Effects of probenecid and cimetidine on the pharmacokinetics of nemonoxacin in healthy Chinese volunteers
文献类型：期刊论文
| 作者 | Zhang, Yi-fan1 ; Dai, Xiao-jian1; Yang, Yong1; Chen, Xiao-yan1; Wang, Ting2; Tang, Yun-biao3; Tsai, Cheng-yuan4; Chang, Li-wen4; Chang, Yu-ting4; Zhong, Da-fang1
|
| 刊名 | DRUG DESIGN DEVELOPMENT AND THERAPY
 |
| 出版日期 | 2016 |
| 卷号 | 10页码:357-370 |
| 关键词 | nemonoxacin probenecid cimetidine clinical pharmacokinetics drug-drug interaction |
| ISSN号 | 1177-8881 |
| 文献子类 | Article |
| 英文摘要 | Purpose: To investigate the effects of probenecid and cimetidine on the pharmacokinetics of nemonoxacin in humans. Methods: Two independent, open-label, randomized, crossover studies were conducted in 24 (12 per study) healthy Chinese volunteers. In Study 1, each volunteer received a single oral dose of 500 mg of nemonoxacin alone or with 1.5 g of probenecid divided into three doses within 25 hours. In Study 2, each volunteer received a single oral dose of 500 mg of nemonoxacin alone or with multiple doses of cimetidine (400 mg thrice daily for 7 days). The plasma and urine nemonoxacin concentrations were determined using validated liquid chromatography-tandem mass spectrometry methods. Results: Coadministration of nemonoxacin with probenecid reduced the renal clearance (CLr) of nemonoxacin by 22.6%, and increased the area under the plasma concentration-time curve from time 0 to infinity (AUC(0-8)) by 26.2%. Coadministration of nemonoxacin with cimetidine reduced the CLr of nemonoxacin by 13.3% and increased AUC(0-8) by 9.4%. Coadministration of nemonoxacin with probenecid or cimetidine did not significantly affect the maximum concentration of nemonoxacin or the percentage of the administered dose recovered in the urine. Conclusion: Although probenecid reduced the CLr and increased the plasma exposure of nemonoxacin, these effects are unlikely to be clinically meaningful at therapeutic doses. Cimetidine had weaker, clinically meaningless effects on the pharmacokinetics of nemonoxacin. |
| WOS关键词 | NON-FLUORINATED QUINOLONE ; RENAL TUBULAR SECRETION ; CLINICAL PHARMACOKINETICS ; COMPETITIVE-INHIBITION ; TG-873870 ; SINGLE ; TRANSPORTERS ; LEVOFLOXACIN ; GEMIFLOXACIN ; SAFETY |
| 资助项目 | National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program" of China[2012ZX0931-001] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000368487900003 |
| 出版者 | DOVE MEDICAL PRESS LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276257]  |
| 专题 | 上海药物代谢研究中心 中科院受体结构与功能重点实验室 新药研究国家重点实验室 |
| 通讯作者 | Zhong, Da-fang |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 501 Haike Rd, Shanghai 201203, Peoples R China; 2.Lanzhou Univ, Hosp 1, Dept Pharm, Lanzhou 730000, Peoples R China; 3.Gen Hosp Shenyang Mil Reg, Dept Pharm, Shenyang, Peoples R China; 4.TaiGen Biotechnol Co Ltd, Taipei, Taiwan |
| 推荐引用方式 GB/T 7714 | Zhang, Yi-fan,Dai, Xiao-jian,Yang, Yong,et al. Effects of probenecid and cimetidine on the pharmacokinetics of nemonoxacin in healthy Chinese volunteers[J]. DRUG DESIGN DEVELOPMENT AND THERAPY,2016,10:357-370. |
| APA | Zhang, Yi-fan.,Dai, Xiao-jian.,Yang, Yong.,Chen, Xiao-yan.,Wang, Ting.,...&Zhong, Da-fang.(2016).Effects of probenecid and cimetidine on the pharmacokinetics of nemonoxacin in healthy Chinese volunteers.DRUG DESIGN DEVELOPMENT AND THERAPY,10,357-370. |
| MLA | Zhang, Yi-fan,et al."Effects of probenecid and cimetidine on the pharmacokinetics of nemonoxacin in healthy Chinese volunteers".DRUG DESIGN DEVELOPMENT AND THERAPY 10(2016):357-370. |
入库方式： OAI收割
来源：上海药物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。