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.
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.
Nebivolol tab 5mg N56 (Northern Star)
Pharmacodynamic interaction With the simultaneous use of β-blockers with blockers of “slow” calcium channels (SCBC) (verapamil and diltiazem), the negative effect on myocardial contractility and AV conductivity increases. IV administration of verapamil is contraindicated while using nebivolol. When nebivolol is used concomitantly with antihypertensive drugs, nitroglycerin or BMCC, severe arterial hypotension may develop (special caution is required when combined with prazosin). The simultaneous use of baclofen and amifostine with antihypertensive drugs can cause a significant drop in blood pressure, so dose adjustment of antihypertensive drugs is required. With the simultaneous use of nebivolol 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 is possible. With the simultaneous use of nebivolol with class I antiarrhythmic drugs 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, there was no increase in the effect on slowing AV conduction. The simultaneous use of nebivolol and drugs for general anesthesia may suppress reflex tachycardia and increase the risk of developing arterial hypotension. There is no clinically significant interaction between nebivolol and non-steroidal anti-inflammatory drugs (NSAIDs). Concomitant use of nebivolol with tricyclic antidepressants, barbiturates and phenothiazine derivatives may enhance the hypotensive effect of nebivolol. The simultaneous use of nebivolol and floctafenine is contraindicated, as there is a risk of a pronounced decrease in blood pressure or shock. The simultaneous use of nebivolol and sultopride is contraindicated, as the risk of developing ventricular arrhythmia, especially of the “pirouette” type, increases. When nebivolol is used simultaneously with insulin and oral hypoglycemic agents, the symptoms of hypoglycemia (tachycardia) may be masked. When used concomitantly, sympathomimetic agents inhibit the activity of nebivolol. Pharmacokinetic interaction: With simultaneous use of nebivolol 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 bradycardia. When used concomitantly with digoxin, nebivolol does not affect the pharmacokinetic parameters of digoxin. With simultaneous use of nebivolol with cimetidine, the concentration of nebivolol in the blood plasma increases. The simultaneous use of nebivolol and ranitidine does not affect the pharmacokinetic parameters of nebivolol. With simultaneous use of nebivolol with nicardipine, the concentrations of active substances in the blood plasma increase slightly, but this does not have clinical significance. Concomitant use of nebivolol and ethanol, furosemide or hydrochlorothiazide does not affect the pharmacokinetics of nebivolol. No clinically significant interaction between nebivolol and warfarin has been established.
