Methapyrapone
Brand names,
Methapyrapone
Analogs
Methapyrapone
Brand Names Mixture
Methapyrapone
Chemical_Formula
C12H18N2O4
Methapyrapone
RX_link
http://www.rxlist.com/cgi/generic3/midodrine.htm
Methapyrapone
fda sheet
Methapyrapone
msds (material safety sheet)
Methapyrapone
Synthesis Reference
No information avaliable
Methapyrapone
Molecular Weight
254.282 g/mol
Methapyrapone
Melting Point
200 to 203°C
Methapyrapone
H2O Solubility
Soluble
Methapyrapone
State
Solid
Methapyrapone
LogP
0.159
Methapyrapone
Dosage Forms
2.5-mg and 5-mg tablets for oral administration
Methapyrapone
Indication
For the treatment of symptomatic orthostatic hypotension (OH).
Methapyrapone
Pharmacology
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.
Methapyrapone
Absorption
Rapidly absorbed following oral administration. The absolute bioavailability of midodrine (measured as desglymidodrine) is 93% and is not affected by food.
Methapyrapone
side effects and 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.
Methapyrapone
Patient Information
No information avaliable
Methapyrapone
Organisms Affected
Humans and other mammals