Physiologically based pharmacokinetic modelling of lisinopril in children: A case story of angiotensin converting enzyme inhibitors.
PBPK
angiotensin converting enzyme
children
lisinopril
paediatric
Journal
British journal of clinical pharmacology
ISSN: 1365-2125
Titre abrégé: Br J Clin Pharmacol
Pays: England
ID NLM: 7503323
Informations de publication
Date de publication:
03 2021
03 2021
Historique:
received:
27
01
2020
revised:
09
07
2020
accepted:
12
07
2020
pubmed:
22
7
2020
medline:
27
7
2021
entrez:
22
7
2020
Statut:
ppublish
Résumé
Lisinopril is an angiotensin converting enzyme inhibitor to treat hypertension. It shows complex pharmacokinetics (PK), and its PK behaviour in paediatric populations is not well characterized. The aim of this study was to develop a physiologically based PK (PBPK) model for lisinopril to describe the drug's PK in children. The PBPK model development was performed in a step-wise manner. An adult model was initially developed to characterize lisinopril's disposition and absorption and verified using literature data. Subsequently, the adult PBPK model was extrapolated to the paediatric population (0.5-18 years old) by accounting for age-dependent physiological and anatomical changes. Model performance was evaluated by comparing the PK profiles and drug exposures of observed vs predicted data. The disposition of lisinopril was well described by a minimal PBPK model-an effective strategy to capture the biphasic elimination of the drug. The absorption of lisinopril was described by the intestinal peptide transporter-mediated uptake. The adult model adequately described the literature data with predictions within a twofold range of clinical observations. Good model predictivity was also observed in children older than 6 years of age. The model overpredicted the drug exposure in children under 6 years, probably due to not incorporating the actual, unknown ontogeny of the intestinal peptide transporter. The PBPK model predicted the PK of lisinopril in adults and children above 6 years of age well. Model refinement in children under 6 years warrants future informative ontogeny data of the intestinal peptide transporter.
Substances chimiques
Angiotensin-Converting Enzyme Inhibitors
0
Lisinopril
E7199S1YWR
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
1203-1214Subventions
Organisme : Agency for Innovation by Science and Technology in Flanders
ID : IWT/SBO 130033
Informations de copyright
© 2020 The British Pharmacological Society.
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