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ANTAGONISTS
Department of Pharmacology
Medical School Padjadjaran University
OPIOID RESEPTORS
1. On the membranes of certain cells in the CNS
2. On nerve terminals in the periphery
3. On the cells of the GIT
Pentazocine
Mainly at mu recept.
Agonist at kappa
Partial antagonist at mu
+
Mu
Kappa
Sigma
Kappa receptors :
1. Spinal analgesia
2. Sedation/dysphoria
3. Pupil constriction
Sigma receptors :
1. Dysphoria
2. Hallucination
3. Psychomimetic effects
4. Pupil dilatation
Morphine
Crude opium contains major analgesic morphine
and lower concentration of codein
Both have high affinity to Mu, varying to Kappa
and Delta and low to Sigma receptors
The prototype agonist
Mechanism of action :
Interacting with opioid receptors in CNS and GIT :
ACTION of morphine
1. Analgesia result of raising threshold at SC
level and altering the brains perception of
pain (aware the presence of pain but the
sensation is not unpleasant
specific
, tone
constipation