PMID- 11394733 OWN - NLM STAT- MEDLINE DCOM- 20011011 LR - 20190921 IS - 0149-2918 (Print) IS - 0149-2918 (Linking) VI - 23 IP - 5 DP - 2001 May TI - A comparison of the effects on saliva output of oxybutynin chloride and tolterodine tartrate. PG - 753-60 AB - BACKGROUND: Oxybutynin chloride and tolterodine tartrate are anticholinergic agents used to suppress involuntary bladder contractions in urinary incontinence. They act by inhibiting binding of acetylcholine to the muscarinic receptors in the detrusor muscle of the bladder. The same types of muscarinic receptors are found in the salivary glands; thus anticholinergic agents may decrease saliva production and cause dry mouth, a commonly cited reason for discontinuation of therapy. OBJECTIVE: The primary objective of this study was to compare saliva output, which is an objective measure of dry mouth, in subjects taking immediate- or extended-release oxybutynin, tolterodine, or placebo. METHODS: This was a single-site, single-dose, randomized, double-blind, 4-treatment, 4-period crossover study. Subjects were randomly assigned to 1 of 4 treatment sequences that included extended-release oxybutynin 10 mg, tolterodine 2 mg, immediate-release oxybutynin 5 mg, and placebo. Saliva output was measured objectively before dosing with each treatment and at 0.5, 1, 2, 3, 4, 6, 8, 10, and 12 hours after dosing. RESULTS: Thirty-six healthy adult volunteers (22 women and 14 men) participated in the study. They ranged in age from 19 to 42 years (mean, 27 years). Thirty-one were white, 3 Asian, and 2 black. There were no significant differences in predose saliva output between the 4 study groups. With placebo, saliva output increased throughout the day. Saliva output was maintained at predose levels throughout the day with extended-release oxybutynin. Two hours after dosing with tolterodine and immediate-release oxybutynin, saliva output decreased nearly 0.5 g in specimens collected over 2 minutes. All 3 active treatments were associated with lower saliva output compared with placebo. Extended-release oxybutynin and tolterodine were similar with respect to area under the saliva concentration-time curve but were associated with significantly greater saliva output than was immediate-release oxybutynin (P < 0.01). There were no serious adverse events (AEs) in this study. AEs were similar between treatments, although the incidence of headache was higher in the active-treatment groups than with placebo. CONCLUSIONS: Objective assessment of saliva output in healthy adult volunteers indicated that extended-release oxybutynin and tolterodine had less impact on saliva output than did conventional immediate-release oxybutynin, suggesting that they may yield lower levels of dry mouth. FAU - Chancellor, M B AU - Chancellor MB AD - Department of Urology, University of Pittsburgh School of Medicine, Pennsylvania 15213, USA. chancellormb@msx.upmc.edu FAU - Appell, R A AU - Appell RA FAU - Sathyan, G AU - Sathyan G FAU - Gupta, S K AU - Gupta SK LA - eng PT - Clinical Trial PT - Comparative Study PT - Journal Article PT - Randomized Controlled Trial PT - Research Support, Non-U.S. Gov't PL - United States TA - Clin Ther JT - Clinical therapeutics JID - 7706726 RN - 0 (Benzhydryl Compounds) RN - 0 (Cholinergic Antagonists) RN - 0 (Cresols) RN - 0 (Mandelic Acids) RN - 0 (Tartrates) RN - 33RU150WUN (Phenylpropanolamine) RN - 5T619TQR3R (Tolterodine Tartrate) RN - K9P6MC7092 (oxybutynin) SB - IM CIN - J Urol. 2005 Aug;174(2):588-9. PMID: 16006904 MH - Adult MH - Area Under Curve MH - Benzhydryl Compounds/adverse effects/*pharmacology MH - Cholinergic Antagonists/adverse effects/*pharmacology MH - Cresols/adverse effects/*pharmacology MH - Cross-Over Studies MH - Double-Blind Method MH - Female MH - Headache/chemically induced MH - Humans MH - Male MH - Mandelic Acids/adverse effects/*pharmacology MH - *Phenylpropanolamine MH - Saliva/metabolism MH - Salivation/*drug effects MH - Tartrates/adverse effects/*pharmacology MH - Tolterodine Tartrate EDAT- 2001/06/08 10:00 MHDA- 2001/10/12 10:01 CRDT- 2001/06/08 10:00 PHST- 2001/06/08 10:00 [pubmed] PHST- 2001/10/12 10:01 [medline] PHST- 2001/06/08 10:00 [entrez] AID - S0149291801800242 [pii] AID - 10.1016/s0149-2918(01)80024-2 [doi] PST - ppublish SO - Clin Ther. 2001 May;23(5):753-60. doi: 10.1016/s0149-2918(01)80024-2.