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
Mechanism of Action
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).
Oral: Well absorbed
Vdss: 67 to 80 L
Tedizolid phosphate is converted by phosphatases to tedizolid (active, parent drug); no other significant circulating metabolites.
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
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
There are no contraindications listed in the manufacturer's labeling.
Dosage and Administration
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.
Refer to adult dosing.
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).
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.
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).
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
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
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.
- 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).
Baseline complete blood count (CBC) with differential
Adverse events were observed in animal reproduction studies.
What is this drug used for?
- It is used to treat bacterial infections.
Frequently reported side effects of this drug
Other side effects of this drug: Talk with your doctor right away if you have any of these signs of:
- Clostridium difficile (C. diff)-associated diarrhea like abdominal pain or cramps, severe diarrhea or watery stools, or bloody stools.
- Signs of a significant reaction like 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. Talk to your doctor if you have questions.
Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about this medicine. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using this medicine.