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The most common side effect is transient drowsiness, which occurs in the first 2 to 3 days of initiating therapy, or after a dosage increase.
Cardiovascular
aggravation of angina pectoris, bradycardia (occasional), congestive heart failure, hypertension (rare, following abrupt discontinuation of oral dose), orthostatic hypotension (indicates a need to reduce dosage), prolonged carotid sinus hypersensitivity, sodium and fluid retention (can be controlled with diuretics)
CNS
common (occurs early in therapy): asthenia, drowsiness, vertigo, weakness, headache; rare: Bell’s palsy, depression, impaired concentration, involuntary choreoathetoid movements (indicates a need to discontinue methyldopa), memory impairment, nightmares, parasthesia, parkinsonism, reversible mild psychosis
Gastrointestinal
colitis, constipation, diarrhea, distention, dry mouth, flatulence, nausea, sore or black tongue, vomiting
Hematologic
positive Coombs’ test (10-20%), hemolytic anemia (0.1-0.2% of patients who develop a positive Coomb’s test), leukopenia (rare, primarily granulocytopenia), immune thrombocytopenia (rare), bone marrow depression, positive lupus and rheumatoid factor tests, hemolysis in patients with glucose-6-phosphate dehydrogenase deficiency
Hepatic
rare: abnormal liver function tests, cholestatis, jaundice, hepatitis, hepatic necrosis
Miscellaneous
nasal congestion (common), decreased libido (frequent), impotence (16%), rare: amenorrhea, breast enlargement, gynecomastia, hyperprolactinemia, lactation, increased BUN and serum amylase, blurred vision, nocturia
Immune
drug related fever, myocarditis, pericarditis, lupus like syndrome
Skin
eczema, hyperkeratosis, lichenoid eruptions, rash, toxic epidermal necrolysis, ulceration of the soles of the feet, urticaria
Drug-Drug Interactions
Table 1: Methyldopa Established or Predicted Drug-Drug Interactions
| Drug Name |
Effect |
Clinical Comment |
| Haloperidol |
Methyldopa may increase the effects of haloperidol |
Use alternative therapy |
| Iron |
Iron may decrease the extent of methyldopa absorption |
Use an alternative antihypertensive or give methyldopa 2 hours before or 6 hours after oral iron. Monitor blood pressure |
| Levodopa |
May increase the effect of both levodopa and methyldopa |
Monitor blood pressure and signs of levodopa toxicity. Consider using alternative therapy. |
| Lithium |
Methyldopa may increase lithium toxicity |
Monitor for lithium toxicity. Consider using an alternative antihypertensive. |
| MAOI |
May cause hallucinations, excitation and severe hypertension |
MAOIs are contraindicated with methyldopa therapy |
| Norepinephrine |
Methyldopa may prolong the pressor effects of norepinephrine |
monitor for increased blood pressure |
Drug-Food Interactions
Methyldopa tablets can be taken with or without food.
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