Pilot study of controlled-release pilocarpine in normal subjects

• Published in: Oral surgery, oral medicine, oral pathology, oral radiology and endodontics Vol. 82; no. 5; pp. 517 - 524
• Main Authors: Lockhart, Peter B., Fox, Philip C., Gentry, Anne C., Acharya, Ramesh, Norton, H. James
• Format: Journal Article
• Language: English
• Published: St. Louis, MO Mosby, Inc 01-11-1996; Elsevier
• Subjects: Adult; Analysis of Variance; Biological and medical sciences; Delayed-Action Preparations; Dentistry; Ent. Stomatology; Humans; Medical sciences; Parasympathomimetics - administration & dosage; Parasympathomimetics - blood; Parasympathomimetics - pharmacology; Parotid Gland - drug effects; Parotid Gland - metabolism; Pharmacology. Drug treatments; Pilocarpine - administration & dosage; Pilocarpine - blood; Pilocarpine - pharmacology; Pilot Projects; Saliva - metabolism; Secretory Rate - drug effects; Statistics, Nonparametric; Antiglaucomatous agent; Human; Immunopathology; Stomatology; Tolerance; Autoimmune disease; Pilocarpine; Experimental study; Sjögren syndrome; Parasympathomimetic; Eye disease; Chemotherapy; Treatment; Efficiency; Systemic disease; Secondary effect; Safety; Duration of action
• ISSN: 1079-2104; 1528-395X
• DOI: 10.1016/S1079-2104(96)80196-X

Current systemic treatments with sialogogues for patients with xerostomia are limited because of minimal efficacy, short duration of activity, or problems with side effects. The purpose of this pilot study was an initial assessment of safety, efficacy, duration of action, multiple dose tolerance, and side effects of a controlled-release formulation of pilocarpine hydrochloride.
Eight healthy hospitalized subjects were given 15 mg of a controlled-release pilocarpine formulation every 12 hours for three doses. Saliva and blood samples were collected at assigned intervals. Repeated measures analysis and paired
t tests were used for statistical analyses.
A significant (
p<0.05) increase in both parotid and whole saliva output followed all three doses beginning within 1 hour of dosing and lasting over 10 hours. Mean plasma pilocarpine concentration reached a maximum of 8.2 ng/ml at approximately 1 hour after the first dose, 11.5 ng/ml after the third dose, and declined to near baseline (0.06 ng/ml) 24 hours after the final dose. None of the participants showed evidence of adverse effects including complaints of sweating or gastrointestinal discomfort.
A controlled-release formulation of pilocarpine may overcome the therapeutic weaknesses of current pilocarpine preparations by prolonging salivary secretion and reducing undesirable side effects.