The recovery time‐course of CYP3A after induction by St John's wort administration

Imai, Hiromitsu; Kotegawa, Tsutomu; Tsutsumi, Kimiko; Morimoto, Takahiro; Eshima, Nobuoki; Nakano, Shigeyuki; Ohashi, Kyoichi

doi:10.1111/j.1365-2125.2008.03120.x

Cited by 53 publications

(30 citation statements)

References 26 publications

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“…The magnitude of this interaction has been reported to decline over 3 to 7 d for CYP3A4 substrates such as simvastatin, midazolam, and triazolam. 19,20) The results of our pharmacokinetic analysis of midazolam are consistent with those of previous analyses. Grapefruit juice interactions with OATPs expressed in the intestine may be mediated through inhibition of transporter activity rather than through a reduction in protein expression.…”

Section: Discussionsupporting

confidence: 90%

“…These reports show that for some drugs, the magnitude of interaction declines over several days, consistent with enzyme regeneration following inhibition. [17][18][19] However, little attention has been devoted to the duration of the interaction between OATP and grapefruit juice. Thus, our goal was to determine the duration of the inhibitory effect of grapefruit juice on OATP by comparison with the duration of the grapefruit juice-mediated effects on CYP3A4 activity.…”

mentioning

confidence: 99%

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Comparison of Inhibitory Duration of Grapefruit Juice on Organic Anion-Transporting Polypeptide and Cytochrome P450 3A4

Tanaka

Uchida

Miyakawa

et al. 2013

Biological & Pharmaceutical Bulletin

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Recently, a new type of interaction has been reported in which fruit juices diminish oral drug bioavailability through inhibition of organic anion-transporting polypeptide (OATP). In this study, we aimed to clarify the duration of OATP inhibition by grapefruit juice (GFJ), and to compare it with the duration of GFJ-induced inhibition of cytochrome P450 (CYP) 3A4 activity. Seven healthy volunteers were enrolled in this open-label, single-sequence study. They were orally administered celiprolol (100 mg) and midazolam (15 µg/kg) with water on the control day. Three days later, they ingested GFJ (200 mL) 3 times a day for 3 d. On day 1, the same drugs were administered with GFJ. On days 3 and 7, the same drugs were administered with water. Pharmacokinetics of both drugs were evaluated on each trial day. The peak plasma concentration (C max ) and the area under the plasma concentration-time curve from 0 to 8 h (AUC 0-8 ) of celiprolol significantly decreased on day 1, and the mean ratios of these values and the corresponding control-day values were 0.18 and 0.25, respectively. The C max and AUC 0-8 returned to the control levels on days 3 and 7. In contrast, AUC 0-8 of midazolam were higher on days 1 and 3 than on the control day (mean ratio, 2.12 and 1.47, respectively). The AUC 0-8 returned to the control level on day 7. In conclusion, results of this study indicated that the OATP inhibition caused by GFJ dissipated faster than GFJ-mediated alterations in CYP3A4 activity, which were sustained for at least 48 h.Key words organic anion-transporting polypeptide; cytochrome P450; grapefruit juice Food and medication are often taken together. However, certain foods interact with drugs by altering mechanisms that are important determinants of systemic drug availability. In particular, grapefruit juice is known to alter the pharmacokinetics of over 30 prescription drugs by affecting their bioavailability.1-3) The mechanism of this interaction is inhibition of intestinal cytochrome P450 (CYP) 3A4 activity and increased systemic exposure of CYP3A4 substrates. [4][5][6][7][8] In 2012, the United States Food and Drug Administration issued a press release to warn consumers that the intake of grapefruit juice along with medication could cause dangerous side effects. 9)Recently, a new type of interaction has been reported in which fruit juices diminish oral drug bioavailability through inhibition of the organic anion-transporting polypeptide (OATP) uptake transporter, which is a family of membrane solute carrier (SLC) transporters. OATP influences the intestinal absorption of several drugs in clinical use. [10][11][12][13][14] Grapefruit juice decreases the plasma concentrations of some drugs including β-adrenoceptor blocking agents and antihistamines by this mechanism. For example, grapefruit juice was reported to reduce the area under the plasma concentration-time curve (AUC) value for fexofenadine to a mean value of 58% of that when the drug was administered with the corresponding volume of water.10) Furthermore, celiprolol, ...

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Section: Discussionsupporting

confidence: 90%

mentioning

confidence: 99%

Comparison of Inhibitory Duration of Grapefruit Juice on Organic Anion-Transporting Polypeptide and Cytochrome P450 3A4

Tanaka

Uchida

Miyakawa

et al. 2013

Biological & Pharmaceutical Bulletin

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“…Consistently, a number of clinical trials have shown that SJW decreased plasma levels of alprazolam (20) and midazolam (17,18,22,25,28,29,42) in healthy volunteers. Such effect is not observed with low hyperforin-containing extracts (21) or after a short (i.e., 3 days) period (19) of treatment.…”

Section: Benzodiazepinesmentioning

confidence: 53%

“…Strong evidence from animal studies as well as preclinical and clinical studies suggests that SJW may modulate CYP activity. Using well-established probe drugs (e.g., alprazolam and midazolam for CYP3A4, caffeine for CYP1A2, chlorzoxazone for CYP2E1, dextromethorphan and debrisoquine for CYP2D6, tolbutamide for CYP2C9, and omeprazole for CYP2C19), a number of clinical trials have consistently shown that SJW induces CYP3A4, CYP2E1, and CYP2C19, with no effect on CYP1A2, CYP2D6, or CYP2C9 (16)(17)(18)(19)(20)(21)(22)(23)(24)(25)(26)(27)(28)(29)(30). Some authors have also suggested that SJW may induce CYP1A2 only in females (24).…”

Section: Influence Of St John's Wort On Cytochrome P450 Enzymes and Pmentioning

confidence: 99%

Herb–Drug Interactions with St John’s Wort (Hypericum perforatum): an Update on Clinical Observations

Borrelli

Izzo

2009

AAPS J

236

190

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Abstract. St John's wort (SJW) extracts, prepared from the aerial parts of Hypericum perforatum, contain numerous pharmacologically active ingredients, including naphthodianthrones (e.g., hypericin and its derivatives), phloroglucinols derivatives (e.g., hyperforin, which inhibits the reuptake of a number of neurotransmitters, including serotonin), and flavonoids. Such extracts are widely used for the treatment of mild-to-moderate depression. As a monotherapy, SJW has an encouraging safety profile. However, relevant and, in some case, life-threatening interactions have been reported, particularly with drugs which are substrate of cytochrome P450 and/or P-glycoprotein. Well-documented SJW interactions include (1) reduced blood cyclosporin concentration, as suggested by multiple case reports as well as by clinical trials, (2) serotonin syndrome or lethargy when SJW was given with serotonin reuptake inhibitors, (3) unwanted pregnancies in women while using oral contraceptives and SJW, and (4) reduced plasma drug concentration of antiretroviral (e.g., indinavir, nevirapine) and anticancer (i.e., irinotecan, imatinib) drugs. Hyperforin, which is believed to contribute to the antidepressant action of St John's wort, is also strongly suspected to be responsible of most of the described interactions.

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“…225 The inductive effects appear to last at least 7 days after stopping St John's wort but may last up to 30 days. 20,226 …”

Section: Human and Clinical Studiesmentioning

confidence: 99%

Drug—Botanical Interactions: A Review of the Laboratory, Animal, and Human Data for 8 Common Botanicals

2009

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Many Americans use complementary and alternative medicine (CAM) to prevent or alleviate common illnesses, and these medicines are commonly used by individuals with cancer. These medicines or botanicals share the same metabolic and transport proteins, including cytochrome P450 enzymes (CYP), glucuronosyltransferases (UGTs), and P-glycoprotein (Pgp), with over-thecounter and prescription medicines increasing the likelihood of drug-botanical interactions. This review provides a brief description of the different proteins, such as CYPs, UGTs, and Pgp. The potential effects of drug-botanical interactions on the pharmacokinetics and pharmacodynamics of the drug or botanical and a summary of the more common models used to study drug metabolism are described. The remaining portion of this review summarizes the data extracted from several laboratory, animal, and clinical studies that describe the metabolism, transport, and potential interactions of 8 selected botanicals. The 8 botanicals include black cohosh, Echinacea, garlic, Gingko biloba, green tea, kava, milk thistle, and St John's wort; these botanicals are among some of the more common botanicals taken by individuals with cancer. These examples are included to demonstrate how to interpret the different studies and how to use these data to predict the likelihood of a clinically significant drug-botanical interaction.

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The recovery time‐course of CYP3A after induction by St John's wort administration

Cited by 53 publications

References 26 publications

Comparison of Inhibitory Duration of Grapefruit Juice on Organic Anion-Transporting Polypeptide and Cytochrome P450 3A4

Comparison of Inhibitory Duration of Grapefruit Juice on Organic Anion-Transporting Polypeptide and Cytochrome P450 3A4

Herb–Drug Interactions with St John’s Wort (Hypericum perforatum): an Update on Clinical Observations

Drug—Botanical Interactions: A Review of the Laboratory, Animal, and Human Data for 8 Common Botanicals

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