Methyldopa

Table of contents

  • Brand Names
  • Drug Combinations
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Aldometil; Belgium: Aldomet; Bulgaria: Dopegyt; Cyprus: Methyldopa; Czech Republic: Dopegyt; France: Aldomet; Germany: Dopegyt, Methyldopa, Presinol; Greece: Aldomet, Dopamed, Methyldopa; Hungary: Dopegyt; Italy: Aldomet; Latvia: Dopegyt; Lithuania: Dopegyt; Luxembourg: Aldomet; Malta: Methyldopa; Netherlands: Methyldopa; Poland: Dopegyt; Portugal: Aldomet; Romania: Dopegyt; Slovakia: Dopegyt; Spain: Aldomet; Sweden: Aldomet; UK: Aldomet, Methyldopa.

North America

Canada: Methyldopa, Novo-Medopa; USA: Methyldopa.

Latin America

Argentina: Aldomet, Metildopa; Brazil: Aldomet, Aldotensin, Alfusina, Angimet, Dimipress, Dopametil Alfusina, Ductomet, Etildopanan, Kindomet, Metildopa, Metil-DT, Metilpress, Metilprod, Tensioval, Tildomet; Mexico: Aldomet, Amender, Hipermessel, Medopal, Selm, Toparal.

Asia

Japan: Aldomet, Datleal, Decabolamin, Dopamide, Halfdopa, Nichidopa, Sankaira, U-pressdopa.

Drug combinations

Methyldopa and Hydrochlorothiazide

Chemistry

Methyldopa: C~10~H~13~NO~4~ 1½H~2~O. Mw: 238.24. (1) L-tyrosine, 3-hydroxy-α-methyl-, sesquihydrate; (2) L-3-(3,4-dihydroxyphenyl)-2-methylalanine sesquihydrate. CAS-41372-08-1; CAS-555-30-6 (anhydrous)(1962).

Pharmacologic Category

Sympathomimetic (Adrenergic) Agents; α-Adrenergic Agonists. Hypotensive Agents; Central α-Agonists. α~2~-Adrenergic Agonist. (ATC-Code: C02AB).

Mechanism of action

Stimulation of central α-adrenergic receptors by false transmitter that results in decreased sympathetic outflow to heart, kidneys, and peripheral vasculature.

Therapeutic use

Management of moderate-to-severe hypertension.

Pregnancy and lactiation implications

Crosses placenta and may cause hypotension. Overall, medication appears to be safe during pregnancy and lactation.

Unlabeled use

Contraindications

Hypersensitivity to methyldopa or any component of the formulation. Active hepatic disease. Liver disorders previously associated with use of methyldopa. MAOIs. Bisulfite allergy if using oral suspension or injectable.

Warnings and precautions

May rarely produce hemolytic anemia. May rarely produce liver disorders (use with caution in previous liver disease or dysfunction). Usually transient sedation might occur during initial therapy or whenever dose is increased. Use with caution in renal impairment. Active metabolites of methyldopa accumulate in uremia. Use with caution in the elderly (might experience syncope). Often considered drug of choice for treatment of hypertension in pregnancy. Do not use injectable if bisulfite allergy. Tolerance might occur usually between 2^nd^ and 3^rd^ month of therapy.

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