Linezolid

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General

  • Type: Oxazolidinone antibiotic
  • Dosage Forms: PO/IV
  • Common Trade Names: Zyvox
  • Bacteriostatic, so prefer another agent in bacteremia, such as ceftaroline in vancomycin resistant MRSA

Adult Dosing

  • VRE infections:
    • 600 mg PO/IV Q12H x 14-28 days
  • Pneumonia, community-acquired:
    • 600 mg PO/IV Q12H x 5 days
  • Pneumonia, hospital-acquired or ventilator-associated:
    • 600 mg PO/IV Q12H x 5 days
  • Uncomplicated skin infections:
    • 400 mg PO Q12H x 10-14 days
  • Complicated skin infections:
    • 600 mg PO/IV Q12H x 10-14 days
  • Endocarditis
    • 600 mg PO/IV Q12H x 6 weeks

Pediatric Dosing

  • >12 years old: 600mg IV/PO q12h
  • <12 years: 10mg/kg IV/PO q8-12h

Special Populations

  • Pregnancy Rating: C
  • Lactation: Infant risk cannot be ruled out
  • Renal Dosing
    • Renal impairment: no adjustment
    • Hemodialysis: give dose after HD

Hepatic dosing: no adjustment for mild-moderate impairment (Child-Pugh Class A or B)

Contraindications

  • Allergy to class/drug
  • Use of MAOIs, concomitantly or within past 14 days

Adverse Reactions

Serious

  • Serotonin syndrome can be caused with concomitant use with an SSRI or MAOI
  • Myelosuppression can occur after two week of use
  • Peripheral and optic neuropathy
  • Lactic acidosis
  • Clostridium difficile diarrhea
  • Liver injury
  • Seizure

Common

  • GI upset
  • Headache
  • Fever

Pharmacology

  • Half-life: adults- 4.7-5.1h, pediatrics- 1.5-4.1
  • Metabolism:
  • Excretion:

Mechanism of Action

Antibiotic Sensitivities[1]

Group Organism Sensitivity
Gram Positive Strep. Group A, B, C, G S
Strep. Pneumoniae S
Viridans strep X1
Strep. anginosus gp X1
Enterococcus faecalis S
Enterococcus faecium S
MSSA S
MRSA S
CA-MRSA S
Staph. Epidermidis S
C. jeikeium S
L. monocytogenes S
Gram Negatives N. gonorrhoeae X1
N. meningitidis R
Moraxella catarrhalis I
H. influenzae I
E. coli R
Klebsiella sp R
E. coli/Klebsiella ESBL+ R
E coli/Klebsiella KPC+ R
Enterobacter sp, AmpC neg R
Enterobacter sp, AmpC pos R
Serratia sp X1
Serratia marcescens R
Salmonella sp R
Shigella sp R
Proteus mirabilis X1
Proteus vulgaris R
Providencia sp. X1
Morganella sp. X1
Citrobacter freundii X1
Citrobacter diversus X1
Citrobacter sp. X1
Aeromonas sp X1
Acinetobacter sp. R
Pseudomonas aeruginosa R
Burkholderia cepacia R
Stenotrophomonas maltophilia R
Yersinia enterocolitica R
Francisella tularensis R
Brucella sp. R
Legionella sp. X1
Pasteurella multocida X1
Haemophilus ducreyi X1
Vibrio vulnificus X1
Misc Chlamydophila sp X2
Mycoplasm pneumoniae R
Rickettsia sp X1
Mycobacterium avium R
Anaerobes Actinomyces X1
Bacteroides fragilis I
Prevotella melaninogenica X1
Clostridium difficile I
Clostridium (not difficile) X2
Fusobacterium necrophorum X1
Peptostreptococcus sp. S

Key

  • S susceptible/sensitive (usually)
  • I intermediate (variably susceptible/resistant)
  • R resistant (or not effective clinically)
  • S+ synergistic with cell wall antibiotics
  • U sensitive for UTI only (non systemic infection)
  • X1 no data
  • X2 active in vitro, but not used clinically
  • X3 active in vitro, but not clinically effective for Group A strep pharyngitis or infections due to E. faecalis
  • X4 active in vitro, but not clinically effective for strep pneumonia

See Also

Source

  1. Sanford Guide to Antimicrobial Therapy 2014