tolterodine / Generic mfg. - LARVOL DELTA

GLANCE-aided snapshotting for sustainable integration of synchronous spectrofluorimetry and micellar boosting for nanoscale assay of tolterodine binary mixtures in crucial matrices. (PubMed, Sci Rep) - "Tolterodine tartrate (TLD) has recently demonstrated remarkable synergism when combined with either of two α1-adrenergic antagonists, doxazosin mesilate (DXZ) or terazosin hydrochloride dihydrate (TRZ), for treating urinary tract issues. The outcomes demonstrated the excellence of the designed methodology over reported approaches, offering proficient sensitivity, sustainability, facility, and practicability across diverse crucial matrices. These findings provide compelling evidence that the proposed work serves as an efficient, eco-friendly quantification tool for use in quality control, biological, and environmental sectors, fostering a more eco-conscious and sustainable scientific community."

Journal

Enantiodivergent Rh-Catalyzed Reductive Hydroformylation of Alkenyl Boronic Esters. (PubMed, Angew Chem Int Ed Engl) - "The chiral γ-boryl alcohol or diol products are versatile building blocks applicable to the synthesis of a series of APIs including (S)-tolterodine, (S)-dapoxetine, and (R)-atomaxetine. DFT calculation has revealed the origin of enantiodivergence of Rh-catalyzed reductive AHF of alkenyl boronic esters with Ph-BPE as the chiral ligand. The transformation is promised to provide great synthetic potential in both academia and industry."

Journal

Response to anticholinergic therapy and its predictors in pediatric overactive bladder. (PubMed, Eur J Pediatr) - P | "Anticholinergics show similar efficacy in treating OAB, though oxybutynin is associated with more side effects. Tolterodine reduced the odds of non-complete response, while a higher daily voids increased it."

Journal • Retrospective data • Overactive Bladder • Pediatrics

A randomized controlled study on the treatment for children with spleen-kidney qi deficiency type neurogenic urination (ChiCTR) - P=N/A | N=102 | Not yet recruiting | Sponsor: Beijing Children’s Hospital, Capital Medical University; Beijing Children’s Hospital, Capital Medical University

New trial

Evaluation of the Potential Inhibitory Effects of Medications for Detrusor Overactivity on Platelet-Activating Factor (PAF)-Induced Mechanical Activity in Guinea Pig Bladder Smooth Muscle. (PubMed, Biol Pharm Bull) - "Ten clinically used DO drugs-oxybutynin, tolterodine, fesoterodine, propiverine, propantheline, solifenacin, imidafenacin, flavoxate, urapidil, and clenbuterol-were tested at a concentration of 10 μM, exceeding typical therapeutic plasma levels. Furthermore, oxybutynin (10 μM) also decreased 60 mM KCl-induced contractions by a similar extent and nearly abolished acetylcholine (ACh, 10 μM)-induced contractions. These findings suggest that oxybutynin suppresses PAF-induced UBSM hyperactivity through a mechanism distinct from its anticholinergic effect, likely mediated by blockade of voltage-dependent Ca2+ channels (VDCCs)."

Journal • Overactive Bladder

Overactive bladder medications and risk of emergency hospital admissions with delirium in adults without dementia: self-controlled case series. (PubMed, Age Ageing) - "We observed increased hospital admission rates with delirium for adults without dementia whilst prescribed OAB anticholinergics, but not whilst prescribed mirabegron. Delirium risk remained raised for longer for men and was greater in older men. Alternative management options for OAB in older people should be considered before prescribing anticholinergic medications."

Journal • Alzheimer's Disease • CNS Disorders • Dementia • Overactive Bladder

LIFE-THREATENING GENERALIZED MUSCLE WEAKNESS DEVELOPING AFTER INTRAVESICAL BOTULINUM TOXIN APPLICATION IN A CASE WITH NEUROGENIC BLADDER (ESPN 2025) - " Case: A 6-year-old girl who underwent surgery for meningomyocele, was on tolterodine for neurogenic bladder, and had a clean intermittent catheter, and showed bilateral grade 5 vesicoureteral reflux (VUR) taken for recurrent urinary tract infection. Subureteric transurethral injection (STING) and intravesical 30 units/kilogram abobotulinumtoxinA were applied... BTX prevents the fusion of neurosecretory vesicles at presynaptic nerve endings and the release of acetylcholine. It can be applied cystoscopically to the detrusor muscles to reduce intravesical pressure in the storage or to the sphincters to facilitate voiding in detrusorsphincter dyssynergia. Side effects occur when the toxin passes into the bloodstream and affects neuromuscular junctions in separate regions or through retrograde axonal transport to spinal motor neurons."

Clinical • Ataxia • Infectious Disease • Nephrology • Otorhinolaryngology • Pediatrics • Respiratory Diseases • STING

Effectiveness and safety of electroacupuncture in female overactive bladder: a randomized controlled trial investigating sacral and tibial nerve modulation. (PubMed, Front Med (Lausanne)) - "One group received EA treatment at BL33 and SP6 acupoints three times weekly for 4 weeks, while the control group received tolterodine, a standard antimuscarinic medication...Further research is needed to optimize its clinical application. clinicaltrials.gov, identifier ChiCTR-1900021372."

Journal • Overactive Bladder • BDNF

Long-term clinical efficacy and cognitive impact of medications for overactive bladder related to the central nervous system. (PubMed, Int Urol Nephrol) - "OAB medication efficacy was comparable across medication types, but tolerability varied significantly, with the dementia, PD and solifenacin groups showing higher discontinuation rates. Cognitive impairment significantly influenced treatment outcomes, underscoring the need for tailored therapeutic strategies and regular cognitive assessments to optimise treatment effectiveness and maintain quality of life in patients with CNS-related OAB."

Journal • Alzheimer's Disease • Cardiovascular • CNS Disorders • Cognitive Disorders • Dementia • Movement Disorders • Overactive Bladder • Parkinson's Disease

HSPiP and QbD oriented optimized nanocubosomes for ameliorated absorption of tolterodine tartrate: In vitro and in vivo evaluations. (PubMed, Int J Pharm X) - "In vitro hemolysis, along with biochemical and hematological assays, ensured the safety of OCUB1 for oral delivery. Conclusively, OCUB1 presents a promised alternative to conventional capsule, offering reduced side effects and enhanced patient compliance."

Journal • Preclinical • Hematological Disorders

The Effect of Nighttime Mirabegron, Solifenacin, Tolterodine, or Oxybutynin on Nocturia, Sexual Function, Autonomic Function, and Lower Urinary Tract Blood Flow Perfusion in Women With Overactive Bladder Syndrome: Randomized Controlled Trial (clinicaltrials.gov) - P3 | N=220 | Not yet recruiting | Sponsor: Far Eastern Memorial Hospital

New P3 trial • Overactive Bladder

Antimuscarinics for burn patients: Helpful or harmful for sensation recovery? (PubMed, Burns) - "Burn patients on antimuscarinic therapy were more likely to develop paresthesia, possibly indicating nerve regeneration. While this may reflect sensory recovery, it could also lead to abnormal or painful sensations that negatively impact quality of life. Further research is needed to assess functional outcomes."

Journal • Diabetes • Metabolic Disorders • Overactive Bladder • Pain • Thermal Injury

Diisopromine as a non-labelled CYP3A4 substrate: Implications for breath test development. (PubMed, Bioorg Chem) - "This study explores diisopromine as a potential substrate due to its structural similarity to tolterodine, the first identified non-labelled CYP3A4 substrate producing a volatile metabolite. The production of both metabolites in HepG2-CYP3A4 cells was significantly inhibited following treatment with either 1-aminobenzotriazole or ketoconazole. These findings highlight that the minor structural modification in diisopromine enhances the biotransformation efficiency, paving the way for its potential development for a (non-) invasive CYP assay."

Journal • Review • CYP2C9 • CYP3A4

Pharmacological treatment of pediatric nocturnal enuresis: a systematic review and network meta-analysis. (PubMed, Pediatr Nephrol) - "Combination therapy may be superior to monotherapy in NE management. The most frequently used combination therapy is desmopressin plus anticholinergic agents. All drugs seemed to be safe."

Journal • Retrospective data • Review • Pediatrics • Urinary Incontinence

Treatment of Overactive Bladder With Anticholinergic Agents (clinicaltrials.gov) - P=N/A | N=120 | Active, not recruiting | Sponsor: Sehit Prof. Dr. Ilhan Varank Sancaktepe Training and Research Hospital

Biomarker • New trial • Overactive Bladder • Pediatrics

An Investigation of the Effect of Combining Tolterodine and Duloxetine in the Treatment of Mixed-Type Urinary Incontinence and the Factors Affecting Success. (PubMed, J Clin Med) - "Baseline ICIQ-SF scores may predict treatment success. Further prospective studies are needed."

Journal • Constipation • Gastroenterology • Gastrointestinal Disorder • Overactive Bladder • Urinary Incontinence • Urology

Effectiveness of simultaneous electroacupuncture stimulation on the tibial and ilioinguinal-iliohypogastric nerves in the treatment of refractory overactive bladder syndrome in women. (PubMed, Curr Urol) - "All patients in both groups had received anticholinergic muscarinic receptor antagonists (tolterodine/solifenacin), β3 receptor agonists, flupentixol/melitracen, and other basic treatment regimens with poor results. This therapy is safe, convenient, and free of significant adverse reactions, providing a new approach for the clinical treatment of refractory OAB in these patients. It significantly improves bladder symptoms and alleviates anxiety and depression, thereby markedly enhancing the patients' quality of life."

Journal • CNS Disorders • Depression • Mood Disorders • Overactive Bladder • Psychiatry • Urology

In vitro-in vivo scaling of cytochrome P450-mediated metabolic clearance using a relative activity factor approach. (PubMed, Drug Metab Dispos) - "We selected multiple probe substrates for CYP1A2 (caffeine, tizanidine, phenacetin), CYP2C9 ((S)-acenocoumarol, glimepiride, lornoxicam, tolbutamide, (S)-warfarin), CYP2C19 ((S)-lansoprazole, omeprazole, pantoprazole), CYP2D6 (desipramine, metoprolol, nebivolol, tolterodine), and CYP3A4 (alprazolam, felodipine, midazolam, nisoldipine, sildenafil, triazolam) to calculate the representative RAF value for each P450 isoform based on the in vivo-to-in vitro clearance ratio of the multiple probe substrates...The fm values of the responsible P450 isoform(s) could be well predicted for mexiletine, tamsulosin, risperidone, celecoxib, and glibenclamide...By applying relative activity factor values obtained from multiple probe substrates, this study was able to quantitatively predict the in vivo clearances mediated by CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4. This simple, practical method will help optimize metabolic clearances via the major cytochrome P450..."

Journal • Preclinical • CYP1A2 • CYP2C19 • CYP2C9 • CYP3A4

Novel O-methylpyrimidine prodrugs of phenolic compounds bioactivated by aldehyde oxidase: Enhancing metabolic stability against first-pass conjugative metabolism in the intestine. (PubMed, Drug Metab Dispos) - "Prototypical prodrugs of 4-hydroxy-tamoxifen (4OH-TAM), raloxifene (RAL), rotigotine, 5-hydroxy-tolterodine, and phentolamine were all substrates for AO-mediated parent drug release in liver cytosol from humans and every preclinical species evaluated. Reaction phenotyping confirmed the role of AO; hydralazine inhibited production of 4OH-TAM and RAL from their respective prodrugs in the human liver cytosol, and recombinant human AO activated those same prodrugs...SIGNIFICANCE STATEMENT: An aldehyde oxidase-mediated biotransformation that cleaves O-linked methylpyrimidine-masked phenolic moieties was identified, and this system employed for a novel prodrug bioactivation strategy. The research herein expands existing knowledge surrounding the metabolism capabilities of this enzyme and provides medicinal chemists with a tool to enhance the oral bioavailability of phenolic compounds that otherwise would be limited due to extensive phase II metabolism and possibly low..."

Journal

Pharmacotherapy for overactive bladder syndrome and the risk of incident dementia. (PubMed, World J Urol) - "Most anticholinergic medications and mirabegron are associated with an increased risk of dementia compared to untreated controls with OAB, while fesoterodine was not found to be associated with an increased risk in any group."

Clinical • Journal • Retrospective data • Alzheimer's Disease • CNS Disorders • Dementia • Overactive Bladder

Green HPLC-Fluorescence detection method for concurrent analysis of Tamsulosin hydrochloride and Tolterodine tartrate in dosage forms and biological fluids. (PubMed, Sci Rep) - "To evaluate the method's greenness, GAPI and AGREE tools were employed. The results indicated significant adherence to green chemistry principles."

Journal

Long-term efficacy of Mirabegron-anticholinergic combination in paediatric neurogenic bladder. (PubMed, J Pediatr Urol) - "MAC combination effectively manages paediatric neurogenic bladder resistant to AC and BTX therapy. The VUD benefits (present in 77.8 %) and symptom benefits (present in 61 %) are maintained and ongoing for a significant period (median 33 and 43 months respectively) when commenced before significant loss of compliance. MAC presents a promising long-term treatment option for the paediatric neurogenic bladder."

Journal • Retrospective data • CNS Disorders • Constipation • Fatigue • Gastroenterology • Gastrointestinal Disorder • Oncology • Orthopedics • Pediatrics

Prevalence and Factors with Potentially Inappropriate Prescribing among Older Surgical Outpatients in China: A Nationwide Cross-sectional Study in 100 Hospitals. (PubMed, J Epidemiol Glob Health) - "The study found that while the prevalence of PIP among older surgical outpatients in China is relatively low, attention is needed to the widespread use of certain PIMs."

Journal • Observational data • Benign Prostatic Hyperplasia • Cardiovascular • CNS Disorders • Hypertension • Pain • Sleep Disorder

A Multidisciplinary, Multimodal Bundled Care Approach to Chronic Pelvic Pain (clinicaltrials.gov) - P3 | N=26 | Active, not recruiting | Sponsor: Jocelyn Fitzgerald | Trial completion date: Jan 2025 ➔ Oct 2025 | Recruiting ➔ Active, not recruiting | N=80 ➔ 26

Enrollment change • Enrollment closed • Trial completion date • Gynecology • Interstitial Cystitis • Musculoskeletal Pain • Pain

Comparisons of urinary bladder responses to common antimuscarinics reveals unique effects of darifenacin. (PubMed, Front Physiol) - "Carbachol concentration-response curves were performed on paired tissues in the absence or presence of commonly prescribed antimuscarinics: darifenacin, fesoterodine, oxybutynin, solifenacin, trospium, and tolterodine. Darifenacin reduced the maximum contraction in adult U&LP preparations to carbachol by 49% and to αβ-methylene-ATP by 35%. Darifenacin presents as an antimuscarinic medication that influences non-muscarinic pathways in urinary bladder tissue, indicating its potential to assist OAB patients with non-muscarinic pathophysiology."

Journal • Overactive Bladder