Tetracyclines Flashcards
MOA
Inhibits protein synthesis by binding to the 30S subunit
Bacteriostatic–>Time-dependent
MOR
Tetracycline-specific efflux pumps
Ribosomal protection proteins
Enzymatic inactivation
Spectrum of activity (Tetracyclines)
Gram (+) aerobes–>monocycline and doxycycline are most active
- MSSA
Gram (-) aerobes
- H. influenza
Anaerobes
Atypical bacteria
- Legionella pneumonphila, chlamoydophila, pneumoniae, and psittaci
Spectrum of activity (Tetracycline analogs)
Gram (+) aerobes
- MSSA, MRSA
Gram (-) aerobes
- EEACKSS
- Tetracycline analogs are NOT active against Proteus or Pseudomonas aeruginosa
Anaerobes:
- ADA
- BDA
Atypical bacteria
Absorption
Tigecycline and eravacycline are only available IV; doxycycline and minocycline are available IV and PO. tetracycline is only available PO
Absorption of the oral tetracyclines and omadacycline is impaired by concurrent ingestion of ZICAM + bismuth
Distribution
Widely distributed into tissues and fluids–> prostatic and seminal fluids
Only small amounts of tetracyclines and tetracycline analogs diffuse into the CSF
Elimination
Tetracyclines are excreted mainly by non-renal routes, and do not require dose adjustments in renal insufficiency
Tetracycline analogs are mainly eliminated by biliary/fecal excretion
- No renal dose adjustments but dose adjustments of tigecycline and eravacycline are required in severe hepatic impairment
Clinical uses (Tetracyclines)
Mild to moderate outpatient community-acquired pneumonia (doxycycline)
Chlamydial infections including nongonococcal urethritis
Clinical uses (Tetracycline analogs)
NOT proteus spp. or Pseudomonas spp.
Adverse effects
GI–>N/V/D
Photosensitivity
Pregnancy Category D–> permanent discoloration teeth (black/gray)