Oxazolidinones

Question 1

Linezolid

Answer 1

Developed in response to need for antibiotics against resistant gram+ like VRE, MRSA, VISA

Question 2

Linezolid MoA

Answer 2

Binds to 50S ribosomal subunit, causes inhibition of 10S initiation complex and INHIBITS PROTEIN SYNTHESIS

Bacterio static (cidal vs strep pneumo)

Question 3

Linezoilid MoR

Answer 3

Alterations in ribosomal binding sites (rare)

Cross-resistance with other protein synthesis inhibitors is unlikely

Question 4

Linezolid Pharmacology

Answer 4

Time-dependent bacteriostatic

PAE for Gram+s

100% bioavailable

CSF penetration (better than vanco for meningitis)

Eliminated renally and nonrenally NO ADJUSTMENT NEEDED

Question 5

Linezolid Clinical Uses

Answer 5

Very expensive

Usually reserved for serious/complicated infections by resistant gram+s

VRE bacteremia/endocarditis/meningitis/osteo (NOT UTIs) complicated SSTI, nosocomial pneumone from MRSA

Question 6

Linezolid Drug Interactions

Answer 6

With adrenergic or serotonergic agents -> enhancement of pressor response

Serotonin syndrome with SSRIs/MAOIs

Question 7

Linezolid AE

Answer 7

Nausea, vomiting, diarrhea, lactic acidosis, peripheral neuropathy, thrombocytopenia or anemia

Question 8

Tedizolid

Answer 8

Acute bacterial SSSIs (staph, strep, enterococcus)

More potent than linezolid

NO SSRI INTERACTIONS LIKE LINEZOLID

But can cause headache, N/V/D, dizziness, neuropathy (peripheral and optic)