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1. We investigated the effects of selective alpha 1-adrenoceptor antagonists on rhythmic bladder contraction and cystometrograms as representative of urinary bladder function in urethane-anesthetized rats. 2. The selective alpha 1-adrenoceptor antagonists tamsulosin (0.03-3 micrograms/kg IV), prazosin (0.03-3 micrograms/ kg IV) and bunazosin (0.03-3 micrograms/kg IV) exerted little effect on the amplitude and frequency of rhythmic bladder contraction in anesthetized rats. In contrast, the antipollakiuria agent flavoxate (5 and 10 mg/kg IV) induced a dose-dependent disappearance in frequency without affecting the amplitude of the contractions. 3. Tamsulosin (1 and 3 micrograms/kg IV), prazosin (1 and 3 micrograms/kg IV), and bunazosin (1 and 3 micrograms/kg IV) exerted no effect on the cystometrogram, either. However, flavoxate (5 and 10 mg/kg IV) raised the micturition threshold pressure and prolonged the time to micturition. 4. These results suggest that the alpha 1-adrenoceptor plays little role in urinary bladder contraction in anesthetized rats.
To investigate the effect of flavoxate (Urispadol) treatment on patients with symptomatic benign prostatic hypertrophy (BPH), with the main weight on the irritative symptoms, a randomized, double-blind, parallel-group, placebo-controlled and multicenter investigation was carried out. Seventy patients entered the study, 37 were allocated to flavoxate treatment on a daily dose of 1,200 mg (400 mg t.i.d.) for 12 weeks, and 33 patients were allocated to placebo treatment. In spite of a sufficient power, the study did not discriminate the two treatment groups in a statistically significant way (p > 0.05), when considering the main endpoints: the irritative symptom score and the global patient evaluation. Conservative treatment of micturition disorders accompanying BPH with flavoxate in doses of 1,200 mg/day cannot be recommended for clinical use.
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Physical examination, liver function tests, serology tests, autoantibody tests, genetic analysis of the TATA box of the UGT1A1 gene, ultrasonography and CT scan; MRI cholangiography; liver biopsy.
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To evaluate what type of patient received tolterodine compared with the spasmolytic drugs previously marketed (oxybutynin, flavoxate, emepronium).
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Only a small proportion of incontinent NH residents with mobility and cognitive function potentially suitable for specific treatment for incontinence receives drug therapy for their condition. Further research is needed to determine whether low drug use reflects an unmet need for treating UI, or appropriate prescribing practices based on the multiple and interacting factors that influence decisions on drug therapy in the NH population.
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The antispasmodic effects of the flavone compounds flavoxate hydrochloride, 3-methylflavone carboxylic acid (MFCA), and REC 15/2053 (and in the case of the detrusor, oxybutynin), on the human detrusor, prostatic adenoma, prostatic capsule, and bladder neck, were studied by the in vitro isometric method. All the compounds inhibited, in different orders of potency, potassium-induced contractions of the tissues. Flavoxate showed a slightly greater activity than the other two compounds in the prostatic and bladder neck tissues. However, REC 15/2053 displayed greater activity in the detrusor than in the other tissues. The relaxant effect on the prostatic tissues suggests a potential use for these compounds in benign prostatic obstruction.
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Thirty-five patients with PV received NSAI drugs in the following intermittently steps (over a 3-month period): 1) Pygeum 100 mg twice a day for 14 consecutive days per month; 2) flavoxate-propyphenazone 400 mg twice a day plus Serratiopeptidase 10 000 U twice a day for the subsequent 14 days per month. All patients underwent semen analysis and TRUS scans in the pre-treatment and after 3 months of therapy.
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The present study aimed to clarify, by means of micro-spectroscopy, the mechanism of aggregation of particles into granules during high-shear granulation. We used two types of pharmaceutical granules prepared by high-shear granulator, one containing mefenamic acid and the other containing flavoxate hydrochloride as poorly soluble active pharmaceutical ingredients (APIs). Lactose, cornstarch, and microcrystalline cellulose were used as excipients; and hydroxypropyl cellulose (HPC) was used as the binding agent. The distributions of components in granules were visualized by mapping cross-sections of individual granules with techniques utilizing mid-infrared spectroscopy at the SPring-8 synchrotron radiation facility and micro-Raman spectroscopy. In the distribution maps of mefenamic acid granules, distributions of mefenamic acid, cornstarch, and microcrystalline cellulose overlapped; in flavoxate hydrochloride granules, on the other hand, distributions of flavoxate hydrochloride and lactose overlapped. Assessment of the surface free energy of each component found that ingredients with overlapping distribution had similar surface properties. Therefore, it was revealed that in high-shear granulation, in addition to the granulator operating conditions and general properties of the formulation itself (such as the solubility and particle size of each ingredient), the surface properties of the ingredients and their interrelationships were also factors that determined the aggregation behavior of the particles.
Flavoxate and tibolone were discontinued. Liver function test results improved progressively and normalized after almost 2 months.
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One of the more prevalent conditions associated with aging is urinary incontinence (UI), which may affect up to 55% of women and 34% of men older than 65 years. As a result of increasing longevity in developed nations, the proportion of UI-susceptible individuals continues to grow, presenting clinical and economic challenges to healthcare providers.
The objective of this study was to develop simple, precise, accurate and sensitive UV spectrophotometric methods for the simultaneous determination of ofloxacin (OFX) and flavoxate HCl (FLX) in pharmaceutical formulations. The first method is based on absorption ratio method, by formation of Q absorbance equation at 289 nm (λmax of OFX) and 322.4 nm (isoabsorptive point). The linearity range was found to be 1 to 30 μg/ml for FLX and OFX. In the method-II second derivative absorption at 311.4 nm for OFX (zero crossing for FLX) and at 246.2 nm for FLX (zero crossing for OFX) was used for the determination of the drugs and the linearity range was found to be 2 to 30 μg/ml for OFX and 2-75 μg /ml for FLX. The accuracy and precision of the methods were determined and validated statistically. Both the methods showed good reproducibility and recovery with % RSD less than 1.5%. Both the methods were found to be rapid, specific, precise and accurate and can be successfully applied for the routine analysis of OFX and FLX in combined dosage form.
The effect of Flavoxate on hyperactive detrusor contraction was studied in 37 patients, including 11 patients in whom the drug was administered intravenously during the urodynamic study. Beside the evaluation of frequency, nocturia and enuresis, the amplitude and the onset of uninhibited detrusor contraction (in correlation to bladder volume) was registered. The results showed subjective improvement in 61.3%. The complaints mentioned above improved in approximately 50%. The urodynamic data showed diminishing of the mean pressure during uninhibited detrusor contraction by almost 50% and the delay of the onset by 80% of bladder capacity. However, average bladder capacity increase was only 19%. It finally became obvious that the effect of Flavoxate was markedly worse in the neurogenic bladder group in comparison to the motoric urge patients.
To identify the factors that influence response to treatment of vesical instability.
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Effect of terodiline on isolated rabbit and guinea pig detrusor was investigated in comparison with that of flavoxate and oxybutynin. Terodiline (10(-6) M) parallelly shifted the dose-response curve for carbachol in rabbit detrusor to the right, and high doses of terodiline (3 X 10(-6)-3 X 10(-5) M) inhibited the maximal contraction. Flavoxate (10(-5) M or more) also inhibited the maximal contraction. Oxybutynin (10(-8) M or more) shifted the dose-response curve to the right, but did not affect the maximal contraction. At 3 X 10(-6) M or more, terodiline dose-dependently inhibited the Ca-contraction of rabbit detrusor. While the contraction of rabbit detrusor induced by electrical field stimulation was inhibited by atropine (3 X 10(-7) M) or nifedipine (3 X 10(-6) M) by 35% or 73%, respectively, the combination of atropine (10(-7) M) and nifedipine (10(-6) M) abolished it. Oxybutynin (3 X 10(-7) M) inhibited it by about 30%; terodiline (10(-6) M or more) and flavoxate (10(-5) M or more) dose-dependently inhibited it, and abolished at 10(-4) M and 3 X 10(-4) M, respectively. Terodiline inhibited the 1-quinuclidinyl-[phenyl-4-3H]-benzilate binding to the microsomal fraction of guinea pig urinary bladder, brain, atria and ileum dose-dependently, and it had similar affinity among these fractions. Terodiline (3 X 10(-6) M or more) inhibited the 45Ca uptake to minced guinea pig urinary bladder dose-dependently, but did not influence the 45Ca efflux even at 10(-4) M. Flavoxate (10(-4) M) only slightly inhibited the 45Ca uptake.(ABSTRACT TRUNCATED AT 250 WORDS)
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The effects on urodynamic parameters of i.v. administration of different drugs utilized in the therapy of detrusor instability, have been studied in conscious catheterized rats. Emepronium bromide, oxybutynin and nifedipine affected in a dose-dependent way the micturition pressure (MP), with sporadic changes in bladder volume capacity (BVC). Terodiline induced significant increases in BVC values in a wide range of doses. These changes, however, were always not dose-dependent. The drug significantly reduced MP only at the higher administered dose (10 mg/kg). Flavoxate induced increases of bladder capacity (BVC) not dependent on the administered doses, with no changes in micturition pressure (MP). Indomethacin significantly increased BVC and weakly reduced MP, but the effects were not dose-related. The effects of drugs on BVC were unrelated with the basal value of this parameter, whereas the decrease of MP seems to be related to high basal values before treatment. From a quantitative point of view, cystometrographic recordings in conscious normal rats can provide comparative data among drugs acting on bladder contractility (MP) such as anticholinergics and strong calcium antagonists.
A large organized database of prescriptions constructed by a database vendor was used in the study. Symmetry analysis was used to identify the risk of LUTS after using statins over the period January 2006 to August 2013. Statin use in combination with drugs administered for storage LUTS was examined by prescription sequence symmetry analysis (PSSA).
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Persistence with antimuscarinic therapy in overactive bladder (OAB) is poor, but may be different for mirabegron, a β3-adrenoceptor agonist with a different adverse event profile.
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Continuous cystometry was performed in 28 female rats. After the interval between bladder contractions was shortened by noradrenaline injection in the medial frontal lobe we injected glutamate or flavoxate hydrochloride in the rostral pontine reticular formation or intravenously injected flavoxate or propiverine. The change in bladder activity was examined.
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To examine the management of urinary incontinence (UI) among nursing home (NH) residents in the United States, particularly drug therapy for UI in those who may be suitable candidates for such treatment based on their functional status.
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Study patients were adults (aged e 18 years), with at least 1 pharmacy claim for either tolterodine extended-release (tol-ER), oxybutynin extended-release (oxy-ER), tolterodine immediate-release (tol-IR), or oxybutynin immediate-release (oxy-IR) during the period from July 1, 1999, to December 31, 2003, and were continuously eligible for benefits from 6 months before through 12 months after the initial OAB pharmacy claim (index) date. A retrospective cohort study design was used following patients from the index date to the occurrence of non-persistence with the index medication (i.e., a gap of > 45 days between successive prescription fills or a switch to any other OAB medication), or the end of a 1-year follow-up period, through December 31, 2004. Switching was defined as any change from the index medication, including a change in dose form (e.g., tol-IR to tol-ER), to one of the other 3 study drugs, or to a different OAB treatment (e.g., trospium chloride, oxybutynin patch, flavoxate, hyoscyamine sulfate, or propantheline bromide) during the follow-up period. Adherence was measured as the proportion of patients with a medication possession ratio (MPR) of at least 80%. MPR was calculated as (1) the sum of days supply for all pharmacy claims except the last pharmacy claim, divided by (2) the total number of days from the first fill date to the fill date of the last pharmacy claim. The association of drug therapy with study outcomes was assessed with bivariate and adjusted (multivariate) analyses. Multivariate analyses controlled for demographic and clinical characteristics, plan type, patient out-of-pocket cost for the index medication, and year of therapy initiation.