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Methyldopa


Mechanism of action:

Methyldopa is an α₂-adrenergic agonist. Methyldopa is a prodrug that, after entering the central nervous system, is converted by aromatic L-amino acid decarboxylase and dopamine β-hydroxylase into the active compound α-methylnorepinephrine. α-Methylnorepinephrine stimulates α₂-adrenergic receptors in the brainstem, particularly in the medullary vasomotor center, suppressing central sympathetic outflow and thereby reducing peripheral vascular resistance, heart rate, and cardiac output.

Reference(s):

1. Mah GT et al. (2009). Methyldopa for primary hypertension. Cochrane Database Syst Rev. 


2. Sica DA et al. (2007). Centrally acting antihypertensive agents: an update. J Clin Hypertens (Greenwich). 


3. van Zwieten PA et al. (1980). Pharmacology of centrally acting hypotensive drugs. Br J Clin Pharmacol.

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