Nebivolol detailed information
{{drugbox |
| IUPAC_name = 1-(6-fluorochroman-2-yl)-{[2-(6-fluorochroman-2-yl)-
2-hydroxy-ethyl]amino}ethanol
| image = Nebivolol_svg.png
| CAS_number = 99200-09-6
| ATC_prefix = C07
| ATC_suffix = AB12
| PubChem = 71301
| DrugBank =
| C = 22 |H = 25 |F = 2 |N = 1 |O = 4
| molecular_weight = 405.435 g/mol
| bioavailability =
| protein_bound = 98%
| metabolism = Hepatic (CYP2D6-mediated)
| elimination_half-life = 10 hours
| excretion = Renal and fecal
| pregnancy_category =
| legal_status = POM (UK)
| routes_of_administration = Oral
}}
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]
Overview
Nebivolol is a highly cardioselective vasodilatory beta1 receptor blocker used in treatment of hypertension. In most countries, this medication is available only by prescription.
Nebivolol lowers blood pressure (BP) by reducing peripheral vascular resistance, and significantly increases stroke volume with preservation of cardiac output.[1] The net hemodynamic effect of nebivolol is the result of a balance between the depressant effects of beta-blockade and an action that maintains cardiac output.[2] As well as being an effective antihypertensive treatment, nebivolol is not associated with many typical beta-blocker related side effects, such as fatigue, clinical depression, bradycardia, or impotence.[3][4][5]
Mylan Laboratories licensed the U.S. and Canadian rights to nebivolol from Janssen Pharmaceutica N.V. in 2001. Nebivolol is already registered and successfully marketed in more than 50 other countries outside of North America. It is marketed under the brand name Nebilet. Nebivolol is manufactured by Forest Laboratories, Inc. In India, Nebivolol is available as ''''Nebilong 5 mg(Micro Labs) Nebicard-5 (Torrent), Nubeta (Nicholas Piramal) and Nodon (Unichem). In Greece and Italy, Nebivolol is marketed under the name Lobivon from Menarini pharmaceutical.
On February 18, 2008, Mylan and Forest Laboratories will receive final approval from the Federal Drug Administration for nebivolol in the US, which is marketed under the tradename Bystolic®.
Contraindications
- Hepatic insufficiency
- Children
- Pregnancy
- Lactation
Adverse Drug Reactions
- Headache
- Parasthesia
- Dizziness
References
- ↑ Kamp, O., G.T. Sieswerda, and C.A. Visser, Comparison of effects on systolic and diastolic left ventricular function of nebivolol versus atenolol in patients with uncomplicated essential hypertension. Am J Cardiol, 2003. 92(3): p. 344-8.
- ↑ Gielen, W., T.J. Cleophas, and R. Agrawal, Nebivolol: a review of its clinical and pharmacological characteristics. Int J Clin Pharmacol Ther, 2006. 44(8): p. 344-57.
- ↑ Pessina, A.C., Metabolic effects and safety profile of nebivolol. J Cardiovasc Pharmacol, 2001. 38 Suppl 3: p. S33-5.
- ↑ Weber, M.A., The role of the new beta-blockers in treating cardiovascular disease. Am J Hypertens, 2005. 18(12 Pt 2): p. 169S-176S.
- ↑ Poirier, L., et al., Effects of nebivolol and atenolol on insulin sensitivity and haemodynamics in hypertensive patients. J Hypertens, 2001. 19(8): p. 1429-35.