Tedizolid Phosphate

Indications

Tedizolid Phosphate is used for: Acute bacterial skin and skin structure infections (ABSSSI)

Adult Dose

Adult: 200 mg PO/IV once daily for 6 days Hepatic impairment: No dosage adjustment required

Child Dose

<18 years: Safety and efficacy not established

Renal Dose

Renal impairment or hemodialysis: No dosage adjustment required

Administration

Oral Administration May take with or without food IV Administration Administer as IV infusion over 1 hr Do NOT give as IV push or bolus Not for intra-arterial, IM, IT, intraperitoneal, or SC administration

Contra Indications

Contraindicated for patients with hypersensitivity to Tedizolid and ingredients

Precautions

Patients w/ neutropenia (neutrophil counts <1,000 cells/mm3). Discontinue if C. difficile-associated diarrhoea (CDAD) is suspected or confirmed. Patients w/ concomitant complicated skin & soft tissue infection & secondary bacteremia & in treatment of ABSSSI w/ severe sepsis or septic shock; diabetic foot infections, decubitus or ischaemic ulcers, bone or joint infections, severe burns, necrotizing infections or gangrene. May affect ability to drive or operate machinery. Pregnancy & lactation. Childn <18 yr. Elderly ≥75 yr.

Pregnancy-Lactation

Pregnancy There are no adequate and well-controlled studies in pregnant women Only use during pregnancy only if the potential benefit justifies the potential risk to the fetus Animal data In embryo-fetal studies in mice and rats, drug was shown to produce fetal developmental toxicities in mice and maternal toxicity and fetal developmental toxicities in rats Drug administered orally during organogenesis to pregnant animals was associated with reduced fetal weights and an increased incidence of costal cartilage anomalies in the absence of maternal toxicity in mice; and maternal toxicity, decreased fetal weights, and increased skeletal variations in rats at plasma exposures approximately 4- and 6-times respectively, the human plasma exposure at the maximum recommended human dose (MRHD) of 200 mg/day In female rats, drug administered during organogenesis through lactation, did not show evidence of fetal toxicity, developmental delays, or impaired reproduction in offspring at plasma exposures approximately equivalent to the human plasma exposure at the MRHD Lactation Tedizolid is excreted in the breast milk of rats; when drug is present in animal milk, it is likely that the drug will be present in human milk Unknown whether tedizolid is excreted in human milk Exercise caution when administering to a nursing woman; developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on breastfed child from drug or from underlying maternal condition

Interactions

Increased AUC & Cmax of rosuvastatin. Inhibition of BCRP at the intestinal level, increased plasma conc of BCRP substrates, & the potential for adverse reactions especially for BCRP substrates w/ narrow therapeutic index (eg, methotrexate or topotecan), or rosuvastatin.

Adverse Effects

Side effects of Tedizolid Phosphate : 2-10% Nausea (8%) Headache (6%) Diarrhea (4%) Hemoglobin <10.1 g/dL (3.1%) Vomiting (3%) Platelets <112 x 10³/mm³ (2.3%) Dizziness (2%) <2% Blood and lymphatic system disorders: Anemia Cardiovascular: Palpitations, tachycardia Eye disorders: Asthenopia, vision blurred, visual impairment, vitreous floaters General disorders and administration site conditions: Infusion-related reactions Immune system disorders: Drug hypersensitivity Infections and infestations: Clostridium difficile colitis, oral candidiasis, vulvovaginal mycotic infection Investigations: Hepatic transaminases increased, decreased WBCs Nervous system disorders: Hypoesthesia, paresthesia, seventh nerve paralysis Psychiatric disorders: Insomnia Skin and subcutaneous tissue disorders: Pruritus, urticaria, dermatitis Vascular disorders: Flushing, hypertension

Mechanism of Action

Inhibits protein synthesis by binding with 50S ribosomal sub-unit in bacteria