Last reviewed 01/2018

Centrally acting antihypertensives reduce arteriolar muscular tone by reducing sympathetic activity.

First generation drugs, such as clonidine and methydopa, act as alpha-2 adrenoceptor agonists resulting in inhibition of the sympathetic nuclei in the rostroventrolateral medulla. Side-effects of these agents preclude their widespread use as first line hypertensive agents.

A second generation centrally-acting antihypertensive was subsequently introduced

  • Moxonidine is an agonist at the imidazoline I1 receptor
    • the I1 receptor is found in the rostroventrallateral medulla and in the kidney
    • stimulation of I1 results in reduced sympathetic tone and a lowering of blood pressure

The summary of product characteristics should be consulted before prescribing this drug.