Pharm Chem Exam 1 Part 3

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crmozingo
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131004
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Pharm Chem Exam 1 Part 3
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2012-01-27 13:51:18
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Pharm Chem Exam 1 Part 3
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  1. Major Depression
    • 20% population
    • women > men
    • central dogma theory: imbalance between 5-HT and NE
    • serotonin biomarker: 5-HIAA (catabolite)
    • NE biomarker: MHPG
    • HVA and DOPAC increase postmortem schiz
  2. Tricyclic Antidepressants
    • 1G ADs
    • 3rd line agents

    • "dirty": (especially tertiary amines)
    • anticholinergic
    • antihistaminic SE (drowsiness)
    • anti-alpha-adrenergic activity (CV effects)
  3. Imipramine (Tofranil)
    • prototype 1G TCA
    • inhibits NE transporter and SERT (5-HT transproter)
    • increases tone for acute; chronic decreases efficacy
    • polymorphic
    • tertiary amine (dirty) influences 5-HT more than NE but when you hydroxylate it, it becomes a secondary amine (Desipramine) which is more effective on NE
  4. Desipramine
    • 1G TCA
    • secondary amine - therefore more effective on NE vs 5-HT
  5. Amitriptyline
    • 1G TCA
    • carbon isostere of imipramine
    • demethylated to form nortryptyline
    • tertiary amine - more effective on 5-HT
  6. Nortryptyline
    • pre-metabolized form of amiriptyline
    • secondary amine - more effective on NE
  7. Cyclobenzaprine
    • NOT TCA, muslce relaxant
    • alkene isostere of amitriptyline
  8. Clomipramine (Anafranil)
    • 1G TCA
    • Tx: OCD
    • N-demethylated to norclomipramine (metabolized from tertiary to secondary)
  9. Doxepin (Sinequan)
    • 1G TCA
    • oxygen isostere of amitriptyline
    • racemic (trans predominate)
    • cis and trans have opposite affects on CNS
  10. Buproprion (Wellbutrin)
    • 2G TCA
    • only AD acting on the DA synapse
    • autoinduction
    • smoking cessation
    • metabolized 2B6
  11. CYP2B6
    • rare and inducible
    • prototype substrate is Bupropion and nicotine
  12. CYP2A6
    • rare
    • metabolizes nicotine forming nornicotine
    • inducible by nicotine
    • nonpolymorphic
  13. Amoxapine (Asendin)
    • 2G AD
    • only AD associated with EPS, therefore not used
    • NOTE: Amoxapine = N-desmethyl-loxapine
  14. Loxapine (Loxitane)
    • 2G AD
    • has EPS SEs
  15. Trazodone (Desryl)
    Last 2G AD
  16. 3G AD
    5-HT selective reuptake inhibitors (SSRIs)
  17. Fluoxetine (Prozac)
    • 3G SSRI
    • racemic - S is more active than R
    • sympathomimetic SE
    • morning dosing
    • **no MAOIs for weeks after discontinuation because the half life is 7-15 days and MAOIs have many DDIs**
    • **F-unk : FDA will not allow IV administration**
    • metabolized 2D6, 3A4
  18. (R)-Fluoxetine
    less active but eliminates polymorphism from S-form being metabolized by 2D6
  19. Paroxetine (Paxil)
    • 3G SSRI
    • potent 2D6 inhibitor and substrate
  20. Sertraline (Zoloft)
    • 3G SSRI
    • not a potent @2D6 inhibitor
    • Tx: Post traumatic stress disorder (PTSD)
  21. Citalopram (Celexa)
    • 3G SSRI
    • SERT blockade
  22. SSRI
    inhibit the reuptake of serotonin more than NE
  23. Escitalopram (Lexapro)
    • 3G SSRI
    • racemic switch allowing for lower dosing = more effective
    • R isomer antagonizes the effects of the S isomer
    • *S-isomer*
  24. Vilazodone (Viibryd)
    • 3G SSRI and serotonin partial agonist (post synaptic agonist activity)
    • partial agonist increases 5-HT tone
    • contains cyano group
  25. Fluvoxamine (generic)
    • prototype 1A2 inhibitor
    • smokers require higher dose
  26. St. John's Wort
    • miscellaneous AD
    • contains hypericin
    • allows the antidepressant endobiotic to breach BBB because it contains a Pgp inhibitor
    • PD: unknown
  27. Dual Action AD
    • act at both 5-HT and NE reuptake inhibitors
    • used for those that are nonresponsive to SSRI
  28. Venlafaxine (Effexor)
    • Dual Action AD
    • "Prozac with a boost"
    • Tx: refractory depression
  29. Desvenlafaxine (Pristiq)
    • Dual action AD
    • decreased 2D6 metabolism therefore decreases DDI and polymorphism
    • "premetabolized" form of Venlafaxine (hydroxyl group in place of the ether group)
  30. Nefazodone (Serzone)
    • Dual action AD
    • 3A4 DDI
    • reduces sexual dysfunction (common SE of ADs)
    • forms toxic metabolite (serotonin syndrome)
  31. Duloxetine (Cymbalta)
    • Dual action AD
    • Tx: stress urinary incontinence (women)
  32. Mirtazapine (Remeron)
    • Dual action AD
    • less sexual dysfunction/less GI SEs
    • sex dimorphism (women>men) because
    • more Pgp in men or more 3A4 in women
    • ---paradox
  33. Antidepressant PD
    • 1. acute Tx increases 5-HT and NE through inhibiton of SERT and NET
    • 2. chronic Tx decreases beta-NE and 5-HT
    • 3. upregualtes cAMP through inhibition of PDE (phosphodiesterase)
    • 4. equanimity
  34. 5-HT 1A receptor
    most closely associated with depression
  35. Monoamine oxidase inhibitors (MAOIs)
    • more DDI than any other drug types
    • two types: MAO-A and MAO-B
    • MAO-A: depression
    • MAO-B: dopamine
  36. Phenelzine (Nardil)
    • MAOI
    • irreversible suicide inhibitor of MAO-A
    • N-acetylated
    • many DDI that occur long after therapy is discontinued
    • Ex: Norfluoxetine --- CVA
  37. Acetylator polymorphs
    • 2 types of N-acetyltransferases: NAT1 and NAT2
    • NAT2: trimodal, prototype substrate: isoniazid, increases SLE
  38. Tranylcypromine (Parnate)
    • MAO-A I
    • trans-substituted cyclopropane
    • cyclized amphetamine - produces amphetamine-like effects
    • competitive/reversible inhibitor of MAO-A therefore it is safer -- "less cheese effect"
  39. "Cheese Effect"
    • phenelzine or tranylcypromine (MAO-A Is) which increase tyramine bioavailabilty
    • tyramine is found in putrefaction products (wine, cheese, and escargo)
    • tyramine being hydroxylated to octopamine within NE vesicles displaces NE which leads to CVA
  40. MAO expression
    proximal to distal
  41. Selegiline (Eldepryl)
    • MAO-B inhibitor
    • Tx: Parkinson's Disease
    • suicide inhibitor
    • phenethylamine pharmacophore

    • works by
    • 1. preserves limited amounts of DA
    • 2. induces superoxid dismutase (SD) (neuroprotectant)
    • 3. induces catalase reduces hydrogen peroxide (Neuroprotectant)
  42. Rasagiline (Azilect)
    • 2G MAO-B I
    • increase potency and decreases pressor effect
    • due to no pehnethylamine pharmacophore as with Selegiline
    • Tx: monotherapy Parkinson's disease
    • aminoindane with cyano group
  43. Lithium
    • Tx: Bipolar/Manic
    • found in Perrier
    • narrow NTI and implications for generic substitution
    • regulation of sodium intake: increased sodium decreased lithium reabsorption --- underdosage, subtherapeutic effect
    • lithium interrupts inositol recycling by inhibiting phosphatase (AKA: inhibiting dephosphorylation) and increasing refractory time

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