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MICABI - Exam 1

oxazolidinon and streptogramins (last of macrolide lecture)

first commericially available oxazolidinone antibiotic linezolid
linezolid mechanism of action binds 23S portion of 50S subunit close to the peptidyl transferase and chloramphenicol binding sites; stops 30S and 50S from binding together - prevents protein synthesis
linezolid spectrum gram-positive bacteria and some Gram-negative anaerobic species (no Gram-neg aerobes) Multi-drug resistant organisms such as MRSA, staphyl with reduced susceptibility to vancomycin, penicillin- and macrolide-resistant pneumococci and VRE fully susceptible
linezolid clinical use save it for the nasty stuff - usually reserved for the treatment of serious bacterial infections where older antibiotics have failed due to antibiotic resistance; skin infections or nosocomial pneumonia with methicillin/penicillin resistance
linezolid PK almost 100% bioavailability; AUC almost identical after oral and iv. administration
linezolid SEs Thrombocytopenia in use for longer than 2 weeks; is a MAOI and can't be used with tyramine containing foods or pseudoephedrine
group of natural cyclic peptides produced by bacteria, consists of two structurally unrelated molecules streptogramins
strepogramins mechanism of action bind to distinct sites on the 50S ribosomal subunit. Cooperate to inhibit protein synthesis
Synercid Quinupristin/dalfopristin - streptogramin approved by FDA
Streptogramin spectrum (general) Active against most gram positive bacteria and most respiratory pathogens including pneumococci, Mycoplasma pneumoniae, Legionella pneumophilia, Chlamydia pneumoniae
Streptogramin spectrum (special) 90% of Staph. aureus and coagulase negative staphylococci including MR strains; pencillin resistant pneumococci; Enterococcus faecium including strains which are resistant to ampicillin, gentamicin and vancomycin. Not active against E. faecalis
Streptogramin metabolism (Quinupristin/dalfopristin - Synercid) metabolized by liver and excreted in bile
Streptogramin SEs infusion site reactions
streptogramin interactions potent CYP3A4 inhibitor
Streptogramin clinical use bacteremia and life-threatening infection caused by vancomycin-resistant Enterococcus faecium (VREF); complicated skin structure infection caused by Staphylococcus aureus and Streptococcus pyogenes
Created by: Krafty