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The effects of tetraalkylammonium salts and sodium dodecyl sulphate on the migration behaviour of human urinary components and other negatively charged or neutral solutes were investigated. The sulphate acted mainly on hydrophobic and positively charged substances, whereas the ammonium salts acted mainly on negatively charged solutes. By choosing the components of the eluent carefully, the free and conjugate forms of 3-methylflavone-8-carboxylic acid (MFA) in human urine, the major metabolites of flavoxate, could be simultaneously determined without pretreatment, using fenprofen as an internal standard. The calibration curve of MFA was linear in the range 1-50 micrograms/ml and the detection limit was 0.2 microgram/ml, which covered the urine levels encountered in pharmacokinetic studies. The intra-day and inter-day precisions of the method, expressed as the relative standard deviation, were less than 2 and 3%, respectively. This method was successfully applied to an excretion study of MFA in eight healthy volunteers, and the results were in agreement with data in the literature obtained by gas chromatography.
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Cystometric changes produced by 3 parenterally administered drugs, flavoxate hydrochloride, emepronium bromide and imipramine hydrochloride, have been evaluated in 15 female patients with detrusor instability. Each patient was given 2 of the 3 drugs and cystometric recordings were done 10 and 30 minutes after the administration of each drug. Emepronium bromide was found to be the only drug to cause a significant improvement in bladder capacity and reduction in detrusor pressure.
NS-21 is under development for the treatment of urinary frequency and urinary incontinence. The purpose of this study was to investigate the effects of NS-21 and its active metabolite, RCC-36, on lower urinary tract function in an experimental rat model of urinary frequency.
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Noradrenaline injection in the medial frontal lobe shortened the interval between bladder contractions. In contrast to the bladder contraction interval before and after noradrenaline injection in the medial frontal lobe, the interval was prolonged after noradrenaline injection when glutamate or flavoxate was injected in the rostral pontine reticular formation, or flavoxate was injected intravenously. Noradrenaline injection in the medial frontal lobe plus intravenous propiverine injection also prolonged the interval compared to that after noradrenaline injection alone. However, the interval after noradrenaline injection in the medial frontal lobe plus intravenous injection of propiverine was shorter than that before noradrenaline injection only.
Flavoxate hydrochloride is a flavone derivative with smooth muscle relaxing activity. The product has a broad range of indications and has found one major application in the treatment of urge incontinence. Information on different forms of incontinence and epidemiologic data are summarized. Differences between the myolytic agent flavoxate and anticholinergics are highlighted. The vast amount of information deriving from some 20 years of clinical experience is analysed and major conclusions are drawn. The compound has valid therapeutic efficacy and excellent tolerability. By this token flavoxate is the agent of choice for therapy of disorders caused by smooth muscle spasms.
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Agents which exert their effect on the lower urinary tract by stimulating or depressing the activity of smooth muscle directly are discussed. Many of these drugs also exert other actions on the urinary tract mediated via the autonomic nervous system.
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Synonyms for radiation therapy and for the spectrum of radiation toxicity to the bladder in both text and MeSH terms were combined and applied to a range of databases without restriction of year of publication, methodology or language.
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In the current meta-analysis, 43 relevant published studies were considered which clearly demonstrated that flavoxate had improved clinical efficacy than placebo, emepronium, propantheline, and phenazopyridine.
Aged > or = 18 years, noninstitutionalized; initial therapy with tolterodine, oxybutynin, flavoxate, or emepronium.
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Sixty-three reports met the stated inclusion criteria. The majority were predominantly retrospective case series with the exception of two trials which were unrandomised and unblinded studies with a control group for comparison of effect. Although these two trials, Micic 1988, (intravesical placental extract) and Milani 1988, (flavoxate) provided the strongest evidence they were not randomised and were essentially isolated controlled studies.
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To compare persistence, adherence, and switch rates for the IR and ER formulations of oxybutynin and tolterodine for patients enrolled in a regional managed care plan.
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A 22-year-old man was referred to us complaining of enuresis. The excretory urogram and cystogram were almost normal. Spina bifida was not present. The results of the urodynamic examination including uroflowmetry, cystometry, urethral pressure profile, electromyogram and sensory threshold of external urethral sphincter were within normal limits. Amitriptyline hydrochloride and flavoxate hydrochloride showed no effects. Because we found a positive spike wave on the electroencephalogram, the patient was referred to a psychopathologist, and was diagnosed as being in the early stage of schizophrenia. He complained of enuresis as his olfactive hallucination of urine. Psychopathological treatment for 1 year and 2 months resulted in disappearance of his complaining of enuresis.
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The effect of flavoxate hydrochloride (flavoxate), an anti-pollakiurea agent, on cyclic AMP (cAMP) formation was investigated in the rat brain and a possible involvement of brain G proteins in the action of flavoxate on the bladder function was subsequently examined. Flavoxate (10(-8)-10(-5) M) inhibited cAMP formation in a concentration-dependent manner, an action which was completely abolished by pretreating the membranes with pertussis toxin (PTX). The inhibitory effect of flavoxate was also completely antagonized by combined treatment with any two antagonists for adenosine A1 (8-cyclopentyl-1,3-dipropylxanthine), dopamine D2 (sulpiride) or adrenergic alpha 2 (yohimbine) receptors, although each antagonist alone did not significantly block the flavoxate-induced inhibition of cAMP formation. Radioligand binding studies indicated that flavoxate at micro- or submicromolar concentrations has affinity for Gi-coupled receptors such as A1, D2 and alpha 2 receptors. Therefore, flavoxate may inhibit cAMP formation by the stimulation of A1, D2 and alpha 2 receptors. To clarify the involvement of brain Gi proteins in the flavoxate-induced inhibition of the micturition reflex, the effect of pretreatment with PTX (i.c.v.) on the flavoxate-induced inhibition of isovolumetric rhythmic bladder contractions was examined in rats. Flavoxate (3 mg/kg, i.v.) completely abolished rhythmic bladder contractions in vehicle-pretreated rats, but not in PTX-pretreated rats. These findings suggest that signal transduction via Gi-coupled receptors is involved, at least in part, in the inhibition of the micturition reflex by flavoxate in rats. These results also provide the first evidence suggesting a negative role of brain PTX-sensitive G proteins in the micturition reflex.
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To identify the factors that influence response to treatment of vesical instability.
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We performed a literature synthesis to identify the full spectrum of compounds implicated in drug-induced, bilateral secondary angle-closure glaucoma (2° ACG).