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 |
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Pathways | Not Available |
Acitretin
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