oxazolidinon and streptogramins (last of macrolide lecture)
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each of the black spaces below before clicking
on it to display the answer.
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| first commericially available oxazolidinone antibiotic | linezolid
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| 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
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| 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
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| 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
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| linezolid PK | almost 100% bioavailability; AUC almost identical after oral and iv. administration
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| linezolid SEs | Thrombocytopenia in use for longer than 2 weeks; is a MAOI and can't be used with tyramine containing foods or pseudoephedrine
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| group of natural cyclic peptides produced by bacteria, consists of two structurally unrelated molecules | streptogramins
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| strepogramins mechanism of action | bind to distinct sites on the 50S ribosomal subunit. Cooperate to inhibit protein synthesis
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| Synercid | Quinupristin/dalfopristin - streptogramin approved by FDA
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| Streptogramin spectrum (general) | Active against most gram positive bacteria and most respiratory pathogens including pneumococci, Mycoplasma pneumoniae, Legionella pneumophilia, Chlamydia pneumoniae
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| 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
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| Streptogramin metabolism (Quinupristin/dalfopristin - Synercid) | metabolized by liver and excreted in bile
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| Streptogramin SEs | infusion site reactions
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| streptogramin interactions | potent CYP3A4 inhibitor
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| 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
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