Methyldopa
ALDOMET
What it isCentral alpha-2 agonist through its active metabolite; hypertension, especially during pregnancy.
Why this oneIts exceptionally long pregnancy safety record keeps it useful despite poor tolerability outside pregnancy.
What limits itSedation is common; monitor for hepatitis and Coombs-positive hemolytic anemia.
FDA-approved for
- hypertension (~1962)
Off-label
- hypertension in pregnancy
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Hypertension | Adult | 250 mg BID–TID | 500 mg–2 g/day divided BID–QID | 3 g/day |
| Hypertension | Pediatric | 10 mg/kg/day divided BID–QID | 65 mg/kg or 3 g/day, whichever less |
Titration Adjust at intervals of not less than 2 days
Renal Impaired renal function may respond to smaller doses
Hepatic Undefined
Instructions
- Start dosage increases in the evening to minimize sedation
- When added to a non-thiazide antihypertensive, limit initial dose to 500 mg/day divided
- Tolerance may occur at 2nd–3rd month; add a diuretic or increase dose to restore control
Contraindications
- MAOIs
- Active hepatic disease (acute hepatitis, active cirrhosis)
- Prior liver disorder associated with methyldopa therapy
- Concurrent MAO inhibitor therapy
Cautions
- Hepatic disorders: hepatitis, jaundice, abnormal LFTs (may be fatal)
- Hemolytic anemia and positive direct Coombs test
- Bone marrow depression / cytopenias
- Sedation, orthostatic hypotension
Adverse reactions
- Sedation
- Headache, asthenia/weakness
- Orthostatic hypotension
- Edema/weight gain
- Bradycardia
- Hemolytic anemia, positive Coombs
- Hepatitis/jaundice
- Dry mouth
Pregnancy Use only if clearly needed; extensive human use suggests fetal harm remote
Lactation Undefined
NO BOXED WARNINGS
Principal riskCoombs-positive hemolytic anemia; sedation
Classes and tags
Clinical profile
Active metabolites
Mechanism of action: Methyldopa ballicule
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