Cevimeline

A muscarinic receptor agonist

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5mg

￥1137.00

910.00

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10mg

￥1650.00

1320.00

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50mg

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Background

Cevimeline is a muscarinic receptor agonist especially on the M1 and M₃ receptors. [1]

Cevimeline has been approved for use against symptoms of dry mouth by activating the M₃ receptors of the parasympathetic nervous system. Cevimeline is effective and safe in improving symptoms of dry eye with 20 mg three times per day [2]. Cevimeline increased the intracellular Ca⁺ level in parotid gland acinar cells over 1 μM and rat, enhanced the excitability via muscarinic receptors, thereby, cevimeline alleviates dry mouth symptoms by stimulating secretion by the salivary glands. Cevimeline has a longer duration of salivation[3]. Cevimeline plays a part in Alzheimer’s disease. Cevimeline decreased Aβ (1–40) level in the cerebrospinal fluid (CSF) at 1 mg/kg without changing α-APPs in rabbit and significantly decreased CSF Aβ in AD patients.[4]

参考文献:
1.?F. B. Vivino, I. Al-Hashimi, Z. Khan, F. G. LeVeque, P. L. Salisbury, 3rd, T. K. Tran-Johnson, C. C. Muscoplat, M. Trivedi, B. Goldlust and S. C. Gallagher, Arch Intern Med 1999, 159, 174-181.
2.?M. Ono, E. Takamura, K. Shinozaki, T. Tsumura, T. Hamano, Y. Yagi and K. Tsubota, Am J Ophthalmol 2004, 138, 6-17.
3.?K. Ono, T. Inagaki, T. Iida, R. Hosokawa and K. Inenaga, J Med Invest 2009, 56 Suppl, 375.
4.?A. Fisher, Z. Pittel, R. Haring, N. Bar-Ner, M. Kliger-Spatz, N. Natan, I. Egozi, H. Sonego, I. Marcovitch and R. Brandeis, J Mol Neurosci 2003, 20, 349-356.