Multicyclic Opioids 3

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    What receptor do these drugs work at and what structure indicates this?
    • Pentacyclic
    • “Antagonism”
    • Mu antagonists:
    • N-allyl or N-cyclopropylmethyl on the nitrogen atom
    • 7,8 dihydro-6-one
    • 14  B-OH
    • (Naloxone and Naltrexone)
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    By what mechanism do these drugs cause high affinity mu antagonism?
    • Induce conformational changes that uncouples the receptors from their G-proteins
    • (Naloxone and Naltrexone)
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    If you had a patient on a mu agonist,what considerations would need to be made prior to staring one of these drugs?
    • To prevent withdrawal:
    • Must be agonist free for 7-10 days before one of these antagonists can be administered
    • Unless trying to rescue a patient from fatal overdose (Ggive STAT)
    • (Naloxone and Naltrexone)
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     How does the potency of these two drugs compare?
    • Naltrexone is twice as potent as naloxone
    • Due to an enhanced lipophilicity of Naltrexone and distribution to CNS
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    Is this drug orally active?
    Yes
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    Why is this drug useful for opioid addiction therapy?
    • Mu antagonist
    • Blocks opioid receptors in opioid-free patients = thwarts euphoria of agonists if patient relapses
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    (True/False) Naltrexone has shown efficacy in the treatment of alcoholism.
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    Low doses (4.5 mg daily) naltrexone has shown efficacy in what ailment?
    Bowel ulcerations and enhancing immunity in active Crohn’s disease
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    Why would you choose an IM version over an oral version of Naltrexone for opioid addiction therapy?
    • IM contains a slow release polymer that makes it last for 4 weeks
    • Increases convenience and adherence
  10. How would the daily exposure to Naltrexone compare between an IM Q4weeks and a 50 mg tablet QD and why?
    • Greater exposure with the IM version
    • Avoids 1st pass metabolism so: Much less metabolite is formed IM
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    What is the primary metabolite of this drug and what enzyme produces it?
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    • 6B-naltrexo
    • Cytosolic enzyme dihydrodiol dehydrogenase
    • (Naltrexone)
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     is this drug orally active?
    • No
    • (Naloxone)
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    Why is this drug not orally active?
    • Due to inactivating pre-hepatic and first pass metabolism
    • Allyl group is oxidized and conjugated
    • (Naloxone)
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    What is the primary urinary metabolite of this drug?
    • C3 glucuronide
    • (Naloxone)
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    In what form is this drug available?
    • IV
    • (Naloxone)
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    What is this drug used for?
    • Reverse life-threatening opioid overdose, respiratory and CNS depression
    • (Naloxone)
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    Will this drug precipitate withdrawal in mu agonist users?
    • Yes, mu Antagonist
    • (Naloxone)
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    Why will symptom of withdrawal be short lived when this drug is given to a mu agonist user?
    • 1-2 hour half-life
    • (Naloxone)
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    What was this drug used for?
    • IV use in reversing life-threatening opioid overdose
    • Mu antagonist
    • (nalmefene)
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    Why was this drug likely taken off the market?
    • Excessively long DOA (11 hours) to be used for reversing opioid overdose
    • Caused prolonged withdrawal symptoms
    • (nalmefene)
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     Is this drug orally active?
    • Yes
    • (nalmefene)
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    Why does this drug have such a long half life (11 hours)?
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    • High affinity binding as a mu antagonist due to the 6-exocyclic methylene moiety
    • (nalmefene)
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    Other than treating life threatening overdose, what other uses could this drug have due to its long half life and high oral bioavailability?
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    • Preventing relapse in recovering alcoholics
    • Blocking mu agonist effects of fentanyl
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Multicyclic Opioids 3
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Multicyclic Opioids 3
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