Linezolid Dosing in Renal Impairment
No dose adjustment of linezolid is required for patients with renal impairment, including those with severe renal dysfunction or end-stage renal disease (ESRD), as the pharmacokinetics of the parent drug remain unchanged regardless of renal function. 1
Standard Dosing Across All Levels of Renal Function
The recommended dose is 600 mg every 12 hours (oral or IV) for adults with any degree of renal impairment, including mild, moderate, severe, or ESRD requiring hemodialysis. 1
This standard dosing applies because linezolid clearance is not altered by renal dysfunction—the parent drug's AUC, half-life, and volume of distribution remain similar to those in patients with normal renal function. 1
Critical Caveat: Metabolite Accumulation
While the parent drug does not accumulate, the two primary inactive metabolites do accumulate significantly in renal impairment, with accumulation severity increasing proportionally to renal dysfunction. 1
In patients with severe renal impairment (CrCl 10-30 mL/min), metabolite A AUC increases approximately 7-fold (from 7.6 to 56.5 mcg·h/mL) and metabolite B AUC increases approximately 7-fold (from 30.5 to 203 mcg·h/mL) compared to patients with normal renal function. 1
In ESRD patients on hemodialysis receiving 600 mg every 12 hours for 14.5 days, metabolite A AUC reached 153 mcg·h/mL and metabolite B AUC reached 356 mcg·h/mL. 1
The clinical significance of metabolite accumulation remains unknown, so use linezolid with caution in severe renal impairment and weigh the benefits against potential risks of metabolite accumulation. 1
Hemodialysis Considerations
Administer linezolid after hemodialysis sessions, as approximately 30% of a dose is removed during a 3-hour hemodialysis session when started 3 hours post-dose. 1
Despite dialytic removal, no supplemental dosing is required—maintain the standard 600 mg every 12 hours schedule. 1
Duration-Specific Dosing for Tuberculosis
For multidrug-resistant tuberculosis (MDR-TB) treated with BPaLM regimen, linezolid 600 mg once daily for 26 weeks is recommended, which differs from the twice-daily dosing used for other infections. 2
If toxicity develops during TB treatment, the dose may be reduced to 300 mg daily, though 600 mg daily throughout the regimen is preferred. 2
Monitoring Recommendations
Monitor complete blood counts weekly in patients receiving linezolid for more than 14 days, as reversible thrombocytopenia, anemia, and neutropenia can occur, particularly with prolonged therapy. 3
Consider therapeutic drug monitoring (TDM) in patients with renal insufficiency or those on renal replacement therapy to optimize dosing and minimize toxicity risk, targeting AUC/MIC ratios of 80-120 for optimal efficacy. 4, 5