Protein Synthesis Inhibitors Flashcards
What are the aminoglycs?
Gentamicin, Neomycin, Amikacin (Amikin), Tobramycin, Streptomycin (GNATS)
MOA Aminoglycs?
Inhibit formation of initiation complex and cause misreading of mRNA, blocks translocation
What are aminoglycs specifically ineffective at covering? Why?
Anaerobes b/c require O2 for uptake
Aminoglyc coverage?
Severe G- rod
Which aminoglyc is used for boweel surgery?
Neomycin
Toxicity of Aminoglycs
Nephrotox, Neuromsk blockade, ototox, teratogen
Aminoglyc MOR
Bacterial transferase enzymes inactivate drug by acetylation, phosph, or adenylation
What are the tetracyclines?
Tetracycline (Sumycin), doxycycline , minocycline
MOA of Tetracyclines?
Bind to 30S and prevent attachment of aminoacyl-tRNA
What is a limit of tetracyclines?
Limited CNS penetration
A pt w/ which comorbidity should doxy be used? Why?
Fecally eliminated - can be used in renal failure,
Dietary restrictions when taking tetracyclines?
No milk or antacids or iron-containing preps b/c they decrease absorption in gut
Clinical use of tetracyclines?
B. burgdorferi, M. pneumoniae, Rickettsia, Chlamydia
Why are tetras so effective against Rickettsia and Chlamydia?
Good intracellular accumulation
Contraindications to tetracycline use?
Children, pregnant women (Teeth discoloration and teratogenicity)
MOR tetracyclines?
Decreased uptake/Increased efflux via plasmid-encoded pump
What are the Macrolides?
Azithromycin (Zithromax), Clarithromycin (Biaxin), erythromycin
MOA of Macrolides?
Inhibit protein synth by blocking translocation; bind to 23S rRNA of 50S ribosomal subunit
Macrolide coverage?
Atypical pneumonias (Mycoplasma, Chlamydia, Legionella), G+ cocci (Strep infections in patients allegic to penicillin)
Macrolide toxicity?
GI motility issues, Arrhythmia caused by prolonged QT, acute cholestatic hepatitis, eosinophilia, Rash
Cross-reactivity of Macrolides?
Increases serum conc of theophyllines, and oral anticoags
MOR of macrolides?
Methylation of 23S rRNA-binding site prevents binding of drug
To what class does Clindamycin (Cleocin) belong?
Clindamycin
MOA of Clindamycin
Blocks peptide transfer (translocation) at 50S ribosomal subunit