48-49-Antibiotics II Flashcards
Which penicillins are “very narrow spectrum”
What is special about these?
Methicillin
Nafcillin
Oxacillin
These are beta-lactamase resistant!
Which penicillins are “narrow spectrum”
Penicillin G
Penicillin V
Which penicillins are “broad spectrum”
Ampicillin
Amoxicillin
Which penicillins are “extended spectrum”
Piperacillin
Ticarcillin
Azlocillin
What is the beta-lactamase inhibiting drug?
Clavulanic acid
What are the 1st generation cephalosporins?
Cefazolin
Cephalexin
What are the 2nd generation cephalosporins?
Cefotetan
Cefaclor
Cefuroxime (enters CNS)
What are the 3rd generation cephalosporins?
Ceftriaxone Cefotaxime Cefdinir Cefixime (most enter CNS)
What are the 4th generation cephalosporins?
Cefepime
beta lactamase resistant, enters CNS
Which cephalosporins are narrow versus broad spectrum?
Narrow are 1st generation getting broader until 4th generation is broad.
Monobactam compounds
name
Aztreonam
used to treat very serious infections like pneumonia, meningitis, and sepsis
beta-lactamase resistant
Carbapenem compounds (seize the carbapenems boys!)
"diem" carpe diem! doripenem imipenem (administered with cilastatin to prevent inactivation in the kidneys) ertapenem meropenem
Glycopeptide cell wall inhibitor
(name)
(mechanism)
(adverse)
Vancomycin (no CNS penetration)
binds to D-ala-D-ala pentapeptide and acts as an inhibitor.
Causes “red-man syndrome”
Polypeptide cell wall inhibitor
(name)
(mechanism)
Bacitracin
Blocks incorporation of amino acids into the cell wall
Phosphoenolpyruvate cell wall inhibitor
(name)
(mechanism)
(use)
Fosfomycin
Blocks synthesis of UDP-N-acetylmuramic acid
Used to treat uncomplicated UTI in women
Lipopeptide that targets cell membrane (name) (mechanism) (adverse) (resistance)
Daptomycin
Calcium dependent insertion into membrane. Causes depolarization of bacterial membrane that is bactericidal.
musculoskeletal problems
Mutation in mprF causing increased positive charge of membrane repels Daptomycin
Detergent targeting cell membrane
(name)
(mechanism)
Polymyxin B
binds to phospholipids in cell membrane and “punches holes” in it
What are the antibiotic actions at the 30s ribosome that disrupt protein synthesis?
Tetracyclines prevent binding of charged tRNA molecule
Aminoglycosides disrupt initiation of peptide formation, causes misreading of mRNA, breaks up the ribosomal structure
What are the antibiotic actions at the 50s ribosome that disrupt protein synthesis?
Chloramphenicol blocks peptide bond formation
Macrolides prevent translocation
linezolid binds to P site
clindamycin blocks initiation
Aminoglycosides
(name)
(mechanism)
(adverse)
all end in “mycin or acin”
bind to 30s subunit and disrupts initiation, causes misreading, and breaks up ribosome
Nephrotoxic and Ototoxic
Macrolides
(name)
(mechanism)
(adverse)
macROlides all end in "ROmycin" Erythromycin Clarithromycin Azithromycin bind 50s subunit and prevent elongation GI effects (motillin receptor agonist)
Tetracylines
(name)
(mechanism)
(adverse)
all end in “cycline”
Tetracycline, Minocycline, Doxycycline, Tigecycline
bind 30s subunit and prevents amino acid addition
Nutrient interaction (binds calcium), disrupts normal flora, photosensitivity
Clindamycin
subunit, adverse
binds 50s
GI effects
can cause C. difficile infection
Chloramphenicol
subunit, adverse
binds 50s
RBC suppression, Gray Baby Syndrome
Oxazolidinones
(name)
(mechanism)
(adverse)
Linezolid
binds P site of 50s inhibiting formation of ribosomal-fMet-tRNA complex
myelosuppression
Sulfonamides (name) (mechanism) (adverse) (resistance)
start with “sulfa”
block folate synthesis (and thus DNA synthesis) by binding PABA
skin (hypersensitive, photosensitive, steven-johnsons)
less sensitive drug target, increased PABA, scavenge folate
Trimethoprim drugs (name) (mechanism) (adverse) (resistance)
Trimethoprim and Pyrimethamine
inhibits bacterial dihydrofolate reductase impairing DNA synthesis
blood issues
change in drug uptake or reduced binding
Fluoroquinolones (name) (mechanism) (adverse) (resistance)
all end in “floxacin”
inhibit topoisomerase II and IV
GI, Drug-nutrient (bind divalent like calcium), Cardio (QT prolongation)
less sensitive target and efflux
Metronidazole
(mechanism)
(adverse)
(resistance)
damages DNA
GI and disulfiram-effect (avoid alcohol)
mutation in rdxA gene decreases drug activation