Skin and soft tissue infection (alternative agent):
Note: Reserve for patients with or at risk for methicillin-resistant S. aureus infection who cannot receive preferred agents (Spelman 2021).
Oral, IV: 200 mg once daily (Moran 2014; Prokocimer 2013). Total duration of therapy is ≥5 days; may extend up to 14 days depending on severity and clinical response (IDSA [Stevens 2014]; Spelman 2021).
Missed doses: Administer as soon as possible any time up to 8 hours prior to the next scheduled dose; if less than 8 hours remain before the next dose, wait until the next scheduled dose.
No dosage adjustment necessary.
No dosage adjustment necessary.
(For additional information see "Tedizolid: Pediatric drug information")
Skin and skin structure infections: Children ≥12 years and Adolescents: Oral, IV: 200 mg once daily for 6 days.
No dosage adjustment necessary; not removed by hemodialysis.
No dosage adjustment necessary.
Refer to adult dosing.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution Reconstituted, Intravenous, as phosphate [preservative free]:
Sivextro: 200 mg (1 ea)
Tablet, Oral, as phosphate:
Sivextro: 200 mg
No
Oral: Administer with or without food.
Intravenous: Administer as an IV infusion over 1 hour; do not administer as an IV push or bolus. Not for intra-arterial, IM, intrathecal, intraperitoneal, or subcutaneous administration. If the same IV line is to be used for sequential infusion of other drugs or solutions, the line should be flushed with NS before and after tedizolid infusion.
Oral: Administer with or without food.
Missed dose: Administer as soon as possible if ≥8 hours until next scheduled dose; otherwise, wait until next scheduled dose. All 6 doses should be administered even if a dose is missed.
Parenteral: IV: Administer as an IV infusion over 1 hour; do not administer as an IV push or bolus. Not for intra-arterial, IM, intrathecal, intraperitoneal, or subcutaneous administration. If the same IV line is to be used for sequential infusion of other drugs or solutions, the line should be flushed with NS before and after tedizolid infusion.
200 mg in 250 mL (concentration: 0.8 mg/mL) of NS only
Skin and soft tissue infections: Treatment of adults and pediatric patients ≥12 years of age with acute bacterial skin and soft tissue infections 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.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Reported adverse reactions are for adults unless otherwise specified.
1% to 10%:
Cardiovascular: Flushing (<2%), hypertension (<2%), palpitations (<2%), phlebitis (adolescents: 3%), tachycardia (<2%)
Dermatologic: Dermatitis (<2%), pruritus (<2%), urticaria (<2%)
Endocrine & metabolic: Increased gamma-glutamyl transferase (<2%)
Gastrointestinal: Clostridioides difficile colitis (<2%), diarrhea (4%), nausea (7%), oral candidiasis (<2%), vomiting (adolescents and adults: 1% to 3%)
Genitourinary: Vulvovaginal infection (fungal: <2%)
Hematologic & oncologic: Anemia (adolescents and adults: <2%), decreased platelet count (<112,000/mm3: Adolescents and adults: 1% to 2%), decreased white blood cell count (<2%)
Hepatic: Increased serum alanine aminotransferase (adolescents and adults: ≤3%), increased serum aspartate aminotransferase (adolescents and adults: ≤3%)
Hypersensitivity: Hypersensitivity reaction (<2%)
Local: Injection site reaction (≤4%)
Nervous system: Dizziness (2%), facial nerve paralysis (<2%), headache (5%), hypoesthesia (<2%), insomnia (<2%), paresthesia (<2%), peripheral neuropathy (1%)
Ophthalmic: Asthenopia (<2%), blurred vision (<2%), visual impairment (<2%), vitreous opacity (<2%)
Miscellaneous: Infusion related reaction (≤4%)
<1%:
Hematologic & oncologic: Decrease in absolute neutrophil count (<800/mm3)
Ophthalmic: Optic neuropathy
Postmarketing: Hematologic & oncologic: Thrombocytopenia
There are no contraindications listed in the manufacturer's labeling.
Concerns related to adverse effects:
• Superinfection: Prolonged use may result in fungal or bacterial superinfection, including C. difficile-associated diarrhea (CDAD) and pseudomembranous colitis; CDAD has been observed >2 months postantibiotic treatment.
Disease-related concerns:
• Neutropenia: Not recommended for use in patients with neutrophil counts <1000 cells/mm3. Alternative therapies should be considered when treating patients with neutropenia and acute bacterial skin and skin structure infections (ABSSI).
Inhibits BCRP/ABCG2
5-Aminosalicylic Acid Derivatives: May enhance the myelosuppressive effect of Myelosuppressive Agents. Risk C: Monitor therapy
Alpelisib: BCRP/ABCG2 Inhibitors may increase the serum concentration of Alpelisib. Management: Avoid coadministration of BCRP/ABCG2 inhibitors and alpelisib due to the potential for increased alpelisib concentrations and toxicities. If coadministration cannot be avoided, closely monitor for increased alpelisib adverse reactions. Risk D: Consider therapy modification
Amifampridine: Agents With Seizure Threshold Lowering Potential may enhance the neuroexcitatory and/or seizure-potentiating effect of Amifampridine. Risk C: Monitor therapy
BCG (Intravesical): Antibiotics may diminish the therapeutic effect of BCG (Intravesical). Risk X: Avoid combination
BCG (Intravesical): Myelosuppressive Agents may diminish the therapeutic effect of BCG (Intravesical). Risk X: Avoid combination
BCG Vaccine (Immunization): Antibiotics may diminish the therapeutic effect of BCG Vaccine (Immunization). Risk C: Monitor therapy
BCRP/ABCG2 Substrates BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors): Tedizolid may increase the serum concentration of BCRP/ABCG2 Substrates BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor therapy
Berotralstat: BCRP/ABCG2 Inhibitors may increase the serum concentration of Berotralstat. Management: Decrease the berotralstat dose to 110 mg daily when combined with BCRP inhibitors. Risk D: Consider therapy modification
BuPROPion: May enhance the neuroexcitatory and/or seizure-potentiating effect of Agents With Seizure Threshold Lowering Potential. Risk C: Monitor therapy
Chloramphenicol (Ophthalmic): May enhance the adverse/toxic effect of Myelosuppressive Agents. Risk C: Monitor therapy
Cholera Vaccine: Antibiotics may diminish the therapeutic effect of Cholera Vaccine. Management: Avoid cholera vaccine in patients receiving systemic antibiotics, and within 14 days following the use of oral or parenteral antibiotics. Risk X: Avoid combination
Cladribine: May enhance the myelosuppressive effect of Myelosuppressive Agents. Risk X: Avoid combination
CloZAPine: Myelosuppressive Agents may enhance the adverse/toxic effect of CloZAPine. Specifically, the risk for neutropenia may be increased. Risk C: Monitor therapy
Deferiprone: Myelosuppressive Agents may enhance the neutropenic effect of Deferiprone. Management: Avoid the concomitant use of deferiprone and myelosuppressive agents whenever possible. If this combination cannot be avoided, monitor the absolute neutrophil count more closely. Risk D: Consider therapy modification
Dipyrone: May enhance the adverse/toxic effect of Myelosuppressive Agents. Specifically, the risk for agranulocytosis and pancytopenia may be increased Risk X: Avoid combination
Fexinidazole: Myelosuppressive Agents may enhance the myelosuppressive effect of Fexinidazole. Risk X: Avoid combination
Immune Checkpoint Inhibitors: Antibiotics may diminish the therapeutic effect of Immune Checkpoint Inhibitors. Risk C: Monitor therapy
Iohexol: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Iohexol. Specifically, the risk for seizures may be increased. Management: Discontinue agents that may lower the seizure threshold 48 hours prior to intrathecal use of iohexol. Wait at least 24 hours after the procedure to resume such agents. In nonelective procedures, consider use of prophylactic antiseizure drugs. Risk D: Consider therapy modification
Iomeprol: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Iomeprol. Specifically, the risk for seizures may be increased. Management: Discontinue agents that may lower the seizure threshold 48 hours prior to intrathecal use of iomeprol. Wait at least 24 hours after the procedure to resume such agents. In nonelective procedures, consider use of prophylactic antiseizure drugs. Risk D: Consider therapy modification
Iopamidol: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Iopamidol. Specifically, the risk for seizures may be increased. Management: Discontinue agents that may lower the seizure threshold 48 hours prior to intrathecal use of iopamidol. Wait at least 24 hours after the procedure to resume such agents. In nonelective procedures, consider use of prophylactic antiseizure drugs. Risk D: Consider therapy modification
Lactobacillus and Estriol: Antibiotics may diminish the therapeutic effect of Lactobacillus and Estriol. Risk C: Monitor therapy
PAZOPanib: BCRP/ABCG2 Inhibitors may increase the serum concentration of PAZOPanib. Risk X: Avoid combination
Promazine: May enhance the myelosuppressive effect of Myelosuppressive Agents. Risk C: Monitor therapy
Ropeginterferon Alfa-2b: Myelosuppressive Agents may enhance the myelosuppressive effect of Ropeginterferon Alfa-2b. Management: Avoid coadministration of ropeginterferon alfa-2b and other myelosuppressive agents. If this combination cannot be avoided, monitor patients for excessive myelosuppressive effects. Risk D: Consider therapy modification
Sodium Picosulfate: Antibiotics may diminish the therapeutic effect of Sodium Picosulfate. Management: Consider using an alternative product for bowel cleansing prior to a colonoscopy in patients who have recently used or are concurrently using an antibiotic. Risk D: Consider therapy modification
Sympathomimetics: Tedizolid may enhance the hypertensive effect of Sympathomimetics. Tedizolid may enhance the tachycardic effect of Sympathomimetics. Risk C: Monitor therapy
Talazoparib: BCRP/ABCG2 Inhibitors may increase the serum concentration of Talazoparib. Risk C: Monitor therapy
Topotecan: BCRP/ABCG2 Inhibitors may increase the serum concentration of Topotecan. Risk X: Avoid combination
Typhoid Vaccine: Antibiotics may diminish the therapeutic effect of Typhoid Vaccine. Only the live attenuated Ty21a strain is affected. Management: Avoid use of live attenuated typhoid vaccine (Ty21a) in patients being treated with systemic antibacterial agents. Postpone vaccination until 3 days after cessation of antibiotics and avoid starting antibiotics within 3 days of last vaccine dose. Risk D: Consider therapy modification
Ubrogepant: BCRP/ABCG2 Inhibitors may increase the serum concentration of Ubrogepant. Management: Use an initial ubrogepant dose of 50 mg and second dose (at least 2 hours later if needed) of 50 mg when used with a BCRP inhibitor. Risk D: Consider therapy modification
Adverse events were observed in animal reproduction studies.
It is not known if tedizolid is present in breast milk.
According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and benefits of treatment to the mother.
Baseline complete blood count (CBC) with differential
After conversion from the prodrug, tedizolid phosphate, tedizolid binds to the 50S bacterial ribosomal subunit. This prevents the formation of a functional 70S initiation complex that is essential for the bacterial translation process and subsequently inhibits protein synthesis. Tedizolid is bacteriostatic against enterococci, staphylococci, and streptococci (Kisgen 2014).
Absorption: Oral: Well absorbed.
Distribution: Vdss:
Adolescents 12 to 17 years of age (mean weight: 55.3 kg): 54.2 ± 10.2 L (Bradley 2016).
Adults: 67 to 80 L.
Protein binding: 70% to 90%.
Metabolism: Tedizolid phosphate is converted by phosphatases to tedizolid (active, parent drug); no other significant circulating metabolites.
Bioavailability: Oral: ~91%.
Half-life elimination:
Adolescents 12 to 17 years of age: ~6.6 to 8.3 hours (Bradley 2016).
Adults: ~12 hours.
Time to peak: Oral: ~3 hours; IV: 1 to 1.5 hours.
Excretion: Feces (82%) and urine (18%), both as inactive sulfate conjugates. Less than 3% excreted in feces or urine as parent drug.
Anti-infective considerations:
Parameters associated with efficacy:
S. aureus: fAUC24/minimum inhibitory concentration; goal: ~20 to 50 (bacteriostasis); ~35 to 105 (1-log kill) (Lepak 2012; Louie 2011).
Expected drug exposure in patients with normal renal function:
Cmax (peak):
Single dose, 200 mg:
Adolescents 12 to 17 years of age: Oral: 2.23 ± 0.55 mg/L; IV: 3.85 ± 1.51 mg/L (Bradley 2016).
Adults, BMI <30 kg/m2: Oral: 2.3 mg/L; IV: 2.9 mg/L (Flanagan 2017).
Adults, BMI ≥30 kg/m2: Oral: 1.9 mg/L; IV: 2.5 mg/L (Flanagan 2017).
Multiple dose (steady state), 200 mg once daily:
Adults: Oral: 2.2 ± 0.6 mg/L; IV: 3 ± 0.7 mg/L.
AUC:
Single dose, 200 mg: AUC0 to ∞:
Adolescents 12 to 17 years of age: Oral: 25.2 ± 9.2 mg•hour/L; IV: 27.8 ± 7.3 mg•hour/L (Bradley 2016).
Adults, BMI <30 kg/m2: Oral: 28.5 mg•hour/L; IV: 28.7 mg•hour/L (Flanagan 2017).
Adults, BMI ≥30 kg/m2: Oral: 25.4 mg•hour/L; IV: 25.4 mg•hour/L (Flanagan 2017).
Multiple dose (steady state), 200 mg once daily: AUC24:
Adults: Oral: 25.6 ± 8.5 mg•hour/L; IV: 29.2 ± 6.2 mg•hour/L.
Postantibiotic effect: Staphylococcus spp. (including methicillin-resistant): 0.05 to 0.7 hours; Enterococcus spp. (including vancomycin-resistant): 0.1 to 1.3 hours (Locke 2014).
Solution (reconstituted) (Sivextro Intravenous)
200 mg (per each): $369.29
Tablets (Sivextro Oral)
200 mg (per each): $463.60
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