Efficacy of the combination of KPR-5714, a novel transient receptor potential melastatin 8 (TRPM8) antagonist, and β < sub > 3 < /sub > -adrenoceptor agonist or anticholinergic agent on bladder dysfunction in rats with bladder overactivity
Eur J Pharmacol. 2021 Mar 3:173995. doi: 10.1016/j.ejphar.2021.173995. Online ahead of print.ABSTRACTTransient receptor potential melastatin 8 (TRPM8) channels may contribute to the pathophysiological bladder afferent hyperactivity, thus a TRPM8 antagonist would be a promising therapeutic target for the bladder hypersensitive disorders including urinary urgency in overactive bladder (OAB). We aimed to investigate a pharmacological effect of KPR-5714, a novel selective TRPM8 antagonist, on TRPM8 channels, M3 receptors and β3-adrenoceptors using the transfected cells of each gene at first. Then, combination effects of KPR-5...
Source: European Journal of Pharmacology - March 6, 2021 Category: Drugs & Pharmacology Authors: Naoki Aizawa Yoshikazu Fujimori Osamu Nakanishi Takemitsu Hayashi Yoshiaki Goi Jun-Ichi Kobayashi Tomoe Fujita Source Type: research

Efficacy of the combination of KPR-5714, a novel transient receptor potential melastatin 8 (TRPM8) antagonist, and β < sub > 3 < /sub > -adrenoceptor agonist or anticholinergic agent on bladder dysfunction in rats with bladder overactivity
Eur J Pharmacol. 2021 Mar 3:173995. doi: 10.1016/j.ejphar.2021.173995. Online ahead of print.ABSTRACTTransient receptor potential melastatin 8 (TRPM8) channels may contribute to the pathophysiological bladder afferent hyperactivity, thus a TRPM8 antagonist would be a promising therapeutic target for the bladder hypersensitive disorders including urinary urgency in overactive bladder (OAB). We aimed to investigate a pharmacological effect of KPR-5714, a novel selective TRPM8 antagonist, on TRPM8 channels, M3 receptors and β3-adrenoceptors using the transfected cells of each gene at first. Then, combination effects of KPR-5...
Source: European Journal of Pharmacology - March 6, 2021 Category: Drugs & Pharmacology Authors: Naoki Aizawa Yoshikazu Fujimori Osamu Nakanishi Takemitsu Hayashi Yoshiaki Goi Jun-Ichi Kobayashi Tomoe Fujita Source Type: research

Potential of mirabegron and its extended-release formulations for the treatment of overactive bladder syndrome.
Conclusion: Mirabegron shows a distinct mode of action, i.e., targeting β3-adrenoreceptors and improve bladder storage without altering void contractions. The limited side effects, high safety, efficacy and tolerability of mirabegron present an adequate substitute to antimuscarinics. However, long-term analysis and clinical studies are prerequisites for assessing the safety , tolerebility and efficacy profile of mirabegron. PMID: 32334500 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - April 24, 2020 Category: Drugs & Pharmacology Authors: Mandpe P, Prabhakar B, Shende P Tags: Curr Drug Metab Source Type: research

Acupuncture for overactive bladder in adults: a systematic review and meta-analysis.
CONCLUSIONS: No significant differences in effectiveness or efficacy were found between acupuncture and drug or between verum and sham acupuncture, respectively. Further high-quality studies are required. PMID: 31433197 [PubMed - as supplied by publisher] (Source: Acupuncture in Medicine : journal of the British Medical Acupuncture Society)
Source: Acupuncture in Medicine : journal of the British Medical Acupuncture Society - August 20, 2019 Category: Complementary Medicine Authors: Mak TC, Cho WC, Chen HY Tags: Acupunct Med Source Type: research

Which antimuscarinic agents used in the treatment of overactive bladder increase heart rate? a prospective randomized clinical trial
ConclusionsOur results showed that heart rate significantly increased in OAB patients treated with non-selective antimuscarinic drugs. Trospium chloride, tolterodine tartrate, fesoterodine fumarate and propiverine hydrochloride seem to have the most unfavorable properties with regard to increased heart rate side effect when compared to the other antimuscarinic drugs (darifenacin hydrobromide, solifenacin succinate and oxybutynin hydrochloride). (Source: International Urology and Nephrology)
Source: International Urology and Nephrology - February 6, 2019 Category: Urology & Nephrology Source Type: research

Influence of CYP2D6 genetic polymorphism on pharmacokinetics of active moiety of tolterodine.
This study investigated the relationship between CYP2D6 genotypes and pharmacokinetics of tolterodine and its active metabolite in healthy Korean subjects. All volunteers were genotyped for CYP2D6 and divided into four different genotype groups (CYP2D6*wt/*wt [*wt = *1 or *2], CYP2D6*wt/*10, CYP2D6*10/*10, and CYP2D6*5/*10). Each subject received a single oral dose of tolterodine tartrate (2 mg) in single-dose phase of the study. After the single-dose phase of the study, the same subjects received a single oral dose of tolterodine tartrate (2 mg) once daily for 1 week during multiple-dose tolterodine administration ...
Source: Archives of Pharmacal Research - December 12, 2018 Category: Drugs & Pharmacology Authors: Byeon JY, Lee CM, Lee YJ, Kim YH, Kim SH, Jung EH, Chae WK, Lee YJ, Jang CG, Lee SY Tags: Arch Pharm Res Source Type: research

Validated electroanalytical determination of flavoxate hydrochloride and tolterodine tartrate drugs in bulk, dosage forms and urine using modified carbon paste electrodes
Publication date: May 2018Source: Arabian Journal of Chemistry, Volume 11, Issue 4Author(s): Ali K. Attia, Eman Y.Z. Frag, Heba E. AhmedAbstractSimple, precise, inexpensive and sensitive voltammetric methods have been developed for the determination of flavoxate HCl (FLXHC) and tolterodine tartrate (TOLT) in the bulk, pharmaceutical dosage forms and human urine using ferrocene modified carbon paste electrode (FMCPE) for FLXHC and polyethylene glycol modified carbon paste electrode (PEGMCPE) for TOLT. The electrochemical behavior of FLXHC and TOLT showed irreversible diffusion-controlled oxidation processes in Britton-Robin...
Source: Arabian Journal of Chemistry - July 11, 2018 Category: Chemistry Source Type: research

Clinical observation on electroacupuncture at four sacral points for overactive bladder syndrome
ConclusionEA at four sacral points is an effective method for overactive bladder syndrome. (Source: Journal of Acupuncture and Tuina Science)
Source: Journal of Acupuncture and Tuina Science - June 1, 2018 Category: Complementary Medicine Source Type: research

Transdermal delivery of tolterodine tartrate for overactive bladder treatment: In vitro and in vivo evaluation.
Abstract The purpose of the study was to develop a transdermal tolterodine tartrate (TT) patch and to analyse its efficacy for overactive bladder (OAB) treatment. Patches were prepared using various polymers and plasticizers via the solvent casting method. The patches were characterized for tensile strength, thickness, moisture content, modulus of elasticity and water absorption capacity. Differential scanning calorimetry and Fourier transform infrared analyses were also performed. To determine patch effectiveness, in vitro release, permeation and animal studies were performed. The patches showed satisfact...
Source: Acta Pharmaceutica - September 1, 2017 Category: Drugs & Pharmacology Authors: Rajabalaya R, Mun CY, Chellian J, Chakravarthi S, David SR Tags: Acta Pharm Source Type: research

Validated electroanalytical determination of flavoxate hydrochloride and tolterodine tartrate drugs in bulk, dosage forms and urine using modified carbon paste electrodes
Publication date: Available online 30 July 2016 Source:Arabian Journal of Chemistry Author(s): Ali K. Attia, Eman Y.Z. Frag, Heba E. Ahmed A simple, precise, inexpensive and sensitive voltammetric methods have been developed for the determination of flavoxate HCl (FLXHC) and toltoridine tartarate (TOLT) in the bulk, pharmaceutical dosage forms and human urine using ferrocene modified carbon paste electrode (FMCPE) for FLXHC and polyethylene glycol modified carbon paste electrode (PEGMCPE) for TOLT. The electrochemical behavior of FLXHC and TOLT showed irreversible diffusion-controlled oxidation processes in Britton-Ro...
Source: Arabian Journal of Chemistry - July 31, 2016 Category: Chemistry Source Type: research

Combined Tolterodine and Vaginal Estradiol Cream for Overactive Bladder Symptoms After Randomized Single-Therapy Treatment
Conclusions: Significant within-group improvement in OAB-q symptom bother was noted in both the intravaginal estradiol and tolterodine groups for OAB symptoms, with no difference between groups. Greater improvement from 12-week single therapy to 24 and 52 weeks of combined therapy was noted in the group originally assigned to intravaginal estradiol. The role of combined medical therapy for OAB symptoms needs further investigation. (Source: Journal of Pelvic Medicine and Surgery)
Source: Journal of Pelvic Medicine and Surgery - June 24, 2016 Category: Surgery Tags: Original Articles Source Type: research

Results of a randomized, double ‐blind, active‐controlled clinical trial with propiverine extended release 30 mg in patients with overactive bladder
ConclusionsPropiverine ER 30 mg was confirmed to be an effective and well‐tolerated treatment option for patients with OAB symptoms. This first head‐to‐head study showed non‐inferiority of propiverine ER 30 mg compared with tolterodine ER 4 mg. (Source: BJU International)
Source: BJU International - May 12, 2016 Category: Urology & Nephrology Authors: Jing Leng, Limin Liao, Ben Wan, Chuanjun Du, Wei Li, Keji Xie, Zhoujun Shen, Zhuoqun Xu, Shiliang Wu, Zujun Fang, Lulin Ma, Shaomei Han, Cornelia Feustel, Yong Yang, Helmut Madersbacher Tags: Original Article Source Type: research

Results of a randomized, double‐blind, active‐controlled clinical trial with propiverine extended release 30 mg in patients with overactive bladder
ConclusionsPropiverine ER 30 mg was confirmed to be an effective and well‐tolerated treatment option for patients with OAB symptoms. This first head‐to‐head study showed non‐inferiority of propiverine ER 30 mg compared with tolterodine ER 4 mg. (Source: BJU International)
Source: BJU International - May 12, 2016 Category: Urology & Nephrology Authors: Jing Leng, Limin Liao, Ben Wan, Chuanjun Du, Wei Li, Keji Xie, Zhoujun Shen, Zhuoqun Xu, Shiliang Wu, Zujun Fang, Lulin Ma, Shaomei Han, Cornelia Feustel, Yong Yang, Helmut Madersbacher Tags: Original Article Source Type: research