tedizolid

Inhibits bacterial protein synthesis at the level of the 23S ribosome of the 50S subunit.

Therapeutic effects:

Bacteriostatic action against enterococci, staphylococci, and streptococci, resulting in resolution of infection.

Spectrum:

Active against Staphylococcus aureus, including methicillin-resistant strains (MRSA), Streptococcus pyogens, Streptococcus agalactiae, Streptococcus anginosus group (including Streptococcus anginosus, Streptococcus intermedius, Streptococcus constellatus), and Enterococcus faecalis.

Pharmacokinetics ⬆ ⬇

Absorption: IV administration results in complete bioavailability; well absorbed (91%) following oral administration.

Distribution: Well distributed to tissues.

Metabolism/Excretion: Rapidly converted by phosphatases to its active form; primarily excreted in feces (82%) and urine (18%) (<3% excreted unchanged in urine or feces).

Half-Life: 12 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	2.5 hr	24 hr
IV	rapid	end of infusion	24 hr

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Uncontrolled hypertension, pheochromocytoma, thyrotoxicosis, or concurrent use of sympathomimetic agents, vasopressors, or dopaminergic agents (↑ risk of hypertensive response);
Carcinoid syndrome (↑ risk of serotonin syndrome);
OB: Pregnancy.

Use Cautiously in:

Neutropenia (safety and efficacy not established if WBC <1000 cells/mm³);
Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant.

Adv. Reactions/Side Effects ⬆ ⬇

GI: CLOSTRIDIOIDES DIFFICILE-ASSOCIATED DIARRHEA (CDAD), diarrhea, nausea, vomiting

Neuro: dizziness, headache

Misc: infusion reactions

Interactions ⬆ ⬇

Drug-drug:

↑risk of hypertensive response with MAO inhibitors, sympathomimetics (e.g., pseudoephedrine), vasopressors (e.g., epinephrine, norepinephrine), and dopaminergic agents (e.g., dopamine, dobutamine); concurrent or recent use should be avoided.
↑risk of serotonin syndrome with SSRIs, TCAs, triptans, meperidine, bupropion, or buspirone; avoid concurrent use.
May ↑ levels and risk of toxicity of methotrexate, topotecan, or rosuvastatin; discontinue these medications temporarily during tedizolid treatment.

Route/Dosage ⬆ ⬇

Tablets should NOT be used in children who weigh 35 kg.

PO IV (Adults and Children ≥35 kg): 200 mg once daily for 6 days.
IV (Children ≥26 wk gestational age and 20–<35 kg): 60 mg twice daily for 6 days.
IV (Children ≥26 wk gestational age and 14–<20 kg): 40 mg twice daily for 6 days.
IV (Children ≥26 wk gestational age and 10–<14 kg): 30 mg twice daily for 6 days.
IV (Children ≥26 wk gestational age and 6–<10 kg): 20 mg twice daily for 6 days.
IV (Children ≥26 wk gestational age and 3–<6 kg): 12 mg twice daily for 6 days.
IV (Children ≥26 wk gestational age and 2–<3 kg): 6 mg twice daily for 6 days.
IV (Children ≥26 wk gestational age and 1–<2 kg): 3 mg/kg twice daily for 6 days.

Availability ⬆ ⬇

Tablets: 200 mg
Lyophilized powder for injection: 200 mg/vial

Assessment ⬆ ⬇

Assess for signs/symptoms of infection (vital signs; appearance of wound, sputum, urine, and stool; WBC) at beginning of and during therapy.
Monitor for signs/symptoms of CDAD (diarrhea, abdominal cramping, fever, bloody stools). If CDAD occurs, discontinue tedizolid and treat as indicated. May begin up to several months following cessation of therapy.

Lab Test Considerations:

Obtain specimens for culture and sensitivity prior to initiating therapy. First dose may be given before receiving results.
- Consider alternate therapies in patients with neutrophil counts <1000 cells/mm³.
- May cause anemia.

Implementation ⬆ ⬇

Dose adjustment is not necessary when switching from IV to oral formulation.
PO: Administer without regard to food.

IV Administration:

Intermittent Infusion: Reconstitution: Reconstitute each vial with 4 mL of sterile water for injection. Gently swirl and let vial stand until completely dissolved; avoid shaking. Concentration: 50 mg/mL. Diluent: For patients weighing 35 kg: Slowly inject reconstituted solution into 250 mL bag of 0.9% NaCl or D5W. For patients weighing 35 kg: Prepare a stock solution by slowly injecting 1.6 mL of reconstituted solution into bag with 98.4 mL of 0.9% NaCl or D5W. Do not invert the vial during extraction. 0.8 mg/mL. Next, add appropriate volume of stock solution to obtain dose to empty infusion bag or syringe. It may be necessary to round to the nearest graduation mark for smaller volumes. Gently invert bag to mix; avoid shaking to minimize foaming. Solution is clear and colorless to pale yellow; do not administer solution that is discolored or contains particulates. Must be infused within 24 hr after reconstitution at room temperature or under refrigeration.
Rate: Infuse over 1 hr.
Y-Site Compatibility:
- amikacin
- amiodarone
- ampicillin/sulbactam
- anidulafungin
- azithromycin
- aztreonam
- bumetanide
- cefazolin
- cefepime
- cefiderocol
- ceftazidime
- ceftazidime/avibactam
- ceftolozane/tazobactam
- ceftriaxone
- cefuroxime
- ciprofloxacin
- cisatracurium
- daptomycin
- dexamethasone
- dexmedetomidine
- digoxin
- diltiazem
- dopamine
- epinephrine
- eptifibatide
- ertapenem
- esomeprazole
- famotidine
- fentanyl
- fosphenytoin
- furosemide
- heparin
- hydrocortisone
- hydromorphone
- imipenem/cilastatin
- insulin regular
- labetalol
- levofloxacin
- lidocaine
- lorazepam
- mannitol
- meperidine
- meropenem
- meropenem/vaborbactam
- mesna
- methylprednisolone
- metoclopramide
- metronidazole
- micafungin
- midazolam
- milrinone
- morphine
- naloxone
- nitroglycerin
- norepinephrine
- ondansetron
- pantoprazole
- penicillin G potassium
- phenylephrine
- piperacillin/tazobactam
- plazomicin
- potassium chloride
- potassium phosphate
- rocuronium
- sodium bicarbonate
- sodium phosphate
- tacrolimus
- tigecycline
- vancomycin
- vasopressin
- vecuronium
Y-Site Incompatibility:
- albumin (human)
- calcium chloride
- calcium gluconate
- caspofungin
- ceftaroline
- cyclosporine
- diphenhydramine
- dobutamine
- doxycycline
- esmolol
- gentamicin
- isavuconazonium
- magnesium sulfate
- nicardipine
- phenytoin
- tobramycin

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication. Advise patient to read Patient Information before starting therapy.
Advise patient to take full course of therapy, even if feeling better. Take missed doses as soon as remembered unless <8 hr before next dose; then wait until next scheduled dose. Do not double dose.
Advise patient to notify health care provider of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care provider before taking other medications.
Instruct patient to notify health care provider if changes in vision occur or immediately if diarrhea, abdominal cramping, fever, or bloody stools occur and not to treat with antidiarrheal without consulting health care provider.
Rep: May cause fetal harm. Advise women of reproductive potential to notify health care provider if pregnancy is planned or suspected or if breastfeeding.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇