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Etretinate has been replaced by acitretin, the free acid (without the ethyl ester). While acitretin is less lipophilic and has a half-life of only 50 hours, it is partly metabolized to etretinate in the body, [ 2 ] so that it is still a long-acting teratogen and pregnancy is prohibited for two years after therapy.
Acitretin is a metabolite of etretinate, which was used prior to the introduction of acitretin. Etretinate was discontinued because it had a narrow therapeutic index as well as a long elimination half-life (t 1/2 = 120 days), making dosing difficult. In contrast, acitretin's half-life is approximately 2 days.
All classes of retinoid bind to many proteins. Natural retinoids such as retinol and retinyl esters bind to carrier proteins such as RBP4, chylomicrons and VLDL while synthetic retinoids likely bind to these and other proteins. [17] First generation retinoids are rapidly metabolized by Cytochrome p450 enzymes, typically of the Cyp26 family. [18]
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Alitretinoin is a form of vitamin A. Alitretinoin has been administered in oncological clinical studies at dosages of more than 10-times of the therapeutic dosage given for chronic hand eczema. The adverse effects observed were consistent with retinoid toxicity, and included severe headache, diarrhoea, facial flushing and hypertriglyceridemia ...
Tretinoin, also known as all-trans retinoic acid (ATRA), is a medication used for the treatment of acne and acute promyelocytic leukemia. [8] [9] [10] For acne, it is applied to the skin as a cream, gel or ointment. [10]