Timing of Tedizolid Administration
Tedizolid can be administered at any time of day without regard to meals, as food does not alter total drug exposure, though it may delay absorption and reduce peak concentrations. 1, 2
Administration Flexibility
The key advantage of tedizolid is that timing flexibility does not compromise efficacy:
- Once-daily dosing at a consistent time each day is recommended to maintain steady therapeutic levels, though the specific time of day is not critical 1
- Peak plasma concentrations occur approximately 3 hours after oral administration under fasting conditions 1, 3
- When administered with food (high-fat, high-calorie meal), tedizolid absorption is delayed and maximum concentration (Cmax) is reduced, but total systemic exposure (AUC) remains unchanged 1, 2
- No dosage adjustment is necessary between intravenous and oral administration due to approximately 91% absolute bioavailability 1
Pharmacokinetic Rationale
The pharmacokinetic profile supports flexible timing:
- Tedizolid has a half-life of approximately 12 hours, allowing once-daily dosing 1, 4
- Steady-state concentrations are achieved within approximately 3 days with about 30% accumulation 1
- The pharmacodynamic parameter most closely associated with efficacy is fAUC(0-24h)/MIC (free drug area under the curve over 24 hours divided by minimum inhibitory concentration), not peak concentration 4, 5
Clinical Trial Dosing
In the pivotal ESTABLISH-1 and ESTABLISH-2 Phase III trials:
- Tedizolid 200 mg once daily for 6 days demonstrated non-inferior efficacy compared to linezolid 600 mg twice daily for 10 days 6, 7
- Both oral and sequential IV-to-oral regimens were studied with comparable efficacy 7
- The shorter 6-day course with once-daily dosing aligns with antimicrobial stewardship principles 7
Practical Considerations
For optimal patient adherence and therapeutic outcomes:
- Administer at the same time each day to maintain consistent drug levels 1
- Either oral or IV formulation can be given without timing adjustments between routes 1
- Patients can take tedizolid with or without food based on personal preference or tolerability 1, 2
- The 200 mg once-daily dose requires no adjustment for renal or hepatic dysfunction 1