Centrally acting antihypertensive drugs & Adrenergic Neuron Blockers

  • Adrenergic neurone blocking action by preventing the granular uptake of catecholamines where it stays outside the granules (in the cytoplasm) to be inactivated by MAO enzyme.
  • Parasympathomimetic action.

The hypotension effect is due to:

  • Adrenergic neurone blocking action.
  • Central action (inhibition of VMC and tranquilization)
  • Depletion of suprarenal medulla.

Adverse Effects:

  1. Bradycardia, flushing and nasal stuffiness. (parasympathetic actions due lost sympathetic)
  2. Hyperacidity, peptic ulceration, salivation and diarrhea.
  3. Loss of libido and impotence in males.
  4. Salt and water retention.
  5. Psychic depression (Due to deficient norepinephrine) , suicidal attempts, parkinsonian-like rigidity and nightmares, cancer breast.
Uses :
  • Less common nowadays due its side effects.
  • Not alone but as part of combination therapy for treatment of hypertension.