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.

Recently a second generation centrally-acting antihypertensive has been 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.