Impact of Green Tea Catechin Ingestion on the Pharmacokinetics of Lisinopril in Healthy Volunteers

Misaka, Shingen; Ono, Yuko; Uchida, Atsushi; Ono, Tomoyuki; Abe, Osamu; Ogata, Hiroshi; Sato, Hideyuki; Shimada, Masahiko; Onoue, Satomi; Shikama, Yayoi; Shimomura, Kenju

doi:10.1111/cts.12905

Cited by 11 publications

(11 citation statements)

References 26 publications

(64 reference statements)

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“…Drug concentrations of elderly patients (> 65 years) have been reported to be approximately double those of younger patients [ 28 ]. And a recent study demonstrated that a concomitant ingestion of epigallocatechin gallate (EGCG)-concentrated green tea extract significantly decreased lisinopril C max , AUC 0-24 and AUC 0-∞ by 71%, 69% and 67%, without altering renal clearance of Lisinopril [ 29 ]. However, in the present study, the enrolled subjects was all between 18 and 50 years old, and those who have drink too much tea were excluded.…”

Section: Discussionmentioning

confidence: 99%

Bioequivalence evaluation and food effect assessment of Lisinopril/amlodipine tablets in healthy Chinese subjects under fasting and fed conditions

Liu

et al. 2022

BMC Pharmacol Toxicol

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Purpose The combination of lisinopril and amlodipine has a marked additional effect on blood pressure and fewer side effects than individual monotherapy. This study was conducted to compare the pharmacokinetic parameters and evaluate the bioequivalence between two Lisinopril/amlodipine tablets in healthy Chinese subjects. Methods A single center, randomized, open-label, single-dose, two-period crossover bioequivalence study was designed in healthy Chinese subjects under both fasting and fed conditions. Blood samples were collected before drug administration and at 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 24, 36, 48, 72, 96, 144, 168 h after administration. Liquid chromatography-tandem mass spectrometry (LC–MS/MS) was applied to determine the plasma concentration of lisinopril and amlodipine. Maximum concentration (Cmax) and area under the concentration–time curve (AUC) were used to evaluate bioequivalence. Adverse events were recorded. Results Ninety-two healthy subjects were enrolled, and 75 completed the study. The 90% confidence intervals (CIs) of the ratio of geometric means (GMRs) of Cmax, AUC0-t, and AUC0-∞ of lisinopril and amlodipine under both fasting and fed conditions fell within the conventional bioequivalence criteria of 0.80–1.25. A high-fat meal appeared to decrease the Cmax and AUC of lisinopril. No severe adverse events were observed. Conclusion The trial demonstrated that the test and the reference lisinopril/amlodipine tablets were bioequivalent and well tolerated in Chinese people under fasting and fed conditions. Trial registration Clinical Trails.gov identifier, NCT04885660 (retrospectively registered in 13/05/ 2021).

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Section: Discussionmentioning

confidence: 99%

Bioequivalence evaluation and food effect assessment of Lisinopril/amlodipine tablets in healthy Chinese subjects under fasting and fed conditions

Liu

et al. 2022

BMC Pharmacol Toxicol

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“…In addition, whereas fexofenadine is mainly eliminated by hepato‐biliary elimination, pseudoephedrine is mostly excreted into urine. Previous clinical studies imply that GT and its main component, EGCG, may reduce the intestinal absorption of hydrophilic drugs with a relatively low bioavailability, including nadolol and lisinopril 2–4 . Therefore, taken together with data showing that GTE did not alter the apparent t 1/2 of fexofenadine, it is suggested that EGCG in the GTE mainly inhibits the intestinal absorption of fexofenadine.…”

Section: Discussionmentioning

confidence: 96%

mentioning

confidence: 99%

“…Green tea (GT; Camellia sinensis ) and its main components, catechins, are perpetrators of clinically relevant food‐drug interactions with hydrophilic and nonmetabolized drugs, such as nadolol and lisinopril 1–4 . Among naturally occurring catechins, (−)‐epigallocatechin gallate (EGCG) plays a major role in GT–drug interactions 2,4 . Orally ingested EGCG likely inhibits membrane permeation of drugs into enterocytes mediated by uptake transporters expressed in the apical membrane, such as organic anion transporting polypeptide (OATP)s 1,2,5–7 .…”

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confidence: 99%

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Exposure of Fexofenadine, but Not Pseudoephedrine, Is Markedly Decreased by Green Tea Extract in Healthy Volunteers

Misaka

Ono

Taudte

et al. 2022

Clin Pharma and Therapeutics

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Green tea (GT) alters the disposition of a number of drugs, such as nadolol and lisinopril. However, it is unknown whether GT affects disposition of hydrophilic anti-allergic drugs. The purpose of this study was to investigate whether pharmacokinetics of fexofenadine and pseudoephedrine are affected by catechins, major GT components.A randomized, open, 2-phase crossover study was conducted in 10 healthy Japanese volunteers. After overnight fasting, subjects were simultaneously administered fexofenadine (60 mg) and pseudoephedrine (120 mg) with an aqueous solution of green tea extract (GTE) containing (−)-epigallocatechin gallate (EGCG) of ~ 300 mg or water (control). In vitro transport assays were performed using HEK293 cells stably expressing organic anion transporting polypeptide (OATP)1A2 to evaluate the inhibitory effect of EGCG on OATP1A2-mediated fexofenadine transport. In the GTE phase, the area under the plasma concentration-time curve and the amount excreted unchanged into urine for 24 hours of fexofenadine were significantly decreased by 70% (P < 0.001) and 67% (P < 0.001), respectively, compared with control. There were no differences in time to maximum plasma concentration and the elimination half-life of fexofenadine between phases. Fexofenadine was confirmed to be a substrate of OATP1A2, and EGCG (100 and 1,000 μM) and GTE (0.1 and 1 mg/mL) inhibited OATP1A2-mediated uptake of fexofenadine. On the contrary, the concomitant administration of GTE did not influence the pharmacokinetics of pseudoephedrine. These results suggest that intake of GT may result in a markedly reduced exposure of fexofenadine, but not of pseudoephedrine, putatively by inhibiting OATP1A2-mediated intestinal absorption.

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“…Common mechanisms include induction or inhibition of drug metabolizing enzymes, particularly the cytochrome P450s (CYPs), and transporters. Regarding transporters, studies showed green tea to decrease systemic area under the plasma concentration versus time curve (AUC) to the minimally metabolized drugs digoxin, fexofenadine, lisinopril, and nadolol 8–12 . These observations were attributed to inhibition of an intestinal uptake transporter(s) by green tea.…”

Section: Introductionmentioning

confidence: 99%

Co‐consuming green tea with raloxifene decreases raloxifene systemic exposure in healthy adult participants

Clarke,

Judson,

Tian

et al. 2023

Clinical Translational Sci

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Green tea is a popular beverage worldwide. The abundant green tea catechin (−)‐epigallocatechin gallate (EGCG) is a potent in vitro inhibitor of intestinal UDP‐glucuronosyltransferase (UGT) activity (Ki ~2 μM). Co‐consuming green tea with intestinal UGT drug substrates, including raloxifene, could increase systemic drug exposure. The effects of a well‐characterized green tea on the pharmacokinetics of raloxifene, raloxifene 4′‐glucuronide, and raloxifene 6‐glucuronide were evaluated in 16 healthy adults via a three‐arm crossover, fixed‐sequence study. Raloxifene (60 mg) was administered orally with water (baseline), with green tea for 1 day (acute), and on the fifth day after daily green tea administration for 4 days (chronic). Unexpectedly, green tea decreased the geometric mean green tea/baseline raloxifene AUC0–96h ratio to ~0.60 after both acute and chronic administration, which is below the predefined no‐effect range (0.75–1.33). Lack of change in terminal half‐life and glucuronide‐to‐raloxifene ratios indicated the predominant mechanism was not inhibition of intestinal UGT. One potential mechanism includes inhibition of intestinal transport. Using established transfected cell systems, a green tea extract normalized to EGCG inhibited 10 of 16 transporters tested (IC50, 0.37–12 μM). Another potential mechanism, interruption by green tea of gut microbe‐mediated raloxifene reabsorption, prompted a follow‐up exploratory clinical study to evaluate the potential for a green tea–gut microbiota–drug interaction. No clear mechanisms were identified. Overall, results highlight that improvements in current models and methods used to predict UGT‐mediated drug interactions are needed. Informing patients about the risk of co‐consuming green tea with raloxifene may be considered.

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Impact of Green Tea Catechin Ingestion on the Pharmacokinetics of Lisinopril in Healthy Volunteers

Cited by 11 publications

References 26 publications

Bioequivalence evaluation and food effect assessment of Lisinopril/amlodipine tablets in healthy Chinese subjects under fasting and fed conditions

Bioequivalence evaluation and food effect assessment of Lisinopril/amlodipine tablets in healthy Chinese subjects under fasting and fed conditions

Exposure of Fexofenadine, but Not Pseudoephedrine, Is Markedly Decreased by Green Tea Extract in Healthy Volunteers

Co‐consuming green tea with raloxifene decreases raloxifene systemic exposure in healthy adult participants

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