Interaction of a caffeine overdose with clinical doses of contraceptive ethinyl estradiol in a young woman
Abstract Aim The overdose of caffeine, a cytochrome P450 1A2 probe, in young women has become a problem. The aim of this study was to evaluate possible drug interactions between intentionally overdosed caffeine (12 g) and oral contraceptive doses of ethinyl estradiol prescribed to a young woman in a...
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| Format: | Article |
| Language: | English |
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Wiley
2024-01-01
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| Series: | Acute Medicine & Surgery |
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| Online Access: | https://doi.org/10.1002/ams2.985 |
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| author | Koichiro Adachi Maki Murata Akiyoshi Inada Takeyori Morimoto Makiko Shimizu Satoru Beppu Hiroshi Yamazaki |
| author_facet | Koichiro Adachi Maki Murata Akiyoshi Inada Takeyori Morimoto Makiko Shimizu Satoru Beppu Hiroshi Yamazaki |
| author_sort | Koichiro Adachi |
| collection | DOAJ |
| description | Abstract Aim The overdose of caffeine, a cytochrome P450 1A2 probe, in young women has become a problem. The aim of this study was to evaluate possible drug interactions between intentionally overdosed caffeine (12 g) and oral contraceptive doses of ethinyl estradiol prescribed to a young woman in a suicide attempt. Methods The serum concentrations of caffeine in the patient and the time‐dependent ethinyl estradiol inhibition of caffeine oxidation in vitro were evaluated. Results The serum concentration of caffeine 4 h after overdose was 136 μg/mL; from the data obtained between 4 and 28 h after overdose, the half‐life was estimated to be 33 h, which is many times larger than the normal value. Prescribed ethinyl estradiol prolonged caffeine elimination in vivo and inhibited paraxanthine formation, as evidenced by the low serum concentrations. In human liver microsomes, ethinyl estradiol (50 nM) inhibited half of caffeine N3‐demethylation. Pre‐incubation of human liver microsomes with ethinyl estradiol resulted in a powerful time‐dependent inhibitory effect on caffeine N3‐demethylation in human liver microsomes. Conclusion These results suggest that a prescription history of contraceptives at clinical doses may have a strong effect on the pharmacokinetics of overdosed caffeine in young women, resulting in dangerous drug interactions. |
| format | Article |
| id | doaj-art-8da4ac54aafc46f0a455d99f3cfd3c1b |
| institution | Kabale University |
| issn | 2052-8817 |
| language | English |
| publishDate | 2024-01-01 |
| publisher | Wiley |
| record_format | Article |
| series | Acute Medicine & Surgery |
| spelling | doaj-art-8da4ac54aafc46f0a455d99f3cfd3c1b2024-12-30T10:18:37ZengWileyAcute Medicine & Surgery2052-88172024-01-01111n/an/a10.1002/ams2.985Interaction of a caffeine overdose with clinical doses of contraceptive ethinyl estradiol in a young womanKoichiro Adachi0Maki Murata1Akiyoshi Inada2Takeyori Morimoto3Makiko Shimizu4Satoru Beppu5Hiroshi Yamazaki6Laboratory of Drug Metabolism and Pharmacokinetics Showa Pharmaceutical University Machida, Tokyo JapanEmergency Medicine and Critical Care Department NHO Kyoto Medical Center Fushimi‐ku, Kyoto JapanPharmaceutical Department NHO Kyoto Medical Center Fushimi‐ku, Kyoto JapanPharmaceutical Department NHO Kyoto Medical Center Fushimi‐ku, Kyoto JapanLaboratory of Drug Metabolism and Pharmacokinetics Showa Pharmaceutical University Machida, Tokyo JapanEmergency Medicine and Critical Care Department NHO Kyoto Medical Center Fushimi‐ku, Kyoto JapanLaboratory of Drug Metabolism and Pharmacokinetics Showa Pharmaceutical University Machida, Tokyo JapanAbstract Aim The overdose of caffeine, a cytochrome P450 1A2 probe, in young women has become a problem. The aim of this study was to evaluate possible drug interactions between intentionally overdosed caffeine (12 g) and oral contraceptive doses of ethinyl estradiol prescribed to a young woman in a suicide attempt. Methods The serum concentrations of caffeine in the patient and the time‐dependent ethinyl estradiol inhibition of caffeine oxidation in vitro were evaluated. Results The serum concentration of caffeine 4 h after overdose was 136 μg/mL; from the data obtained between 4 and 28 h after overdose, the half‐life was estimated to be 33 h, which is many times larger than the normal value. Prescribed ethinyl estradiol prolonged caffeine elimination in vivo and inhibited paraxanthine formation, as evidenced by the low serum concentrations. In human liver microsomes, ethinyl estradiol (50 nM) inhibited half of caffeine N3‐demethylation. Pre‐incubation of human liver microsomes with ethinyl estradiol resulted in a powerful time‐dependent inhibitory effect on caffeine N3‐demethylation in human liver microsomes. Conclusion These results suggest that a prescription history of contraceptives at clinical doses may have a strong effect on the pharmacokinetics of overdosed caffeine in young women, resulting in dangerous drug interactions.https://doi.org/10.1002/ams2.985caffeineethinyl estradioloverdosepharmacokinetics |
| spellingShingle | Koichiro Adachi Maki Murata Akiyoshi Inada Takeyori Morimoto Makiko Shimizu Satoru Beppu Hiroshi Yamazaki Interaction of a caffeine overdose with clinical doses of contraceptive ethinyl estradiol in a young woman Acute Medicine & Surgery caffeine ethinyl estradiol overdose pharmacokinetics |
| title | Interaction of a caffeine overdose with clinical doses of contraceptive ethinyl estradiol in a young woman |
| title_full | Interaction of a caffeine overdose with clinical doses of contraceptive ethinyl estradiol in a young woman |
| title_fullStr | Interaction of a caffeine overdose with clinical doses of contraceptive ethinyl estradiol in a young woman |
| title_full_unstemmed | Interaction of a caffeine overdose with clinical doses of contraceptive ethinyl estradiol in a young woman |
| title_short | Interaction of a caffeine overdose with clinical doses of contraceptive ethinyl estradiol in a young woman |
| title_sort | interaction of a caffeine overdose with clinical doses of contraceptive ethinyl estradiol in a young woman |
| topic | caffeine ethinyl estradiol overdose pharmacokinetics |
| url | https://doi.org/10.1002/ams2.985 |
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