Pharmacological properties of the central antihypertensive agent, moxonidine

Cardiovasc Ther. 2012 Aug;30(4):199-208. doi: 10.1111/j.1755-5922.2011.00268.x. Epub 2011 Apr 5.


The sympathetic nervous system plays a central role in the pathophysiology not only of hypertension and other cardiovascular diseases but also metabolic disorders including disturbances of glucose and lipid homeostasis. A centrally acting sympathetic agent is therefore attractive not only for lowering blood pressure, but also intervening with multiple disease processes. Older agents such as clonidine and guanabenz have numerous side effects, including sedation and dry mouth that limit their acceptability to patients. Moxonidine and the related agent rilmenidine have greatly reduced side effects, because they have reduced activity at the α(2) -adrenergic receptors that mediate these undesirable actions. Instead, moxonidine and rilmenidine act primarily through a novel cellular site, termed the I(1) -imidazoline receptor. The molecular biology of the I(1) -imidazoline receptor protein has recently been described, and the cell signaling pathways linked to this protein have been characterized. Moxonidine has unique effects on a number of cell types through this unusual cellular site of action. There are multiple therapeutic implications of these cellular actions, especially for metabolic syndrome and its associated derangements in glucose and lipid metabolism. Finally, the clinical trials that seemed to identify an unfavorable outcome in severe heart failure are dissected and critiqued. We conclude that moxonidine and future successors to this agent could be of great value in treating multiple chronic diseases.

Publication types

  • Review

MeSH terms

  • Animals
  • Antihypertensive Agents / adverse effects
  • Antihypertensive Agents / therapeutic use*
  • Blood Pressure / drug effects*
  • Central Nervous System / drug effects*
  • Central Nervous System / physiopathology
  • Heart Failure / drug therapy
  • Humans
  • Hypertension / drug therapy*
  • Hypertension / physiopathology
  • Imidazoles / therapeutic use*
  • Insulin Resistance
  • Metabolic Syndrome / drug therapy
  • Sympathetic Nervous System / drug effects*
  • Sympathetic Nervous System / physiopathology
  • Sympatholytics / adverse effects
  • Sympatholytics / therapeutic use*
  • Treatment Outcome


  • Antihypertensive Agents
  • Imidazoles
  • Sympatholytics
  • moxonidine