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