Antimicrobials Flashcards
irreversibly inhibits transpeptidase by covalently binding to the serine residue of the active site of the penicillin binding proteins (PBPs) thus inhibiting cell wall synthesis
MOA of B-Lactam Antibiotics
Old penicillin
Penicillium notatum
clinical trials of penicillin
freeze-drying” or “lyophilization”
New penicillin
P. chrysogenum or P. rubens
Alternative to penicillin if allergic
Erythromycin
major product of acid degradation
Penilloic acid
Penicillin SAR in the R or side chain: addition of electron withdrawing group
acid stability
Penicillin SAR in the R or side chain:
addition of amino group
increases spectrum of activity
may be given with Probenecid to improve bioavailability
Penicillin G
“Narrow Spectrum” penicillins
Natural Penicillins
T/F. Sulfur atom in thiazolidine ring is nonessential
True
depot forms if pen G given IM but is rapidly excreted
benzathine penicillin, procaine penicillin
major product of enzymatic degradation of penicillin
by B-lactamase
Penicilloic acid:
phenoxymethyl penicillin
Penicillin V
A natural penicillin given orally and only for minor infections
Penicillin V