Ribosome Stuff Flashcards
Aminoglycosides
- Gentamicin
- Neomycin
- Amikacin
- Tobramycin
- Streptomycin
Aminoglycoside mechanism
Bactericidal.
Irreversible inhibition of initiation complex through binding of the 30S subunit. Can cause misreading of mRNA. Also block translocation.
Require O2 for uptake; therefore ineffective against anaerobes.
Aminoglycoside clinical use
Severe gram-negative rod infections. Synergistic with β-lactam antibiotics.
Neomycin for bowel surgery.
Aminoglycoside toxicity
- Nephrotoxicity
- Neuromuscular blockade
- Ototoxicity (especially when used with loop diuretics)
- Teratogen.
Aminoglycoside resistance
Bacterial transferase enzymes inactivate the drug by
- acetylation
- phosphorylation
- or adenylation
Tetracyclines
- Tetracycline
- Doxycycline
- Minocycline
Tetracycline mechanism
Bacteriostatic.
Bind to 30S and prevent attachment of aminoacyl-tRNA.
Limited CNS penetration. Doxycycline is fecally eliminated and can be used in patients with renal failure.
Do not take tetracyclines with
- milk (Ca2+),
- antacids (Ca2+ or Mg2+),
- or iron-containing preparations
because divalent cations inhibit drugs’ absorption in the gut.
Tetracycline clinical use
- Borrelia burgdorferi
- M. pneumoniae
Drugs’ ability to accumulate intracellularly makes them very effective against Rickettsia and Chlamydia. Also used to treat acne.
Tetracycline toxicity
- GI distress
- discoloration of teeth
- inhibition of bone growth in children
- photosensitivity
- Contraindicated in pregnancy.
Tetracycline resistance
↓ uptake or ↑ efflux out of bacterial cells by plasmid-encoded transport pumps.
Chloramphenicol mechanism
Blocks peptidyltransferase at 50S ribosomal subunit. Bacteriostatic.
Chloramphenicol clinical use
Meningitis
- Haemophilus influenzae
- Neisseria meningitidis
- Streptococcus pneumoniae
Rocky Mountain spotted fever
- Rickettsia rickettsii
Limited use owing to toxicities but often still used in developing countries because of low cost.
Chloramphenicol toxicity
- Anemia (dose dependent)
- aplastic anemia (dose independent)
- gray baby syndrome (in premature infants because they lack liver UDP-glucuronyl transferase).
Chloramphenicol mechanism of resistance
Plasmid-encoded acetyltransferase inactivates the drug.
Lincosamide
Clindamycin