Metopirone

• Adrenergic alpha-Agonists
• Sympathomimetics
• Vasoconstrictor Agents
• ATC:C01CA17

• Mepyrapone
• Metapirone
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• Metapyrone
• Methapyrapone
• Methbipyranone
• Methopirapone
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C₁₂H₁₈N₂O₄

http://www.rxlist.com/cgi/generic3/midodrine.htm

Metopirone FDA

No information avaliable

254.282 g/mol

200 to 203°C

Soluble

Solid

0.159

2.5-mg and 5-mg tablets for oral administration

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 a rise in standing, sitting, and supine systolic and diastolic blood pressure in patients with orthostatic hypotension of various etiologies. Standing systolic blood pressure is elevated by approximately 15 to 30 mmHg at 1 hour after a 10-mg dose of midodrine, with some effect persisting for 2 to 3 hours. Midodrine has no clinically significant effect on standing or supine pulse rates in patients with autonomic failure.

Rapidly absorbed following oral administration. The absolute bioavailability of midodrine (measured as desglymidodrine) is 93% and is not affected by food.

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.

No information avaliable

Humans and other mammals