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- opiate are alkaloids extracted from opium poppy,
- opioid is a substances that mimic effects of morphine
What's the difference between opiate and opioid?
from opium plant
- Thebaine, morphine, codeine
where are natural opioids found?
reated from natural opioids — heronin
what are semisynthetic opioids?
created in a lab
- ex: fentanyl and methadone
What are synthetic opioids?
"Skin popping"
In administration of opioids, What is the term for subcutaneous injection of heroin called?
"mainlining"
in administration of opioids, What is the term for IV injection of heronin?
chasing the dragon
What is it called when you smoke heronin?
in the liver
Where are most opioids broken down?
Morphine and Morphine-6-glucuronide(M6G)
- Active metabolites
What is heroin metabolized into?
powerful pain relieving effects
what does M6G produce
M6G and morphine
What is codeine metabolized into?
first order kinetics
How are opioids removed from the body?
~ 7 hours
What is the half life of fentanyl?
~ 2-3 hours
What is the half life of morphine?
~ 1 hour
What is the half life of heroin?
~ 3 hours
What is the half life of codeine?
- Endorphins
- Enkephalins
- Dynorphins
Name the 3 major families of endogenous opioid neuropeptides?
hypothalamus and pituitary gland
Where are endorphins synthesized?
reinforce analgesia and euphoria effects of opioid uses, can cause respiratory depression
What are the effects of endorphins?
throughout CNS and adrenal medulla(PNS)
Where are enkephalins produced?
in the hypothalamus, striatum, hippocampus, and spinal cord
Where are dynorphins produced?
- Pain/stress
- Learning and memory
What are dynorphins involved in?
- Mu receptor
- Delta receptor
- Kappa receptor
What 3 receptors are the effects of opiates mediated by?
Mu
The location of ____ receptors reflect the effects of morphine?
endorphin
Which endogenous peptides of Mu receptors are involved?
- Thalamus
- PAG
- Raphe nuclei
- Spinal cord
Which locations of Mu receptors are involved with the effects of analgesia?
nucleus accumbens
Which location of Mu receptors are involved with the effects of reinforcement?
brainstem
Which location of Mu receptors are involved with the effects of cardiovascular, respiratory depression, nausea, and vomiting?
thalamus and striatum
Which location of Mu receptors are involved with the effects of sensorimotor integration?
endorphin and enkephalin
Which endogenous peptides are involved delta receptors?
- cerebral cortex
- Thalamus
- Striatum
- Spinal cord
Where in the brain are delta receptors found?
- Olfaction
- Motor integration
- Reinforcement
- Cognitive functions
What is the role of delta receptors?
dynorphin
For kappa receptors what is the major peptide?
- Striatum
- Hippocampus
- Amygdala
- Hypothalamus
- Pituitary
Where are kappa receptors found in the brain?
dysphoria, stress, memory
The kappa receptors found in the hippocampus, amygdala, hypothalamus, pituitary are involved in what?
Gut motility and feeding
The kappa receptors found in hypothalamus is involved with what?
local GABA interneurons
What is activity of DA neurons in the VTA controlled by(decrease DA)?
B-endorphin increase VTA firing by inhibiting GABA cells
- Increase DA
How do opioids alter mesolimbic DA?
act on Kappa receptor on DA neuron terminals
- Reduce release of DA —> cause dysphoria
How do dynorphins affect DA?
- Heroin
- Morphin
- Fentanyl
- Oxycodone
What opiates are agonists at the MU receptor?
buprenorphine
What opiates are partial agonists at the MU receptor?
- Narcan
- Naltrexone
What opiates are antagonists at the MU receptor?
- Rush
- High
- Nod
- Straight
List the subjective effects of opioids?
loperamide(Imodium)
What type of opium and morphine is used to treat diarrhea?
Nociceptors
What type of pain receptors detect chemical, mechanical or therm pain?
pain signals to neurons in spinal cord
What happens when Mu opioid receptors found presynaptically on 1st order spinothalamic neurons transmit?
cause IPSP
What happens when binding of piate drugs on postsynaptic Mu opioid receptors on 2nd order spinothalamic neurons?
acupuncture
What is the term for releasing endogenous opioids?