Midodrine forms an active metabolite, desglymidodrine, that is an alpha1-agonist. This agent increases arteriolar and venous tone resulting in a rise in standing, sitting, and supine systolic and diastolic blood pressure in patients with orthostatic hypotension.
藥動學
Onset: 45-90 min; Duration: 2-6 hrs. Bioavailability: 93%. Protein binding: none. Metabolism: midodrine is a prodrug which undergoes rapid deglycination to desglymidodrine; metabolism occurs in many tissues and plasma. Excretion: renal: 40-75%, feces: 1-2%. Elimination half-life: midodrine: 0.5 hrs, desglymidodrine: 2-4 hrs. Midodrine and desglymidodrine are dialyzable by hemodialysis.
禁忌症
patient with severe organic heart disease or CHF; acute renal disease; urinary retention; pheochromocytoma; thyrotoxicosis; hypersensitivity to midodrine; supine hypertension, persistent and excessive.
Adult: 2.5mg PO BID-TID, MAX dose: 40 mg/day. Do not administer after evening meal or less than 4 hours before bedtime. Safety and efficacy not established in pediatric patients