A study of the effectiveness and side effects of salivation-inducers in patients with Sjögren’s syndrome ～ Comparison between cevimeline hydrochloride and pilocarpine hydrochloride ～

Abstract

Abstract:Objectives: Cevimeline hydrochloride （CH） and pilocarpine hydrochloride （PH） are recognized as salivation-inducers with a high affinity for M3 muscarinic receptors. However, these drugs have a high frequency of side effects, including digestive symptoms and hyperhidrosis. We compared the effectiveness and side effects of these two drugs before and after a medication change.Materials and Methods: Seventy-six patients with Sjögren' s syndrome were divided into the following four groups: 1） CH group, CH was administered for 12 months; 2） PH group, PH was administered for 12 months; 3） CH-PH group, CH was administered for 6 months followed by PH for 6 months; 4） PH-CH group, PH was administered for 6 months followed by CH for 6 months. We measured the salivary flow rate and recorded the subjective symptoms in each group.Results: In each group, stimulated whole saliva （SWS） and unstimulated whole saliva （UWS） significantly increased after 3 months and 6 months, respectively, and subjective symptoms improved after 3 months. The incremental changes in both SWS and UWS did not differ significantly between the groups. The CH and PH groups both had digestive symptoms （32.3% and 32.1%, respectively） and hyperhidrosis （29.0% and 39.3%, respectively） . We found no significant difference in salivary flow rate or subjective symptoms after the medication change. However, the frequencies of side effects in the CH-PH and PH-CH groups decreased significantly for both digestive symptoms （9.7% and 10.7%, respectively） and hyperhidrosis （25.8% and 14.3%, respectively） .Conclusions: After changing the salivation-inducing drug, there was no significant difference in salivary function or subjective symptoms, while the frequency of side effects markedly decreased. These results suggest that changing the salivation-inducing drug effectively reduces side effects.

Safety of Pilocarpine Therapy in Patients With Sjögren’s Syndrome: A Single-Arm Interventional, Post-Market Surveillance Study

“…The frequency of AEs due to pilocarpine treatment may be reduced by starting with a low dose (e.g., 5 mg once or twice daily), and then increasing the dose gradually until the maintenance dose of 5 mg QID is achieved. According to a previous study, gastrointestinal adverse events caused by pilocarpine treatment tended to decrease over time, but not for sweating [23]. The dosing frequency used in our study ranged from once daily to QID.…”

“…Based on the assumption of the distinctive safety profiles between pilocarpine and cevimeline, the eligible subjects in the Japanese study were divided into four groups, with two groups receiving pilocarpine first and then cevimeline and vice versa. The frequencies of AEs including digestive symptoms and increased sweating decreased significantly in those two groups [23]. Thus, prescribing either pilocarpine or cevimeline is beneficial to patients with Sjögren's syndrome.…”

“…In a study conducted in the National Taiwan University Hospital, 5 patients (21.7%) in the pilocarpine group experienced sweating, and 3 of them withdrew from the study [19]. A stepup dosing study in Japan found that 39.3% of subjects receiving pilocarpine experienced sweating [23]. Adequate patient education for sweating may be important for improving patient compliance after pilocarpine treatment.…”