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Centrally acting α2-agonist Pregnancy: Methyldopa has been used under close medical supervision for the treatment of hypertension during pregnancy; there was no clinical evidence that it caused foetal abnormalities or affected the neonate, and published reports across all trimesters indicate the possibility of foetal harm appears remote. It crosses the placental barrier and appears in cord blood, so anticipated benefits must be weighed against possible risks in women who are or may become pregnant. Methyldopa appears in breast milk; use in breast-feeding mothers requires benefits to be weighed against possible risks.

Methyldopa

Brand names: Aldomet

Used in: Pre-eclampsia & Obstetric Emergencies

Methyldopa is a centrally-acting antihypertensive used in obstetrics as a long-established oral treatment for hypertension in pregnancy.

Auto-extracted from the source labelling — not yet independently clinician-verified. These values were distilled from the UK SPC (or the US label where noted) but have not had a clinician sign-off. Confirm against the current SmPC before prescribing.

Adult dose

Dose: Initially 250 mg two or three times a day for two days, then adjusted at intervals of not less than two days until an adequate response is obtained
Route: Oral
Frequency: Two or three times daily initially
Max: 3 g daily (adults); 2 g daily in the elderly
Many patients experience sedation for two or three days when therapy is started or when the dose is increased, so when increasing the dosage it may be desirable to increase the evening dose first. Withdrawal of methyldopa is followed by return of hypertension, usually within 48 hours. Renal impairment: methyldopa is largely excreted by the kidney and patients with impaired renal function may respond to smaller doses. Patients already on other antihypertensives: terminate the other agents gradually if required; limit methyldopa to an initial dose of not more than 500 mg daily, increased as required at intervals of not less than two days, and adjust the dose of the other agents to effect a smooth transition. When 500 mg of methyldopa is added to 50 mg of hydrochlorothiazide, the two agents may be given together once daily. Elderly: initial dose should be kept as low as possible, not exceeding 250 mg daily; an appropriate starting dose would be 125 mg twice daily, increasing slowly as required, not exceeding a maximum daily dosage of 2 g. Syncope in older patients may relate to increased sensitivity and advanced arteriosclerotic vascular disease and may be avoided by lower doses. Liver function tests and a total and differential white blood cell count are advisable before therapy and at intervals during the first six to twelve weeks of therapy, or whenever an unexplained fever occurs; withdraw therapy if fever, abnormal liver function or jaundice occurs.

Paediatric dose

Dose: 10 mg/kg
Route: Oral
Frequency: Daily in 2-4 divided doses
Max: 65 mg/kg or 3.0 g daily, whichever is less
SPC section 4.2 states the initial paediatric dosage is based on 10 mg/kg body weight daily in 2-4 oral doses; the daily dose is then increased or decreased until an adequate response is obtained. Verify against a children's formulary before prescribing.

Dose adjustments

Renal

Methyldopa is largely excreted by the kidney; patients with impaired renal function may respond to smaller doses

Dose auto-extracted from UK Summary of Product Characteristics (SPC) via the eMC; US FDA prescribing information (openFDA / DailyMed) — cross-check; US labelling may differ from UK — not yet clinician-verified. Always confirm against the product SmPC and your local formulary before prescribing.

Paediatric weight-based calculator

SPC section 4.2 states the initial paediatric dosage is based on 10 mg/kg body weight daily in 2-4 oral doses; the daily dose is then increased or decreased until an adequate response is obtained. Verify against a children's formulary before prescribing.

Verify in a children's formulary

Contraindications

  • Depression
  • Active hepatic disease such as acute hepatitis and active cirrhosis
  • Hypersensitivity to methyldopa or any excipient, including hepatic disorders associated with previous methyldopa therapy
  • Therapy with monoamine oxidase inhibitors (MAOIs)
  • Catecholamine-secreting tumour such as phaeochromocytoma or paraganglioma
  • Porphyria

Side effects

  • Sedation (usually transient), particularly on initiation or dose increase; headache, asthenia or weakness as early transient symptoms
  • Haemolytic anaemia, leukopenia, granulocytopenia, thrombocytopenia, bone-marrow failure
  • Positive Coombs test (incidence averages 10-20% on continued therapy; dose-related, lowest at 1 g/day or less)
  • Liver disorders including hepatitis and jaundice; abnormal liver function tests
  • Orthostatic hypotension, bradycardia; oedema and weight gain
  • Psychic disturbances including nightmares, reversible mild psychoses or depression

Interactions

  • Monoamine oxidase inhibitors - contraindicated (SPC section 4.3)
  • Other antihypertensive drugs - potentiation of antihypertensive effect may occur; follow patients carefully
  • Anaesthetics - patients may require reduced doses; hypotension during anaesthesia can usually be controlled by vasopressors
  • Lithium - monitor carefully for symptoms of lithium toxicity when given concomitantly
  • Ferrous sulfate or ferrous gluconate - decrease the bioavailability of methyldopa and may adversely affect blood pressure control; coadministration is not recommended

Clinical monograph

How it works

It is converted centrally to alpha-methylnoradrenaline, which stimulates central alpha-2 adrenoceptors to reduce sympathetic outflow and lower peripheral vascular resistance.

Prescribing in practice

  • It has a long record of fetal safety in pregnancy but is best avoided in women with a history of depression and is conventionally discontinued shortly after delivery because of the risk of postnatal depression.
  • Sedation, dizziness and dry mouth are common, particularly on initiation and dose increases.
  • It can rarely cause a positive direct antiglobulin (Coombs) test, haemolytic anaemia and abnormal liver function.

Monitoring

Monitor blood pressure and, with prolonged therapy, full blood count and liver function.

Counselling the patient

  • Drowsiness is common early in treatment; take care with driving until you know how it affects you.
  • Do not stop the medicine suddenly without advice.
  • Tell your clinician about low mood, as this medicine is usually changed around the time of delivery.

Evidence & guidelines

Methyldopa remains a recommended first-line option for hypertension in pregnancy in NICE guidance, supported by extensive long-term safety data.

Reference: NICE NG133; Drug verified in RxNorm (NLM); confirm dosing against the manufacturer SPC (eMC). Verify against your local formulary and current prescribing references before prescribing. The structured dose values shown have been reviewed by a clinician. Monograph status: clinician-reviewed (2026-07-04).

Related

Curated clinical cross-links plus same-class fallbacks.