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Tedizolid

Medically reviewed by Drugs.com. Last updated on Nov 3, 2019.

Pronunciation

(ted eye ZOE lid)

Index Terms

  • DA-7157
  • DA-7158
  • DA-7218
  • Tedizolid Phosphate
  • Torezolid
  • TR-700
  • TR-701 FA

Dosage Forms

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

Brand Names: U.S.

  • Sivextro

Pharmacologic Category

  • Antibiotic, Oxazolidinone

Pharmacology

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: 67 to 80 L

Metabolism

Tedizolid phosphate is converted by phosphatases to tedizolid (active, parent drug); no other significant circulating metabolites.

Excretion

Feces (82%) and urine (18%), both as inactive sulfate conjugates. Less than 3% excreted in feces or urine as parent drug.

Time to Peak

Oral: ~3 hours; IV: 1 to 1.5 hours

Half-Life Elimination

~12 hours

Protein Binding

70% to 90%

Use: Labeled Indications

Skin and skin structure infections: Treatment of adult patients with acute bacterial skin and skin structure infections caused by susceptible isolates of the following gram-positive microorganisms: Staphylococcus aureus (including methicillin-resistant [MRSA] and methicillin-susceptible [MSSA] isolates), Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus anginosus group (including Streptococcus anginosus, Streptococcus intermedius, and Streptococcus constellatus), and Enterococcus faecalis

Contraindications

There are no contraindications listed in the manufacturer's labeling.

Dosing: Adult

Skin and skin structure infections: Oral, IV: 200 mg once daily for 6 days.

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.

Dosing: Geriatric

Refer to adult dosing.

Reconstitution

Reconstitute with 4 mL SWFI. Do NOT shake. Gently swirl the contents and let the vial stand until the cake has completely dissolved and any foam disperses. If necessary, invert the vial to dissolve any remaining powder and swirl gently to prevent foaming. The reconstituted solution is clear and colorless to pale-yellow in color; Tilt the upright vial and insert a syringe into the bottom corner of the vial and remove 4 mL of the reconstituted solution. Do NOT invert the vial during extraction. The reconstituted solution must be further diluted in 250 mL of NS only. Invert the bag gently to mix. Do not shake the bag (may cause foaming).

Administration

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.

Storage

Store at 20°C to 25°C (68°F to 77°F); excursions are permitted between 15°C and 30°C (59°F and 86°F) The total storage time of the reconstituted solution should not exceed 24 hours at either room temperature or under refrigeration at 2°C to 8°C (36°F to 46°F).

Drug Interactions

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. Consider therapy modification

Amifampridine: Agents With Seizure Threshold Lowering Potential may enhance the neuroexcitatory and/or seizure-potentiating effect of Amifampridine. Monitor therapy

BCG (Intravesical): Antibiotics may diminish the therapeutic effect of BCG (Intravesical). Avoid combination

BCG (Intravesical): Myelosuppressive Agents may diminish the therapeutic effect of BCG (Intravesical). Avoid combination

BCG Vaccine (Immunization): Antibiotics may diminish the therapeutic effect of BCG Vaccine (Immunization). Monitor therapy

BCRP/ABCG2 Substrates: Tedizolid may increase the serum concentration of BCRP/ABCG2 Substrates. Monitor therapy

BuPROPion: May enhance the neuroexcitatory and/or seizure-potentiating effect of Agents With Seizure Threshold Lowering Potential. Monitor therapy

Chloramphenicol (Ophthalmic): May enhance the adverse/toxic effect of Myelosuppressive Agents. 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. Avoid combination

Cladribine: May enhance the myelosuppressive effect of Myelosuppressive Agents. Avoid combination

CloZAPine: Myelosuppressive Agents may enhance the adverse/toxic effect of CloZAPine. Specifically, the risk for neutropenia may be increased. 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. Consider therapy modification

Dipyrone: May enhance the adverse/toxic effect of Myelosuppressive Agents. Specifically, the risk for agranulocytosis and pancytopenia may be increased Avoid combination

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 anticonvulsants. 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 anticonvulsants. 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 anticonvulsants. Consider therapy modification

Lactobacillus and Estriol: Antibiotics may diminish the therapeutic effect of Lactobacillus and Estriol. Monitor therapy

Mesalamine: May enhance the myelosuppressive effect of Myelosuppressive Agents. Monitor therapy

PAZOPanib: BCRP/ABCG2 Inhibitors may increase the serum concentration of PAZOPanib. Avoid combination

Promazine: May enhance the myelosuppressive effect of Myelosuppressive Agents. Monitor therapy

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. Consider therapy modification

Sympathomimetics: Tedizolid may enhance the hypertensive effect of Sympathomimetics. Tedizolid may enhance the tachycardic effect of Sympathomimetics. Monitor therapy

Talazoparib: BCRP/ABCG2 Inhibitors may increase the serum concentration of Talazoparib. Monitor therapy

Topotecan: BCRP/ABCG2 Inhibitors may increase the serum concentration of Topotecan. Avoid combination

Typhoid Vaccine: Antibiotics may diminish the therapeutic effect of Typhoid Vaccine. Only the live attenuated Ty21a strain is affected. Management: Vaccination with live attenuated typhoid vaccine (Ty21a) should be avoided in patients being treated with systemic antibacterial agents. Use of this vaccine should be postponed until at least 3 days after cessation of antibacterial agents. 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 (if needed) of 50 mg when used with a BCRP inhibitor. Consider therapy modification

Adverse Reactions

1% to 10%:

Cardiovascular: Flushing (<2%), hypertension (<2%), palpitations (<2%), tachycardia (<2%)

Central nervous system: Headache (5%), dizziness (2%), facial nerve paralysis (<2%), hypoesthesia (<2%), insomnia (<2%), paresthesia (<2%), peripheral neuropathy (1%)

Dermatologic: Dermatitis (<2%), pruritus (<2%), urticaria (<2%)

Endocrine & metabolic: Increased gamma-glutamyl transferase (<2%)

Gastrointestinal: Nausea (7%), diarrhea (4%), vomiting (3%), Clostridioides difficile colitis (<2%), oral candidiasis (<2%)

Hematologic & oncologic: Decreased hemoglobin (males <10.1 g/dL; females <9 g/dL: 3%), decreased platelet count (<112,000/mm3: 2%), anemia (<2%), decreased white blood cell count (<2%)

Hepatic: Increased serum alanine aminotransferase (<2%), increased serum aspartate transaminase (<2%), increased serum transaminases (<2%)

Hypersensitivity: Hypersensitivity (<2%)

Infection: Fungal infection (vulvovaginal: <2%)

Local: Injection site reaction (≤4%)

Ophthalmic: Asthenopia (<2%), blurred vision (<2%), visual impairment (<2%), vitreous opacity (<2%)

Miscellaneous: Infusion related reaction (≤4%)

<1%, postmarketing, and/or case reports: Clostridioides difficile associated diarrhea, decrease in absolute neutrophil count (<800/mm3), optic neuropathy

Warnings/Precautions

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).

Monitoring Parameters

Baseline complete blood count (CBC) with differential

Pregnancy Considerations

Adverse events were observed in animal reproduction studies.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience diarrhea, dizziness, headache, vomiting, or nausea. Have patient report immediately to prescriber signs of Clostridium difficile (C. diff)-associated diarrhea (abdominal pain or cramps, severe diarrhea or watery stools, or bloody stools) (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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