Antimicrobials Flashcards
Which 4 drug groups belong to the class of beta lactams?
Penicillins
Cephalosporins
Carbapenems
Monobactam
Are drugs that target the cell wall bactericidal or bacteriostatic?
Bactericidal
Name drug groups that target the cell wall?
Penicillins
Cephalosporins
Carbapenems
Monobactam
Glycopeptides
Fosfomycin
Bacitracin
How do beta-lactams work?
Beta lactams bind to PBP (protein binding penicillin), a transpeptidase
PBP inhibited from cross-linking the pentapeptides = instability
Activation of autolytic pathways to cleave crosslinking
Water leaks in = cell death
Which drug class would cause a rash in somebody with glandular fever?
Penicillins
Notably ampicillin and amoxicillin
Which beta-lactams are not sensitive to beta-lactamases?
Carbapenems
Monobactams
Co-amoxiclav
Tazocin
What are 4 mechanisms of resistance against beta-lactams
Hyperproduction of existing PBP (induce saturation of abx)
Mutation of PBP to produce a new PBP with a different active site
Production of beta-lactamases to inactivate beta-lactams
What are 2 beta-lactamase inhibitors?
Clavulanic avid
(added to amoxicillin = co-amoxiclav)
(added to ticarcillin = timentin)
Tazobactam
(added to piperacillin = tazocin)
What is a notable side effect of carbapenems?
Reduces seizure threshold
What are side effects of vancomycin?
Nephrotoxic
Ototoxic
Red man syndrome
Neutropenia
Hypotension
Steven-Johnson Syndrome
What other drugs should not be given in a severe penicillin allergy?
Cephalosporins
Carbapenems
How do glycopeptides destroy the cell wall?
Binds to 2-d-alanine in the pentapeptide
This blocks the formation of cross-linking between the amino acids and peptide bonds between the peptidoglycan chains
How does fosfomycin destroy the cell wall?
Irrevseribly inhibits an enzyme that is required in the first step of cell wall synthesis
How does bacitracin destroy the cell wall?
Prevents dephosphorylation of transport proteins which inhibits cell wall synthesis
How did MRSA come about?
Mutation in cell wall genes of bacteria = new PBP produced - different active site - penicillins no longer fit in the target
What are 2 enzymes beta-lactamases can produce?
ESBL
CPE
How do bacteria mediate resistance against glycopeptides?
Mediated by transposons = alterations in peptide chains = reduced affinity to glycopeptides
Which penicillin has activity against pseudomonas?
Piperacillin
(+Tazobactam = tazocin)
What is vancomycin against?
MRSA
C.diff
Gram + -> staph, strep, bacillus
How do polymyxins work and what is it active against?
Active against gram negative bacteria - outer membrane
Bind to LPS in the membrane - act as a detergent to disrupt the membrane = cellular permeability and demise
What antibiotics are used against the cell membrane and are they bactericidal or static?
Polymyxins - gram negative
Daptomycin - gram positive
Bactericidal
How does daptomycin disrupt the cell membrane and what is it active against?
Combines with calcium to form complex
Complex inserts in to cell membrane
Forms pore like structures
Allows potassium to leak out = cell death
Active against gram positive - inner membrane
Which drugs work against the cell membranes?
Polymyxins
Daptomycin