Department of Medicine, Division of Infectious Diseases, St John Hospital and Medical Center, Detroit, Michigan.
Department of Medicine, Division of Infectious Diseases, Indiana University School of Medicine, Indianapolis.
Clin Infect Dis. 2014 Jul 15;59(2):265-71. doi: 10.1093/cid/ciu221. Epub 2014 Apr 9.
Dolutegravir (DTG), a next-generation integrase strand transfer inhibitor (INSTI), was recently approved for use in the treatment of human immunodeficiency virus infection. In treatment-naive trial participants, DTG given at 50 mg once daily without pharmacologic boosting combined with a standard nucleoside backbone was shown to be noninferior or superior to first-line regimens containing efavirenz, darunavir/ritonavir, or raltegravir regardless of pretreatment viral load. This drug also exhibited efficacy in antiretroviral therapy-experienced participants and has proven to retain activity when dosed twice daily in some participants harboring resistance to the other INSTIs, raltegravir and elvitegravir. DTG has few drug interactions and is taken without regard to meals. It causes benign elevations in serum creatinine based on its inhibition of tubular creatinine secretion without affecting the glomerular filtration rate. Overall, DTG is well tolerated, with headache and insomnia being the most frequently reported adverse events.
多替拉韦（DTG），一种新一代的整合酶链转移抑制剂（INSTI），最近被批准用于治疗人类免疫缺陷病毒感染。在初治试验参与者中，每日一次给予 50mg 剂量、不进行药物增效的多替拉韦联合标准核苷类药物骨干方案，与包含依非韦伦、达芦那韦/利托那韦或拉替拉韦的一线方案相比，无论治疗前病毒载量如何，均显示出非劣效或优效性。该药在抗逆转录病毒治疗经验丰富的参与者中也表现出疗效，并且在一些对其他 INSTIs（拉替拉韦和艾维雷韦）耐药的参与者中，每日两次给药也被证明具有活性。DTG 药物相互作用少，无需考虑进餐时间。它通过抑制管状肌酐分泌引起血清肌酐的良性升高，而不影响肾小球滤过率。总体而言，DTG 具有良好的耐受性，最常报告的不良反应是头痛和失眠。
