食物对整合酶抑制剂多替拉韦的药代动力学的影响。
Effect of food on the pharmacokinetics of the integrase inhibitor dolutegravir.
机构信息
GlaxoSmithKline, Research Triangle Park, North Carolina, USA.
出版信息
Antimicrob Agents Chemother. 2012 Mar;56(3):1627-9. doi: 10.1128/AAC.05739-11. Epub 2011 Dec 19.
Abstract
Healthy subjects received dolutegravir at 50 mg in a single-dose crossover study while they were in the fasted state or with low-, moderate-, or high-fat meals. Food increased dolutegravir exposure and reduced the rate of absorption. The area under the concentration-time curve from 0 h to infinity (AUC(0-∞)) increased by 33%, 41%, and 66% when administered with low-, moderate-, or high-fat meals, respectively, compared with fasting. This increase in dolutegravir exposure is not anticipated to impact clinical safety, and therefore dolutegravir can be taken with or without food and without regard to fat content.
摘要
在一项禁食或进低、中、高脂肪餐的单剂量交叉研究中，健康受试者接受了 50 毫克的多替拉韦。食物增加了多替拉韦的暴露量并降低了其吸收速率。与禁食相比，分别与低、中、高脂肪餐同服时，多替拉韦暴露量的 AUC(0-∞)增加了 33%、41%和 66%。这种多替拉韦暴露量的增加预计不会影响临床安全性，因此多替拉韦可以空腹或进食时服用，且无需考虑脂肪含量。
相似文献
1
Effect of food on the pharmacokinetics of the integrase inhibitor dolutegravir.食物对整合酶抑制剂多替拉韦的药代动力学的影响。
Antimicrob Agents Chemother. 2012 Mar;56(3):1627-9. doi: 10.1128/AAC.05739-11. Epub 2011 Dec 19.
2
Pharmacokinetics of dolutegravir when administered with mineral supplements in healthy adult subjects.多替拉韦与矿物质补充剂联合给药在健康成年受试者中的药代动力学。
J Clin Pharmacol. 2015 May;55(5):490-6. doi: 10.1002/jcph.439. Epub 2014 Dec 30.
3
Bioequivalence and Food Effect Assessment of 2 Fixed-Dose Combination Formulations of Dolutegravir and Lamivudine.度鲁特韦/拉米夫定 2 种固定剂量复方制剂的生物等效性和食物影响评估。
Clin Pharmacol Drug Dev. 2020 Feb;9(2):189-202. doi: 10.1002/cpdd.740. Epub 2019 Nov 14.
4
Lack of pharmacokinetic interaction between rilpivirine and integrase inhibitors dolutegravir and GSK1265744.利匹韦林与整合酶抑制剂多替拉韦和 GSK1265744 之间不存在药代动力学相互作用。
Antimicrob Agents Chemother. 2013 Nov;57(11):5472-7. doi: 10.1128/AAC.01235-13. Epub 2013 Aug 26.
5
Relative bioavailability of a paediatric granule formulation of the HIV integrase inhibitor dolutegravir in healthy adult subjects.HIV整合酶抑制剂多替拉韦儿科颗粒制剂在健康成年受试者中的相对生物利用度。
Antivir Ther. 2014;19(3):229-33. doi: 10.3851/IMP2708. Epub 2013 Nov 25.
6
Effect of prednisone on the pharmacokinetics of the integrase inhibitor dolutegravir.泼尼松对整合酶抑制剂多替拉韦药代动力学的影响。
Antimicrob Agents Chemother. 2013 Sep;57(9):4394-7. doi: 10.1128/AAC.00728-13. Epub 2013 Jul 1.
7
A Two-Way Steady-State Pharmacokinetic Interaction Study of Doravirine (MK-1439) and Dolutegravir.多瑞韦拉（MK-1439）与度鲁特韦的双向稳态药代动力学相互作用研究
Clin Pharmacokinet. 2017 Jun;56(6):661-669. doi: 10.1007/s40262-016-0458-4.
8
Effect of fosamprenavir-ritonavir on the pharmacokinetics of dolutegravir in healthy subjects.福沙普那韦-利托那韦对健康受试者中多替拉韦药代动力学的影响。
Antimicrob Agents Chemother. 2014 Nov;58(11):6696-700. doi: 10.1128/AAC.03282-14. Epub 2014 Aug 25.
9
Effects of enzyme inducers efavirenz and tipranavir/ritonavir on the pharmacokinetics of the HIV integrase inhibitor dolutegravir.依非韦伦和替拉那韦/ritonavir 对 HIV 整合酶抑制剂多替拉韦的药代动力学的影响。
Eur J Clin Pharmacol. 2014 Oct;70(10):1173-9. doi: 10.1007/s00228-014-1732-8. Epub 2014 Aug 23.
10
Simplified dolutegravir dosing for children with HIV weighing 20 kg or more: pharmacokinetic and safety substudies of the multicentre, randomised ODYSSEY trial.简化体重 20 公斤及以上的 HIV 感染儿童的多替拉韦剂量：多中心、随机 ODYSSEY 试验的药代动力学和安全性子研究。
Lancet HIV. 2020 Aug;7(8):e533-e544. doi: 10.1016/S2352-3018(20)30189-2.
引用本文的文献
1
Drug-Drug Interactions Between HIV Antivirals and Concomitant Drugs in HIV Patients: What We Know and What We Need to Know.HIV患者中抗逆转录病毒药物与合并用药之间的药物相互作用：我们已知与未知的情况。
Pharmaceutics. 2024 Dec 28;17(1):31. doi: 10.3390/pharmaceutics17010031.
2
Immuno-hematological parameters among adult HIV patients before and after initiation of Dolutegravir based antiretroviral therapy, Addis Ababa, Ethiopia.在开始基于多替拉韦的抗逆转录病毒治疗前后，埃塞俄比亚亚的斯亚贝巴成年艾滋病毒感染者的免疫血液学参数。
PLoS One. 2024 Oct 31;19(10):e0310239. doi: 10.1371/journal.pone.0310239. eCollection 2024.
3
The population pharmacokinetics of dolutegravir co-administered with rifampicin in Thai people living with HIV: Assessment of alternative dosing regimens.多替拉韦与利福平联合给药在泰国HIV感染者中的群体药代动力学：替代给药方案评估
CPT Pharmacometrics Syst Pharmacol. 2025 Jan;14(1):95-104. doi: 10.1002/psp4.13244. Epub 2024 Sep 23.
4
Population Pharmacokinetics of Dolutegravir in African Children: Results From the CHAPAS-4 Trial.多替拉韦在非洲儿童中的群体药代动力学：来自 CHAPAS-4 试验的结果。
J Pediatric Infect Dis Soc. 2024 Sep 26;13(9):496-500. doi: 10.1093/jpids/piae076.
5
Pharmacokinetic Data of Dolutegravir in Second-line Treatment of Children With Human Immunodeficiency Virus: Results From the CHAPAS4 Trial.多替拉韦二线治疗儿童人类免疫缺陷病毒感染的药代动力学数据：CHAPAS4 试验结果。
Clin Infect Dis. 2023 Nov 11;77(9):1312-1317. doi: 10.1093/cid/ciad346.
6
Effect of Food on the Pediatric Dispersible Tablet Formulations of TRIUMEQ and DOVATO in Healthy Adult Participants.食物对TRIUMEQ和DOVATO儿科分散片制剂在健康成年受试者中的影响。
Pharmaceutics. 2023 May 11;15(5):1470. doi: 10.3390/pharmaceutics15051470.
7
Interactions of Antiretroviral Drugs with Food, Beverages, Dietary Supplements, and Alcohol: A Systematic Review and Meta-analyses.抗逆转录病毒药物与食物、饮料、膳食补充剂和酒精的相互作用：系统评价和荟萃分析。
AIDS Behav. 2023 May;27(5):1441-1468. doi: 10.1007/s10461-022-03880-6. Epub 2022 Nov 1.
8
In-vivo pharmacokinetic studies of Dolutegravir loaded spray dried Chitosan nanoparticles as milk admixture for paediatrics infected with HIV.载多替拉韦喷雾干燥壳聚糖纳米粒作为含乳添加剂经体内药代动力学研究用于治疗感染 HIV 的儿科患者。
Sci Rep. 2022 Aug 16;12(1):13907. doi: 10.1038/s41598-022-18009-x.
9
Population Pharmacokinetic Model and Alternative Dosing Regimens for Dolutegravir Coadministered with Rifampicin.人群药代动力学模型和与利福平联合使用时的多替拉韦的替代给药方案。
Antimicrob Agents Chemother. 2022 Jun 21;66(6):e0021522. doi: 10.1128/aac.00215-22. Epub 2022 May 23.
10
Pharmacokinetics, safety, tolerability, and antiviral activity of dolutegravir dispersible tablets in infants and children with HIV-1 (IMPAACT P1093): results of an open-label, phase 1-2 trial.在感染 HIV-1 的婴儿和儿童中，多替拉韦分散片的药代动力学、安全性、耐受性和抗病毒活性（IMPAACT P1093）：一项开放标签、1 期-2 期试验的结果。
Lancet HIV. 2022 May;9(5):e332-e340. doi: 10.1016/S2352-3018(22)00044-3.
本文引用的文献
1
Once daily dolutegravir (S/GSK1349572) in combination therapy in antiretroviral-naive adults with HIV: planned interim 48 week results from SPRING-1, a dose-ranging, randomised, phase 2b trial.每日一次多替拉韦（S/GSK1349572）联合治疗方案用于初治 HIV 成人：SPRING-1 剂量范围、随机、2b 期试验的 48 周计划中期结果。
Lancet Infect Dis. 2012 Feb;12(2):111-8. doi: 10.1016/S1473-3099(11)70290-0. Epub 2011 Oct 20.
2
S/GSK1349572, a new integrase inhibitor for the treatment of HIV: promises and challenges.S/GSK1349572，一种新型整合酶抑制剂，用于治疗 HIV：前景与挑战。
Expert Opin Investig Drugs. 2011 Apr;20(4):537-48. doi: 10.1517/13543784.2011.562189. Epub 2011 Mar 8.
3
In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor.在体抗逆转录病毒特性的 S/GSK1349572，下一代 HIV 整合酶抑制剂。
Antimicrob Agents Chemother. 2011 Feb;55(2):813-21. doi: 10.1128/AAC.01209-10. Epub 2010 Nov 29.
4
Effect of low-, moderate-, and high-fat meals on raltegravir pharmacokinetics.低脂、适度脂肪和高脂餐对拉替拉韦药代动力学的影响。
J Clin Pharmacol. 2011 Mar;51(3):422-7. doi: 10.1177/0091270010367652. Epub 2010 May 10.
5
Pharmacokinetics and safety of S/GSK1349572, a next-generation HIV integrase inhibitor, in healthy volunteers.在健康志愿者中评估 S/GSK1349572（一种下一代 HIV 整合酶抑制剂）的药代动力学和安全性。
Antimicrob Agents Chemother. 2010 Jan;54(1):254-8. doi: 10.1128/AAC.00842-09. Epub 2009 Nov 2.
Zotero 插件