Methyldopa
Antihypertensive · Central alpha agonist
Indications
All grades of hypertension.
Dosage
Tab: Adults: Initially 250 mg two or three times daily, adjust at two day intervals; max 3 gm daily. Elderly: Initially 125 mg twice a day, dose should be increased gradually. Max: 2 gm/day. Children: Not recommended.
Adverse Effects
Sedation, headache, asthaenia, depression, bradycardia, nasal congestion, dry mouth, Gl upset, positive Coomb's test, jaundice haemolytic anaemia.
Risk Factor (Pregnancy/Lactation)
Pregnancy: No evidence of risk in humans. Lactation: Caution advised or effect undetermined. Contraindications: Active liver disease. Depression. Catecholamine-secreting tumours (e.g., phaeochromocytoma, paraganglioma). Precautions: Haemolytic anaemia. History of liver disorder. Monitor liver function and WBC before therapy and for first 6-12 weeks or in case of fever. Renal impairment. Anaesthesia. Severe bilateral cerebrovascular disease. Porphyria.
Interactions
TCADs, MAOIs, other antihypertensives, rauwolfia alkaloids, hydralazine, phenothiazines, lithium, iron, sympathomimetics.
Advice to Patient
Take with or without meals. Contact prescriber if there is disturbed mental status (increased nervousness, depression, anxiety, nightmares); rapid weight gain; unusual or constant swelling of ankles, feet or extremities; rapid heartbeat; palpitations; fever; bruising; rash; prolonged dizziness; constant weakness; yellow eyes or skin; unusual bleeding or fatigue. Hypertension can return within 48 hours after stopping drug. Do not stop taking medication abruptly. Gradually slow down the dosage. To minimize daytime drowsiness, take medicine at bed time. Change position slowly. Weigh yourself in same dress at the same time of day once weekly, report to prescriber if weight gain is more than 5 lb in 2 days.
Pharmacokinetics
Onset: Oral: 3-6 hrs. IV: 4-6 hrs. Duration: Oral: 12-24 hrs. IV: 10-16 hrs. Absorption: Oral: Variably and incompletely absorbed. Approx. 50%. Metabolism: Extensive hepatic. Half-life elimination: Biphasic. Initial phase: 1.7 hrs. Second phase: More prolonged. Time to peak, plasma: Oral/IV: 4-6 hrs. Excretion: Urine (70%). Faeces (30%-50%).
Brands with this active ingredient
Compiled by Healify Pharmacy from published drug references. How we compile it →
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