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ANALGETIK OPIOID

SEJARAH
KLASIFIKASI
Mechanism of Action
• Opioids act as agonists at specific opioid receptors at presynaptic and
postsynaptic sites in the central nervous system (CNS) (mainly the
brainstem and spinal cord) as well as in the periphery.
• Opioid receptors normally are activated by three endogenous peptide
opioid receptor ligands known as enkephalins, endorphins, and
dynorphins.
• Opioids mimic the actions of these en- dogenous ligands by binding
to opioid receptors, result- ing in activation of pain-modulating
(antinociceptive) systems.
• The principal effect of opioid receptor activation is a decrease in
neurotransmission, by presynaptic inhibition of neurotransmitter
release (acetylcholine, dopamine, norepinephrine, substance P)
• Th m receptors are principally responsible for su- praspinal and spinal
analgesia.
• Theoretically, activation of a subpopulation of m receptors (mu1) is
speculated to produce analgesia, whereas mu2 receptors are
responsi- ble for hypoventilation, bradycardia, and physical depen-
dence.
• Activation of k receptors results in inhibition of neu- rotransmitter
release via N-type calcium channels.

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