Methyldopa

Class
Antihypertensives
Subclass
α2-adrenergic receptor agonists
Substance name
Methyldopa
Brand names
Aldomet®
Common formulations
Film-coated tablet
Dosage and administration
Adults patients
Hypertension
•
Start at: 250 mg PO BID-TID for 2 days
•
Maintenance: 500-2,000 mg PO daily, in 2-4 divided doses
•
Maximum: 3,000 mg per day
Hypertension in pregnancy • Off-label
•
Start at: 250 mg PO BID-TID
•
Maintenance: 500-1,500 mg PO daily, in 2-4 divided doses
•
Maximum: 3,000 mg per day
Postural orthostatic tachycardia syndrome • Off-label
•
Start at: 125 mg PO qHS
•
Maintenance: 250 mg PO BID
Indications for use
Labeled indications
Adults
•
Treatment of hypertension
Children
•
Treatment of hypertension
Off-label indications
Adults
•
Treatment of hypertension in pregnancy
•
Treatment of postural orthostatic tachycardia syndrome
Safety risks
Contraindications
Hypersensitivity to methyldopa or its components
Active liver disease or liver disorders previously associated with methyldopa
Concomitant use of MAOIs
Warnings and precautions
Choreoathetosis
•
Use caution in patients with severe bilateral cerebrovascular disease. Discontinue if choreoathetotic movements occur.
Hemolytic anemia, positive direct Coombs test
•
Maintain a high level of suspicion, as prolonged therapy with methyldopa has been associated with an increased risk for these adverse events. Obtain CBC and Coombs test before initiating treatment and periodically thereafter.
Increased serum transaminases, increased serum TBIL, prolonged PT, jaundice, fever
•
Maintain a high level of suspicion, as methyldopa has been associated with an increased risk for these adverse events. Assess liver enzymes before initiating treatment and periodically thereafter.
Peripheral edema
•
Maintain a high level of suspicion, as methyldopa has been associated with an increased risk for these adverse events. Discontinue if edema progresses or signs of HF occur.
Specific populations
Renal impairment
CrCl > 50 mL/min
•
Do not exceed frequency of TID.
CrCl 10-50 mL/min
•
Do not exceed frequency of BID-TID.
CrCl < 10 mL/min
•
Do not exceed frequency of q12-24h.
Renal replacement therapy
Continuous renal replacement
•
Dose as in CrCl 10-50 mL/min. Monitor blood pressure.
Intermittent hemodialysis
•
Administer the dose after dialysis session. Monitor blood pressure.
Peritoneal dialysis
•
Dose as in CrCl < 10 mL/min. Monitor blood pressure.
Hepatic impairment
Acute or decompensated chronic liver disease
•
Do not use.
Any severity
•
Do not use.
Pregnancy and breastfeeding
Pregnancy
All trimesters • Australia Category: A
•
Generally acceptable for use. Oral methyldopa is considered to be the antihypertensive medication of choice in pregnancy due to its long record of safety and efficacy.
Breastfeeding
Acceptable for use during breastfeeding.
Undetectable levels in breastfed infants.
No overt adverse effects reported in breastfed infants.
Some adverse effects on lactation reported.
Adverse reactions
Very common > 10%
•
⊕ direct Coombs test, ↓ libido, dizziness, ejaculation difficulties, erectile dysfunction
Common 1-10%
•
Hemolytic anemia, raynaud's phenomenon, headache
Unknown frequency
•
Acute pancreatitis, agranulocytosis, bradycardia, choreoathetosis, colitis, ↓ WBC count, ↓ platelet count, gynecomastia, heart failure, atrioventricular block, hepatitis, hypotension, ↑ blood eosinophil count, ↑ liver enzymes, jaundice, ↑ serum prolactin, myocarditis, pericarditis, amenorrhea, angina pectoris, anorgasmia, arthralgia, constipation, nasal congestion, depression, diarrhea, dry mouth, fever, flatulence, galactorrhea, myalgia, nasal congestion, nausea, nightmares, paresthesia, skin rash, somnolence, vertigo, vomiting, toxic epidermal necrolysis, urticaria
Interactions
Drug(s)
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