Tedizolid Phosphate is an oxazolidinone-class antibacterial indicated for the treatment of acute bacterial skin and skin structure infections (ABSSSI) caused by susceptible isolates of the following Gram-positive microorganisms: Staphylococcus aureus (including methicillin-resistant and methicillin-susceptible isolates), Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus anginosus Group (including Streptococcus anginosus, Streptococcus intermedius, and Streptococcus constellatus), and Enterococcus faecalis.

Tedizolid Phosphate is a prodrug that is converted by phosphatases to Tedizolid, the microbiologically active moiety, following oral and intravenous administration. Following multiple once-daily oral or intravenous administration, steady-state concentrations are achieved within approximately three days with Tedizolid, with accumulation of approximately 30% (Tedizolid half-life of approximately 12 hours). Peak plasma Tedizolid concentrations are achieved within approximately 3 hours following oral administration under fasting conditions. The absolute bioavailability is approximately 91%, and no dosage adjustment is necessary between intravenous and oral administration. Protein binding of Tedizolid to human plasma proteins is approximately 70 to 90%. Other than Tedizolid Phosphate, which accounts for approximately 95% of the total radiocarbon AUC in plasma, there are no other significant circulating metabolites in humans. There was no degradation of Tedizolid in human liver microsomes, indicating Tedizolid Phosphate is unlikely to be a substrate for hepatic CYP450 enzymes. Following single oral administration of 14C-labeled Tedizolid Phosphate under fasted conditions, the majority of elimination occurred via the liver, with 82% of the radioactive dose recovered in feces and 18% in urine.

Tedizolid Phosphate is recommended in patients with 18 years of age or older. Tedizolid should be administered 200 mg once daily for six (6) days orally (with or without food). If patients miss a dose, they should take it as soon as possible at 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.

Use in Children & Adolescents: Safety and effectiveness in paediatric patients below the age of 18 have not been established. No overall differences in pharmacokinetics were observed between elderly subjects and younger subjects.

No potential drug interactions with Tedizolid Phosphate were identified in in vitro CYP inhibition or induction studies. No clinically significant inhibition of any transporter was observed at Tedizolid Phosphate circulating plasma concentrations. Tedizolid Phosphate is a reversible inhibitor of monoamine oxidase in vitro.

Tedizolid Phosphate is contraindicated in patients who have known hypersensitivity to Tedizolid Phosphate or any other components of Tedizolid Phosphate.

The most common side effects in patients treated with Tedizolid Phosphate are nausea, headache, diarrhea, vomiting, and dizziness. The following selected adverse reactions may be reported in Tedizolid Phosphate treated patients: anemia, palpitations, tachycardia, blurred vision, visual impairment, infusion-related reactions, drug hypersensitivity, insomnia, pruritus, urticaria, dermatitis, and hypertension, etc.

Pregnancy & Lactation
Pregnancy category C. There are no adequate and well-controlled studies of Tedizolid Phosphate in pregnant women. Tedizolid Phosphate should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. It is not known whether Tedizolid Phosphate is excreted in human milk.

Precautions & Warnings
Alternative therapies should be considered when treating patients with neutropenia and acute bacterial skin and skin structure infection, Clostridium difficile-associated diarrhea, and the risk of the development of drug-resistant bacteria.

Pharmaceutical precautions: Administer Tedizolid Phosphate infusion as an intravenous infusion only. The intravenous bag containing the reconstituted and diluted intravenous solution should be inspected visually for particulate matter prior to administration. After reconstitution and dilution, it is to be administered via intravenous infusion using a total time of 1 hour. The total time from reconstitution to administration should not exceed 24 hours at room temperature or under refrigeration at 2°C to 8°C.

Overdose Effects
Tedizolid Phosphate should be discontinued and general supportive treatment given.

Therapeutic Class
Other antibiotic

Storage Conditions
Store in a cool (below 30°C) and dry place, away from light. Keep out of the reach of children.

Pregnancy category C. There are no adequate and well-controlled studies of Tedizolid Phosphate in pregnant women. Tedizolid Phosphate should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. It is not known whether Tedizolid Phosphate is excreted in human milk.

Alternative therapies should be considered when treating patients with neutropenia and acute bacterial skin and skin structure infection, Clostridium difficile-associated diarrhea, and the risk of the development of drug-resistant bacteria.

Pharmaceutical precautions: Administer Tedizolid Phosphate infusion as an intravenous infusion only. The intravenous bag containing the reconstituted and diluted intravenous solution should be inspected visually for particulate matter prior to administration. After reconstitution and dilution, it is to be administered via intravenous infusion using a total time of 1 hour. The total time from reconstitution to administration should not exceed 24 hours at room temperature or under refrigeration at 2°C to 8°C.

Tedizolid Phosphate should be discontinued and general supportive treatment given.

Other antibiotic

Store in a cool (below 30°C) and dry place, away from light. Keep out of the reach of children.