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After conversion to its active form by phosphatases, tedizolid exerts its antibacterial activity through inhibition of protein synthesis by binding to the 50S ribosomal subunit of susceptible Gram-positive bacteria. Cross-resistance between other non-oxazolidinone antibacterial drugs is unlikely as it inhibits bacterial protein synthesis through a different mechanism.
Tedizolid is an oxazolidinone-class antibacterial drug indicated in adults for the treatment of acute bacterial skin and skin structure infections (ABSSSI) caused by designated susceptible bacteria.
To reduce the development of drug-resistant bacteria and maintain the effectiveness of Tedizolid and other antibacterial drugs, Tedizolid should be used only to treat or prevent infections that are proven or strongly suspected to be caused by susceptible bacteria
Acute Bacterial Skin and Skin Structure Infection (ABSSSI):
No dose adjustment is necessary when changing from intravenous to oral Tedizolid. If patients miss a dose, they should take it as soon as possible anytime up to 8 hours prior to their next scheduled dose. If less than 8 hours remain before the next dose, wait until their next scheduled dose.
None
The most common adverse reactions (>2%) are nausea, headache, diarrhea, vomiting, and dizziness
Overdose Effects
In the event of overdosage, Tedizolid should be discontinued and general supportive treatment given. Hemodialysis does not result in meaningful removal of tedizolid from systemic circulation
Patients with neutropenia: The safety and efficacy of Tedizolid in patients with neutropenia (neutrophil counts <1000 cells/mm3) have not been adequately evaluated. In an animal model of infection, the antibacterial activity of Tedizolid was reduced in the absence of granulocytes. Consider alternative therapies in neutropenic patients.
Clostridium difficile-associated diarrhea: Evaluate if diarrhea occurs.
Use in Special Populations
Pediatric Use: Safety and effectiveness in pediatric patients below the age of 18 have not been established.
Geriatric Use: Clinical studies of Tedizolid did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. No overall differences in pharmacokinetics were observed between elderly subjects and younger subjects
Pregnancy & Lactation
Pregnancy category C. There are no adequate and well-controlled studies of Tedizolid in pregnant women. Tedizolid should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Nursing Mothers: Tedizolid is excreted in the breast milk of rats. It is not known whether tedizolid is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Tedizolid is administered to a nursing woman.