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59 Cards in this Set
- Front
- Back
4 basic types of nociceptors
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1)heat response
2)cold response 2)acid response 3)pressure response |
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Chemical mediators of pain in tissues (3)
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1)PG
2)K+/H+ 3)prostanoids |
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Chemical mediators of pain in plasma
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bradykinin
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Chemical mediators of pain in nerve terminals (3)
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1)substance P
2)CGRP 3)glutamate |
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Opoid receptor subtypes (4)
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1)mu (MOP)
2)delta (DOP) 3)kappa (KOP) 4)ORL1 (NOP) |
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Mu agonists
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enkephalin
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Delta agonists (2)
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1)enkephalin
2)endorphin |
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kappa agonists
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dynorphin
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ORL1/NOP agonists (2)
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1)orphanin FQ
2)nociceptin |
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Mu receptor agents (3)
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1)morphine
2)fentanyl 3)oxycodone |
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Kappa receptor agents (3)
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1)butorphanol
2)levorphanol 3)pentazocine |
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Descending pain pathway is always off b/c of...
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GABA
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Opioid analgesics mechanism (4)
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1)directly inhibit release of NTs that activate ascending pain pathways
2)inhibit release of NTs that inhibit descending pain pathway 3)activate descending analgesic pathways (promoting release of opioid peptides) 4)stimulate descending inhibitory pathways (5-HT, NE) |
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DXM properties (3)
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1)little addictive potential
2)less constipating than codeine*** 3)NMDA receptor antagonist |
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Anti-diarrheal effects of opioids (4)
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1)incr tone
2)decr gut motility 3)stim mu2/delta receptors in brain and GI nerve plexus 4)loperamide crosses BBB poorly |
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Diphenoxylate
a)____ analog b)_____ prevents abuse |
a)meperidine
b)anticholinergic SE's |
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Opioids can also be used for...(2)
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1)dyspnea of acute pulmonary edema
2)anesthesia |
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Dyspnea of acute pulmonary edema def (2)
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1)associated w/ MI
2)labored/difficult breathing associated w/ pain |
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....(3) used as regional anesthetics b/c....
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1)morphine, fentanyl, lidocaine
2)produce spinal analgesia |
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a)Nociception vs.
b)Hyperalgesia vs. c)Allodynia |
a)normal response to noxious stimulus
b)enhanced response to a noxious stimulus c)when a non-noxious stimulus is perceived as noxious |
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Acute pain desc. (5)
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1)pain following an injury, stops when treated
2)important for survival 3)pt knows pain will end @ some point 4)clinical assessment correlates well w/ pt self-reporting 5)important to prevent it from becoming chronic pain |
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Chronic pain characteristics (4)
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1)lasts for more than several weeks (episodic or continuous)
2)no survival benefit 3)more pronounced psychological harm 4)poor correlation b/w clinical assessment and pt assessment |
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Plant that morpheine/codeine comes from and it is...
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papaver somniferum
gold standard for pain relief since 3rd century BC |
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Morphine metabolized in liver to: and characteristics of them (2)
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1)morphine-6-glucuronide, active 100-800x more potent than morphine
2)morphine-3-glucuronide, no analgesia, may cause tremors |
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Codeine is metabolized to...(2)
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1)5-10% to morphine-6G
2)80% to codeine-6G |
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Genetic variability w/ codeine (3)
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a)coversion to morphine via CYP2D6
b)10% of whites don't have this so codeine is ineffective c)chinese have lower CYP2D6 and produce less morphine-6G |
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2 main ways to block pain
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1)block glutamate receptor
2)activate descending pain inhibitory tracts |
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Semisynthetic opioids (3)
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1)hydrocodone
2)oxymorphone 3)oxycodone |
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Oxycodone (Oxycontin) (4)
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1)mu agonist
2)8x more potent than codeine 3)active metabolites, but less potent 4)treat acute pain >> than chronic |
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Methadone (dolophine) (5)
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1)mu agonist
2)effective orally w/ long half-life (so long time to SS) 3)less sedation than morphine 4)higher doses for addiction than pain 5)racemic mixtures activate mu and antagonize NMDA |
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Methadone cautions (2) and interactions (3)
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1)will accumulate to toxic levels if dosed too freq.
2)may prolong Q-T 1/2)rifampin and phenytoin incr metabolism 3)cimetidine inhibits metabolism |
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Meperidine (demerol) (5)
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1)normepiridine is antimuscarinic
2)don't use for more than 48hrs w/ doses >600mg/day 3)no antitussive 4)less constipation, spasm, retention than morphine 5)mu agonist |
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Normeperidine properties (3)
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1)half as efficacious as meperidine w/ 2x greater half-life
2)decreases seizure threshold 3)increases CNS excitability |
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Pentazocine
a)receptor b)other (4) |
a)weak mu agonist/antagonist, kappa agonist
b1)can precipitate withdrawal b2)w/ naloxone to prevent euphoria b3)can't reverse MS respiratory depression b4)no active metabolites |
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Pentazocine
a)use b)SE's (3) c)avoid use in... |
a)pt w/ chronic pain or w/ former opioid addicts
b)less urinary retention, constipation, dysphoria @ high doses c)CAD |
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Butorphanol
a)receptor b)other (2) |
a)mu ANTAgonist, kappa agonist
b1)ceiling effect on respiratory depression b2)good for acute pain |
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Butorphanol
a)approved for... b)SE's (2) |
1)severe HA, post-labor, surgery
2)CV effects like pentazocine, sedation |
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Nalbuphine (Nubain)
a)receptor b)other (3) |
a)mu ANTAgonist, kappa agonist
b1)less dysphoria than pentazocine b2)no CV effects (so good for MI) b3)abstinence syndrome |
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Dysphoria
a)cause |
a)kappa receptor agonists
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Respiratory depression
a)cause b)other (3) |
a)mu2 agonist in brain
b1)primary cause of death b2)dose dependent b3)tolerance develops |
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Miosis
a)cause b)other (3) |
a)mu/kappa agonists
b1)dose dependent b2)NO TOLERANCE DEVELOPS b3)GOOD INDICATOR OF OPIOID O.D. IF pt unconscious |
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Constipation
a)cause b)other (2) |
a)mu2/delta receptors in brain and GI nerve plexus
b1)little/no tolerance b2)initiate laxatives early |
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Sensitivity rxns
a)cause b)other (2) |
a)wheals @ site of injexn due to histamine
b1)urticaria, rashes b2)anaphylaxis RARE |
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Biliary Tract
a)what happens b)prevented by... c)reversed by... |
a)incr tone in sphincter of Oddi
b)atropine c)opioid antagonists |
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GU effects (2)
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1)decr renal fxn by decr renal blood flow
2)urinary retention |
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Use of agonists w/ agonist/antagonist can lead to.... (2)
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1)diminished analgesia
2)precipitated withdrawal |
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Use of opioids in pregnancy (2)
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1)fetus may become dependent
2)manifest withdrawal after delivery |
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Use of opioids in pts w/ endocrine disease
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1)pts w/ addison's or myxedema may be more sensitivie
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Use of opioids in pts w/ impaired pulmonary fxn =
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acute respiratory failure
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Use morphine w/ care in asthmatics b/c...
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it may induce histamine release (fentanyl doesn't release histamine)
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Acute overdose of opioids characterized by... (4)
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1)coma
2)pinpoint pupils 3)respiratory depression 4)maybe needle marks |
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Pure opioids antagonist...
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naloxone
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Naloxone (Narcan)
a)affinities b)treat... c)induces |
a)mu > kappa1 > delta > kappa3
b)acute opioid overdose c)abstinence syndrome |
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Naltrexone (Revia)
a)affinities b)adv over Naloxone c)treat... |
a)mu > kappa1 > delta > kappa3
b)longer half-life c)chronic alcoholism/opioid addiction NOT overdose |
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____ is not used for opioid induced constipation
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NO BULK LAXATIVES
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If you are switching opioids you must...
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make sure you are switching from mu agonist to mu agonist...etc.
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Thermoregulation def. (3)
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1)maintain normal body temp.
2)set pt is normal body temp (97-99F) 3)diurnal temp variations in set pt (lowest in morn, peak in late afternoon/early evening) |
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Temp. regualtion center
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hypothalamus
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Thermoreceptors
a)where b)fxn |
a)thruout body
b)transmit temp changes to hypothalamus so it can thermoregulate properly |