Alprazolam

0 comments
Absorption Readily absorbed from the gastrointestinal tract. Bioavailability is 80-90%.
Volume of distribution Not Available
Protein binding 80% (mainly to albumin)
Metabolism
Hepatic. Hydroxylated in the liver to α-hydroxyalprazolam, which is also active. This and other metabolites are later excreted in urine as glucuronides.
Enzyme Metabolite Reaction Km Vmax
Cytochrome P450 3A5 alpha-Hydroxyalprazolam hydroxylation

Cytochrome P450 3A4 4-Hydroxyalprazolam 4-hydroxylation

Cytochrome P450 3A4 4-OH Alprazolam 4-hydroxylation 81 3470.16
Cytochrome P450 3A4 1'-OH Alprazolam 1'-hydroxylation 55 69.75
Cytochrome P450 2C9 alpha-Hydroxyalprazolam hydroxylation

Cytochrome P450 2C19 alpha-Hydroxyalprazolam hydroxylation

Route of elimination Alprazolam and its metabolites are excreted primarily in the urine.
Half life 6.3-26.9 hours
Clearance
  • 2.13 +/- 0.54 mL/min/kg [CYP3A inducers]
  • 0.90 +/- 0.21 mL/min/kg [without CYP3A inducers]
Toxicity Oral, mouse: LD50=1020 mg/kg. Symptoms of overdose include confusion, coma, impaired coordination, sleepiness, and slowed reaction time.
Affected organisms
  • Humans and other mammals
Pathways Not Available

0 comments:

Post a Comment

Copyright 2011 Pharmacokinetics of Drugs.
Blogger Template by Noct.