Methyldopa: Wikis

  

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Methyldopa
Systematic (IUPAC) name
(S)-2-amino-3-(3,4-dihydroxyphenyl)-2-methyl-propanoic acid
Identifiers
CAS number 555-30-6
ATC code C02AB01
PubChem 4138
DrugBank APRD01106
Chemical data
Formula C 10H13NO4  
Mol. mass 211.215 g/mol
Pharmacokinetic data
Bioavailability approximately 50%
Metabolism Hepatic
Half life 105 minutes
Excretion Renal for metabolites
Therapeutic considerations
Pregnancy cat. a drug of choice in PIH
Legal status Prescription only
Routes Oral, IV
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Methyldopa (L-α-Methyl-3,4-dihydr oxyphenylalanine; Aldomet, Aldoril, Dopamet, Dopegyt, etc) is a psychoactive drug used as a sympatholytic or antihypertensive. Its use is now deprecated following introduction of alternative safer classes of agents. However, it continues to have a role in otherwise difficult to treat hypertension and gestational hypertension (also known as pregnancy-induced hypertension (PIH)).

Contents

Indications

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

Pharmacology

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.

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.[1] Side effects may include:

Rebound/withdrawal

Rebound hypertension via withdrawal on account of tolerance upon the abrupt discontinuation of methyldopa has been reported.[2]

See also

  • D-DOPA (Dextrodopa)
  • L-DOPA (Levodopa; Sinemet, Parcopa, Atamet, Stalevo, Madopar, Prolopa, etc)
  • L-DOPS (Droxidopa)
  • Dopamine (Intropan, Inovan, Revivan, Rivimine, Dopastat, Dynatra, etc)
  • Norepinephrine (Noradrenaline; Levophed, etc)
  • Epinephrine (Adrenaline; Adrenalin, EpiPed, Twinject, etc)

References

  1. ^ British National Formulary 56. September 2008. p. 95–96. ISBN 978-0-85369-778-7.  
  2. ^ Methyldopa (PIM 342)







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