tedizolid phosphate: clinical use

Prescribing considerations

• Reserve antibiotic: use should reflect antimicrobial stewardship, susceptibility information and local microbiology advice.
• Clinical experience is limited in secondary bacteraemia and absent in severe sepsis or septic shock associated with the licensed infection.
• Alternative therapy should be considered in neutropenia because clinical efficacy has not been established in this group.
• Oral and intravenous exposure is similar, supporting route conversion when clinically appropriate.

Contraindications and cautions

• Hypersensitivity to tedizolid phosphate or a formulation excipient.
• Use caution with previous hypersensitivity to another oxazolidinone because cross-reactivity may occur.
• Use caution with prior antibiotic-associated diarrhoea, renal impairment, bleeding tendency or concomitant serotonergic medicines.

Monitoring

• Review for diarrhoea during and after treatment and investigate suspected Clostridioides difficile infection.
• Check blood counts if myelosuppression is suspected or relevant risk factors are present.
• Assess promptly for visual disturbance or peripheral neuropathy symptoms.
• Monitor for serotonin syndrome when serotonergic medicines cannot be avoided.

Clinical pharmacology

Tedizolid phosphate is converted by phosphatases to tedizolid. Tedizolid inhibits bacterial protein synthesis at the 50S ribosomal subunit and is mainly active against Gram-positive organisms. Oral bioavailability exceeds 90%; metabolism is not substantially dependent on cytochrome P450 enzymes.

Formulation and product differences

• Tablets are swallowed whole and may be taken with or without food.
• The powder formulation requires reconstitution and dilution and must be given by intravenous infusion, not intravenous bolus.
• The infusion is incompatible with solutions containing divalent cations, including Hartmann’s and lactated Ringer’s solutions.
• The intravenous formulation is essentially sodium-free.

Solution for infusion

Route: Intravenous

Strengths: 200 mg

Tablet

Route: Oral

Strengths: 200 mg