Effects of berberine on the blood concentration of cyclosporin A in renal transplanted recipients: Clinical and pharmacokinetic study
Abstract
Objective To study the effects of berberine (BBR) on the blood concentration and pharmacokinetics of cyclosporin A (CsA) in renal-transplant recipients.Methods In a randomized and controlled clinical trial, 52 renal-transplant recipients were treated with CsA and 0.2 g BBR three times daily for 3 months, while another 52 subjects received CsA without BBR co-administration. Blood trough concentration of CsA and biochemistry indexes for hepatic and renal functions were determined. For the pharmacokinetic study, six renal-transplant recipients were included with a 3-mg/kg dosage of CsA twice daily before and after oral co-administration of 0.2 g BBR three times daily for 12 days.Results The trough blood concentrations and the ratios of concentration/dose of CsA in the BBR-treated group increased by 88.9% and 98.4%, respectively, compared with those at baseline (P < 0.05). As for the BBR-free group, they rose by 64.5% and 69.4%, respectively, relative to those at baseline (P < 0.01). Nevertheless, the final blood concentrations and the ratios of concentration/dose of CsA in BBR-treated patients were still 29.3% and 27.8%, respectively, higher than those in BBR-free patients (P < 0.05). No significant effects on liver or renal functions were observed under coadministration of BBR. After co-administration of BBR in six patients for 12 days, the mean AUC of CsA was increased by 34.5% (P < 0.05). The mean time taken to reach the peak blood concentration (t(max)) and the mean half-life (t(1/2)) of CsA were increased by 1.7 h and 2.7 h, respectively (P < 0.05). The average percentage increases in the steady-state drug concentration (Css) and minimum blood concentration (Cmin) were 34.5% and 88.3%, respectively (P < 0.05). In addition, the average percentage decrease in CL/F was 40.4% (P < 0.05) and the peak-to-through fluctuation index was significantly reduced (P < 0.01).Conclusion The BBR can markedly elevate the blood concentration of CsA in renal-transplant recipients in both clinical and pharmacokinetic studies. This combination may allow a reduction of the CsA dosage. The mechanism for this interaction is most likely explained by inhibition of CYP3A4 by BBR in the liver and/or small intestine.
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In a pharmacokinetic substudy (n = 6), 12 days of berberine 0.2 g three times daily increased cyclosporine AUC by 34.5% and reduced apparent oral clearance by 40.4%.
“In a pharmacokinetic substudy (n = 6), 12 days of berberine 0.2 g three times daily increased cyclosporine AUC by 34.5% and reduced apparent oral clearance by 40.4%.”
From Berberine-Drug Interactions: Mechanisms, Clinical Relevance and Risk Stratification-A Narrative Review (2026) · cites this paper as [118]
In the parallel controlled trial (n = 104), trough concentrations rose by 88.9% from baseline in the berberine group; because the berberine-free group also rose by 64.5% from baseline, the between-group difference at study end was 29.3% for trough concentration and 27.8% for the concentration/dose ratio.
“In the parallel controlled trial (n = 104), trough concentrations rose by 88.9% from baseline in the berberine group; because the berberine-free group also rose by 64.5% from baseline, the between-group difference at study end was 29.3% for trough concentration and 27.8% for the concentration/dose ratio [118].”
From Berberine-Drug Interactions: Mechanisms, Clinical Relevance and Risk Stratification-A Narrative Review (2026) · cites this paper as [118]
The anchor evidence for berberine-drug interactions is the interaction with cyclosporine, demonstrated clinically in renal-transplant recipients.
“The anchor evidence is the interaction with cyclosporine, demonstrated clinically in renal-transplant recipients.”
From Berberine-Drug Interactions: Mechanisms, Clinical Relevance and Risk Stratification-A Narrative Review (2026) · cites this paper as [118]
A synthesis resting on three human studies cannot support strong statements about effect size in practice, whatever the mechanistic literature suggests.
“A synthesis resting on three human studies cannot support strong statements about effect size in practice, whatever the mechanistic literature suggests [35,83,118].”
From Berberine-Drug Interactions: Mechanisms, Clinical Relevance and Risk Stratification-A Narrative Review (2026) · cites this paper as [118]
Across the whole field, the paper identified one controlled study in patients (renal-transplant recipients receiving cyclosporine), one probe-cocktail study in healthy volunteers, and one human enzyme-phenotyping study; everything else is preclinical, in vitro or observational.
“Across the whole field we identified one controlled study in patients, in renal-transplant recipients receiving cyclosporine, one probe-cocktail study in healthy volunteers, and one human enzyme-phenotyping study; everything else is preclinical, in vitro or observational.”
From Berberine-Drug Interactions: Mechanisms, Clinical Relevance and Risk Stratification-A Narrative Review (2026) · cites this paper as [118]
The clinical anchor evidence on cyclosporine and the torsades de pointes signals compel a reassessment of the perception of harmlessness.
“The clinical anchor evidence on cyclosporine and the torsades de pointes signals compel a reassessment of the perception of harmlessness [39,118].”
From Berberine-Drug Interactions: Mechanisms, Clinical Relevance and Risk Stratification-A Narrative Review (2026) · cites this paper as [118]
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References 26 · Cited by 90
- Authors
- Wu, X., Li, Q., Xin, H., Yu, A., & Zhong, M.
- Affiliations
- Wuhan General Hospital of Guangzhou (CN)
- Corresponding author
- Wu, Xiaochun
- Venue
- European Journal of Clinical Pharmacology
- Published
- 2005-08-26
- Volume
- 61
- Issue
- 8
- Pages
- 567-572
- ISSN
- 0031-6970 (ISSN-L)
- 1432-1041
- OpenAlex
- W2015154953
- Cited by
- 90
- References
- 26
- Citations by year
- 2026: 6 · 2025: 2 · 2024: 3 · 2023: 7 · 2022: 4 · 2021: 3 · 2020: 7 · 2019: 4 · 2018: 3 · 2017: 5 · 2016: 8 · 2015: 2 · 2014: 7 · 2013: 4 · 2012: 11
- FWCI
- 1.13
- Type
- journal article
- Language
- en
- Open access
- closed
- Licence
- www.springer.com/tdm (tdm)
- Locations
- European Journal of Clinical Pharmacology (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Transplantation › Renal Transplantation Outcomes and Treatments
- Health Sciences › Medicine › Pharmacology › Berberine and alkaloids research
- Health Sciences › Medicine › Oncology › Drug Transport and Resistance Mechanisms
- Keywords
- berberine, cyclosporine, drug-drug interactions, kidney transplantation, pharmacokinetics, trough concentration, bioavailability, drug clearance, immunosuppressive therapy, liver and kidney function, half-life, area under the curve, dose proportionality, renal function decline, peak-to-valley ratio
- MeSH terms
- Adult, Antidiarrheals, Berberine, Drug Interactions, Female, Humans, Male, Medicine, Chinese Traditional, Middle Aged, Kidney Transplantation, Cyclosporine
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