Instructions for use CARVEDILOL-MIC

Pharmacodynamics and Pharmacokinetics

The mechanism of action of Carvedilol is a racemic mixture in which non-selective beta-adrenergic receptors block the activity of the S (+) enantiomer and alpha-adrenergic receptors block the activity of the R (+) and S (-) enantiomers with equal effectiveness. Carvedilol also reduces systemic vascular resistance by blocking alpha-adrenergic receptors .

The active substance of the drug and its metabolite BM-910228 (a less powerful beta blocker, but a stronger antioxidant) restores the inotropic response to Ca 2+ in OH - free radicals in the myocardium , and also reduces the content of active induced radicals in the sarcoplasmic reticulum Ca 2 + -ATPases. Thus, Carvedilol and its metabolites may be useful in chronic heart failure and in preventing free radical damage.

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.

Carvedilol or Metoprolol – which is better?

Manufacturer: OZON LLC, Russian Federation
Release form: tablets

Active ingredient: metoprolol tartrate 25 mg, 50 mg, 100 mg

Synonyms: Metokard, Egilok

Metoprolol is a domestic analogue of Carvedilol tablets, belonging to the group of cardioselective beta1-blockers. The medication has an antihypertensive effect and has an antiarrhythmic effect. Metoprolol is prescribed for the following conditions:

• high blood pressure;
• angina pectoris;
• tachycardia of various origins;
• stable CHF;
• repeated prophylaxis after myocardial infarction;
• prevention of migraine attacks.

Which drug is better, Carvedilol or an analogue, for the treatment of cardiovascular pathologies should be decided by the doctor.

Analogues containing metoprolol tartrate are not used for heart failure and in the post-infarction period. For these conditions, metoprolol succinate is prescribed.

Contraindications

Carvedilol is contraindicated in patients with:

• bronchial asthma (2 cases of death from status asthmaticus in patients were registered) or related bronchospastic symptoms of the second or third degree;
• sick sinus syndrome or severe bradycardia (if a permanent pacemaker is in place);
• cardiogenic shock or decompensated heart failure requiring the use of intravenous infusions;
• clinically obvious liver failure ;
• hypersensitivity to any of the components of the drug.

Side effects

Patients taking this drug may experience dizziness , headaches, and even fainting.

The most common side effects when taking Carvedilol:

• hyperglycemia or high blood sugar;
• excessive thirst;
• frequent urination;
• feeling of extreme hunger;
• weakness;
• blurred vision.

If patients taking this drug experience any of these symptoms, they should consult their doctor as soon as possible.

Side effects observed in rare cases:

• nausea;
• vomit;
• diarrhea;
• joint pain;
• insomnia;
• cough;
• dry eyes;
• blurred vision;
• numbness or tingling in the limbs;
• weight gain;
• chest pain;
• swelling of the arms and legs;
• rash;
• hives;
• itching.

Carvedilol, instructions for use (Method and dosage)

Instructions for use of Carvedilol: the drug is taken orally with plenty of liquid and preferably after meals. The dosage and duration of taking the drug is selected individually depending on the severity of the patient’s condition.

For arterial hypertension, the drug is used for 1 - 2 weeks at a dosage of 12.5 mg per day. It is preferable to take the drug after a hearty breakfast. At the discretion of the attending physician, the daily dose can be divided into two equal parts - 6.25 mg each. Afterwards the dosage is increased to 25 mg per day.

For angina pectoris , the drug is prescribed in a dosage of 25 mg per day. The dosage is divided into 2 doses in equal proportions. After a week of using the drug, the daily dose can be increased to 50 mg at the discretion of the attending physician.

Instructions:

Clinical and pharmacological group

01.002 (Beta1-, beta2-blocker. Alpha1-blocker)

Release form, composition and packaging

The tablets are flat-cylindrical, white, with a chamfer and a score.

Excipients: lactose, sucrose, polyvidone K25, crospovidone, methylcellulose, croscarmellose sodium.

10 pieces. — contour cell packaging (3) — cardboard packs. 30 pcs. — cellular contour packages (1) — cardboard packs.

pharmachologic effect

Alpha and beta blocker without intrinsic sympathomimetic activity.

Blocks α1-, β1 and β2-adrenergic receptors. It has a vasodilating, antianginal and antiarrhythmic effect.

The vasodilating effect is mainly associated with blockade of α1-adrenergic receptors. Thanks to vasodilation, it reduces peripheral vascular resistance. Has membrane-stabilizing properties. The combination of vasodilation and blockade of beta-adrenergic receptors leads to the following effects: in patients with arterial hypertension, a decrease in blood pressure is not accompanied by an increase in peripheral blood flow, and peripheral blood flow does not decrease (unlike beta-blockers). Heart rate decreases slightly.

In patients with ischemic heart disease it has an antianginal effect. Reduces pre- and afterload on the heart. Does not have a pronounced effect on lipid metabolism and the content of potassium, sodium, and magnesium in the blood plasma. In patients with impaired left ventricular function or circulatory failure, it has a beneficial effect on hemodynamic parameters and improves ejection fraction and left ventricular dimensions. Has an antioxidant effect, eliminating free oxygen radicals.

Pharmacokinetics

Suction

After oral administration, carvedilol is quickly and almost completely absorbed from the gastrointestinal tract. Bioavailability is 25% (due to the high degree of metabolism in the liver). The concentration in blood plasma is proportional to the dose taken. Cmax in blood plasma is reached after 1 hour. Food intake slows down the absorption of carvedilol without affecting its bioavailability.

Distribution

Plasma protein binding is almost complete - 98-99%. Penetrates the placental barrier and is excreted in breast milk.

Metabolism

Metabolized to form metabolites with a high ability to block β-adrenergic receptors.

Removal

T1/2 - 6-10 hours. Excreted mainly in bile.

Pharmacokinetics in special clinical situations

In elderly patients, carvedilol plasma concentrations are approximately 50% higher than in younger patients.

In patients with impaired liver function, bioavailability can increase up to 80%.

Dosage

The dosage regimen is set individually.

The drug is taken orally, regardless of food intake.

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 in 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.

For stable angina, the initial dose of Carvedilol is 12.5 mg (1 tablet 12.5 mg) 2 times a day. After 7-14 days, the dose can be increased to 25 mg (1 tablet 25 mg) 2 times a day. If there is insufficient effectiveness and good tolerability, after 14 days the dose of Carvedilol may be further increased. The daily dose of Carvedilol for angina pectoris should not exceed 50 mg (2 tablets of 25 mg), prescribed 2 times a day.

For patients over 70 years of age, the daily dose of Carvedilol should not exceed 25 mg (1 tablet 25 mg) 2 times a day.

When discontinuing the drug, the dose should be reduced gradually over 1-2 weeks.

If you miss the next dose, the drug should be taken as soon as possible. However, if it is time for the next dose, you only need to take one single dose (without doubling).

If there is a break in taking the drug for more than 2 weeks, it is necessary to resume treatment with the lowest doses of Carvedilol.

The tablets are taken after meals with a small amount of water.

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 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.

Overdose

Symptoms: severe arterial hypotension, bradycardia, respiratory disorders (including bronchospasm), heart failure, cardiogenic shock, cardiac arrest.

Treatment: if the patient is conscious, induce vomiting. The patient should be placed in a horizontal position with legs elevated.

The unconscious patient should be placed on his side and measures should be taken to remove the unabsorbed drug. In such cases, hospitalization is required.

If necessary, symptomatic therapy is carried out, adrenoreceptor agonists are administered.

Drug interactions

During therapy with Carvedilol, diltiazem and verapamil should not be administered intravenously due to a possible pronounced decrease in heart rate and a pronounced decrease in blood pressure.

Some antiarrhythmic drugs, anesthesia drugs, antihypertensive drugs, antianginal drugs, other beta-blockers (including those used in the form of eye drops), MAO inhibitors, sympatholytics (reserpine) and cardiac glycosides may enhance the effect of Carvedilol. When administered concomitantly with Carvedilol, the doses of these drugs should be selected with caution.

When used simultaneously with liver enzyme inducers (for example, rifampicin, phenobarbital), the concentration of carvedilol in the blood plasma may decrease, and when used together with liver enzyme inhibitors (for example, cimetidine), the concentration of carvedilol in plasma may increase.

With simultaneous use, Carvedilol may increase the concentration of digoxin in the blood plasma.

The simultaneous administration of Carvedilol with ergot alkaloids worsens peripheral circulation.

Carvedilol may enhance the effect of hypoglycemic drugs and mask the manifestations of hypoglycemia (it is recommended to regularly monitor blood glucose levels).

Use during pregnancy and lactation

The drug is contraindicated for use during pregnancy and lactation (breastfeeding).

Side effects

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

From the cardiovascular system: bradycardia, orthostatic hypotension, angina pectoris, AV block; rarely - peripheral circulatory disorders, intermittent claudication, progression of heart failure.

From the digestive system: dry mouth, nausea, abdominal pain, diarrhea, constipation, vomiting, increased activity of liver transaminases.

From the hematopoietic system: thrombocytopenia, leukopenia.

From the urinary system: severe renal dysfunction, edema.

Allergic reactions: skin reactions (exanthema, urticaria, itching, rash), exacerbation of psoriasis, sneezing, nasal congestion, bronchospasm, shortness of breath (in predisposed patients).

Other: flu-like syndrome, pain in the extremities, decreased lacrimation, weight gain.

Storage conditions and periods

List B. The drug should be stored out of the reach of children, in a dry place, protected from light, at a temperature not exceeding 25°C. Shelf life: 3 years.

Indications

- arterial hypertension (as mono- or combination therapy);

- stable angina pectoris;

- chronic heart failure (as part of combination therapy).

Contraindications

- severe liver failure;

— severe bradycardia (heart rate less than 50 beats/min);

— SSSU;

- AV blockade of II and III degrees (except for patients with an artificial pacemaker);

— chronic heart failure in the stage of decompensation;

- acute heart failure;

- cardiogenic shock;

- arterial hypotension (systolic blood pressure less than 85 mm Hg);

- pregnancy;

- lactation (breastfeeding);

- children and adolescents up to 18 years of age;

- hypersensitivity to carvedilol and other components of the drug.

The drug is prescribed with caution for 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, hypoglycemia, depression, myasthenia gravis.

special instructions

The drug should be prescribed with caution to patients with bronchospastic syndrome, chronic bronchitis, and pulmonary emphysema.

At the beginning of treatment with Carvedilol and with increasing doses of the drug, a sharp decrease in blood pressure and orthostatic reactions are possible. Dizziness and even fainting may occur, especially in elderly patients, with heart failure, when using combination antihypertensive therapy or when using diuretics.

The drug is not recommended for use in patients with low blood pressure.

Treatment with Carvedilol should not be stopped abruptly, especially in patients with angina pectoris, because this may make the condition worse. The dose reduction should be gradual over 1-2 weeks.

During the period of use of Carvedilol, it is necessary to monitor renal function in patients with renal failure, coronary artery disease, peripheral vascular disease, arterial hypotension and/or heart failure. If renal function deteriorates, the drug should be discontinued.

Prescribing beta-blockers to patients with peripheral vascular diseases, psoriasis and a history of anaphylactic reactions can lead to a worsening of the disease, and in Prinzmetal's angina it can provoke the appearance of chest pain. In addition, the use of Carvedilol may reduce the sensitivity of allergy tests.

Prescribing the drug may mask the symptoms of thyrotoxicosis and early symptoms of hyperglycemia. For diabetes mellitus, regular monitoring of blood glucose levels and, if necessary, adjustment of hypoglycemic therapy is recommended.

While using Carvedilol, general anesthesia should be used with caution using drugs with negative inotropic effects (ether, cyclopropane, trichlorethylene). The patient should inform the doctor about taking Carvedilol. Before major surgical interventions, gradual withdrawal of the drug is recommended.

Caution must be exercised when using the drug in cases of severe metabolic acidosis.

When using the drug in patients with pheochromocytoma, alpha-blockers are prescribed before starting therapy.

The use of the drug should be avoided when wearing contact lenses due to a decrease in tear production.

During the period of use of the drug, you should avoid drinking alcohol.

It should be taken into account that if it is necessary to discontinue combination therapy with Carvedilol and clonidine, Carvedilol should be discontinued first, several days before the dose of clonidine is gradually reduced.

Use in pediatrics

The safety and effectiveness of Carvedilol in children and adolescents under 18 years of age have not been established.

Impact on the ability to drive vehicles and operate machinery

It should be borne in mind that at the beginning of treatment and with increasing doses of Carvedilol, blood pressure may decrease excessively, causing dizziness. Therefore, during the treatment period, patients should refrain from engaging in potentially hazardous activities that require increased attention and speed of psychomotor reactions.

Use for renal impairment

The drug is prescribed with caution in case of renal failure.

Use for liver dysfunction

Contraindicated in severe liver failure.

Conditions for dispensing from pharmacies

The drug is available with a prescription.

Overdose

An overdose of Carvedilol can lead to the following symptoms:

• pronounced decrease in blood pressure ;
• arrhythmia with low heart rate;
• respiratory dysfunction;
• heart failure;
• extreme left ventricular failure;
• heart failure.

At the first manifestation of overdose symptoms, you must urgently seek qualified help. You can get rid of the symptoms of overdose by gastric lavage and prescribing adrenergic agonists.

Interaction with other drugs

• Acetohexamide, Insulin - Carvedilol may reduce symptoms of hypoglycemia ;
• Citalopram bradycardia may occur ;
• Clonidine is a manifestation of hypertension ;
• Cyclosporine - Carvedilol may enhance the therapeutic and side effects of Cyclosporine;
• Digoxin - the effect of Digoxin when taken simultaneously with the described drug is enhanced;
• Dihydroergotamine, Ergotamine - ischemia with a risk of gangrene ;
• Adrenaline – development of hypertension and bradycardia ;
• Etravirine - when using Carvedilol and Etravirine (CYP2C9 inhibitor) simultaneously, an increase in the concentration of the active substance in the blood serum may be observed;
• Gliclazide, Glipizide - may reduce symptoms of hypoglycemia;
• - risk of inhibition of renal prostaglandins;
• Indomethacin , Ibuprofen - risk of inhibition of renal prostaglandins;
• Lidocaine - may increase the effect and toxicity of Lidocaine;
• Piroxicam - risk of inhibition of renal prostaglandins;
• Prazosin – risk of hypotension at the beginning of therapy;
• Verapamil - increases the effect of both drugs.

special instructions

At the beginning of the use of Carvedilol and with increasing its dosage, orthostatic hypotension may develop, especially in elderly patients, as well as with heart failure, combination antihypertensive therapy or the use of diuretics.

During the treatment period, it is recommended to monitor renal function in patients with renal failure, coronary heart disease, peripheral vascular pathology, and heart failure. If renal function deteriorates, discontinuation of the drug is required.

Treatment should not be stopped abruptly, especially in patients with angina, as this may worsen the condition. The tablets should be discontinued gradually over 1-2 weeks.

In case of simultaneous therapy with Carvedilol and Clonidine, first stop using the first drug, and then the second.

The use of beta-blockers in the treatment of patients with a history of anaphylactic reactions, peripheral vascular pathology or psoriasis can lead to a deterioration in health, and in Prinzmetal's angina - to the appearance of chest pain.

Carvedilol can reduce the sensitivity of allergy tests, mask the manifestations of hyperthyroidism and early symptoms of acute hyperglycemia. In diabetes mellitus, blood glucose levels should be regularly monitored and hypoglycemic therapy adjusted if necessary.

General anesthesia using drugs such as ether, cyclopropane, trichlorethylene must be carried out with caution during the use of Carvedilol. Before planned major surgical operations, the drug should be discontinued in advance.

For pheochromocytoma, alpha-blockers are prescribed before starting therapy with Carvedilol.

The use of the drug should be avoided in patients who wear contact lenses due to a decrease in tear production.

During the treatment period, you must refrain from drinking alcohol.

It is not recommended to engage in activities that require increased concentration and speed of psychomotor reactions.

Analogues of Carvedilol

Level 4 ATC code matches:
Acridilol

Dilatrend

Coriol

Corvasan

Analogues of Carvedilol by ATC code and composition include the following drugs:

• Atram;
• Carvetrend;
• Carvidex;
• Alotendin;
• Amlodak-AO;
• Anaprilin;
• Aodak-AO;
• Karvedigamma;
• Carvedilol Obolenskoe;
• Carvedilol-KV;
• Carvedilol Hexal;
• Carvedilol-Lugal;
• Carvedilol Sandoz;
• Cardivas;
• Carvidil;
• Credex;
• Talliton;
• Coriol;
• Dilatrend.

Anaprilin

Manufacturer: JSC PFK Update, Russian Federation
Release form: tablets

Active ingredient: propranolol hydrochloride 40 mg

Anaprilin is a cheap analogue of Carvedilol, the price of which is on average 50–70 rubles. The drug has a hypotensive and antiarrhythmic effect, reduces the likelihood of angina pectoris. Anaprilin is used for high blood pressure, tachycardia and angina, as a prevention of myocardial infarction.

The regimen of use and dosage regimen of the medicine depends on the condition and age characteristics.

Reviews of Carvedilol

Reviews about Carvedilol on the forums cannot be called unanimous, but most of them are still positive.

Feedback from one Internet user:

“My mother suffered 2 heart attacks, and therefore regularly ends up in the cardiology department of the local hospital. Recently, her doctor prescribed her to take the drug Carvedilol, first for 2 weeks, half a tablet (12.5 mg), and then 1 tablet (25 mg) per day. After the specified period of taking the medicine, my mother showed noticeable improvements in her health. At least there were no heart attacks. The positive dynamics satisfied the attending physician, but he recommended continuing to take the drug, but gradually reducing the dose. I hope everything will be fine now."

Composition and release form

The drug Carvedilol is round white tablets intended for oral use . According to the instructions, the medication containing the main component 12.5 and 25 mg is distributed in blister packs of 10 pieces. 3 packages are packed into 1 cardboard box. The active substances in the chemical composition demonstrate a pronounced hypotensive effect.

Carvedilol price

The price of Carvedilol is relatively affordable, which sets Carvedilol apart from existing analogues. For example, 12.5 mg tablets, 30 pieces per pack, cost from 99 rubles in pharmacies. But the analogue of the drug Carvedilol-Teva (company Pliva Krakow, Poland) costs 212 - 219 rubles.

• Online pharmacies in RussiaRussia
• Online pharmacies in UkraineUkraine

ZdravCity

• Carvedilol-Akrikhin tablets 25 mg 30 pcs. JSC Akrikhin
  230 rub. order
• Carvedilol tablets 12.5 mg 30 pcs. Ozon LLC

  147 RUR order

• Carvedilol-obl tablets 12.5 mg 30 pcs. JSC Obolenskoe farm. company

  150 rub. order

• Carvedilol Zentiva tablets 6.25 mg 30 pcs. Zentiva s.s.

  185 rub. order

• Carvedilol-Teva tablets 6.25 mg 30 pcs. Pliva Krakow, Pharm. z-d/Teva Operations Poland

  RUB 161 order

Pharmacy Dialogue

• Carvedilol-OBL (tab. 12.5 mg No. 30) Obolenskoye pharmaceutical representative.

  RUB 144 order

• Carvedilol-Teva tablets 25 mg No. 30Teva

  RUB 262 order

• Carvedilol tablets 12.5 mg No. 30 Salutas Pharma GmbH

  RUB 269 order

• Carvedilol tablets 25 mg No. 30Zentiva

  RUB 197 order

• Carvedilol-Akrikhin tablets 12.5 mg No. 30 Akrikhin OJSC

  RUB 208 order

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Pharmacy24

• Carvedilol 12.5 mg N30 tablets PAT "Kiev Vitamin Plant", Kiev, Ukraine
  33 UAH. order
• Carvedilol 25 mg N30 tablets PAT "Kiev Vitamin Plant", Kiev, Ukraine

  45 UAH order

Carvedilol or Bisoprolol – which is better?

Manufacturer: OZONE PHARM LLC, VELFARM LLC, Teva LLC, Russian Federation
Release form: tablets

Active ingredient: bisoprolol fumarate 2.5 mg, 5 mg, 10 mg, 20 mg

Synonyms: Biol, Concor, Coronal, Niperten

Bisoprolol is a substitute for Carvedilol, produced by domestic and foreign pharmaceutical companies. The analogue has antihypertensive, antianginal and antiarrhythmic effects. Bisoprolol is indicated for arterial hypertension, stable angina and CHF.

The medication in the recommended dosage is taken once a day, in the morning, with a small amount of liquid.

If we compare Carvedilol with Bisoprolol, the latter does not affect the resistance of the respiratory tract and other organs.