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Tedizolid (Monograph)

Brand name: Sivextro
Drug class: Oxazolidinones
Chemical name: (5R)-3-[3-Fluoro-4-[6-(2-methyl-2H-tetrazol-5-yl)-3-pyridinyl]phenyl]-5-(hydroxymethyl)-2-oxazolidinone
Molecular formula: C17H15FN6O3C17H16FN6O6P
CAS number: 856866-72-3


Antibacterial; oxazolidinone.

Uses for Tedizolid

Skin and Skin Structure Infections

Treatment of acute bacterial skin and skin structure infections (ABSSSI) caused by susceptible Staphylococcus aureus (including methicillin-resistant S. aureus [MRSA; also known as oxacillin-resistant S. aureus or ORSA] and methicillin-susceptible S. aureus), Streptococcus pyogenes (group A β-hemolytic streptococci, GAS), S. agalactiae (group B streptococci, GBS), S. anginosus group (includes S. anginosus, S. intermedius, and S. constellatus), or Enterococcus faecalis.

Tedizolid Dosage and Administration


Administer orally or by IV infusion.

Oral Administration

Administer orally without regard to meals.

IV Administration

For solution and drug compatibility information, see Compatibility under Stability.

Administer only by IV infusion; do not administer by rapid or direct IV injection. Not intended for IM, intra-arterial, intrathecal, intraperitoneal, or sub-Q administration.

Must be reconstituted and further diluted prior to IV infusion.

Do not add or infuse simultaneously with other IV substances, additives, or drugs.

If the same IV line is used for sequential infusion of several different drugs, flush IV line with 0.9% sodium chloride injection before and after infusion.

Vials contain no preservatives; for single use only.


Reconstitute vial containing 200 mg of tedizolid phosphate by adding 4 mL of sterile water for injection. Gently swirl vial; leave standing until lyophilized powder or cake dissolves and foam disperses. Avoid vigorous agitation or shaking to minimize foaming.

Inspect to ensure that no particulate matter, powder, or cake is attached to sides of vial. If needed, invert and gently swirl vial to dissolve any remaining powder. Reconstituted solution should appear clear and colorless to pale yellow.


Tilt reconstituted vial and withdraw 4 mL of reconstituted solution from bottom corner of vial using a syringe; avoid inverting vial while withdrawing solution. Slowly add the 4 mL of reconstituted solution to IV bag containing 250 mL of 0.9% sodium chloride injection. Gently invert bag to mix; do not shake.

Reconstituted and diluted IV solution should appear clear and colorless to pale yellow. Inspect visually for particulate matter prior to administration; discard if particles are observed.

Rate of Administration

Administer by IV infusion over 1 hour.


Available as tedizolid phosphate (inactive prodrug of tedizolid); dosage expressed in terms of tedizolid phosphate.


Skin and Skin Structure Infections
Oral or IV

200 mg once daily for 6 days.

Special Populations

Dosage adjustments not needed based on gender, race, body weight, or body mass index (BMI).

Hepatic Impairment

Dosage adjustments not needed in patients with hepatic impairment.

Renal Impairment

Dosage adjustments not needed in patients with renal impairment or undergoing hemodialysis.

Geriatric Patients

Dosage adjustments not needed based on age.

Cautions for Tedizolid



Patients with Neutropenia

Safety and efficacy in patients with neutropenia (i.e., neutrophil counts <1000 cells/mm3) not evaluated. In an animal model of infection, antibacterial activity of tedizolid was reduced in the absence of granulocytes.

Consider alternative therapies when treating acute bacterial skin and skin structure infections in patients with neutropenia.

Hematologic Effects

In phase 1 studies in healthy adults receiving tedizolid for 21 days, there was evidence of possible dose and duration effect on hematologic parameters after day 6. In phase 3 studies in patients with acute bacterial skin and skin structure infections, rate of clinically important hematologic changes generally were similar in those treated with tedizolid (6-day regimen) or linezolid (10-day regimen).


Peripheral and optic neuropathies reported in patients who received >28 days of treatment with another oxazolidinone anti-infective (not tedizolid). In phase 3 studies of tedizolid in patients with acute bacterial skin and skin structure infections, peripheral neuropathy and optic nerve disorders reported in similar frequencies in those treated with tedizolid or linezolid. Data not available for patients exposed to >6 days of tedizolid.

Superinfection/Clostridium difficile-associated Diarrhea and Colitis (CDAD)

Possible emergence and overgrowth of nonsusceptible bacteria or fungi. Monitor carefully; institute appropriate therapy if superinfection occurs.

Treatment with anti-infectives alters normal colon flora and may permit overgrowth of Clostridium difficile. C. difficile infection (CDI) and C. difficile-associated diarrhea and colitis (CDAD; also known as antibiotic-associated diarrhea and colitis or pseudomembranous colitis) reported with nearly all anti-infectives, including tedizolid, and may range in severity from mild diarrhea to fatal colitis. C. difficile produces toxins A and B which contribute to development of CDAD; hypertoxin-producing strains of C. difficile are associated with increased morbidity and mortality since they may be refractory to anti-infectives and colectomy may be required.

Consider CDAD if diarrhea develops during or after therapy and manage accordingly. Obtain careful medical history since CDAD may occur as late as ≥2 months after anti-infective therapy is discontinued.

If CDAD suspected or confirmed, discontinue anti-infectives not directed against C. difficile whenever possible. Initiate appropriate supportive therapy (e.g., fluid and electrolyte management, protein supplementation), anti-infective therapy directed against C. difficile (e.g., metronidazole, vancomycin), and surgical evaluation as clinically indicated.

Selection and Use of Anti-infectives

To reduce development of drug-resistant bacteria and maintain effectiveness of tedizolid and other antibacterials, use only for treatment of infections proven or strongly suspected to be caused by susceptible bacteria.

When selecting or modifying anti-infective therapy, use results of culture and in vitro susceptibility testing. In the absence of such data, consider local epidemiology and susceptibility patterns when selecting anti-infectives for empiric therapy.

Specific Populations


Category C.

Use during pregnancy only if potential benefits justify potential risks to fetus.

No adequate and well-controlled studies in pregnant women; animal studies (mice, rats, rabbits) revealed reduced fetal weight, costal cartilage anomalies, increased skeletal variations, and/or reduced maternal weight at dosages at least 4 times estimated human exposure.


Distributed into milk in rats; not known whether distributed into human milk.

Use with caution in nursing women.

Pediatric Use

Safety and efficacy not established in pediatric patients <18 years of age.

Geriatric Use

Insufficient numbers of patients ≥65 years of age in clinical studies to determine whether they respond differently than younger adults. Differences in pharmacokinetics not observed between elderly and younger patients; dosage adjustments not needed.

Hepatic Impairment

Moderate or severe hepatic impairment (Child-Pugh class B or C): No clinically important pharmacokinetic changes.

Renal Impairment

Severe renal impairment (Clcr <30 mL/minute per 1.73 m2): No clinically important pharmacokinetic changes; no clinically important removal during hemodialysis.

Common Adverse Effects

Nausea, headache, diarrhea, vomiting, dizziness, fatigue.

Drug Interactions

Tedizolid phosphate and tedizolid not substrates for and do not inhibit or induce CYP isoenzymes (CYP1A2, 2B6, 2D6, 2C8, 2C9, 2C19, 3A4) in vitro. Drug interactions involving oxidative metabolism and CYP isoenzymes unlikely.

No clinically important effect on drug uptake or drug efflux membrane transporters (e.g., organic anion transporter [OAT] 1, OAT3, organic anion transporting polypeptide [OATP] 1B1, OATP1B3, organic cation transporter [OCT] 1, OCT2, P-glycoprotein [P-gp], breast cancer resistance protein [BCRP]) in vitro.

Specific Drugs and Foods




Antibacterials (aztreonam, ceftazidime, ceftriaxone, ciprofloxacin, clindamycin, co-trimoxazole, daptomycin, gentamicin, imipenem, minocycline, rifampin, vancomycin)

No in vitro evidence of synergistic or antagonistic effects against gram-positive or gram-negative bacteria

Antifungals (amphotericin B, ketoconazole, terbinafine)

No in vitro evidence of synergistic or antagonistic effects against gram-positive bacteria

Food, tyramine-containing

Recommended dosage (200 mg of tedizolid phosphate daily) not expected to exert clinically important pressor response in patients receiving a tyramine-rich meal; palpitations reported in 72% of patient receiving tedizolid with tyramine compared with 46% of patients receiving tyramine with placebo

Restrictions of foods high in tyramine not needed

MAO inhibitors

Tedizolid is a weak reversible inhibitor of MAO in vitro; interactions with MAO inhibitors not evaluated in clinical studies


No substantial increase in maximum BP or heart rate when recommended dosage (200 mg of tedizolid phosphate daily) used with pseudoephedrine (60 mg); no effect on pharmacokinetics of either drug

Serotonergic drugs (SSRIs, tricyclic antidepressants, serotonin type 1 [5-hydroxytryptamine; 5-HT1] receptor agonists [“triptans”], meperidine, buspirone)

No evidence of serotonergic activity in mouse model using tedizolid dosages up to 30-fold higher than equivalent human dosages; interactions with serotonergic agents not evaluated in clinical studies

Tedizolid Pharmacokinetics



Tedizolid phosphate rapidly converted in vivo by phosphatases to the active moiety, tedizolid. Well absorbed following oral administration; absolute bioavailability approximately 91%.

Peak plasma concentrations of tedizolid achieved approximately 3 hours after oral administration in the fasted state or at end of a 1-hour IV infusion.


Systemic exposure similar whether given orally in the fasted state or with high-fat, high-calorie meal.

Plasma Concentrations

Steady-state concentrations achieved within approximately 3 days with oral or IV administration; accumulation is about 30% after ≥7 days of once-daily dosing.



Distributed into interstitial space fluid of adipose and skeletal muscle tissue at concentrations similar to plasma concentrations.

Distributed into epithelial lining fluid of pulmonary tissue in concentrations higher than plasma concentrations.

Distributed into milk in rats; not known whether distributed into human milk.

Plasma Protein Binding

70–90% bound to plasma proteins.



Tedizolid phosphate and tedizolid do not appear to be substrates of CYP enzymes.

A major metabolite (tedizolid sulfate) and several minor metabolites identified in feces and urine.

Elimination Route

Following single oral dose of tedizolid phosphate, excreted in feces (82%) and urine (18%), principally as the noncirculating sulfate conjugate; <3% eliminated in feces and urine as unchanged tedizolid.

Approximately 10% of a dose removed by hemodialysis.


12 hours.

Special Populations

No clinically important changes in peak plasma concentrations or AUC observed in adults with moderate or severe hepatic impairment (Child-Pugh class B or C), adults with severe renal impairment (Clcr <30 mL/minute per 1.73 m2), or geriatric adults ≥65 years of age.





20–25°C (may be exposed to 15–30°C).


Powder for IV Infusion

20–25°C (may be exposed to 15–30°C).

Store reconstituted or diluted solutions under refrigeration (i.e., 2–8°C) or at room temperature.

Total time from reconstitution to administration should not exceed 24 hours whether stored at 2–8°C or room temperature.



Solution Compatibility1


Sodium chloride 0.9%


Dextrose 5% in Ringer's injection

Dextrose 5% in Ringer's injection, lactated

Hartmann's solution

Ringer's injection

Ringer's injection, lactated

Actions and Spectrum

Advice to Patients


Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Tedizolid Phosphate


Dosage Forms


Brand Names



Tablets, film-coated

200 mg




For injection, for IV infusion only

200 mg



AHFS DI Essentials™. © Copyright 2024, Selected Revisions April 8, 2015. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

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