Specific opioid agents Flashcards
Agonists with high oral bioavailability
Levorphanol
Codeine
Methadone
Agonists with low/no oral bioavailability
Fentanyl
Morphine
Morphine
Mu agonist (kappa and delta at higher)
Hydromorphone
Mu agonist (kappa and delta at higher)
Oxymorphone
Mu agonist (kappa and delta at higher)
Heroin
Full mu agonist
Codeine
Mu agonist
Oxycodone
Mu agonist
Hydrocodone
Mu agonist
Meperdine
Mu agonist
DOESNT CROSS PLACENTA!
Fentanyl
Mu agonist
VERY POTENT
Fast onset, SHORT duration
Sufentanil
Mu agonist
VERY potent
FAST onset, SHORT duration
Remifentanyl
Mu agonist
VERY potent
FAST onset, SHORT duration
Levorphanol
Mu agonist (synthetic) Also antagonizes NMDA receptors
Methadone
WEAK mu agonist (used for addiction to reduce cravings and withdrawal symptoms)
Naloxone
Mu, Kappa, and Delta ANTAGONIST
SHORT acting
Naltrexone
Mu, Kappa, and Delta ANTAGONIST
LONG acting
Nalmefene
SELECTIVE mu antagonist
Pentazocine
Partial mu agonist, K agonist
Low doses good
High doses bad, start getting dysphoria/psychomimetic activity from k agonism
Which antagonists are injectable only?
All of them!
Which antagonists are available orally?
None of them!
Nalbuphine
Full K agonist, mu antagonist
More effective in women
Butorphanol
Partial mu agonist, full K agonist
Buprenorphine
Partial mu agonist, full K antagonist
In suboxone!
Tramadol
Weak mu agonist + SERT/NET inhibition
Tapentadol
Weak mu agonist + NET inhibition
Spiradoline
Full K antagonist
BAD
CR845
Didn’t say what it does?
Doesn’t cross BBB!
Outstanding analgesia!
Dextramorphan
D-isomer of codeine
No analgesia; does not bind opioid receptor
Used for cough
Diphenoxylate
Weak mu agonist
Used as antidiarrheal
Schedule V - high doses can cause CNS effects (euphoria, abuse liability)
Loperamide
Weak mu agonist, crosses BBB but is pumped out by P-GP transporter
Which mixed action drugs are available orally?
Pentazokine
CR845
Buprenorphine
Which mixed action drugs are not available orally?
Nalbuphine
Spiradoline
Which mixed action drug is a nasal spray?
Butorphanol