Pharm Chem Exam 1 Part 2

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crmozingo
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Pharm Chem Exam 1 Part 2
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2012-01-27 12:23:02
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Pharm Chem Exam 1 Part 2
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  1. Neuropathology of Schizophrenia
    hyperdopaminergic theory: too much DA release or too many DA receptors = disinhibition of GABA = psychosis

    hypoglutamatergic theory: too little DA = disinhibition of GABA = psychosis

    increased DA hyperpolarizes GABA = psychosis
  2. Antipsychotics / DA antagonists - first generation
    • -neuroleptics
    • -EPS/TD (extrapyramidal SE/Tardive dyskinesia)
    • -3 penothiazine sub-types: aliphatic, piperidine, piperazine
    • -bind to DA receptor preventing conformation change

    **superimpose DA on commone phenothiazine pharmacophore**
  3. Chlorpromazine
    • -aliphatic 1G antipychotic
    • -low potency
    • -hydroxylated by 3A4, the metabolite then accumulates in the BBB
    • -can induce itself
    • -drug metabolism can cause psychosis to resume over time requiring an increase in dose
  4. Thioridazine
    • piperidine 1G antipsychotic
    • intermediate potency -- "dirty"
    • anti-ACh
    • metabolized by 2D6 adds another chiral center onthe sulfoxide creating 4 enantiomers
    • propranolol taken at the same time can increase the concentration of both drugs because they are both subject to glucoronidation
  5. Fluphenazine
    • piperazine 1G antipsychotic
    • high potency
    • free alcohol
    • forces compliance (IM)
    • metabolized by CE2
  6. Perphenazine
    • piperazine 1G antipsychotic
    • CATIE found it to be equally effective as new meds
    • smoking induces metabolism (1A2)
    • African Americns metabolize it quicker than whites
  7. Promethazine (fenergan)
    • non-neuroleptic phenothiazine
    • 2 carbon link between ring and aliphatic nitrogen so it is not as antidopaminergic vs 3 carbon link of chlorpromazine (sim structure) but potent muscarinic blocking agent
    • anticholinergic
    • Tx: motion sickness
  8. Haloperidol
    • butyrophenone
    • PO: alcohol
    • IM: prodrug (decanoate) - ester hydrolyzed to alcohol
    • **superimposes on designer drug MPTP-to-MPP
  9. Neurtotoxicology of chronic 1G antiphsychotics:
    extrapyramidal SE -- tardive dyskinesia theories:

    1. upregulation of DA receptors (why dose has to be increased over time)

    2. D1 and D2 recrptors (decoupling/separate)
  10. Tx: ESP/TD
    • 1. escalate dose and/or
    • 2. anticholinergic
    • or adminster 2 or 3G antipsychotics
  11. Benztropine
    • anticholinergic
    • atropine derivative
  12. 2G Antipsychotics
    • reduce EPS/TD
    • Tx: "positive" Sx (hallucinations) or "negative" Sx (anhedonia, social withdrawal)
  13. Clozapine
    • earliest 2G
    • SE: agranulocytosis (decrease leukocytes, require blood work-- decreases compliance) and hyperlipidemia
    • N-desmethyl -- new drug
    • reduced efficacy (D/M)
  14. Olanzapine
    • best tolerated 2G antipsychotic (less SEs)
    • IM
    • no agranulocytosis
    • thio-isostere of clozapine
    • if this does not work, switch to clozapine
    • new
  15. Symbyax
    combination product of fluoxetine and olanzapine
  16. Risperidone
    • 2G antipsychotic
    • long-acting IM
    • Paliperidone is the 9-OH metabolite (pre-metabolized)
    • 2D6 metabolism
  17. Paliperidone
    • antispychotic
    • "son of Risperiodne"
    • "pre-metabolized" (not subject to 2D6 polymorphism)
    • atypical
    • heterologous expresssion because it is polymorphic
  18. Quetiapine
    • 2G antipsychotic
    • XR (increases compliance, tid to qd)
    • only 3A4 substrate
    • no DDIs
  19. Ziprasidone
    • 2G antipsychotic
    • highest level of 5-HT blockade (characteristic of 2G)
    • not metabolized by CYPs therefore no DDIs
    • metabolized by aldehyde oxidase (AO)
  20. Aldehyde Oxidase (AO)
    • no PGx polymorphism (no CYPs)
    • hypatic cytosol
    • uses molybdenum cofactor
  21. Asenapine
    • 2G antipsychotic
    • sub-lingual (rapid onset of action)
    • dopaminergic and serotonergic blockade
  22. 3G Antipsychotics
    • atypical
    • further reduce EPS/TD
    • partial agonists
  23. Aripiprazole (Ambilify)
    • 3G antipsychotic
    • partial dopamine agonist
    • sertonin antagonist
  24. Nomenclatures for DA receptor subtypes
    • -biochemical
    • 1. D1-like (increases cAMP)
    • 2. D2-like (decreases cAMP or no effect)

    • -molecular biology subtyping
    • -D1-like (includes D1 and D5)
    • -D2-like (includes D2,D3,D4)
  25. Neurochemical basis for atypicality
    high D2-like low 5-HT = 1G (Haloperidol)

    low D2-like high 5-HT = 2/3G (Clozapine)

    high D2-like high 5-HT = 2/3G (Risperidone,Olanzapine)

    high 5-HT: more likely for 2/3G increases efficacy, decreases SE (EPS/TD)
  26. Serotonin
    • presynaptically inhibits DA
    • Serotonin antagonists: increase the amounts of DA
    • Theory: sclutping the extent of DA antagonism
    • 5-HT influences DA release

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