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Cards In This Set
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1. Rank order potency of alfentanyl, fentanyl, morphine, remi-fent, sufentanyl2. Mu, Kappa and Delta are which type of receptors?
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1. morphine - 10mgalfentanyl - 20x'sFent/ Remi - 100x'sSuFent - 1000x's2. G-protein
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Opioid DIvisions1. Naturally occuring - 42. semi-synthetic3. synthetic
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1. morphine, codiene, papaverine, thebaine2. heroin, dihydormorphone, morphinone, thebaine derivatives (etorphine, buprenorphine) "-one"3. morphinan series (levophanol, butorphanol)diphenylpropylamine series (methadone)benxomorphan series (pentazocine)phenylpiperidine series (meperidine, the 4 fentanyls)
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Mu Receptors1. locations of Mu receptors2. 2 opioid Mu receptor antagonists (generic names)3. 2 natural endogenous ligands4. 3 agonists
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1. brain and spinal cord2. naloxone and naltexone3. Beta-endorphin and endomorphin4. morphine, fentanyl, and DAMGO
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Delta Receptors1. locations2. 2 natural endogenous ligands3. 2 agonists4. 2 antagonists
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1. brain and spinal cord2. Leu - enkephalin and Met - enkephalin3. DPDPE and deltorphin4. naloxone and naltrindole
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Kappa Receptors1. locations2. natural/ endogenous ligand3. agonists (3)4. antagonists (2)
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1. brain and spinal cord2. dynorphin3. buprenorphine, pentazocine (Talwin) and morphine4. naloxone and norBNI
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Opioid Recpetor - G- Protein coupled signal trasnduction (mainly G (i/o) )when opioid binds:1. 2 things that are suppressed2. 2 things that are activated3. overall, any or all of above result in what?
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1. - N-type, pre-synaptic voltage Ca channels (no Ca is released into cell)- adenylate cyclase- inhibits formation of ATP-> AMP2. - inwardly-recitfying K channels= k leaves cell causing hyperpolarization - Mitogen Activated Protein Kinase cascade = gene expression and phospholipase A --> producing prostaglandins and leukotrienes 3. decreased neuronal activity (decreased excitability)
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Pain/ Pain Inhibition Pathway1. 3 basic steps2. result of pre and post-synaptic inhibition
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1a) pain stimulus (A or C fibers) - afferent neuronb) rls of glutamate or Sub. P -> up spinothalamic tractc) descending pain inhibitory tract = rls enkephalin -> pre-synaptic (affects Ca entry, NTM not released); post-synaptic (signal not transduced)
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1. Opioids can directly activate the _____ which in turn activated the emetic center
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1. chemoreceptor trigger zone (CTZ)
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Analgesia- Supraspinal/ Spinal1. receptors2. agonist3. antagonist
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1. M, D, K2. analgesia3. no effect
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Respiratory Function1. receptors2. agonist3. antagonist
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1. Mu2. decreases3. no effect
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GI1. receptors2. agonist3. antagonist
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1. M, K2. decreases transit3. no effect
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Feeding (animal model)1. receptors2. agonist3. antagonist
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1. M, K, D2. increases3. decreases
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Sedation1. rec2. agonist3. antagonist
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1. M, K2. increases3. U/K
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Diuresis1. receptors2. agonist3. antagonist
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1. K2. increases3. U/K
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Prolactin secretion1. receptors2. agonist3. antagonistGrowth Hormone Secretion4. receptors5. agonist6. antagonist
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1. Mu2. increases3. decreases4. Mu and/or kappa5. increases6. decreases
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