Tolterodine

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BACKGROUND AND OBJECTIVE: Fesoterodine is a muscarinic receptor antagonist approved for the treatment of overactive bladder (OAB) in adults and neurogenic detrusor overactivity (NDO) in pediatric patients. This work aimed to characterize the population pharmacokinetics of 5-hydroxymethyl tolterodine (5-HMT, the active metabolite of fesoterodine) and its pharmacokinetic/pharmacodynamic relationship in pediatric patients with OAB or NDO following administration of fesoterodine...

BACKGROUND: Catheter-related bladder discomfort (CRBD) is a common postoperative bladder pain syndrome. Many drugs and interventions for managing CRBD have been studied, but their comparative effectiveness remains controversial. We made a study to assess the comparative effectiveness of interventions included Ketorolac, Lidocaine, Chlorpheniramine, Gabapentin, Magnesium, Nefopam, Oxycodone, Parecoxib, Solifenacin, Tolterodine, Bupivancaine, Dexmedetomidine, Hyoscine N-butyl bromide, Ketamine, Penile nerve block on urological postoperative CRBD...

OBJECTIVES: The aim of this study was to indirectly compare the efficacy and safety of mirabegron and vibegron in patients with overactive bladder. METHODS: A systematic search was performed on Pubmed, Web of Science, Embase, and the Cochrane Central Register of Controlled Trials databases to identify studies from the date of database inception to January 1, 2022. All randomized controlled trials comparing mirabegron or vibegron with tolterodine, imidafenacin, or placebo were eligible...

Tolterodine (TOL) is an antimuscarinic drug used for the treatment of patients with overactive bladder presenting urinary frequency, urgency, and urge incontinence. During the clinical use of TOL, adverse events such as liver injury took place. The present study aimed at the investigation of the metabolic activation of TOL possibly associated with its hepatotoxicity. One GSH conjugate, two NAC conjugates, and two cysteine conjugates were found in both mouse and human liver microsomal incubations supplemented with TOL, GSH/NAC/cysteine, and NADPH...

BACKGROUND: Few studies have addressed whether anticholinergic (AC) medications for overactive bladder (OAB) cause cognitive decline in individuals with existing cognitive impairment, and whether the APOE ε4 gene increases this risk. OBJECTIVE: To determine whether OAB AC use is associated with a clinically relevant change in cognitive measures among adults with normal and abnormal cognition. DESIGN SETTING AND PARTICIPANTS: This was a retrospective cohort study using data from the National Alzheimer's Coordinating Center...

BACKGROUND: Neurogenic detrusor overactivity (NDO) can damage the upper urinary tract leading to chronic renal impairment. Antimuscarinic therapy is used to improve urinary incontinence and protect the upper urinary tract in patients with NDO. OBJECTIVE: This study investigated safety and efficacy of fesoterodine, a muscarinic receptor antagonist, in 6‒<18-year-old patients with NDO (NCT01557244). STUDY DESIGN: This open-label phase 3 study included 2 pediatric cohorts...

IMPORTANCE: The international phase 3 EMPOWUR trial demonstrated efficacy and safety of vibegron, a newer β3-adrenergic receptor agonist, in adults with overactive bladder (OAB). Women are disproportionately affected by OAB, especially those with bothersome symptoms, such as urge urinary incontinence (UUI). OBJECTIVE: This subgroup analysis from EMPOWUR assessed efficacy and safety of vibegron in women. STUDY DESIGN: In EMPOWUR, patients with OAB were randomized 5:5:4 to 12 weeks of treatment with once-daily vibegron 75 mg, placebo, or tolterodine 4-mg extended release...

A nickel complex of isoquinox promoted enantioselective conjugate arylation and heteroarylation of enones using aryl and heteroaryl halides directly. The reaction was successfully applied to stereoselective syntheses of ar -turmerone, chiral fragments of (+)-tolterodine and AZD5672. Mechanistically, experiments and calculations supported that an arylnickel(I) complex inserted to enones via an elementary 1,4-addition.

BACKGROUND: Few randomized controlled trials evaluate the long-term efficacy and safety of pharmacotherapy for overactive bladder (OAB). This network meta- analysis compares the long-term (52-week) efficacy and safety of vibegron, mirabegron and anticholinergics for the treatment of OAB. METHODS: A systematic literature review and network meta-analysis were conducted following PRISMA guidelines using MEDLINE, Embase and Cochrane Central Register of Controlled Trials and terms related to OAB...

To summarize the differences in urodynamic outcomes between oral antimuscarinic drugs and OnabotulinumtoxinA, and finding a therapy that maintains good urodynamics in neurogenic detrusor overactivity (NDO). We conducted a literature search of EMBASE and PubMed, with the language limited to English. In the analysis, all of the published randomized trials of OnabotulinumtoxinA or antimuscarinic drugs used to treat NDO were found and the results were finally obtained through Bayesian model analysis. A total of 12 RCTs and 2208 patients were included...

Three-component, solvent-dependent, Brønsted-acid catalyzed reaction of benzaldehydes, silyl enolates and arene nucleophiles has been developed for the synthesis of potential drug candidate 3-aryl-1-indanones. This reaction features three C-C bond formation, high regioselectivity under one-pot strategy, broad substrate generality, facile scalability (1.04 gm), high functional group tolerance and viable substrates. The in situ generated β- O -silyl ethers from Mukaiyama aldol reaction subjected to acid-catalyzed benzylic arylation with strong as well as weak nucleophiles and the resultant β , β-di-aryl esters can undergo the third C─C bond formation with excellent regioselectivity via intramolecular cyclization to afford the indanone products in the same pot...

BACKGROUND: Overactive bladder (OAB) is defined as urinary urgency, usually with urinary frequency and nocturia. . The current treatment for OAB includes conservative management, surgery, and pharmacotherapy. Mirabegron is a new drug acting by the ß3-adrenoceptor agonism. This study aimed to review the cost-effectiveness of mirabegron in the treatment of OAB. AREAS COVERED: We searched published articles in electronic search databases. Ten studies were included in the qualitative analysis...

Validation of risk-stratification method for the chronic atrioventricular block cynomolgus monkey model and its mechanistic interpretation were performed using 6 pharmacologically-distinct drugs. The following drugs were orally administered in conscious state, astemizole: 1, 5 and 10 mg/kg (n = 6); haloperidol: 1, 10 and 30 mg/kg (n = 5); amiodarone: 30 mg/kg (n = 4); famotidine: 10 mg/kg (n = 4); levofloxacin: 100 mg/kg (n = 4); and tolterodine: 0.2, 1 and 4.5 mg/kg (n = 4)...

Tolterodine is a first-line antimuscarinic drug used to treat overactive bladder. Adverse cardiac effects including tachycardia and palpitations have been observed, presumably due to its inhibition of the human ether-à-go-go-related gene (hERG) K+ channel. However, the molecular mechanism of hERG channel inhibition by tolterodine is largely unclear. In this study we performed molecular docking to identify potential binding sites of tolterodine in hERG channel, and two-microelectrode voltage-clamp to record the currents of hERG and its mutants expressed in Xenopus oocytes...

BACKGROUND: Antimuscarinic (AM) and beta-3-agonist (B3A) treatment are the standard first line pharmacological treatment used to manage overactive bladder (OAB) patients. Aim of our study was to analyze real-life data of adverse events related to AMs and B3A reported on Eudra-Vigilance (EV) database. METHODS: EV database is the system for managing and analyzing information on suspected adverse reactions to medicines which have been authorized or being studied in clinical trials in the European Economic Area (EEA)...

BACKGROUND: Overactive bladder (OAB) is characterized by urgency and frequency with (OAB wet) or without (OAB dry) urge urinary incontinence (UUI). In the phase 3 EMPOWUR trial, vibegron-a selective β 3 -adrenergic receptor agonist for the treatment of OAB-significantly improved daily number of urgency episodes and micturitions vs. placebo ( P  < 0.01). These post hoc analyses aimed to compare the efficacy of vibegron vs. placebo in OAB dry and wet populations. METHODS: Patients were randomly assigned 5:5:4 to receive once-daily vibegron 75 mg, placebo, or tolterodine 4 mg extended release, respectively, for 12 weeks...

IMPORTANCE: Clinical data on the use of overactive bladder (OAB) medications are limited by the physician interpretation of adverse effects rather than those that are patient reported. OBJECTIVE: The aim of the study was to evaluate the association between OAB medications and adverse drug events (ADEs) through the self-reporting U.S. Food and Drug Administration Adverse Event Report System database. STUDY DESIGN: The U.S. Food and Drug Administration Adverse Event Report System (FAERS) database was queried from 2004 to 2019...

INTRODUCTION: Overactive bladder (OAB) is a chronic condition highly prevalent in children and causing bothersome symptoms. It is often associated with deterioration of quality of life and can be devastating for patients and their families. Prompt initiation of conservative measures should be the backbone of treatment. When conservative management fails, pharmacological options must be considered. AREAS COVERED: Although antimuscarinics are considered the mainstay of pharmacological treatment for OAB, only two agents are currently approved for the pediatric population...

Efficient kinetic resolution (KR) occurs in asymmetric transfer hydrogenation (ATH) reactions of racemic 3-aryl-1-indanones using commercial ( R , R )- or ( S , S )-Ts-DENEB as a catalyst, a 1 : 5 mixture of HCO2 H and Et3 N as a hydrogen source and MeOH as solvent. This process at room temperature produces near equal yields of cis -3-arylindanols with high dr and ee, and unreacted 3-arylindanones with excellent ee. Stereoselective transformations of 3-arylindanols and 3-arylindanones, generated by using the ATH-KR protocol, were carried out to form (+)-indatraline and synthetically valuable ( R )-6-methyl-4-phenylcoumarine, which is a key intermediate in the preparation of ( R )-tolterodine, ( S )-4-aryl-3,4-dihydroquinoline-2(1 H )-one and ( S )-4-aryl-3,4-dihydroisoquinoline-1(2 H )-one...