Alpha-methyldopa, produced in vivo metabolite α- methyl demethylation norepinephrine, blocking the central α receptor, thereby inhibiting the heart, kidney and peripheral vascular sympathetic impulse output, at the same time, peripheral vascular resistance and renal plasma prime activity also decreased blood pressure and thus lowered.
Indefinite oral absorption of about 50%. And plasma protein binding and less, only less than 20%. Metabolized in the liver to produce the active metabolite of α-methyl-noradrenaline. After a single oral dose of 4 to 6 hours and reached the peak antihypertensive effect, which lasted for 12 to 24 hours; after repeated oral administration of 2 to 3 days antihypertensive effect reached the peak, which lasted for 24 to 48 hours after treatment. Normal half-life of 1.7 hours, no urine was 3.6 hours. By renal excretion, absorption of the drug for 70% of the prototype and a few metabolites from the urine. Blood or peritoneal dialysis can remove the product.
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