Midodrine (proamatine) is an orally effective a1 receptor agonist. It is a prodrug; its activity is due to its conversion to an active metabolite, desglymidodrine, which achieves peak concentrations ~1 hour after a dose of midodrine. The t/2 of desglymidodrine is ~3 hours; its duration of action is 4-6 hours. Midodrine stimulates contraction of both arterial and venous smooth muscle, and has useful effects in treating autonomic insufficiency and postural hypotension. A frequent complication in these patients is supine hypertension, which can be minimized by avoiding dosing prior to bedtime and by elevating the head of the bed. Typical dosing, achieved by careful titration of blood pressure responses, is 2.5-10 mg 3 times daily.
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