Pharm Test 4: Antipsychotic Agents, Lithium

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BrookeNH10
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201223
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Pharm Test 4: Antipsychotic Agents, Lithium
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2013-02-17 16:03:24
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Pharm Test Antipsychotic Agents Lithium
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Pharm Test 4 Antipsychotic Agents, Lithium
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  1. Dopamine Hypothesis (of Schizophrenia)
    Disorder caused by excess functional activity of DA in brain

    • Based on:
    • 1)  Many antipsychotic drugs block DA receptors (esp. D2)
    • 2)  DA agonist drugs (amphetamine, levadopa) exacerbate schizophrenia
    • 3)  Increased density of DA receptors has been detected in certain brain regions of untreated schizos.

    *Not fully satisfactory b/c antipsychotic drugs are only partially effective and other effective drugs have a higher affinity for other (including 5-HT) receptors.
  2. Blockage of D2 receptors causes
    Extrapyramidal symptoms (Parkinson-like symptoms)
  3. Involuntary movement of the tongue, lips, neck, trunk and limbs.  Tx?
    Tardive dyskinesia

    Tx= Increased antipsychotic drug dose (results in DA sensitization)
  4. D2 receptor type
    G-coupled receptor (inhibitory)

    *GI receptor:  Inhibts due to blockage of ACh, cAMP/PKA pathway
  5. Name the Typical Antipsychotics
    • Phenothiazines- Chloropromazine, Fluphenazine, Tifluperazine
    • Thioxanthanes- Thioridazine
    • Butyrophenones- Haloperidol
  6. Muscular rigidity, fever, altered mental status and stupor, impairment of sweating, unstable BP, and myoglobinemia
    Neuroleptic Syndrome

    *Can be fatal
  7. Neuroleptic Syndrome tx
    • Withdraw drug immediately
    • Administer either:
    • Dantrolene
    • Bromocriptine
    • Diazepam
    • DA Agonist
  8. All antipsychotics block A1 and H1 receptor to some extent except
    Haloperidol (doesn't block H1, but still blocks A1)
  9. New Age Antipsychotic drugs act on
    5-HT2 receptors
  10. Name the New Age Antipsychotic drugs
    • Clozapine
    • Olanzapine
    • Quetiapine
    • Risperidone
    • Zipasidone
  11. Side effects of New Age Antipsychotics
    • Endocrine and metabolic changes
    • Obesity
    • Diabetes
    • Prolactin Release
  12. Most prominent for elevated prolactin levels
    Risperidine
  13. Most prominent drugs for weight gain and hyperglycemia side effects
    • Clozapine
    • Olanzapine
  14. New antipsychotic that can be used in pregnant women
    Olanzapine
  15. Reserved for tx-resistant schizophrenia
    Clozapine
  16. Causes hematotoxicity (agranulocytosis)
    Clozapine
  17. Clozapine side effect
    Hematotoxicity
  18. Side effects of this drug include gynecomastia, amenorrhea-galactorrhea syndrome, infertility
    Risperidone (due to elevated prolactin levels)
  19. Two drugs that have QT prolongation and can produce Torsades de Pointes
    • Ziprasidone
    • Quetiapine
  20. Quietiapine treats
    • Schizo
    • Bipolar
    • MDD
  21. Lithium is affective for what phase of bipolar disorder
    Manic
  22. Disadvantage of lithium
    slow-onset
  23. Lithium:  MoA
    Inhibits the Phosphoinositol 2nd messenger cascade
  24. Lithium:  Metabolism
    • Excreted almost entirely in the urine
    • Clearance Reduced by:  Diuretics, NSAIDs, ACE inhibitors, Metronidazole (Ribosomal and  Mitochondrial DNA)
    • Clearance increased by: Acetazolamide, Alkalinizing agents, Urea, Xanthen preparations (including caffeine)
  25. Lithium:  Adverse Effects
    • Reversible Nephrogenic Diabetes Insipidus
    • Thyroid Enlargment
    • Ebstein's Anomaly in babies of nursing mothers
  26. Effective in lithium non-responders (now becoming 1st choice drug for BPD in the US)
    Valproate
  27. Used in maintenance tx of bipolar disorder and can cause Stevens-Johnson Syndrome
    Lamotrigine

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