Chapter 8 Structures Flashcards
(4 cards)
Vancomycin
glycopeptide, HCl salt (so be careful with mixing basic drugs)
uncompetitive enzyme inhibitor, binds substrate
big and polar
oral and IV (not IM)
intrinsically ineffective against G -
Use: G +, MRSA, PRSP, enterococci, Staph enterocolitis, and CDAD (however metronidazole is drug of choice for CDAD)
has halogenated a.a. so body thinks this is foreign = immunologic ADR
cyclic peptide portion = kills bacteria
sugar doesn’t contribute to activity
does not bind PBP, so no BLase
forms 5 H bonds with peptidoglycan complex (resistance = making PDG that only needs 4 H bonds)
Instead of D - Ala - D - Ala, we have D - Ala - D - Lac = resistance against vanco
Poor distribution, cleared renally, no metab (no liver), low PPB
ADR: red neck syndrome
teicoplanin
similar to methicillin
defines vancomycin resistance
Daptomycin
lipopeptide
antibiotic derived from strep roseosporus
Use; G + , listeria, corynebact, MRSA
CANNOT penetrate G -
lipid portion is important in MOA. It disrupts bacterial membrane. Doesn’t bind PDG so it has activity against VRE. Is not inactivated by BLases
It is subject to cyclization in aqueous acid and hydrolysis in aqueous base
IV
high PPB, renal clearance, NO CYP
ADR: GI, injection site pain, elevations in serum creatine phosphokinase (CPK), myopathy
DDI: statin, HMG-CoA
CANNOT USE IN PNEUMONIA: Dapto’s immunogenic character induce HSR Type I (eosinophilic pneumonia) AND dapto is bound by surfactants in the lung
Telavancin
lipoglycopeptide
Use: G + bugs, MRSA, PRSP, E. faecalis (not VRE)
Use in complicated SSTI, HAP, VAP
MOA: inhibits bacterial cell wall synthesis by interferring with cross linking of PDG. Binds to bacterial membrane, disrupting barrier fxn
IV, high PPB, eliminated renally as parent drug
ADR: nephrotoxicit, N/V, do not use in pregnancy, taste disturbance, infusion related red man syndrome, QTc prolongation
CYP 3A4 inhibitor
interferes with coagulation testing
