antibiotics for osteomyelitis and skin infections med chem Flashcards
tetracycline drugs
tetracycline
monocycline
doxycycline
tigecycline
tetracycline MoA
interacts with 30S subunit of ribosome and sits in A site to prevent elongation (bacteriostatic)
tetracycline general pharmacophore
4 rings and dimethylamine pointing into the board
ways to inactivate tetracyclines
- make dimethylamine come out of the board
- dehydration of OH on north side
- breaking C ring through intramolecular reaction
avoid taking tetracyclines with what
multivitamins and milk because of chelation with ions
tetracyclines clinical use
- Gm+
- MRSA
- limited Gm-
tetracycline resistance
widespread in forms of
- efflux
- mutations in ribosome
- cell wall variation
side effects of tetracyclines
- light sensitivity
- severe kidney damage
- incorporation into bones and teeth
tigecycline unique structure feature
the claw on the tetracycline ring that prevents efflux based resistance
tigecycline clinical use
broad spectrum, typically saved for instances of resistance
hits basically everything but pseudomonas
clindamycin MoA
sits in 50S peptidyltransferase to inhibit the enzyme
clindamycin clinical use
- Gm+ (staph, strep)
- used w/ aminoglycosides for Gm-
- some anaerobes
- used if PCN allergy
- PO/IV
clindamycin side effects
- GI
- pseudomembranous colitis caused by C.difficile
linezolid MoA
prevents formation of 70S subunit complex by binding w/ 50S subunit
linezolid clinical use
- Gm+
- MRSA
- VRE
- IV/PO
linezolid resistance
still rare but can be seen as:
- point mutation of ribosome
- efflux pump in Gm-