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Opioid drugs:
Full agonists Morphine is a full agonist at the receptor
Partial agonists Codeine (weak receptor agonists)
Antagonists Naloxone
Pharmacokinetics
Absorption
Most opioid analgesics are well absorbed when
given by subcutaneous, intramuscular & oral
routes.
Because of the first-pass effect, the oral dose of
the opioid (eg, morphine) may need to be much
higher than the parenteral dose to elicit a
therapeutic effect.
Distribution
All opioids bind to plasma proteins with varying affinity, the
Metabolism
The opioids are converted in large part to polar
Excretion
Polar metabolites, including glucuronide conjugates of
Pharmacodynamics
Mechanism of Action
Opioid agonists produce analgesia by binding
to specific G protein-coupled receptors, located
primarily in brain & spinal cord regions involved
in the transmission & modulation of pain.
Receptor Types
three major classes of opioid receptors , dan
All are members of the G protein-coupled family of
receptors and show significant amino acid sequence
homologies
Multiple receptor subtypes 1, 2, 1, 2, 1, 2,
& 3.