Blood concentration of cevimeline hydrochloride hydrate after oral rinsing

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  • MATSUBARA Makoto
    Department of Oral and Maxillofacial Surgery, Division of Oral Pathogenesis and Disease Control, Asahi University School of Dentistry
  • SHIKIMORI Michio
    Department of Oral and Maxillofacial Surgery, Division of Oral Pathogenesis and Disease Control, Asahi University School of Dentistry
  • FUJIMOTO Masako
    Department of Oral and Maxillofacial Surgery, Division of Oral Pathogenesis and Disease Control, Asahi University School of Dentistry
  • OHTA Takahisa
    Department of Oral and Maxillofacial Surgery, Division of Oral Pathogenesis and Disease Control, Asahi University School of Dentistry
  • TANAKA Shiro
    Department of Oral and Maxillofacial Surgery, Division of Oral Pathogenesis and Disease Control, Asahi University School of Dentistry
  • SUMITOMO Shinichiro
    Department of Oral and Maxillofacial Surgery, Division of Oral Pathogenesis and Disease Control, Asahi University School of Dentistry

Bibliographic Information

Other Title
  • セビメリン塩酸塩水和物による口腔リンス法後の血中濃度の推移
  • セビメリン エンサンエン スイワブツ ニ ヨル コウコウ リンスホウ ゴ ノ ケッチュウ ノウド ノ スイイ

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Description

Cevimeline hydrochloride hydrate (cevimeline) is used in the treatment of xerostomia associated with Sjogren's syndrome. However, this medication has muscarinic agonist activity and is associated with several adverse effects, including nausea, vomiting, and diarrhea. Oral rinsing with cevimeline is recommended to avoid these adverse effects, but cevimeline blood concentration after rinsing has not been thoroughly investigated. This study measured blood cevimeline concentration after oral rinsing at a concentration of 30 mg in 50 ml of water and determined that the maximum plasma concentration of 4.04 ± 1.10 ng/ml occurred two hours later, which is longer than the time to maximum concentration after an oral administration of 30 mg. Furthermore, the maximum concentration after rinsing was 5.5% of the maximum concentration after oral administration, and the half-life after rinsing was 6 hours, which is longer than the half-life after oral administration.

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