Fong D G, Angulo P, Burgart L J, Lindor K D
Division of Gastroenterology and Hepatology, Mayo Clinic, Rochester, Minnesota 55905, USA.
J Clin Gastroenterol. 2000 Oct;31(3):250-3. doi: 10.1097/00004836-200010000-00016.
Cetirizine, a human metabolite of hydroxyzine, is a selective H1-receptor antagonist currently approved for the treatment of seasonal allergic rhinitis, perennial allergic rhinitis, and chronic urticaria. In U.S. clinical trials, transient reversible hepatic transaminase elevations were observed in <2% of patients during cetirizine therapy. We report a case of cetirizine-induced cholestasis in a 28-year-old man with no previous hepatobiliary disease after a 2-year period of taking cetirizine on a daily basis. The treatment of this patient included the use of ursodeoxycholic acid, as well as hydroxyzine, for symptomatic relief of pruritus. In light of the patient's clinical and biochemical improvement while using hydroxyzine, it appears that the hepatic metabolism of hydroxyzine to metabolites, including cetirizine, is not involved in the pathogenesis of this particular case of drug-induced hepatotoxicity. Cetirizine should be considered as a potential cause of drug-induced cholestasis.
西替利嗪是羟嗪的人体代谢产物，是一种选择性H1受体拮抗剂，目前已被批准用于治疗季节性过敏性鼻炎、常年性过敏性鼻炎和慢性荨麻疹。在美国的临床试验中，接受西替利嗪治疗的患者中，<2%出现了短暂可逆的肝转氨酶升高。我们报告一例28岁男性患者，在每日服用西替利嗪两年后出现西替利嗪诱导的胆汁淤积，该患者既往无肝胆疾病。该患者的治疗包括使用熊去氧胆酸以及羟嗪，以缓解瘙痒症状。鉴于患者在使用羟嗪时临床和生化指标有所改善，看来羟嗪代谢为包括西替利嗪在内的代谢产物的肝脏代谢过程与这一特定药物性肝毒性病例的发病机制无关。西替利嗪应被视为药物性胆汁淤积的潜在病因。
