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10 Cards in this Set
- Front
- Back
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B endorphin receptor: |
-Mu receptor -increase K+ efflux, hyper polarize neuron |
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dynorphins receptor: |
-kappa receptor -decrease Ca++ influx, less neurotransmitter release |
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enkephalins receptor: |
-delta receptor -increase K+ efflux |
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Morphine receptors: duration: |
-Mu agonist -low oral to parenteral potency ratio- 3:1 (need 3 times the dose) -larger first pass effect -duration: 4-5hrs |
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Heroin receptors: site of action: |
-mu receptor -diacetyl morphine--activated by metabolism to 6-mono-acetyl morphine and morphine -high abuse potential -more lipophilic, better brain solubility |
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Codeine receptor: |
-mild to moderate pain control -morphine life efficacy is not achievable at any dose -some is metabolized to morphine |
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Oxycodone (percocet) Hydrocodone (vicodin) receptor: use: efficacy: |
-often used in combo with aspirin or acetaminophen -oxycodone is more efficacious and useful in moderate to severe pain -high abuse problem |
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Methadone receptor: use: |
-mu agonist -equipotent with morphine, good oral bioavailability -longer duration of action -used to treat opioid abuse and chronic pain |
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Meperidine receptor: use: |
-shorter duration of analgesia than morphine -forms toxic metabolite, normeperdine, which can accumulate with prolonged use -interactions with MAO inhibitors |
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Fentanyl receptor: use: |
-mu agonist -100x as potent as morphine -short acting 1-5hrs -injectable or transdermal patch |
