialties. 2. Part of a word or phrase used to indicate a type of treatment (oxygen therapy\; hemotherapy - treatment with blood products)). In circulatory insufficiency, it is better to take with meals to slow down absorption and reduce the risk of orthostatic reactions. The tablet is swallowed without chewing with a sufficient amount of liquid.

Arterial hypertension. The initial dose is usually 12.5 mg 1 time per day for the first 2 days (the dose can be divided into two doses of 6.25 mg), which may already provide the desired effect. If necessary, the dose can be increased after 2 days to 25 mg 1 time per day, then at intervals of at least two weeks to 50 mg per day, once or in 2 doses (morning and evening, 25 mg). The maximum daily dose is 50 mg.

Angina. The initial dose is usually 12.5 mg 2 times a day for the first 2 days, then 25 mg 2 times a day (morning and evening). If necessary, the dose can be increased at intervals of at least two weeks up to a maximum daily dose of 100 mg divided into 2 divided doses. For elderly patients, the maximum daily dose is 50 mg, divided into 2 doses.

Chronic heart failure. The dose is selected individually, carefully monitoring the patient's condition. The patient should be under constant observation in the first 2-3 hours after the first dose of the drug and after taking an increased dose. Doses of digoxin, diuretics and angiotensin-converting inhibitors enzymes (Enzymes- specific proteins that can significantly accelerate chemical reactions occurring in the body, without being part of the final reaction products, i.e. are biological catalysts. Each type of enzyme catalyzes the transformation of certain substances (substrates), sometimes only a single substance in a single direction. Therefore, numerous biochemical reactions in cells are carried out by a huge number of different enzymes. Enzyme preparations are widely used in medicine) should be fixed prior to prescribing the drug. The recommended starting dose is usually 6.25 mg once daily. With good tolerance and the need to increase the dose, it is increased at intervals of at least two weeks to 6.25 mg twice a day, then to 12.5 mg twice a day, after which to 25 mg twice a day. For patients weighing less than 85 kg, the maximum daily dose is 50 mg in two divided doses, for patients weighing more than 85 kg - 100 mg in two divided doses.

Application features

With caution and under the supervision of a physician (especially at the beginning of treatment and with each dose increase), the drug should be used in the elderly, with diabetes mellitus (masks the clinical manifestations of hyperglycemia) and hypoglycemia (hypoglycemia- a condition caused by low plasma glucose levels. It is characterized by signs of increased sympathetic activity and the release of adrenaline (sweating, anxiety, tremor, palpitations, hunger) and symptoms from the central nervous system (fainting, blurred vision, convulsions, coma)), thyrotoxicosis (Thyrotoxicosis- a syndrome caused by the action of an excess of thyroxine and triiodothyronine on target tissues. There are many reasons for thyrotoxicosis; the most common cause is diffuse toxic goiter (Graves' disease). The clinical picture includes the action of hormones on different organs. Symptoms of activation of the sympathoadrenal system are characteristic: tachycardia, tremor, sweating, anxiety. These symptoms are eliminated by beta-blockers), occlusive diseases of peripheral vessels, atrioventricular block I degree, chronic obstructive pulmonary disease, Prinzmetal's vasospastic angina (may provoke seizures), psoriasis (Psoriasis- a chronic hereditary skin disease with diverse clinical manifestations. The most common common psoriasis is abundantly scaly papules and plaques on the scalp, elbows, forearms, hands, shins, feet, lower back, buttocks. Complaints of itching. In this disease, keratinocytes are formed 28 times more than normal), impaired renal function, depression (Depression- mental disorder: dreary, depressed mood with pessimism, monotony of ideas, decreased urges, inhibition of movements, various somatic disorders), myasthenia gravis (myasthenia gravis- chronic neuromuscular disease associated with impaired neuromuscular conduction. Characterized by weakness, painful fatigue of striated muscles), in patients with pheochromocytoma (only in combination with alpha-blockers), with extensive surgical interventions and general anesthesia (Anesthesia- lack of sensitivity, as well as against the background of treatment with alpha-blockers, alpha-agonists, digitalis preparations, diuretics and / or inhibitors monoamine oxidase (Monoamine oxidase an enzyme that catabolizes monoamines. In these cases, treatment should be initiated at low doses followed by a slow increase to effective doses. At the beginning of treatment or with an increase in the dose of the drug in patients, especially in the elderly, there may be an excessive decrease in blood pressure, especially when standing up, which requires dose adjustment.

Patients with heart failure are advised to take the drug with meals to prevent orthostatic hypotension (orthostatic hypotension- a sharp drop in blood pressure when moving to a vertical position, cause medicinal substances that disrupt autonomic reflex mechanisms or cause hypovolemia). When these patients develop edema (Edema- swelling of tissues as a result of a pathological increase in the volume of interstitial fluid) and / or an increase in symptoms of heart failure, the dose of diuretics should be increased and, if necessary, the dose of carvedilol should be reduced until the patient's condition stabilizes. If the heart rate drops to 55 beats / min, the drug should be discontinued.

When prescribing to patients with circulatory failure, low blood pressure (systolic blood pressure less than 100 mm Hg), coronary heart disease and / or renal failure, it is necessary to monitor kidney function, if it worsens, reduce the dose or stop the drug and increase the dose of diuretics.

In patients with chronic obstructive pulmonary disease with a bronchospastic component who are not receiving anti-asthma drugs, carvedilol should be prescribed only if the benefit of its use outweighs the potential risk. In persons with severe allergies or who are undergoing desensitization, carvedilol may exacerbate allergic reactions. Patients who have experienced or worsened psoriasis during treatment with beta-blockers should only be given the drug after a careful assessment of the possible benefits and risks. Like other beta-blockers, carvedilol can reduce the severity of thyrotoxicosis. In the case of surgery using general anesthesia, the anesthesiologist should be warned about previous therapy with carvedilol. Patients with pheochromocytoma should be given alpha-blockers before starting therapy. Persons using contact lenses should be warned about the possibility of reduced tearing. During treatment, the use of ethanol should be avoided.

If it is necessary to simultaneously prescribe blockers of "slow" calcium channels - derivatives of phenylalkylamine (verapamil) and benzothiazepine (diltiazem), as well as class I antiarrhythmic drugs (amiodarone), constant monitoring is recommended. ECG (ECG- a method for studying the heart muscle by recording the bioelectric potentials of the working heart. A waveform recorded on a moving paper tape or photographic film is called an electrocardiogram (ECG). Plays an important role in the diagnosis of many heart diseases) and blood pressure.

When canceling simultaneous therapy with clonidine, you should first stop treatment with carvedilol, then, after a few days, cancel clonidine. Carvedilol does not affect concentration glucose (Glucose- grape sugar, a carbohydrate from the group of monosaccharides. One of the key metabolic products that provides energy to living cells) in the blood and does not cause changes in the glucose tolerance test in patients with non-insulin-dependent diabetes mellitus.

Therapy should be carried out for a long time and should not be abruptly discontinued, especially in patients with coronary heart disease due to the possibility of worsening the course of the underlying disease. It is recommended to reduce the dose by half every 3 days for 1-2 weeks. If treatment is interrupted for 2 weeks or more, treatment should be resumed with minimal doses.

Carvedilol should not be taken with alcohol.

Use during pregnancy or lactation.

The drug is contraindicated in pregnancy. If necessary, use during the period lactation (Lactation- secretion of milk by the mammary gland breastfeeding should be stopped.

Children.

The drug is contraindicated in children under the age of 18 years.

The ability to influence the reaction rate when driving vehicles or working with other mechanisms.

During the period of treatment, one should refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.

Side effect

The drug is usually well tolerated. Rarely can be observed:

From the side of the cardiovascular system: bradycardia, orthostatic hypotension, angina pectoris, atrioventricular blockade, progression of circulatory failure (cold extremities), progression of heart failure, edema of the lower extremities.

From the side of the central and peripheral nervous system: headache, dizziness, weakness, muscle weakness (usually at the beginning of treatment), depression, sleep disorders, paresthesia.

From the digestive system: dry mouth, nausea, abdominal pain, diarrhea (Diarrhea- rapid release of liquid stools associated with the accelerated passage of intestinal contents due to increased peristalsis, impaired absorption of water in the large intestine and the release of a significant amount of inflammatory secretion by the intestinal wall) or constipation, elevated liver transaminases.

From the side of metabolism: hyperglycemia, weight gain, hypercholesterolemia.

From the hematopoietic system: thrombocytopenia (Thrombocytopenia- decrease in the number of platelets), leukopenia.

From the respiratory system:dyspnea (Dyspnea- violation of the frequency, rhythm and depth of breathing, accompanied by a feeling of lack of air), bronchospastic reactions in predisposed patients.

Allergic reactions: exanthema, itching (Itching- a modified feeling of pain due to irritation of the nerve endings of pain receptors), skin rashes, the appearance and / or exacerbation of psoriasis, sneezing, nasal congestion; very rarely - anaphylactoid reaction.

Others: very rarely - exacerbation of the syndrome of "intermittent" claudication, Raynaud's syndrome, pain in the extremities, impaired urination and / or kidney function, flu-like syndrome, decreased tear secretion, manifestation of latent current diabetes mellitus or an increase in its symptoms.

Interaction with other drugs

Carvedilol should not be used if the patient is receiving intravenous injections of verapamil, diltiazem, antiarrhythmic drugs (especially class 1). Potentiation (Potentiation(synonymous with supraadditive synergism) - a type of synergy in which the final pharmacological effect of a combination of drugs quantitatively significantly exceeds the sum of the individual effects of all components of the combination. The implementation of potentiation is carried out due to different mechanisms, as well as the localization of the action of the components of the combination) effect is observed when taken simultaneously with antihypertensive agents, nitrates and antiarrhythmic drugs. Drugs that reduce the content catecholamines (Catecholamines- natural catecholamines (adrenaline, norepinephrine, dopamine) - mediators of the nervous system. Participate in the metabolism and adaptive reactions of the body. With physical and mental stress (stress), some diseases, the content of catecholamines in the blood and urine increases sharply)(reserpine, monoamine oxidase inhibitors), and clonidine increase the risk of arterial hypotension and bradycardia. Microsomal oxidation inhibitors (cimetidine) enhance, and inductors (Inductor- chemicals that stimulate one's own metabolism or the metabolism of other compounds (drugs) upon repeated administration)(phenobarbital, rifampicin) - weaken the effects of carvedilol. Simultaneous use with ergot alkaloids impairs peripheral circulation. When used with cardiac glycosides (Glycosides- organic substances, the molecules of which consist of a carbohydrate and a non-carbohydrate component (aglycone). Widely distributed in plants, where they can be a form of transport and storage of various substances)(digoxin), verapamil and diltiazem, atrioventricular conduction disturbances are possible, rarely with hemodynamic disturbances. Carvedilol increases the content of digoxin and cyclosporine in the blood, which requires adjustment of their doses. Are common anesthetics (Anesthetics- drugs that have an anesthetic effect are divided into local and general) amplify the negative inotropic (Inotropic- changes the force of heart contraction) and hypotensive effects of carvedilol. Carvedilol may potentiate the action of insulin and oral (oral- the route of administration of the drug through the mouth (per os)) hypoglycemic agents (Hypoglycemic agents medicines that lower blood sugar are used to treat diabetes, masking the symptoms of hypoglycemia (especially tachycardia), which requires regular monitoring of blood glucose levels.

Overdose

Symptoms: severe arterial hypotension (systolic pressure of 80 mm Hg and below), bradycardia (less than 50 bpm), cardiogenic shock (Shock- a condition characterized by a sharp decrease in blood flow in the organs (regional blood flow); is a consequence of hypovolemia, sepsis, heart failure or decreased sympathetic tone. The cause of shock is a decrease in the effective volume of circulating blood (the ratio of bcc to the capacity of the vascular bed) or a deterioration in the pumping function of the heart. The shock clinic is determined by a decrease in blood flow in vital organs: the brain (consciousness and breathing disappear), kidneys (diuresis disappears), heart (myocardial hypoxia). Hypovolemic shock is caused by loss of blood or plasma. Septic shock complicates the course of sepsis: the waste products of microorganisms that have entered the blood cause dilation of blood vessels and increase capillary permeability. Clinically manifested as hypovolemic shock with signs of infection. Hemodynamics in septic shock is constantly changing. To restore the BCC, infusion therapy is needed. Cardiogenic shock develops due to a deterioration in the pumping function of the heart. Use drugs that enhance myocardial contractility: dopamine, norepinephrine, dobutamine, epinephrine, isoprenaline. Neurogenic shock - a decrease in the effective volume of circulating blood due to the loss of sympathetic tone and the expansion of arteries and venules with the deposition of blood in the veins; develops with spinal cord injuries and as a complication of spinal anesthesia), impaired respiratory function (bronchospasm), circulatory failure, convulsions, cardiac arrest.

Treatment: during the first hours - induction of vomiting and gastric lavage, then - control and correction of vital signs in the intensive care unit. Maintenance therapy: with severe bradycardia - atropine 0.5-2 mg intravenously; to maintain cardiac activity - glucagon 1-5 mg (maximum dose - 10 mg) intravenously by stream, then 2-5 mg / hour as infusions (Infusion(in / in the introduction) - the introduction of liquids, drugs or blood products / components into a venous vessel) and / or adrenomimetics (orciprenaline, isoprenaline) 0.5–1 mg intravenously. With the predominance of peripheral vasodilating action, prescribe norepinephrine (Norepinephrine- a compound from the group of catecholamines, a neurohormone. It is formed in the adrenal medulla and in the nervous system, where it serves as a mediator (transmitter) for conducting a nerve impulse through the synapse. Increases blood pressure, stimulates carbohydrate metabolism, etc.) in repeated doses of 5-10 micrograms or as an infusion of 5 micrograms / min. For relief of bronchospasm, beta 2-adrenomimetics are used in the form of an aerosol, with inefficiency - intravenously or aminophylline intravenously. With convulsions - diazepam or clonazepam intravenously slowly. In severe cases intoxication (Intoxication- poisoning of the body with toxic substances) in cardiogenic shock, maintenance therapy is continued long enough until the patient's condition stabilizes and taking into account the half-life of carvedilol.

Product General Information

Best before date. 2 years.

Storage conditions. Store in original packaging at a temperature not exceeding 25 °C. Keep out of the reach of children!

Package. 10 tablets in a blister; 3 blisters in a pack.

Manufacturer.Public Joint Stock Company "Kyiv Vitamin Plant".

Location. 04073, Ukraine, Kiev, st. Kopylovskaya, 38.

Website. www.vitamin.com.ua

Preparations with the same active ingredient

• Corvasan - "Arterium"

This material is presented in free form on the basis of the official instructions for the medical use of the drug.