Abstract：
PURPOSE:To conduct a mechanistic investigation of the interaction between aliskiren and grapefruit juice in healthy subjects. METHODS:Twenty-eight subjects received an oral dose of aliskiren 300 mg (highest recommended clinical dose) with 300 mL of either water or grapefruit juice in a two-way crossover design. Safety and pharmacokinetic analyses were performed. In vitro studies were performed in HEK293 cells to investigate the role of organic anion transporting polypeptide (OATP) transporter-mediated uptake of aliskiren. RESULTS:Co-administration of a single dose of aliskiren with grapefruit juice decreased the plasma concentration of aliskiren, with mean decreases in the AUC(inf), AUC(last), and C(max) of 38, 37, and 61%, respectively. The uptake of [¹⁴C]aliskiren into OATP2B1-expressing cells was essentially the same as that into control cells, and the inhibitor combination atorvastatin and rifamycin had no effect on [¹⁴C]aliskiren accumulation in either cell type. The uptake of [¹⁴C]aliskiren and [³H]fexofenadine was linear in OATP1A2-expressing cells and was reduced by naringin, with IC₅₀ values of 75.5 ± 11.6 and 24.2 ± 2.0 μM, respectively. CONCLUSIONS:Grapefruit juice decreases exposure of aliskiren partially via inhibition of intestinal OATP1A2.
journal_name
Eur J Clin Pharmacoljournal_title
European journal of clinical pharmacologyauthors
Rebello S,Zhao S,Hariry S,Dahlke M,Alexander N,Vapurcuyan A,Hanna I,Jarugula Vdoi
10.1007/s00228-011-1167-4subject
Has Abstractpub_date
2012-05-01 00:00:00pages
697-708issue
5eissn
0031-6970issn
1432-1041journal_volume
68pub_type
临床试验,杂志文章,随机对照试验abstract：:A randomized, single-blind trial of repeated intravenous infusion of Brinase was carried out in 70 petients with severe chronic limb ischemia, who were candidates for lumbar sympathectomy or amputation. The enzyme caused s significant increase in calf and ankle pressure index. At six months follow-up, the clinical res...
journal_title：European journal of clinical pharmacology
pub_type： 临床试验,杂志文章,随机对照试验
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journal_title：European journal of clinical pharmacology
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