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Methyldopa

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Methyldopa
File:(S)-Methyldopa Structural Formulae V.1.svg
Systematic (IUPAC) name
(S)-2-amino-3-(3,4-dihydroxyphenyl)-2-methyl-propanoic acid
Clinical data
AHFS/Drugs.com monograph
MedlinePlus a682242
  • AU: A
  • US: B (No risk in non-human studies)
Oral, IV
Pharmacokinetic data
Bioavailability approximately 50%
Metabolism Hepatic
Half-life 105 minutes
Excretion Renal for metabolites
Identifiers
555-30-6 7pxY
C02AB01
C02AB02 (racemic)
PubChem CID 38853
DrugBank DB00968 7pxY
ChemSpider 35562 7pxN
UNII 56LH93261Y 7pxY
ChEMBL CHEMBL459 7pxN
Chemical data
Formula C10H13NO4
211.215 g/mol
 14pxN (what is this?)  (verify)

Methyldopa (L-α-Methyl-3,4-dihydroxyphenylalanine; Aldomet, Aldoril, Dopamet, Dopegyt, etc.) is an alpha-adrenergic agonist (selective for α2-adrenergic receptors) psychoactive drug used as a sympatholytic or antihypertensive. Its use is now mostly deprecated following the introduction of alternative safer classes of agents. However, it continues to have a role in otherwise difficult to treat hypertension and gestational hypertension (previously known as pregnancy-induced hypertension (PIH)).

It is on the World Health Organization's List of Essential Medicines, a list of the most important medication needed in a basic health system.[1]

Medical uses

Methyldopa is used in the clinical treatment of the following disorders:

Side effects

Methyldopa is capable of inducing a number of adverse side effects, which range from mild to severe. Nevertheless, they are generally mild when the dose is less than 1 gram per day.[2] Side effects may include:

Rebound/withdrawal

Rebound hypertension via withdrawal on account of tolerance upon the abrupt discontinuation of methyldopa has been reported.[3]

See also

Mechanism of Action

Methyldopa has a dual mechanism of action:

Pharmacokinetics

Methyldopa exhibits variable absorption from the gastrointestinal tract. It is metabolized in the liver and intestines and is excreted in urine.

History

When methyldopa was first introduced, it was the mainstay of antihypertensive treatment, but its use has declined on account of relatively severe adverse side effects, with increased use of other safer and more tolerable agents such as alpha blockers, beta blockers, and calcium channel blockers. Nonetheless, one of methyldopa's still current indications is in the management of pregnancy-induced hypertension (PIH), as it is relatively safe in pregnancy compared to many other antihypertensives which may affect the fetus.

References

  1. "WHO Model List of EssentialMedicines" (PDF). World Health Organization. October 2013. Retrieved 22 April 2014. 
  2. British National Formulary 56. September 2008. pp. 95–96. ISBN 978-0-85369-778-7. 
  3. Methyldopa (PIM 342)