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Methyldopa

AEMPS

Centrally-acting antiadrenergic agent

ATC code: C02AB02

Updated · Methodology

Indications

A

Hypertension in pregnancy

First line

Hypertension in pregnancy. Per 222 (2020), SEGO 2023, and 2011, first-line with the longest clinical track record. Dose 250–500 mg 2–4 times daily, max 3 g/day. Onset 2–3 h, peak at 6–8 h. No fetal distress, no impact on fetal peripheral resistance.

Sources

  1. AEMPS: Ficha técnica de Metildopa (2024)
  2. Cochrane Database Syst Rev: Antihypertensive drug therapy for mild to moderate hypertension during pregnancy. (2018)
  3. ACOG: ACOG Practice Bulletin No. 222: Gestational Hypertension and Preeclampsia (2020)

ICD-10: O13 · ICD-11: JA23

How to read tiers A–F
  • AStrong evidence – first or second line in international guidelines
  • BRecommended in selected cases
  • CStudy data contradict each other
  • DBenefit not proven, no documented harm
  • FDocumented harm, or risk without benefit

Mechanism of action

Converted to alpha-methyl-norepinephrine, stimulates brainstem alpha-2 receptors, reduces sympathetic outflow. Lowers peripheral vascular resistance without heart rate change. Longest clinical experience in pregnancy (since 1960s), with no teratogenicity confirmed.

Safety

Contraindications

  • Hypersensitivity
  • Active hepatitis, cirrhosis
  • History of depression (relative)
  • Pheochromocytoma

Serious adverse effects

  • Coombs-positive hemolytic anemia
  • Hepatotoxicity
  • Depression
  • Drug fever

Common adverse effects

  • Sedation
  • Dry mouth
  • Headache
  • Orthostatic hypotension
  • Libido changes
  • Weight gain

Pregnancy: can you take Methyldopa?

Safe. Drug of choice. Used since the 1960s without teratogenicity.

Breastfeeding: can you take Methyldopa?

Hale L2 · Probably compatible

Fully compatible. Hale L2. RID 0.2–0.34%. Possible maternal sedation – discuss alternative if marked.

RID, infant dose via milk
0.3%
Maternal half-life
2 h
Maternal peak time
4 h
Peak milk concentration
0.2 mg/L
Milk-to-plasma ratio
0.5
Calculate RIDSafe feeding windowFull profile on NIH LactMed ↗

Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.

Practical notes

Monitoring

BP twice daily, CBC at 3 months (Coombs-positive hemolytic anemia in 10–20%, clinically significant rare). Monitor ALT/AST – hepatotoxicity risk.
Label mentions24 mentions

Verbatim lines from the interaction sections, in the language of the label

From this drug’s label

  • CriticalIMAOclass named in the label
    «tratamiento con inhibidores de la monoamino oxidasa (IMAO).»

    AEMPS, section 4.3 · Open on CIMA

  • MajorLithium
    «Drug Interactions: When methyldopa is used with other antihypertensive drugs, potentiation of antihypertensive effect may occur. Patients should be followed carefully to detect side reactions or…»

    FDA, section 7 · Open on DailyMed

  • ModerateLithium
    «Litio: Cuando se administran de forma conjunta metildopa y litio, se debe vigilar cuidadosamente a los pacientes por la aparición de síntomas de toxicidad del litio.»

    AEMPS, section 4.5 · Open on CIMA

  • antidepresivos tricíclicosclass named in the label
    «El efecto antihipertensivo de Aldomet puede verse disminuido por los simpaticomiméticos, las fenotiazinas, los antidepresivos tricíclicos y por los IMAO (ver sección 4.3 "Contraindicaciones")…»

    AEMPS, section 4.5 · Open on CIMA

  • simpaticomiméticosclass named in the label
    «El efecto antihipertensivo de Aldomet puede verse disminuido por los simpaticomiméticos, las fenotiazinas, los antidepresivos tricíclicos y por los IMAO (ver sección 4.3 "Contraindicaciones")…»

    AEMPS, section 4.5 · Open on CIMA

From other drugs’ labels

  • CriticalPhenelzine
    «CONTRAINDICATIONS: The potentiation of sympathomimetic substances and related compounds by MAO inhibitors may result in hypertensive crises (see WARNINGS ). Therefore, patients being treated with…»

    FDA, section 4 · Open on DailyMed

  • CriticalTranylcypromine
    «Combination with Certain Drugs: cyclobenzaprine methyldopa tetrabenazine»

    FDA, section 4 · Open on DailyMed

  • MajorAmitriptyline
    «Bloqueantes neuronales adrenérgicos: Los antidepresivos tricíclicos pueden contrarrestar los efectos antihipertensivos de los antihipertensivos de acción central como la guanetidina, la betanidina…»

    AEMPS, section 4.5 · Open on CIMA

  • MajorBisoprolol
    «Antihipertensivos de acción central como clonidina y otros (ej. metildopa, moxonodina, rilmenidina): El uso concomitante de fármacos antihipertensivos de acción central puede empeorar la…»

    AEMPS, section 4.5 · Open on CIMA

  • MajorNebivolol
    «Antihipertensivos de acción central (clonidina, guanfacina, moxonidina, metildopa, rilmenidina): el uso concomitante de antihipertensivos de acción central puede empeorar la insuficiencia cardiaca a…»

    AEMPS, section 4.5 · Open on CIMA

  • MajorXylometazoline
    «Metildopa.»

    AEMPS, section 4.5 · Open on CIMA

  • ModerateChlortalidone
    «Inhibidores de la ECA (por ejemplo, captopril, enalapril): Otros diuréticos, otros medicamentos antihipertensivos (p. ej., betabloqueantes, antagonistas del calcio, inhibidores de la ECA…»

    AEMPS, section 4.5 · Open on CIMA

  • ModerateHydrochlorothiazide
    «Metildopa: Se han reportado casos aislados de hemólisis debido a la formación de anticuerpos anti hidroclorotiazida durante el uso concomitante con metildopa.»

    AEMPS, section 4.5 · Open on CIMA

  • ModerateLithium
    «Antihipertensivos como metildopa: Agentes bloqueadores de los canales de calcio (ej. diltiazem, nifedipino, verapamilo): e l uso concomitante de estos medicamentos puede aumentar el riesgo de…»

    AEMPS, section 4.5 · Open on CIMA

  • ModerateLithium
    «Drugs Having Clinically Important Interactions with Lithium: Intervention: Monitor patients closely for adverse reactions of methyldopa, phenytoin, and carbamazepine.»

    FDA, section 7 · Open on DailyMed

  • ModeratePseudoephedrine
    «Antihipertensivos o diuréticos usados como antihipertensivos : con algunos como los betabloqueantes, metildopa, reserpina y guanetidina puede haber una disminución de sus efectos antihipertensivos…»

    AEMPS, section 4.5 · Open on CIMA

  • Doxylamine
    «Fármacos antihipertensivos con efecto sedante sobre el SNC (especialmente alfa-metildopa), ya que pueden intensificar el efecto sedante cuando se adminisatran con antihistamínicos.»

    AEMPS, section 4.5 · Open on CIMA

  • Enalapril
    «Other Cardiovascular Agents: Enalapril maleate has been used concomitantly with beta adrenergic-blocking agents, methyldopa, nitrates, calcium-blocking agents, hydralazine, prazosin and digoxin…»

    FDA, section 7 · Open on DailyMed

  • Haloperidol
    «El haloperidol puede aumentar la depresión del SNC producida por el alcohol y otros depresores del SNC como hipnóticos, sedantes o analgésicos potentes. Se ha notificado un aumento del efecto sobre…»

    AEMPS, section 4.5 · Open on CIMA

  • Lactoferrin
    «Los derivados del hierro pueden reducir la absorción o biodisponibilidad de las tetraciclinas, quinolonas, micofenolato mofetilo, bifosfonatos, penicilamina, hormonas tiroideas, levodopa, carbidopa…»

    AEMPS, section 4.5 · Open on CIMA

  • Nifedipine
    «alfa-metildopa»

    AEMPS, section 4.5 · Open on CIMA

  • Oxymetazoline
    «Metildopa.»

    AEMPS, section 4.5 · Open on CIMA

  • Propranolol
    «Combinación no recomendada: Antihipertensivos de acción central (clonidina, moxonidina, metildopa):»

    AEMPS, section 4.5 · Open on CIMA

  • Tranylcypromine
    «Influencia en el efecto de otros medicamentos: El efecto hipotensor de los agentes antihipertensivos (por ejemplo, guanetidina, metildopa) puede potenciarse con tranilcipromina; en casos individuales…»

    AEMPS, section 4.5 · Open on CIMA

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Frequently asked

What is Methyldopa used for?

Methyldopa is evaluated for the following indications with varying evidence strength: Hypertension in pregnancy (evidence tier A), Hypertension during breastfeeding (evidence tier A). See the full indication matrix with dosing and citations above on this page.

What are the side effects of Methyldopa?

Common side effects of Methyldopa (≥ 1 in 100): Sedation, Dry mouth, Headache, Orthostatic hypotension, Libido changes, Weight gain. See the Safety section for uncommon and serious reactions.

Is Methyldopa safe during pregnancy?

Safe. Drug of choice. Used since the 1960s without teratogenicity.

Is Methyldopa compatible with breastfeeding?

Fully compatible. Hale L2. RID 0.2–0.34%. Possible maternal sedation – discuss alternative if marked.

Who should not take Methyldopa?

Methyldopa is contraindicated in: Hypersensitivity; Active hepatitis, cirrhosis; History of depression (relative); Pheochromocytoma. Full list in the Safety section.

Official sources

Direct links to regulator labels. Open in a new tab.

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