Inhibition of chlorzoxazone metabolism, a clinical probe for CYP2E1, by a single ingestion of watercress

Leclercq, Isabelle;Horsmans, Yves;Desager, Jean-Pierre
(1998) Clinical Pharmacology and Therapeutics — Vol. 64, n° 2, p. 144-149 (1998)

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To investigate the effect of watercress on the metabolism of chlorzoxazone, an in vivo probe for CYP2E1, the oral pharmacokinetics of chlorzoxazone was studied in 10 healthy volunteers before and after a single ingestion of a watercress homogenate (50 gm). A third chlorzoxazone pharmacokinetic study was performed after a 1-week treatment with isoniazid (300 mg/day), a well-known CYP2E1 inhibitor. Ingestion of watercress or isoniazid did not affect the oral absorption of chlorzoxazone. The area under the chlorzoxazone plasma concentration-time curve was significantly increased by 56% (p < 0.05) after watercress ingestion and by 135% (p < 0.001) with isoniaxid treatment. Similarly, chlorzoxazone elimination half-life was prolonged after watercress (53%; p < 0.05) and isoniazid (104%; p < 0.01) administration. These results show that a single ingestion of watercress inhibits the hydroxylation of chlorzoxazone, an in vivo probe for CYP2E1.
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Leclercq, I., Horsmans, Y., & Desager, J.-P. (1998). Inhibition of chlorzoxazone metabolism, a clinical probe for CYP2E1, by a single ingestion of watercress. Clinical Pharmacology and Therapeutics, 64(2), 144-149. https://hdl.handle.net/2078.5/62708 (Original work published 1998)