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QuickView for Midodrine (compound)

Name: Midodrine
PubChem Compound ID: 18340
Description: An ethanolamine derivative that is an adrenergic alpha-1 agonist. It is used as a vasoconstrictor agent in the treatment of HYPOTENSION.
Molecular formula: C12H19ClN2O4
Molecular weight: 290.743 g/mol
Pro-Amatine (TN); Amatine; Acetamide, 2-amino-N-(beta-hydroxy-2,5-dimethoxyphenethyl)-, hydrochloride; ProAmatine; 2-Amino-N-(2-(2,5-dimethoxyphenyl)-2-hydroxyethyl)acetamide monohydrochloride; 3092-17-9; Alphamine; 43218-56-0; Metligene; D01307.
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Name: Midodrine
Name (isomeric): DB00211
Drug Type: small molecule
Description: An ethanolamine derivative that is an adrenergic alpha-1 agonist. It is used as a vasoconstrictor agent in the treatment of HYPOTENSION.
Midodrina [INN-Spanish]; Midodrin; Midodrinum [INN-Latin]; midodrine hydrochloride; Midodrine HCL
Brand: ProAmatine
Category: Adrenergic alpha-Agonists, Sympathomimetics, Vasoconstrictor Agents
CAS number: 133163-28-7
Indication: For the treatment of symptomatic orthostatic hypotension (OH).
Midodrine is a prodrug, i.e., the therapeutic effect of orally administered midodrine is due to the major metabolite desglymidodrine formed by deglycination of midodrine. Desglymidodrine diffuses poorly across the blood-brain barrier, and is therefore not associated with effects on the central nervous system. Administration of midodrine results in ...
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Mechanism of Action: Midodrine forms an active metabolite, desglymidodrine, that is an alpha1-agonist, and exerts its actions via activation of the alpha-adrenergic receptors of the arteriolar and venous vasculature, producing an increase in vascular tone and elevation of blood pressure. Desglymidodrine does not stimulate cardiac beta-adrenergic receptors.
Absorption: Rapidly absorbed following oral administration. The absolute bioavailability of midodrine (measured as desglymidodrine) is 93% and is not affected by food.
Biotransformation: Thorough metabolic studies have not been conducted, but it appears that deglycination of midodrine to desglymidodrine takes place in many tissues, and both compounds are metabolized in part by the liver.
Half Life: The plasma levels of the prodrug peak after about half an hour, and decline with a half-life of approximately 25 minutes, while the metabolite reaches peak blood concentrations about 1 to 2 hours after a dose of midodrine and has a half-life of about 3 to 4 hours.
Clearance: Renal cl=385 mL/minute
Toxicity: Symptoms of overdose could include hypertension, piloerection (goosebumps), a sensation of coldness and urinary retention. The single doses that would be associated with symptoms of overdosage or would be potentially life- threatening are unknown. The oral LD50 is approximately 30 to 50 mg/kg in rats, 675 mg/kg in mice, and 125 to 160 mg/kg in dogs. Desglymidodrine is dialyzable.
Affected organisms: Humans and other mammals
Food interaction:
Take without regard to meals.
Drug interaction:
PseudoephedrineIncreased arterial pressure
PrednisoneIncreased arterial pressure
FludrocortisoneIncreased arterial pressure
RasagilineRisk of hypertensive crisis.
ProcaterolIncreased arterial pressure
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