Adult Dosing

Hypertension

• 250-500 mg IV q6 hrs
• MAX: 1 g q6 hrs

Pediatric Dosing

Hypertension

• 20-40 mg/kg/day IV divided q6 hrs
• MAX: 65 mg/kg/day in divided doses or 3 g/day whichever is less

• Hypertension

• Hypersensitivity to any of the ingredients of the product
• Active hepatic disease such as acute hepatitis and active cirrhosis
• Liver disorders previously associated with methyldopa
• Concomitant therapy with monoamine oxidase (MAO) inhibitors

• N/A

Renal Dose Adjustment

• Renal impairment: Reduce dose/adjust frequency; dose adjustments not defined

Hepatic Dose Adjustment

• Hepatic cirrhosis/Hepatitis: Contraindicated
• Previous hepatic impairment with methyldopa: Contraindicated

• Positive Coombs test, hemolytic anemia, and liver disorders may occur; monitor patient closely because of potentially fatal complications
• With prelonged therapy 10-20% patients develop a positive direct Coombs test which usually occurs between 6 and 12 months of therapy
• If Coombs-positive hemolytic anemia occurs, discontinue the therapy
• Monitor CBC at baseline; liver function tests during 1st 6-12 wks of treatment; if unexplained fever then periodically
• Monitor hematocrit, Hb, cardiac function at baseline, then periodically
• If need of transfusion arrises in patients receiving therapy, both a direct and indirect Coombs test should be performed
• Jaundice, with or without fever may occur with onset within first 2-3 months of therapy
• Rarely fatal hepatic necrosis has been reported with use of methyldopa
• If fever, abnormalities in liver function tests or jaundice appear discontinue therapy
• Patients taking methyldopa may have experience clinical edema, CHF or weight gain which may be controlled by a diuretic
• Pardoxical pressor response has ben reported with IV administration
• Rarely involuntary choreoathetotic movements have been observed during therapy with methyldopa in patients with severe cerebrovascular disease, if synptoms occur discontinue the therapy

Pregnancy Category:C

Breastfeeding: Probably safe; methyldopa is excreted in breastmilk in small amounts and thus would not be expected to cause any adeverse events in breastfed infants. This information is based upon LactMed database (available at http://toxnet.nlm.nih.gov/cgi-bin/sis/htmlgen?LACT last accessed 12 July 2013). According to the manufacturer caution should be exercised when administering methyldopate to a nursing women.

• CNS: Sedation, headache, asthenia, depression, dizziness, light headedness
• PSYCHIATRIC: Parkinsonism, Bell's palsy, decreased mental acuity, involuntary choreoathetotic movements, symptoms of cerebrovascular insufficiency, psychic disturbances, paresthesias
• CV: Aggravation of angina pectoris, congestive heart failure, prolonged carotid sinus hypersensitivity, orthostatic hypotension, hypotension, bradycardia
• GI: Pancreaitis, colitis, vomiting, diarrhea, sialadenitis, sore tongue, nausea, constipation, distension, flatus, dryness of mouth
• METABOLIC: Hyperprolactinemia, Rise in BUN
• HEMA: Bone marrow depression, leukopenia, granulocytopenia, thrombocytopenia, hemolytic anemia, LE cells, rheumatoid factor, positive Coombs test
• HEPA: Liver disorders including hepatitis, jaundice, abnormal liver function tests
• MUSC: Arthralgia, myalgia
• RESP: Nasal stuffiness
• DERM: Toxic epidermal necrolysis, rash
• GU: Amenorrhea, breast enlargement, gynecomastia, lactation, impotence, decreased libido, disorder of ejaculation, impotence
• Misc: Systemic lupus erythematosus, drug fever

• Antihypertensive agent; undergoes metabolism to form alpha-methyl-norepinephrine, which then lowers arterial pressure by stimulation of central inhibitory alpha-adrenergic receptors, false neurotransmission, and/or reduction of plasma renin activity
• Extensively metabolised in liver
• Excretion: 49% excreted as methyldopa and its mono-O-sulfate
• Half-life: 90-127 minutes

US Trade Name(s)

• Only generic available

US Availability

methyldopate (generic)

• INJ: 50 mg/ml

Canadian Trade Name(s)

• N/A

Canadian Availability

• N/A

UK Trade Name(s)

• N/A

UK Availability

• N/A

Australian Trade Name(s)

• N/A

Australian Availability

• N/A

Cardiovascular

Antihypertensives