The cholinesterase inhibitor physostigmine for the local treatment of dry mouth: a randomized study

Abstract

Application of physostigmine to the oromucosal surface with the aim of stimulating underlying mucin-producing glands while reducing cholinergic systemic effects might be a strategy for treating dry mouth. Subjects suffering from dry mouth and with hyposalivation participated in a crossover, double-blind, randomized study. A gel containing physostigmine (0.9, 1.8, 3.6, and 7.2 mg) or placebo was applied to the inside of the lips and distributed with the tongue. The feeling of dryness was assessed using a visual analogue scale (VAS) (where a score of 100 = extremely dry) and systemic effects were registered. Based on assessments of efficacy and safety, the dose of 1.8 mg of physostigmine was selected for use in the second part of the study to make objective measurements of saliva volumes. Physostigmine (1.8 mg) produced long-lasting (120 min) relief (evident as a score reduction of 25 on the VAS) in the feeling of dryness. Judging from AUC values related to baseline over 180 min, the improvement for both mouth and lips in response to physostigmine was six times greater than that to placebo. At higher doses of physostigmine, gastrointestinal discomfort predominantly occurred. The volume of saliva collected in response to physostigmine was five times higher over 180 min than that collected in response to placebo. Physostigmine, applied locally, therefore appears to be a promising modality for dry-mouth treatment.

The diagnostic suitability of a xerostomia questionnaire and the association between xerostomia, hyposalivation and medication use in a group of nursing home residents

“…This phenomenon has also been reported in several previous studies [1, 11, 31, 42]. It has been suggested that the menopause and female hormone oestrogen are influencing the salivary function in common with many other physiological and psychological functions.…”

“…Also gustatory and mechanical salivary stimulating techniques may be helpful to relieve the feelings of xerostomia, such as consuming sugar-free chewing gum, candies, and mints, as well as acidic drinks and foods [30, 45]. Systemic medication of pilocarpine or cevimeline or application of physostigmine to the oral mucosal surface may improve saliva secretion, but the possible side effects should be determined and, if possible, anticipated or controlled [42, 46, 47]. When stimulating salivary secretion is not possible or not adequate, symptomatic relief of the oral complaints becomes the primary management strategy.…”

Efficacy of a newly developed mouth gel for xerostomia relief—A randomized double‐blind trial

“…Further research should focus on other symptom‐relieving systems, such as intraoral relieving devices or containers and new methods with focus on the underlying reasons for xerostomia. Promising and innovative methods have been presented over recent years (Alajbeg et al, ; Khosravani, Birkhed, & Ekstrom, ; Strietzel et al, ). Due to their relatively short time span of symptom relief, it remains questionable whether the mouth gels investigated in our study should be used for whole‐day symptom relief; instead, they could be used for short‐term relief of symptoms in planned situations (e.g.…”

Is rivastigmine safe as pretreatment against nerve agents poisoning? A pharmacological, physiological and cognitive assessment in healthy young adult volunteers

“…Sialometry results can be parsimoniously explained by the summation of two opposing effects: decreased salivation during stress and increased salivation following ChE inhibition (Hugo et al, 2008;Khosravani et al, 2009). The stress associated with the study induced decreased salivation, as is evident in the placebo group, and this was counteracted by rivastigmine.…”