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18 Cards in this Set
- Front
- Back
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B endorphin |
Endogenous Opiate -Mu receptor -Modulates pain transmission by increasing K+ efflux, hyperpolarizing neuron -Analgesia, CV depression, respiratory depression, anti-tussive, vomiting, sensorimotor integration |
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dynorphins |
Endogenous Opiate -kappa receptor -Modulates pain transmission by decreasing Ca2+ influx, preventing neurotransmitter release -Neuroendocrine function, water balance, feeding, temperature control, dysphoria, analgesia |
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enkephalins |
Endogenous Opiate -delta receptor -Modulates pain transmission by increasing K+ efflux -Analgesia, reinforcement, cognitive function, olfaction, motor integration |
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Morphine |
Opioids -Mu agonist -Gold standard opioid analgesic -Given IV or sublingual due to 70% 1st pass -Slow onset, long duration -2-3 hour half life -Hydrophilic -- slow CNS penetration & exit -At presynaptic terminal: inhibits cAMP formation & calcium uptake - thus inhibiting neurotransmitter release -At post-synaptic terminal: opens K+ channel, hyperpolarizing cell & dampening neuron firing |
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Heroin |
-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 |
-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) |
-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 |
-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 |
-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 |
-mu agonist -100x as potent as morphine -short acting 1-5hrs -injectable or transdermal patch |
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Hydromorphone (Dilaudid) |
-2-3x as potent as morphine |
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Nalbuphine |
-mu ANTagonist, kappa AGonist -similiar in efficacy and potency to morphine -lower abuse potential -can precipitate withdrawal in opioid dependent pts -injectable form only |
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Buprenorphine |
-partial mu agonist, 25-30x greater potency than morphine -treat moderate to severe pain -comes in a patch form |
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Suboxone |
-oral buprenorphine combined with naloxone (opioid antagonist) -treat opioid dependence |
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Naloxone |
-high affinity for mu receptor, less for kappa and delta -much greater activity parenterally than oral (combined with other opioid drugs to make ineffective is shot up) -duration 1-2hrs -treat opioid overdose -combine with opioids to reduce parenteral abuse liability |
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Naltrexone |
-orally active, long half life 24hrs -treat alcoholism and opiate addiction |
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Dextromethorphan |
-dextro isomer of levorphenol (mu agonist) -not an opioid! no analgesic effects (not a mu agonist!) -NDMA antagonist -cough suppressant- antitussive |
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Tramadol |
-weak mu agonist -blocks NE and 5HT uptake -use for mild to moderate pain |
