Cargando…

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...

Descripción completa

Detalles Bibliográficos
Autores principales: Marques, Lara, Costa, Bárbara, Vale, Nuno
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9502491/
https://www.ncbi.nlm.nih.gov/pubmed/36145659
http://dx.doi.org/10.3390/pharmaceutics14091911
_version_ 1784795718917029888
author Marques, Lara
Costa, Bárbara
Vale, Nuno
author_facet Marques, Lara
Costa, Bárbara
Vale, Nuno
author_sort Marques, Lara
collection PubMed
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.
format Online
Article
Text
id pubmed-9502491
institution National Center for Biotechnology Information
language English
publishDate 2022
publisher MDPI
record_format MEDLINE/PubMed
spelling pubmed-95024912022-09-24 New Data for Nebivolol after In Silico PK Study: Focus on Young Patients and Dosage Regimen Marques, Lara Costa, Bárbara Vale, Nuno Pharmaceutics Article 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. MDPI 2022-09-09 /pmc/articles/PMC9502491/ /pubmed/36145659 http://dx.doi.org/10.3390/pharmaceutics14091911 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Marques, Lara
Costa, Bárbara
Vale, Nuno
New Data for Nebivolol after In Silico PK Study: Focus on Young Patients and 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 Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9502491/
https://www.ncbi.nlm.nih.gov/pubmed/36145659
http://dx.doi.org/10.3390/pharmaceutics14091911
work_keys_str_mv AT marqueslara newdatafornebivololafterinsilicopkstudyfocusonyoungpatientsanddosageregimen
AT costabarbara newdatafornebivololafterinsilicopkstudyfocusonyoungpatientsanddosageregimen
AT valenuno newdatafornebivololafterinsilicopkstudyfocusonyoungpatientsanddosageregimen