One liners about Antipsychotics


Mechanism of typical vs atypical antipsychotics:

One liners:

  1. D2 receptor antagonism is responsible for antipsychotic action of typical antipsychotics
  2. Typical antipsychotics cause more extrapyramidal side effects but less metabolic side effects
  3. Extrapyramidal side effects (EPSE):
    • First EPSE to develop: Acute muscular dystonia (Rx: IV Promethazine)
    • MC EPSE: Akathisia (inner restlessness), Rx: Propranolol
    • Pseudoparkinsonism:
      • Tremor, salivation, bradycardia
      • Can be mistaken as negative symptoms of parkinsonism
      • Rx: Anticholinergics.
    • Neuroleptic malignant syndrome:
      • Fever + tachycardia + leukocytosis + rigidity + elevated CPK +
        fluctuating BP + confusion
      • Pathophysiology: Blockade of dopamine receptors induce massive glutamate release; generating catatonia, neurotoxicity and myotoxicity
      • DOC: Dantrolene.
    • Tardive dyskinesia:
      • Tardive = Slow, Dyskinesia = Abnormal movement
      • Extrapyramidal symptom due to long term use of typical antipsychotics drugs (Ex: Haloperidol)
      • Cause: Supersensitivity of dopamine receptors
      • Clozapine is DOC for replacement (of haloperidol)
      • Clozapine is also the most effective treatment of tardive dyskinesia
      • DOC for tardive dyskinesia: VMAT inhibitors (dopamine depletors); Ex: Valbenazine & Tetrabenazine.
  4. 5HT2A antagonism is responsible for anti-psychotic action of atypical antipsychotics
  5. Atypical antipsychotics cause less extrapyramidal side effects but more metabolic side effects
  6. Metabolic side effects of atypical antipsychotics are due to 5HT2C antagonism
  7. Maximum metabolic side effects/ maximum weight gain: Clozapine > Olanzapine
  8. Antipsychotics not causing weight gain:
    a. Aripiprazole: Causes maximum akathisia
    b. Ziprasidone: Causes QT prolongation
    c. Asenapine: Sublingually given.
  9. Broadest action antipsychotic (acts on multiple receptors): Clozapine
  10. Drug having the potential of causing agranulocytosis (and thus requiring blood level monitoring): Clozapine
  11. Chlorpromazine causes corneal deposits and cholestatic jaundice
  12. Thioridazine causes retinal pigmentation
  13. Maximum hyperprolactinemia is caused by Risperidone > Olanzapine
  14. IV administration of Haloperidol can lead to sudden death due to cardiac arrhythmia.

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