Isotretinoin is a synthetic analogue of vitamin A. It is used primarily in the treatment of cystic acne.
藥理
Isotretinoin is the oral retinoid of choice for the treatment of nodulocystic acne. Isotretinoin and etretinate have both been effective and superior to other agents in the treatment of Darier's disease.
藥動學
Following oral administration of isotretinoin, there is an apparent lag time of about 0.5–2 hours before the drug appears in systemic circulation. Distribution of isotretinoin into human body tissues and fluids has not been fully characterized. It is 99.9% bound to plasma proteins, principally albumin. Isotretinoin is metabolized in the liver by the cytochrome P-450 (CYP) microsomal enzyme system, principally by CYP2C8, CYP2C9, CYP3A4, and CYP2B6 isoenzymes. Isotretinoin and its metabolites are conjugated, possibly with glucuronic acid, before being excreted in urine and feces. In adults with normal renal function, the half-life in the initial phase (t?α) averages 0.5 hours53 and the half-life in the terminal phase (t?β) averages 10–20 hours (range: 7–39 hours).
禁忌症
Isotretinoin should not be administered to woman, who has the possible bearing child.
懷孕分類
X
哺乳分類
It is not known whether isotretinoin is distributed into milk. Because of the potential for serious adverse reactions to isotretinoin in nursing infants, isotretinoin should not be administered to women who are breast-feeding.
副作用
cutaneous reactions including dry skin, pruritus, and dry mouth. Other effects include: lipid abnormality, hypercalcemia, menstrual disorder, and sexual dysfunction