The effects of Puerarin on CYP2D6 and CYP1A2 activities In vivo

Jiao, Zheng; Chen, Bin; Bing, Jiang; Zeng, Ling; Tang, Zhenchen; Li, Fan; Zhou, Hong‐Hao

doi:10.1007/s12272-010-0209-2

Cited by 30 publications

(15 citation statements)

References 14 publications

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“…An in vitro study showed puerarin and Radix Puerariae extract could enhance the activity of some cytochrome P450 enzymes, such as CYP 1A1/2, CYP 2A1, CYP 2C11, and inhibit CYP 2B1, CYP 2E1, and CYP 3A in Wistar rats . In addition, a clinical trial in vivo study indicated puerarin induced the expression of CYP 1A2 and inhibit the activity of CYP 2D6 . These findings suggests Radix Puerariae or its products, such as puerarin, extract or total flavones, may change the metabolism of substrates of the above mentioned CYP isoenzymes.…”

Section: Herb–drug Interactionsmentioning

confidence: 88%

RadixPuerariae: An overview of Its Chemistry, Pharmacology, Pharmacokinetics, and Clinical Use

Zhang

Lam

Zuo

2013

The Journal of Clinical Pharmacology

195

130

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Radix Puerariae has been traditionally used for the treatment of diarrhea, acute dysentery, deafness and cardiovascular diseases. Yege (Gegen or Radix Puerariae lobatae), the dried root of Pueraria lobata (Wild.) Ohwi, has been widely used in China and, to a lesser extent, in Japan, Korea, and the United States. Although they have been classified into different categories in Chinese Pharmacopoeia, Yege is often used interchangeably in practice with Fenge (Radix Puerariae thomsonii), which is the dried root of Pueraria thomsonii Benth. Among various commercially available products of Radix Puerariae, injection of puerarin, the major isoflavone from Radix Puerariae, has been most widely used as a vasodilator for the treatment of angina and myocardial infarction. Considering the extensive clinical usage and recent alert of fatal herb-drug interaction of Radix Puerariae, the current review is proposed to cover its traditional applications, pharmacological activities, pharmacokinetics, clinical efficacy, and potential herb-drug interactions aiming to fill in the information gaps of this herb for frontline practitioners. Although various small, poorly designed clinical trials have demonstrated the safety, efficacy, and significant clinical benefits of Radix Puerariae, prospective randomized controlled clinical trials are needed to further establish its effective and safe use.

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Section: Herb–drug Interactionsmentioning

confidence: 88%

RadixPuerariae: An overview of Its Chemistry, Pharmacology, Pharmacokinetics, and Clinical Use

Zhang

Lam

Zuo

2013

The Journal of Clinical Pharmacology

195

130

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“…The 12 h pharmacokinetics of omeprazole, midazolam, caffeine, and 0–8 h losartan/E-3174 as well as dextromethorphan/dextrorphan urinary ratio were measured. Midazolam/1′-hydroxymidazolam ratio at 1 h, caffeine/paraxanthine ratio at 6 h, and omeprazole/5′-hydroxyomeprazole ratio at 4 h in plasma were used as extra phenotypic indices [6–8] for quantifying corresponding enzyme activity change. Blood and urine samples were prepared as previously reported [6].…”

Section: Methodsmentioning

confidence: 99%

Repeated administration of berberine inhibits cytochromes P450 in humans

Guo

Chen

Tan

et al. 2011

Eur J Clin Pharmacol

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Purpose Berberine is a plant alkaloid that is widely used to treat gastrointestinal infections, diabetes, hypertension, and hypercholesterolemia. Many studies have reported interactions between berberine-containing products and cytochromes P450 (CYPs), but little is known about whether berberine alters CYP activities in humans, especially after repeated doses. Methods A two-phase randomized-crossover clinical study in healthy male subjects was performed. After 2 weeks of berberine (300 mg, t.i.d., p.o.) administration, midazolam, omeprazole, dextromethorphan, losartan, and caffeine were used to evaluate enzyme activities of CYP3A4, 2C19, 2D6, 2C9, and CYP1A2, respectively. Results A decrease in CYP2D6 activity was observed as the 0–8 h urinary dextromethorphan/dextrorphan increased ninefold (P<0.01). In addition, losartan/E-3174 ratio doubled (P<0.01) after BBR administration, indicating a decrease in CYP2C9 activity. CYP3A4 activity was also inhibited, as the Cmax, AUC0–∞, and AUC0–12 of midazolam were increased 38% (P<0.05), 40% (P<0.01), and 37% (P<0.05) after BBR treatment, respectively. Compared with the placebo period, the Tmax and T1/2 of midazolam during BBR administration were prolonged from 3.03±0.27 to 3.66±0.37 h and 0.66±0.08 to 0.99±0.09 h, respectively; the oral clearance of midazolam was decreased 27% (P< 0.05); and the phenotypic indices of 1 h midazolam/1′-hydroxymidazolam increased 59% (P<0.01). There were no statistically significant differences in the pharmacokinetic parameters of the other probe drugs between placebo and the BBR-treated group. Conclusions Repeated administration of berberine (300 mg, t.i.d., p.o.) decreased CYP2D6, 2C9, and CYP3A4 activities. Drug-drug interactions should be considered when berberine is administered.

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“…Puerarin (400 mg/d, i.v.) was given to eighteen healthy Chinese male volunteers for 10 days, and induced the expression of CYP 1A2 and declined the activity of CYP 2D6 (Zheng et al, 2010). In addition, administration of puerarin (200 mg/kg, i.g.)…”

Section: Potential Herb-drug Interactionsmentioning

confidence: 99%