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| Content Provider | World Health Organization (WHO)-Global Index Medicus |
|---|---|
| Author | Taesotikul, Theerada Nakajima, Miki Tassaneeyakul, Wichittra Yokoi, Tsuyoshi |
| Description | Country affiliation: Thailand Author Affiliation: Taesotikul T ( Department of Pharmacology, Faculty of Medicine, Khon Kaen University, Khon Kaen, Thailand.) |
| Abstract | Phyllanthus amarus, a commonly used medicinal herb, was investigated for possible herb-drug interactions. The effect on CYP3A-mediated drug metabolism in rats after single dose administration of P. amarus extract was investigated using midazolam (MDZ) as a probe substrate. The effect of multiple dose administration of P. amarus extract on activity and expression of various CYP isoforms were studied. Oral administration of P. amarus extract (800 mg/kg) 1 h before oral MDZ increased the C(max) and AUC(0--∞) of MDZ by 3.9- and 9.6-fold and decreased the clearance by 12%, but did not alter the pharmacokinetics of intravenous MDZ. Daily administration of P. amarus extract (200 or 800 mg/kg/day) for 15 days in rats increased the activity and expression of CYP3A and CYP2B1/2. In contrast, the activities and expressions of CYP1A, CYP2C and CYP2E1 were not significantly changed. The dual effects of P. amarus extract on CYP enzymes were demonstrated. Single dose administration of the extract increased oral bioavailability of MDZ through inhibition of intestinal CYP3A whereas repeated administration of the extract slightly induced hepatic CYP3A and CYP2B1/2 in rats, which suggested that herb-drug interactions by P. amarus may potentially occur via CYP3A and 2B. |
| File Format | HTM / HTML |
| ISSN | 00498254 |
| Issue Number | 7 |
| Volume Number | 42 |
| e-ISSN | 13665928 |
| Journal | Xenobiotica |
| Language | English |
| Publisher | Taylor & Francis |
| Publisher Date | 2012-07-01 |
| Publisher Place | Great Britain (UK) |
| Access Restriction | One Nation One Subscription (ONOS) |
| Subject Keyword | Discipline Toxicology Cytochrome P-450 Enzyme System Metabolism Midazolam Pharmacokinetics Phyllanthus Plant Preparations Administration & Dosage Animals Biological Availability Herb-drug Interactions Liver Male Pharmacology Rats Rats, Sprague-dawley Journal Article Research Support, Non-u.s. Gov't |
| Content Type | Text |
| Resource Type | Article |
| Subject | Health, Toxicology and Mutagenesis Medicine Biochemistry Toxicology Pharmacology |
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