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PHARMACEUTICAL LIBRARY

Pk and Pd of neuroleptics

PHARMACOKINETICS OF NEUROLEPTICS

  • ADMINISTRATION: per os
  • ½♥: 20-40 hrs
  • PLASMA PROTEIN BINDIGN: 70%
  • REACHES CNS: 30 MINS/ 1 HRS (HIGH LIPOSOLUBIILTY)
  • HEPATIC METABOLISM: CYP2D6

PHARMACODYNAMIC OF NEUROLEPTICS

Neuroleptics block D2 receptors in the mesolimbic system, so they are effective on positive symptoms, and not on negative and cognitive symptoms.

  • Block D2 receptors in the nigrostriatal system (NSc) (With extrapyramidal side effects and tardive diskinesias).
  • Block D2 receptors in the tuber-infundibular system (Hyperprolactinemia with sexual disfunctions and osteoporosis).
  • Block D2 receptors in the mesocortical system (Inducing or worsening negative symptoms).
  • Block α1 receptors (Causing dizziness sedation and orthostatic hypotension).
  • Block M receptors (Causing loss of memory, xerostomy, blurred vision, constipation and urinary retention).
  • Block H1 receptors (Causing sedation and weight gain).
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