Opioids Flashcards
Fentanyl
full mu agonist
no active metabolite
Morphine
full mu agonist hydromorphone oxymorphone contraindicated in brain injury and emphysema Met by CYP3A4 to inactive metabolite
Buprenorphine
partial mu agonist
delta agonist
kappa antagonist
office based detox/withdrawal
Codeine
Full agonist moderate analgesic hydrocodone oxycodone met to morphine by CYP2D6 weak mu agonist less potential for drug dependence and respiratory depression antitussive
Levorphanol
full mu agonist
meperidine
Demerol
full mu agonist
moderate analgesic
causes mydriasis rather than miosis (avoid detection of abuse)
toxic metabolite, normeperidine can cause seizures
tramadol
full mu agonist
methadone
full mu agonist
longer half life and bioavailability compared to morphine
used for withdrawal and detox
Butorphanol
Kappa agonist
partial mu agonist
Nalbuphine
partial mu agonist
kappa agonist
Naltrexone
oral full antagonist
antidote for OD
long duration of action
eluxadoline
mixed agonist/antagonist
GI specific
Naloxegol
GI specific full antagonist
Mu Receptor Effects
analgesia (supra-spinal) euphoria CNS and respiratory depression Dependence Miosis Constipation
Kappa receptor effects
analgesia (spinal)
CNS and respiratory depression
Miosis
Dysphoria/disorientation