inhibit protein synthesis Flashcards
site of action for aminoglycosides
interfere with formation of the initiation complex from the 30s side, are only ones that are bacterialcidal
site of action of the tetracyclines
block attachment of tRNA to the acceptor site from the 30s side
site of action for dalfopristin/quinpristin
block attach of tRNA from the 50s side
site of action of the chloramphenecol
inhibits activity peptidyltransferase from the 50s side, which inhibits formation of peptide bonds
site of action of macrolides and clindamycin
work from 50s side, and they inhibit translocation of peptidyl-tRNA from acceptor site to donor site; they stop the “slide”
aminoglycosides special need
needs a O2-dep. pump to enter cell
aminoglycosides targets
gram - rods, streptomycin is for TB and DOC for bubonic plauge and tularemia
aminoglycosides examples
gentamicin, tobramycin, amikacin, streptomycin, kanamycin, neomycin, netilmicin, paromomycin
major SE of aminoglycosides
nephrotox, ototox, NMJ blockade, contact dermatitis (topical neomycin)
Tetracyclines targets
broadspectrum and can work on atypical bacteria (chlamydia an mycoplasma), H. pylori, rickettsia, borrelia (lymes), brucella, vibrio, treponema
DOC for lymes and rickettsia
doxycycline
tetracycline drugs
doxycycline, minocycline, demeclocycline, methacycline, oxytetracycline, tetracycline, chlortetracycline
special SE of demeclocycline
also can block ADH receptors, can be used in SIADH
tetracyclines can also work as
chelters for 2+ ions
SE of tetracyclines
tooth enamel dysplasia, and possible low bone growth in kids, CI in kids and pregnancy, phototoxiciity (dont go in sun), balance tox
tetracyclines work in bone?
NO
tetracylcine resistance
pumps to push tetracyclines out of bacterial cell
chloramphenicaol name is special why?
very lipid solubility due to ring shape
targets of choramphenical
enourmous broad range, mainly used for sepsis and meningitis, has great distrubution in CSF and tissue
choramphenical SE
bone marrow suppression thus lmits use, causes gray baby syndome
macrolides targets
very broad, gram + cocci, atypical organisms (chlamydia, mycoplasma, ureaplasma), legionella (DOC), campylobacter jejuni, MAC (the bird TB thing), H. pylorei
macrolides name trick
thro, means macrolides
only macrolide to not inhibit cytocchrome P450
azithromycin
macrolides SE
stimulates motilin which is a good use for surgeons to help stim GI, reversible deafness,
telithromycin target
macrolide resistant Strept. Pneumonia, also drug is a ketolide not a macrolide
resistantce to macrolides
bacteria methylate their tRNA so that they cannot bind to it
clindamycin
not a macrolide but same mechanism
clindamycin targets
gram + (includes S. aureus), anaerobes like bacteriodies (aspiration pneumonia also), can go to bone for osteomyelitis (S. aureus)
Quinolones and bone infection
can be used for the odd infections in sickel cell and diabetics due to infections are gram -
SE of clindamycin
C. Diff induced pseudomembraneous colitis
resistance to clindamycin
same as macrolides
linezolid targets
VRSA, VRE, drug resistant pneumococci
linezolid SE
bone marrow suppression mainly platelets
dalfopristin/quinupristin targets
VRSA, VRE
group that dalfopristin/quinupristin are part of
streptogramins
Classes that stop formation of initiation complex
Linezolid(50s), aminoglycosides(30s)
Amunoglycosides are the only class in this section that are
Bacterialcidal due to causing mis reads in the mRNA
Classes that stop elongation of the translation
Tetracyclines (30s), dalfopristin/quinupriatin (50s)….A site
Class that stop formation of peptide bond
Chloramphenicol (50s), inhibit activity of peptidyltransferase
Class of drugs that inhibit translocation, stop the “slide”
Macrolides and clindamycin both work on 50s, inhibit translocation of peptidyl-tRNA from acceptor to donor site
How aminoglycosides enter cells
Accumulated intracellularly via O2 dependent uptake thus CANNOT work on anaerobes
Spectrum of aminoglycosides
Gram - rods mainly and gram + enterococcus
Drugs in aminoglycosides
Amikacin, gentamicin, kanamycin, neomycin, netilmicin, paromomycin, streptomycin, tobramycin
Streptomycin is used also for
TB and is DOC for bubonic plague and tularemia
Aminoglycosides SE
Nephrotoxicity, usually just 1 dose, ototoxocity, neuromuscular blockade(like botulism), contact dermatitis for neomycin
