Comparison of the Effects of Pilocarpine Solution and Tablet on Salivary Flow Rate

  • Park, Jo-Eun (Department of Oral Medicine, College of Dentistry, Dankook University) ;
  • Song, Chan-Woo (Department of Oral Medicine, College of Dentistry, Dankook University) ;
  • Kim, Ki-Suk (Department of Oral Medicine, College of Dentistry, Dankook University) ;
  • Kim, Mee-Eun (Department of Oral Medicine, College of Dentistry, Dankook University)
  • 투고 : 2014.12.30
  • 심사 : 2015.01.20
  • 발행 : 2015.03.30


Purpose: Pilocarpine has the effects on improvement of salivary flow and subjective symptoms for xerostomic patients. Because of unwanted side effects following its systemic administration, topical pilocarpine has been paid attention as an alternative. This study aimed to investigate effects of pilocarpine solution as mouthwash on salivary flow and adverse effects compared to systemic administration of 5 mg pilocarpine tablet in healthy subjects. Methods: The study was a double blind, placebo-controlled, crossover clinical trial. Five milligrams pilocarpine tablets, 4 mL of 2% pilocarpine solution and placebo solution were given to 12 healthy volunteers (6 males and 6 females) in a predetermined order with wash-out period of at least two days and unstimulated whole saliva was collected before and after administration of each drug. Blood pressure and pulse rate was also measured and subjective effect and potential side effects were evaluated by a self-administrated questionnaire. Results: Systemic (5 mg tablet) and topical (2% solution) use of pilocarpine significantly increased salivary flow rate in healthy subjects compared to placebo (p<0.001). In both the pilocarpine solution and tablet groups, salivary flow rates at 120 minutes after administration remained increased. Subjective effect on salivation was the largest in the pilocarpine tablet group, followed by the pilocarpine solution group (p<0.05). There was no significant difference in blood pressure and pulse rate after administration of all three drugs. Fewer side effects reported in the pilocarpine solution group than in the tablet group. Conclusions: Two percents pilocarpine solution as mouthwash increases salivary flow rate, definitely superior to placebo solution and comparable to pilocarpine tablet, with fewer side effects in healthy subjects. It indicates a possibility of pilocarpine solution as a useful alternative of pilocarpine tablets for the xerostomic patients with systemic diseases.


  1. Mandel ID. Sialochemistry in diseases and clinical situations affecting salivary glands. Crit Rev Clin Lab Sci 1980;12:321-366.
  2. Sreebny LM. Xerostomia: diagnosis, management, clinical complications. In: Edgar WM, O'Mullane DM, eds. Saliva and oral health. 2nd ed. London: British Dental Association; 1996. pp. 43-46.
  3. Ishii M, Kurachi Y. Muscarinic acetylcholine receptors. Curr Pharm Des 2006;12:3573-3581.
  4. Frydrych AM, Davies GR, Slack-Smith LM, Heywood J. An investigation into the use of pilocarpine as a sialagogue in patients with radiation induced xerostomia. Aust Dent J 2002;47:249-253.
  5. Hamlar DD, Schuller DE, Gahbauer RA, et al. Determination of the efficacy of topical oral pilocarpine for postirradiation xerostomia in patients with head and neck carcinoma. Laryngoscope 1996;106:972-976.
  6. Lockhart PB, Fox PC, Gentry AC, Acharya R, Norton HJ. Pilot study of controlled-release pilocarpine in normal subjects. Oral Surg Oral Med Oral Pathol Oral Radiol Endod 1996;82:517-524.
  7. Berk L. Systemic pilocarpine for treatment of xerostomia. Expert Opin Drug Metab Toxicol 2008;4:1333-1340.
  8. Bernardi R, Perin C, Becker FL, et al. Effect of pilocarpine mouthwash on salivary flow. Braz J Med Biol Res 2002;35:105-110.
  9. Taweechaisupapong S, Pesee M, Aromdee C, Laopaiboon M, Khunkitti W. Efficacy of pilocarpine lozenge for post-radiation xerostomia in patients with head and neck cancer. Aust Dent J 2006;51:333-337.
  10. Mikhail AR, inventor. Pilocarpine mouthwash for dry mouth relief. United States patent US 4,209,505. 1980 Jun 24.
  11. Kim JH, Park JH, Kwon JS, Ahn HJ. Effect of pilocarpine mouthwash on xerostomia. Korean J Oral Med 2011;36:21-24.
  12. Fox PC, Atkinson JC, Macynski AA, et al. Pilocarpine treatment of salivary gland hypofunction and dry mouth (xerostomia). Arch Intern Med 1991;151:1149-1152.
  13. Wiseman LR, Faulds D. Oral pilocarpine: a review of its pharmacological properties and clinical potential in xerostomia. Drugs 1995;49:143-155.
  14. Ferguson MM. Pilocarpine and other cholinergic drugs in the management of salivary gland dysfunction. Oral Surg Oral Med Oral Pathol 1993;75:186-191.
  15. Peters GR, Novak E, Batts DH, Bye A, Nichols DJ, Francom SF. Multiple-dose, double-blind, placebo controlled intravenous tolerance and pharmacokinetic study of trospectomycin sulfate (U-63, 366F) in healthy male volunteers. Int J Clin Pharmacol Ther Toxicol 1990;28:361-368.
  16. Aromdee C, Ferguson MM, Ledger R, Wall J. A pilot study of the disposition of pilocarpine in plasma, saliva and urine after a single oral dose. Eur J Pharm Sci 1999;8:81-83.
  17. Hearnden V, Sankar V, Hull K, et al. New developments and opportunities in oral mucosal drug delivery for local and systemic disease. Adv Drug Deliv Rev 2012;64:16-28.
  18. Zimmerman RP, Mark RJ, Tran LM, Juillard GF. Concomitant pilocarpine during head and neck irradiation is associated with decreased posttreatment xerostomia. Int J Radiat Oncol Biol Phys 1997;37:571-575.
  19. Fox PC. Salivary enhancement therapies. Caries Res 2004;38:241-246.
  20. Fox PC, van der Ven PF, Baum BJ, Mandel ID. Pilocarpine for the treatment of xerostomia associated with salivary gland dysfunction. Oral Surg Oral Med Oral Pathol 1986;61:243-248.
  21. Salagen tablet. In: Physician's desk reference: PDR. 51th ed. Montvale: Medical Economics Books; 1997. pp. 1546-1547.
  22. Aframian DJ, Helcer M, Livni D, Robinson SD, Markitziu A, Nadler C. Pilocarpine treatment in a mixed cohort of xerostomic patients. Oral Dis 2007;13:88-92.
  23. Tsifetaki N, Kitsos G, Paschides CA, et al. Oral pilocarpine for the treatment of ocular symptoms in patients with Sjogren's syndrome: a randomised 12 week controlled study. Ann Rheum Dis 2003;62:1204-1207.