Tezolid 200-MG Tablet

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.

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 Tezolid were identified in vitro CYP inhibition or induction studies. No clinically significant inhibition of any transporter was observed at Tezolid circulating plasma concentrations. Tezolid 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 Tezolid are nausea, headache, diarrhea, vomiting and dizziness. The following selected adverse reactions may be reported in Tezolid treated patients: anemia, palpitations, tachycardia, blurred vision, visual impairment, infusion-related reactions, drug hypersensitivity, insomnia, pruritus, urticaria, dérmatitis and hypertension etc.

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 Tezolid 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.

Tezolid should be discontinued & general supportive treatment given.

Other antibacterial preparation

The contents of the vial should be reconstituted using aseptic technique as follows:

To minimize foaming, avoid vigorous agitation or shaking of the vial during or after reconstitution.

Reconstitute the Tezolid vial with 4 ml of normal saline from the bottle with the syringe.

Gently swirl the contents and let the vial stand until the cake has completely dissolved and any foam disperses.

Inspect the vial to ensure the solution contains no particulate matter and no cake or powder remains attached to the sides of the vial. If necessary, invert the vial to dissolve any remaining powder and swirl gently to prevent foaming. The total storage time should not exceed 24 hours at either room temperature or under refrigeration at 2°C to 8°C.

The reconstituted solution must be further diluted by rest of the normal saline. Invert the bag gently to mix. Do not shake the bag as this may cause foaming.

After reconstitution and dilution, Tezolid is to be administered via intravenous infusion using a total time of 1 hour.

Compatible infusion fluid: Tezolid is compatible with normal saline (0.9% Sodium Chloride Injection, USP).

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