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
Pregnancy
category
  • a drug of choice in PIH
Routes of
administration
Oral, IV
Legal status
Legal status
  • ℞ (Prescription only)
Pharmacokinetic data
Bioavailability approximately 50%
Metabolism Hepatic
Biological half-life 105 minutes
Excretion Renal for metabolites
Identifiers
CAS Number 555-30-6
ATC code C02AB01 (WHO)
PubChem CID 4138
DrugBank APRD01106
Chemical data
Formula C10H13NO4
Molar mass 211.215 g/mol[[Script error: No such module "String".]]
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Methyldopa (L-α-Methyl-3,4-dihydroxyphenylalanine; 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)).

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

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