Pharm Pain, Martin I Flashcards
What are the full agonists for opioid R
morphine
fentanyl
heroin
methadone
what are the partial agonists for opioid R
codeine, hydrocondone, oxycodone
what are the mixed agonists/antagonists
buprenorphine
opioid antagonists
naloxone
what are the weak opioid antonists or reuptake inhibitors
tramadol
tapentadol
what are the non opioid analgesics
acetaminphen, aspirin, other NSAIDs and selective COX2 inhibitors
what is analgesia
attenuation of pain perception without loss of consciousness
how is analgeisa accomplised
raising pain threshold at level of spinal cord and altering brains perception of pain
sensory component of pain
perceived as result of direct stimulatino of pain R
reactive component of pain
intensity of pain dramatically altered by lvel of anxiety and stress response related to original insult
narcotic
substance producing stupor associated with analgesia
opiates
natural products and dervatives obtained from opium poppy
opium, morphine, heroin, codeine
opioids
bind to opioid R
includes agonists, antagonists, partial agonists and mixed agonists/antagonists
endogenous opioid agonists
endorphin enkephalin, dynorphin and others
where are endogenous opioid peptides made
in nucleus and transported down
endogenous opioid peptide precursoe
pro-opiomelanocortin POMC
opioid effect in peraqueductal gray
inhibit GABA release which increase inhibitory nerve activity regulating projections to medulla that alter dorsal horn excitability
how do opiates work on spinal cord
presynaptically to block Ca influx and NT release
or
postsynaptically to open K Ch causing hyeprpolarization
mu opiod R
endorphins>enkephalins>dynorphins supraspinal and spinal analgesia sedation inhibition respiration slowed GI modulation hormone and NT release
kappa opioid R
enkephalins>endorphins=dynorphins
supraspinal and spinal analgesia
modulation hormone and NT release
delta opioid R
dynorphins>endorphins>enkephalins
supraspinal and spinal analgesia
psychomimetic effects and slowed GI transit
principle signal mech of opioid R
GPCR
- inhbiit cAMP
- open K Channels allowing efflux and hyperpolarization
- reduce presynaptic Ca influx inhibiting NT release