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ANTAGONISTS
By : Asep Sukohar
Departement of Pharmacology
Medical School Lampung 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 treshold at SC
level and altering the brains perception of
pain (aware the presence of pain but the
sensation is not unpleasant)
specific
, tone
constipation
Pharmacokinetics :
Adm. : Morfin usually not be given orally
IM,SC,IV. Codein orally
Distrib. : Morfin to allbody tissues and cross into
the fetus. Morfin is yhe least lipophilic, cross the
BBB in a very small amount : Fentanyl and Heroin
are fat soluble rush euphoria.
Fate : Transformed to glucuronides Morfine-6glucuronide very potent analgesics.
Excretion : Urine >>, a small amount into bile
DOA of morfine is 4 6 hours in native individuals
ADVERSE EFFECTS
Severe respiratory depression
DRUG INTERACTIONS
The depressant effect of morphine is enhanced
by phenothiazines, MAOI, tricyclic
antidepressants.
Amphetamine low dose and Hydroxyzine
Increase analgesic effect
MEPERIDINE
A synthetic opioid
Binds particularly kappa receptors
Causes respiratory depression
Orally no significant Cardiovascular
action
IV peripheral resistence decrease,
peripheral blood flow increase cardiac rate
increase
Moderate antagonist
Propoxyphen : Combined with aspirin or
acetaminophen. SE : as morphin but weaker
Combined with alcohol and sedative causes CNS
depression death by resp. depress. And
cardiotoxicity; Toxic dose : Like morphin =some
patients cardiotoxic and pulmo edema