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Journal of Nippon Medical School

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-Case Reports-

Sialorrhea Successfully Treated by the Combined Use of Selective M1 and M3 Muscarinic Acetylcholine Receptor Antagonists

Yukie Yamamura and Manabu Nonaka

Department of Otolaryngology, Tokyo Women's Medical University


Sialorrhea is often treated with anticholinergic agents, but they can have undesirable side effects such as drowsiness, sedation, and constipation. Effective medication that acts selectively on the salivary glands is needed.
We report the case of a patient with sialorrhea who was successfully treated by the combined use of pirenzepine and solifenacin (M1 and M3 muscarinic receptor antagonists, respectively). The patient was a 51-year-old man with mean unstimulated and stimulated salivary flow rates per 10 min of 6.1 mL and 41.7 mL, respectively (both were measured three times). 99mTcO4− salivary gland scintigraphy revealed characteristic spontaneous saliva secretion without stimulation. He was treated with Scopolia extract, escitalopram, solifenacin succinate, and the combined administration of solifenacin succinate and pirenzepine. A statistically significant decrease was observed from the pre-medication unstimulated and stimulated salivary flow rates only following the combined administration of solifenacin and pirenzepine.
The major muscarinic receptor subtype expressed in the salivary glands is M3; however, M1 is also present. A study using knockout mice demonstrated that the presence of either M1 or M3 receptors was sufficient for salivation. Thus, the combined use of selective M1 and M3 antagonists could provide a good treatment option for sialorrhea.

J Nippon Med Sch 2019; 86: 117-121

Keywords
sialorrhea, M1 and M3 muscarinic receptor antagonists, 99mTcO4− salivary gland scintigraphy

Correspondence to
Yukie Yamamura, Department of Otolaryngology, Tokyo Women's Medical University, 8-1 Kawada-Cho, Shinjuku-ku, Tokyo 162-8666, Japan
yukie@fd5.so-net.ne.jp

Received, May 28, 2018
Accepted, September 26, 2018