OPIOID ANALGESICS AND ANTAGONISTS

- Derived from opium

- Opium- dried exudate of the poppy
seed capsule

1) Morphine
- phenolic hydroxyl group
- analgesic activity- p- phenyl-N-
alkylpiperidine moiety
(piperidine ring is in the chair
form and is perpendicular to the
aromatic ring, alkly grp-methyl)
2) Natural of synthetic opioids
a. phenanthrenes
eg. morphine, hydromorphone,
codeine, hydrocodone,
nalbuphine, buprenorphine,
nalorphine, maloxone,
naltrexone
Methylation of the phenolic 3-
hydroxyl grpp w/ or w/o
modification of the 6-hydroxyl
grp- reduced agonist potency
but enhanced oral
bioavailability

b. phenylheptylamine
eg. Methadone, propoxyphene
c. phenylpiperidine
eg. Meperidine, fentanyl,
sufentanil
eg. Loperamide, diphenoxylate
d. morphinan
eg. Levorphanol

3) Opioid antagonists