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Nebivolol
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| Systematic (IUPAC) name | |
| 1-(6-fluorochroman-2-yl)-{[2-(6-fluorochroman-2-yl)- 2-hydroxy-ethyl]amino}ethanol OR 2,2'-azanediylbis(1-(6-fluorochroman-2-yl)ethanol) |
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| Identifiers | |
| CAS number | |
| ATC code | C07 |
| PubChem | |
| Chemical data | |
| Formula | C22H25F2NO4 |
| Mol. mass | 405.435 g/mol |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Protein binding | 98% |
| Metabolism | Hepatic (CYP2D6-mediated) |
| Half life | 10 hours |
| Excretion | Renal and fecal |
| Therapeutic considerations | |
| Licence data |
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| Pregnancy cat. |
C(US) |
| Legal status | |
| Routes | Oral |
Nebivolol is a highly cardioselective beta1 receptor blocker with nitric oxide-potentiating vasodilatory effect used in treatment of hypertension and, in Europe, also for left ventricular failure.[1]
Contents |
Pharmacology and biochemistry
β1 Selectivity
Nebivolol is the most β1-selective of the β-blockers, being approximately 3.5 times more β1-selective than bisoprolol.[2][3]
Vasodilator action
Nebivolol is unique[4] as a beta-blocker in also having a nitric oxide (NO)-potentiating, vasodilatory effect.[5]
Antihypertensive effect
Nebivolol lowers blood pressure (BP) by reducing peripheral vascular resistance, and significantly increases stroke volume with preservation of cardiac output.[6] 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.[7]
Pharmacology of side-effects
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.[8][9][10]
FDA warning letter about advertising claims
In late August 2008, the FDA issued a warning letter to Forest Laboratories citing exaggerated and misleading claims in a journal advert, in particular over claims of superiority and novelty of action. [11]
Contraindications
- Hepatic insufficiency
- Children
- Pregnancy
- Lactation
Adverse Drug Reactions
- Headache
- Parasthesia
- Dizziness
History
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, including the US. 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. In the US, it is marketed under the brand name Bystolic from Mylan Laboratories and Forest Laboratories.
References
- ^ de Boer RA, Voors AA, van Veldhuisen DJ (July 2007). "Nebivolol: third-generation beta-blockade". Expert Opin Pharmacother 8 (10): 1539–50. doi:. PMID 17661735.
- ^ Bundkirchen A, Brixius K, Bölck B, Nguyen Q, Schwinger RH (January 2003). "Beta 1-adrenoceptor selectivity of nebivolol and bisoprolol. A comparison of [3H]CGP 12.177 and [125I]iodocyanopindolol binding studies". Eur. J. Pharmacol. 460 (1): 19–26. doi:. PMID 12535855.
- ^ Nuttall SL, Routledge HC, Kendall MJ (June 2003). "A comparison of the beta1-selectivity of three beta1-selective beta-blockers". J Clin Pharm Ther 28 (3): 179–86. PMID 12795776.
- ^ Agabiti Rosei E, Rizzoni D (2007). "Metabolic profile of nebivolol, a beta-adrenoceptor antagonist with unique characteristics". Drugs 67 (8): 1097–107. PMID 17521213.
- ^ Weiss R (2006). "Nebivolol: a novel beta-blocker with nitric oxide-induced vasodilatation". Vasc Health Risk Manag 2 (3): 303–8. PMID 17326335.
- ^ Kamp O, Sieswerda GT, Visser CA (August 2003). "Comparison of effects on systolic and diastolic left ventricular function of nebivolol versus atenolol in patients with uncomplicated essential hypertension". Am. J. Cardiol. 92 (3): 344–8. PMID 12888152.
- ^ Gielen W, Cleophas TJ, Agrawal R (August 2006). "Nebivolol: a review of its clinical and pharmacological characteristics". Int J Clin Pharmacol Ther 44 (8): 344–57. PMID 16961165.
- ^ Pessina AC (December 2001). "Metabolic effects and safety profile of nebivolol". J. Cardiovasc. Pharmacol. 38 Suppl 3: S33–5. PMID 11811391.
- ^ Weber MA (December 2005). "The role of the new beta-blockers in treating cardiovascular disease". Am. J. Hypertens. 18 (12 Pt 2): 169S–176S. doi:. PMID 16373195.
- ^ Poirier L, Cléroux J, Nadeau A, Lacourcière Y (August 2001). "Effects of nebivolol and atenolol on insulin sensitivity and haemodynamics in hypertensive patients". J. Hypertens. 19 (8): 1429–35. PMID 11518851.
- ^ Thomas Abrams (8/28/2008). "Warning Letter" (PDF). Food and Drug Administration. Retrieved on 2008. "FDA is not aware of any substantial evidence or substantial clinical experience that demonstrates that Bystolic represents a 'novel' or 'next generation' beta blocker for the treatment of hypertension. Indeed, we are not aware of any well-designed trials comparing Systolic to other ß-blockers. Furthermore, FDA is not aware of any data that would render Bystolic's mechanism of action 'unique.'"
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Wikipedia content modification information:
- This page was last modified on 7 October 2008, at 04:30.
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