Pilot study of controlled-release pilocarpine in normal subjects

Lockhart, Peter B.; Fox, Philip C.; Gentry, Anne; Acharya, Ramesh Raj; Norton, H. James; Jacobson, Jed J.; Dis, Margot Van

doi:10.1016/s1079-2104(96)80196-x

Cited by 16 publications

(9 citation statements)

References 22 publications

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“…In previous studies, the pilocarpine-evoked saliva fluid secretion was examined in vivo by intravenous or intraperitoneal injection or oral administration of pilocarpine. After administration of pilocarpine, the plasma concentration of pilocarpine ranging from 4 nM to 0.81 μM induces saliva flow (5)(6)(7)(8)(9). In such experiments, threshold is lower than that in our experiments.…”

Section: Less Effect Of Tetrodotoxin On Pilocarpine-induced Salivary contrasting

confidence: 51%

Pilocarpine-induced salivary fluid secretion in the perfused submandibular gland of the rat

Narita

Saito

et al. 2009

J. Med. Invest.

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Xerostomia is the symptom of dry mouth often seen in patients who receive head and neck radiation therapy or in patients who have Sjögren's syndrome. The primary treatment to relieve xerostomia symptom is oral administration of pilocarpine, a parasympathomimetic agent with muscarinic action. Increase in salivary secretion induced by systemic administration of pilocarpine is considered to be mediated by actions on muscarinic cholinergic receptors in the central nervous system and salivary glands. In this study, we investigated the direct effect of pilocarpine on salivary fluid secretion in the isolated, perfused rat submandibular gland. Pilocarpine provoked salivary fluid secretion in a dose-dependent manner. The Na(+)-channel blocker tetrodotoxin had almost no effect on the pilocarpine-induced salivary fluid secretion, indicating that pilocarpine directly stimulates submandibular gland. Pilocarpine induced an increase in intracellular Ca(2+) concentration in dispersed submandibular gland cells at 37 degrees C, but not 25 degrees C. The salivary fluid secretion induced by pilocarpine was consisted of a rapid and transient phase and a subsequent sustained phase, which profile was different from that evoked by carbachol, another typical muscarinic agonist. Pilocarpine also induced Lucifer yellow secretion via paracellular route.

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Section: Less Effect Of Tetrodotoxin On Pilocarpine-induced Salivary contrasting

confidence: 51%

Pilocarpine-induced salivary fluid secretion in the perfused submandibular gland of the rat

Narita

Saito

et al. 2009

J. Med. Invest.

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“…In the field of pharmacological stimulation of salivary glands, slow release delivery systems for pilocarpine have been introduced 60. A significant increase in both whole and parotid salivary secretion lasting over 10 hours seems to be promising.…”

Section: Future Prospectsmentioning

confidence: 99%

Treatment of oral dryness related complaints (xerostomia) in Sjogren's syndrome

Reijden

Vissink

Veerman

et al. 1999

Annals of the Rheumatic Diseases

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Primary Sjögren's syndrome (SS) is a systemic autoimmune disorder characterised by a chronic, progressive loss of salivary and lacrimal function resulting in symptoms of oral and ocular dryness. The involvement of exocrine glands is the result of a focal, periductal mononuclear cell infiltrate and the subsequent loss of secretory epithelial cells.1 As a consequence, major changes occur in both the salivary flow rate and salivary composition. 2-9

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“…Though the rationale for topical administration of pilocarpine is to minimize adverse side effects of systemic pilocarpine, topical use is expected to offer some other benefits: there is mechanical salivary stimulation. [8][9][10][11][12] There exist a few studies concerning about topical use of pilocarpine. In 1980, topical use of pilocarpine was mentioned in a United States patent document, reporting that the 0.025% to 1% pilocarpine mouthwash was effective for dry mouth relief.…”

Section: Introductionmentioning

confidence: 99%

Dose- and Time-Related Effects of Pilocarpine Mouthwash on Salivation

Song¹,

Park²,

Kim³

et al. 2017

Journal of Oral Medicine and Pain

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Purpose: Pilocarpine as a salivation stimulant in pill form has mostly been used to relieve oral dryness for xerostomic patients but its use may often be limited due to variable side effects from systemic absorption. Therefore, the purpose of this study was to investigate the effects of pilocarpine mouthwash on salivation according to the variable concentration and duration for healthy volunteers. Related adverse effects and subjective assessment on its effects on salivation were also examined. Methods:This study was performed as placebo-controlled, double-blind, randomized clinical trial. Thirty healthy volunteers (male=23, mean age=22.2 years) were randomly allocated to 6 groups with the different concentration of pilocarpine mouthwash (placebo, 0.1%, 0.5%, 1.0%, 1.5%, and 2.0%). The whole experiment consisted of 3 sessions according to the duration of mouthwash, i.e., 1, 3, and 5 minutes with the mean wash-out period ≥2 days between the sessions. Unstimulated whole saliva was collected before and after gargling with a mouthwash.Results: Salivation of the higher concentration groups ≥1% significantly increased than those of lower concentration group. The application period of mouthwash did not cause any changes of salivary flow rate at the higher concentrations ≥1.0%. The lower concentrations of 0.5% and 0.1% had no effects on salivation even after 5-minute mouthwash. There was no significant difference between blood pressure and pulse rate before and after use of mouthwash. Conclusions:From the results of the current study, pilocarpine mouthwash with at least 1.0% concentration more than a minute might be clinically effective in salivation without any serious side effects. Dose of mouthwash rather than duration seems to be a critical factor to salivation.

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Pilot study of controlled-release pilocarpine in normal subjects

Cited by 16 publications

References 22 publications

Pilocarpine-induced salivary fluid secretion in the perfused submandibular gland of the rat

Pilocarpine-induced salivary fluid secretion in the perfused submandibular gland of the rat

Treatment of oral dryness related complaints (xerostomia) in Sjogren's syndrome

Dose- and Time-Related Effects of Pilocarpine Mouthwash on Salivation

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