Kato Y, Fujii T, Mizoguchi N, Takata N, Ueda K, Feldman M D, Kayser S R
Department of Pediatrics, Hiroshima University Medical Hospital, Japan.
Pharmacotherapy. 2000 Jul;20(7):851-4. doi: 10.1592/phco.20.9.851.35206.
Ritonavir (RTV), a protease inhibitor, and carbamazepine (CBZ), an anticonvulsant, were administered concurrently to a patient who had human immunodeficiency virus infection and epilepsy. The combination resulted in elevated serum concentrations of CBZ, with accompanying vomiting, vertigo, and transient liver dysfunction. After discontinuing RTV and reducing the dosage of CBZ, the serum concentration of CBZ returned to the optimal range, symptoms subsided, and liver function returned to baseline. Carbamazepine is metabolized in the liver to a large extent by the cytochrome P450 (CYP) system, especially CYP3A4, 2C8, and 1A2, whereas RTV is metabolized primarily by CYP3A and is a potent inhibitor of this enzyme. Careful clinical monitoring may help prevent adverse drug interactions when these drugs are administered concurrently.
蛋白酶抑制剂利托那韦（RTV）和抗惊厥药卡马西平（CBZ）同时用于一名感染人类免疫缺陷病毒且患有癫痫的患者。这一联合用药导致CBZ血清浓度升高，并伴有呕吐、眩晕和短暂性肝功能障碍。停用RTV并降低CBZ剂量后，CBZ血清浓度恢复至最佳范围，症状消退，肝功能恢复至基线水平。卡马西平在肝脏中很大程度上由细胞色素P450（CYP）系统代谢，尤其是CYP3A4、2C8和1A2，而RTV主要由CYP3A代谢，并且是该酶的强效抑制剂。当同时使用这些药物时，仔细的临床监测可能有助于预防药物不良反应。
