New Data for Nebivolol after In Silico PK Study: Focus on Young Patients and Dosage Regimen

Nebivolol (NEB) is a highly selective β1 receptor antagonist with a distinct pharmacological profile. This drug is approved for the treatment of hypertension in the US, and hypertension and heart failure in Europe. Here, we review observations based on age dependence and explore new drug regimens wi...

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Main Authors: Lara Marques, Bárbara Costa, Nuno Vale
Format: Article
Language:English
Published: MDPI AG 2022-09-01
Series:Pharmaceutics
Subjects:
Online Access:https://www.mdpi.com/1999-4923/14/9/1911
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author Lara Marques
Bárbara Costa
Nuno Vale
author_facet Lara Marques
Bárbara Costa
Nuno Vale
author_sort Lara Marques
collection DOAJ
description Nebivolol (NEB) is a highly selective β1 receptor antagonist with a distinct pharmacological profile. This drug is approved for the treatment of hypertension in the US, and hypertension and heart failure in Europe. Here, we review observations based on age dependence and explore new drug regimens with in-silico studies, to achieve better efficacy and safety. The clinical data were obtained from six published literature reports. Then the data were used for model building, evaluation, and simulation. A two-compartment model with first-order absorption, lag time, linear elimination, and the following covariates: age and genotype were the ones best describing our population. Simulation of different dose regimens resulted in an increase chance of efficacy and safety when the dose regimen was altered to 6 mg every 36 h. It is worth noting that our population in this study constituted of young and healthy individuals. Studies regarding the effects of NEB according to age are scarce; however, they are needed to further improve efficacy and safety, and reduce adverse effects.
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spelling doaj.art-161ef9fccbbf4ea398b320807bc4a0e42023-11-23T18:22:50ZengMDPI AGPharmaceutics1999-49232022-09-01149191110.3390/pharmaceutics14091911New Data for Nebivolol after In Silico PK Study: Focus on Young Patients and Dosage RegimenLara Marques0Bárbara Costa1Nuno Vale2OncoPharma Research Group, Center for Health Technology and Services Research (CINTESIS), Rua Dr. Plácido da Costa, 4200-450 Porto, PortugalOncoPharma Research Group, Center for Health Technology and Services Research (CINTESIS), Rua Dr. Plácido da Costa, 4200-450 Porto, PortugalOncoPharma Research Group, Center for Health Technology and Services Research (CINTESIS), Rua Dr. Plácido da Costa, 4200-450 Porto, PortugalNebivolol (NEB) is a highly selective β1 receptor antagonist with a distinct pharmacological profile. This drug is approved for the treatment of hypertension in the US, and hypertension and heart failure in Europe. Here, we review observations based on age dependence and explore new drug regimens with in-silico studies, to achieve better efficacy and safety. The clinical data were obtained from six published literature reports. Then the data were used for model building, evaluation, and simulation. A two-compartment model with first-order absorption, lag time, linear elimination, and the following covariates: age and genotype were the ones best describing our population. Simulation of different dose regimens resulted in an increase chance of efficacy and safety when the dose regimen was altered to 6 mg every 36 h. It is worth noting that our population in this study constituted of young and healthy individuals. Studies regarding the effects of NEB according to age are scarce; however, they are needed to further improve efficacy and safety, and reduce adverse effects.https://www.mdpi.com/1999-4923/14/9/1911Nebivololin silico pharmacologypopulation PKdosage regimen
spellingShingle Lara Marques
Bárbara Costa
Nuno Vale
New Data for Nebivolol after In Silico PK Study: Focus on Young Patients and Dosage Regimen
Pharmaceutics
Nebivolol
in silico pharmacology
population PK
dosage regimen
title New Data for Nebivolol after In Silico PK Study: Focus on Young Patients and Dosage Regimen
title_full New Data for Nebivolol after In Silico PK Study: Focus on Young Patients and Dosage Regimen
title_fullStr New Data for Nebivolol after In Silico PK Study: Focus on Young Patients and Dosage Regimen
title_full_unstemmed New Data for Nebivolol after In Silico PK Study: Focus on Young Patients and Dosage Regimen
title_short New Data for Nebivolol after In Silico PK Study: Focus on Young Patients and Dosage Regimen
title_sort new data for nebivolol after in silico pk study focus on young patients and dosage regimen
topic Nebivolol
in silico pharmacology
population PK
dosage regimen
url https://www.mdpi.com/1999-4923/14/9/1911
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