Medicine - Concor

Compatibility of Nebivolol and alcohol

? If both substances are consumed simultaneously, the following effects occur for the human body:

• penetration of drugs, ethanol into the central nervous system, which causes depression, decreased attention, sleep disturbance, hallucinations;
• decreased therapeutic effect, since ethanol affects the kidneys, causing excessive urine excretion along with the medicine;
• toxic effect on the liver, which tries to remove both substances from the body, so hepatocytes are damaged and organ function decreases;
• deterioration of the patient’s well-being with heart failure with a high risk of death.

The impact on the human body is gradually increasing. Therefore, before irreversible consequences occur, the patient should stop using both substances.

Side effects

Taking Concor may be accompanied by side effects:

• From the nervous system: increased fatigue, dizziness, headache, sleep disturbances, depression may be observed (especially at the beginning of therapy), rarely - hallucinations (usually mild and disappear within 1-2 weeks), sometimes - paresthesia.
• On the part of the organ of vision: visual disturbances, decreased tear production (must be taken into account when wearing contact lenses), conjunctivitis.
• From the cardiovascular system: in some cases - orthostatic hypotension, bradycardia, AV conduction disturbances, decompensation of heart failure with the development of peripheral edema, at the beginning of treatment - deterioration of the condition of patients with intermittent claudication or Raynaud's syndrome.
• From the respiratory system: in isolated cases - shortness of breath (in patients prone to bronchospasm).
• From the gastrointestinal tract: in some cases - diarrhea, constipation, nausea, abdominal pain, increased activity of liver enzymes in the blood serum (AST, ALT), hepatitis.
• From the musculoskeletal system: in some cases - muscle weakness, cramps, arthropathy affecting one or more joints (mono- or polyarthritis).
• From the endocrine system: decreased glucose tolerance (with latent diabetes mellitus) and masking of signs of hypoglycemia, in some cases - increased TG levels in the blood, potency disorders.
• On the skin: sometimes - itching, skin hyperemia, increased sweating, rash. When treated with beta-adrenergic receptor blockers, hair loss, hearing impairment or tinnitus, weight gain, mood changes, short-term memory loss, allergic rhinitis, and priapism are observed in some cases.

Brief characteristics of the drug

This is a drug from the group of 3rd generation cardioselective beta-blockers.

Due to the active substance of the same name, the following effects occur in the body:

• decrease in heart rate, pressure;
• reducing the load on the heart;
• vasodilation in patients with coronary heart disease;
• restoration of heart rhythm.

The effects of the drug occur gradually when the active component accumulates in the tissues.

Indications for use:

• high blood pressure;
• coronary heart disease, angina pectoris;
• chronic heart failure.

Adverse reactions:

• headache, dizziness, sudden mood swings, depression, numbness of extremities, sleep disturbance, fainting, hallucinations;
• dyspeptic reactions, dry mouth, increased gas formation, changes in stool;
• excessive decrease in heart rate up to bradycardia, excessive decrease in blood pressure, swelling, acute myocardial failure, cardiac arrhythmia;
• allergic skin reactions, angioedema, rarely psoriasis;
• bronchospasm.

Contraindications for use:

• decompensated chronic heart failure, low blood pressure and heart rate, cardiogenic shock;
• adrenal tumor;
• acidosis in the blood and tissues;
• serious pathologies of liver tissue;
• minor age;
• psychological disorders, depression;
• hypersensitivity to 1 of the components of the product.

The medicine is prescribed to pregnant and lactating women, but only for vital signs, when the effect of the medicine outweighs the risk of side effects. The drug can be used for kidney pathology, but with great caution.

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Contraindications

Concor should not be used for the following diseases:

• cardiogenic shock;
• acute heart failure;
• chronic heart failure (CHF) in the stage of decompensation, which requires the use of inotropic therapy;
• sinoatrial block;
• atrioventricular (AV) block of II–III degree in patients without a pacemaker;
• severe bradycardia with heart rate less than 60 beats per minute;
• sick sinus syndrome;
• severe arterial hypotension [systolic blood pressure (BP) below 100 mmHg];
• Raynaud's syndrome or severe peripheral arterial circulation disorder;
• severe form of bronchial asthma;
• chronic obstructive pulmonary disease in severe form;
• metabolic acidosis;
• pheochromocytoma (without simultaneous use of alpha-blockers);
• age under 18 years;
• breastfeeding period;
• hypersensitivity to the components of the drug.

Use of the drug for alcoholism

If a patient suffers from alcoholism against the background of cardiovascular disorders, his condition worsens sharply. Central nervous system pathologies occur in the form of convulsions, hallucinations, headaches, delirium, depression, and delirium tremens.

An increased effect on the kidneys and liver is formed, which causes alcoholic hepatitis, fibrosis, cirrhosis, glomerulonephritis, and organ failure.

If you start drug therapy against the background of alcohol disorders, the patient’s well-being will worsen. The risk of heart attack and stroke increases with diseases of the cardiovascular system.

The patient experiences disorders of the central and peripheral nervous system with high frequency. Gradually he does not realize who he is or where he is. Chronic kidney and liver diseases are getting worse.

Doses and method of administration Concor

Dosage and method of use of the drug Concor

Concor is taken orally (do not chew or crush) once a day with a glass of water, regardless of meals. But there is a dependence on the time of day. The medicine should be taken exclusively in the first half of the day, that is, you cannot take Concor during the day, evening or at night.

As for the duration of therapy, it is determined by the body’s reaction and the decision of the attending physician.

• Arterial hypertension and angina pectoris

The dose of the drug is calculated taking into account the heart rate and general condition of the patient.

To begin with, Concor is prescribed 5 mg, one tablet per day. Then they go up to 10 mg. And in the treatment of hypertension and angina pectoris, the maximum recommended dose is 20 mg per day.

• Chronic heart failure without signs of exacerbation

Initially, 1.25 mg once a day. If the patient tolerates the dosage well, then it is gradually increased every two weeks to 2.5 mg, 3.75 mg, 5 mg, 7.5 mg and 10 mg.

If the dosage is poorly tolerated, then it should be reduced. The maximum recommended dose is 10 mg per day.

Consequences of drinking alcohol

If a person simultaneously uses substances, the following consequences arise:

• blood pressure rises and falls, which leads to the formation of a hypertensive crisis;
• the heart rate increases, there is an increased load on the heart, creating a risk of heart attack;
• substances penetrate the brain, leading to a change in a person’s psycho-emotional background, he becomes depressed, aggressive, apathetic;
• Nausea and vomiting occur; often the medicine is eliminated from the body along with vomit, so there is no therapeutic effect;
• diuresis increases, so most of the active component of the drug is excreted from the body, reducing the quality of therapy.

All consequences that occur in the internal organs and systems of a person threaten his life and health. A hypertensive crisis, heart attack, stroke, or death can occur at any moment.

When can you take the drug, after how long

How long after you can take the medicine depends on the degree of addiction to alcoholic beverages and the concentration of ethanol in the blood:

• periodic consumption of small doses of alcoholic beverages – 1 day after the last intake;
• frequent consumption of drinks based on ethyl alcohol without the formation of dependence - at least 1 week;
• alcoholism – treatment of cardiovascular pathologies is possible only after treatment in a drug treatment clinic; at least 5 weeks must pass from the moment the last dose was taken

The sooner a person gives up alcohol, the higher the opportunity to keep the disease under control.

Nebivolol and beer

Nebivolol and beer are incompatible. This is a cardioselective beta blocker. The medicine should not be taken with beer or other alcoholic beverages.

This will lead to an exacerbation of the underlying disease, a deterioration in the person’s well-being, and an increased risk of hypertensive crisis due to surges in blood pressure. A heart attack may occur due to disruption of blood flow to the heart muscle.

When a patient constantly drinks beer and the drug, there is an increased load on the liver, the organ becomes inflamed, and liver transaminases increase. If the remedy is not canceled, the parenchyma will begin to be replaced by connective tissue.

Organs affected by the toxin

The combined use of pharmacological agents and alcohol has a toxic effect on the internal organs and environments of the body. Alcohol, entering into a chemical reaction with a medicine, leads to poisoning, disrupts physiological processes, enhances or weakens the healing properties of drugs.

The liver suffers more than other organs. She gets hit twice. Many medications have a side effect - hepatotoxicity, destroy cells, and disrupt the physiology of the organ. In the liver, alcohol breaks down to ethanal, a substance 20-30 times more toxic than ethanol, which causes the death of hepatocytes.

Dangerous groups of drugs for the organ in combination with alcohol:

• anti-inflammatory;
• hormonal;
• antibacterial;
• antifungal;
• glucose control agents for diabetes mellitus;
• anti-tuberculosis;
• cytostatics (chemotherapy drugs);
• tranquilizers (anti-epileptic, psychotropic).

In second place among the internal organs exposed to the harmful effects of alcohol together with medications are the heart and vascular system. Strong drinks during drug therapy constrict blood vessels and increase blood pressure. The simultaneous intake of alcohol and chemical substances leads to failure of the myocardium and increases the risk of developing an attack of angina pectoris and a heart attack.

A mixture of ethanol and pharmaceuticals disrupts the quality of the blood and reduces clotting. This is dangerous due to internal bleeding and strokes.

Nebivolol

Pharmacodynamic interaction

Concomitant use with floctafenine is contraindicated: nebivolol can interfere with compensatory reactions of the cardiovascular system associated with arterial hypotension or shock, which can be caused by floctafenine.

The simultaneous use of nebivolol and sultopride is contraindicated, since with their simultaneous use there is an increased risk of ventricular arrhythmia, especially polymorphic ventricular tachycardia of the “pirouette” type.

Combinations not recommended

When used simultaneously with class I antiarrhythmic drugs (quinidine, hydroquinidine, flecainide, cibenzoline, disopyramide, lidocaine, mexiletine, propafenone), the negative inotropic effect may be enhanced and the time of excitation through the atrioventricular node may be prolonged.

With the simultaneous use of beta-blockers with blockers of “slow” calcium channels (SCBC) (verapamil and diltiazem), the negative effect on myocardial contractility and atrioventricular conduction increases. Intravenous administration of verapamil is contraindicated while taking nebivolol.

When used simultaneously with centrally acting antihypertensive drugs (clonidine, guanfacine, moxonidine, methyldopa, rilmenidine), the course of heart failure may worsen due to a decrease in sympathetic tone (decreased heart rate and cardiac output, symptoms of vasodilation). In case of abrupt withdrawal of these drugs, especially before discontinuation of nebivolol, the development of “rebound” arterial hypertension (withdrawal syndrome) is possible.

Combinations to use with caution

When used simultaneously with class III antiarrhythmic drugs (amiodarone), the effect on conduction time through the atrioventricular node may be enhanced.

When nebivolol is used simultaneously with insulin and oral hypoglycemic agents, the symptoms of hypoglycemia (rapid heartbeat, tachycardia) may be masked.

The simultaneous use of nebivolol and drugs for general anesthesia may suppress reflex tachycardia and increase the risk of developing arterial hypotension.

Simultaneous use of nebivolol with baclofen, amifostine, and antihypertensive drugs can cause a significant drop in blood pressure, so dose adjustment of antihypertensive drugs is required.

Combinations to Consider

With simultaneous use of nebivolol with cardiac glycosides, atrioventricular conduction may slow down. Nebivolol does not affect the pharmacokinetic parameters of digoxin.

The simultaneous use of nebivolol and dihydropyridine BMCC (amlodipine, felodipine, lacidipine, nifedipine, nicardipine, nimodipine, nitrendipine) may increase the risk of arterial hypotension. An increased risk of further reduction in myocardial contractility in patients with heart failure cannot be excluded.

When nebivolol is used simultaneously with antihypertensive drugs, nitroglycerin, severe arterial hypotension may develop (special caution is required when combined with prazosin).

The simultaneous use of tricyclic antidepressants, barbiturates and phenothiazine derivatives, anxiolytics, and hypnotics may enhance the antihypertensive effect of nebivolol.

There is no clinically significant interaction between nebivolol and nonsteroidal anti-inflammatory drugs (NSAIDs). Acetylsalicylic acid as an antiplatelet agent can be used simultaneously with nebivolol. When used concomitantly, sympathomimetic agents may inhibit the activity of beta-blockers.

Theoretically, concomitant use of mefloquine with nebivolol may lead to prolongation of the QT interval.

Pharmacokinetic interactions

When nebivolol is used in combination with drugs that inhibit serotonin reuptake or other drugs metabolized by the CYP2D6 isoenzyme (for example, paroxetine, fluoxetine, thioridazine, quinidine), the metabolism of nebivolol slows down, the concentration of nebivolol in the blood plasma increases, which may lead to a risk the occurrence of bradycardia and other side effects.

When used simultaneously with cimetidine, it is possible to increase the concentration of nebivolol in the blood plasma (there are no data on the effect on the pharmacological effects of the drug).

Concomitant use of ranitidine had no effect on the pharmacokinetic parameters of nebivolol.

Rifampin increases the metabolism of nebivolol.

With simultaneous use of nebivolol with nicardipine, the concentrations of active substances in the blood plasma increase slightly without changing the clinical effect.

Concomitant use of ethanol, furosemide or hydrochlorothiazide does not affect the pharmacokinetics of nebivolol.

No clinically significant interaction between nebivolol and warfarin has been established.

Rules for taking medications and alcohol

Drinking alcohol during treatment minimizes the clinical effect of therapy and creates a risk of developing complications of the disease.

If this cannot be avoided, follow the rules of behavior that will reduce the occurrence of negative consequences:

1. Do not drink strong drinks (vodka, cognac, whiskey), choose dry wine (100-150 ml), beer (no more than 300 ml). Don't drink alcohol on an empty stomach.
2. The interval between taking the medicine and alcohol should be at least 2 hours.
3. To reduce the toxic effect, take medications that protect the liver (hepatoprotectors), pancreas (pancreatin), and stomach (antacids ─ Rennie, Almagel).

If a person takes antiviral medications for colds, anti-inflammatory drugs, alcohol in moderation does not pose a threat to the body.

Alcoholic drinks during treatment are strictly contraindicated in cases of liver cirrhosis, severe infectious diseases, and during a course of chemotherapy.

Medicines, alcohol and chronic diseases

If a person has chronic diseases, simultaneous use of alcohol and medications is potentially dangerous for the functioning of vital organs. Since patients systematically take prescribed medications, the influence of alcohol can lead to negative consequences.

People with chronic heart disease (angina pectoris, heart defects) develop arrhythmias of varying severity. Heart attacks with severe pain syndrome develop, which is not relieved by Nitroglycerin, and the risk of developing myocardial infarction increases significantly.

In case of chronic liver diseases (viral hepatitis, hepatosis), alcohol during treatment can become a trigger in the development of cirrhosis and hepatocellular carcinoma (cancer).

Drinking alcohol during cirrhosis leads to the following consequences:

• bleeding into the abdominal cavity;
• liver decomposition, infection, peritonitis;
• hepatic coma;
• death.

If a person is on long-term treatment with sedatives, psychotropic drugs, tranquilizers, he is contraindicated in drinking alcohol. This leads to severe depression and the appearance of obsessive states (hallucinations, phobias). Suicidal feelings develop. Such a patient needs constant monitoring and assistance from a psychiatrist.

Nebivolol tablets 5 mg No. 28

Compound

Active substance: nebivolol hydrochloride in an amount equivalent to 5 mg of nebivolol.
Excipients: lactose monohydrate 147.15 mg, microcrystalline cellulose 35.00 mg, povidone 6.00 mg, croscarmellose sodium 4.00 mg, polysorbate-80 0.40 mg, magnesium stearate 2.00 mg.

Pharmacokinetics

Suction

After oral administration, both enantiomers of nebivolol are rapidly absorbed from the gastrointestinal tract. Eating does not affect absorption. Bioavailability averages 12% in patients with rapid metabolism (first-pass effect) and is almost complete in patients with slow metabolizers.

Distribution

Plasma clearance in most patients (with rapid metabolism) is achieved within 24 hours, and for hydroxymetabolites - after several days. Plasma concentrations of 1-30 mcg/l are proportional to the dose.

The binding to plasma proteins (mainly albumin) for D-nebivolol is 98.1%, for L-nebivolol - 97.9%.

Metabolism

Nebivolol is actively metabolized, partially with the formation of active hydroxymetabolites. The metabolism of nebivolol occurs through alicyclic and aromatic hydroxylation, partial N-dealkylation and glucuronidation, in addition, glucuronides of hydroxymetabolites are formed. The rate of metabolism of nebivolol by aromatic hydroxylation is genetically determined by oxidative polymorphism and depends on the CYP2D6 isoenzyme.

Removal

A week after administration, 38% (the amount of unchanged active substance is less than 0.5%) of the dose is excreted by the kidneys and 48% through the intestines. In patients with rapid metabolism, the half-life of nebivolol enantiomers from blood plasma averages 10 hours. In patients with slow metabolism, these values ​​increase by 3-5 times.

In patients with rapid metabolism, the half-life of hydroxymetabolites of both enantiomers from blood plasma averages 24 hours; in patients with slow metabolizers, these values ​​increase approximately 2-fold. Given differences in metabolic rates, the dose of the drug should always be individualized: patients with slow metabolism require a lower dose. Pharmacokinetic parameters do not have age or gender differences.

Indications for use

- arterial hypertension,

- coronary heart disease: prevention of angina attacks,

chronic heart failure (as part of combination therapy).

Contraindications

Symptoms:

Marked decrease in blood pressure, severe bradycardia, acute heart failure, atrioventricular block, cardiogenic shock, cardiac arrest, bronchospasm, loss of consciousness, convulsions, coma, nausea, vomiting, hypoglycemia, cyanosis. Treatment:

Gastric lavage, taking activated carbon. In case of a pronounced decrease in blood pressure, it is necessary to place the patient in a horizontal position with elevated legs, and, if necessary, administer intravenous fluid and vasopressors. For bradycardia, 0.5 - 2 mg of atropine should be administered intravenously; if there is no positive effect, a transvenous or intracardiac pacemaker may be installed. In case of atrioventricular block (N-III stage), intravenous administration of beta-adrenergic stimulants is recommended; if they are ineffective, the issue of installing an artificial pacemaker should be considered. In case of heart failure, treatment begins with the administration of cardiac glycosides and diuretics; if there is no effect, it is advisable to administer dopamine, dobutamine or vasodilators. For bronchospasm, betag-agonists are used intravenously. For ventricular extrasystole - lidocaine (class IA antiarrhythmic drugs cannot be administered). For convulsions, intravenous administration of diazepam. For hypoglycemia, intravenous dextrose (glucose) may be indicated.

Directions for use and doses

Orally, at the same time, regardless of the time of meal, without chewing and with a sufficient amount of liquid.

Arterial hypertension and coronary heart disease

The average daily dose is 2.5-5 mg (1/2 tablet - 1 tablet of 5 mg) 1 time / day. The optimal therapeutic effect is achieved after 1-2 weeks of treatment, in some cases - after 4 weeks.

If necessary, the dose can be increased to a maximum daily dose of 10 mg (2 tablets of 5 mg in one dose). The maximum daily dose is 10 mg (2 tablets of 5 mg).

The drug can be used in monotherapy or in combination with other antihypertensive drugs.

Patients with renal failure:

The initial dose is 2.5 mg (1/2 tablet of 5 mg) 1 time/day. If necessary, the daily dose can be increased to 5 mg.

Patients with liver failure:

Experience with the use of nebivolol in patients with liver failure is limited, so the drug should be prescribed with caution. For patients with mild to moderate liver failure, the recommended initial dose is 2.5 mg (1/2 tablet of 5 mg) 1 time / day; if necessary, the daily dose of the drug can be increased to 5 mg. The effect of nebivolol in patients with severe hepatic impairment has not been studied, therefore the use of nebivolol in severe hepatic impairment is contraindicated.

Elderly patients:

For patients over 65 years of age, the initial dose is 2.5 mg (1/2 tablet of 5 mg). If necessary, the daily dose can be increased to 5 mg. However, given the limited experience with the drug in elderly patients, nebivolol should be prescribed with caution and careful evaluation of patients over 65 years of age.

Chronic heart failure

Treatment of stable chronic heart failure should begin with gradual titration of the dose until an individual optimal maintenance dose is achieved. Patients must not have had an episode of acute heart failure in the past 6 weeks. It is recommended to carry out treatment under close medical supervision.

For patients taking diuretics, cardiac glycosides, angiotensin-converting enzyme (ACE) inhibitors, angiotensin II receptor antagonists, drug doses should be stable for at least two weeks before starting Nebivolol therapy.

It is necessary to begin treatment of chronic heart failure with beta-adrenergic receptor blockers if the patient’s condition has been clinically stable for the last 2 weeks. Dose selection at the beginning of therapy should be carried out according to the following scheme, maintaining 2-week intervals: the initial dose of 1.25 mg/day (1/4 tablet of 5 mg) can be increased to 2.5 mg/day (1/ 2 tablets of 5 mg), then up to 5-10 mg/day (1-2 tablets of 5 mg). The maximum daily dose is 10 mg (2 tablets of 5 mg).

Each dose increase should be carried out at least after 2 weeks, depending on the individual tolerability of the drug.

The initiation of therapy and each increase in the dose of the drug should be carried out under the strict supervision of a physician, at least during the first 2 hours. During titration, regular monitoring of blood pressure, heart rate and symptoms of chronic heart failure is recommended.

Treatment of stable chronic heart failure is usually long-term. Treatment with Nebivolol is not recommended to be stopped abruptly, as this may lead to a temporary exacerbation of chronic heart failure. If it is necessary to stop taking the drug, discontinuation is carried out gradually, reducing the dose by half over the course of a week.

Patients with renal failure:

In case of mild to moderate renal failure (creatinine clearance more than 20 ml/min), there is no need for dose adjustment, so it is necessary to select the dose individually, gradually increasing it to the maximum tolerated. There is no experience with the use of nebivolol in patients with severe renal dysfunction (creatinine clearance less than 20 ml/min), so its use in such patients is not recommended.

Patients with liver failure:

Experience with the use of nebivolol in patients with hepatic insufficiency is limited, so the drug should be prescribed with caution to patients with mild to moderate hepatic insufficiency, the dose should be selected individually, gradually increasing to the maximum tolerated, if necessary, the daily dose of the drug can be increased to 5 mg / day (1 tablet of 5 mg). The effect of nebivolol in patients with severe hepatic impairment has not been studied, therefore the use of nebivolol in severe hepatic impairment is contraindicated.

Elderly patients:

There is no need for dose adjustment, so it is necessary to individually select the dose, gradually increasing it to the maximum tolerated.

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25 C.

Keep out of the reach of children.

Best before date

2 years. Do not use after expiration date.

special instructions

It is unacceptable to abruptly stop taking beta-blockers (with abrupt cessation of treatment, withdrawal syndrome may develop); if possible, treatment should be stopped gradually, reducing the dose over 10 days (1-2 weeks in patients with coronary heart disease).

Treatment of chronic heart failure with nebivolol is carried out against the background of stable indicators of the cardiovascular system, no earlier than 6 weeks after the end of the decompensation period. Nebivolol can be used for the treatment of chronic heart failure simultaneously with thiazide diuretics, digoxin, ACE inhibitors or angiotensin II receptor antagonists.

For stable angina, the selected dose should ensure that the heart rate at rest is within 55-60 beats/min, and during exercise - no more than 110 beats/min. Beta blockers can cause bradycardia: the dose should be reduced if the heart rate is less than 55-60 beats/min.

Beta blockers should be used with caution in patients with chronic obstructive pulmonary disease, as bronchospasm may increase.

In smoking patients, the effectiveness of beta-blockers is lower.

Nebivolol has no effect on glucose concentrations in patients with diabetes, however, under the influence of nebivolol, signs of hypoglycemia (tachycardia, palpitations) caused by the use of hypoglycemic agents may be masked.

Beta-blockers should be used with caution in patients with hyperthyroidism due to the fact that clinical signs of hyperthyroidism, such as tachycardia, may be masked by nebivolol. Abrupt withdrawal of the drug can cause exacerbation of symptoms of the disease and the development of thyrotoxic crisis.

Monitoring of patients taking beta-blockers includes monitoring heart rate and blood pressure (daily at the beginning of treatment, then once every 3-4 months), blood glucose concentration in patients with diabetes mellitus (once every 4 months). -5 months).

In elderly patients, it is recommended to monitor renal function (once every 4-5 months). Nebivolol may increase symptoms of peripheral circulatory disorders. Beta blockers may increase sensitivity to allergens and the severity of anaphylactic reactions. Nebivolol may cause severe reactions to a number of allergens when administered to patients with a history of severe anaphylactic reactions to these allergens. These patients may not respond to the usual doses of epinephrine (adrenaline) used to treat anaphylactic shock.

When deciding whether to prescribe the drug to patients with psoriasis, the expected benefits of using the drug should be carefully weighed against the possible risk of exacerbation of psoriasis.

Patients who use contact lenses should take into account that during treatment with beta-blockers, there may be a decrease in the production of tear fluid.

If during therapy with Nebivolol the patient requires surgical intervention, it is necessary to inform the surgeon and/or anesthesiologist about the nature of the therapy being performed.

Description

tablets are white or almost white, round, flat-cylindrical in shape, with a chamfer and a cross-shaped mark on one side.

Conditions for dispensing from pharmacies

On prescription

Dosage form

pills

Manufacturer and organization accepting consumer complaints

Berezovsky Pharmaceutical Plant, JSC

Pharmacodynamics

Cardioselective beta-blocker with vasodilating properties. Nebivolol has antihypertensive, antianginal and antiarrhythmic effects. Reduces high blood pressure (BP) at rest, during physical exertion and stress. Competitively and selectively blocks postsynaptic beta-adrenergic receptors, making them inaccessible to catecholamines, modulates the release of endothelial vasodilating factor nitric oxide. Nebivolol is a racemate consisting of two enantiomers: D-nebivolol (SRRR-nebivolol) and L-nebivolol (RSSS-nebivolol), combining two pharmacological actions:

— D-nebivolol is a competitive and highly selective beta)-adrenergic receptor blocker,

— L-nebivolol has a mild vasodilator effect by modulating the release of vasodilating factor from the vascular endothelium.

The antihypertensive effect is also due to a decrease in the activity of the renin-angiotensin-aldosterone system (RAAS) (does not directly correlate with changes in renin activity in the blood plasma).

A stable antihypertensive effect develops after 1-2 weeks of regular use of the drug, and in some cases - after 4 weeks; a stable effect is observed after 1-2 months.

By reducing myocardial oxygen demand (decrease in heart rate (HR), decrease in preload and afterload), nebivolol reduces the number and severity of angina attacks and increases exercise tolerance. The antiarrhythmic effect is due to the suppression of pathological automatism of the heart (including in the pathological focus) and the slowing of atrioventricular conduction.

Side effects

The frequency of side effects listed below was determined according to the World Health Organization classification: very common (more than 10%), common (more than 1% and less than 10%), uncommon (more than 0.1% and less than 1%), rare (more than 0). .01% and less than 0.1%), very rarely (less than 0.01%), including isolated reports.

Nervous system disorders: often: headache, dizziness, fatigue, weakness, paresthesia, infrequently, depression, nightmares, confusion, insomnia, very rarely, fainting, hallucinations.

Gastrointestinal disorders: often: nausea, constipation, diarrhea, infrequently: dyspepsia, flatulence, vomiting.

Disorders of the cardiovascular system: often: peripheral edema, infrequently: bradycardia, heart failure, atrioventricular block, orthostatic hypotension, Raynaud's syndrome, cardiac arrhythmias, cardialgia, worsening of chronic heart failure, marked decrease in blood pressure.

Disorders of the skin and subcutaneous tissues: infrequently: erythematous skin rash, itching, very rarely, aggravation of psoriasis, in some cases: angioedema, alopecia.

Disorders of the respiratory system: often: shortness of breath, infrequently: bronchospasm (including in the absence of a history of obstructive pulmonary diseases).

Other:

Uncommon: visual disturbances, impotence, photosensitivity reactions, hyperhidrosis, Rare: dry eye mucosa.

Use during pregnancy and breastfeeding

Nebivolol may have harmful effects on pregnancy, the fetus and the newborn. Reduced placental perfusion under the influence of beta-blockers can cause fetal growth restriction, intrauterine fetal death, miscarriage and premature birth. Newborns may experience bradycardia, decreased blood pressure, hypoglycemia, and respiratory paralysis.

Use during pregnancy is possible only if the expected benefit to the mother outweighs the potential risk to the fetus. Nebivolol should be stopped 48-72 hours before birth. In cases where this is not possible, it is necessary to ensure strict monitoring of newborns for 48-72 hours after birth. Nebivolol is excreted in breast milk. If it is necessary to use the drug during lactation, breastfeeding should be stopped.

Interaction

Pharmacodynamic interaction

With the simultaneous use of beta-blockers with slow calcium channel blockers (SCBC) (verapamil and diltiazem), the negative effect on myocardial contractility and atrioventricular conduction increases. Intravenous administration of verapamil is contraindicated while taking nebivolol.

When nebivolol is used simultaneously with antihypertensive drugs, nitroglycerin, severe arterial hypotension may develop (special caution is required when combined with prazosin).

The simultaneous use of nebivolol and dihydropyridine BMCC (amlodipine, felodipine, lacidipine, nifedipine, nicardipine, nimodipine, nitrendipine) may increase the risk of arterial hypotension.

The possibility of a further decrease in myocardial contractility in patients with chronic heart failure cannot be excluded.

When used simultaneously with centrally acting antihypertensive drugs (clonidine, guanfacine, moxonidine, methyldopa, rilmenidine), the course of heart failure may worsen due to a decrease in sympathetic tone (decreased heart rate and cardiac output, symptoms of vasodilation). If these drugs are abruptly discontinued, especially before nebivolol is discontinued, rebound hypertension may develop.

When used simultaneously with class I antiarrhythmic drugs (quinidine, hydroquinidine, flecainide, cibenzoline, disopyramide, lidocaine, mexiletine, propafenone) and amiodarone, the negative inotropic effect may be enhanced and the time of excitation through the atria may be prolonged.

With simultaneous use of nebivolol with cardiac glycosides, atrioventricular conduction may slow down.

The simultaneous use of nebivolol and general anesthesia may suppress reflex tachycardia and increase the risk of developing arterial hypotension.

There is no clinically significant interaction between nebivolol and nonsteroidal anti-inflammatory drugs (NSAIDs).

Acetylsalicylic acid as an antiplatelet agent can be used simultaneously with nebivolol.

The simultaneous use of tricyclic antidepressants, barbiturates and phenothiazine derivatives, anxiolytics, hypnotics, ethanol may enhance the antihypertensive effect of nebivolol.

Nebivolol does not affect plasma glucose concentrations in patients with diabetes mellitus. However, with simultaneous use of nebivolol with insulin and oral hypoglycemic agents, the symptoms of hypoglycemia (palpitations, tachycardia) may be masked.

Concomitant use with floctafenine is contraindicated: nebivolol can interfere with compensatory reactions of the cardiovascular system associated with arterial hypotension or shock, which can be caused by floctafenine. Concomitant use of nebivolol with baclofen and amifostine leads to increased arterial hypotension.

Concomitant use with sultopride is contraindicated due to the increased risk of developing ventricular arrhythmia of the torsade de pointes type.

Pharmacokinetic interaction

When used simultaneously with drugs that inhibit serotonin reuptake or other drugs that are biotransformed with the participation of the CYP2D6 isoenzyme, the concentration of nebivolol in the blood plasma increases, the metabolism of nebivolol slows down, which can lead to the risk of developing bradycardia.

When used concomitantly, nebivolol had no effect on the pharmacokinetic parameters of digoxin.

When used simultaneously with cimetidine, the concentration of nebivolol in the blood plasma increases (there are no data on the effect on the pharmacological effects of the drug). Concomitant use of ranitidine had no effect on the pharmacokinetic parameters of nebivolol.

Rifampin increases the metabolism of nebivolol.

With simultaneous use of nebivolol with nicardipine, the concentrations of active substances in the blood plasma increased slightly (which has no clinical significance). With simultaneous use of nebivolol and ethanol, furosemide or hydrochlorothiazide, there is no change in the pharmacokinetic parameters of nebivolol. No clinically significant interaction between nebivolol and warfarin has been established. When used concomitantly, sympathomimetic agents inhibit the pharmacological activity of nebivolol.

Overdose

Symptoms:

Marked decrease in blood pressure, severe bradycardia, acute heart failure, atrioventricular block, cardiogenic shock, cardiac arrest, bronchospasm, loss of consciousness, convulsions, coma, nausea, vomiting, hypoglycemia, cyanosis. Treatment:

Gastric lavage, taking activated carbon. In case of a pronounced decrease in blood pressure, it is necessary to place the patient in a horizontal position with elevated legs, and, if necessary, administer intravenous fluid and vasopressors. For bradycardia, 0.5 - 2 mg of atropine should be administered intravenously; if there is no positive effect, a transvenous or intracardiac pacemaker may be installed. In case of atrioventricular block (N-III stage), intravenous administration of beta-adrenergic stimulants is recommended; if they are ineffective, the issue of installing an artificial pacemaker should be considered. In case of heart failure, treatment begins with the administration of cardiac glycosides and diuretics; if there is no effect, it is advisable to administer dopamine, dobutamine or vasodilators. For bronchospasm, betag-agonists are used intravenously. For ventricular extrasystole - lidocaine (class IA antiarrhythmic drugs cannot be administered). For convulsions, intravenous administration of diazepam. For hypoglycemia, intravenous dextrose (glucose) may be indicated.

Impact on the ability to drive vehicles and operate machinery

treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

The most dangerous combinations and consequences

The combination of alcohol and chemical-based drugs can lead to serious disorders in the body, and in some cases to fatal consequences.

List of medications and their side effects in combination with alcohol: