Bagodolol - instructions for use, dose, side effects, contraindications

Excipients: Povidone K30; silicon dioxide colloidal anhydrous; sodium starch glycolate; sucrose, magnesium stearate; microcrystalline cellulose, iron oxide (III).

Tablets 6.25 mg:

active substance: carvedilol 6.25 mg;

Excipients: Povidone K30; silicon dioxide colloidal anhydrous; sodium starch glycolate; sucrose, magnesium stearate; microcrystalline cellulose.

Tablets 12.5 mg:

active substance: carvedilol 12.5 mg;

Excipients: Povidone K30; silicon dioxide colloidal anhydrous; sodium starch glycolate; sucrose, magnesium stearate; microcrystalline cellulose.

Tablets 25 mg:

active substance: carvedilol 25.0 mg;

Excipients: Povidone K30; silicon dioxide colloidal anhydrous; sodium starch glycolate; sucrose, magnesium stearate; microcrystalline cellulose.

Description:

Tablets 3,125 mg

Red color round biconvex tablets with a risk, with engraved "C" "3" on one side and the logo of the firm on the other side.

Tablets 6.25 mg

White round biconvex tablets with a risk, with engraving "C" "6" on one side and the company logo on the other side.

Tablets 12.5 mg

White round biconvex tablets with a risk, with engraving "C" "12" on one side and the logo of the firm on the other side.

Tablets 25 mg

White round biconvex tablets with a risk, with engraving "C" "25" on one side and the logo of the firm on the other side.

Pharmacotherapeutic group:Alpha- and beta-blocker

ATX: & nbsp

C.07.A.G.02 Carvedilol

Pharmacodynamics:

Carvedilol is a non-selective competitive blocker β₁-, β₂- and α₁ adrenoreceptors, has a combined vasodilating, anti-anginal and antiarrhythmic effect, has a negative chrono-, dromo-, batmo- and inotropic effect, slows conduction in the atrioventricular (AV) node and can reduce the heart rate (heart rate).

A combination of vasodilator and p-adrenoblocking properties of carvedilol is manifested by the following clinical effects:

With arterial hypertension The use of carvedilol is not accompanied by an increase in the total peripheral resistance, as in the case of the use of other β-blockers. As a vasodilator, carvedilol reduces peripheral vascular resistance, and as β-adrenoblocker inhibits the renin-angiotensin-aldosterone system, which leads to a decrease in renin activity in the blood plasma, causes fluid retention in the body and leaves unchanged renal perfusion and their functions. As peripheral circulation also does not change, the sensation of cold extremities with carvedilol is rarely observed, in contrast to the use of β-blockers without vasodilating activity.

Antihypertensive effect occurs 2-3 hours after a single dose and lasts 24 hours. With prolonged treatment, the maximum effect is observed after 3-4 weeks.

With ischemic heart diseasea carvedilol has anti-ischemic and antianginal action. Hemodynamic studies have shown that carvedilol reduces pre- and postnagruzku on the heart.

The favorable effect of carvedilol on the hemodynamics of the heart, the fraction of the ejection of the left ventricle is observed both in dilated cardiomyopathy and in the ischemic form of heart failure. With heart failure carvedilol reduces the end-systolic and end-diastolic volume, as well as peripheral and pulmonary vascular resistance.

The ejection fraction with normal heart function does not change.

In the case of a violation of the function of the left ventricle carvedilol has a beneficial effect on hemodynamic parameters, increases the fraction of ejection of the left ventricle and reduces its size.

Carvedilol has no significant effect on lipid metabolism and K content⁺, Na⁺and Mg²⁺ in the blood plasma.

Pharmacokinetics:

After oral administration, it is rapidly absorbed from the gastrointestinal tract. It is exposed to metabolism at the "first passage" through the liver, bioavailability is approximately 25-35%. In patients with hepatic insufficiency, bioavailability is 80%. The volume of distribution is about 2 l / kg. The maximum concentration (C_mOh) in the blood plasma is reached about 1 hour after ingestion. Pharmacokinetics of carvedilol is linear (concentration in the blood plasma is proportional to the dose taken). Concomitant food intake does not affect the bioavailability and C_mOh, however, the time to achieve the maximum effect can increase. Carvedilol is a lipophilic compound, its binding to plasma proteins reaches more than 96%. It is metabolized predominantly in the liver with the formation of active metabolites with padrenoblokiruyuschey activity, vasodilating and antioxidant properties. The half-life of carvedilol is 6-10 hours. It is excreted mainly with bile, less than 2% is excreted unchanged by the kidneys. Carvedilol and its metabolites can penetrate the placenta, and also excrete with breast milk. Carvedilol practically not removed from the blood during hemodialysis.

In elderly patients The concentration of carvedilol in blood plasma is 50% higher than in young people.

Patients with impaired renal function: as carvedilol is excreted mainly through the gastrointestinal tract, renal dysfunction is not accompanied by its cumulation.

In patients with impaired liver function systemic bioavailability increases due to a decrease in metabolism during the "first passage" through the liver. In severe violations of liver function carvedilol is contraindicated.

Indications:

Arterial hypertension (monotherapy and in combination with diuretics).

Ischemic heart disease: stable angina.

Chronic heart failure (as part of combination therapy).

Contraindications:

Hypersensitivity to carvedilol or other components of the drug, acute and decompensated chronic heart failure, requiring intravenous inotropic drugs, severe hepatic insufficiency, atrioventricular blockade II-III arterial hypotension (systolic blood pressure less than 85 mm Hg), cardiogenic shock, chronic obstructive pulmonary disease, bronchial asthma , age to 18 years (efficacy and safety of use not established).

Carefully:

With bronchospastic syndrome, chronic bronchitis, pulmonary emphysema, Prinzmetal angina, diabetes mellitus, hypoglycemia, thyrotoxicosis, pheochromocytoma (only stabilized by the appointment of α-blockers), peripheral vascular occlusive diseases, AV blockade of the first degree, unstable angina pectoris, impaired renal and hepatic function, decompensated chronic heart failure (IV functional class according to NYHA) depression, myasthenia gravis, psoriasis, in treatment (α₁adrenoblockers or α₂-adrenomimetics, with the joint use of MAO inhibitors, in preparation for surgical interventions and general anesthesia.

Pregnancy and lactation:

Controlled studies of the use of carvedilol in pregnant women have not been carried out, and therefore the prescription of this category of patients is possible only in cases when the benefit to the mother exceeds the potential risk for the fetus.

Not recommended breastfeeding during treatment with carvedilol.

Dosing and Administration:

Inside, regardless of food intake, with enough liquid.

With arterial hypertension: the recommended initial dose of Bagodolol® is 6.25-12.5 mg once a day for 2 days (1 table 12.5 mg in the morning or 1 table 6.25 mg twice daily in the morning and evening). The recommended maintenance dose is 25 mg (1 table 25 mg in the morning or 1 table 12.5 mg 2 times a day - morning and evening). In case of unsatisfactory results, but not earlier than 14 days of treatment, the dose can be increased to a maximum of 50 mg per day (1 table 25 mg twice a day - in the morning and in the evening). The maximum single dose is 25 mg, the daily dose should not exceed 50 mg.

Stable anginaI: the recommended initial dose of Bagololol® is 12.5 mg twice a day (morning and evening) in the first two days of treatment. Then 25 mg twice a day. If the antianginal effect is inadequate after 2 weeks of therapy, the dose may be increased 2-fold. The maximum recommended daily dose of the drug is 100 mg per day, divided into 2 receptions of 50 mg.

Chronic heart failure: the dose should be selected individually, during the dose increase, careful monitoring should be carried out. It is necessary to observe the patient's condition within 2-3 hours after the first intake or after the first increased dose. Additional use requires a stable clinical state. The dose and administration of medications such as digoxin, diuretics, and ACE inhibitors should be recorded before the appointment of Bagodolol®. Patients should take pills during meals (to reduce the risk of orthostatic hypotension).

The recommended initial dose of Bagodolol® is 3,125 mg 2 times a day (morning and evening) for 14 days. If treatment is tolerated by the patient well and there is a need, the dose can be increased to 6.25 mg x 2 times a day.Possible a subsequent increase in the dose to 12.5 mg x 2 times a day (1 table 12.5 mg in the morning and in the evening), then to 25 mg x 2 times a day (1 table 25 mg in the morning and in the evening). Patients are prescribed the maximum tolerated dose. The maximum recommended dose is 25 mg twice a day (1 table 25 mg in the morning and 1 table in the evening) for patients with a body weight of up to 85 kg and 50 mg twice daily (2 tablets, 25 mg in the morning and 2 Table - in the evening) for patients with a body weight of more than 85 kg. Patients with heart failure to prevent orthostatic hypotension are advised to take the drug while eating.

If the treatment is interrupted for more than 2 weeks, the resumption of admission of Bagolol® begins with a dose of 3,125 mg 2 times a day, followed by a dose increase.

Side effects:

From the central nervous system: dizziness, headache (usually not strong at the beginning of treatment), loss of consciousness, myasthenia gravis (often at the beginning of treatment), fatigue, depression, sleep disturbance, paresthesia.

From the side of the cardiovascular system: bradycardia, orthostatic hypotension, atrioventricular blockade of II-III st., rarely - violation of peripheral circulation, progression of heart failure (in the period of increasing doses), swelling of the lower extremities, angina,marked reduction in blood pressure.

From the side of the digestive tract: dry mouth, nausea, diarrhea or constipation, vomiting, abdominal pain, loss of appetite, increased activity of "liver" transaminases.

On the part of the hematopoiesis system: rarely - thrombocytopenia, leukopenia.

From the side of metabolism: increase in body weight, violation of carbohydrate metabolism.

Allergic reactions: skin allergic reactions, exacerbation of psoriasis, nasal congestion.

From the respiratory system: dyspnea and bronchospasm (in predisposed patients).

Other: impaired vision, reduced tearing, flu-like syndrome, sneezing, myalgia, arthralgia, pain in the extremities, "intermittent" lameness, rarely - urination disorder, renal dysfunction.

Overdose:

Symptoms: marked reduction in blood pressure (accompanied by dizziness or fainting), bradycardia (less than 50 beats per minute). There may be shortness of breath due to bronchospasm. In severe cases, cardiogenic shock, respiratory failure, confusion, AV conduction, hypoglycemia.

Treatment: it is necessary to monitor and correct vital signs, if necessary - in the intensive care unit. Treatment is symptomatic. It is expedient to use intravenous m-holinoblokatorov (atropine), adrenomimetics (epinephrine, norepinephrine).

Interaction:

Carvedilol should be used with caution at the same time:

- with funds depleting supplies of catecholamines (reserpine, MAO inhibitors). possible pronounced bradycardia and lowering blood pressure;

- with blockers of "slow" calcium channels (verapamil, diltiazem) and antiarrhythmic drugs (especially I class), because they can provoke a marked decrease in blood pressure and heart failure. In / in the administration of these drugs in conjunction with the use of carvedilol is contraindicated.

- with alpha and beta-adrenomimetics because of the possibility of increasing blood pressure, expressed reflex bradycardia and asystole, as well as reducing β-adrenoblocking action of carvedilol;

- clonidine and carvedilol can enhance the ability of each other to reduce blood pressure and heart rate; When combined, the cancellation should be done gradually: at first it is excluded carvedilol, then, in a few days, the clone dine can be gradually phased out;

- with digoxin, t. slows down AV conductivity;

- with insulin and hypoglycemic agents for oral administration because of the increase hypotensive action and masking of symptoms of hypoglycemia;

- with nitrates and hypotensive drugs (clonidine, guanethidine, methyldopa, guanfacine and others) because of the intensification of hypotensive action and a decrease in heart rate;

- with funds for anesthesia due to their negative inotropic action and hypotensive effect;

- with agents that affect the central nervous system (hypnotics, tranquilizers, tricyclic antidepressants and ethyl alcohol), because of the possibility of mutual enhancement of effects;

- with non-steroidal anti-inflammatory drugs due to a decrease in hypotensive effect due to decreased production of prostaglandins;

- with ergotamine: it is necessary to take into account the vasoconstrictive effect of ergotamine;

- with xanthine derivatives (aminophylline, theophylline) due to a decrease in β-adrenergic blocking action.

Because the carvedilol is subjected to oxidative metabolism, its pharmacokinetics can change with the induction or inhibition of the enzymatic system of cytochrome P450, therefore the influence of:

- Rifampicin, t.there is a 70% reduction in serum carvedilol concentrations;

- barbiturates, tk. they reduce the action of carvedilol;

- inhibitors of isoenzyme CYP2D6 (quinidine, fluoxetine, paroxetine, propafenone): we can assume an increase in concentration R(+) carvedilol enantiomer;

- cimetidine, t.p. it increases the bioavailability of carvedilol by 30%.

Carvedilol delays the metabolism of cyclosporine, increases the concentration of digoxin in the blood plasma.

Special instructions:

Therapy should be carried out for a long time and should not abruptly cease, especially in patients with coronary heart disease, since this can lead to a worsening of the course of the underlying disease. If necessary, the dose reduction should be gradual, within 1-2 weeks.

At the beginning of therapy with carvedilol or with an increase in the dose of the drug in patients, especially the elderly, there may be an excessive decrease in blood pressure, mainly on rising. A dose adjustment is necessary. In patients with chronic heart failure, the choice of a dose may increase the symptoms of heart failure, the appearance of edema.In this case, do not increase the dose of carvedilol, recommended the appointment of large doses of diuretics until the stabilization of the patient.

It is recommended to continuously monitor the electrocardiogram and blood pressure with the simultaneous administration of carvedilol and blockers of "slow" calcium channels, phenylalkylamine derivatives (verapamil) and benzodiazepine (diltiazem), and also with antiarrhythmic agents of the first class, intravenous administration of which should be avoided when taking carvedilol.

In patients taking digitalis preparations, diuretics and ACE inhibitors, dosages of these drugs should be stabilized before treatment with carvedilol.

It is recommended to monitor kidney function in patients with chronic renal failure, arterial hypotension and chronic heart failure.

Tranquilizers (barbiturates, phenothiazines), tricyclic antidepressants, vasodilators - can enhance the hypotensive effect of carvedilol. In the case of a surgical procedure using general anesthesia, an anesthesiologist should be alerted to prior carvedilol therapy.

Carvedilol does not affect the concentration of glucose in the blood and does not cause changes in the glucose tolerance test in patients with non-insulin dependent diabetes mellitus.

Patients with diabetes mellitus, who are characterized by significant fluctuations in glycemia, and patients on a strict diet require special attention in carvedilol treatment. The level of glucose should be monitored particularly carefully.

Taking carvedilol can mask the symptoms of thyrotoxicosis.

During the treatment should be avoided the use of ethanol.

Patients with pheochromocytoma prior to initiation of therapy should be assigned alpha-blockers.

Patients wearing contact lenses should note that the drug can cause a decrease in tearing.

In patients suffering from psoriasis, symptoms may worsen. Carvedilol can cause (psoriasis-like) skin irritation and exacerbation of Raynaud's disease.

Carvedilol, like other β-blockers, can increase sensitivity to allergens and the severity of anaphylactic reactions.

Effect on the ability to drive transp. cf. and fur:

It is not recommended to drive at the beginning of therapy and with increasing doses of carvedilol.It is necessary to refrain from other activities associated with the need for high concentration of attention and rapid psychomotor reactions.

Form release / dosage:

Tablets 3,125 mg, 6.25 mg, 12.5 mg and 25 mg.

Packaging:

For 14 tablets in a blister of the film PA / A1 / PVC-aluminum foil.

For 2 blisters in a cardboard box with instructions for use.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-001043/09

Date of registration:12.02.2009

Expiration Date:Unlimited

The owner of the registration certificate: Laboratorios Bago S.A. Laboratorios Bago S.A. Argentina

Manufacturer: & nbsp

Laboratorios BAGO, S.A. Argentina

Representation: & nbspBBC FARMA BV BBC FARMA BV Netherlands

Information update date: & nbsp11.01.17

Illustrated instructions

Instructions

Bagolol® (Bagodilol®)