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Uses

Hypertension

Nebivolol hydrochloride is used alone or in combination with other classes of antihypertensive agents in the management of hypertension. Although β-adrenergic blocking agents (β-blockers) were previously considered a drug of choice for the initial management of hypertension, most current guidelines no longer recommend these drugs as first-line therapy because of the lack of established superiority over other recommended drug classes and at least one study demonstrating that they may be less effective than angiotensin II receptor antagonists in preventing cardiovascular death, myocardial infarction, or stroke. However, β-blockers may still be considered in hypertensive patients who have a compelling indication (e.g., prior myocardial infarction, ischemic heart disease, heart failure) for their use or as add-on therapy in those who do not respond adequately to the preferred drug classes (angiotensin-converting enzyme [ACE] inhibitors, angiotensin II receptor antagonists, calcium-channel blockers, and thiazide diuretics). and in

Efficacy of nebivolol in the treatment of hypertension has been established in several placebo-controlled studies of 12 weeks' duration in patients with mild to moderate hypertension. In these patients, usual dosages of nebivolol (5-40 mg once daily) as monotherapy decreased placebo-controlled seated systolic blood pressure by about 2.6-11.7 mm Hg and diastolic blood pressure by about 3.2-8.3 mm Hg. In patients whose blood pressure was inadequately controlled by an ACE inhibitor, angiotensin II receptor antagonist, and/or a thiazide diuretic, addition of nebivolol (5-20 mg daily) to the existing antihypertensive regimen resulted in further reductions in blood pressure. Although nebivolol monotherapy reduced blood pressure in black patients, the magnitude of the effect was somewhat smaller in black patients than in Caucasian patients.

In general, black hypertensive patients tend to respond better to monotherapy with thiazide diuretics or calcium-channel blocking agents than to monotherapy with ACE inhibitors, angiotensin II receptor antagonists, or β-blockers. Although β-blockers have lowered blood pressure in all races studied, monotherapy with these agents has produced a smaller reduction in blood pressure in black hypertensive patients; however, this population difference in response does not appear to occur during combined therapy with a β-blocker and a thiazide diuretic. and in Comparative studies are needed to determine the relative efficacy of nebivolol and other β-blockers for controlling blood pressure in black patients.

Nebivolol is at least as effective in the management of hypertension as other β-blockers (e.g., atenolol, bisoprolol, metoprolol), calcium-channel blocking agents (e.g., nifedipine, amlodipine), ACE inhibitors (e.g., lisinopril, enalapril), and angiotensin II receptor antagonists (e.g., losartan).

Dosage and Administration

General

Careful monitoring of blood pressure during initial titration or subsequent upward adjustment in dosage of nebivolol is recommended.

The goal of hypertension management and prevention is to achieve and maintain optimal control of blood pressure; specific target levels of blood pressure should be individualized based on consideration of multiple factors, including patient age and comorbidities, and the currently available evidence from clinical studies.

Administration

Nebivolol hydrochloride is administered orally once daily without regard to meals.

Dosage

Dosage of nebivolol hydrochloride is expressed in terms of nebivolol.

Adults

Hypertension

Dosage of nebivolol should be individualized according to the response of the patient. If nebivolol therapy is to be discontinued, dosage of the drug should be reduced gradually over a period of 1-2 weeks when possible.

For the treatment of hypertension in adults, the usual initial dosage of nebivolol is 5 mg once daily as monotherapy or in combination with other antihypertensive agents. In patients whose blood pressure is not controlled adequately with the initial nebivolol dosage, dosage can be increased at 2-week intervals up to 40 mg daily. Administering the drug more frequently (i.e., in divided doses daily) is unlikely to be more beneficial than once-daily administration.

The panel members appointed to the Eighth Joint National Committee on the Prevention, Detection, Evaluation, and Treatment of High Blood Pressure (JNC 8 expert panel) state that evidence-based dosing information should be used when available to determine target dosages of antihypertensive agents. Target dosages of antihypertensive agents generally can be achieved within 2-4 weeks, but it may take up to several months.

In patients who experience intolerable adverse effects with nebivolol, dosage reduction should be considered; if adverse effects worsen or fail to resolve, it may be necessary to discontinue the β-blocker and initiate another class of antihypertensive agent.

Special Populations

In patients with severe renal (creatinine clearance less than 30 mL/minute) or moderate hepatic (Child-Pugh class B) impairment, the recommended initial dosage of nebivolol is 2.5 mg once daily. If necessary, dosage may be increased carefully. Nebivolol is contraindicated in patients with severe hepatic (Child-Pugh class C) impairment. (See Renal Impairment and also Hepatic Impairment under Warnings/Precautions: Specific Populations, in Cautions.) No dosage adjustment of nebivolol is needed in geriatric patients.

Although polymorphisms in cytochrome P-450 (CYP) isoenzyme 2D6 affect metabolism of nebivolol, both the parent drug and the main circulating metabolites contribute to the drug's activity, and no dosage adjustment of nebivolol is needed in patients with the poor metabolizer phenotype (see Description).

Cautions

Contraindications

Severe bradycardia, heart block greater than first degree, cardiogenic shock, decompensated cardiac failure, sick sinus syndrome (unless a permanent pacemaker is in place), or severe hepatic impairment (Child-Pugh class C). Known hypersensitivity to nebivolol or any ingredient in the formulation.

Warnings/Precautions

Warnings

Abrupt Withdrawal of Therapy

Abrupt withdrawal of β-adrenergic blocking agents (β-blockers) may exacerbate angina symptoms and/or precipitate myocardial infarction and ventricular arrhythmias in patients with coronary artery disease. Therefore, patients receiving nebivolol (especially those with ischemic heart disease) should be warned not to interrupt or abruptly discontinue therapy without consulting their clinician. When discontinuance of nebivolol therapy is planned, dosage of the drug should be reduced gradually over a period of 1-2 weeks. Patients should be carefully monitored and advised to temporarily limit their physical activity. If exacerbation of angina occurs or acute coronary insufficiency develops after nebivolol therapy is interrupted or discontinued, treatment with the drug should be reinstituted, at least temporarily. Because coronary artery disease is common and may be unrecognized, the manufacturer cautions that nebivolol therapy should not be discontinued abruptly, even in patients being treated only for hypertension.

Heart Failure

In patients with heart failure, sympathetic stimulation is vital for support of circulatory function. Nebivolol should be used with caution in patients with inadequate cardiac function, since further depression of myocardial contractility and cardiac failure may be precipitated.

Although β-blockers should be avoided in patients with overt heart failure (see Cautions: Contraindications), nebivolol may be administered cautiously, if necessary, to patients with well-compensated heart failure. If heart failure worsens, discontinuance of nebivolol should be considered.

Ischemic Heart Disease

Safety and efficacy of nebivolol in patients with angina pectoris or recent myocardial infarction have not been established to date.

Anesthesia and Major Surgery

Nebivolol should be used with caution in patients undergoing major surgery involving general anesthesia. Particular caution should be employed if anesthetics that depress the myocardium are used. Severe, protracted hypotension and difficulty in restarting or maintaining a heart beat have occurred during surgery in some patients who have received β-blockers. The β-adrenergic blocking effects of nebivolol can be reversed by administration of β-agonists (e.g., dobutamine, isoproterenol).

Bronchospastic Diseases

Patients with bronchospastic disease generally should not receive β-blockers.

Diabetes Mellitus and Hypoglycemia

β-Blockers may mask signs and symptoms of hypoglycemia (e.g., tachycardia). Nonselective β-blockers may potentiate insulin-induced hypoglycemia and delay recovery of serum glucose concentrations.

Nebivolol should be used with caution in patients subject to spontaneous hypoglycemia and in diabetic patients receiving insulin or oral hypoglycemic agents.

Thyrotoxicosis

β-Blockers may mask signs of hyperthyroidism (e.g., tachycardia). Abrupt withdrawal of β-adrenergic blockade may exacerbate manifestations of hyperthyroidism or precipitate thyroid storm.

Peripheral Vascular Disease

β-Blockers may precipitate or aggravate symptoms of arterial insufficiency in patients with peripheral vascular disease; nebivolol should be used with caution in these patients.

Nondihydropyridine Calcium-channel Blocking Agents

Because of their negative inotropic and chronotropic effects, nebivolol and nondihydropyridine calcium-channel blocking agents (e.g. verapamil, diltiazem) should be used concomitantly with caution.(See Calcium-channel Blocking Agents under Drug Interactions: Drugs Affecting Cardiac Conduction.)

General Precautions

Risk of Anaphylactic Reactions

Patients who have a history of anaphylactic reactions to a variety of allergens reportedly may be more reactive to repeated accidental, diagnostic, or therapeutic challenges with such allergens while taking β-blockers and may be unresponsive to usual doses of epinephrine used to treat such reactions.

Pheochromocytoma

In patients with known or suspected pheochromocytoma, treatment with an α-adrenergic blocking agent should be instituted prior to use of a β-blocker (e.g., nebivolol).

Specific Populations

Pregnancy

Category C.

Lactation

Distributed into milk in rats; not known whether nebivolol is distributed into human milk. Discontinue nursing or drug.

Pediatric Use

Safety and efficacy not established in children younger than 18 years of age.

Geriatric Use

No substantial differences in safety or efficacy relative to younger adults.(See Dosage and Administration: Special Populations.)

Renal Impairment

Use with caution in patients with severe renal impairment (creatinine clearance less than 30 mL/minute), since clearance is decreased by about 53%.(See Dosage and Administration: Special Populations.) Not specifically studied in patients undergoing dialysis; use with caution in these patients.

Hepatic Impairment

Use with caution in patients with moderate hepatic impairment because of decreased hepatic metabolism; clearance is decreased by about 86% and systemic exposure is increased approximately tenfold.(See Dosage and Administration: Special Populations.) Safety and efficacy not established in patients with severe hepatic impairment; use is contraindicated in these patients.

Common Adverse Effects

Adverse effects reported in 1% or more of patients receiving nebivolol in clinical trials and more frequently with nebivolol than with placebo include headache, fatigue, dizziness, diarrhea, nausea, insomnia, chest pain, bradycardia, dyspnea, rash, and peripheral edema. Other adverse effects reported in 1% or more of patients receiving nebivolol during worldwide clinical trials include asthenia, abdominal pain, hypercholesterolemia, hyperuricemia, and paresthesia.

Drug Interactions

Drugs Affecting Hepatic Microsomal Enzymes

Nebivolol is metabolized by cytochrome P-450 (CYP) isoenzyme 2D6 but does not inhibit CYP isoenzymes at clinically relevant concentrations.

Potent inhibitors of CYP2D6 (e.g., quinidine, propafenone, fluoxetine, paroxetine): Potential pharmacokinetic interaction (increased plasma concentrations of nebivolol). Monitor patient carefully; adjust nebivolol dosage according to blood pressure response.

Drugs Affecting Cardiac Conduction

Antiarrhythmic Agents

Possible conduction disturbance when nebivolol is used concomitantly with antiarrhythmic agents (e.g., amiodarone, disopyramide). Use concomitantly with caution.

β-Adrenergic Blocking Agents

Possible additive negative effects on AV conduction and heart rate. Concomitant use of nebivolol with other β-adrenergic blocking agents (β-blockers) is not recommended.

Calcium-channel Blocking Agents

Possible conduction disturbance when nebivolol is used concomitantly with nondihydropyridine calcium-channel blocking agents (e.g., diltiazem, verapamil). Use concomitantly with caution; monitor blood pressure and ECG with concomitant use.

Digoxin

Possible additive negative effects on AV conduction and heart rate; increased risk of bradycardia. Use concomitantly with caution. Concomitant use of digoxin (0.25 mg once daily) and nebivolol (10 mg once daily) for 10 days in healthy adults did not affect the pharmacokinetics of either drug.

Catecholamine-depleting Agents

Potential additive effects (e.g., hypotension, bradycardia) with catecholamine-depleting agents (e.g., reserpine, guanethidine). Monitor closely for symptoms (e.g., vertigo, syncope, postural hypotension).

Other Cardiovascular Drugs

Clonidine

Potential pharmacologic interaction (increased rebound hypertension following discontinuance of clonidine). When clonidine is to be discontinued in patients receiving clonidine and nebivolol concurrently, nebivolol should be discontinued several days before gradual withdrawal of clonidine.

Diuretics

No pharmacokinetic interactions observed in healthy individuals receiving nebivolol (10 mg daily for 10 days) and a diuretic (single 40-mg dose of furosemide, hydrochlorothiazide 25 mg once daily for 10 days, or spironolactone 25 mg once daily for 10 days).

Losartan

No pharmacokinetic interaction observed following single-dose administration of nebivolol (10 mg) and losartan potassium (50 mg).

Propafenone

Potential pharmacokinetic interaction (increased plasma concentrations of nebivolol). Use concomitantly with caution.

Quinidine

Potential pharmacokinetic interaction (increased plasma concentrations of nebivolol). Use concomitantly with caution.

Ramipril

No pharmacokinetic interaction observed following concomitant administration of nebivolol (10 mg once daily) and ramipril (5 mg once daily) for 10 days.

Sildenafil

Potential pharmacokinetic interaction (modest [21-23%] decrease in peak plasma concentration and area under the plasma concentration-time curve [AUC] of sildenafil, modest [less than 20%] effect on peak plasma concentration and AUC of d-nebivolol). Nebivolol and sildenafil have additive effects on blood pressure and pulse.

GI Drugs

Activated Charcoal

No effect on nebivolol pharmacokinetics following single-dose administration of nebivolol (10 mg) and repeated-dose administration of activated charcoal over 48 hours.

Cimetidine

Potential pharmacokinetic interaction (modest [21-23%] increase in plasma nebivolol concentrations) observed following concomitant administration of nebivolol (single 5-mg dose) and cimetidine (400 mg twice daily for 3 days). No apparent change in pharmacodynamics of nebivolol (e.g., blood pressure, heart rate).

Ranitidine

No effect on nebivolol pharmacokinetics or pharmacodynamics (e.g., blood pressure, heart rate) observed following concomitant administration of nebivolol (single 5-mg dose) and ranitidine (150 mg twice daily for 3 days).

Psychotherapeutic Agents

Fluoxetine

Potential pharmacokinetic interaction (increased plasma concentrations of nebivolol). Eightfold increase in AUC and threefold increase in peak plasma concentration of d-nebivolol observed in healthy individuals receiving a single 10-mg dose of nebivolol following administration of fluoxetine 20 mg daily for 21 days. Use concomitantly with caution.

Paroxetine

Potential pharmacokinetic interaction (increased plasma concentrations of nebivolol). Use concomitantly with caution.

Warfarin

No effect on warfarin or nebivolol pharmacokinetics observed in individuals receiving warfarin (single 10-mg dose) and nebivolol (10 mg once daily for 10 days); no effect on prothrombin times after a single warfarin dose.

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