Clinical pharmacokinetics of nebivolol: a systematic review

Abstract

Nebivolol is a beta-1 receptor blocker used to treat hypertension, heart failure, erectile dysfunction, vascular disease, and diabetes mellitus. This review investigated the data regarding pharmacokinetic (PK) parameters, drug-drug interactions, dextrorotatory (D), and levorotatory (L) stereoisomers of nebivolol. The articles related to the PK of nebivolol were retrieved by searching the five databases; Google Scholar, PubMed, Cochrane Library, ScienceDirect, and EBSCO. A total of 20 studies comprising plasma concentration-time profile data following the nebivolol’s oral and intravenous (IV) administration were included. The area under the concentration-time curve from zero to infinity (AUC_0-∞) was 15 times greater in poor metabolizers (PMs) than in extensive metabolizers (EMs). In hypertensive patients, L–nebivolol expressed a higher maximum plasma concentration (C_max) than D–nebivolol, i.e. 2.5 ng/ml vs 1.2 ng/ml. The AUC_0-∞ of nebivolol was 3-fold greater in chronic kidney disease (CKD). The clearance (CL) was increased in obese than in controls from 51.6 ± 11.6 L/h to 71.6 ± 17.4 L/h when 0.5 mg/ml IV solution was infused. Nebivolol showed higher C_max, AUC_0-∞ and half-life (t_1/2) when co-administered with bupropion, duloxetine, fluvoxamine, paroxetine, lansoprazole, and fluoxetine. This concise review of nebivolol would be advantageous in assessing all PK parameters, which may be crucial for clinicians to avoid drug-drug interactions, prevent adverse drug events and optimize the dosage regimen in diseased patients diagnosed with hypertension and cardiovascular disorders.

Keywords:

• Nebivolol
• beta-blockers
• PK parameters
• systematic review
• D and L enantiomers
• CYP2D6 genotype
• hypertension

Availability of data

All the data supporting the results used for this publication is presented in the main article or in the Supplementary Information.

Disclosure statement

The authors declare that they have no potential conflicts of interest that might be relevant to the contents of this manuscript.

Additional information

Funding

This work was funded by the Distinguished Scientist Fellowship program at King Saud University, Riyadh, Saudi Arabia, through research supporting project number (RSP2023R131).