Source: Υπουργείο Υγείας (CY) Revision Year: 2015 Publisher: MEDOCHEMIE LTD, 1-10 Constantinoupoleos street, 3011 Limassol, Cyprus
Pharmacoterapeutic group: Antiadrenergic agents, centrally acting
ATC code: C02AB01
It appears that several mechanisms of action account for the clinically useful effects of methyldopa and the current generally accepted view is that its principal action is on the central nervous system.
The antihypertensive effect of methyldopa is probably doe to its metabolism to alpha-methylnoradrenaline, which lowers arterial pressure by stimulation of central inhibitory alpha-adrenergic receptors, false neutrotransmission, and/or reduction of plasma rennin activity. Methyldopa has been shown to cause a net reduction in the tissue concentration of serotonin, dopamine, epinephrine (adrenaline) and norepinephrine (noradrenaline).
Absorption of oral methyldopa is variable and incomplete. Bioavailability after oral administration averages around 25%. Peak concentrations in plasma occur at two to three hours, and elimination of the drug is biphasic regardless of the route of administration. Plasma half-life is 1.8 ± 0.2 hours. Renal excretion accounts for about two thirds of drug clearance from plasma.
No relevant information.
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