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50 Cards in this Set
- Front
- Back
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what triggers the pain modulation pathway in the brain?
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the pain signal itself
stress caused by pain certain analgesic drugs like morphine |
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what Nts play roles in pain modulation
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NE
Seratonin GABA endogenous opioid peptides |
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what drug reverses stimulated analgesia? (the first)
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naloxone
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list some opioids
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opium
morphine codeine heroin |
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3 principal EOP precursors are:
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1. pro-opiomelanocortin (beta endorphin)
2. pro-enkephalin 3. prodynorphin |
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tell me about EOP production
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not produced directly by biosynthesis......you get cleavage of peptides
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what "couters pain and is credited for the placebo effect"
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brain's endogenous opiate system
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acupuncture
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activates endogenous pain modulation pathway
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papaver soniferum
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opium
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list 4 natural/semi-synthetic opioids
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morphine/codeine
hydromorhone hydrocodone oxycodone |
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list 3 synthetic opioids
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1. phenylpiperidines (fentanyl, sulfentanil, meperidine)
2. methadones (propoxyphene, methadone, LAAM) 3. morphinans (levorphanol) |
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list 2 mixed agonist/atagonist opioid drugs
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buprenorphine
pentazocine |
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list 2 antitussive opioids
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codeine
dextromethorphan |
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list 2 opioid antagonists
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naloxone
naltrexone |
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opioid receptors
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mu kappa delta
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2 uses of opioids
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decrease pain (w/out LoC)
decrease cough |
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pain and opiods
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patient still has pain but DOESNT CARE!
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has high oral/parental potentcy ratio
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oxycodone (oxycontin)
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morphine
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slowly absorbed
t1/2 of 2 hrs |
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active metabolite of morphine
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m6g...m3g is inactive
m3g gets excreted.....an m6g transported used to get into brain |
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m6g 2x as potent as __
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morphine
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herioin cross BBB ___ than morphine...bind poorly to ___ receptors and requiires ___ activation w/in the body AND get's converted to __ and __ in brain
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crosses faster....binds poorly to mu receptors...requires metabolic activation in body and gets converted to morh
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tell me about meperidine toxicities
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you have have meperidine-overdose syndrome and mepridine MAOI syndrome
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meperidine overdose syndrome
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nor-meperidine caused.....Sx = restlessness, halucinations, convulsions
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which phenylpiperidine is used during labor and actually causes restlessness and not sedation
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meperidine
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tell me about fentanyl and sulfentanil
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both are phenylpiperidine opioid drugs; both are mu agonists....fentanyl 100x M and sulfentanyl 1000x M; got give rapid recovery and little CV effects
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what are the 3 methadones? and what is the use?
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propoxyphene
methadone LAAM manage withdrawal syndrome |
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dont mix methadone and morphine...why?
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no euphoria
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if you take methadone daily what happens?
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accum in tissues and get a low steady plasm [ ]
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define the properties of mixed agonist/antagonist opioid drugs
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ANTAGONIZE mu receptors
agonize kappa and delta receptors |
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what are the 2 mixed ago/ant opioid drugs?
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pentazocine and buprenorphine
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pentazocine is
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partial mu agonist
full kappa agonist (where you get the analgesia) |
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buprenorphine
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mu partial agonist (no activity on kappa/delta)
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what are 2 antitussive opioids?
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codeine
dextromethorphan |
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cough receptors (targeted)
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not your kappa, delta, mu
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3-O-methyl morhpine
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codeine
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analgesic effect of codeine due to?
antitussive effect of codeine to? |
morphine
tussive do to distince receptors in cough center |
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dextromethorphan properties
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no analgesic or addictive properties
acts to elevate cough threshold |
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2 opioid antagonists...and which one is the fast one
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naloxone - pure and short acting
naltrexone |
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which opioid antagonist muct be given parenterally b/c of high 1st pass effect
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naloxone
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used to treat alcoholism
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naltrexone
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blocks euphoric effects of heroin and reverses the psychotomimetic and dysphoric effects of petaocine
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naloxone
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list some toxicities of opioids at sites not associated w/ analgesia
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miosis
decreased respiration emesis/nausea convulsions GI effects |
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liver disease
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if pt has then be careful using opioids
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rapid tolerance to opioids develops regarding what? but not what?
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analgesia
sedation euphoria nausea/emesis cough NOT constipation, and covulsant EFX |
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EOPs and opioid drugs inhibit __ and ___ Nt function
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pre and postsynaptic
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EOPs and opioid drugs block pre-syn release of what Nts
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AcH, NE, glutamate, serotonin, substance P
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EOPS and opioid drugs inhibit postsynaptic neurotransmitter function by increasing __ efflux and inducing ____of postsynaptic membrane
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K+ efflux and inducing hyperpolarization of the post syn membrane
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opioid agonist at the presyn opioid receptor causes what to happen? and what about the post syn receptor?
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decrease Ca2+ etry and decr Nt release.....at post syn you get increased K+ efflux leading to hyperpolarization
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at the SUPRAspinal levels opioid drugs activate the ___ (though opioids act at moth supra and spinal levels)....causing ANALGESIA
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descending pain modulation pathway
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