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Continence
Published in Andrew Stevens, James Raftery, Jonathan Mant, Sue Simpson, Health Care Needs Assessment, 2018
Catherine W. McGrother, Madeleine Donaldson
Tolterodine has functional selectivity for muscarinic receptors in the bladder compared to the salivary gland. Given in a dose of 2 mg twice per day, there seems to be similar efficacy between oxybutynin and tolterodine, but tolterodine had a more favourable side effect profile in terms of unwanted dry mouth and gastrointestinal effects resulting in less patients needing to stop therapy. Controlled-release tolterodine may have less adverse side effects (Table A4.7).
Substrates of Human CYP2D6
Published in Shufeng Zhou, Cytochrome P450 2D6, 2018
Tolterodine is a relatively new antimuscarinic drug that is used to treat urinary incontinence and other symptoms associated with overactive bladder (Wefer et al. 2001). Tolterodine acts on M1, M2, M3, M4, and M5 subtypes of muscarinic receptors. After oral administration, tolterodine is rapidly absorbed from the gastrointestinal tract and exhibits extensive first-pass metabolism. In humans, approximately 80% of an administered oral dose of tolterodine is excreted in the urine, the major metabolites being the 5-carboxylic acids of tolterodine, N-dealkylated tolterodine, and their glucuronides (Figure 3.92). Less than 1% of the parent compound is excreted unchanged. Tolterodine is mainly metabolized by CYP2D6 with significant contribution from CYP3A4 (Postlind et al. 1998). 5-Hydroxymethyltolterodine is the major metabolite in EMs but undetectable in the plasma of PMs (Brynne et al. 1998, 1999a,b; Olsson and Szamosi 2001a). Although tolterodine concentrations are increased 5- to 10-fold in PMs, the summed active moieties did not differ between EMs and PMs (Brynne et al. 1999a,b; Olsson and Szamosi 2001a,b). This suggests that therapeutic effects would not differ significantly between the two groups, and there is no convincing evidence of an important gene-effect correlation (Brynne et al. 1998).
Urinary Incontinence
Published in David M. Luesley, Mark D. Kilby, Obstetrics & Gynaecology, 2016
Dudley Robinson, Linda Cardozo
Tolterodine has also been developed as an extended-release once-daily preparation. A double-blind multicentre trial of 1235 women has compared extended-release tolterodine to immediate-release tolterodine and placebo. Whilst both formulations were found to reduce the mean number of urge incontinence episodes per week the extended-release preparation was found to be significantly more effective.115
Ocular adverse effects of bladder medication: a systematic review
Published in Cutaneous and Ocular Toxicology, 2022
Arshpreet Bassi, Daiana Roxana Pur, Anthony Chifor, Monali S. Malvankar-Mehta
The anti-muscarinic medications included the largest variation in adverse vision effects which is categorised over 13 types of ocular symptoms (Table 3). Alton-Yaycioglu et al.11, Hsiao, Lin and Kuo20, and Junemann et al.22 reviewed the effects of Tolterodine and highlighted that blurred vision, burning, dry eyes, and foreign body sensation was the most common ocular AEs reported. Patients that took oxybutynin had the same AEs as Totlerodine which included blurred vision, burning, dry eyes, and foreign body sensation, as reported by Alton-Yaycioglu et al.11, Hsiao, Lin and Kuo20, and Wagg et al.30. The most common AE reported by users of Solfenacin Succinate was blurred vision, followed by dry eyes, glaucoma, and other eye disorders, as highlighted in the articles of Sekeroglu et al.3, Chu, Smith, and Uchida14, Gratzke et al.17, Haab et al.18, Hsiao, Lin and Kuo20, Sand et al.28, Swift et al.29, and Waag et al.30.
The clinical pharmacology of the medical treatment for overactive bladder in adults
Published in Expert Review of Clinical Pharmacology, 2020
Hadi Mostafaei, Shahrokh F. Shariat, Hanieh Salehi-Pourmehr, Florian Janisch, Keiichiro Mori, Fahad Quhal, Sakineh Hajebrahimi
Many factors may play a role in the pathophysiology of OAB [24]. The two phases of micturition including storage and periodic elimination of urine depend on the coordinated activity of the urinary bladder and urethral sphincters. This coordination is mediated by a complex neural control system in the brain, the spinal cord, and the peripheral ganglia [29]. Any disruption in this pathway can lead to bladder overactivity. Alteration of N-Methyl-D-aspartic acid glutamatergic mechanisms, dopamine D2 receptor excitatory mechanisms, dopaminergic–glutamatergic interactions in the brain and central mechanism sensitive to nitric oxide are associated with OAB symptoms. In addition, 5-hydroxymethyl tolterodine (5-HMT) has an inhibitory effect on bladder sensory function in pathophysiological conditions. It inhibits mechanosensitive bladder afferent activity of capsaicin-sensitive C fibers by blocking bladder muscarinic receptors (but not Aδ-fibers or capsaicin-insensitive C-fibers) [30].
Pharmacologic therapies for the management of non-neurogenic urinary incontinence in children
Published in Expert Opinion on Pharmacotherapy, 2019
Tiernan Middleton, Pamela Ellsworth
Tolterodine is a potent competitive muscarinic antagonist exhibiting some selectivity toward the antimuscarinic activity of the bladder (in animal models). It is FDA approved for use in adults with OAB symptoms. A Clinical Pharmacology and Biopharmaceutics Review of two pharmacokinetic (PK) safety studies, three pharmacokinetic/pharmacodynamic (PK/PD) studies, two phase III safety, and efficacy trials and two bioequivalence (BE) studies of the liquid formulation performed on 10 October 2003 concluded that tolterodine wasn’t shown to be effective in the pediatric population at the doses studied [59]. A total of four randomized controlled trials and 11 other clinical trials have been performed evaluating the use of tolterodine in children with symptoms of OAB and voiding dysfunction, dysfunctional voiding, and detrusor hyperreflexia. Two additional studies evaluated its use in nocturnal enuresis [59]. Two additional studies evaluated its use in nocturnal enuresis [37,39]. The chemical formula is C26H37NO7 (Figure 1).