Acitretin

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Absorption Oral absorption of acitretin is optimal when given with food, and is linear and proportional with increasing doses from 25 to 100 mg. Approximately 72% (range 47% to 109%) of the administered dose was absorbed after a single 50 mg dose of acitretin was given to 12 healthy subjects.
Volume of distribution Not Available
Protein binding Over 99.9% bound to plasma proteins, primarily albumin.
Metabolism
Following oral absorption, acitretin undergoes extensive metabolism and interconversion by simple isomerization to its 13-cis form (cis-acitretin). Both parent compound and isomer are further metabolized into chain-shortened breakdown products and conjugates, which are excreted.
Route of elimination Both parent compound and isomer are further metabolized into chain-shortened breakdown products and conjugates, which are excreted. The chain-shortened metabolites and conjugates of acitretin and cis-acitretin are ultimately excreted in the feces (34% to 54%) and urine (16% to 53%).
Half life 49 hours (range 33 to 96 hours)
Clearance Not Available
Toxicity Oral, rat: LD50 = >4000 mg/kg. Symptoms of overdose include headache and vertigo.
Affected organisms
  • Humans and other mammals
Pathways Not Available

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