Oxazolidinones Flashcards
Linezolid structure
incorporation of piperazine moiety into basic structure; has 3 rings: hexene with F, 5 membered with N and O inside ring, and 6 membered with N and O inside ring
Linezolid has increased activity due to
hydroxyacetyl group to heterocyclic nitrogen on 5 membered ring and fluorine
Linezolid MOA
acts as a protein synthesis inhibitor by binding to the V-domain of the 23S RNA component of the 50S ribosomal unit
Linezolid is bactericidal/bacteriostatic
bacteriostatic
Linezolid spectrum coverage
GRAM + ONLY
dark purple: streptococcus, s. pnuemoniae, viridans, MSSA, MRSA, e, faecalis, e. faecium, VRE
anaerobes: gram +
Misc: mycobacterium tuberculosis, other mycobacterium, nocardia, actinomycetes
Linezolid oral absorption
100% IV:PO
Linezolid 1/2 life
5 hours so long
Linezolid elimination
30-40% renal
Linezolid PK/PD parameters
T>MIC, AUC:MIC
Linezolid needs/doesnt need renal adjustment
does not
Linezolid CSF penetration
good!
Linezolid dosing
600mg IV or PO q12 hours
Linezolid adverse effects
hematologic toxicities thrombocytopenia (mostly with treatment > 2 weeks) anemia weekly CBC optic neuritis (prolonged use) peripheral neuropathy (prolonged use)
Linezolid drug interactions
does not interact with CYP450s
Linezolid is metabolized by
oxidation
Linezolid is a weak, non-selective _____
monoamine oxidase inhibitor
What is commonly seen with Linezolid?
serotonin syndrome due to excess serotonin in the CNS