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Local treatment of dry mouth by the cholinesterase inhibitor physostigmine

Conference paper
Authors Nina Khosravani
Dowen Birkhed
Jörgen Ekström
Published in 8th European Symposium on Saliva, Eeegmond oon Zee, Netherlands,14-17 june 2008
Publication year 2008
Published at Institute of Odontology
Institute of Neuroscience and Physiology, Department of Pharmacology
Language en
Subject categories Pharmacology and Toxicology, Physiology


The feeling of mouth moistness is associated with the continuous secretion of mucin from submucosal minor glands, rather than with deficits in the watery saliva intermittently secreted from the major glands (Sreebny & Broich, 1988). Animal studies show physostigmine, applied on the oral mucosa, to enhance the cholinergic tone in the submucosal mucin-producing glands underlying the physostigmine-exposed mucosa (Ekström & Helander, 2002). Topical application of physostigmine, aiming at stimulating minor glands while at the same time minimising systemic cholinergic effects, would therefore be an advantageous approach to the treatment of mouth dryness. Presently, twenty subjects suffering from dry mouth participated, in a crossover double blind, randomized study. Physostigmine was applied onto the inside of the lips, at different doses (0.9 mg, 1.8 mg, 3.6 mg and 7.2 mg), while the vehicle served as placebo; the solution (300 ul) was distributed with the tongue. As significantly marked relief of the dry-mouth-feeling (score reduction by 25). Placebo, caused just a transient, initial, decrease in scores (by 7). Since doses above 1.8 mg were assiciated with signs of systemic effects, predominantly gastrointestinal discomfort, the dose 1.8 mg was used for objective assessment of secretion in those subjects previously tested. The volumes of saliva collected after physostigmine were significantly larger than those after placebo; the mean AUC-value (above baseline) over 180 min was almost 5 times that of placebo. Thus, physostigmine locally applied seems promising in the treatment of dry mouth.

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