Abstract
Aims. This serendipitous study revealed an unexpected effect of Jufeng grape juice on the CYP1A2-mediated metabolism of phenacetin. Investigation of the inhibition of CYP1A2 by grapefruit juice was involved but a translation error led to the grape juice substitution. Methods. Twelve healthy subjects took a single oral dose of phenacetin (900 mg) on two randomized occasions together with 200 ml water or grape juice. Plasma phenacetin and paracetamol concentrations were assessed by h.p.l.c. Results. Ingestion of grape juice was associated with reduced plasma phenacetin concentrations, while paracetamol levels were unaffected. Paracetamol to phenacetin AUC ratios increased from 13.9 ± 3.1 to 24.3 ± 3.8 after ingestion of grape juice. Conclusions. These findings suggest enhanced first-pass metabolism of phenacetin, due to CYP1A2 activation by grape juice or to desaturation of CYP1A2 isoenzymes secondary to a slower rate of phenacetin absorption.
| Original language | English |
|---|---|
| Pages (from-to) | 638-640 |
| Number of pages | 3 |
| Journal | British Journal of Clinical Pharmacology |
| Volume | 48 |
| Issue number | 4 |
| DOIs | |
| Publication status | Published - 1999 |
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Keywords
- Cytochrome CYP1A2
- Drug metabolism
- Grape juice
- Paracetamol
- Phenacetin
ASJC Scopus subject areas
- Pharmacology (medical)
- Pharmacology, Toxicology and Pharmaceutics(all)
Cite this
Possible enhancement of the first-pass metabolism of phenacetin by ingestion of grape juice in Chinese subjects. / Xiao Dong, S.; Zhi Ping, Z.; Zhong Xiao, W.; Chong Shu, C.; Fattore, C.; Gatti, G.; D'Urso, S.; Perucca, E.
In: British Journal of Clinical Pharmacology, Vol. 48, No. 4, 1999, p. 638-640.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Possible enhancement of the first-pass metabolism of phenacetin by ingestion of grape juice in Chinese subjects
AU - Xiao Dong, S.
AU - Zhi Ping, Z.
AU - Zhong Xiao, W.
AU - Chong Shu, C.
AU - Fattore, C.
AU - Gatti, G.
AU - D'Urso, S.
AU - Perucca, E.
PY - 1999
Y1 - 1999
N2 - Aims. This serendipitous study revealed an unexpected effect of Jufeng grape juice on the CYP1A2-mediated metabolism of phenacetin. Investigation of the inhibition of CYP1A2 by grapefruit juice was involved but a translation error led to the grape juice substitution. Methods. Twelve healthy subjects took a single oral dose of phenacetin (900 mg) on two randomized occasions together with 200 ml water or grape juice. Plasma phenacetin and paracetamol concentrations were assessed by h.p.l.c. Results. Ingestion of grape juice was associated with reduced plasma phenacetin concentrations, while paracetamol levels were unaffected. Paracetamol to phenacetin AUC ratios increased from 13.9 ± 3.1 to 24.3 ± 3.8 after ingestion of grape juice. Conclusions. These findings suggest enhanced first-pass metabolism of phenacetin, due to CYP1A2 activation by grape juice or to desaturation of CYP1A2 isoenzymes secondary to a slower rate of phenacetin absorption.
AB - Aims. This serendipitous study revealed an unexpected effect of Jufeng grape juice on the CYP1A2-mediated metabolism of phenacetin. Investigation of the inhibition of CYP1A2 by grapefruit juice was involved but a translation error led to the grape juice substitution. Methods. Twelve healthy subjects took a single oral dose of phenacetin (900 mg) on two randomized occasions together with 200 ml water or grape juice. Plasma phenacetin and paracetamol concentrations were assessed by h.p.l.c. Results. Ingestion of grape juice was associated with reduced plasma phenacetin concentrations, while paracetamol levels were unaffected. Paracetamol to phenacetin AUC ratios increased from 13.9 ± 3.1 to 24.3 ± 3.8 after ingestion of grape juice. Conclusions. These findings suggest enhanced first-pass metabolism of phenacetin, due to CYP1A2 activation by grape juice or to desaturation of CYP1A2 isoenzymes secondary to a slower rate of phenacetin absorption.
KW - Cytochrome CYP1A2
KW - Drug metabolism
KW - Grape juice
KW - Paracetamol
KW - Phenacetin
UR - http://www.scopus.com/inward/record.url?scp=0032827826&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0032827826&partnerID=8YFLogxK
U2 - 10.1046/j.1365-2125.1999.00065.x
DO - 10.1046/j.1365-2125.1999.00065.x
M3 - Article
C2 - 10583039
AN - SCOPUS:0032827826
VL - 48
SP - 638
EP - 640
JO - British Journal of Clinical Pharmacology
JF - British Journal of Clinical Pharmacology
SN - 0306-5251
IS - 4
ER -