Trial reportEuropean journal of clinical pharmacology2012
Effect of grapefruit juice on the pharmacokinetics of tolvaptan, a non-peptide arginine vasopressin antagonist, in healthy subjects.
Trial report in European journal of clinical pharmacology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
9 citing papers in PubMed, 25 citations in OpenAlex.
- Vaptans: A Narrative Review of Pharmacokinetics, Pharmacogenetics, and Clinical Applications.Cells · 2026Review
- MD simulation-based screening approach identified tolvaptan as a potential inhibitor of Eg5.Molecular diversity · 2023Article
- Human Sulfotransferases Enhance the Cytotoxicity of Tolvaptan.Toxicological sciences : an official journal of the Society of Toxicology · 2016Article
- Quantification of tolvaptan in rabbit plasma by LC-MS/MS: Application to a pharmacokinetic study.Journal of pharmaceutical analysis · 2015Article
- Effect of CYP3A perpetrators on ibrutinib exposure in healthy participants.Pharmacology research & perspectives · 2015Article
- Mechanisms of tolvaptan-induced toxicity in HepG2 cells.Biochemical pharmacology · 2015Article
- Review of Tolvaptan's Pharmacokinetic and Pharmacodynamic Properties and Drug Interactions.Journal of clinical medicine · 2014Review
- Mechanisms underlying food-drug interactions: inhibition of intestinal metabolism and transport.Pharmacology & therapeutics · 2012Review
- Tolvaptan, hyponatremia, and heart failure.International journal of nephrology and renovascular disease · 2011Article
Corrections and comments
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Authors and funding
3 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeTolvaptan is a selective vasopressin V2 receptor antagonist that can be given orally once daily for treatment of clinically significant hypervolemic and euvolemic hyponatremia (US and Europe) or extracellular volume expansion despite taking other diuretics (Japan). In vitro studies indicated that tolvaptan was a CYP3A4 substrate.
methodsA single-center, randomized, crossover trial of 60-mg tolvaptan with 240 mL of water or with 240 mL of reconstituted grapefruit juice (washout period of 72 h between doses) was conducted in 20 healthy subjects. Blood samples for tolvaptan plasma concentrations were obtained for 48 h postdose.
resultsAll subjects completed the trial. Following co-administration with grapefruit juice, tolvaptan concentrations were elevated compared with tolvaptan alone for only 16 h postdose; consequently, the mean elimination half-life of tolvaptan was unchanged, 5.7 vs 5.1 h respectively. The mean maximal plasma concentration (C(max)) and the area under the curve (AUC(∞)) of tolvaptan were increased 1.86- and 1.56-fold respectively when co-administered with grapefruit juice.
conclusionsIt appears that grapefruit juice increases the bioavailability of tolvaptan, but does not affect its systemic elimination. The adverse event profile was consistent with the aquaretic effect of tolvaptan as urinary frequency, thirst, and dry mouth were the most frequently reported events.
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