Nebivolol is a beta blocker used to treat high blood pressure and heart failure.[6] As with other β-blockers, it is generally a less preferred treatment for high blood pressure. It may be used by itself or with other blood pressure medication. It is taken by mouth.
Common side effects include dizziness, feeling tired, nausea, and headaches. Serious side effects may include heart failure and bronchospasm. Its use in pregnancy and breastfeeding is not recommended.[6][7] It works by blocking β1-adrenergic receptors in the heart and dilating blood vessels.[8][9]
Nebivolol was patented in 1983 and came into medical use in 1997.[10] It is available as a generic medication in the United Kingdom.[6] In 2023, it was the 191st most commonly prescribed medication in the United States, with more than 2million prescriptions.[11][12]
Medical uses
It is used to treat high blood pressure and heart failure.[6] Nebivolol is used in the treatment of angina, to decrease the heart rate and contractile force. This is relevant in patients who need to decrease the oxygen demand of the heart so that the blood supplied from stenosed or constricted arteries is adequate.
ACE inhibitors, angiotensin II receptor antagonists, calcium-channel blockers, and thiazide diuretics are generally preferred over beta blockers for the treatment of primary hypertension in the absence of co-morbidities.[13][14][15][16]
Contraindications
- Severe bradycardia
- Heart block greater than first degree
- Patients with cardiogenic shock
- Decompensated cardiac failure
- Sick sinus syndrome (unless a permanent pacemaker is in place)
- Patients with severe hepatic impairment (Child-Pugh class B)
- Patients who are hypersensitive to any component of this product.
Side effects
Side effects might include headache, tiredness, dizziness, lightheadedness, reduced blood flow to extremities, bradycardia.[17]
Interactions
Due to enzymatic inhibition, fluvoxamine increases the exposure to nebivolol and its active hydroxylated metabolite (4-OH-nebivolol) in healthy volunteers.[18]
Pharmacology
Pharmacodynamics
β1-selectivity
Beta blockers help patients with cardiovascular disease by blocking β1 receptors, while many of the side-effects of these medications are caused by their blockade of β2 receptors.[19] For this reason, beta blockers that selectively block β1 adrenergic receptors (termed cardioselective or β1-selective beta blockers) produce fewer adverse effects (for instance, bronchoconstriction) than those drugs that non-selectively block both β1 and β2 receptors.
In a laboratory experiment conducted on biopsied heart tissue, nebivolol proved to be the most β1-selective of the β-blockers tested, being approximately 3.5 times more β1-selective than bisoprolol.[20] However, the drug's receptor selectivity in humans is more complex and depends on the drug dose and the genetic profile of the patient taking the medication.[21]
Chemistry
The experimental log P of nebivolol is 4.18 and its predicted log P ranges from 2.44 to 4.21.[37][38][39] It is a highly lipophilic beta blocker.[40] The drug showed the fourth highest predicted lipophilicity of 30clinically relevant beta blockers, with the most lipophilic beta blockers predicted to be bopindolol, penbutolol, and carvedilol.[41]
Society and culture
Brand names and marketing
Mylan Laboratories licensed the US and Canadian rights to nebivolol from Janssen Pharmaceutica N.V. in 2001. Nebivolol is already registered and successfully marketed in more than 50 countries, including the United States where it is marketed under the brand name Bystolic from Mylan Laboratories and Forest Laboratories. Nebivolol is manufactured by Forest Laboratories.
In India, nebivolol is available as Nebula (Zydus Healthcare Ltd), Nebizok (Eris life-sciences), Nebicip (Cipla ltd), Nebilong (Micro Labs), Nebistar (Lupin ltd), Nebicard (Torrent), Nubeta (Abbott Healthcare Pvt Ltd – India), and Nodon (Cadila Pharmaceuticals).
In Greece and Italy, nebivolol is marketed by Menarini as Lobivon.
In Germany it is marketed as Nebilet by Berlin Chemie.
In the Middle East, Russia and Australia, it is marketed under the name Nebilet and in Pakistan it is marketed by The Searle Company Limited as Byscard.
Controversies
References
- Nebaloc (Pharmacor Pty Ltd) Therapeutic Goods Administration (TGA), 13 March 2025, retrieved 24 March 2025^
- Drugs@FDA: FDA-Approved Drugs Nebivolol - ALLERGAN accessdata.fda.gov, retrieved 17 August 2022^
- Rationale for nebivolol/valsartan combination for hypertension: review of preclinical and clinical data Journal of Hypertension, September 2017^