Opioids Flashcards
3 types of endogenous opioid peptides
enkephalins
beta-endorphins
dynorphins
opioids receptors
mu
delta
kappa
non-opioid like (NOP)
mu receptor endogenous ligand
beta-endorphin
enkephalin
delta receptor endogenous ligand
enkephalin
kappa receptor endogenous ligand
dynorphin
CYP2D6
potent - codeine to morphine
potent - tramadol to metabolite
hydrocodone and oxycodone variants
CYP3A4
fentanyl, buprenorphine, and methadone metabolism
CYP3B6
methadone and propofol
women have higher activity
mu receptor effect
analgesia euphoria sedation physical dependence respiratory depression miosis constipation urinary retention bradycardia pruitis skeletal muscle rigidity biliary spasm
kappa receptor effect
analgesia dysphoria sedation low abuse potential mitosis antishivering
delta receptor effects
analgesia physical dependence respiratory depression constipation urinary retention
opioid histamine release
codeine
morphine
meperidine
phenanthrene alkaloids
natural occurring: morphine, codeine, thebaine
semisynthetic: heroin, vicodan, dalaudid, oxycontin, oxymorphone, and antagonists (narcan etc.)
synthetic: levorphanol, butorphanol, nalbuphine, pentazocaine
piperidine derivatives
phenylpiperidines: meperidine, loperamide
anilidopiperidines: fentanyl, sufentanil, alfentanil, remifentanil
diphenylheptanes
methadone