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Inhibitors of protein synthesis
Entire lecture overview
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12/10/2012

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Term
Continue to be mainstay against gram negative aerobes; bactericidal; cover staphylococci (but don't use it on staph infection by itself!); second line antitubercular agent
Definition
Aminoglycosides
Term
The most anti-pseudomonal of all the aminoglycosides
Definition
Tobramycin
Term
Binds to 16 S rRNA in 30 S ribosomal subunit (prevents docking of amino-tRNA)
Definition
Tetracyclines
Term
Most active tetracycline especially against S. aureus
Definition
Minocycline
Term
Antibiotics targeting bacterial ribosomes
Definition
Aminoglycosides, Tetracyclines, Macrolides, Clindamycin, Linezolid
Term
Clinically used aminoglycosides
Definition
Streptomycin, Neomycin, Kanamycin, Gentmycin, Tobramycin, Amikacin, Netilmicin
Term
Efficient uptake by active transport linked to oxidative phosphorylation; inhibited by anaerobic conditions and acidic pH
Definition
Aminoglycosides
Term
Aminoglycoside that is most susceptible to resistance
Definition
Gentamicin
Term
Aminoglycoside that is least susceptible to resistance
Definition
Amikacin
Term
Tetracycline spectrum of activity:
Definition
notably atypicals: Mycoplasma, Rickettsia, Chlamydia, Treponema pallidum; also anti-plasmodial activity (malaria)
Term
Clinically used tetracyclines
Definition
tetracycline, doxycycline, minocycline, demeclocycline
Term
Human use of Tetracycline is restricted to:
Definition
Acne vulgaris, Lyme disease, Typhus, spotted fever, chemosuppression of malaria
Term
Tetracycline has a potential role in:
Definition
Anthrax (Bacilla anthracis), Q fever (Coxiella burnetii)
Term
Tetracycline deposition in bone and teeth
Definition
discoloration, growth retardation, contraindicated in pregnancy and children
Term
Bind to 50 S subunit and inhibits translocation of aminoacyl-tRNA and A to P site
Definition
Macrolides
Term
Macrolides Spectrum of activity
Definition
gram positive aerobes, inactive against gram negative aerobes except Neisseria, Haemophilus, Bordetellla, Capylobacter, Legionella spp, Atypicals: Mycoplasma pneumonia, Rickettsia and Chlamydia spp.
Term
Clinically used macrolides
Definition
Erythromycin A, Clarithromycin, Azithromycin, Telithromycin
Term
Erythromycin: formulated as esters of hydrophobic acids to decrease solubility
Definition
Ethylsuccinate, Estolate, Stearate
Term
only clinical agent of Lincosamides
Definition
Clindamycin
Term
Lincosamides spectrum of activity
Definition
ananerobes and gram positive except enterococci; inactive against gram negative aerobes except H. influenza
Term
Clindamycin: topical formulation for acne vulgaris +/-
Definition
benzoyl peroxide
Term
erythromycin derivatives
Definition
Clarithromycin, Azithromycin, Telithromycin
Term
More active against gram positive and H. influenza; CYP3A4 inhibitors (EMA derivative)
Definition
Clarithromycin
Term
no significant CYP2A4 inhibition, long half-life (can be given once daily) (EMO derivative)
Definition
Azithromycin
Term
strongly associated with hepatotoxicity (EMO derivative)
Definition
Telithromycin ("ketolide")
Term
EMA esters
Definition
cholestasis, jaundice, fever, pruritus, rash, hepatomegaly
Term
Potent stimulator of GI motility
Definition
Erythromycin (toxicity)
Term
Useful in disseminated mycobacterium avium infection in AIDS patients
Definition
clarithromycin and azithromycin
Term
Clindamycin
Definition
Anaerobic infections: intra-abdominal, pelvic, periodontal, diabetic foot; first antibiotic to be associated w/ pseudomembranous colitis caused by C. difficile
Term
Inhibits peptidyl transferase in 50 S subunit
Definition
Linezolid
Term
Linezolid
Definition
Active only against gram positive species; important backup to vancomycin against VRE and MRSA, gram negative species intrinsically resistant due to active efflux
Term
Inhibits peptidyl transferase in 50 S subunit
Definition
Chloramphenicol
Term
Chloramphenicol broad spectrum
Definition
many atypical, bactericidal to some strains by unknown mechanism; no longer used in humans
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