Nebivolol

Table of contents

  • Brand Names
  • Drug Combinations
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Induces
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Hypoloc, Nebacop, Nebilan, Nebiphar, Nebispes, Nebivolol, Nomexor; Belgium: Nobiten; Bulgaria: Nebalex, Nebicor, Nebilan, Nebilet, Nebirod, Nebivolol, Nebizita; Cyprus: Lobivon; Czech Republic: Ezocem, Nebilan, Nebilet, Nebinorm, Nebiscal, Nebispes, Nebitrix, Nebivolol; Denmark: Hypoloc, Nebilet; Estonia: Nebicard, Nebilet, Nebiphar, Nebisam, Nebiscop, Nebispes, Nebiten, Nebivolol, Nemirostad; Finland: Hypoloc, Nebilet; France: Nebilox, Temerit; Germany: Ebivol, Hypoloc, Lobivon, Nebigamma, Nebilet, Nebilic, Nebilox, Nebimar, Nebithan, Nebivolol, Nebivololo, Terivolol; Greece: Bivol, Lobibeta; Hungary: Berovan, Esteban, Ezocem, Nebacop, Nebaletor, Nebilet, Nebispes, Nebitrix, Nebivep, Nebivolol, Nevotens; Ireland: Hypoloc, Nebilet, Nebimel, Nebol, Nebtev, Nelet; Italy: Lobivon, Nebilox; Latvia: Nebicard, Nebilet, Nebiphar, Nebisam, Nebiscop, Nebispes, Nebiten, Nebivolol, Nemirostad; Lithuania: Nebicard, Nebilet, Nebinorm, Nebiphar, Nebisam, Nebiscop, Nebispes, Nebiten, Nebivolol, Nemirostad, Nemon, Nerose; Luxembourg: Hypoloc, Nobiten; Malta: Nebilet, Nebivolol; Netherlands: Hypoloc, Lobivon, Nebilet, Nebiloc, Nebivolol; Poland: Ebivol, Ezocem, Lovispes, Nebicard, Nebilenin, Nebilet, Nebinad, Nebispes, Nebitrix, NebivoLek, Nebivolol, Nebivor, Nedal; Portugal: Blokat, Hypoloc, Nebilet, Nebivolol; Romania: Ezocem, Nebacop, Nebalex, Nebicard, Nebilet, Nebinorm, Nebirod, Nebivolol, Neblotensol, Nolet, Voxnebin, X-Pressol; Slovakia: Ezocem, Nebilan, Nebiscal, Nebitrix, Nebivolol; Slovenia: Lovispes, Nebilet, Nebispes, Nebivolol; Spain: Lovibon, Nebivolol, Silostar; Sweden: Hypoloc, Nebivolol; UK: Hypoloc, Nebilet, Nebivolol.

North America

USA: Bystolic.

Latin America

Argentina: Nabila, Nebilet, Syncrocor.

Drug combinations

Nebivolol and Hydrochlorothiazide

Chemistry

Nebivolol: C~22~H~25~F~2~NO~4~. Mw: 405.44. (1) 2-H-1-Benzopyran-2-methanol, α,α’-[iminobis(methylene)bis[6-fluoro-3,4-dihydro-; (2) α,α’-(Iminodimethylene)bis[6-fluoro-2-chromanmethanol]. CAS-99200-09-6.

Pharmacologic Category

β-Adrenergic Blocking Agents; β~1~-Selective β-Blocker. (ATC-Code: C07AB12).

Mechanism of action

Highly-selective inhibitor of β~1~-adrenergic receptors. Nebivolol, unlike other β-blockers, also produces an endothelium-derived nitric oxide-dependent vasodilation resulting in a reduction of systemic vascular resistance.

Therapeutic use

Treatment of hypertension, alone or in combination with other agents.

Pregnancy and lactiation implications

Adverse events observed in animal studies. There are no adequate and well-controlled studies in pregnant women. β-Blockers associated with persistent bradycardia, hypotension, and IUGR; IUGR is probably related to maternal hypertension. Available evidence suggests β-blockers are generally safe during pregnancy. Lactation is not recommended.

Unlabeled use

Heart failure.

Contraindications

Hypersensitivity to nebivolol or any component of the formulation. Severe bradycardia. Heart block greater than first-degree (except in patients with a functioning artificial pacemaker). Cardiogenic shock. Decompensated cardiac failure. Sick sinus syndrome (unless a permanent pacemaker is in place). Severe hepatic impairment.

Warnings and precautions

Use with caution in diabetes mellitus (may potentiate hypoglycemia and/or mask signs and symptoms). Use caution with history of severe anaphylaxis to a variety of allergens; patients taking β-blockers may become more sensitive to repeated challenges. Treatment of anaphylaxis (e.g. epinephrine) in patients taking β-blockers may be ineffective or promote undesirable effects. In general, patients with bronchospastic disease should not receive β-blockers; for patients with bronchospastic disease who do not respond to or cannot tolerate other therapies, initial low doses of β~1~-selective nebivolol may be employed and used cautiously with close monitoring. Consider pre-existing conditions such as sick sinus syndrome before initiating. Use with caution in compensated heart failure. Patients should be stabilized on heart failure regimen prior to initiation of β-blocker. β-Blocker therapy should be initiated at very low doses with gradual and very careful titration. Adjustment of other medications (ACEIs and/or diuretics) may be required. Use with caution in hepatic impairment. Use is contraindicated in patients with Child-Pugh class C hepatic impairment. Use with caution in myasthenia gravis. Peripheral vascular disease (PVD) may precipitate or aggravate symptoms of arterial insufficiency in PVD and Raynaud’s disease (use with caution). Use with caution in history of psychiatric illness (may cause or exacerbate CNS depression). Use with caution in severe renal impairment (CrCl <30 mL/minute). Adequate α-blockade is required prior to use of any β-blocker. Use with caution in patients receiving anesthetic agents which decrease myocardial function (e.g. ether, cyclopropane and trichloroethylene). β-Blockade may mask signs of hyperthyroidism (e.g. tachycardia). Abrupt discontinuation may exacerbate symptoms of hyperthyroidism and may also induce thyroid storm. Use with caution in patients on concurrent verapamil or diltiazem (bradycardia or heart block may occur). β-Blocker therapy should not be withdrawn abruptly (particularly in coronary artery disease), but gradually tapered to avoid acute tachycardia, hypertension, and/or ischemia. Use with caution in patients receiving CYP2D6 inhibitors (e.g. chlorpromazine, fluoxetine, propafenone, propoxyphene, quinidine, ritonavir).

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