EXAM #3 OPIOIDS REVIEW Flashcards
Pain is transmitted via a______That originates where?
three-neuron system that originates
at the periphery and ends at the cerebral cortex.
At periphery tissues, noxious stimuli are mainly received and transmitted by
A beta, A delta, and C fiber neurons.
These first-order neurons synapse with
second-order neurons in the dorsal horn of the spinal cord level.
Second-order neurons
travel up the spinal cord via the
dorsal column and spinothalamic tract and synapse with third-order neurons at the thalamus, which then transmit signals to the cerebral cortex, the site of pain perception.
Opioids exert their effects at
receptors at all three levels of this system.
The major receptors activated by opioids are
mu, delta, and kappa
Opioids receptors are
These are G-coupled receptors, which carry the
mediator-induced signal in conjunction with a second messenger such as cyclic adenosine monophosphate (cAMP).
Opioids receptors are
G-coupled receptors, which carry the mediator-induced signal in conjunction with a second messenger such as cyclic adenosine monophosphate (cAMP).
Where are opioids receptors located? They are located at the
periphery, the dorsal horn of the spinal
cord, and finally the brainstem, thalamus, and cortex.
At the opioid receptor locations, the three major mechanisms of action are:
- Inhibition of presynaptic Ca2+ influx, which depolarizes the cell and inhibits the release of neurotransmitters at the synaptic cleft.
- Increasing postsynaptic K+ efflux, which depolarizes and inhibits cellular signal transmission.
- Activation of the descending inhibitory pain pathway
via inhibition of GABAergic receptors found in the
brainstem.
Opioid analgesia is primarily achieved at the brain, spinal
cord, and peripheral tissues via
mu1 and mu2 receptors.
In the spinal cord, opioids target
mu2 receptors
Supraspinal sites are
periaqueductal gray matter
locus coeruleus
nucleus raphe mmagnus) effects are achieved at mu1 receptor
Supraspinal effects are achieved at
Mu 1 receptor
Morphine on respiratory system
Morphine and other mu1 agonists decrease CO2 responsivity in the medullary respiratory center.
Morphine on ventilatory response
There is a right shift and decrease in the slope of the ventilatory response to CO2 curve
Remifentanil is most notably known for its short
context-sensitive half-life
Morphine : It is primarily metabolized by
hepatic phase II conjugation (3- glucuronidation) to form morphine-3-glucoronide
Methadone protein binding and metabolism
Methadone is 90% protein bound and
undergoes N-demethylation in the liver
Fentanyl metabolism and % excretion
in the liver by N-dealkylation to norfentanyl and only 6% is excreted unchanged by the kidneys.
How does meperidine reduces shivering?
Through kappa-opioid receptors,
Whereas all opioids and propofol in a dose-dependent manner,
suppress motor evoked potentials (MEPs)
Remifentanil and MEPs
suppresses MEPs to a lesser extent.
The partial agonists and mixed agonist–antagonists are have clinical effects at mu and kappa receptors
nalbuphine, butorphanol, and buprenorphine