Moxonidine: some controversy

Expert Opinion on Pharmacotherapy
S A Doggrell

Abstract

Initially it was considered that moxonidine, like clonidine, acted at central (2)-adrenoceptors to reduce blood pressure. With the characterisation of imidazoline binding sites distinct from (2)-adrenoceptors, the consensus became that moxonidine was acting predominantly at imidazoline I(1) receptors in the rostral ventrolateral medulla to lower blood pressure. Moxonidine acts at prejunctional (2)-adrenoceptors on sympathetic nerve endings to decrease noradrenaline release and this may contribute to its ability to lower blood pressure. The predominant site of action of moxonidine may also depend on route of administration, with imidazoline I(1) receptors being predominant after central, and (2)-adrenoceptors predominant after systemic administration. The controversy over the mechanism and site of action with moxonidine is ongoing. In animal models, moxonidine lowers blood pressure, reduces cardiac hypertrophy and remodelling, reduces cardiac arrhythmias and increases blood flow in cerebral ischaemia. Moxonidine also has beneficial effects in animal models of diabetes and kidney disease. Moxonidine increases sodium and water excretion in rats, but not humans. Animal studies indicate that moxonidine may be useful in the treatment...Continue Reading

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Citations

Dec 10, 2003·Expert Opinion on Emerging Drugs·J A Whitworth
Mar 20, 2014·European Journal of Heart Failure·Michael BöhmFelix Mahfoud
Sep 27, 2005·Autonomic Neuroscience : Basic & Clinical·Kevin L WingerdDennis O Clegg
Apr 2, 2003·Circulation·T Douglas Bradley, John S Floras

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