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27 Cards in this Set

  • Front
  • Back
Morphine absorbtion
well absorbed, extensive first-pass metabolism limits oral use (35% bioav)
Morphine chemical structure
polar metabolites excreted in urine;
morphine-6-glucuronide is active metabolite;
renal insuff. can cause agitation, confusion
Morphine analgesia
pain relief, no general sensory effects
dull pain >> sharp pain
morphine: mood and site of action in brain
euphoria
locus coruleus, mesolibic dopamine, n. accumbans
-confusion, sedation not uncommon
morphine effect on pupil
miosis (excites parasymp)
morphine; cough
depressions (cough reflex)
morphine respiratory
depression
causes decreased response to CO2.... consideration with COPD and pain
morphine intracranial pressure
increased (consider with head trauma)
morphine nausea
common in ambulatory patients
morphine cardiovascular
vasodilation, reduced peripheral resistance
morphine GI
decreased contractions, increased water absorption
morphine urine
decreased output, increased sphincter tone
morphine labor
prolongation of labor
morphine GI
decreased contractions, increased water absorption
morphine urine
decreased output, increased sphincter tone
morphine labor
prolongation of labor
Meperidine
rapid onset, short duration
*accumulation of long-lived metabolite
Use limited to ACUTE PAIN
unique tox: seizures, twitches
Codeine
high oral/parenteral potency ratio
weak full agonist
10% lack enzyme for conversion
fentanyl
100x more potent than morphine
short duration of action
delivery routes: patch
effective: break through pain
watch with cyp inhibitors
tramadol
codeine derivative
weak agonist at mu receptors
extended release
seizures? pts on antidepressants are considered to be at increased risk of seizures
tapentadol
tramadol-like
weak mu agonist and NE uptake blockers
buprenorphine
partial agonist at mu receptor
very slow dissociation
Suboxone
approved for opiate dependance
naloxone & naltraxone
opiate receptor antagonist (mu>kappa, delta)
prevention of heavy drinking
diphenoxylate, loperamide
like meperine, but poor absorption from gut
only in diarrhea
methylnaltrexone
injectible OPIOID ANTAGONIST for opioid-induced constipation (terminally ill)
does not cross BBB so does not decrease analgesia
dextromethorphan
antitussive?
no protoypical opioid effects
contraindicated in young children
nalfurafine
kappa receptor agonist
reduces substance-p induced scratching
relief of uremic-induced hemodialysis scratching