Inhibitors of Protein Synthesis
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27 terms
Terms | Definitions |
|---|---|
drugs affecting 30S | aminoglycosides and tetracylcines |
drugs affecting 50S | macrolides and some others |
amikacin, neomycin, gentamicin, streptomycin, tobramycin | aminoglycosides |
aminoglycosides MOA | IM, IV only!; bind to 30S and interfere with protein synthesis |
aminoglycosides MOR | adenylating, acetylation or phosphorylation of aminoglycosides |
aminoglycosides side effects | WORST! renal toxicity; vestibular ototoxicity; neuromuscular jxn - force Ca out and can cause problems (myasthenia gravis or hypocalcemia); **post-antibotic effects and [ ] dependent killers!!!** = decrease side effects by dosing high once and then decreasing doses |
amikacin, tobramycin | tx gram - infections |
neomycin | TOXIC, only used in cream |
tetracyclines | doxycycline, tetracycline, tigecycline |
tetracyclines | broad spectrums; over-used and now fxnlly narrow spectrum; all equally effective (doxy = longest 1/2 life!) |
tetracyclines MOA | bind to 30S; affects eukaryotic, but prokaryotic much better |
tetracylcines MOR | bacterial gain efflux pumps by conjugation |
tetracyclines indications | used for rocky mountain spotted fever and for spirochetal infections - lympe and relapsing fever |
tetracyclines adverse effects | discolorations of teeth and bone; phototoxicity; block absorption - don't take with food; decay over time - DO NOT use expired!! |
macrolides/ketolid/lincosamide | azithromycin** (not prescribed as an antibiotic, now for for GI stim), clarithromycin, erythromycin, telithromycin (ketolide), clindamycin (lincosamide) |
macrolides MOA | block fxn of 50S ribosomal subunit; block peptidyl transferase and translocation step; nice broad spectrum; LEAST side effects!! |
macrolides resistance | increased drug transport out of bacteria (efflux); mutations in the 50S that decrease binding of drug |
macrolides indications | respiratory infections |
macrolides adverse/contra | prolonged QT; are potent inhibitors of P450s!! |
chloramphenicol | SERIOUS side effects - life threatening; readily crosses BBB; tx for meningitis!! use in 3rd world countries |
chloramphenicol MOA | blocks 50S; blocks peptidyl transferase |
chloramphenicol toxicities | idiosyncratic aplastic anemia gray baby syndrome |
streptogramins | quinupristin/dalfopristin; inhibit protein synthesis; used for VRE; prescribed together; $$ |
oxazolidinones | linezolid |
linezolid MOA | bind to P site on 50S; for Gram + |
linezolid indications | VRE, nosocominal pneumonia, complicated skin infections |
linezolid contra | MOA inhibitors - be careful! |
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