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morphine (PK (A (absorbed from the GI tract, significant first past…
morphine
PK
A
absorbed from the GI tract
significant first past metabolism (25% bioavailability)
given parentally or intrathecal or via epidural
D
doesn't concentrate in tissue
M
conjugation, 1 metabolite - same actions as the parent
E
kidneys
PD
full agonist @ mu receptors
actions
induce papillary constriction
direct stimulation for chemo receptor trigger zone (throwing up)
decrease in vascular peripheral resistance
respiratory depression (decrease responsiveness to CO2)
rare with clinical doses
muscular rigidity @ higher doses
blocks nocioception along several points of the pain pathway
inhibits GI motility - CONSTIPATION
dilation of cutaneous blood vessels
immunomodulation (inhibits NK cells)
alters thermoregulation
small lowering of core body temperature
WHY IS THERE SO MANY????
there are mu receptors all throughout the body so morphine can bind everywhere