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.
