Dosing & Uses
Dosage Forms & Strengths
tablet
- 200mg
injection, lyophilized powder for reconstitution
- 200mg/vial
Skin & Skin Structure Infections
Indicated for acute bacterial skin and skin structure infections
200 mg PO/IV qDay for 6 days
Susceptible isolates of 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)
- Enterococcus faecalis
Dosage Modifications
Hepatic impairment: No dosage adjustment required
Renal impairment or hemodialysis: No dosage adjustment required
Dosage Forms & Strengths
tablet
- 200mg
injection, lyophilized powder for reconstitution
- 200mg/vial
Skin & Skin Structure Infections
Indicated for acute bacterial skin and skin structure infections in patients aged ≥12 years
<12 years: Safety and efficacy not established
12-18 years: 200 mg PO/IV qDay for 6 days
Susceptible isolates of 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)
- Enterococcus faecalis
Dosage Modifications
Hepatic impairment: No dosage adjustment required
Renal impairment or hemodialysis: No dosage adjustment required
Interactions
Interaction Checker
No Results

Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor

Contraindicated (1)
- cyproheptadine
tedizolid, cyproheptadine. Other (see comment). Contraindicated. Comment: MAO inhibitors may prolong and intensify the anticholinergic effects of antihistamines. Cyproheptadine may diminish the serotonergic effect of MAO inhibitors.
Serious - Use Alternative (58)
- almotriptan
tedizolid, almotriptan. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- amitriptyline
tedizolid, amitriptyline. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- amoxapine
tedizolid, amoxapine. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- bupropion
tedizolid, bupropion. Either increases levels of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- cholera vaccine
tedizolid, cholera vaccine. pharmacodynamic antagonism. Avoid or Use Alternate Drug. Avoid coadministration of cholera vaccine with systemic antibiotics since these agents may be active against the vaccine strain. Do not administer cholera vaccine to patients who have received oral or parenteral antibiotics within 14 days prior to vaccination.
- citalopram
tedizolid, citalopram. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- clomipramine
tedizolid, clomipramine. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- cyclobenzaprine
tedizolid, cyclobenzaprine. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- deferiprone
deferiprone, tedizolid. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid use of deferiprone with other drugs known to be associated with neutropenia or agranulocytosis; if an alternative is not possible, monitor absolute neutrophil count more frequently.
- desipramine
tedizolid, desipramine. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- desvenlafaxine
tedizolid, desvenlafaxine. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- dextroamphetamine
tedizolid, dextroamphetamine. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- dolasetron
tedizolid, dolasetron. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- doxepin
tedizolid, doxepin. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- duloxetine
tedizolid, duloxetine. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- eletriptan
tedizolid, eletriptan. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- escitalopram
tedizolid, escitalopram. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- fentanyl
tedizolid, fentanyl. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- fluoxetine
tedizolid, fluoxetine. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- fluvoxamine
fluvoxamine and tedizolid both increase serotonin levels. Avoid or Use Alternate Drug.
- frovatriptan
tedizolid, frovatriptan. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- granisetron
tedizolid, granisetron. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- imipramine
tedizolid, imipramine. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- isocarboxazid
tedizolid, isocarboxazid. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. Interaction with MAOIs were not studied in clinical trials; drugs within the same class(eg linezolid) are contraindicated with MAOIs.
- levomilnacipran
tedizolid, levomilnacipran. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- lisdexamfetamine
tedizolid, lisdexamfetamine. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- meperidine
tedizolid, meperidine. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- metformin
tedizolid will increase the level or effect of metformin by unspecified interaction mechanism. Avoid or Use Alternate Drug.
- methamphetamine
tedizolid, methamphetamine. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- methylene blue
tedizolid, methylene blue. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase levels of serotonin; increased risk of serotonin syndrome.
- microbiota oral
tedizolid decreases effects of microbiota oral by pharmacodynamic antagonism. Avoid or Use Alternate Drug. Microbiota oral contains bacterial spores. Antibacterial agents may decrease efficacy if coadministered. Complete antibiotic regimens 2-4 days before initiating microbiota oral. .
- mirtazapine
tedizolid, mirtazapine. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- naratriptan
tedizolid, naratriptan. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- nefazodone
tedizolid, nefazodone. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- nortriptyline
tedizolid, nortriptyline. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- ondansetron
tedizolid, ondansetron. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- palonosetron
tedizolid, palonosetron. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- paroxetine
tedizolid, paroxetine. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- phenelzine
tedizolid, phenelzine. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. Interaction with MAOIs were not studied in clinical trials; drugs within the same class(eg linezolid) are contraindicated with MAOIs.
- protriptyline
tedizolid, protriptyline. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- rasagiline
tedizolid, rasagiline. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. Interaction with MAOIs were not studied in clinical trials; drugs within the same class(eg linezolid) are contraindicated with MAOIs.
- rizatriptan
tedizolid, rizatriptan. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- ropeginterferon alfa 2b
ropeginterferon alfa 2b, tedizolid. Either increases toxicity of the other by Other (see comment). Avoid or Use Alternate Drug. Comment: Myelosuppressive agents can produce additive myelosuppression. Avoid use and monitor patients receiving the combination for effects of excessive myelosuppression.
- selegiline
tedizolid, selegiline. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. Interaction with MAOIs were not studied in clinical trials; drugs within the same class(eg linezolid) are contraindicated with MAOIs.
- selegiline transdermal
tedizolid, selegiline transdermal. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. Interaction with MAOIs were not studied in clinical trials; drugs within the same class(eg linezolid) are contraindicated with MAOIs.
- sertraline
tedizolid, sertraline. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- sumatriptan
tedizolid, sumatriptan. Either increases levels of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- sumatriptan intranasal
tedizolid, sumatriptan intranasal. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- tapentadol
tedizolid, tapentadol. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- tramadol
tedizolid, tramadol. Either increases levels of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- tranylcypromine
tedizolid, tranylcypromine. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. Interaction with MAOIs were not studied in clinical trials; drugs within the same class(eg linezolid) are contraindicated with MAOIs.
- trazodone
tedizolid, trazodone. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- trimipramine
tedizolid, trimipramine. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- tyramine
tedizolid, tyramine. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- venlafaxine
tedizolid, venlafaxine. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- vilazodone
tedizolid, vilazodone. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- vortioxetine
tedizolid, vortioxetine. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
- zolmitriptan
tedizolid, zolmitriptan. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. both increase serotonin levels; increased risk of serotonin syndrome.
Monitor Closely (1)
- levodopa inhaled
levodopa inhaled increases effects of tedizolid by dopaminergic effects. Use Caution/Monitor. Coadministration of selective MAO-B inhibitors with levodopa may be associated with orthostatic hypotension.
Minor (0)
Adverse Effects
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
Postmarketing Reports
Blood and Lymphatic System Disorders: Thrombocytopenia
Warnings
Contraindications
None
Cautions
Safety and efficacy in patients with neutropenia (<1000 cells/mm³) is uncertain; in animal models of infection, tedizolid antibacterial activity was reduced in animal models with neutropenia
In postmarketing experience, thrombocytopenia reported in patients receiving therapy; in one postmarketing report, patients who experienced thrombocytopenia were treated with tedizolid for a median duration of 26.5 days; duration of treatment beyond 6 days not approved
Prescribing antibiotics in the absence of a proven or strongly suspected bacterial infection is unlikely to provide benefit and increases the risk of the development of drug-resistant bacteria
Clostridioides difficile-associated diarrhea
- Clostridioides difficile-associated diarrhea (CDAD) reported, with severity ranging from mild diarrhea to fatal colitis; treatment with antibacterial agents can alter normal flora of the colon and may permit overgrowth of C. difficile
- C. difficile produces toxins A and B which contribute to development of CDAD; hypertoxin-producing strains of C. difficile cause increased morbidity and mortality, as these infections can be refractory to antibacterial therapy and may require colectomy
- CDAD must be considered in all patients who present with diarrhea following antibacterial drug use; careful medical history is necessary because CDAD has been reported to occur more than two months after the administration of antibacterial agents
- If CDAD is suspected or confirmed, antibacterial use not directed against C. difficile should be discontinued, if possible; appropriate measures such as fluid and electrolyte management, protein supplementation, antibacterial treatment of C. difficile, and surgical evaluation should be instituted as clinically indicated
Drug interactions overview
- Clinical trials of tedizolid to date have excluded patients receiving MAOIs, SSRIs, and SNRIs and TCAs; however, the risk of serotonin syndrome may be a class effect and appropriate caution should be taken to avoid coadministration of these agents with tedizolid
- Oral tedizolid inhibits breast cancer resistance protein (BCRP) in the intestine, which may increase plasma concentrations and/or adverse reactions of orally administered BCRP substrates; consider avoiding BCRP substrates during oral tedizolid treatment especially for BCRP substrates with a narrow therapeutic index (eg, methotrexate or topotecan); if coadministration cannot be avoided, monitor for adverse reactions related to the concomitantly administered BCRP substrates
Pregnancy & Lactation
Pregnancy
Based on animal reproduction studies, may cause fetal harm when administered to pregnant females; 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
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Tedizolid phosphate is the prodrug of tedizolid
Oxazolidione antibiotic; action is mediated by binding to the 50S subunit of the bacterial ribosome, resulting in inhibition of protein synthesis
Absorption
Bioavailability: 91% (PO and IV); no dosage adjustment is needed between IV and PO dose
Peak plasma concentration, steady-state: 2.2 mcg/mL (PO); 3 mcg/mL (IV)
Peak plasma time: 3 hr (PO fasting); at end of 1 hr infusion (IV)
AUC, steady-state: 8.4 mcg•hr/mL (PO); 5.9 mcg•hr/mL (IV)
Distribution
Protein bound: 70-90%
Vd: 67-80 L
Metabolism
There was no degradation of tedizolid in human liver microsomes, indicating tedizolid is unlikely to be a substrate for hepatic CYP450 enzymes
Elimination
Half-life: 12 hr
Excretion: 82% feces; 18% urine
Administration
Oral Administration
May take with or without food
IV Compatibilities
0.9% NaCl
IV Incompatibilities
Any solution containing divalent cations (eg, Ca2+, Mg2+), including lactated Ringer injection and Hartmann solution
IV Preparation
Reconstitute 200 mg vial with 4 mL sterile water for injection
Gently swirl the contents and let the vial stand until the lyophilized powder cake has completely dissolved and any foam disperses
Inspect vial for particulate matter
Reconstituted solution should be clear and colorless to pale-yellow
Tilt vial and insert a syringe with appropriately sized needle into the bottom corner of the vial and remove 4 mL of the reconstituted solution; do not invert the vial during extraction
Must be further diluted with 250 mL of 0.9% NaCl; slowly inject the 4 mL of reconstituted solution into the 250 mL bag, invert IV bag gently to mix
Do NOT shake IV bag (may cause foaming)
IV Administration
Infuse over 1 hr
Do NOT give as IV push or bolus
Not for intra-arterial, IM, IT, intraperitoneal, or SC administration
Missed Dose
- Take missed dose as soon as possible anytime up to 8 hr prior to the next scheduled dose
- If <8 hr remain before the next dose, wait until the next scheduled dose
Storage
Unreconstituted vial: Store at controlled room temperature (20-25°C [68-77°F]); excursions permitted to 15-30°C (59-86°F)
Reconstituted vial or diluted IV bag: Do not exceed 24 hr at either room temperature or refrigerated (2-8°C [36-46°F])
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