tedizolid

tedizolid

(ted-eye-zoe-lid ),

Sivextro

(trade name)

Classification

Therapeutic: anti infectives
Pharmacologic: oxazolidinones
Pregnancy Category: C

Indications

Treatment of acute bacterial skin and skin structure infections (ABSSSI).

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 is resolution of infection.
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, rapidly converted by phosphatases to its active form.
Distribution: Penetrates interstitial fluid space of adipose and skeletal muscle resulting in similar levels to plasma.
Metabolism and Excretion: Eliminated via liver with inactive metabolites excreted in feces (82%) and urine (18%); <3% excreted unchanged in urine or feces.
Half-life: 12 hr.

Time/action profile (blood levels)

ROUTEONSETPEAKDURATION
POunknown2.5 hr24 hr
IVrapidend of infusion24 hr

Contraindications/Precautions

Contraindicated in: Uncontrolled HTN, pheochromocytoma, thyrotoxicosis, or concurrent use of sympathomimetic agents, vasopressors, or dopaminergic agents (↑ risk of hypertensive response); Concurrent or recent (<2 wk) use of monoamine oxidase (MAO) inhibitors (↑ risk of hypertensive response); Carcinoid syndrome or concurrent use of SSRIs, TCAs, triptans, meperidine, or buspirone (↑ risk of serotonin syndrome).
Use Cautiously in: Neutropenia (safety and efficacy not established if WBC <1000 cells/mm3) Obstetric: Use in pregnancy only in potential maternal benefit justifies potential risk to fetus; Lactation: Use cautiously if breastfeeding; Pediatric: Safe and effective use in children <18 yr has not been established.

Adverse Reactions/Side Effects

Central nervous system

  • dizziness
  • headache

Gastrointestinal

  • pseudomembranous colitis (life-threatening)
  • nausea
  • diarrhea
  • vomiting

Interactions

Drug-Drug interaction

↑ 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.

Route/Dosage

Oral Intravenous (Adults) 200 mg once daily for six days.

Availability

Tablets: 200 mg
Lyophilized powder for intravenous injection (requires reconstitution): 200 mg/vial

Nursing implications

Nursing 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.
  • Monitor bowel function. Diarrhea, abdominal cramping, fever, and bloody stools should be reported to health care professional promptly as a sign of pseudomembranous colitis. 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.

Potential Nursing Diagnoses

Risk for infection (Indications)
Diarrhea (Adverse Reactions)

Implementation

  • Dose adjustment is not necessary when switching from IV to oral dose.
  • Oral: May be administered with or without food.
  • Intravenous Administration
  • Intermittent Infusion: 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 slowing 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 hrs of reconstitution at room temperature or under refrigeration.
  • Rate: Infuse over 1 hr.
  • Y-Site Incompatibility: solutions containing calcium or magnesium, Lactated Ringer's, Hartmann's solution

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 hrs before next dose; if less than 8 hrs 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.
  • Advise female patient 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.

Evaluation/Desired Outcomes

  • Resolution of signs and symptoms of infection. Length of time for complete resolution depends on organism and site of infection.
References in periodicals archive ?
8) Currently, the therapeutic options approved by Food and Drug Administration (FDA) for the SSTIs by MRSA include daptomycin, linezolid, and the recently introduced, tedizolid.
Oral linezolid and tedizolid can also be used to treat CA-MRSA, but cost and the potential for drug interaction may prohibit their use.
Last year, FDA approved three new drugs: tedizolid phosphate (SIVEXTRO[R]), oritavancin (ORBACTIV[TM]), and dalbavancin
The seven new anti-infectives and their indications are dalbavancin (Dalvance) for treatment of skin infections caused by gram-positive organisms; efinaconazole (Jublia) for treatment of fungal infections of the toenails; miltefosine (Impavido) for treatment of visceral, cutaneous, and mucosal infections by various Leishmania species; oritavancin (Orbactiv) for skin infections caused by gram-positive bacteria; peramivir (Rapivab) for acute uncomplicated influenza; tavaborole (Kerydin) for treatment of fungal infections of the toenails; and tedizolid (Sivextro) for treatment of bacterial skin infections.
The seven new anti-infectives and their indications are dalbavancin (Dalvance) for treatment of skin infections caused by gram-positive organisms; efinaconazole (Jublia), for treatment of fungal infections of the toenails; miltefosine (Impavido) for treatment of visceral, cutaneous, and mucosal infections by various Leishmania species; oritavancin (Orbactiv) for skin infections caused by gram-positive bacteria; peramivir (Rapivab), for acute uncomplicated influenza; tavaborole (Kerydin) for treatment of fungal infections of the toenails; and tedizolid (Sivextro) for treatment of bacterial skin infections.
They were dalbavancin (Dalvance), approved in May; tedizolid (Sivextro), approved in June; and oritavancin (Orbactiv), approved in August.
Approval of Sivextro, known also as tedizolid, comes in the aftermath of regulatory clearance of the drug Dalvance for the same condition and manufactured by Durata Therapeutics Inc.
The acquisition will expand Cubista[euro](tm)s portfolio by adding tedizolid phosphate (TR-701), a late-stage antibiotic candidate developed for the potential treatment of certain Gram-positive infections such as methicillin-resistant Staphylococcus aureus (MRSA).
The trial, designated TR701-113, is testing tedizolid phosphate (formerly known as torezolid phosphate) administered initially as a once-daily intravenous (IV) infusion with the possibility to switch to once-daily oral therapy in ABSSSI patients.
Five of the emerging therapies slated to launch by 2021--Rib-X's delafloxacin, Furiex's JNJ-Q2, Trius/Bayer's tedizolid, Tetraphase's eravacycline and Nabriva/Forest's BC-3781--are being developed in both intravenous and oral formulations.
Tedizolid phosphate is a novel oxazolidinone antibiotic (20) with at least 4-times higher potency than linezolid against Gram-positive bacteria including MRSA, vancomycinresistant enterococci (VRE), linezolid-resistant cfr+ S.
The agency approved dalbavancin (Dalvance) in May and tedizolid (Sivextro) in June.