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oxybutynin (oxybutynin, TIMERx / Ditropan CR / Cystrin CR)

✓ Approved

Takeda · CHRM1 · 小分子

什么是 oxybutynin？

oxybutynin 是一种小分子，由Takeda研发。该药已获批，用于治疗相关适应症，给药途径：Oral (PO)。

药物档案

商品名oxybutynin, TIMERx, Ditropan CR, Cystrin CR
公司Takeda
药物类别小分子
分子靶点CHRM1, CHRM2, CHRM3, CHRM4
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Takeda

作用机制

分子靶点

oxybutynin 作用于 4 个分子靶点：

CHRM1cholinergic receptor muscarinic 1 (M1, HM1)
CHRM2cholinergic receptor muscarinic 2 (HM2)
CHRM3cholinergic receptor muscarinic 3 (HM3, PBS)
CHRM4cholinergic receptor muscarinic 4 (HM4, M4R)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

oxybutynin 针对 1 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Renal and urinary disordersUrinary incontinence✓ Approved

相关研究文献

PubMedThe journal of spinal cord medicine2026-08-20

Off-target effects of percutaneous epidural spinal cord and dorsal root ganglion stimulation with task-specific training on lower urinary tract function in individuals with chronic spinal cord injury.

Soong Christina C, Veith Daniel D DD, Gill Megan L ML, Beck Lisa A LA et al.

This study aimed to evaluate the off-target effects of motor-optimized SCS-enabled task-specific training (SCS-TST) on lower urinary tract function through self-reported data from individuals with chronic spinal cord injury (SCI), using the Neurogenic Bladder Symptom Score (NBSS). A secondary objective was to explore whether participant characteristics or bladder treatments were associated with changes in NBSS outcomes. Datasets from two prospective pilot trials using percutaneous spinal cord stimulation (SCS) to enable motor function were analyzed and reported. Department of Physical Medicine and Rehabilitation, Mayo Clinic, Rochester, Minnesota. Adults ≥ 1-year post traumatic SCI. Participants received either 12 days of epidural stimulation (ES) or 10 days of ES and dorsal root ganglion stimulation (ESDRS), each coupled with 6-8 SCS-TST sessions. NBSS was administered pre- and post-intervention. Analysis of 23 participants (ES, n = 3; ESDRS, n = 20) showed no significant group-level changes in total NBSS (p = 0.49) or functional domains (p = 0.56-0.85). Individually, 83% demonstrated no clinically meaningful change, while 9% improved and 9% worsened. Exploratory analyses identified that symptom change was associated with neurological level of injury (p = 0.017), age (p = 0.026), and marginally associated with injury severity (p = 0.055). Oxybutynin use was associated with lower symptom variability, without statistical significance (p = 0.074). Motor-optimized SCS-TST did not lead to significant group-level changes in patient-reported urinary symptoms. However, a subset of individuals experienced improvement or worsening, suggesting that injury characteristics and medication use may influence urinary outcomes. These preliminary findings warrant confirmation in larger, adequately powered trials.Trial Registration: ClinicalTrials.gov identifiers: NCT05095454, NCT04736849.

PMID 42622482
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PubMedSleep & breathing = Schlaf & Atmung2026-08-06

Pharmacotherapy in obstructive sleep apnoea: a clinical guide.

Shastry Shashank S, Kimoff John R JR, Pinto Lancelot Mark LM

Obstructive Sleep Apnoea (OSA) is a common, yet underdiagnosed disorder, with significant health implications. Continuous positive airway pressure (CPAP) remains the reference standard and first-line therapy. However, successful CPAP usage is influenced by factors such as access, cost, tolerance, patient education, early troubleshooting, and long-term adherence, all of which can be challenging and resource-demanding. Adding therapeutic options to the armamentarium is therefore welcome. There is a need for clinicians to be abreast of all the available therapeutic options for treatment of OSA. We conducted an extensive literature review of the published studies that were conducted using non-CPAP pharmacotherapeutic modalities for OSA. This narrative review summarises the current landscape of OSA pharmacotherapy, focusing on mechanisms of action, clinical trial evidence, and endotype-based selection strategies. Emerging therapies such as the atomoxetine-oxybutynin combination and topiramate show promise in reducing severity of OSA, and improving sleep quality. GLP-1 receptor agonists like liraglutide and tirzepatide offer benefits beyond reducing the severity of OSA. Other agents such as sulthiame, solriamfetol, and pitolisant have also demonstrated efficacy. Wake-promoting agents like modafinil and armodafinil target the commonest symptom of OSA, sleepiness. This review provides a practical, endotype-aligned summary of pharmacologic options for the management of OSA.

PMID 42557390
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PubMedJournal of rhinology : official journal of the Korean Rhinologic Society2026-08-04

Current Updates on Pharmacotherapy for Obstructive Sleep Apnea.

Kim Sang-Wook SW

Obstructive sleep apnea (OSA) is a common sleep disorder associated with substantial cardiovascular morbidity and mortality. Although positive airway pressure (PAP) remains the gold-standard treatment, poor long-term adherence often limits its clinical effectiveness, underscoring the need for safe and effective pharmacological alternatives. Advances in the understanding of OSA endotypes, including anatomical collapsibility, upper airway muscle responsiveness, arousal threshold, and loop gain, have shifted research toward precision pharmacotherapy. Early studies of single-agent therapies, such as protriptyline and acetazolamide, were limited by modest efficacy or clinically significant adverse effects. More recent dual-drug combinations and anti-obesity medications have shown greater promise. In particular, atomoxetine plus oxybutynin has demonstrated significant reductions in the apnea-hypopnea index (AHI) by enhancing upper airway muscle tone across sleep stages. In parallel, glucagon-like peptide-1 receptor agonists have substantially changed the management of obesity-related OSA. Tirzepatide, in particular, has produced marked weight loss of nearly 20% and an AHI reduction of more than 50%, leading to its recent U.S. Food and Drug Administration approval for OSA. Despite earlier skepticism, the shift from broad-spectrum agents toward endotype-specific and metabolic-targeted therapies may improve the management of selected patients with OSA. However, long-term safety and cost-effectiveness require further evaluation before these emerging pharmacological options can be broadly integrated into care for patients who cannot tolerate conventional PAP therapy.

PMID 42548223
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PubMedEuropean urology open science2026-08-02

Intravaginal Delivery of Oxybutynin: An Alternative Administration Route to Improve its Pharmacokinetic and Pharmacodynamic Effects.

Peltenburg Sophie I SI, Meijs Anouk C AC, Pagan Lisa L, Somohardjo Emily E et al.

While oxybutynin is the most efficacious oral antimuscarinic treatment to reduce incontinence episodes in patients with an overactive bladder, oxybutynin is often discontinued due to significant side effects. This is hypothesized to be caused by its metabolite. The purpose of the study was to determine whether intravaginal oxybutynin administration leads to fewer anticholinergic side effects than oral oxybutynin. Additionally, the pharmacokinetics (PK), safety, and tolerability were compared. The study had a single-blind, placebo-controlled, three-way cross-over design in 24 healthy women. Participants randomly received repeatedly 2.5 mg intravaginal oxybutynin via the MedRing, 5 mg oral oxybutynin, and placebo. Anticholinergic side effects were assessed with the NeuroCart test battery. Additionally, quantitative electro-encephalography (qEEG), salivary flow, dry mouth symptoms, pharmacokinetics, safety, and tolerability were assessed. Neither intravaginal nor oral oxybutynin demonstrated a significant effect on the adaptive tracking test compared to placebo. However, both oxybutynin administration routes resulted in broad qEEG amplitude decreases. Participants reported less dry mouth symptoms, and the saliva weight was significantly higher after intravaginal oxybutynin (estimated difference, 0.51 g [95% confidence interval, 0.16-0.87], p = 0.006). Intravaginal oxybutynin led to a ∼10-fold lower metabolite/parent ratio and was generally safe and well-tolerated.Limitations include the lack of measured cognitive effect in this population, and the ultimately single-blind study conduct because of subtle differences in the appearance of the ring. This study provides a solid basis for intravaginal oxybutynin via the MedRing as an alternative route of administration. Intravaginal oxybutynin could be considered an alternative to reduce side effect-related discontinuation rates.

PMID 42540451
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PubMedThe Prostate2026-08-02

Treatment of Hot Flashes in Men With Prostate Cancer Undergoing Androgen Deprivation Therapy.

Schaldemose Ellen Lund EL, Poulsen Mads Hvid MH, Nørby Bettina B, Madsen Christine Vestergaard CV

Hot flashes are common and often debilitating side effects of castration therapy; a cornerstone in the treatment of metastatic prostate cancer (PCa) as well as in localized or locally advanced PCa when combined with radiotherapy. The evidence for relieving vasomotor symptoms is limited. This systematic review presents both pharmacological and non-pharmacological interventions for treating hot flashes in men with PCa undergoing castration therapy, primarily androgen deprivation therapy (ADT). a systematic literature search was conducted in PubMed using ("hot flash*" OR "hot flush*" OR "vasomotor*") AND ("prostate") as keywords. Studies with intervention for hot flashes due to castration therapy, estimation of treatment response (e.g., reduction in frequency or impact on quality of life) and patients with PCa (any stage) were eligible. Of 469 papers, 35 were included in the review. The included studies evaluated cyproterone acetate, estrogen or estrogen derivatives, progesterone derivatives, selective serotonin reuptake inhibitors (SSRIs), gabapentin, oxybutynin, and clonidine, as well as non-pharmacological interventions such as acupuncture, cognitive behavioral therapy (CBT), and dietary supplements (e.g., Dong Quai/Angelica Sinensis, Serelys Homme, soy protein, and Salvia officinalis). Across all blinded pharmacological interventions, the relative reduction in hot flash frequency ranged from -21% to -84%, and the placebo effect was between -19% and -30%. Hormonal agents such as cyproterone acetate and estrogen appear to be the most effective treatments, although they are associated with side effects. Non-pharmacological options like acupuncture and CBT may offer some benefit, while dietary supplements seem to be ineffective. Future studies are needed also to evaluate newer treatments, such as fezolinetant, in this patient population.

PMID 42542970
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PubMedEuropean journal of hospital pharmacy : science and practice2026-07-31

When simple syrup is not so simple: pH-dependent instability of an extemporaneous oxybutynin oral solution.

Castro-Luaces Susana S, Lago-Blanco Ana Belén AB, Fortes Gonzalez Susana S

PMID 42532673
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