Reserpine (Adrenergic Neuron Blocker) 
  • Reserpine inhibits the function of postganglionic adrenergic neurons, thus inhibiting sympathetic function.
  • Reserpine binds to noradrenergic storage vesicles in central and peripheral sympathetic nerve terminals.
    • Storage vesicles become nonfunctional as a result of interacting with reserpine and lose the ability to store and concentrate norepinephrine (N.E.) and dopamine.
    • N.E. and dopamine leaking from vesicles are enzymatically destroyed in the cytoplasm and as a consequence little transmitter is released upon nerve ending depolarization.
  • Depletion of transmitter in both the central and peripheral nervous system suggest that both sites by be important mediators of the antihypertensive response.
  • Chronic adrenergic neuronal blockade by reserpine results in a reduction of cardiac output and peripheral vascular resistance.

 

Adverse Effect
  • CNS effects predominate, including sedation, inability to concentrate, and depression.