Pharm Chem Exam 1 Part 4

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crmozingo
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131013
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Pharm Chem Exam 1 Part 4
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2012-01-27 16:29:27
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Pharm Chem Exam 1 Part 4
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  1. Opiod Analgesics
    • anything with morphine-like activity
    • opiates---poppy plants--- Dorothy
  2. Morphine (MSIR)
    • opiod analgesic
    • where tolerance is absent oral LD90 is approximatley 200 mg --- respiratory depression
    • antitussive
    • enterohepatic recirculation leads to it being more detected in the blood over a long period of time
    • decrease pH of urine --- increase excretion of morphine; increase in pH of urin --- increase excretion of M6G
    • M3G antagonist
    • really potent: ng/ml
    • M6G- glucoronidated form is 100x more potent, important for BBB
    • metabolized by 2B7
  3. glucoronidation
    metabolizes the majority of drugs through Phase II metabolic enzymes
  4. UDP glucoronosylatransferases
    • two types: UGT1 and UGT2
    • UGT1A1: associated with bilirubin and steroids
    • 2B15 is subject to polymorphism
  5. Codeine
    • opiate/analgesic
    • demethylated to morphine via 2D6
    • prodrug for pain
    • PM: therapeutic failure
    • UM: idiosyncratic response; metabolites are toxic to infant
    • antitussive (codeine cough syrup)
    • codeine is a morphine methyl ether
    • metabolically reduced to dihydrocodeine with increased potencey
  6. Heroin (Diamorf/Junk)
    • semisynthetic opiate
    • AKA: diacetylmorphine
    • each ester is subject to hydrolysis by CES1 --- 2 monoesters and morphine (all active)
  7. Semi-synthetic opiates
    • Morphine Series:
    • (hydromorphone and oxymorphone)
    • start with morphine or codeine
    • 1. oxidizes alcohol --- ketone
    • 2. reduces the alkene --- alkane
    • 3. adds OH that increases PD

    • Codeine Series:
    • Hydrocodoen and oxycodone
    • 1. oxidizes alcohol --- ketone
    • 2. reduces the alkene --- alkane
    • 3. adds OH that increases PD
  8. Combination products: APAP and codeine
    • FDA limites APAP to 325 mg when taking hydrocodone and oxycodone --- liver toxicity
    • Zyhdro is a non-APAP form of hydrocodone
    • Oxycodone (RIP Heath Ledger/ "hillbilly heroin") DDIs
  9. CYP3A4 mediated DDIs
    • taking ketoconazole --- inhibition --- no effect
    • increases oxycodone exposure (AUC) increasing SEs (nausea, drowsiness, analgesia)
  10. Meperidine (Demerol)
    • synthetic opioid
    • long term pain management --- CNS toxic normeperidine accumulation
    • used when a patient is allergic to morphine (minimal pharmacophore of morphine)
    • -"designer heroin" contains toxic MPTP byproduct
  11. Depehnoxylate (Lomotil) and Loperamide (Imodium)
    • synthetic opiods
    • antidiarrheals with little abuse potential
    • structurally similar to meperidince
    • not water soluble in order to stop diarrhea
  12. Loperamide (Imodium)
    • enter BBB through quinidine inhibition of Pgp
    • PGx: synonymous/nonsynonymous SNPS, indels
  13. Phase III Drug Disposition
    • = transport NOT metabolism
    • P-gp is also called multidrug resistance protein (MDR1 or ABCB1)
    • inducible
    • P-gp acts as a drug efflux pump
    • sex dimorphism: men express more P-gp, women express more 3A4
    • grapefruit juice induces P-gp
  14. Levorphanol (Levo-Dromoran)
    • synthetic opiod analgesic
    • dextromethorphan
    • 2D6 phenotype probe
    • non-superimpossable mirror image of dextromethorphan
  15. Tramadol (Ultram)
    • synthetic opioid
    • racemic synthetic codeine congener
    • racemic switch will not be logical --- racemate is more active than either isomer
    • d-isomer is a mu agonist
    • i-isomer is a NE reuptake (NET) inhibitor (alpha 2 agonist)
    • O-demethylated metabolite is most active
    • *note resemblance to venlafaxine and codeine
  16. Tapentadol
    • monotherapy for chronic pain and depression
    • superimposable on codeine and venlafaxine
  17. Fentanyl (Sublimase)
    • synthetic opioid
    • way more potent than meperidine (fast SL absorption --- lollipops)
  18. X Propoxyphene (Darvocet)
    • CIV analgesic to manage mild pain
    • banned because of fatal heart arrhythmias
  19. Opioid substitution therapy
    • used to treat addiction/analgesic
    • ex: methadone, LAAM
  20. Methadone (Dolophine)
    • opioid substitution therapy
    • 2D6 PM decreased clearance increases risk of OD
    • N,N-demethylated to inactive cyclic metabolite
  21. LAAM (levo-alpha-acetylmethadol)
    • opioid substitution therapy
    • does not cyclic intermediate due to absence of the ketone group
  22. Opioid SAR
    • 3 types: allyl, cyclopropyl, cyclobutyl
    • 3 functions: partial agonists, mixed agonists/antagonists, antagonists
  23. opioid partial agonist
    cannot produce a profound agonist effect
  24. Butorphanol (Nasal Spray)
    • opioid partial agonist
    • SAR: cyclobutyl
  25. Pentazocine
    • opioid partial agoinst
    • SAR: allyl
  26. Buprenoprphine
    • opiod partial agonist
    • SAR: cyclopropyl
  27. Nalbuphine
    • mixed opioid agonist/antagonist
    • Rx but not controlled substance
    • SAR: cyclobutyo
  28. Opioid antagonist
    treat opioid/ethanol dependence, opioid OD
  29. Naolxone (Suboxone)
    • opioid antagonist
    • SAR: allyl
    • when combined partial agonist = REWARD
  30. Naltrexone (vivitol)
    • opioid antagoninst
    • SAR: cyclopropyl
    • tx: opioid addiction, alcoholism
  31. Morphine and Fentanyl
    opioid agonists
  32. Endorphins
    • endogenous opioid (morphine)
    • beta-endorphins --- jogger high
  33. Opioid PD
    • receptors agonists produce presyntaptic inhibitory effects on the excitatory neurons
    • chronic use leads to addiction/tolerance:
    • 1. increase adenylate cyclase
    • 2. opioid can change affinity through internalization
    • withdrawal: cAMP accumulation

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