Cevimeline hydrochloride

CAS No. : 107220-28-0

Cevimeline hydrochloride,107220-28-0
Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000332
Synonyms:AF 102B;SNI 2011;SNK 508
Molecular Formula:C10H17NOS HCl
Molecular Weight:235.8
Target:M3 receptor
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Appearance:A crystalline solid
Cat No:I000332
Cas No:107220-28-0
Product-Name:Cevimeline hydrochloride

Cevimeline hydrochloride(cas 107220-28-0) is a parasympathomimetic and muscarinic agonist, with particular effect on M3 receptors; used in the treatment of dry mouth associated with sjogren/'s syndrome.

1. Arch Intern Med. 2002 Jun 10;162(11):1293-300.
Cevimeline for the treatment of xerostomia in patients with Sjögren syndrome: a randomized trial.
Fife RS(1), Chase WF, Dore RK, Wiesenhutter CW, Lockhart PB, Tindall E, Suen JY.
Author information:
(1)Department of Medicine, Indiana University School of Medicine, 535 Barnhill Dr, Room 150, Indianapolis, IN 46202, USA.
BACKGROUND: Cevimeline hydrochloride is a cholinergic agent with muscarinic agonist activity prominently affecting the M1 and M3 receptors prevalent in exocrine glands. We evaluated the safety and efficacy of cevimeline in the treatment of xerostomia in patients with Sjögren syndrome. METHODS: Seventy-five patients with Sjögren syndrome and associated salivary gland dysfunction were enrolled in a double-blind, randomized, placebo-controlled trial at 8 university- and office-based outpatient clinical facilities in the United States. Eligible study participants were randomized to receive 30 mg of cevimeline 3 times daily, 60 mg of cevimeline 3 times daily, or placebo for 6 weeks. Subjective responses were determined using global patient evaluation and visual analog scales. Salivary flow was measured objectively. RESULTS: Sixty-one participants completed the study. Patients in both cevimeline groups had significant improvements in dry mouth, as indicated by symptoms, salivary flow, and use of artificial saliva, compared with the placebo group. The drug was generally well tolerated, with expected adverse events resulting from the drug/'s muscarinic agonist action. Fourteen patients withdrew from the study because of adverse events, the most frequent being nausea. CONCLUSIONS: Therapy with cevimeline, 30 mg 3 times daily, seems to be well tolerated and to provide substantive relief of xerostomia symptoms. Although both dosages of cevimeline provided symptomatic improvement, 60 mg 3 times daily was associated with an increase in the occurrence of adverse events, particularly gastrointestinal tract disorders. Use of 30 mg of cevimeline provides a new option for the treatment of xerostomia in Sjögren syndrome.
2. Arthritis Rheum. 2002 Mar;46(3):748-54.
A double-blind, randomized, placebo-controlled study of cevimeline in Sjögren/'s syndrome patients with xerostomia and keratoconjunctivitis sicca.
Petrone D(1), Condemi JJ, Fife R, Gluck O, Cohen S, Dalgin P.
Author information:
(1)Baylor University Medical Center and Arthritis Centers of Texas, Dallas 75246, USA. trone6534@aol.com
OBJECTIVE: To evaluate the safety and efficacy of 2 dosages of cevimeline for the treatment of xerostomia and keratoconjunctivitis sicca in patients with Sjögren/'s syndrome.
METHODS: A 12-week double-blind, randomized, placebo-controlled study was performed. Patients were randomly assigned to receive either placebo, 15 mg of cevimeline 3 times daily, or 30 mg of cevimeline 3 times daily. Patients were evaluated at baseline and throughout the study for their global assessment of dryness (mouth, eyes, overall) as well as their subjective assessment of the specific symptoms of dry mouth and dry eyes. Total saliva and tear flow also were measured.
RESULTS: Patients taking 30 mg of cevimeline 3 times daily had statistically significant improvements in their subjective global assessment of dry eyes (P = 0.0453), dry mouth (P = 0.0004), and increased salivary flow (P = 0.007). Patients receiving the 30-mg dosage also showed greater objective improvement (increased salivary and lacrimal flow rates, as measured by Schirmer/'s test) than did patients receiving placebo. Frequently reported adverse events included headache, increased sweating, abdominal pain, and nausea. CONCLUSION: Treatment with cevimeline at a dosage of 30 mg 3 times daily resulted in substantive improvement by increasing the rate of saliva and tear flow in patients with Sjögren/'s syndrome, as well as improving subjective symptoms of dry mouth, dry eyes, and overall dryness. The 15-mg dosage relieved some symptoms, and both dosages were well tolerated.
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