Nebivolol

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Nebivolol
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)
Identifiers
CAS number 99200-09-6
ATC code C07AB12
PubChem 71301
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
Pregnancy cat.

C(US)
Legal status

POM(UK) ℞-only(US)
Routes Oral

Nebivolol is a highly cardioselective vasodilatory beta1 receptor blocker used in treatment of hypertension. In most countries, this medication is available only by prescription.

Contents


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, 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.

[edit] Contraindications

  • Hepatic insufficiency
  • Children
  • Pregnancy
  • Lactation

[edit] Adverse Drug Reactions

[edit] References

  1. ^ 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.
  2. ^ 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.
  3. ^ Pessina, A.C., Metabolic effects and safety profile of nebivolol. J Cardiovasc Pharmacol, 2001. 38 Suppl 3: p. S33-5.
  4. ^ 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.
  5. ^ 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.
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Beta blockers (C07)
Non-selective β antagonists
β1 antagonists (cardioselective)
Atenolol • Acebutolol • Celiprolol • Betaxolol • Bisoprolol • Esmolol • Metoprolol • Nebivolol
Mixed α1/β antagonists