Exam 4 - opioid analgesics Flashcards
The descending pain modulating system projects via the _____ to the spinal cord ____ ____. Contains high concentrations of endogenous _____ _____. It is activated by _____ analgesics like certain kinds of ____.
Medulla Dorsal horn Opioid peptides Opiate Stress
Opiates produce analgesia by ____ ____ on the CNS
Direct action
Name for pain receptors?
Nociceptors
How do systemic administration of opiates produce analgesia?
By acting at widely distributed sites throughout the CNS
The pain suppression system is controlled by what?
Serotonin and also partially enkephalin-mediated
What 4 things is the pain suppression system activated by?
- Noxious stimuli
- Pain
- Psychological factors (including placebos)
- Opioids
What do opioid analgesics take place?
Analgesia system
The analgesia system is mediated by what 3 things?
- periaqueductal grey matter (midbrain)
- nucleus raphe magnus (medulla)
- pain inhibitory neurons (dorsal horn)
Proper name for endogenous morphine?
Endorphin - opiate like effect
What 5 places are endorphins found?
- GUT
- sns
- adrenal medullart chromaffin cells
- cns (arcuate nucleus hypothalamus, pituitary/nucleus tractus solitarii, visceral afferents from CN VII, IX, X)
- pancreatic islet cells
T/F endorphins are involved in blood pressure regulation, temperature regulation, and food intake.
True
What are the 3 precursor molecules of endorphins?
- proenkephalin A
- pro-opiomelanocortin (POMC) = B-endorphin
- Proenkephalin B (prodynorphin) = dynorphins
Endorphins act via what receptor in the GI tract?
What side effect does this cause?
Mu receptor
Side effect = constipation
_____ mimics opiate activity = weak analgesics
Enkephalins
Where are enkephalins found in the body?
Widely distributed - NT in many brain areas: PAG, RVM, spinal cord laminea
May be responsible for producing analgesia in placebo responders like _____.
Acupuncture
What receptors do enkephalins act through?
Mu and delta
What works through the kappa receptors?
Dynorphins
What 3 places are dynorphins found?
- Spinal cord
- through out brain
- hypothalamus
Opiate effect depends on what?
Site of binding - highly specific = STEREOSPECIFIC
Only levo-isomers have biological activity