Antipsychotics

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mp
ID:
205222
Filename:
Antipsychotics
Updated:
2013-03-05 19:53:25
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Pharmacology II Antipsychotics
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Antipsychotics
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  1. Phenothiazines -- Class of drugs (FGA)
    • Chlorpromazine (Thorazine)
    • Prochlorperazine (Compazine)
    • Thioridazine (Mellaril)
  2. CNS effects of Phenothiazines (FGA)
    • sedation
    • blockade of DA causing release of prolactin (hyperprolactinemia)
    • antiemetic effect -- action on CTZ
    • EPS -- iatro. parkinsonism, tardive dyskinesia, dystonias
  3. Tardive Dyskinesia -- different than other EPS
    • excess of DA activity
    • involuntary buccolingual-masticatory movements
    • D/C anticholinergics (need an increase of ACh)
  4. Peripheral effects of Phenothiazines
    • Alpha block, DA antagonism
    • anticholinergic effects
    • antihistamine effects
  5. Neuroleptic Malignant Syndrome (NMS)
    • muslce rigidity
    • fever
    • seizures
    • coma
    • respiratory and cardiac failure
    • Treatment:
    •      DA agonists -- bromocriptine
    •      direct skeletal muscle relaxant -- dantrolene
  6. Atypical Antipsychotic Agents (SGA)
    • Clozapine (Clozaril)
    • Risperidone (Risperdal)
    • Olanzapine (Zyprexa)
    • Quetiapine (Seroquel)
    • Ziprasidone (Geodon)
    • Aripiprazole (Abilify)
    • Paliperidone (Invega)
  7. Clozapine (Clozaril) -- Atypical
    • blockade of D4 over D2 so less EPS and 5HT2a receptors
    • also blocks alpha, muscarinic and histamine receptors
    • agranulocytosis in 1-3%
    • seizures in 3%
  8. Risperidone (Risperdal)
    • 5HT2a and D2 antagonist
    • also alpha, muscarinic and histamine receptors
    • claimed to decrease negative symptoms
  9. Olanzapine (Zyprexa)
    • 5HT2a and D 1,2,4 antagonist
    • also alpha, muscarinic and histamine receptors
    • both positive and negative symptoms
    • lower EPS SE and less CV rxn
  10. Quetiapine (Seroquel)
    • 5HT2a and D 1,2,4 antagonist
    • both positive and negative symptoms
    • lower EPS SE and less CV rxn
  11. Ziprasidone (Geodon)
    • blocks D2, 5HT2a, H1
    • schizophrenia and BPD
    • seldom causes wt gain, hyperlipidemia or hyperglycemia
    • QT interval and EPS in 5% of pts
  12. Aripiprazole (Abilify)
    • "DA stabilizer"
    • little/no effect on wt
    • schizophrenia, BPD and adjunct in depression
    • anxiety, HA, N, constipation, light headedness and akathisia
  13. Paliperidone (Invega)
    • active metabolite of risperidone
    • 5HT2a and D2 antagonist
    • claimed to decrease negative symptoms
  14. Schizophrenia Drug therapy
    • Most FGA and SGA (atypicals) are equally effective
    • except for clozapine, is more effective than the rest
    • FGAs -- significant risk of EPS
    • SGAs -- risk of metabolic effects (wt gain)
    • FGAs cost much less than SGAs

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