H1 antagonist

• If BBB-crossing:
• Sedation
• Weight gain (↑ intake, ↓ expenditure, ↑ fat storage)
• Anxiolytic and antiemetic effects
• ↓ seizure threshold
• Anti-allergy effects

H1 antagonist (1/2)

• The principal mechanism of sedation by antidepressants/antipsychotics
• ➔ act at hypothalamus and cerebral cortex
• ➔ suppress the histamine-mediated wakefulness network
• The single strongest predictor of weight gain across antipsychotic and antidepressant classes
• ➔ at least 3 converging mechanisms ◇ increased caloric intake ◇ reduced energy expenditure ◇ enhanced fat storage.
• Decreased allergic response
• ➔ reduced inflammatory mediator release
• ➔ decreased vascular permeability
• Anxiolytic effects

H1 antagonist (2/2)

• Antiemetic effects
• ↓ seizure threshold

Drugs with this mechanism (97)

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