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Published Online, 8 February 2005, www.theannals.com, DOI 10.1345/aph.1E486.
The Annals of Pharmacotherapy: Vol. 39, No. 3, pp. 567-571. DOI 10.1345/aph.1E486
© 2005 Harvey Whitney Books Company.
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Improvement of Dry Mouth by Replacing Paroxetine with Fluvoxamine

Yuka Arima, BSc

Department of Medico-Pharmaceutical Sciences, Graduate School of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan

Chiharu Kubo, MD PhD

Professor, Department of Psychosomatic Medicine, Graduate School of Medical Sciences, Kyushu University

Masayuki Tsujimoto, MS (Pharm)

Assistant, Department of Medico-Pharmaceutical Sciences, Graduate School of Pharmaceutical Sciences, Kyushu University

Hisakazu Ohtani, PhD

Associate Professor, Department of Medico-Pharmaceutical Sciences, Graduate School of Pharmaceutical Sciences, Kyushu University

Yasufumi Sawada, PhD

Professor, Department of Medico-Pharmaceutical Sciences, Graduate School of Pharmaceutical Sciences, Kyushu University

Reprints: Dr. Sawada, Department of Medico-Pharmaceutical Sciences, Graduate School of Pharmaceutical Sciences, Kyushu University, 3-1-1 Maidashi, Higashi-ku, Fukuoka 812-8582, Japan, fax 81-92-642-6614, sawada{at}phar.kyushu-u.ac.jp

OBJECTIVE: To present a case of improvement of paroxetine-induced dry mouth by substitution of fluvoxamine and analyze this case based on receptor occupancy theory.

CASE SUMMARY: A 66-year-old woman with major depressive disorder had been treated with brotizolam 0.5 mg/day, flunitrazepam 2 mg/day, sulpiride 100 mg/day, bromazepam 2 mg/day, trazodone 25 mg/day, and paroxetine hydrochloride 10 mg/day. Although her psychological symptoms improved gradually, she complained of dry mouth. Paroxetine was replaced with fluvoxamine maleate 50 mg/day, and the dryness disappeared within a month.

DISCUSSION: We calculated the time courses of muscarinic acetylcholine (mACh) receptor occupancy after oral administration of paroxetine and fluvoxamine at the treatment doses by using pharmacokinetic parameters obtained from the literature. The mACh receptor occupancy was estimated to be decreased from 0.22% to 0.020% by replacing paroxetine with fluvoxamine.

CONCLUSIONS: The improvement of dry mouth observed after the replacement of paroxetine with fluvoxamine in this patient may have been due to a decrease in the mACh receptor occupancy.

Key Words: dry mouth, fluvoxamine, paroxetine

Published Online, February 8, 2005. www.theannals.com, DOI 10.1345/aph.1E486





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