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tamsulosin + tolterodine (Roliflo OD)

✓ Approved

Ranbaxy Laboratories Limited · ADRA1A · 小分子

什么是 tamsulosin + tolterodine？

tamsulosin + tolterodine 是一种小分子，由Ranbaxy Laboratories Limited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Roliflo OD
公司Ranbaxy Laboratories Limited
药物类别小分子
分子靶点ADRA1A, CHRM1, CHRM2, CHRM3, CHRM4
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Ranbaxy Laboratories Limited

作用机制

分子靶点

tamsulosin + tolterodine 作用于 5 个分子靶点：

ADRA1Aadrenoceptor alpha 1A (ADRA1L1, ADRA1C)
CHRM1cholinergic receptor muscarinic 1 (M1, HM1)
CHRM2cholinergic receptor muscarinic 2 (HM2)
CHRM3cholinergic receptor muscarinic 3 (EGBRS, m3AChR)
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

tamsulosin + tolterodine 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 disordersHypertonic bladder✓ Approved

相关研究文献

PubMedDiabetes, obesity & metabolism2026-08-04

Absence of Interaction Between 5α-Reductase Inhibitors and Glucocorticoids on Incidence of Myocardial Infarction in People With Type 2 Diabetes.

Tu Haolan H, Ju Chengsheng C, McGurnaghan Stuart J SJ, Blackbourn Luke A K LAK et al.

People with Type 2 diabetes experience higher cardiometabolic risk, and both synthetic glucocorticoids and use of 5α-reductase inhibitors have been individually linked to increased risk of myocardial infarction. We tested whether the increase in risk is exacerbated by co-prescription of both drugs. We performed a population-based cohort study in the Scottish Diabetes Research Network-National Diabetes Dataset (SDRN-NDS) and IQVIA Medical Research Data-UK (IMRD-UK). Patients with Type 2 diabetes aged ≥ 40 years receiving 5α-reductase inhibitors or tamsulosin, who were incident users of systemic glucocorticoids during 2006-2021 were included. We modelled the joint effect of 5α-reductase inhibitors and cumulative exposure to glucocorticoids on the risk of myocardial infarction using a time-varying Cox proportional hazards model. A total of 13 161 patients with Type 2 diabetes were included in SDRN-NDS and 15 084 in IMRD-UK. Mean age was 71.4 ± 9.6 and 72.3 ± 9.4 years, with mean follow-up of 4.7 (3.6) and 5.6 (4.0) years, respectively. Median (IQR) total glucocorticoids exposure was 210 (96-630) and 420 (200-1240) prednisolone-equivalent milligram. Risk for myocardial infarction was increased among users of 5α-reductase inhibitors (HR [95% CI]: SDRN-NDS, 1.21 [1.02-1.43]; IMRD-UK, 1.27 [1.02-1.59]) and per SD increase in cumulative glucocorticoid exposure (HR [95% CI]: SDRN-NDS, 1.09 [1.03-1.14]; IMRD-UK, 1.08 [1.01-1.15]). We did not observe a multiplicative interaction (SDRN-NDS, p = 0.44; IMRD-UK, p = 0.68) between the use of the two drugs. People with Type 2 diabetes exposed to 5α-reductase inhibitors or glucocorticoids are at an increased risk of myocardial infarction, although a multiplicative interaction between the use of the two drugs was not found.

PMID 42547757
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PubMedCureus2026-08-02

Painless Ischemic Priapism Associated With Tamsulosin Use: A Case Report and Literature Review.

Rector Caitlin E CE, Lei Kevin K, Hubbard Lael L, Ovasapians Navasard N et al.

Tamsulosin, a selective α1-adrenergic antagonist prescribed for benign prostatic hyperplasia and expulsion of ureteral stones, carries a rare risk of priapism. We present a 59-year-old male with hypogonadism, hypertension, and hyperlipidemia who developed painless priapism 72 hours after initiating tamsulosin for ureterolithiasis. Despite the atypical absence of pain, penile blood gas analysis confirmed ischemic priapism. Initial treatment with intracavernosal phenylephrine (1000 mcg) failed, requiring bilateral corpus spongiosum shunts for resolution. A literature review revealed that many of the 14 existing cases identified occurred within 24 hours of drug initiation in middle-aged or older patients without additional risk factors. Approximately half responded to intracavernosal vasoconstrictors, while refractory cases required surgical intervention. To our knowledge, this is the first reported case of painless tamsulosin-induced ischemic priapism, emphasizing the importance of patient counseling and prompt evaluation of persistent erections regardless of pain intensity.

PMID 42540804
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PubMedAmerican journal of men's health2026-07-30

Concurrent Jackstone Calculus and Prostate Cancer: Should They Be Treated Concurrently or Sequentially?

Tian Shuo S, Li Huijuan H, Jiang Yuliang Y, Wang Cheng C et al.

Jackstone calculus is a rare urinary stone morphology with a distinctive spiculated appearance, most often reported in the bladder and usually associated with urinary stasis or outlet obstruction. We report a 70-year-old man with 1 year of progressive dysuria and intermittent interruption of urinary stream despite tamsulosin and finasteride. Urinalysis showed pyuria, hematuria, and bacteriuria. Ultrasonography and pelvic computed tomography identified an irregular star-shaped bladder stone and marked prostatic enlargement, with an estimated prostate volume of approximately 125 mL on ultrasonography. Serum total prostate-specific antigen was 16.2 ng/mL, with a free-to-total ratio of 0.138. Systematic transrectal biopsy showed adenocarcinoma in 2 of 12 cores, Gleason score 3 + 3 = 6 (Grade Group 1). After multidisciplinary discussion, the patient underwent laparoscopic radical prostatectomy with concomitant intact stone removal. The 3.1-cm stone showed classic jackstone morphology. Final pathology showed Gleason 3 + 4 = 7 adenocarcinoma (Grade Group 2), upgraded from biopsy, with negative surgical margins. Telephone follow-up at 1, 3, and 12 months showed sustained improvement of lower urinary tract symptoms without recurrent urinary tract infection-related symptoms. Postoperative imaging and prostate-specific antigen data were unavailable. This case is relevant to men's health because a visually distinctive bladder stone may coexist with clinically relevant prostatic disease. In men with lower urinary tract symptoms and abnormal prostate-specific antigen values, bladder outlet obstruction, infection, or bladder stones should not preclude further oncologic evaluation. In selected patients in whom definitive prostate surgery is chosen, combined stone removal can be a practical single-stage approach.

PMID 42531155
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PubMedEuropean journal of obstetrics, gynecology, and reproductive biology2026-07-26

Comparing the safety and efficacy of vibegron, mirabegron and tolterodine in patients with overactive bladder: a systematic review and network meta-analysis.

Mohamed-Ahmed R R, Rantell A A, Robinson D D

Overactive bladder (OAB) is defined as 'urinary urgency with or without urinary urgency incontinence (UUI), usually associated with urinary frequency and/or nocturia, in the absence of urinary tract infection'. OAB is known to be a common disorder with a significant impact on quality of life. First line treatments include weight loss in those with a BMI > 30, bladder retraining and fluid advice. Pharmacotherapy treatment includes antimuscarinics and mirabegron, a beta 3 agonist. The National Institute of Clinical Excellence (NICE), has recently incorporated the use of a newer beta 3 agonist, vibegron, into its recommendations for the management of overactive bladder (OAB). There are no head-to-head studies which directly compare the efficacy of vibegron with mirabegron, an older beta 3 agonist. This network meta-analysis aims to compare the safety and efficacy of vibegron when compared to mirabegron and tolterodine, more longstanding treatments for OAB. A systematic review was conducted to identify phase III randomised controlled trials, for patients with idiopathic OAB, which compared mirabegron and/or vibegron and/or tolterodine. The primary outcome was the change from baseline in episodes of urinary urgency (UU). The secondary outcomes assessed were:The study was registered on PROSPERO (CRD 420250636077) and analysis was performed using MetaInsight. Of the 2,647 identified articles, five studies were deemed suitable to include in the network meta-analysis. Results for the primary outcome included 5,317 patients and demonstrated a greater improvement in UU episodes in the vibegron group, when compared to placebo, tolterodine and mirabegron. Vibegron also ranked favourably in reduction in episodes of UUI and improvement in maximum voided volume per void. Whereas mirabegron had the greater improvement in reduction in episodes of urinary frequency. The incidence of any adverse event was highest in the vibegron group. Tolterodine had the highest rate of hypertension and dry mouth. Constipation was highest in the vibegron group. However, it is important to note the large heterogeneity in definitions of adverse events as well as discrepancy in their reporting. Vibegron appears to rank more favourably for improvement in episodes of UU, UUI and maximum voided volume per void, when compared to mirabegron and tolterodine. Mirabegron ranks more favourably for improvement in episodes of urinary frequency over 24 h. Mirabegron is least likely to be associated with hypertension, although reporting of adverse events is non-standardised and therefore may not be comparable. This network meta-analysis does not account for other factors which may influence drug therapy choice i.e. contraindications, difficulties with swallowing and available treatment options.

PMID 42501511
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PubMedGalen medical journal2026-07-25

Effect of Tamsulosin on Osteopontin Gene Expression in Preventing Ethylene Glycol-Induced Kidney Stone in Male Wistar Rats : Short title: Effect of Tamsulosin on Osteopontin Gene Expression.

Parvizrad Ramin R, Ghorbani Marghamlki Elahe E, Nikfar Somayeh S, Khalili Dermani Sara S

Tamsulosin, an α1-adrenergic receptor antagonist, has been proposed as a potential therapeutic agent against urolithiasis-induced renal damage. However, limited in vivo evidence exists regarding its renoprotective mechanisms. Forty male Wistar rats were randomly allocated into four groups (n=10/group): positive control, negative control (ethylene glycol-induced urolithiasis), prevention (tamsulosin administered simultaneously with ethylene glycol), and treatment (tamsulosin administered after model induction). Biochemical parameters including serum creatinine, urea, uric acid, calcium, and phosphorus were measured using rat-validated commercial kits (Pars Azmun, Iran). Normal ranges were defined based on published reference values. Gene expression was analyzed by qPCR using the 2^-ΔΔCt method. Study design and reporting followed the ARRIVE checklist. At day 30, the prevention group exhibited significantly lower serum creatinine (0.60 ± 0.08 mg/dL) compared to the negative control (0.98 ± 0.12 mg/dL, P0.01). Although urea levels were slightly higher in the prevention group (4.0 ± 0.7 mg/dL) versus the negative control (3.22 ± 0.6 mg/dL), the calculated BUN/creatinine ratio was significantly improved (46.7 vs. 33.0, P0.05). No significant changes were observed in serum calcium or phosphorus. Gene expression analysis showed upregulation of protective markers in the prevention group. In vivo findings on the beneficial effects of tamsulosin on the renal profile in ethylene glycol-induced urolithiasis illustrate its protective effects on the renal system through improvement of creatinine clearance and BUN/creatinine balance. This underscores its probable use as a protective therapeutic agent against renal injury of crystallization origin.

PMID 42499366
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PubMedClinical pharmacology in drug development2026-07-20

Pharmacokinetics and Bioequivalence of Tamsulosin Hydrochloride Extended-Release Capsules in Healthy Chinese Volunteers: A Randomized, Open-Label, Crossover Study Under Fasting and Fed Conditions.

Du Lijie L, Wang Xiaolu X, Zhang Yi Y, Yang Jiamin J et al.

Tamsulosin hydrochloride is a long-acting, highly selective α1A receptor antagonist, primarily used to treat benign prostatic hyperplasia. It effectively alleviates lower urinary tract symptoms, including dysuria, nocturia, and urgency caused by prostate enlargement. This study aimed to evaluate the pharmacokinetics and bioequivalence of two tamsulosin extended-release capsules in Chinese volunteers under both fasting and fed conditions. A single-center, randomized, open-label, two-formulation, single-dose, two-period, two-way crossover design was used. A total of 64 healthy volunteers were enrolled, with 28 in the fasting group and 36 in the fed group. In the fasting group, each subject received a single dose of either the test or reference formulation in a randomized crossover design. In the fed group, volunteers consumed a high-fat meal 1 h before dosing. Blood samples were collected for up to 72 h post-dose, and plasma tamsulosin concentrations were measured using liquid chromatography-tandem mass spectrometry. The geometric mean ratios and 90% confidence intervals for key exposure metrics for both formulations under fasting and fed conditions were within the 0.8000-1.2500 bioequivalence range. Both formulations demonstrated bioequivalence under both conditions, and no severe adverse events were observed.

PMID 42474264
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