Nebivolol tab 5mg N56 (Northern Star)

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.

Nebivolol drug overdose, symptoms and treatment

There are no data on overdose. Typically, symptoms of overdose of beta-adrenergic blockers are bradycardia, arterial hypotension, bronchospasm and acute heart failure. In case of overdose, gastric lavage is performed, activated charcoal and laxatives are prescribed, and, if indicated, mechanical ventilation is performed. For severe bradycardia, atropine or methylatropine is administered. For arterial hypotension and shock, plasma preparations or plasma substitutes are administered, and, if necessary, catecholamines. Blockade of β-adrenergic receptors can be eliminated by slow intravenous administration of isoprenaline hydrochloride, starting at a dose of 5 mcg/min, or dobutamine, starting at a dose of 2.5 mcg/min, until a therapeutic effect is obtained, or (if resistance to therapy) - a combination of these drugs. If there is no effect, glucagon is administered intravenously at a rate of 50–100 mcg/kg; if necessary, the administration is repeated after 1 hour and, if the effect is insufficient, an additional dose of 70 mcg/kg every hour. In extreme cases (with bradycardia that is not amenable to drug therapy), a temporary pacemaker is used.

List of pharmacies where you can buy Nebivolol:

• Moscow
• Saint Petersburg

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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Side effects of the drug Nebivolol

Usually mild or moderate. The most common symptoms are headache, dizziness, fatigue, paresthesia, diarrhea, constipation, nausea, shortness of breath, peripheral edema; less often (less than 1% of cases) - bradycardia, slow AV conduction or AV block, arterial hypotension, manifestations of heart failure, increased intermittent claudication, blurred vision, impotence, depression, nightmares, dyspepsia, flatulence, vomiting, bronchospasm, skin reactions. The use of beta-adrenergic receptor blockers in some cases can cause hallucinations, psychosis, confusion, a feeling of coldness and cyanosis of the extremities, Raynaud's syndrome, and dry eye mucosa.

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.

Pharmacological properties of the drug Nebivolol

Nebivolol ([2R*[R*[R*(S*)]]]-α,α-iminobis-(methylene)bis6-fluoro-3, 4-dihydro-2H - 1 -benzopyran-2-methanol) is a racemate consisting of two enantiomers: SRRR-nebivolol (or D-nebivolol) and RSSS-nebivolol (or L-nebivolol). It is a highly selective competitive β1-adrenergic receptor blocker (this effect is associated with the D-enantiomer) and has a moderate vasodilating effect due to metabolic interaction with L-arginine/nitric oxide (NO) (this effect is associated with the L-enantiomer). Does not have BCA. In therapeutic doses it does not have membrane-stabilizing and α-adrenergic blocking activity. Reduces heart rate and lowers blood pressure at rest and during exercise in both patients with normal blood pressure and hypertension (arterial hypertension). The hypotensive effect persists with long-term treatment. Does not have a significant effect on exercise tolerance. After oral administration, both enantiomers of nebivolol are rapidly absorbed from the digestive tract. Eating does not affect the absorption of the drug. Metabolized in the body to form active hydroxymetabolites. The metabolism of nebivolol is carried out by alicyclic and aromatic hydroxylation, N-dealkylation and glucuronidation, in addition, glucuronides of hydroxy metabolites are formed. The metabolism of nebivolol by aromatic hydroxylation is associated with a genetic oxidative polymorphism dependent on CYP 2D6. The oral bioavailability of nebivolol averages 12% in patients in whom it is rapidly metabolized, and is almost complete in those in whom nebivolol is metabolized slowly. When steady state is reached using equal doses, the maximum concentration of unchanged nebivolol in slow metabolizers is approximately 23 times higher than in fast metabolizers; Taking this into account, people with slow metabolism are prescribed nebivolol in lower doses. In fast metabolizers, the half-life of nebivolol enantiomers averages 10 hours; in slow metabolizers, the half-life of nebivolol enantiomers is 3–5 times longer. In rapid metabolizers, the plasma concentration of RSSS-nebivolol is slightly higher than that of SRRR-nebivolol. In people with slow metabolism, this difference is greater. The state of equilibrium concentration in the blood plasma for nebivolol in most patients (persons with rapid metabolism) is achieved within 24 hours, and for hydroxymetabolites - after several days. Pharmacokinetics are the same in patients of different ages. Both enantiomers bind to plasma proteins, predominantly albumin. Plasma protein binding for SRRR-nebivolol is 98.1%, and for RSSS-nebivolol is 97.9%. 1 week after administration, approximately 38% of the dose of nebivolol is excreted in the urine and 48% in the feces. No more than 0.5% of nebivolol is excreted unchanged in the urine.

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.

Academpharm

The tablets should be taken orally with a sufficient amount of liquid (for example, one glass of chilled boiled water), regardless of meals.

Arterial hypertension Adults The dose is 1 tablet (5 mg nebivolol) per day; It is advisable to always take it at the same time. A noticeable hypotensive effect appears after 1-2 weeks of treatment. Sometimes the optimal effect is achieved only after 4 weeks.

Combination with other antihypertensive drugs

β-blockers can be used both as monotherapy and in combination with other antihypertensive drugs. Until now, an additional hypotensive effect was observed only when nebivolol was combined with 12.5-25 mg hydrochlorothiazide.

Patients with kidney failure

For patients suffering from renal failure, the recommended starting dose is 2.5 mg per day. If necessary, the daily dose can be increased to 5 mg.

Patients with liver failure

Experience with nebivolol in patients with liver failure or impaired liver function is limited. For this reason, the use of nebivolol in such patients is contraindicated.

Elderly patients

For patients over 65 years of age, the recommended starting dose is 2.5 mg per day. If necessary, the daily dose can be increased to 5 mg. However, given the insufficient experience with nebivolol in patients over 75 years of age, caution and close monitoring are required when prescribing it to these patients.

Children and teenagers

The safety and effectiveness of nebivolol in children and adolescents under 18 years of age have not been established. For this reason, the use of nebivolol in this age group is not recommended.

Chronic heart failure

Treatment of stable chronic heart failure should begin with slow dose titration until the individual optimal maintenance dose is achieved.

Such patients are prescribed nebivolol if they have stable chronic heart failure without episodes of acute decompensation during the last 6 weeks. The attending physician should have experience in treating chronic heart failure. In patients taking other cardiovascular medications, including diuretics and/or digoxin and/or ACE inhibitors and/or angiotensin II antagonists, the titrated dose of these medications should be stable for the last 2 weeks before starting treatment with nebivolol.

The initial titration of the dose should be carried out according to the following scheme, maintaining intervals of one to two weeks and focusing on the patient’s tolerance of this dose: 1.25 mg of nebivolol 1 time / day, can be increased to 2.5 mg 1 time / day, then - up to 5 mg 1 time per day, and then up to 10 mg 1 time per day. The maximum recommended dose is 10 mg nebivolol once a day.

At the beginning of treatment and at each dose increase, the patient should be under the supervision of an experienced physician for at least 2 hours to ensure that the clinical condition remains stable (especially regarding blood pressure, heart rate, conduction disturbances, and symptoms of worsening heart disease). insufficiency). The occurrence of side effects may mean that not all patients can be treated with the highest recommended doses. If necessary, the already achieved dose can also be gradually reduced or, accordingly, returned to it again. If heart failure worsens or if nebivolol is intolerant during its titration phase, it is recommended to first reduce the dose of nebivolol or, if necessary, immediately discontinue it (if severe hypotension occurs, worsening heart failure with acute pulmonary edema, with the development of cardiogenic shock, symptomatic bradycardia or AV block ). As a rule, treatment of stable chronic heart failure with nebivolol is long-term.

Treatment with nebivolol should not be stopped suddenly as this may lead to a temporary worsening of heart failure. If discontinuation of nebivolol is necessary, the dose should be reduced in stages, reducing it by half per week.

Patients with kidney failure

Since dose titration to the maximum tolerated dose is individualized, dose adjustment is not required in patients with mild to moderate renal impairment. There is no experience with the use of nebivolol in patients with severe renal failure (serum creatinine > 250 µmol/l). Therefore, the use of nebivolol in these patients is not recommended.

Patients with liver failure

Experience with nebivolol in patients with hepatic impairment is limited. For this reason, the use of nebivolol in such patients is contraindicated.

Elderly patients

Since titration of the dose to the maximum tolerated is carried out on an individual basis, its adjustment is not required in elderly patients.

Children and teenagers

The safety and effectiveness of nebivolol in children and adolescents under 18 years of age have not been established. For this reason, the use of the drug Nebivolol-NAN in this age group is not recommended.

Skipping the next dose of the drug You should not skip taking the drug Nebivolol-NAN. But if you forget to take a dose of the medicine and remember about it a short time later, take the missed dose and the next one at the usual time. However, if several hours have passed and it is near time for your next dose, skip the forgotten dose and take the next one as prescribed at your usual time. Do not take a double dose to make up for a forgotten one. Repeatedly skipping doses should be avoided.

Unintentionally taking a larger dose of the drug You should not take a larger dose than your doctor prescribed. If you accidentally take more tablets than prescribed, which may lead to symptoms of overdose, tell your doctor immediately (see also section “Overdose”). While waiting for the doctor to arrive, you can take activated charcoal if you have it in your home medicine cabinet.

Stopping taking the drug Do not stop taking Nebivolol-NAN without consulting your doctor. You should not stop treatment suddenly as this may worsen your heart failure. If it is necessary to stop taking the drug Nebivolol-NAN, used for chronic heart failure, the daily dose should be reduced gradually, halving the dose at intervals of one week.

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.

Special instructions for the use of Nebivolol

Nebivolol should be discontinued 24 hours before induction of anesthesia and surgery. Before prescribing nebivolol, patients with congestive heart failure should be treated appropriately until the condition is fully compensated. Treatment with the drug in patients with coronary artery disease should be discontinued gradually over 1–2 weeks. β-adrenergic blockers may cause bradycardia. If resting heart rate decreases to 50–55 beats/min, the dose of nebivolol should be reduced. Caution should be exercised when prescribing nebivolol to patients with severe peripheral circulatory disorders (Raynaud's disease, intermittent claudication), in patients with AV blockade, diabetes mellitus (can mask symptoms of hypoglycemia), thyrotoxicosis (can eliminate tachycardia), with COPD (increases the risk of bronchial obstruction) . Beta-adrenergic receptor blockers should be prescribed to patients with a history of psoriasis only after careful comparison of the possible risks and the expected benefits of using the drug. β-adrenergic blockers can increase sensitivity to allergens and increase the severity of anaphylactic reactions. β-adrenergic receptor blockers reduce blood supply to the placenta, which can lead to intrauterine fetal death and spontaneous abortion or premature birth. In addition, negative effects (hypoglycemia and bradycardia) may occur in the fetus and newborn. There is an increased risk of heart and lung complications in the newborn, so the drug should not be used during pregnancy. Most β-adrenergic receptor blockers, especially lipophilic substances, pass into breast milk, so taking nebivolol during breastfeeding is contraindicated. Nebivolol does not affect psychomotor reactions, however, when driving vehicles or working with potentially dangerous mechanisms, it should be taken into account that its use can sometimes cause dizziness and a feeling of fatigue.

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.

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: