Linezolid
Common Brand Names: Zyvox
Therapeutic Class: Oxazolidinone antibiotic
Common Injectable Dosage Forms:
Premixed bags: 200 mg (100 mL), 400 mg (200 mL), and 600 mg (300 mL)
Dosage Ranges:
Vancomycin-resistant enterococci (VRE) infections in infants and children <12 years old: 10 mg/kg every 8-12 hours for 14-28 days.
Nosocomial pneumonia, community-acquired pneumonia, and complicated skin infections:
Children <12 years old: 10 mg/kg every 8-12 hours for 10-14 days.
Adults: 400-600 mg every 12 hours for 10-14 days.
No adjustment necessary in elderly, renal, or hepatic impairment.
Administration and Stability: Administer IV over 30-120 minutes, and do not mix with other medications. Yellow color may intensify over time without affecting potency. Protect from light and keep infusion bags in overwrap until ready to use. pH 4.8
Pharmacology/Pharmacokinetics: Linezolid inhibits bacterial protein synthesis by binding to bacterial 23S ribosomal RNA of the 50S unit to prevent formation of functional 70S complex. This stops the bacterial translation process. Linezolid is bacteriostatic against enterococci and staphylococci. Absorption is rapid and extensive, with a volume of distribution around 40-50 L. Elimination half-life is 4.5 hours in adults, 1.5-3 hours in children.
Drug and Lab Interactions: Linezolid is a nonselective inhibitor of MAO. Serotonergic agents (TCAs, venlafaxine, trazodone, SSRIs, etc.) may cause serotonin syndrome when used together. Concomitant use with adrenergic agents (pseudoephedrine, vasopressor, or dopaminergic agents) may cause hypertension. Use with tramadol may cause seizures.
Contraindications/Precautions: Contraindicated in patients with hypersensitivity to linezolid. May cause myelosuppression therefore used with caution in patients with preexisting myelosuppression or in chronic infection. Use with caution in uncontrolled hypertension or hyperthyroidism and in patients with a history of seizures. Pregnancy Category C.
Monitoring Parameters: CBC, visual function
Adverse Effects: Possible adverse effects include headache, dizziness, rash, fever, insomnia, increased pancreatic enzymes, increased BUN, abnormal LFTs, and myelosuppression (especially when treated for more than 2 weeks).
Common Clinical Applications: Used in the treatment of vancomycin-resistant Enterococcus faecium infections (VRE), nosocomial pneumonia (including MRSA), complicated and uncomplicated skin structure infections (without osteomyelitis) and community-acquired pneumonia.
