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Pharmacokinetics of acitretin
W E Lambert1, E Meyer, A P De Leenheer
1Laboratory for Medical Biochemistry and Clinical Analysis, University of Ghent, Belgium.
Acta Dermato-Venereologica. Supplementum
|January 1, 1994
Summary
Acitretin is rapidly eliminated, but can convert back to etretinate in the body. This necessitates a 2-year contraception period after acitretin therapy due to potential risks.
Area of Science:
- Dermatology
- Pharmacology
- Toxicology
Background:
- Acitretin, a metabolite of etretinate, was initially thought to be eliminated rapidly.
- This led to recommendations for shorter contraception periods post-therapy.
- However, etretinate has been detected in patients treated with acitretin.
Purpose of the Study:
- To review studies on acitretin metabolism in light of new findings.
- To re-evaluate recommended contraception periods after acitretin therapy.
Main Methods:
- Review of existing studies on acitretin and etretinate.
- Analysis of recently discovered metabolic pathways of acitretin.
Main Results:
- Acitretin can be re-esterified back to etretinate in the body.
- This metabolic pathway negates the rapid elimination advantage of acitretin.
- Etretinate presence confirmed in patients undergoing acitretin treatment.
Conclusions:
- The re-esterification of acitretin to etretinate poses a significant risk.
- The recommended contraception period following acitretin therapy must be extended.
- A 2-year contraception period is now advised after acitretin treatment.