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Pharmacokinetics of nebivolol
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<blockquote data-quote="madman" data-source="post: 268524" data-attributes="member: 13851"><p><strong>ABSTRACT</strong></p><p></p><p><em><strong>Nebivolol is a beta-1 receptor blocker used to treat hypertension, heart failure, erectile dysfunction, vascular disease, and diabetes mellitus.</strong> <strong>This review investigated the data regarding pharmacokinetic (PK) parameters, drug-drug interactions, dextrorotatory (D), and levorotatory (L)stereoisomers of nebivolol. </strong>The articles related to the PK of nebivolol were retrieved by searchingthe 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. <strong>The area under the concentration-time curve from zero to infinity (AUC0-1) was 15 times greater in poor metabolizers (PMs) than in extensive metabolizers (EMs). In hypertensive patients, L–nebivolol expressed a higher maximum plasma concentration (Cmax) than D–nebivolol, i.e. 2.5 ng/ml vs 1.2 ng/ml. The AUC0-1 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 Cmax, AUC0-1, and half-life (t1/2) when co-administered with bupropion, duloxetine, fluvoxamine, paroxetine, lansoprazole, and fluoxetine. </strong>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.</em></p><p></p><p></p><p></p><p></p><p><strong>1. Introduction</strong></p><p></p><p><em><strong>Nebivolol is a third-generation, long-acting, cardioselective b1-adrenoreceptor antagonist, approved by the United States Food and Drug Administration (FDA)in December 2007 for the <u>treatment of hypertension</u> (Wojciechowski and Papademetriou 2008; Fongemieand Felix-Getzik 2015).<u> It is effective in diabetes mellitus, erectile dysfunction, vascular disease, and angina pectoris, along with its off-label use in heart failure</u> (Cheng 2009; Priyadarshni and Curry 2022). <u>Nebivolol is highly selective for the b1 receptor blockade, promoting vasodilation through endothelium-dependent nitric oxide (NO) stimulation</u> (Toblli et al. 2012). <u>Nebivolol differs from other b-blockers due to its unusual vasodilatory activity by L-arginine–NO pathway</u> (Gray and Ndefo 2008). Nebivolol is a racemate of dextrorotatory(D) and levorotatory (L) enantiomers, among which D–nebivolol is involved in b1-receptor blocking activity, whereas L–nebivolol exhibits vasodilator properties (Marketou et al. 2017). It is mainly administered through the extravascular route (Priyadarshni and Curry 2022).</strong></em></p><p></p><p></p><p></p><p></p><p><strong>5. Conclusion</strong></p><p></p><p><em><strong>This review reveals all the human data of nebivolol regarding its PK parameters, dosage form characteristics, and drug-drug interactions in healthy and diseased participants. <u>The Cmax, Tmax, and AUC0-1 are greater in poor metabolizers than in extensive metabolizers</u>.<u> The CYP2D6 phenotypes do not affect the PK of nebivolol, whereas the AUC0-1 notably increases in CKD patients</u>. <u>This comprehensive review compiles all the PK parameters that could be helpful in the development of PK models</u>. <u>Additionally, it will be convenient for practitioners to predict the dose and eliminate the drug-drug interactions in hypertension, cardiac failure, and renal impairment</u>. Furthermore, it will be beneficial in the amendment of future clinical trials.</strong></em></p></blockquote><p></p>
[QUOTE="madman, post: 268524, member: 13851"] [B]ABSTRACT[/B] [I][B]Nebivolol is a beta-1 receptor blocker used to treat hypertension, heart failure, erectile dysfunction, vascular disease, and diabetes mellitus.[/B] [B]This review investigated the data regarding pharmacokinetic (PK) parameters, drug-drug interactions, dextrorotatory (D), and levorotatory (L)stereoisomers of nebivolol. [/B]The articles related to the PK of nebivolol were retrieved by searchingthe 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. [B]The area under the concentration-time curve from zero to infinity (AUC0-1) was 15 times greater in poor metabolizers (PMs) than in extensive metabolizers (EMs). In hypertensive patients, L–nebivolol expressed a higher maximum plasma concentration (Cmax) than D–nebivolol, i.e. 2.5 ng/ml vs 1.2 ng/ml. The AUC0-1 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 Cmax, AUC0-1, and half-life (t1/2) when co-administered with bupropion, duloxetine, fluvoxamine, paroxetine, lansoprazole, and fluoxetine. [/B]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.[/I] [B]1. Introduction[/B] [I][B]Nebivolol is a third-generation, long-acting, cardioselective b1-adrenoreceptor antagonist, approved by the United States Food and Drug Administration (FDA)in December 2007 for the [U]treatment of hypertension[/U] (Wojciechowski and Papademetriou 2008; Fongemieand Felix-Getzik 2015).[U] It is effective in diabetes mellitus, erectile dysfunction, vascular disease, and angina pectoris, along with its off-label use in heart failure[/U] (Cheng 2009; Priyadarshni and Curry 2022). [U]Nebivolol is highly selective for the b1 receptor blockade, promoting vasodilation through endothelium-dependent nitric oxide (NO) stimulation[/U] (Toblli et al. 2012). [U]Nebivolol differs from other b-blockers due to its unusual vasodilatory activity by L-arginine–NO pathway[/U] (Gray and Ndefo 2008). Nebivolol is a racemate of dextrorotatory(D) and levorotatory (L) enantiomers, among which D–nebivolol is involved in b1-receptor blocking activity, whereas L–nebivolol exhibits vasodilator properties (Marketou et al. 2017). It is mainly administered through the extravascular route (Priyadarshni and Curry 2022).[/B][/I] [B]5. Conclusion[/B] [I][B]This review reveals all the human data of nebivolol regarding its PK parameters, dosage form characteristics, and drug-drug interactions in healthy and diseased participants. [U]The Cmax, Tmax, and AUC0-1 are greater in poor metabolizers than in extensive metabolizers[/U].[U] The CYP2D6 phenotypes do not affect the PK of nebivolol, whereas the AUC0-1 notably increases in CKD patients[/U]. [U]This comprehensive review compiles all the PK parameters that could be helpful in the development of PK models[/U]. [U]Additionally, it will be convenient for practitioners to predict the dose and eliminate the drug-drug interactions in hypertension, cardiac failure, and renal impairment[/U]. Furthermore, it will be beneficial in the amendment of future clinical trials.[/B][/I] [/QUOTE]
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