Protein Synthesis Inhibitors Flashcards
MOA of Aminoglycosides?
Blocks initiation of translation by blocking Metf tRNA to P site. Induces frameshift mutation.
Cidal
Resistance to aminoglycosides?
Conjugation inactivates (adenylylation, acetylation)
name five aminoglycosides?
Gentamycin Neomycin Amikacin Tobramycin Streptomycin
SE’s of Mean GNATS?
NOT nephrotoxic, neuromuscular blockade ototoxic teratogen dose dependent (hence given only once daily)
On what group of bacteria do aminoglycosides not work?
Anaerobes. oxygen dependent uptake of drug
MOA of tetracyclines?
Blocks binding of aminoacyl tRNA to the A site
MOR to tetracyclines?
activation of efflux pumps
Use of tatracyclines?
Chlamydia, Mycoplasma Ricketsia, Borrelia, Treponema H pylori Brucella Vibrio Acne
Tetracycline with high concentration in prostate and liver metabolism?
Doxycycline
drug stays in saliva tears, dental applications
Monocycline
Why are tetracycline not taken with food?
they chelate Ca and Fe reducing the absorption
Major side effects of tetracyclines?
enamel discoloration, phototoxicity, contraindicated in pregnancy
Tetracycline used to treat SIADH?
demeclocycline blocks ADH receptor
Drug that inhibits translocation of peptidyl tRNA (50s) and is not a macrolide?
Chloramphnicol
Metabolism of Chloramphenicol
P450
Two SEs of Chloramphenicol
bone marrow suppression
Grey baby syndrome
(neonatal lack of glucuronosyl transferase)
DOC for Legionella
Macrolides
Drug that inhibits translocation of peptidyl tRNA (50s) and DOC for community acquired pneumonia?
Macrolides
Erythromycin is what class?
macrolide “thro”
class of Azithromycin?
macrolide “thro”
Class of clarithromycin?
macrolide “thro”
metabolism of macrolides?
P450
MOR for macrolides?
methylation of RNA bases disrupts binding to 50s
biggest side effect of macrolides?
Increased GI motility.
causes people to “thro” up.
Class of Clindamycin
It’s own class. Not a macrolide although same mechanism.
Clindamycin is useful in what anatomical infection?
bone infections, osteomyelitis
SE of clindamycin
C diff pseudomembranous collitis
Drug used on VRSA, VRE?
linezolid or streptogramins
MOA of linezolid?
binds 50s and inhibits association of 30s
SE of linezolid?
bone marrow suppression
thrombocytopenia
Name both streptogramins?
Quinipristin
Dalfopristin
MOA of streptogramins?
binds 50s and prevents tRNA from binding acceptor site
