Fesoterodine for the treatment of overactive bladder: pharmacological bases and clinical results

Kuzmin, Igor V.; Валентинович, Кузьмин Игорь; Аль-Шукри, С Х; Хасунович, Аль-Шукри Сальман

doi:10.17816/uroved102163-171

Cited by 6 publications

(2 citation statements)

References 52 publications

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“…Тропность к обоим указанным субтипам М-холинорецепторов обеспечивает торможение непроизвольных сокращений детрузора, блокирование механизмов, препятствующих его расслаблению, а также уменьшение чувствительности мочевого пузыря [23]. Можно констатировать, что двойной эффект контроля сократительной активности и чувствительности мочевого пузыря вследствие сбалансированной М2-и М3-рецепторной аффинности фезотеродина является важным фармакологическим преимуществом препарата [24].…”

Section: фезотеродинаunclassified

Anticholinergic therapy of an overactive bladder: clinical practice aspects

Kuzmin¹,

Кузьмина²

2021

Russian Medical Inquiry

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The review presents data on the epidemiology, clinical course and modern methods to the treatment of overactive bladder. It also describes the pharmacological bases of anticholinergic drug use, which are first-line in the treatment of this disease. The pharmacological and clinical aspects of the new M-holinoblocker, fesoterodine, are considered. The drug belongs to the competitive blockers of M2-and M3-cholinergic receptors. The conducted studies have shown the high clinical efficacy of fesoterodine. Due to the low lipophilicity and large molecular weight, the drug’s ability to penetrate the blood-brain barrier is minimal, which causes a low frequency of adverse events from the central nervous system. The pharmacokinetic and pharmacodynamic properties of fesoterodine allow it to be prescribed to "vulnerable" groups of patients — the elderly, patients with CNS diseases and cognitive disorders. According to the FORTA system, fesoterodine is the only antimuscarinic drug classified in category B. The results of a multiple-criteria decision-making showed a favorable benefit-risk profile of fesoterodine, prescribed according to a flexible dosage regimen of 4 mg and 8 mg. Important benefits of fesoterodine are the convenience of intake, the possibility of dose titration, as well as the ratio of treatment costs and its efficacy. The practical issues of using fesoterodine in various clinical cases are considered. KEYWORDS: overactive bladder, anticholinergic therapy, fesoterodine, multiple-criteria decision-making, FORTA classification. FOR CITATION: Kuzmin I.V., Kuzmina S.V. Anticholinergic therapy of an overactive bladder: clinical practice aspects. Russian Medical Inquiry. 2021;5(5):273–279 (in Russ.). DOI: 10.32364/2587-6821-2021-5-5-273-279.

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Section: фезотеродинаunclassified

Anticholinergic therapy of an overactive bladder: clinical practice aspects

Kuzmin¹,

Кузьмина²

2021

Russian Medical Inquiry

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“…Fesoterodine has limited potential to cross the blood-brain barrier, which is manifested clinically by a low incidence of central nervous system (CNS) adverse effects. Consequently, it is not contraindicated in patients with CNS diseases [ 5 ]. Although it is efficacious for the treatment of OAB, such as other muscarinic receptor antagonists, it has several side effects, such as constipation, insomnia, headaches, dry mouth, and blurred vision.…”

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confidence: 99%

Inhibition of voltage-dependent K⁺ channels by antimuscarinic drug fesoterodine in coronary arterial smooth muscle cells

Park

Kang

Heo

et al. 2022

Korean J Physiol Pharmacol

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Fesoterodine, an antimuscarinic drug, is widely used to treat overactive bladder syndrome. However, there is little information about its effects on vascular K + channels. In this study, voltage-dependent K + (Kv) channel inhibition by fesoterodine was investigated using the patch-clamp technique in rabbit coronary artery. In whole-cell patches, the addition of fesoterodine to the bath inhibited the Kv currents in a concentration-dependent manner, with an IC 50 value of 3.19 ± 0.91 μM and a Hill coefficient of 0.56 ± 0.03. Although the drug did not alter the voltage-dependence of steady-state activation, it shifted the steady-state inactivation curve to a more negative potential, suggesting that fesoterodine affects the voltage-sensor of the Kv channel. Inhibition by fesoterodine was significantly enhanced by repetitive train pulses (1 or 2 Hz). Furthermore, it significantly increased the recovery time constant from inactivation, suggesting that the Kv channel inhibition by fesoterodine is use (state)-dependent. Its inhibitory effect disappeared by pretreatment with a Kv 1.5 inhibitor. However, pretreatment with Kv2.1 or Kv7 inhibitors did not affect the inhibitory effects on Kv channels. Based on these results, we conclude that fesoterodine inhibits vascular Kv channels (mainly the Kv1.5 subtype) in a concentration- and use (state)-dependent manner, independent of muscarinic receptor antagonism.

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Long-term botulinum therapy for overactive bladder: myths and reality

Kuzmin¹,

Slesarevskaya²,

Amdiy³

et al. 2022

Urology reports (St. - Petersburg)

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The review article presents data on the efficacy and tolerability of intravesical injections of botulinum toxin in patients with overactive bladder. The pharmacological bases of the use of botulinum therapy in this category of patients are described in detail. Data on the history of the use of botulinum toxin for medical purposes are presented. Experience to date shows that intravesical botulinum toxin injections are highly effective and well tolerated in patients with refractory overactive bladder. Botulinum therapy is included in domestic and foreign clinical guidelines as a 3rd line treatment for idiopathic and neurogenic overactive bladder. Indications for its implementation are the inefficiency and/or poor tolerability of oral pharmacotherapy. It is noted that the only botulinum toxin recommended for use in clinical practice for the treatment of overactive bladder is onabotulinumtoxin A (Botox). The results of clinical studies are presented, showing that the effectiveness and safety of botulinum therapy do not decrease over time.

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Fesoterodine for the treatment of overactive bladder: pharmacological bases and clinical results

Abstract: The results of the clinical use of the new anticholinergic drug fesoterodine in the treatment of patients with overactive bladder was presented in the review. An analysis was made of the pharmacological effects of fesoterodine, which provide its high clinical efficacy and good tolerance.

Cited by 6 publications

References 52 publications

Anticholinergic therapy of an overactive bladder: clinical practice aspects

Anticholinergic therapy of an overactive bladder: clinical practice aspects

Inhibition of voltage-dependent K⁺ channels by antimuscarinic drug fesoterodine in coronary arterial smooth muscle cells

Long-term botulinum therapy for overactive bladder: myths and reality

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Fesoterodine for the treatment of overactive bladder: pharmacological bases and clinical results

Abstract: The results of the clinical use of the new anticholinergic drug fesoterodine in the treatment of patients with overactive bladder was presented in the review. An analysis was made of the pharmacological effects of fesoterodine, which provide its high clinical efficacy and good tolerance.

Cited by 6 publications

References 52 publications

Anticholinergic therapy of an overactive bladder: clinical practice aspects

Anticholinergic therapy of an overactive bladder: clinical practice aspects

Inhibition of voltage-dependent K+ channels by antimuscarinic drug fesoterodine in coronary arterial smooth muscle cells

Long-term botulinum therapy for overactive bladder: myths and reality

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Inhibition of voltage-dependent K⁺ channels by antimuscarinic drug fesoterodine in coronary arterial smooth muscle cells