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Population Pharmacokinetics of Linezolid: A Systematic Review
  • +2
  • Yan Qin,
  • Li-li Zhang,
  • Yan-rong Ye,
  • Yue-ting Chen,
  • Zheng Jiao
Yan Qin
Shanghai Chest Hospital

Corresponding Author:celeryan@163.com

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Li-li Zhang
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Yan-rong Ye
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Yue-ting Chen
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Zheng Jiao
Shanghai Jiao Tong University Affiliated Chest Hospital
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Background Linezolid is often used for the infections caused by drug-resistant Gram-positive bacteria. Recent studies suggested that large between-subject variability (BSV) and within-subject variability could alter drug pharmacokinetics (PK) during linezolid therapy due to pathophysiological changes. Objective The review synthesized information on linezolid population PK studies and summarized the significant covariates that influence the PKs of linezolid. Methods A literature search was performed from PubMed, Web of Science, and Embase from their inception to 30 September 2021. Published studies were included if they contained data analyzing linezolid PK parameters in humans using a population approach with a nonlinear mixed-effects model. Results Twenty-five studies were included in adults and five studies in pediatric patients. One- and two-compartment models were the commonly used structural models for linezolid. Body size [weight, lean body weight, and body surface area], creatinine clearance (CLcr), and age significantly influenced linezolid PK. The median clearance (CL) values (range) in infants [0.128 L/h/kg (0.121-0.135)] and children [0.107 L/h/kg (0.088-0.151)] were higher than in adults [0.098 L/h/kg (0.044-0.237)]. For patients with severe renal impairment (CLcr ≤ 30 mL/min), the CL was 37.2% (15.2-55.3%) lower than in patients with normal renal function. Conclusion Linezolid’s optimal dosage could be adjusted based on the patient’s body size, renal function, and age. More studies are needed to explore the exact mechanism of elimination of linezolid and evaluate PK characteristics in pediatric patients.
29 Jan 2022Submitted to British Journal of Clinical Pharmacology
31 Jan 2022Submission Checks Completed
31 Jan 2022Assigned to Editor
10 Feb 2022Reviewer(s) Assigned
10 Mar 2022Review(s) Completed, Editorial Evaluation Pending
11 Mar 2022Editorial Decision: Revise Major
15 Apr 20221st Revision Received
16 Apr 2022Submission Checks Completed
16 Apr 2022Assigned to Editor
16 Apr 2022Review(s) Completed, Editorial Evaluation Pending
20 Apr 2022Editorial Decision: Accept