Antibiotics: Inhibitors of Protein Synthesis Flashcards
Macrolides MOA
Bind the 50 s subunit irreversibly.
Macrolides spectrum
Gram positives. Bacteriostatic.
Macrolides elimination
fecal.
Macrolides resistance
efflux pumps and methylation of the drug binding site.
Macrolides toxicity
Diarrhea (erythro), QT pronlongation, hepatotoxicity and drug interactions (CYP 3A4)
Erythromycin
Macrolide. Oral/IV. Has immense GI effects and drug interactions.
Clarithromycin (biaxin)
Macrolide. Oral. Least GI disturbance but still has drug interactions.
Azithromycin (zithromax)
Macrolide. Oral/IV. Has some GI disturbances but has the least drug interactions.
Chlamydia DOC
Azithromycin or tetracycline
Ketolides: Telithromycin (ketek) MOA
Binds the 50S subunit with great affinity.
Telithromycin (ketek) spectrum
broad spectrum. Bacteriostatic. Good for erythromycin/penicillin resistant respiratory pathogens like pneumococci.
Telithromycin (ketek)
Ketolide. Oral.
Telithromycin (ketek) toxicity
Diarrhea, hepatotoxicity, drug interactions (CYP3A4).
Clindamycin (cleocin) MOA
Reversibly binds the 50S subunit.
Clindamycin spectrum
Aerobic gram positives and some anaerobic gram negative and positive organisms. Can be used for strep and staph infections (MRSA). Static or cidal depending on the concentration.
Osteomyelitis DOC
Clindamycin
Toxic Shock DOC
Clindamycin
Toxoplasma encephalitis DOC
Clindamycin
Clindamycin toxicity
pseudomembranous colitis (C-Diff). Hepatotoxicity. Crosses the placenta and breast milk.
Streptogramins
Dalfopristin;Quinupristin (synercid)
Synercid MOA
Blocks ribosome function. Dalfo in the early phase and Quin in the late phase. Bactericidal.
Synercid
Streptogramin. Dalfopristin;Quinupristin. IV.
Synercid toxicity
GI disturbance and drug interactions (CYP3A4)
Oxazolidinone
Linezolid (zyvox)
Linezolid MOA
prevents formation of a functional 70S ribosome.
Linezolid spectrum
Aerobic gram positive. Reserved as an alternate to prevent resistance.
Synercid Spectrum
Aerobic Gram positive. MSSA, MRSA, VRE.
Linezolid (zyvox)
Oxazolidinone. IV/Oral.
Linezolid toxicity
Reversible, nonselective inhibitor of monoamine oxidase (MAO) causing an increase in serotonin and NE.
Aminoglycosides MOA
Irreversibly inhibit protein synthesis by binding the 30S subunit. Bactericidal. Extremely polar so has to be actively transported into the baceteria using oxygen so limited to aerobes. Concentration dependent killing. With a long PAE.
Aminoglycosides spectrum
Aerobic gram negative enteric bacterial rods. Often combined with beta lactam antibiotics.
Streptomycin
Aminoglycoside. Second line TB drug. IV/IM.
Gentamicin
Aminoglycoside. IV/IM, topical.
Tobramycin
Aminoglycoside. IV/IM, topical.
Amikacin
Aminoglycoside. IV/IM.
Neomycin
Aminoglycoside. Oral, topical.
Enterococcus infection DOC
Aminoglycoside and a penicillin.
Pseudomonas aerginosa DOC
tobramycin with an antipsuedomonal penicillin
Tuleremia DOC
Gentamycin
Aminoglycoside toxicity
ototoxicity and nephrotoxicity.
Broad spectrum antibiotics (3)
Chloramphenicol (chloromycetin), tetracyclines and glycylcyclines.
Chloramphenicol (choloromycetin) MOA
Binds the 50s subunit and prevents attachment of tRNA. Bacteriostatic. Can have effects on mammalian mitochondria.
Chloramphenicol spectrum
reserved for life threatening infections. Broad spectrum. Best CNS penetration.
Chloramphenicol treats:
typhoid fever, meningitis (H. influ, N. meningitides (pen resistant), S. pneumoniae), rickettsia, brucellosis, rocky mountain spotted fever, meliodosis, bacterial conjunctivitis (topical).
Chloramphenicol toxicity
bone marrow suppression, fatal aplastic anemia, gray baby syndrome.
Chloramphenicol elimination
Conjugated with glucuronic acid in the liver.
Chloramphenicol Resistance
acetyl transferase can be produced which acetylates the chloramphenicol and inactivates it.
Tetracyclines MOA
inhibit protein synthesis by binding the 30S subunit to block tRNA binding. bacteriostatic.
Tetracycline spectrum
broad spectrum. Chelation with calcium and iron.
Tetracycline contraindications
pregnant women and kids younger than 8.
Tetracycline toxicity
Inhibits bone growth and teeth discoloration, photosensitivity, GI, superinfection, hepatotoxicity.
Aminoglycoside elimination
excreted rapidly by the kidneys.
Tetracycline
Oral.
doxycycline
tetracycline. oral.
minocycline
tetracyclne. oral.
Cholera DOC
Tetracycline
Mycoplasma Pneumonia
Tetracycline
Lyme disease (early)
Tetracycline
Vibrio
Tetracycline
Rocky mountain spotted fever
Tetracycline (doxycycline)
Glycylcycline MOA
Similar to tetracycline but active against tetracycline resistant organisms.
Glycylcycline treats
MRSA, MRSE (S. epidermis), PRSP (pen resistant strep. pneumoniae), VRE.