Methyldopa

Generic Details

Generic Name

Methyldopa

Other Names

  • Aldomet

Drug Class

  • Antihypertensive

Chemical Formula

C10H13NO4

Molecular Weight

211.216 g/mol

Mechanism of Action

  • Methyldopa is a prodrug that is metabolized to alpha-methyl norepinephrine, which acts centrally to reduce sympathetic outflow, leading to decreased peripheral resistance and a subsequent decrease in blood pressure.

Indications

  • Hypertension

Common Dosage Forms

  • Tablet
  • Injection

Typical Dosage

  • 250-500 mg 2-4 times per day

Pediatric Dosage

  • Dosage for children should be calculated based on body weight and under the supervision of a healthcare provider.

Geriatric Dosage

  • Dosage adjustments may be necessary in elderly patients due to age-related changes in drug metabolism.

Side Effects

  • Drowsiness
  • Orthostatic hypotension
  • Dry mouth
  • Nausea
  • Headache

Contraindications

  • Hypersensitivity to methyldopa
  • Active hepatic disease

Pregnancy Category

  • Category B - No evidence of risk in humans

Lactation Safety

  • Safe to use while breastfeeding with monitoring for potential side effects in the infant

Drug Interactions

  • Monoamine oxidase inhibitors (MAOIs) may potentiate the hypotensive effect of methyldopa

Overdose Symptoms

  • Severe hypotension
  • Bradycardia
  • CNS depression

Antidote for Overdose

  • Supportive care, monitoring, and symptomatic treatment

Storage Conditions

  • Store at room temperature away from moisture and heat.

Pharmacokinetics

  • Absorption: Well absorbed from the gastrointestinal tract
  • Distribution: Crosses the blood-brain barrier and placenta; distributes into breast milk
  • Metabolism: Metabolized to alpha-methyl norepinephrine
  • Excretion: Primarily renal excretion

Precautions

  • Caution in patients with a history of depression or psychiatric disorders

Warnings

  • Abrupt withdrawal can lead to rebound hypertension

Others

  • Methyldopa may cause a positive Coombs test result.