The antihypertensive effect of methyldopa is believed to be due to its metabolism to α-

methylnorepinephrine, which then lowers arterial pressure by:

false neurotransmission (by replacing vesicular norepinephrine with α-methylnorepinephrine)

activation of presynaptic α2 receptors in the brainstem reduces sympathetic outflow, lowering blood
pressure (similar to clonidine)

reduction of plasma renin activity