tedizolid
Brand: Sivextro
Prototype: linezolid
Drug Class: oxazolidinone antibiotic
Drug Family: antibiotic
Subclass: next-generation oxazolidinone
Organ Systems: infectious-disease
Mechanism of Action
Prodrug phosphate ester hydrolyzed in vivo to active tedizolid; binds 50S ribosomal subunit at same site as linezolid, blocking initiation complex formation; 4–16-fold more potent than linezolid in vitro with less myelosuppression.
50S ribosomal subunit (23S rRNA)
Indications
- acute bacterial skin and skin structure infections (ABSSSI) due to gram-positive organisms including MRSA
Contraindications
- oxazolidinone hypersensitivity
- concurrent MAOI use
Adverse Effects
Common
- nausea
- headache
- diarrhea
- vomiting
Serious
- myelosuppression (less than linezolid)
- serotonin syndrome
- peripheral neuropathy (less common than linezolid at 6 days)
Pharmacokinetics (ADME)
| Absorption | 91% oral bioavailability; IV and oral interchangeable |
| Distribution | widely distributed; high tissue concentrations |
| Metabolism | prodrug hydrolyzed to active form |
| Excretion | primarily fecal (81%) — no dose adjustment in renal or hepatic impairment |
| Half-life | 12 hours |
| Onset | rapid |
| Peak | 3 hours (oral) |
| Duration | 24 hours (once-daily) |
| Protein Binding | 70–90% |
| Vd | large |
Drug Interactions
| Drug / Agent | Mechanism | Severity |
|---|---|---|
| serotonergic drugs | weak MAO-A inhibition; serotonin syndrome risk (lower than linezolid) | moderate |
| dopaminergic drugs | MAO-A inhibition may potentiate; lower risk than linezolid | minor |
Nursing Considerations
- Once-daily dosing for only 6 days makes tedizolid adherence-friendly; confirm the patient understands the 6-day duration.
- No renal or hepatic dose adjustment needed — an advantage over linezolid.
- Serotonergic interactions are a class effect; screen for SSRIs, SNRIs, and other serotonergic drugs, though risk is lower than with linezolid.
- CBC monitoring is not routinely required for the 6-day course due to low myelosuppression risk at this duration.
Clinical Pearls
- Tedizolid's shorter 6-day treatment course and once-daily dosing, combined with lower rates of myelosuppression than linezolid, give it a favorable safety profile for short-duration ABSSSI treatment.
- Tedizolid is active against some linezolid-resistant organisms (cfr-gene mediated resistance) due to structural modifications, though high-level cross-resistance remains an ongoing concern.
Safety Profile
Pregnancy use-with-caution
Lactation use-with-caution
Renal Adjustment Not required
Hepatic Adjustment Not required
TDM Not required
Concordance Terms
Cross-referenced clinical concepts — click any term to see all content where it appears.