20. Tetracyclins Flashcards
Tetracyclins from drug list
- chlortetracycline
- oxytetracycline
- tetracycline
- doxycycline
- minocycline
- tigecycline
Classification of tetracyclins:
Short-acting:
- tetracycline
- oxytetracycline
- chlortetracycline
Long-acting:
- doxycycline
- minocycline
Structure of tetracyclines:
4 rings -› TETRAcyclines
Tetracyclins. Mechanism of action
Inhibition of protein synthesis (30S)
Tetracyclins. Mode of action
bacteriostatic
at high concentrations can be bactericidal effect
Tetracyclins. Antimicrobial spectrum
- all tetracyclins similar. In theory spectrum is broad but in practice RESISTANCE! (old and cheap drug -› overuse)
- both aerobic and anaerobic
- Gram+ and gram– bacteria
Mycoplasma (haemofelis) - on the surface of RBCs (cats!)
Anaplasma phagocytophilum - inside of WBCs (dogs!)
Rickettsiae (small IC bacteria)
Chlamydophiliae - drugs of choice
Wolbachia (lives inside of the heart worm)
Borellia (Lyme disease)
Bordetella bronchiseptica,
gram– fastidious bacteria
Also against some protozoa: Plasmodium, Entamoeba histolytica, Babesia and Theileria spp.
Tetracyclins. Mechanisms of bacteria resistance
- Impaired uptake into bacteia (AB can’t penetrate)
- Active efflux (drug is pumped out from bacteria)
- Decomposition
- Altering binding site
Resistance is common in E. coli, Salmonella, Pasteurella multocida, Mannheimia haemolytica
Tetracyclins. Pharmakokinetics
long acting TTCs (doxycycline, minocycline) can cross BBB!
Indications and applications of tetracyclins
- bronchopneumonia (Bordetella bronchiseptica, gram– fastidious bacteria)
- foot diseases (mainly anaerobic bacteria)
- UTI (not really because there are better drugs, 1st choice - amoxiclav)
- metritis, mastitis
Specific conditions when tetracyclins are indicated
- Lyme disease (doxycycline!)
- chlamydophilosis
- feline mycoplasmosis
- infectious keratoconjunctivitis in cattle (Moraxella bovis)
- proliferative enteropathy in horses (Lawsonia intracellularis)
- heartworm
- nocardiosis, anaplasmosis
Tetracyclines. Side effects and toxicity
- GI disturbances
- Dysbacteriosis
- rapid IV: collapse
- tissue necrosis (if IM)
- yellow discolouration of the teeth
- hepatotoxicity
- nephrotoxicity
- photosensitivity