Tolterodine-A New Bladder-Selective Antimuscarinic Agent

Nilvebrant, Lisbeth; Andersson, Karin; Gillberg, P.-G.; Stahl, Matthias; Sparf, Bengt

doi:10.1016/s0022-5347(01)62872-6

Cited by 41 publications

(58 citation statements)

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“…In numerous in vitro functional studies ( Table 2), tolterodine showed comparable potency to oxybutynin for inhibition of carbachol-induced contractions of guinea-pig detrusor muscle [15] and human bladder [15,16]. Naerger et al [18] reported similar findings in bladder samples from patients with OAB.…”

Section: Antimuscarinic Activity In Vitro and In Vivomentioning

confidence: 79%

“…Tolterodine's 'bladder-selective' profile (mirrored by 5-HM) was subsequently shown in in vivo models [15,17]. In these studies, both tolterodine and 5-HM showed a more pronounced inhibitory effect on acetylcholine-induced bladder contraction than electrically stimulated salivation, whereas the converse was apparent for oxybutynin (Table 4).…”

Section: Antimuscarinic Activity In Vitro and In Vivomentioning

confidence: 92%

“…Tolterodine is a potent, competitive antagonist at muscarinic receptors [14][15][16] and demonstrates high affinity in the absence of selectivity for any particular muscarinic receptor subtype (Table 1) [14,15]. The major 5-hydroxymethyl metabolite (5-HM) of tolterodine (Figure 1) [14] (see section 5) exhibits a similar pharmacological profile [16,17].…”

Section: Antimuscarinic Activity In Vitro and In Vivomentioning

confidence: 99%

“…In vitro affinity (radioligand binding studies) § of tolterodine, 5-HM, oxybutynin and atropine for muscarinic receptors in guinea-pig tissues. Data from [15,17].…”

Section: Poor and Extensive Metabolisersmentioning

confidence: 99%

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Evidence for the efficacy and safety of tolterodine in the treatment of overactive bladder

Abrams

2001

Expert Opinion on Pharmacotherapy

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Overactive bladder (OAB) is a chronic and prevalent condition, the symptoms of which (urinary frequency and urgency, with or without urge incontinence) can exert a profound negative effect on a person's daily life activities. Tolterodine (Detrol in North America and Detrusitol in the rest of the world, Pharmacia), a competitive muscarinic antagonist, is the first agent of this class to be specifically developed for the treatment of OAB. This agent displays in vivo functional selectivity for the bladder over other tissues that contain muscarinic receptors (e.g., salivary glands, eye), which translates into good efficacy and tolerability in patients with OAB (including the elderly). Comparative, randomised, double-blind studies show that tolterodine (administered as immediate-release [IR] tablets 2 mg b.i.d.) is as effective as oxybutynin (5 mg t.i.d.) in improving all of the troublesome symptoms of OAB but with a significantly lower incidence and severity of dry mouth. The advent of a new extended-release (ER) capsule formulation of tolterodine (4 mg) for convenient once-daily treatment builds upon these findings, with significantly improved efficacy for reducing urge incontinence episodes and a lower frequency of dry mouth relative to the existing IR tablet (2 mg b.i.d.). Tolterodine can therefore be considered a valuable, well-tolerated treatment option for patients with OAB, providing improvements in symptoms that are both clinically meaningful to patients and sustained during long-term treatment.

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Section: Antimuscarinic Activity In Vitro and In Vivomentioning

confidence: 79%

Section: Antimuscarinic Activity In Vitro and In Vivomentioning

confidence: 92%

Section: Antimuscarinic Activity In Vitro and In Vivomentioning

confidence: 99%

“…In vitro affinity (radioligand binding studies) § of tolterodine, 5-HM, oxybutynin and atropine for muscarinic receptors in guinea-pig tissues. Data from [15,17].…”

Section: Poor and Extensive Metabolisersmentioning

confidence: 99%

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Evidence for the efficacy and safety of tolterodine in the treatment of overactive bladder

Abrams

2001

Expert Opinion on Pharmacotherapy

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“…24 Tolterodine Tolterodine is a competitive muscarinic receptor antagonist with relative functional selectivity for bladder muscarinic receptors 25 ; while it shows no specificity for receptor subtypes it does appear to target the bladder over the salivary glands. 26 The drug is metabolised in the liver to the 5-hydroxymethyl derivative, which is an active metabolite with a similar pharmacokinetic profile and is thought to contribute to the therapeutic effect. 27 Tolterodine is also available as an extended release once daily preparation, Detrusitol XL.…”

Section: Propiverinementioning

confidence: 99%

Management of overactive bladder syndrome

Srikrishna

Robinson

Cardozo

et al. 2007

Postgraduate Medical Journal

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Overactive bladder (OAB) syndrome is the term used to describe the symptom complex of urinary urgency with or without urge incontinence, usually with frequency and nocturia. Drug treatment continues to have an important role in the management of women with OAB. Other treatment options include conservative management with lifestyle interventions, modification of fluid intake, and physiotherapy including bladder retraining. Surgery remains the last resort in the treatment and is usually reserved for intractable detrusor overactivity, as it is associated with significant morbidity. This article reviews the management of the overactive bladder with specific focus on newer developments in the medical treatment of OAB in women.

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Combination of foot stimulation and tolterodine treatment eliminates bladder overactivity in cats

Schwen

Matsuta

Shen

et al. 2013

Neurourology and Urodynamics

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Aims To determine whether transcutaneous foot stimulation combined with a lower dose tolterodine would inhibit bladder overactivity more effectively than either treatment alone. Methods Cystometrograms were performed on α-chloralose anesthetized cats (N = 6) by infusing 0.25% acetic acid (AA) to induce bladder overactivity. Foot stimulation (5 Hz) was applied at 2 and 4 times the threshold (T) intensity in volts (i.e., 2T or 4T) for inducing toe movement to inhibit bladder overactivity. Cumulative doses of tolterodine (0.003–0.3 mg/kg, i.v.) were also administered to determine the effect of combination treatment. Results AA irritation of the bladder significantly (P < 0.0001) reduced bladder capacity to 23.6±7.1% of saline control capacity. Foot stimulation alone at 2T and 4T inhibited bladder overactivity and significantly (P < 0.0001) increased bladder capacity to 50.7±6.8% and 79.0±11.6% of saline control, respectively. Tolterodine alone at 0.3 mg/kg significantly (P < 0.05) increased bladder capacity to 65.6±15.5% of saline control. However, when tolterodine at a threshold dose (0.3 mg/kg) was combined with foot stimulation, the bladder capacity was significantly (P < 0.05) increased to 86.2±6.2% and 107.9±10.6% by 2T and 4T stimulation, respectively. Complete inhibition of bladder overactivity could be achieved at a lower tolterodine dose (0.1 mg/kg) when combined with 4T stimulation (97.0±11.2% of saline control). The amplitude of micturition contraction was not changed by tolterodine treatment. Conclusions This study suggests a novel, efficacious, non-invasive therapy by combining foot stimulation with a lower dose tolterodine to treat bladder overactivity. It also provides the first objective evidence supporting an additive therapeutic benefit of neuromodulation and antimuscarinic combination treatment.

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Tolterodine-A New Bladder-Selective Antimuscarinic Agent

Cited by 41 publications

References 0 publications

Evidence for the efficacy and safety of tolterodine in the treatment of overactive bladder

Evidence for the efficacy and safety of tolterodine in the treatment of overactive bladder

Management of overactive bladder syndrome

Combination of foot stimulation and tolterodine treatment eliminates bladder overactivity in cats

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