Antibiotics Flashcards
What are some 30S inhibitors?
Aminoglycosides
Tetracycline
Are
linezolid
macrolides
chloramphenicol
clindamycin
quinupristin/dalfopristin
30S or 50S inhibitors?
50S inhibitors
*NOTE* linezolid, tetracycline and chloramphenicol interfere with mitochondrial ribosomes - do have effect on us, ie, bone marrow suppression.
What part of translation do linezolid and aminoglycosides inhibit?
Initiation
What part of translation do aminoglycoside, tetracycline, macrolide, chloramphenicol, clyndamycin, quinupristin/dalfoprisitin inhibit?
Elongation
Where else does aminoglycoside inhibit translation?
termination
Are most ribosome inhibitors bacteriostatic or bacteriocidal?
how about things that affect the cell wall?
bacteriostatic.
those would be bactericidal
What do linezolid, tetracycline, and chloramphenicol interfere with?
mitochondrial ribosomes (bone marrow suppression)
What are the steps of prokaryote translation initiation?
1) Initiation factors associate with the 30S ribosomal subunit.
2) Formylmethionine initiator tRNA and mRNA bind to 30S subunit.
3) 50S ribosome then binds and you have the complete initiation complex.
Where does Linezolid bind?
P-site on the 50S subunit
where do aminoglycosides bind and what do they do?
bind to 30S ribosome and freeze initiation complex
Elongation:
Aminoacyl tRNA is inserted in the acceptor site. ____________ interfere here and prevent aminoacyl tRNA attachment to the acceptor site.
TETRACYCLINES
Elongation:
- The peptide bond is formed. ____________ inhibits peptide bond formation.
Chloramphenicol
Elongation:
- fmet tRNA is released from the P site. In prokaryotes, an exit site called the E site binds tRNA after it’s displaced from the P site
- Translocation. A dipeptide tRNA moves from the A to the P site and the ribosome moves one codon along the mRNA. _______________________________ inhibit translocation.
- Another amino acyl tRNA is put in the A site and elongation continues.
Macrolides, Streptotagmins, Clindamycin
what antibiotics should you not use with newborns?
Chloramphenicol (can’t glucuronidate)
Erythromycin (piloric stenosis)
Sulfonimides
What antibiotics can you not use in children?
Tetracyclines
Fluoroquinolones
What antibiotics should you not use during pregnancy?
Tetracycline
Aminoglocosides,
Clarithromycin
Fluoroquinolones
Chloramphenicol
Sulfonimides
What do you need to do with antibiotics for the elderly?
Adjust for reduced renal funtion:
the half life of
beta-lactams
aminoglycosdes
and fluoroquinolones
will be increased
Where do Aminoglycosides
Streptomycin
Neomycin
Amikacin
Gentamicin
Tobramycin
do in Protein Synthesis?
Are they bactericidal, bacteriostatic?
BacterioSTATIC…act on 30S ribosome
What do the Tetracyclines -
Doxycycline,
Minocycline
Demeclocycline
Tetracycline
do in protein synthesis?
Are these bacteriostatic or bactericidal?
inhibit - act on 30S Ribosome
BacterioSTATIC
Where do Macrolides -
erythromycin
azithromycin
clarithromycin
cindamycin
chloramphenicol act in Protein Synthesis?
Are they bacteriostatic or bactericidal?
act on 50S ribosome…
Bacteriostatic
Resistance mechanism that prevents drug from reaching its target in
Beta-lactams
Rifampin
Fluoroquinolones
Sulfonamides
Trimethoprim
Linezolid
Aminoglycosides
Erythromycin, clindamycin, quinupristin/dalfopristin
Tetracyclines
are due to:
alteration of target
Beta-lactams – altered penicillin binding proteins (MRSA)
Vancomycin- altered target
Rifampin - DNA dependent RNA polymerase
Fluoroquinolones - DNA topoisomerase II or IV
Sulfonamides - Dihydropteroate synthetase
Trimethoprim - Dihydrofolate reductase
Linezolid – altered ribosome
Aminoglycosides – altered ribosome (uncommon)
Erythromycin, clindamycin, quinupristin/dalfopristin – methyltransferase modified ribosome
Tetracyclines – production of proteins that interfere with ribosomal binding
Resistance mechanism that prevents drug from reaching its target in
Sulfonamindes
is due to:
Upregulation of target or its substrate