tedizolid

Therapeutic Classification: anti-infectives

Pharmacologic Classification: oxazolidinones

Indications ⬆ ⬇

REMS

Treatment of acute bacterial skin and skin structure infections.

Action ⬆ ⬇

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;
Pedi: Children 12 yr (safety and effectiveness not established).

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 of methotrexate, topotecan, or rosuvastatin; discontinue these medications temporarily during tedizolid treatment.

Route/Dosage ⬆ ⬇

PO IV (Adults and Children ≥12 yr): 200 mg once daily for 6 days.

Availability ⬆ ⬇

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

Assessment ⬆ ⬇

Assess for infection (vital signs; appearance of wound, sputum, urine, and stool; WBC) at beginning of and during therapy.
Obtain specimens for culture and sensitivity prior to initiating therapy. First dose may be given before receiving results.
Monitor bowel function. Diarrhea, abdominal cramping, fever, and bloody stools should be reported to health care professional promptly as a sign of CDAD. May begin up to several mo following cessation of therapy.

Lab Test Considerations:

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: May be administered with or without 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.Diluent: Dilute further with 250 mL of 0.9% NaCl by slowly injecting reconstituted solution into 250 mL bag. Gently invert bag to mix; avoid shaking to minimize foaming. Solution is clear and colorless to pale yellow; do not administer solutions that are discolored or contain particulate material. Must be used within 24 hr of reconstitution at room temperature or under refrigeration.
Rate: Infuse over 1 hr.

Patient/Family Teaching ⬆ ⬇

Advise patients taking oral tedizolid to take as directed, for full course of therapy, even if feeling better. Take missed doses as soon as remembered up to 8 hr before next dose; if less than 8 hr before next dose, wait until next scheduled dose. Do not double dose.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
Instruct patient to notify health care professional if changes in vision occur or immediately if diarrhea, abdominal cramping, fever, or bloody stools occur and not to treat with antidiarrheals without consulting health care professionals.
Rep: May cause fetal harm. Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected, or if breastfeeding.
Advise patient to notify health care professional if no improvement is seen in a few days.

section name header

Pronunciation ⬇

Classifications ⬆ ⬇