Once Daily Controlled Versus Immediate Release Oxybutynin Chloride for Urge Urinary Incontinence

Abstract

Participants taking a single daily does of controlled release oxybutynin had similar reductions in urge incontinence and total incontinence episodes compared to those taking oxybutynin 1 to 4 times daily. A lower incidence of dry mouth was reported for controlled release oxybutynin.

Muscarinic receptors: their distribution and function in body systems, and the implications for treating overactive bladder

“…Figure 3 shows the difference between the IR and ER versions of oxybutynin and tolterodine in terms of serum concentrations of drug over a 24‐h period (Gupta & Sathyan, 1999; Olsson & Szamosi, 2001; Appell et al ., 2003). There is some evidence, for each drug, that once‐daily dosing of the ER preparation leads to a modest increase in efficacy and a decrease in side effects (Table 3) (Anderson et al ., 1999; Gupta & Sathyan, 1999; Appell et al ., 2001; Olsson & Szamosi, 2001; Van Kerrebroeck et al ., 2001; Appell et al ., 2003; Barkin et al ., 2004; Product Information (Ditropan/Ditropan XL), 2004; Product Information, Detrol (US), 2005; Product Information, Ditropan (US), 2005). No information is available on the proportion of patients who would prefer to receive treatment when needed rather than as continuous therapy.…”

Muscarinic receptor antagonists for overactive bladder

“…Dry mouth is probably a consequence of antagonism of the M 3 receptors that regulate salivary secretion in the parotid glands [8,117]. In placebo‐ and active‐controlled trials, the incidence of dry mouth in patients taking oxybutynin IR was 17–97%, oxybutynin ER 23–68%, transdermal oxybutynin 4–39%, propiverine IR 20–47%, propiverine ER 22%, tolterodine IR 8–50%, tolterodine ER 7–34%, trospium 3–41%, solifenacin 8–30%, and darifenacin 18–31% generally exceeded the combined incidence of constipation, headache, and abnormal vision (Table 4[109,112,116,126–141] and Table 5[142–162]). In the Chapple et al .…”

“…Constipation is generally the second most common AE reported by patients receiving oxybutynin IR (4–50%), transdermal oxybutynin (1–21%), propiverine IR (4–17%), propiverine ER (3%), tolterodine ER (3–8%), solifenacin (3–13%), and darifenacin (14–22%). Constipation was reported by 0–8% of patients administered tolterodine IR and 7–10% of those receiving trospium (Table 4[109,112,116,126–141] and Table 5[142–162]). The higher rates of constipation in patients treated with darifenacin compared with other antimuscarinics might be explained by its relatively high selectivity for the M 3 receptor [163], which regulates contraction of intestinal smooth muscle [140]; however, withdrawal rates due to constipation and laxative use among patients who received darifenacin were similar or only mildly elevated compared with those who received placebo [109,141].…”

α1‐Adrenoceptors and muscarinic receptors in voiding function – binding characteristics of therapeutic agents in relation to the pharmacokinetics

“…Oxybutynin was widely used to treat OAB, but its use was often limited by systemic side effects, such as dry mouth, blurred vision, constipation and tachycardia, which appear frequently in patients receiving oral oxybutynin [42]. To overcome these drawbacks, a controlled release dosage form and a transdermal therapeutic system were developed and clinically used, with the advantage of a lower incidence of adverse effects than the immediate release form in patients with OAB [43–45]. These clinical observations coincide with the ex vivo data that oral but not transdermal oxybutynin produced a long‐lasting blockade of muscarinic receptors in the salivary gland [46].…”