دورية أكاديمية
Increased systemic exposure of fimasartan, an angiotensin II receptor antagonist, by ketoconazole and rifampicin
| العنوان: | Increased systemic exposure of fimasartan, an angiotensin II receptor antagonist, by ketoconazole and rifampicin |
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| المساهمون: | College of Medicine, Dept. of Pharmacology, Jung Won Kim, SoJeong Yi, Tae-Eun Kim, Kyoung Soo Lim, Seo Hyun Yoon, Joo-Youn Cho, Min Goo Lee, Im-Sook Song, Sang-Goo Shin, In-Jin Jang, Kyung-Sang Yu, Lee, Min Goo |
| بيانات النشر: | Wiley |
| سنة النشر: | 2013 |
| مصطلحات موضوعية: | Adult, Angiotensin II Type 1 Receptor Blockers/administration & dosage, Angiotensin II Type 1 Receptor Blockers/blood, Angiotensin II Type 1 Receptor Blockers/pharmacokinetics, Animals, Area Under Curve, Biphenyl Compounds/administration & dosage, Biphenyl Compounds/blood, Biphenyl Compounds/pharmacokinetics, Cells, Cultured, Cross-Over Studies, Drug Interactions, Humans, Ketoconazole/administration & dosage, Male Oocytes/drug effects, Oocytes/metabolism, Organic Anion Transport Protein 1/genetics, Organic Anion Transport Protein 1/metabolism, Organic Anion Transporters/genetics, Organic Anion Transporters/metabolism, Pyrimidines/administration & dosage, Pyrimidines/blood, Pyrimidines/pharmacokinetics, Rifampin/administration & dosage, Solute Carrier Organic Anion Transporter Family Member 1b1, Tetrazoles/administration & dosage, Tetrazoles/blood, Tetrazoles/pharmacokinetics, Xenopus laevis |
| الوصف: | The authors studied the effects of ketoconazole and rifampicin on the pharmacokinetics of a single dose of fimasartan (BR-A-657), a newly developed angiotensin II receptor antagonist for the treatment of hypertension, in 22 healthy participants. Ketoconazole increased the maximumplasma concentration (Cmax) and area under the plasma concentration vs time curve to infinity (AUC�닞 of fimasartan by 2.47-fold (90% confidence interval [CI], 1.61-3.79) and 2.03-fold (1.56-2.64), respectively. Concomitant administration of rifampicin increased the C(max) and AUC�닞 of fimasartan by 10.33-fold (90% CI, 6.74-15.81) and 4.60-fold (3.54-5.97). In vitro studies indicated that ketoconazole inhibited the uptake of fimasartan into cells expressing OATP1B1 with a K(i) of 107.7 쨉M, and rifampicin inhibited OAT1- and OATP1B1-mediated fimasartan transport with a K(i) of 212 쨉M and 12.2 쨉M, respectively. The systemic exposure of fimasartan was significantly increased by coadministration of ketoconazole or rifampicin in healthy volunteers. This is consistent with the in vitro results, in which fimasartan is a substrate of CYP3A and OATP1B1. ; restriction |
| نوع الوثيقة: | article in journal/newspaper |
| اللغة: | English |
| تدمد: | 0091-2700 1552-4604 |
| العلاقة: | JOURNAL OF CLINICAL PHARMACOLOGY; J01338; OAK-2013-03372; https://ir.ymlib.yonsei.ac.kr/handle/22282913/158445Test; T201306133; JOURNAL OF CLINICAL PHARMACOLOGY, Vol.53(1) : 75-81, 2013 |
| DOI: | 10.1177/0091270011433328 |
| DOI: | 10.1177/0091270011433328/abstract |
| الإتاحة: | https://doi.org/10.1177/0091270011433328Test https://ir.ymlib.yonsei.ac.kr/handle/22282913/158445Test |
| حقوق: | CC BY-NC-ND 2.0 KR ; https://creativecommons.org/licenses/by-nc-nd/2.0/krTest/ |
| رقم الانضمام: | edsbas.E6CE13E0 |
| قاعدة البيانات: | BASE |
| تدمد: | 00912700 15524604 |
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| DOI: | 10.1177/0091270011433328 |