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
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, 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.
Acute Bacterial Skin and Skin Structure Infection (ABSSSI): Intravenous: 200 mg Once daily 1 hour (Infusion Time) for 6 days Oral: 200 mg Once daily for 6 days 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.
No potential drug interactions with Tedizolid Phosphate were identified 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.
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.
The most common adverse reactions (>2%) are nausea, headache, diarrhea, vomiting, and dizziness
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.
Tedizolid Phosphate should be discontinued & general supportive treatment given.
Store in a cool (below 30°C) and dry place, away from light. Keep out of the reach of children.
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