Population pharmacokinetics and target attainment analysis of linezolid in multidrug-resistant tuberculosis patients.
Mycobacterium tuberculosis
dose optimisation
linezolid
multidrug-resistant
pharmacokinetics
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:
02 2022
02 2022
Historique:
revised:
31
08
2021
received:
08
02
2021
accepted:
22
09
2021
pubmed:
9
10
2021
medline:
27
4
2022
entrez:
8
10
2021
Statut:
ppublish
Résumé
This study investigates the pharmacokinetic/pharmacodynamic (PK/PD) target attainment of linezolid in patients infected with multidrug-resistant (MDR) tuberculosis (TB). A pharmacometric model was developed including 244 timed linezolid concentration samples from 39 patients employing NONMEM 7.4. The probability of target attainment (PTA, PK/PD target: unbound (f) area-under-the-concentration-time-curve (AUC)/minimal inhibitory concentration (MIC) of 119) as well as a region-specific cumulative fraction of response (CFR) were estimated for different dosing regimens. A one-compartment model with linear elimination with a clearance (CL) of 7.69 L/h (interindividual variability 34.1%), a volume of distribution (Vd) of 45.2 L and an absorption constant (KA) of 0.679 h This study showed that a dose of 300 mg twice daily of linezolid might not be sufficient to treat MDR-TB patients from a PK/PD perspective. Thus, it might be recommendable to start with a higher dose of 600 mg twice daily to ensure PK/PD target attainment. Hereby, therapeutic drug monitoring and MIC determination should be performed to control PK/PD target attainment as linezolid shows high variability in its PK in the TB population.
Substances chimiques
Anti-Bacterial Agents
0
Linezolid
ISQ9I6J12J
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
1835-1844Informations de copyright
© 2021 The Authors. British Journal of Clinical Pharmacology published by John Wiley & Sons Ltd on behalf of British Pharmacological Society.
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