Chemistry of opioids and opioid antagonists 3
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12 Terms
Buprenorpine
oripavine derivative
partial MOR agonist - high affinity (t ½ = 37h)
Antagonist at KOR and DOR
analgesia, less sedation (less risk addiction)
fewer withdrawal symptoms
lower effect on respiration
Buprenorphine metabolism
1st pass via CYP3A4 at the cyclopropylmethyl
N-dealkylation
4x less potent
Thebaine
Oripavine
Suboxone
Buprenorphine + Naloxone sublingual tabs
abuse deterrent
replacement therapy for opioid dependence
Nalbuphine
mixed agonist (KOR)/antagonist (MOR)
lower effect on respiration
can cause dysphoria
Levorphanol
5x more potent than morphine
t ½ = 11-16h
LogP = 11-16h
Dextrorphan
result of O-demethylation on dextromethorphan
NMDA antagonist (so is PCP)
psycotropic
→ reason for abuse of dextromethorphan
dextromethorphan
Phencyclidine
“PCP”
Butorphanol
Mixed agonist (KOR - strong)/antagonist (MOR - weak)
5-10x more potent than nalbuphine
extensive 1st pass metabolism
Pentazocine
KOR agonist
MOR antagonist
weakest mixed drug
lacks E and C ring
Note 
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