Pharm 35: Bacterial Mass Murder Flashcards
Peptidoglycan aka
Murein
β lactam antibiotics inhibit _____ that mediate _____
β lactam antibiotics inhibit transpeptidase enzymes that mediate cross linking of sugar polymers
Fosfomycin MOA
Phophoenolpyruvate (PEP) analogue that inhibits bacterial (MurA)
Why doesn’t fosfomycin affect human cells
Structural differences in human and bacterial enzymes that act on PEP
Fosfomycin enters cells via ____
Glycerophosphate and G6P transporters
Fosfomycin is especially effective against
Gram negatives in urinary tract
Which GI bug is fosfomycin effective against
Enterococcus faecalis
Resistance to fosfomycin (common and E.coli)
Common: mutation in transporters (G6P and glycerophosphate)
E.Coli: Modification of enolpyruvate tranferase
Enolpyruvate transferase aka
MurA
Fosfomycin adverse effects
Mild and uncommon.
Headache, diarrhea, nausea
Oral fosfomycin drug interactions
Metoclopramide decreases GI absorbtion
Probenecid reduces renal clearance
Cycloserine MOA
Structural analogue of D-ALa inhibits alanine racemase and ligase
Racemase and ligase functions
Racemase: converts L-Ala to D-Ala
Ligase: joins D-Ala residues together
Cycloserine use
Second line for multidrug resistant TB
Cycloserine adverese effects
Neuro: seizures, psychosis, peripheral neuropathy
Cycloserine inhibits hepatic metabolism of _____
Phenytoin
Bacitracin MOA
Peptide antibiotic that intereferes with bactoprenol diphosphate dephosphorylation.
This makes bactoprenal lipid carrier infective and murein cannot be synthesized
Bacitracin unique amongst cell wall inhibitors because
It targets lipid and not peptide
Bacitracin requires ____ as cofactor
Divalent ions, Zn2+, Mg2+
Bacitracin use
Topical use for derm/eyes
Orally for gut decontamination prior to surgery (not absorbed)
Bacitracin systemic use
Not used systemically due to toxicity to marrow, kidney and neurons
Vancomycin activity
Bactericidal against gram-positive rods and gram positive cocci
Vancomycin, tela vancin, dalba vancin, orita vancin MOA
Lipoglycopeptides that interrupt peptidoglycan polymerization by binding to terminus of D-Ala-D-Ala murein monomer unit.
van drugs with lipid side chain
(and what does it do?)
Telavancin and oritavancin
Lipid chain anchors to bacterial membrane, enhancing drug binding
Dalbavancin has enhanced activity against
Coagulase negative staphylococci
Enteroccoci
Dalbavancin and oritavancine elimination
Long half life, once a week dosing
IV Vanco used for
MRSA pneumonia, sepsis, and endocarditis
IV telavancin used for
MRSA/Strep skin and pneumonia
Oral vanco for C.diff due to
Poor GI absorption
Vancomycin side effects
Red man syndrome: histamine release causing skin flushing and and rash
Nephrotoxicity, otoxic (esp with other meds)
Van drug without nephrotoxicity
Dalbavancin
Antibiotics that bind mess up coagulation tests results
Telavancin, oritavancin, daptomycin
van drug resistance comes from
Plasmide encoded VanH or VanA
These make D-Ala-D-lactate instead of D-Ala-D-Ala
β lactam mechanism
Inhibition of murein cross linking
β lactam ring inhibits cross linking how
Causes formation of dead-end complexes via suicide inhibition
Factor that affects β lactam bactericidalicity
Bactericidal only for actively dividing bacteria
4 β lactam families
Peniccillins
Cephalosporins
Monobactams
Carbepenems
Factor in β lactam activity against gram negs
Hydrophillics can make it through outer membrane, hydrophobics are ineffective
Hydrophilic β lactams
Ampicillin
Amoxiciillin
Piperacillin
Ticacillin
P A T A ( mete las patas en el agua)