Ribosomal Agents Flashcards
30s ribosome
spectinomycin, aminoglycan, tetracyclines
50s ribosome
Chloramphenicol, macrolides, lincosamides, strettogramins, linezolid
Spectinomycin MOA
- Inhibit initiation complex
- bacteriostatic
- bind to 30s subunit
- Parenteral
- Only indication = Gonorrhea
Aminoglycosides Examples
Streptomycin, gentamicin, tobramycin, Neomycin, Amikacin, Netilmicin
Aminoglycosides MOA & MOR
- Bind to 30s subunit
- Prevents initiation AND causes misreading of codon
- bactericidal
- O2 dependent –> needs high pH and aerobic conditions»better activity at high pH
- Resistance = group transferases (acetyl-,adenyl-, phospho-)
If there is resistance to gentamicin, what agent would you use?
Amikacin
Aminoglycosides adverse effects
-OTOTOXICITY
-NEPRHOTOXICITY (must monitor renal function)
(same toxicity as vancomycin)
- Neuromuscular blockade
- Skin reactions
Aminoglycosides indications
AEROBIC gram -
usually combine with beta-lactam
Tetracycline examples
Tetraycline, Doxycycline, MInocycline, Tigecycline, Demeclocycline
Tetracyclines MOA & MOR
- Bind to 30s subunit
- Inhibit binding of aminoacyl-tRNA
- Resistance: efflux protein pump
Tetracyclines indications
- Broad spectrum antibiotics ( gram - & gram +)
- Respiratory ifx (atypical): Mycoplasma, Legionella, Chlamydophila
- Bronchitis: H. flu, pneumococcus
- *Rickettsiae,
- *STDs!! (chlamydia, PID, ureaplasma, chancroid)
- *Lyme disease
- *Acne
- Drug resistent falciparum malaria (doxy)
Chloramphenicol MOA & MOR
- 50s subunit
- inhibit peptidyl transferase
- Resistance: acetyltransferase
Chloramphenicol adverse effects
- gray baby syndrome
- Bone marrow suppression (dose-dep)
- Aplastic anemia
- Decreased iron incorporation into Hgb
- Rare hypersensitivity
Chloramphenicol Indications
- Broad spectrum (but not for staph or pseudomonas)
- typhoid fever (if other unable to use other tx)
- MENINGITIS & Brain Abscess (only if other agents can’t be used)
- Bac conjunctivitis (topical)
- Oral meningitis tx when IV can’t be used
Macrolides Examples
Erythromycin, claritrhomycin, azithromycin, Telithromycin
Macrolides MOA & MOR
- Binds to 50s
- prevents translocation
- Resistance: Methylation (use Telitrhomycin in such cases)
Macrolide adverse effect
- GI problems
Macrolides are oral agents
Macrolide indications
- broad spectrum
- respiratory ifx
Lincosamides examples
lincomycin, clindamycin
Lincosamides MOA & MOR
- Bind to 50s subunit
- prevent translocation
- Resistance methylation
Lincosamides Indications
- anaerobic ifx
- aerobic gram +
Streptogramins MOA & MOR
-Binds to 50s
-Prevents translocation
-Bactericidal
Resistance = methylation
-Example = synercid
Streptogramins indications
PRSP, MRSA, VRSA, VRE tx
Linezolid MOA & MOR
- bactericidal
- Unique site binding to 50s (23s)
- Inhibits initiation AND translocation
- No cross resistance ( resistance only with mutation of 23s binding site)
Linezolid Indications
PRSP, MRSA,VRA, VRE tx
Enterococci tx
not active against G- or anaerobes
only topical or oral aminoglycoside antibiotic
Neomycin–b/c of high nephrotoxicity
all others parenteral
second line drug for tx of drug resistant TB
Streptomycin
Tetracylines adverse effects
absorption inhibited by milk, antacid, Ca+, Iron (metals)
- CONTRAINDICATED: renal failure and pregnant women & children
- teeth discoloration and concentration in bones
- GI effects
- Hepatotoxicity
- Doxy –> esophageal ulcerations, photosensitivity
- Tetra, Mino–> pre-renal azotemia
- Mino –> Vertigo
Erythromycin Indications
Treatment for:
- *Legionnaire’s disease
- *Mycoplasma pneumonia
- *Chlamydia ifx
- *Corynebacterium diphtheria
- *Bordatella pertussis
- *Campylobacter Enteritis
- Use w/ neomycin for surgical bowel prep
This drug exacerbates Myasthenia gravis
Telithromycin