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https://www.readbyqxmd.com/read/28087463/effect-of-22-cyp2d6-variants-found-in-the-chinese-population-on-tolterodine-metabolism-in-vitro
#1
Hao Wang, Da-Peng Dai, Peng Sun, Li-Ping Xu, Bing-Qing Liang, Jian-Ping Cai, Guo-Xin Hu
Cytochrome P450 2D6 (CYP2D6) is an important member of the cytochrome P450 enzyme superfamily. We recently identified 22 novel variants in the Chinese population using PCR and bidirectional sequencing methods. The aim of this study is to characterize the enzymatic activity of these variants and their effects on the metabolism of the antimuscarinic drug tolterodine in vitro. A baculovirus-mediated expression system was used to express wild-type CYP2D6 and 24 variants (CYP2D6*2, CYP2D6*10, and 22 novel CYP2D6 variants) at high levels...
January 10, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28025920/impact-of-overactive-bladder-step-therapy-policies-on-medication-utilization-and-expenditures-among-treated-medicare-members
#2
Ibrahim M Abbass, Eleanor O Caplan, Daniel B Ng, Rita Kristy, Carol R Schermer, Pamela Bradt, Jenna M Collins, Wai Man Maria Chan, Brandon T Suehs
BACKGROUND: The impact of formulary management strategies on utilization and expenditures in overactive bladder (OAB) treatment has not been extensively investigated. In 2013, step therapy (ST) policies for 2 branded OAB treatments, mirabegron and fesoterodine, were removed from Humana Medicare Advantage Prescription Drug (MAPD) plans and Medicare prescription drug plans (PDP), allowing for an examination of the effect of ST policies on OAB medication use patterns and costs. OBJECTIVE: To assess the impact of removal of formulary restriction policies for mirabegron and fesoterodine on medication utilization patterns and costs associated with OAB treatment in Medicare patients...
January 2017: Journal of Managed Care & Specialty Pharmacy
https://www.readbyqxmd.com/read/27965369/pharmacological-characterization-of-a-novel-beta3-adrenergic-agonist-vibegron-evaluation-of-anti-muscarinic-receptor-selectivity-for-optimal-combination-therapy-for-overactive-bladder
#3
Jerry Di Salvo, Hiroshi Nagabukuro, Alexandra Wickham, Catherine Abbadie, Julie A DeMartino, Aileen Fitzmaurice, Loise Gichuru, Alison Kulick, Marcie J Donnelly, Nina Jochnowitz, Amanda Hurley, Antonio Pereira, Anthony Sanfiz, Gregory Veronin, Katherine Villa, John Woods, Beata Zamlynny, Emanuel Zycband, Gino M Salituro, Tara Frenkl, Ann E Weber, Scott D Edmondson, Mary Struthers
Although the physiological role of muscarinic receptors in bladder function and the therapeutic efficacy of muscarinic antagonists for the treatment of overactive bladder are well established, the role of β3-adrenergic receptors (β3ARs) and their potential as therapeutics is just emerging. In this manuscript, we characterized the pharmacology of a novel β3AR agonist vibegron (MK-4618, KRP-114V) and explored mechanistic interactions of β3AR agonism and muscarinic antagonism in urinary bladder function. Vibegron is a potent, selective full β3AR agonist across species and it dose-dependently increased bladder capacity, decreased micturition pressure and increased bladder compliance in rhesus monkeys...
December 13, 2016: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/27958220/efficacy-and-safety-of-medium-to-long-term-use-of-tolterodine-extended-release-with-or-without-tamsulosin-in-patients-with-benign-prostate-hyperplasia-and-larger-prostate-size-a-double-blind-placebo-controlled-randomized-clinical-trial
#4
Jian-Liang Cai, Zhe Zhou, Yan Yang, Yi-Fu Yan, Shuo Jing, Yan-Qun Na
BACKGROUND: The medium-to-long-term use of antimuscarinics alone or in combination with an α-blocker in men with an enlarged prostate is still controversial. This double-blind, placebo-controlled, randomized clinical trial aimed to investigate the efficacy and safety of medium-to-long-term use of tolterodine extended release (ER) with or without tamsulosin in patients with benign prostate hyperplasia (BPH) and larger prostate size. METHODS: Totally, 152 patients (age ≥50 years) with BPH, International Prostate Symptom Score (IPSS) ≥12, quality-of-life (QoL) score ≥3, and total prostate volume ≥25 ml were enrolled in this study...
2016: Chinese Medical Journal
https://www.readbyqxmd.com/read/27935011/electrical-stimulation-with-non-implanted-electrodes-for-overactive-bladder-in-adults
#5
REVIEW
Fiona Stewart, Luis F Gameiro, Regina El Dib, Monica O Gameiro, Anil Kapoor, Joao L Amaro
BACKGROUND: Several options exist for managing overactive bladder (OAB), including electrical stimulation (ES) with non-implanted devices, conservative treatment and drugs. Electrical stimulation with non-implanted devices aims to inhibit contractions of the detrusor muscle, potentially reducing urinary frequency and urgency. OBJECTIVES: To assess the effects of ES with non-implanted electrodes for OAB, with or without urgency urinary incontinence, compared with: placebo or any other active treatment; ES added to another intervention compared with the other intervention alone; different methods of ES compared with each other...
December 9, 2016: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/27878051/anticholinergics-for-overactive-bladder-temporal-trends-in-prescription-and-treatment-persistence
#6
Christopher J D Wallis, Colin Lundeen, Nicole Golda, Hilary Brotherhood, Peter Pommerville, Lesley Carr
INTRODUCTION: We sought to understand the contemporary pharmacologic management of overactive bladder (OAB) in a single-payer system. We examined temporal trends in the use of anticholinergic medications and assessed whether the likelihood of patients changing their anticholinergic therapy was predicted by their current therapy. METHODS: We conducted a retrospective, population-based analysis of prescription records from the PharmaNet database in BC, Canada. We identified patients treated with one or more anticholinergic prescriptions between 2001 and 2009...
August 2016: Canadian Urological Association Journal, Journal de L'Association des Urologues du Canada
https://www.readbyqxmd.com/read/27829538/pharmacokinetic-drug-interaction-study-between-overactive-bladder-drugs-mirabegron-and-tolterodine-in-japanese-healthy-postmenopausal-females
#7
Yuki Nomura, Hiromi Iitsuka, Junko Toyoshima, Kentaro Kuroishi, Toshifumi Hatta, Atsunori Kaibara, Masataka Katashima, Selina Moy, Taiji Sawamoto
Mirabegron, the first selective β3-adrenoceptor agonist for the treatment of overactive bladder (OAB), inhibits cytochrome P450 isozyme CYP2D6. This study was performed in Japanese healthy postmenopausal female volunteers to assess any pharmacokinetic drug interaction between mirabegron and tolterodine, another OAB drug and a sensitive substrate of CYP2D6. Tolterodine 4 mg was orally administered from Days 1-7 and co-administered with mirabegron 50 mg from Days 8-14. Mirabegron 50 mg increased maximum concentration (Cmax) and area under the concentration-time curve from zero to 24 h after dosing (AUC24h) of tolterodine by 2...
December 2016: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27789373/design-of-hydrogels-of-5-hydroxymethyl-tolterodine-and-their-studies-on-pharmacokinetics-pharmacodynamics-and-transdermal-mechanism
#8
Wenhua Liu, Lirong Teng, Kongtong Yu, Xiangshi Sun, Chunyu Fan, Chaoxing Long, Na Liu, Shuang Li, Bing Wu, Qingji Xu, Fengying Sun, Youxin Li
development, single-factor experiments were employed to evaluate the effect of adding different matrix, enhancers, 5-HMT, ethanol and glycerol on drug skin development, single-factor experiments were employed to evaluate the effect of adding different matrix, enhancers, 5-HMT, ethanol and glycerol on drug skin permeation. Finally, Carbopol 940 was selected as the gel matrix with N-methyl pyrrolidone (NMP) chosen as the enhancer. The relationship between time and the steady accumulative percutaneous amount (Q, μgcm(-2)) of optimized 5-HMT hydrogels was Q4-12h=1290...
January 1, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27738922/a-short-review-of-drug-food-interactions-of-medicines-treating-overactive-bladder-syndrome
#9
Paweł Paśko, Tomasz Rodacki, Renata Domagała-Rodacka, Danuta Owczarek
Background Overactive bladder syndrome is a condition where one or more of the symptoms such as pollakiuria, urgent need to urinate, nocturia and urinary incontinence is observed. Its prevalence ranges between 7 and 27 % in men and 9-43 % in women. The role of a pharmacist is to educate the patient on medications administration scheme, and drug interactions with particular food or food components. Aim of the review To assess a potential impact of food and fruit juice on the pharmacokinetic and therapeutic effects of medications used in treating overactive bladder syndrome...
December 2016: International Journal of Clinical Pharmacy
https://www.readbyqxmd.com/read/27695293/application-of-physiologically-based-pharmacokinetic-modeling-in-predicting-drug-drug-interactions-for-sarpogrelate-hydrochloride-in-humans
#10
Jee Sun Min, Doyun Kim, Jung Bae Park, Hyunjin Heo, Soo Hyeon Bae, Jae Hong Seo, Euichaul Oh, Soo Kyung Bae
BACKGROUND: Evaluating the potential risk of metabolic drug-drug interactions (DDIs) is clinically important. OBJECTIVE: To develop a physiologically based pharmacokinetic (PBPK) model for sarpogrelate hydrochloride and its active metabolite, (R,S)-1-{2-[2-(3-methoxyphenyl)ethyl]-phenoxy}-3-(dimethylamino)-2-propanol (M-1), in order to predict DDIs between sarpogrelate and the clinically relevant cytochrome P450 (CYP) 2D6 substrates, metoprolol, desipramine, dextromethorphan, imipramine, and tolterodine...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27681701/antimuscarinic-medication-use-in-elderly-patients-with-overactive-bladder
#11
Nandita Kachru, Sneha Sura, Satabdi Chatterjee, Rajender R Aparasu
BACKGROUND: Antimuscarinic medications are the first-line pharmacological treatment for overactive bladder (OAB); however, little is known about the utilization pattern of antimuscarinic agents in elderly patients with OAB. OBJECTIVE: This study examined the prevalence and predictors of antimuscarinic medication prescribing in elderly patients with OAB, using national ambulatory survey data. METHODS: This cross-sectional study utilized the 2009-2010 National Ambulatory Medical Care Survey and the outpatient component of the National Hospital Ambulatory Medical Care Survey...
October 2016: Drugs & Aging
https://www.readbyqxmd.com/read/27678410/differential-effects-of-the-enantiomers-of-tamsulosin-and-tolterodine-on-p-glycoprotein-and-cytochrome-p450-3a4
#12
Aneta Doricakova, Dirk Theile, Johanna Weiss, Radim Vrzal
The pregnane X receptor (PXR) is a transcription factor regulating P-glycoprotein (P-gp; ABCB1)-mediated transport and cytochrome P450 3A4 (CYP3A4)-mediated metabolism of xenobiotics thereby affecting the pharmacokinetics of many drugs and potentially modulating clinical efficacy. Thus, pharmacokinetic drug-drug interactions can arise from PXR activation. Here, we examined whether the selective α1-adrenoreceptor blocker tamsulosin or the antagonist of muscarinic receptors tolterodine affect PXR-mediated regulation of CYP3A4 and of P-gp at the messenger RNA (mRNA) and protein level in an enantiomer-specific way...
January 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/27589789/tolterodine-tartrate-proniosomal-gel-transdermal-delivery-for-overactive-bladder
#13
Rajan Rajabalaya, Guok Leen, Jestin Chellian, Srikumar Chakravarthi, Sheba R David
The goal of this study was to formulate and evaluate side effects of transdermal delivery of proniosomal gel compared to oral tolterodine tartrate (TT) for the treatment of overactive bladder (OAB). Proniosomal gels are surfactants, lipids and soy lecithin, prepared by coacervation phase separation. Formulations were analyzed for drug entrapment efficiency (EE), vesicle size, surface morphology, attenuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy, in vitro skin permeation, and in vivo effects...
August 31, 2016: Pharmaceutics
https://www.readbyqxmd.com/read/27579830/estimated-budget-impact-of-increased-use-of-mirabegron-a-novel-treatment-for-overactive-bladder
#14
Sinem Perk, Ronald C Wielage, Noll L Campbell, Timothy M Klein, Anthony Perkins, Linda M Posta, Thomas Yuran, Robert W Klein, Daniel B Ng
BACKGROUND: Oral pharmacological treatment for overactive bladder (OAB) consists of antimuscarinics and the beta-3 adrenergic agonist mirabegron. Antimuscarinic adverse events (AEs) such as dry mouth, constipation, and blurry vision can result in frequent treatment discontinuation rates, leaving part of the OAB population untreated. Antimuscarinics also contribute to a patient's anticholinergic cognitive burden (ACB), so the Beers Criteria recommends cautious use of antimuscarinics in elderly patients who take multiple anticholinergic medications or have cognitive impairment...
September 2016: Journal of Managed Care & Specialty Pharmacy
https://www.readbyqxmd.com/read/27574750/estimated-budget-impact-of-increased-use-of-mirabegron-a-novel-treatment-for-overactive-bladder
#15
Sinem Perk, Ronald C Wielage, Noll L Campbell, Timothy M Klein, Anthony Perkins, Linda M Posta, Thomas Yuran, Robert W Klein, Daniel B Ng
BACKGROUND: Oral pharmacological treatment for overactive bladder (OAB) consists of antimuscarinics and the beta-3 adrenergic agonist mirabegron. Antimuscarinic adverse events (AEs) such as dry mouth, constipation, and blurry vision can result in frequent treatment discontinuation rates, leaving part of the OAB population untreated. Antimuscarinics also contribute to a patient's anticholinergic cognitive burden (ACB), so the Beers Criteria recommends cautious use of antimuscarinics in elderly patients who take multiple anticholinergic medications or have cognitive impairment...
September 2016: Journal of Managed Care & Specialty Pharmacy
https://www.readbyqxmd.com/read/27569391/tolterodine-reduces-veratridine-augmented-late-ina-reverse-incx-and-early-afterdepolarizations-in-isolated-rabbit-ventricular-myocytes
#16
Chao Wang, Lei-Lei Wang, Chi Zhang, Zhen-Zhen Cao, An-Tao Luo, Pei-Hua Zhang, Xin-Rong Fan, Ji-Hua Ma
AIM: The augmentation of late sodium current (INa.L) not only causes intracellular Na(+) accumulation, which results in intracellular Ca(2+) overload via the reverse mode of the Na(+)/Ca(2+) exchange current (reverse-INCX), but also prolongs APD and induces early afterdepolarizations (EAD), which can lead to arrhythmia and cardiac dysfunction. Thus, the inhibition of INa.L is considered to be a potential way for therapeutic intervention in ischemia and heart failure. In this study we investigated the effects of tolterodine (Tol), a competitive muscarinic receptor antagonist, on normal and veratridine (Ver)-augmented INa...
November 2016: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/27503124/the-combination-of-herbal-medicine-weng-li-tong-with-tolterodine-may-be-better-than-tolterodine-alone-in-the-treatment-of-overactive-bladder-in-women-a-randomized-placebo-controlled-prospective-trial
#17
Dong-Dong Xiao, Jian-Wei Lv, Xin Xie, Xing-Wei Jin, Mu-Jun Lu, Yuan Shao
BACKGROUND: To assess the efficacy and safety of the herbal medicine, Weng-li-tong (WLT) as monotherapy or combined with tolterodine in women with overactive bladder (OAB). METHODS: A prospective, randomized, single-blind multi-center trial was performed which included 182 OAB patients treated with either placebo (n = 26), WLT (n = 52), tolterodine (n = 52) or WLT plus tolterodine (n = 52). The overactive bladder symptom score (OABSS) and micturition behavior were measured to evaluate treatment efficacy...
August 8, 2016: BMC Urology
https://www.readbyqxmd.com/read/27326725/mirabegron-for-the-treatment-of-overactive-bladder-cost-effectiveness-from-us-commercial-health-plan-and-medicare-advantage-perspectives
#18
Ronald C Wielage, Sinem Perk, Noll L Campbell, Timothy M Klein, Linda M Posta, Thomas Yuran, Robert W Klein, Daniel B Ng
BACKGROUND AND OBJECTIVE: The first class of oral pharmacologic treatments for overactive bladder (OAB) are antimuscarinics that are associated with poor persistence, anticholinergic adverse events, and increased anticholinergic burden (ACB) with risk of cognitive impairment. Mirabegron, a β3-adrenoceptor agonist, is an oral treatment that does not contribute to ACB and has early evidence of improved persistence. The objective of the analysis was to assess the cost-effectiveness of mirabegron for OAB vs six antimuscarinics in the US...
December 2016: Journal of Medical Economics
https://www.readbyqxmd.com/read/27275433/an-overlooked-effect-of-systemic-anticholinergics-alteration-on-accommodation-amplitude
#19
Mehmet Ali Sekeroglu, Emre Hekimoglu, Mustafa Alpaslan Anayol, Yasemin Tasci, Ismail Dolen
AIM: To investigate the effect of oral solifenacin succinate, tolterodine-L-tartarate and oxybutinin hydrochloride (HCl) on accommodation amplitude. METHODS: Female overactive bladder syndrome (OAB) patients who were planned to use oral anticholinergics, patients that uses solifenacin succinate 5 mg (Group I, n=25), tolterodine-L-tartarate 4 mg (Group II, n=25), and oxybutinin HCl 5 mg b.i.d (Group III, n=25) and age matched healthy female subjects (Group IV, n=25) were recruited and complete ophthalmological examination and accommodation amplitude assessment were done at baseline and 4wk after initiation of treatment...
2016: International Journal of Ophthalmology
https://www.readbyqxmd.com/read/27260129/a-randomized-open-label-comparative-study-of-efficacy-and-safety-of-tolterodine-combined-with-tamsulosin-or-doxazosin-in-patients-with-benign-prostatic-hyperplasia
#20
Yanwei Cao, Yonghua Wang, Lei Guo, Xuecheng Yang, Tao Chen, Haitao Niu
BACKGROUND Benign prostatic hyperplasia (BPH), a common disease in men over age 50 years, often causes bladder outlet obstruction and lower urinary tract symptoms (LUTS). Alpha blockers in combination with muscarinic receptor antagonists may have the potential to improve symptoms. This study aimed to assess the efficacy and safety of doxazosin or tamsulosin combined with tolterodine extend release (ER) in patients with BPH and LUTS. MATERIAL AND METHODS In a prospective, randomized, open-label study (ChiCTR-IPR-15005763), 220 consecutive men with BPH and LUTS were allocated to receive doxazosin 4 mg and tolterodine ER 4 mg per day (doxazosin group) or tamsulosin 0...
June 4, 2016: Medical Science Monitor: International Medical Journal of Experimental and Clinical Research
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