Chemical formula: C₁₀H₁₃NO₄ Molecular mass: 211.215 g/mol PubChem compound: 38853
Methyldopa is an antihypertensive agent acting centrally by stimulating alpha adrenergic receptors. It inhibits the decarboxylation of dopa to dopamine but this action is not responsible for the hypotensive effect. It is suggested that a metabolite, alpha methylnoradrenaline may act as a false transmitter in the CNS. It reduces tissue concentration of dopamine noradrenaline, adrenaline and serotonin.
Methyldopa is incompletely absorbed from the gastrointestinal tract. Methyldopa is extensively metabolised through pathways common to the catecholamines utilising dopa decarboxylates and dopamine B-hydroxylase.
Decarboxylation is stereospecific. The bioavailability of an oral dose averages 25% (±16%) and peak plasma levels occur 2 to 3 hours later. Elimination is biphasic. It is partly conjugated mainly to the o-sulphate and is excreted by the kidneys.
The elimination half-life is 1.8 ± 0.2 hours, methyldopa has been shown to cross the placental barrier and is found in the lungs, heart and muscles after 24 hours, detectable quantities are present in the liver and kidneys.
None.
© All content on this website, including data entry, data processing, decision support tools, "RxReasoner" logo and graphics, is the intellectual property of RxReasoner and is protected by copyright laws. Unauthorized reproduction or distribution of any part of this content without explicit written permission from RxReasoner is strictly prohibited. Any third-party content used on this site is acknowledged and utilized under fair use principles.
