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

Carvedilol is a drug prescribed to patients with cardiac pathology.

What is the composition and release form of Carvedilol?

The medicine is produced in flat-cylindrical white tablets, they are scored and chamfered, the active substance is carvedilol in a dose of 12.5 and 25 milligrams. Auxiliary compounds of the cardiac drug: lactose, polyvidone K25, in addition, crospovidone, sucrose, methylcellulose, and croscarmellose sodium.

The tablets are sealed in contour packs of ten or thirty pieces, which are packed in cardboard packs. The medicine Carvedilol is sold by prescription. The shelf life of the medicine is three years, after this time it is contraindicated to use it and must be disposed of.

What is the effect of Carvedilol?

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

After taking the tablets orally, the active substance carvedilol is almost completely absorbed from the digestive tract. Bioavailability reaches 25%. After an hour, maximum plasma concentration occurs. Eating may slightly slow down the absorption of the active compound without affecting bioavailability. Protein binding is almost 98%. Excreted in bile.

What are the indications for use of Carvedilol?

The drug Carvedilol is prescribed for arterial hypertension, stable angina, and also as part of a combination treatment for chronic heart failure.

What are the contraindications for use of Carvedilol?

Contraindications include the following conditions:

Heart failure of acute origin and decompensated chronic;
Severe liver pathology;
Severe bradycardia;
AV block;
Pregnancy;
With cardiogenic shock;
Arterial hypotension;
Hypersensitivity to drug substances;
Breast-feeding;
Medicines are not prescribed for people under eighteen years of age.

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

What are the uses and dosage of Carvedilol?

The amount of Carvedilol taken is determined by the treating specialist, and the dosage regimen of the drug is determined according to the identified pathology. For 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. When discontinuing the drug Carvedilol, the dosage is reduced gradually over two weeks. The tablets are taken after a meal, washed down with the required amount of water.

Overdose from Carvedilol

In case of an overdose of Carvedilol, the instructions for use warn that hypotension, bradycardia will develop, breathing problems, heart failure will occur, and in more severe situations, even cardiac arrest is possible.

If a little time has passed immediately after poisoning, then you can begin to lavage the stomach; to do this, induce 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, paresthesia, dizziness, syncope is not excluded, possible muscle weakness, sleep disturbance, orthostatic hypotension, depression, angina, in addition, dry mouth, AV block, nausea, noted progression of heart failure, as well as abdominal pain.

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

special instructions

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

Drinking alcohol is contraindicated during treatment. The drug may reduce the production of tear fluid. It is worth noting that the dose of the drug should be reduced or discontinued gradually, otherwise a sharp deterioration of the condition may be provoked.

How to replace Carvedilol, what analogues?

The drug Kardivas, Carvetrend, Carvedilol-Teva, Coriol, Acridilol, Carvedigamma, Carvenal, Carvedilol Shtada, Credex, Carvedilol, Carvedilol-OBL, Recardium, Carvedilol Hexal, Talliton, in addition, Bagodilol, Dilatrend, Carvidil, Carvedilol Zentiva, Carvedilol- Pharmaplant, Vedicardol, Carvedilol Obolenskoye, Carvedilol Canon, Carvedilol Sandoz, and Atram are analogues.

Conclusion

Cardiac medications should be prescribed by a specialist; using pills on your own is contraindicated.

Name:

Carvedilol (Carvedilolum)

Pharmacological
action:

Carvedilol – non-selective beta-adrenergic blocker.
It is also a selective alpha receptor blocker.
Has no intrinsic sympathomimetic activity.
Reduces overall precardiac load by selectively blocking alpha-adrenergic receptors. Due to non-selective blockade of beta-adrenergic receptors, suppression of the renal renin-angiotensin system (decreased plasma renin activity), a decrease in blood pressure, heart rate and cardiac output are observed.
By blocking alpha receptors, carvedilol dilates peripheral blood vessels, thereby reducing vascular resistance.
The combination of vasodilation and beta receptor blockade is accompanied by the following effects: in patients with coronary heart disease - prevention of myocardial ischemia, pain syndrome; in patients with arterial hypertension – a decrease in 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 oral administration after 60 minutes.
The drug is characterized by a linear relationship between blood concentration and 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.
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 phenolic 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 13 times greater activity than carvedilol.

The content of metabolites in the blood is approximately 10 times less than the concentration of carvedilol.
The other two metabolites (hydroxycarbazole) have pronounced adrenergic blocking 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 is eliminated by the kidneys.
In elderly patients a higher concentration of the drug is observed (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.
In some patients with hypertension and renal failure(creatinine clearance less than ≤20 ml/min) there is an increase in the drug content in the blood by 40-55% compared to patients with unchanged renal function.

Indications for
application:

Arterial hypertension (in monotherapy and combination with diuretics);
- chonic 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 take the drug during meals (to increase absorption, which reduces the risk of developing orthostatic hypotension).
For arterial hypertension
Recommended dosage: 1-2 times a day.
For adults, the initial dose is 12.5 mg/day for the first 1-2 days.
The maintenance dosage is 25 mg/day. If necessary, you can gradually increase the dosage at intervals of 14 days (no less!) up to the recommended maximum dose of 50 mg/day.
For elderly patients, the initial recommended dose is 12.5 mg/day (single dose). This dose is sometimes sufficient for further administration.
For arterial hypertension, the maximum allowable dosage is no 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 a single dose of 12.5 mg/day 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 failure
Carvedilol is prescribed as an adjuvant to traditional treatment with angiotensin-converting factor inhibitors, diuretics, digitalis drugs and vasodilators.
To take the drug, the patient must be in a stable condition for the last 4 weeks before switching to treatment with cardvedilol.
Other important conditions for prescribing the drug are a heart rate of no more than 50 beats per minute, systolic blood pressure of more than 85 mm Hg.
The starting dose is 6.25 mg once a day.
If well tolerated, the dose can be gradually increased at intervals of 14 days (at least!) according to the following scheme: 6.25 mg 2 times a day - 12.5 mg 2 times a day - 25 mg 2 times a 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 are used in high doses of diuretics and/or with severe cardiovascular insufficiency).
In these cases, discontinuation of the drug is not required; it is only necessary to refrain from increasing the dosage of carvedilol.
When treating with carvedilol, the patient's general condition 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 determining liver function, body weight, heart rate, heart rhythm and blood pressure levels.

If signs of decompensation develop, fluid retention requires symptomatic therapy (increasing the dosage of diuretics).
In this case, you should refrain from increasing the dosage of carvedilol (at least until the patient’s general condition becomes stable).
Sometimes it is necessary to reduce the dose of carvedilol or even temporarily stop treatment (in these cases it is possible to titrate the dose of the drug).
If carvedilol treatment is interrupted Oh, then you need 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 is not prescribed in pediatrics (for patients under 18 years of age), since there is insufficient information about the safety and effectiveness of the drug in this age group.
It is important to remember that when taking carvedilol in elderly patients, constant medical supervision is necessary, since these patients are more sensitive to carvedilol.
To discontinue the drug a gradual dose reduction is necessary over 7-14 days.

Side effects:

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

The cardiovascular system: bradycardia, peripheral circulatory disorders, orthostatic hypotension.
Musculoskeletal system: pain in the limbs.
Respiratory system: dry nasal mucosa, shortness of breath (obstructive syndrome) in patients with COPD.
Skin and subcutaneous tissue: urticaria, allergic exanthema, itching, reaction like lichen planus, psoriasis. If the patient has psoriasis, skin symptoms may worsen.
Other: swelling at the injection site, general weakness.
Rare: angina pectoris, atrioventricular block, exacerbation of signs of peripheral vascular diseases (Raynaud's syndrome, intermittent claudication, etc.).
Taking carvedilol can provoke latent diabetes mellitus, worsening diabetes mellitus, insufficient control over serum glucose levels.
When titrating carvedilol, a decrease in myocardial contractility is possible (rare).

Contraindications:

Acute and decompensated chronic heart failure, requiring intravenous administration of inotropic agents;
- severe liver failure;
- AV blockade II-III stage;
- severe bradycardia (less than 50 beats/min);
- sick sinus syndrome;
- arterial hypotension (systolic blood pressure less than 85 mm Hg);
- cardiogenic shock;
- bronchial asthma;
- chronic obstructive pulmonary disease;
- age under 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, occlusive diseases of peripheral vessels, pheochromocytoma, psoriasis, renal failure, AV block of the first degree, extensive surgical interventions and general anesthesia, diabetes mellitus, hypoglycemia, depression, myasthenia gravis.
Carvedilol Not recommended

Therapy should be carried out over a long period of time and should not be stopped abruptly, especially in patients with coronary heart disease, as this can lead to a worsening of the underlying disease.
If necessary, the dose reduction should be gradual over 1-2 weeks.
At the beginning of therapy with carvedilol or when the dose of the drug is increased in patients, especially elderly patients, an excessive decrease in blood pressure may be observed, mainly when standing up.
A dose adjustment of the drug is necessary.
In patients with chronic heart failure, when selecting a dose, an increase in symptoms of heart failure and the appearance of edema is 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 is stabilized.
Continuous monitoring of the electrocardiogram and blood pressure is recommended while prescribing carvedilol and slow calcium channel blockers, phenylalkylamine derivatives (verapamil) and benzodiazepine (diltiazem), as well as with class I antiarrhythmic drugs.

Recommended monitor kidney function in patients with chronic renal failure, arterial hypotension and chronic heart failure.
In case of surgery using general anesthesia, the anesthesiologist should be warned about previous therapy with carvedilol.
Carvedilol does not affect blood glucose concentration and does not cause changes in glucose tolerance test performance in patients with non-insulin-dependent diabetes mellitus.
Avoid drinking ethanol during treatment.
Patients with pheochromocytoma should be prescribed alpha-blockers before starting therapy.
Patients wearing contact lenses should be aware that the drug may cause a decrease in tear production.
Impact on the ability to drive vehicles and operate machinery
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 that require high concentration of attention and rapid psychomotor reactions.

Interaction
other medicinal
by other means:

Calcium antagonists and antiarrhythmics.
Cases of bradycardia and hypotension have been observed when carvedilol was taken concomitantly with amiodarone, diltiazem and/or verapamil.
Blood pressure monitoring and electrocardiographic examination should be performed 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.
Close medical monitoring is necessary for patients who are taking class I antiarrhythmic drugs or amiodarone concomitantly with carvedilol.
There are reports of cases of ventricular fibrillation, bradycardia and cardiac arrest when initiating carvedilol therapy in patients taking amiodarone.
If an antiarrhythmic drug is administered parenterally, cardiovascular failure may occur (class Ia or Ic antiarrhythmic drugs).

Cases of bradycardia have been reported when combining the drug with guanethidine, reserpine, methyldopa, guanfacine or monooxygenase inhibitors (except group B monooxygenase inhibitors).
In such cases, monitoring of the heart rhythm is necessary.
It is not recommended to use carvedilol and dihydropyridines simultaneously (risk of severe hypotension, cardiovascular failure).
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 level of digoxin in the blood at the beginning of treatment and at the end of the selection of the maintenance dose.
Carvedilol enhances the hypotensive effect of drugs from other pharmacological groups(phenothiazines, barbiturates, tricyclic antidepressants, α1 receptor antagonists, alcohol, vasodilators).

When combining carvedilol with cyclosporine, it is necessary to study the concentration of the latter in the blood, as its content may increase.
Hypoglycemic agents (including insulin).
Carvedilol can neutralize the signs of hypoglycemia, and antidiabetic agents and insulin can be potentiated by carvedilol, so regular monitoring of serum glucose levels in such patients is necessary.
If the patient is taking clonidine-carvedilol combination, and he needs to stop both drugs, then carvedilol is first stopped, and then the dosage of clonidine is gradually reduced.
If inhalation anesthesia is necessary, one should be aware of the negative hypotensive and inotropic interactions of anesthetics with carvedilol.
The effectiveness of carvedilol decreases 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 vasoconstrictor effect.
When combined with neuromuscular blockers There is an increase in blocking of neuromuscular transmission.
The risk of severe bradycardia and hypertension increases when carvedilol is combined with sympathomimetics (beta-, alpha-adrenergic agonists).

Pregnancy:

Carvedilol Not recommended during pregnancy and breastfeeding.
The teratogenic effect of the drug was not confirmed in animal experiments, but there are not enough clinical studies to study the safety of administration in this category of patients.
Carvedilol can reduce placental blood flow, which provokes premature birth or fetal death.
When carvedilol is taken by a pregnant woman, the fetus or newborn may experience bradycardia, hypoglycemia, pulmonary insufficiency, cardiorespiratory complications and hypothermia.
Carvedilol is prescribed during pregnancy only when the expected benefits of the drug outweigh 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 breast milk.
If the drug is taken by a nursing woman, stop breastfeeding.

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 treatment it is necessary to monitor basic vital signs.
Patients with overdose should, if necessary, be kept in an intensive care unit.
Maintenance treatment: for the prevention of severe bradycardia - atropine 0.5–2 mg intravenously, to support the cardiovascular system: glucagon (first 1–10 mg intravenous bolus, then intravenous infusion 2–5 mg/hour).
Sympathimetic drugs are prescribed (isoprenaline, dobutamine or epinephrine - the dose depends on the patient’s body weight).
For bradycardia refractory to drug therapy, electrical stimulation of the heart is used.
To relieve bronchospasm - beta-sympathomimetics in the form of intravenous infusion or inhalation, intravenous aminophylline is also effective.
To relieve convulsive syndrome, diazepam is administered slowly intravenously.
Since carvedilol quickly binds 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:

Carvedilolot tablets 6.25 mg, 12.5 mg and 25 mg white to white with a creamy tint, flat-cylindrical, chamfered; light marbling is allowed in 10, 20, 30 or 60 pieces.
Carvedilolot Zentiva tablets 6.25 mg, 12.5 mg and 25 mg of brownish-yellow color, interspersed, with a mark for division on one side and engraved with the number “12” - on the other, 15 or 30 pcs.
Tablets Karvedilolot Canon 6.25 mg, 12.5 mg and 25 mg flat-cylindrical, with a chamfer and notch, 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.

Carvedilolot Sandoz tablets 3.125 mg, 6.25 mg, 12.5 mg, 25 mg and 50 mg are yellow, round, biconvex, scored on both sides and sides and with the inscription “C2” on one side.
Tablets Karvedilolot Shtad 12.5 mg and 25 mg pinkish-beige, round, biconvex, with a score on both sides and on the sides and with the inscription “C3” on one side, 30 pcs.
Karvedilolot-Teva tablets 3.125 mg, 6.25 mg, 12.5 mg and 25 mg white or off-white, round, biconvex, with "CA3" engraved on one side, 28 or 30 pieces.

Storage conditions:

Store in a dry place, protected from light, 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

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

Updating the description and photo: 13.08.2019

Carvedilol is an alpha and beta adrenergic blocker without intrinsic sympathomimetic activity with antianginal, vasodilating and antiarrhythmic effects.

Release form and composition

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

The active substance is carvedilol, 1 tablet contains 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 primarily to the blockade of alpha 1 adrenergic receptors. Thanks to it, a decrease in total peripheral vascular resistance (TPVR) is observed. Vasodilation, combined with blockade of beta-adrenergic receptors, leads to the fact that in patients with arterial hypertension, blood pressure decreases without increasing peripheral blood flow, and a slowdown in peripheral blood flow (unlike beta-blockers) does not occur. 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 the blood plasma.

In patients with heart failure and/or left ventricular dysfunction, carvedilol normalizes the size of the left ventricle, improves ejection fraction and has a beneficial effect on hemodynamic parameters. The drug also has an antioxidant effect, which consists in eliminating free oxygen radicals.

Carvedilol reduces the number of deaths and hospitalizations, eliminates unpleasant symptoms and improves left ventricular function in patients with chronic heart failure of non-ischemic and ischemic etiology. The therapeutic effects of carvedilol vary in dose dependence.

Pharmacokinetics

Carvedilol is rapidly absorbed from the gastrointestinal tract when taken orally. This compound is highly lipophilic. Its maximum level in the blood is recorded approximately 1 hour after administration. The half-life averages 6–10 hours. Carvedilol is 95–99% bound to plasma proteins. 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 with food, no significant change in this indicator is observed.

Most carvedilol is metabolized primarily in the liver through conjugation and oxidation to form certain metabolites. The substance participates in metabolic processes during the “primary passage” through the liver. The metabolism of carvedilol, carried out through oxidation, is stereoselective. The R(+) isomer is metabolized primarily through the isoenzymes CYP1A2 and CYP2D6. In the case of the S(-) isomer, the CYP2D9 isoenzyme predominantly participates in metabolic processes and, to a lesser extent, the CYP2D6 isoenzyme. Carvedilol is also metabolized through other isoenzymes of cytochrome P 450: CYP2C19, CYP2E1 and CYP3A4. Due to hydroxylation and demethylation of the phenolic ring, 3 metabolites are formed, characterized by vasodilating properties that are less pronounced than those of carvedilol itself. Metabolites have a pronounced adrenergic blocking 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 renal dysfunction, the pharmacokinetic parameters of the drug do not change significantly. The pharmacokinetics of carvedilol remains almost the same regardless of the patient's age (no statistically significant effect of this parameter was found).

In patients with liver cirrhosis, the bioavailability of carvedilol increases by 80% due to a decrease in the rate of metabolism during the “first pass” through the liver. In cases of severe liver dysfunction, the use of carvedilol is not recommended.

Carvedilol crosses the placental barrier and is detected 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 (SSNS);
• Chronic heart failure in the stage of decompensation;
• Atrioventricular block (AV block) II and III degrees (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;
• Pregnancy and breastfeeding period;
• Hypersensitivity to the components of the drug.

According to the instructions, Carvedilol should be used with caution in AV blockade of the first degree, Prinzmetal's angina, occlusive diseases of peripheral vessels, thyrotoxicosis, pheochromocytoma, renal failure, psoriasis, bronchospastic syndrome, pulmonary emphysema, chronic bronchitis, general anesthesia during major surgery, myasthenia gravis , hypoglycemia, diabetes mellitus, depression.

Instructions for use of Carvedilol: method and dosage

The 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. If well tolerated and insufficiently effective, 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. Dose selection must be done strictly individually, under the supervision of the attending physician. For patients with good tolerance to Carvedilol, the dose is increased by a factor of 1 time every 2 weeks and increased to 25 mg 2 times a day over 6 weeks. It is recommended to increase the dose to the maximum tolerated dose by the patient; for patients with body weight 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 frequency of administration 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 regimen.

For elderly patients (over 70 years old), the drug is prescribed in a daily dose of no more than 25 mg with a dosage frequency of 2 times a day.

The drug is discontinued by gradually (1-2 weeks) reducing the dose taken.

If you miss the next dose, you should take the tablet as soon as you remember, but you should not double the dose the next time you take it.

Side effects

The use of Carvedilol may cause undesirable effects:

• From the cardiovascular system: angina pectoris, bradycardia, AV block, orthostatic hypotension; rarely - progression of heart failure, intermittent claudication, peripheral circulatory disorders;
• From the nervous system: muscle weakness (usually 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 hematopoietic 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 limbs, flu-like syndrome, weight gain, decreased lacrimation.

Overdose

Symptoms of a Carvedilol overdose include heart failure, bradycardia, a marked decrease in blood pressure, cardiogenic shock, and cardiac arrest. Vomiting, bronchospasm, breathing problems, 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 permissible to carry out such measures as the administration of sympathomimetics [epinephrine (adrenaline), dobutamine] in various doses depending on the body’s response to maintenance therapy and body weight, the administration of atropine intravenously (0.5–2 mg) for severe symptoms of bradycardia and glucagon (1-10 mg intravenous bolus, then 2-5 mg every hour in the form of long-term infusion therapy) to maintain the functioning of cardiovascular activity. You can also place the patient on his back and elevate his legs.

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

If bradycardia is resistant to treatment procedures, the use of an artificial pacemaker is indicated. For bronchospasm, beta-agonists are prescribed in aerosol form (if proven ineffective, the drug is administered intravenously) or aminophylline intravenously. For convulsions, diazepam should be administered slowly intravenously.

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

special instructions

The drug should not be used to treat patients with low blood pressure.

At the beginning of use and when increasing the dose, 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, severe dizziness and even fainting occur.

Treatment of patients with coronary heart disease, renal failure, arterial hypotension, peripheral vascular diseases, and heart failure should be carried out under regular monitoring of renal function; if laboratory parameters worsen, Carvedilol should be discontinued.

In patients with psoriasis, peripheral vascular diseases, and a history of anaphylactic reactions, the effect of the drug can lead to a worsening of the condition; in patients with Prinzmetal's angina, it can provoke the appearance of chest pain. The use of the drug reduces sensitivity during allergy tests.

While taking the drug, it is recommended to carry out general anesthesia with caution with drugs with negative inotropic effects, such as cyclopropane, ether, trichlorethylene. The patient should inform the doctor about taking Carvedilol. Before planned major surgical operations, 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, and, if necessary, adjusting hypoglycemic therapy.

Particular 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 switches to the use of the drug.

During the treatment period, alcohol consumption is contraindicated.

When discontinuing combination therapy of Carvedilol and clonidine, carvedilol should be gradually discontinued first, and only a few days later, a reduction in the dose of clonidine should begin.

At the beginning of treatment and when the dose is increased, 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 dangerous 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 likely benefit of treatment for the mother outweighs the potential risk to the fetus.

Animal experiments have shown that carvedilol and its metabolites pass into breast milk. There is no data on the penetration of these substances into breast milk in humans, therefore, when prescribing the drug during lactation, breastfeeding must be stopped.

Drug interactions

While taking the drug, intravenous administration of diltiazem and verapamil should not be prescribed due to the risk of a strong decrease in blood pressure and a decrease in heart rate.

The effect of carvedilol is enhanced by 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 simultaneous use of Carvedilol:

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

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

Analogs

Analogues of Carvedilol are: Atram, Alotendin, Anaprilin, Amlodak-AO, Aodak-AO, Dilatrend, Vedicardol, Carvetrend, Karvidex, Carvedigamma, Carvedilol Obolenskoe, Carvedilol-KV, Carvedilol Hexal, Carvedilol-Lugal, Carvedilol Zentiva, Carvedilol Sandoz, Cardivas, Carvidil, Credex, Coriol, Talliton.

Terms and conditions of storage

Store in a dry place, protected from light, 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 other members of this group, which are most often used to treat cardiovascular diseases.

In addition to B2 adrenergic receptors, it also blocks B1 and alpha1 adrenergic receptors. Thanks to this, the drug has additional therapeutic effects, but there are also more side effects 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 release form

Carvedilol is available in film-coated tablets of 12.5 and 25 mg. They have a flat-cylindrical shape and are white. Available in blister packs - 30 tablets.

• This drug contains carvedilol, which is the active substance, as well as a number of excipients.

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

Indications for use

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

• arterial hypertension (usually together with other blood pressure medications);
• stable angina;
• chronic heart failure (stages II–III according to NYHA), together with other drugs - diuretics, digoxin or ACE inhibitors.

pharmachologic effect

Carvedilol is a non-selective beta-adrenergic receptor blocker. It is also a selective alpha receptor blocker. Has no intrinsic sympathomimetic activity. Reduces overall precardiac load by selectively blocking alpha-adrenergic receptors.

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

The combination of vasodilation and beta receptor blockade is accompanied by the following effects: in patients with coronary heart disease - prevention of myocardial ischemia and pain; in patients with arterial hypertension – a decrease in 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.

• For arterial hypertension during the first 7-14 days, the recommended initial dose is 12.5 mg/day (1 tablet) in the morning after breakfast. The dose can be divided into 2 doses of 6.25 mg of Carvedilol (1/2 tablet of 12.5 mg). Next, the drug is prescribed at a dose of 25 mg (1 tablet 25 mg) in 1 dose in the morning, or divided into 2 doses of 12.5 mg (1 tablet 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. If well tolerated and insufficiently effective, 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;
• For 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 a day for 2 weeks. If well tolerated, 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 more than 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 a day, followed by an increase in the dose.

If you miss the next dose, you should take the tablet as soon as you remember, but you should not double the dose the next time you take it. 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 regimen.

• The drug is discontinued by gradually (1-2 weeks) reducing the dose taken.

For elderly patients (over 70 years old), the drug is prescribed in a daily dose of no more than 25 mg with a dosage frequency of 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 components;
5. Bronchial asthma;
6. Kidney, 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 adrenal tumor;
2. Kidney problems;
3. Psoriasis;
4. Diabetes mellitus;
5. Hyperthyroidism;
6. Depressive states;
7. Old age;
8. Chronic obstructive pneumonia;
9. Vascular lesions of the lower extremities.

Carvedilol should not be taken without a doctor’s prescription, and treatment should be carried out under constant monitoring of kidney and liver parameters, blood sugar and insulin levels.

Side effects

Carvedilol can cause the following side effects from organs and systems:

• Nervous system – headache, weakness, dizziness, sleep disturbances, depression, syncope, paresthesia;
• The effect on the cardiovascular system is manifested by a significant decrease in heart rate, disruption in the myocardial conduction system (AV block), decreased pressure, pain in the heart, attacks of angina, increased heart failure, increased symptoms of Raynaud's syndrome, deterioration of blood circulation in the periphery, the appearance swelling.
• Hematopoietic system – leukopenia, thrombocytopenia;
• Changes in the functioning of the digestive system: nausea, sometimes vomiting, frequent loose stools or constipation, dry mouth, abdominal pain, increased levels of liver enzymes (transaminases) in the blood.
• Urinary system – severe renal dysfunction, edema;
• Allergies can manifest as hives, skin itching and various rashes.

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

Analogues of Carvedilol

Structural analogues of 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 instruction should not be used as a guide to self-medication. The need for prescription, methods and doses of the drug are determined exclusively 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 the agonist) alpha and beta adrenergic receptors. ATS code C07A G02.

Pharmacological properties

Pharmacodynamics.

Antihypertensive, vasodilator, antianginal (Antianginal- drugs that improve blood supply to the myocardium by dilating the coronary arteries) means. Non-selective alpha 1 -, beta 1 - and beta 2 -adrenergic blocker, without intrinsic sympathomimetic activity. The vasodilating effect is mainly due to blockade (Blockade- slowing down or interrupting 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- a peptide hormone produced in human blood. Regulates blood pressure and water-salt metabolism in 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 based on changes in the composition of blood plasma. Medicines are prepared from blood plasma) at the same time it decreases without delaying fluid excretion. Reduces blood pressure, total peripheral vascular resistance, pre- and afterload(or afterload) is 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 renal function. The combination of a vasodilator effect and beta-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.) the decrease in 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). 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 passing unchanged from one compound to another and incapable of long-term existence in a free state\; in chemical formulas it is often separated by 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 found mainly in biological membranes and are involved in the transport of substances through them. Determining the content of lipoproteins in the blood has 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 persists for 24 hours. With prolonged treatment, the maximum effect develops after 3–4 weeks. In patients coronary heart disease (Cardiac ischemia– a chronic pathological process that 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 effects. 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) Parts of the human heart) and/or circulatory failure has a beneficial effect on hemodynamic parameters, increasing the ejection fraction of the left ventricle and reducing its size, reduces end-systolic and end-diastolic volumes, as well as peripheral and pulmonary resistance, increases tolerance (Tolerance- a decrease in the reaction to repeated administration of a substance, the body becomes addicted, which is why a larger and larger dose is required to achieve the effect inherent in the substance. They also distinguish 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 the rapid (literally after the first use) development of tolerance to a drug. Also an immunological state of the body in which it is unable to synthesize antibodies in response to the introduction of a specific antigen while maintaining immune reactivity to other antigens. The problem of tolerance is important in organ and tissue transplantation) to physical activity. Ejection fraction and cardiac index do not change with normal cardiac function. The effect of carvedilol is more pronounced in patients with tachycardia (Tachycardia- 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.

Quickly and almost completely absorbed from the gastrointestinal tract. The maximum concentration in the blood is reached after approximately 1 hour. Bioavailability (Bioavailability- an indicator of the degree and speed of entry of a medicinal substance into the blood from the total administered dose) is 25% due to the “first pass through the liver” effect (60–75%). Food intake does not affect bioavailability and maximum concentration levels, but prolongs 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%. It is intensively metabolized mainly in the liver due to its combination with glucuronic acid. As a result of demethylation and hydroxylation, three metabolites with pronounced beta-blocking and antioxidant effects are formed. The volume of distribution is about 2 l/kg and increases with impaired liver function. Passes through the placental barrier and is excreted into breast milk. Half-life (Half-life(T1/2, synonymous with half-elimination period) - the period of time during which the concentration of a drug in the blood plasma decreases by 50% from the initial level. Information about this pharmacokinetic indicator is necessary to prevent the creation of a toxic or, conversely, ineffective level (concentration) of the drug in the blood when determining the intervals between administrations) carvedilol - 6–10 hours, plasma clearance (Clearance(purification, purification) - a pharmacokinetic parameter reflecting the rate of purification of the blood plasma from the drug and denoted by the symbol C1)- about 590 ml/min. Excreted mainly from bile (Bile- a secretion produced by 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 (allochol, decholin, etc.)), a small part of the dose is excreted as metabolites by the kidneys.

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

Indications for use

Arterial hypertension (in the form of monotherapy and in combination with other antihypertensive drugs), 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 occurs during physical activity and disappears after its cessation or taking nitroglycerin under the tongue (angina pectoris)), chronic (Chronic- a long, continuous, protracted process, occurring either constantly or with periodic improvements in the 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 promote the removal of excess water and sodium chloride from the body), digoxin and inhibitors (Inhibitors- chemicals that inhibit enzyme activity. 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 heart contractions to 60 beats per minute or less (absolute bradycardia) or a lag between the increase in heart rate and the 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 degrees (except for patients with an artificial pacemaker), sick sinus syndrome, cardiogenic shock (Cardiogenic shock– one of the most serious complications in the acute period of myocardial infarction, which is characterized by impaired hemodynamics and vital functions of the body), chronic obstructive pulmonary diseases, bronchial asthma, severe liver dysfunction, metabolic acidosis (Acidosis- a shift in the body’s acid-base balance towards increasing acidity (decreasing pH)). Pregnancy, breastfeeding period, childhood (up to 18 years).

Directions for use and doses

Prescribed to adults regardless of food intake. 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 is one of the oldest and main medical specialties. 2. Part of a word or phrase used to indicate the type of treatment (oxygen therapy\; hemotherapy - treatment with blood products)). In case of circulatory insufficiency, it is better to take with food to slow down absorption and reduce the risk of orthostatic reactions. The tablet is swallowed without chewing, washed down 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 can already provide the necessary effect. If necessary, the dose can be increased after 2 days to 25 mg once a day, then at intervals of at least two weeks to 50 mg per day, once or in 2 doses (25 mg in the morning and evening). The maximum daily dose is 50 mg.

Angina pectoris. 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 to a maximum daily dose of 100 mg, divided into 2 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) must be recorded before the drug is prescribed. The recommended starting dose is usually 6.25 mg once daily. If well tolerated 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, and then 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.

Features of application

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. Characterized by signs of increased sympathetic activity and adrenaline release (sweating, anxiety, tremors, palpitations, hunger) and central nervous system symptoms (fainting, blurred vision, convulsions, coma)), thyrotoxicosis (Thyrotoxicosis- a syndrome caused by the effect of excess thyroxine and triiodothyronine on target tissue. There are many causes of thyrotoxicosis\; the most common cause is diffuse toxic goiter (Graves disease). The clinical picture includes the effect 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, first degree atrioventricular block, chronic obstructive pulmonary disease, Prinzmetal vasospastic angina (can provoke attacks), psoriasis (Psoriasis- a chronic hereditary skin disease with diverse clinical manifestations. The most common is ordinary psoriasis - profusely scaly papules and plaques on the scalp, elbows, forearms, hands, legs, feet, lower back, and buttocks. Complaints of itching. In this disease, keratinocytes are formed 28 times more than normal), renal dysfunction, depression (Depression- mental disorder: melancholy, depressed mood with pessimism, monotony of ideas, decreased motivation, retardation of movements, various somatic disorders), myasthenia gravis (Myasthenia gravis- a 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 during treatment with alpha-blockers, alpha-agonists, digitalis preparations, diuretics and/or inhibitors monoamine oxidases (Monoamine oxidase- enzyme that catabolizes monoamines). In these cases, treatment should be started at low doses followed by a slow increase until effective. At the beginning of treatment or when the dose of the drug is increased, patients, especially the elderly, may experience 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 is caused by medicinal substances that disrupt autonomic reflex mechanisms or cause hypovolemia). When these patients develop swelling (Edema– tissue swelling as a result of a pathological increase in the volume of interstitial fluid) and/or increasing 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 is stabilized. If the heart rate decreases to 55 beats/min, the drug should be discontinued.

When prescribed 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 renal function; if it worsens, reduce the dose or discontinue the drug and increase the dose of diuretics.

In patients with chronic obstructive pulmonary disease with a bronchospastic component who are not receiving antiasthmatic drugs, carvedilol should be prescribed only if the benefit outweighs the potential risk. In individuals with severe allergies or undergoing desensitization, carvedilol may increase allergic reactions. For patients who have previously experienced or worsened psoriasis during treatment with beta blockers, the drug can be prescribed only after a thorough assessment of the possible benefits and risks. Like other beta blockers, carvedilol may reduce the severity of thyrotoxicosis. In case of surgery using general anesthesia, the anesthesiologist should be warned about previous therapy with carvedilol. Patients with pheochromocytoma should be prescribed alpha-blockers before starting therapy. Contact lens wearers should be warned about the possibility of decreased tear production. During treatment, ethanol should be avoided.

If it is necessary to simultaneously prescribe blockers of “slow” calcium channels - phenylalkylamine derivatives (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 beating heart. The waveform recorded on moving paper or photographic film is called an electrocardiogram (ECG). Plays an important role in the diagnosis of many heart diseases) and blood pressure.

If concomitant therapy with clonidine is discontinued, treatment with carvedilol should first be discontinued, then clonidine should be discontinued after a few days. Carvedilol does not affect concentrations glucose (Glucose- grape sugar, a carbohydrate from the group of monosaccharides. One of the key metabolic products that provides living cells with energy) 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 over a long period of time and should not be abruptly stopped, 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 over 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 breastfeeding.

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

Children.

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

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

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

Side effect

The drug is generally well tolerated. Rarely may be observed:

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

From 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- frequent discharge of liquid feces, associated with 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, increased levels of liver transaminases.

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

From the hematopoietic system: thrombocytopenia (Thrombocytopenia- decrease in platelet count), leukopenia.

From the respiratory system:dyspnea (Dyspnea– disturbance 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 caused by irritation of the nerve endings of pain receptors), skin rashes, 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 production, manifestation of latent diabetes mellitus or an increase in its symptoms.

Interaction with other drugs

Carvedilol should not be used if the patient is receiving intravenous administration of verapamil, diltiazem, or antiarrhythmic drugs (especially class 1). Potentiation (Potentiation(synonym for supraadditive synergism) is a type of synergism in which the final pharmacological effect of a drug combination 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 drugs, nitrates and antiarrhythmic drugs. Drugs that reduce the content catecholamines (Catecholamines- natural catecholamines (adrenaline, norepinephrine, dopamine) - mediators of the nervous system. Participate in metabolism and adaptive reactions of the body. With physical and mental stress (stress), and certain diseases, the content of catecholamines in the blood and urine increases sharply)(reserpine, monoamine oxidase inhibitors), and clonidine increase the risk of developing arterial hypotension and bradycardia. Inhibitors of microsomal oxidation (cimetidine) enhance and inductors (Inductor- chemical substances that stimulate their own metabolism or the metabolism of other compounds (drugs) upon repeated administration)(phenobarbital, rifampicin) - weaken the effects of carvedilol. Simultaneous use with ergot alkaloids worsens peripheral blood circulation. When used with cardiac glycosides (Glycosides- organic substances whose molecules 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 may impair atrioventricular conduction, rarely with hemodynamic disturbances. Carvedilol increases the levels 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) strengthen the negative inotropic (Inotropic- changing the force of heart contraction) and hypotensive effects of carvedilol. Carvedilol may potentiate the action of insulin and oral (Orally- route of administration of the drug through the mouth (per os)) hypoglycemic agents (Hypoglycemic agents- drugs that lower blood sugar are used to treat diabetes mellitus), masking the symptoms of hypoglycemia (especially tachycardia), which requires regular monitoring of blood glucose levels.

Overdose

Symptoms: severe arterial hypotension (systolic pressure 80 mm Hg and below), bradycardia (less than 50 beats/min), cardiogenic shock (Shock- a condition characterized by a sharp decrease in blood flow in 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 clinical picture of shock 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: waste products of microorganisms entering the blood cause dilation of blood vessels and increase capillary permeability. Clinically manifests as hypovolemic shock with signs of infection. Hemodynamics in septic shock are constantly changing. To restore bcc, infusion therapy is needed. Cardiogenic shock develops due to a deterioration in the pumping function of the heart. Medicinal substances that enhance myocardial contractility are used: dopamine, norepinephrine, dobutamine, epinephrine, isoprenaline. Neurogenic shock - a decrease in the effective volume of circulating blood is caused by the loss of sympathetic tone and dilation of arteries and venules with the deposition of blood in the veins\; develops with spinal cord injuries and as a complication of spinal anesthesia), respiratory dysfunction (bronchospasm), circulatory failure, convulsions, cardiac arrest.

Treatment: during the first hours - induction of vomiting and gastric lavage, then monitoring and correction of vital signs in the intensive care unit. Maintenance therapy: for severe bradycardia - atropine 0.5–2 mg intravenously; to maintain cardiac activity - glucagon 1–5 mg (maximum dose - 10 mg) intravenously in a bolus, then 2–5 mg/hour in the form infusions (Infusion(IV administration) - administration of fluids, medications or blood products/components into a venous vessel) and/or adrenergic agonists (orciprenaline, isoprenaline) 0.5–1 mg intravenously. If the peripheral vasodilator effect predominates, 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 the conduction of nerve impulses through the synapse. Increases blood pressure, stimulates carbohydrate metabolism, etc.) in repeated doses of 5–10 mcg or as an infusion of 5 mcg/min. To relieve bronchospasm, beta 2-adrenergic agonists are used in the form of an aerosol, if ineffective - intravenously or aminophylline intravenously. For convulsions, diazepam or clonazepam is administered slowly intravenously. In severe cases intoxication (Intoxication- poisoning of the body with toxic substances) in case of cardiogenic shock, maintenance therapy is continued for a long time until the patient’s condition stabilizes and taking into account the half-life of carvedilol.

General Product 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 per pack.

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

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

Website. www.vitamin.com.ua

Preparations with similar active ingredients

• Corvasan - "Arterium"

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