Effects of solifenacin succinate (YM905) on detrusor overactivity in conscious cerebral infarcted rats

Suzuki, Michitaka; Ohtake, Akiyoshi; Yoshino, Taiji; Yuyama, Hironori; Hayashi, Aska; Ukai, Masashi; Okutsu, Hiroko; Noguchi, Yukiko; Sato, Shuichi; Sasamata, Masao

doi:10.1016/j.ejphar.2005.02.023

Cited by 31 publications

(17 citation statements)

References 18 publications

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“…In contrast, many studies using either normal healthy or diseased rodent models did not show any bladder capacity increase with antimuscarinics or showed an increase only at the high doses (Sasaki et al, 1997;Angelico et al, 2005;Ohtake et al, 2007;Hegde et al, 2009;Nagabukuro et al, 2010), which were much higher than therapeutic doses. Only in certain disease models, such as cerebral infarction, did antimuscarinics, including tolterodine and solifenacin, increase bladder capacity at reasonable doses from clinical use of these drugs (Suzuki et al, 2005). Our results are consistent with previous observations, but we have tested multiple antimuscarinics with different subtype selectivity and evaluated their pharmacokinetics.…”

supporting

confidence: 80%

Comparative Analysis of the Effects of Antimuscarinic Agents on Bladder Functions in Both Nonhuman Primates and Rodents

Nagabukuro¹,

Villa²,

Wickham³

et al. 2011

J Pharmacol Exp Ther

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Both the physiological role of muscarinic receptors for bladder function and the therapeutic efficacy of antimuscarinic agents for overactive bladder syndrome are well documented. We investigated the effect of antimuscarinic agents with different subtype selectivity on urodynamic parameters in nonhuman primates and rodents and compared plasma levels of these agents between species. Anesthetized rhesus monkeys were transurethrally catheterized, and the bladder was infused with saline. Urodynamic parameters were measured before and after intravenous drug administration. Tolterodine (nonselective) and oxybutynin (moderately M 3 -selective) increased bladder capacity at lower doses than those required to decrease micturition pressure. However, higher doses of darifenacin (M 3 -selective) were needed to increase the bladder capacity than those needed to decrease the micturition pressure. In rats, tolterodine had no effect on the bladder capacity but decreased the micturition pressure at all of the doses administered. Oxybutynin also decreased micturition pressure and increased bladder capacity at the highest dose. Plasma levels of these drugs overlap in both species. These results suggest that, in addition to the M 3 receptor, other muscarinic receptor subtypes contribute to regulate bladder storage function in nonhuman primates, since less subtype-selective tolterodine and oxybutynin showed higher specificity to the bladder capacity effect than the effect on micturition pressure compared with M 3 -selective darifenacin. In addition, the role of muscarinic receptors in bladder storage function varies between primates and rodents. Compared with rodents, muscarinic receptors may play a more active role during the storage phase to regulate the functional bladder capacity in primates.

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supporting

confidence: 80%

Comparative Analysis of the Effects of Antimuscarinic Agents on Bladder Functions in Both Nonhuman Primates and Rodents

Nagabukuro¹,

Villa²,

Wickham³

et al. 2011

J Pharmacol Exp Ther

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“…The effective dose levels of solifenacin succinate, tolterodine tartrate, and propiverine hydrochloride required to increase bladder capacity in the present study were almost consistent with those in the previous reports using normal rats (Hedlund et al 2007;Nomura et al 1989;Ohtake et al 2007), while the effective dose levels of solifenacin succinate and tolterodine tartrate in the present study were different from those in the previous reports using a rat model of OAB induced by cerebral infarction (Suzuki et al 2005;Yokoyama et al 2005). Additionally, the shapes of dose-response curves in terms of bladder capacity increase seem to be relatively steeper in normal rats than in a rat model of OAB in the previous reports (Nomura et al 1989;Ohtake et al 2007;Suzuki et al 2005;Yokoyama et al 2005).…”

Section: Discussioncontrasting

confidence: 54%

In vivo bladder selectivity of imidafenacin, a novel antimuscarinic agent, assessed by using an effectiveness index for bladder capacity in rats

Yamazaki¹,

Muraki²,

Anraku³

2011

Naunyn-Schmiedeberg's Arch Pharmacol

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Imidafenacin (KRP-197) is a novel antimuscarinic agent for overactive bladder treatment. The inhibitory effect of imidafenacin on detrusor contraction has been adopted for assessing their bladder selectivity, but this is becoming less convincing as an effectiveness index. We, therefore, reevaluated the bladder selectivity of imidafenacin and other antimuscarinics using their effects on the bladder capacity as an effectiveness index. Bladder capacity was measured by intermittent cystometry in urethane-anesthetized rats. In the tissues related to antimuscarinic side effects, the inhibitory actions were measured each on salivary secretion by electrical stimulation of chorda tympani, on rhythmical contractions in colon, and on carbamylcholine-induced bradycardia. Imidafenacin, solifenacin succinate, tolterodine tartrate, and propiverine hydrochloride significantly increased the bladder capacity, with minimum effective doses of 0.003, 1, 0.03, and 3 mg/kg (i.v.), respectively. The antimuscarinics tested, except for propiverine hydrochloride, shared a common property of increasing bladder capacity at a dose which did not affect micturition pressure. The relative bladder selectivity of imidafenacin, solifenacin succinate, and tolterodine tartrate was 15-, 1.7-, and 2.5-fold higher over salivary gland; 150-, 1.9-, and 9.2-fold higher over colon; and 50-, 12-, and 4.6-fold higher over heart, respectively, than that of propiverine hydrochloride. Thus, imidafenacin shows the most highly selective for bladder over the tissues related to major antimuscarinic side effects, compared to the other three well-known antimuscarinics tested in the rat.

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“…SOL is a novel muscarinic receptor antagonist and previous findings have suggested that SOL is able to improve detrusor overactivity without causing urinary retention (18). The pharmacological and clinical profile of SOL has indicated that SOL may be a promising drug in the treatment of patients with overactive bladder syndrome, which could be regarded as a novel therapeutic agent for patients with an overactive bladder (19,20).…”

Section: Discussionmentioning

confidence: 99%

Clinical optimal dose of solifenacin succinate forï¿½nursing patients after transurethral resection of the prostate during the perioperative period

Zhang

Jia

et al. 2017

Exp Ther Med

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Abstract. Transurethral plasma kinetic resection is an efficient and safe surgery for the treatment of benign prostatic hyperplasia. Solifenacin succinate (SOL) is safe and clinically efficient for patients who endure transurethral resection of the prostate (TURP) during the perioperative period. The objective of this study was to evaluate the clinical optimal dose of SOL for nursing patients after TURP during the perioperative period.

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Effects of solifenacin succinate (YM905) on detrusor overactivity in conscious cerebral infarcted rats

Cited by 31 publications

References 18 publications

Comparative Analysis of the Effects of Antimuscarinic Agents on Bladder Functions in Both Nonhuman Primates and Rodents

Comparative Analysis of the Effects of Antimuscarinic Agents on Bladder Functions in Both Nonhuman Primates and Rodents

In vivo bladder selectivity of imidafenacin, a novel antimuscarinic agent, assessed by using an effectiveness index for bladder capacity in rats

Clinical optimal dose of solifenacin succinate forï¿½nursing patients after transurethral resection of the prostate during the perioperative period

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