Linezolid
Linezolid. Oxazolidinone — binds 23S rRNA of bacterial 50S subunit blocking 70S initiation complex formation. Active against MRSA + VRE.… Oral half-life 9.5 h.
Oxazolidinone — binds 23S rRNA of bacterial 50S subunit blocking 70S initiation complex formation. Active against MRSA + VRE. Reversible MAO inhibition → serotonin syndrome risk with SSRIs. Bone marrow suppression at courses > 14 days.
PK: Burkhardt 2002 (PMID:12407127), 12 healthy volunteers on 600 mg twice daily, verbatim day-1 terminal half-life "9.53 +/- 2.87" h. F 1 is Welshman 2001 (PMID:11745911), a true absolute-bioavailability study, verbatim "the mean absolute bioavailability (F) of the tablet, using the IV sterile solution as the reference treatment, was 103% (+/-20%)" — stored as 1 rather than 1.03 since a fraction above unity is unphysical. ka 1.81 /h is Plock 2007 (PMID:17639029). None of the values stored until 2026-09-06 came from the cited paper: PMID:12936973 studies renal impairment, reports only clearances, and — decisively — has NO IV ARM despite having been cited for the whole IV block, which now points at the study that does. V dropped: the only human figures are sex-split, "41.6 +/- 4.2 versus 52.2 +/- 3.3 L/70 kg" (PMID:12407127), and collapsing them would be an average; the stored 45 L appears in no primary, only in a review. CAVEAT: exposure accumulates on repeated dosing while the half-life does not change — AUC rose from 140.5 to 220.2 mg.h/L between days 1 and 7 (PMID:12407127) through time-dependent inhibition of clearance (PMID:17639029) — so a fixed one-compartment curve under-predicts steady state.
Pharmacokinetics
- Oral — t½ 9.5 h · F 100% · ka 1.81 h⁻¹
- IV — t½ 9.5 h · F 100%
Sources: PMID:12936973, PMID:12407127, PMID:11745911, PMID:17639029, PMID:23926058