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At least 19 recordsLinked to original sources
PubMed1996

Brain pertussis toxin-sensitive G proteins are involved in the flavoxate hydrochloride-induced suppression of the micturition reflex in rats.

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.

Animals↗
PubMed1984

Pharmacological studies on the mode of action of flavoxate.

Previous studies on the mode of action of flavoxate have shown that the drug exerts a selective and direct muscle relaxant activity. In order to study the mode of action of flavoxate, the following activities were investigated: calcium blocking, inhibition of cyclic AMP phosphodiesterase (PDE), local anaesthetic activity, the effects on the synthesis and release of prostaglandins. In the K+-depolarized guinea-pig taenia coli, contracted by CaCl2, flavoxate and papaverine showed a moderate calcium antagonistic activity. Anticholinergic drugs, such as atropine and emepronium, did not exert a similar action. The antispasmodic activity of a drug can be correlated with inhibition of cyclic AMP phosphodiesterase, and since papaverine is a potent PDE inhibitor, we tested flavoxate for this activity. Flavoxate exerted a PDE inhibitory activity about three and five times greater than that of aminophylline in tissues homogenates of guinea-pig ureter and urinary bladder, respectively. It also showed the same local anaesthetic activity of lidocaine. Finally, the synthesis and release of prostaglandins by urinary bladder muscle in vitro have been investigated before and after treatment with flavoxate. Myolytic activity of papaverine and flavoxate do not involve inhibition of prostaglandins synthesis in rat urinary bladder in vitro. Therefore, the mode of action of flavoxate can be related to a superimposition of myotropic, calcium antagonistic and local anaesthetic activity.

3',5'-Cyclic-AMP Phosphodiesterases↗
PubMed1996

Mechanisms of the suppression of the bladder activity by flavoxate.

BACKGROUND: This study was designed to clarify the primary site of action of flavoxate, clinically used for the treatment of urinary frequency. METHODS: In rats, the effect of flavoxate on contractile responses in isolated detrusor strips, bladder contraction induced by pelvic nerve stimulation, isovolumetric rhythmic bladder contractions, and pelvic nerve activity were examined. In decerebrated cats, flavoxate was microinjected into the nuclei in the pons, and its effect on reflex micturition was observed. RESULTS: Flavoxate suppressed carbachol- and calcium ion (Ca2+)-induced contractions of isolated detrusor strips in a noncompetitive and a competitive manner, respectively. Intravenous flavoxate suppressed both initial phasic, and later tonic, bladder contractions induced by electrical stimulation of the distal end of the pelvic nerve. It abolished isovolumetric rhythmic bladder contractions and the associated efferent pelvic nerve activity, without affecting baseline vesical pressure and afferent pelvic nerve activity. When administered intracerebroventricularly or intrathecally, it abolished isovolumetric rhythmic bladder contractions. Flavoxate microinjected into the nucleus reticularis pontis oralis (PoO; pontine micturition inhibitory region) of decerebrated cats inhibited the reflex micturition, but had no effect when microinjected into the locus coeruleus alpha (pontine micturition center) or locus subcoeruleus (pontine urine storage center). CONCLUSIONS: Flavoxate suppressed the micturition reflex primarily by facilitating the inhibitory action of the PoO on the descending pathways from the pontine micturition center to the sacral parasympathetic intermediolateral nuclei.

Animals↗
PubMed1975

[The effects of flavoxate hydrochloride on the gastrointestinal motility (author's transl)].

The experiments were performed to study the effects of Flavoxate hydrochloride on the gastrointestinal motility and its underlying mechanism. Gastrointestinal motility was inhibited at first and then accelerated markedly after the intravenous injection of Flavoxate hydrochloride (10 mg/kg) in the experiments of anesthetized dogs. For analyzing the underlying mechanism of this response the following experiments were executed. 1) The pendular movements of isolated ileum of rabbits were accelerated with administration of low concentration of Flavoxate hydrochloride less than 10(5) g/ml, while these were reduced with administration of high concentration more than 10(4) g/ml. Because the tetrodotoxin (2.5 times 10(7) g/ml) has no essential effect on these responses, it could be postulated that Flavoxate hydrochloride has direct effect on intestinal smooth muscle itself. 2) Flavoxate hydrochloride (10 mg/kg) induced the differentiated regional response of the sympathetic outflow, that is, the parallel decrease of cutaneous and cardiac sympathetic activities, and the converse increase of splanchnic activity. Therefore, Flavoxate hydrochloride is thought to have an effect on the integrating mechanism of the sympathetic nervous system. This view was also supported by the experiments with neuromuscular preparation of lobster (Panulirus japonicus). It is concluded from these results, that the change of gastrointestinal motility induced by intravenous injection of Flavoxate hydrochloride (10 mg/kg) is influenced both by its effect on the gastrointestinal smooth muscle itself and by its effect via the autonomic nervous system.

Animals↗
PubMed1988

[Clinical effects of terodiline hydrochloride on urinary frequency and sense of residual urine--a double blind clinical trial using flavoxate hydrochloride as a control].

A double blind clinical trial was performed as a multicenter study to determine the usefulness of terodiline hydrochloride (HCl), an anticholinergic and calcium antagonistic agent, for urinary frequency or sense of residual urine in patients with psychogenic diseases, chronic prostatitis or chronic cystitis. Either 24 mg of terodiline HCl a day or 600 mg of flavoxate HCl a day was given for 4 weeks. One hundred and ninety-nine patients completed the test. The final global improvement rating was 70% in patients given terodiline HCl and 48% in patients given flavoxate HCl. The difference was statistically significant (p less than 0.01). Diurnal and nocturnal urinary frequency and urinary incontinence were less in patients given terodiline HCl than in patients given flavoxate HCl (p less than 0.01). No difference was noted between the two agents in relieving sense of residual urine. Compared with the control period, the average urinary frequency decreased 2.0 times a day in patients given terodiline HCl and 0.7 times in patients given flavoxate HCl. The difference was statistically significant (p less than 0.01). Adverse effects were observed in 12% of the patients given terodiline HCl and in 16% of the patients given flavoxate HCl. They included thirst, difficult urination, constipation, slight increase of serum GOT, GPT or alkaline phosphatase, and so forth. They disappeared with discontinued use of the agent. The global utility rating was 68% in patients given terodiline HCl and 45% in patients given flavoxate HCl, the difference being significant (p less than 0.01). These results indicate that terodiline HCl is useful for the treatment of urinary symptoms in patients with psychogenic diseases, chronic prostatitis or chronic cystitis.

Adolescent↗
PubMed1985

Mechanism of flavoxate antispasmodic activity comparative in vitro studies.

In order to clarify the pharmacological activity of flavoxate, its effect on the tone and spontaneous activity of the guinea-pig isolated ureter and of the muscle strip from rat urinary bladder were studied. Flavoxate, as well as papaverine, reduced all three parameters considered on the guinea-pig isolated ureter, namely: peristaltic motility, endoluminal pressure and longitudinal muscle contractility. In the same test, verapamil (a calcium antagonist), emepronium and atropine (both anticholinergic drugs) were used for comparison. Using strips of rat urinary bladder depolarized by KCl, flavoxate, papaverine and verapamil displayed a relaxant activity, while anticholinergic compounds such as atropine, hyoscine and emepronium failed to relax this tissue. In another series of experiments the effects of flavoxate and anticholinergic drugs on the contraction elicited by vagal electrical stimulation of the guinea-pig isolated stomach in toto were assayed. The results obtained suggest that the action of flavoxate is due to direct smooth muscle relaxation and does not involve anticholinergic activity.

Anesthetics, Local↗
PubMed1975

Urinary tract disorders. Clinical comparison of flavoxate and phenazopyridine.

In nine separate clinical trials, 382 patients having symptoms of either prostatitis, acute cystitis, urethritis, and/or trigonitis were randomly assigned to treatment with flavoxate or phenazopyridine. Over-all response was evaluated in 384 patients after five days of therapy. In patients having prostatitis, response was satisfactory in 66 per cent treated with flavoxate and 31 per cent treated with phenazopyridine. In all other patients, satisfactory responses were reported in 80 per cent on flavoxate compared with 56 per cent on phenazopyridine. Similarly, symptom-severity evaluations at two and five days of therapy showed most symptoms improved in more of the patients on flavoxate therapy than on phenazopyridine therapy. Although more adverse effects were reported in patients treated with phenazopyridine than with flavoxate, the difference between medications was not statistically significant.

Acute Disease↗
PubMed1999

Using flavoxate as primary medication for patients suffering from urge symptomatology.

A drug utilization observation study collected data on a total of 1800 patients given flavoxate (Spasuret 200) over 2 weeks for urge incontinence. Efficacy and tolerance parameters were determined. A subgroup of 618 patients without urinary tract infections or benign prostatic hyperplasia were treated with flavoxate only. The subgroup (n = 618) showed a reduction of dysuria (37%), nocturia (53%), and both daytime (61%) and nighttime urge (69%). Bladder volume at first urge sensation increased by 55.1+/-58.8 ml (36%), which was comparable to data from the entire group (1800 patients). In 89.2% of all patients the residual urine volume was stable or decreased. Undesirable side effects occurred in 1.8% of cases. Both groups showed better results with flavoxate four times daily (800 mg), compared to three times daily (600 mg). Flavoxate is effective and well tolerated and causes no additional problems due to residual urine or side effects.

Adult↗
PubMed1978

Comparative in vitro effects of imipramine, oxybutynin, and flavoxate on rabbit detrusor.

The ability of imipramine, oxybutynin, and flavoxate to antagonize carbamylcholine and barium chloride (BaCl2)-induced contractions of rabbit detrusor, and to block impulse conduction in desheathed frog sciatic nerves has been assessed in vitro. Impiramine exerts noncompetitive carbamylcholine and BaCl2 blockade by 10(-5) M and a local anesthetic effect equipotent with that of tetracaine. Oxybutynin exerts a strong competitive antagonism of carbamylcholine by 10(-8) M, a noncompetitive antagonism of BaCl2 equivalent to that of imipramine, and moderate local anesthetic activity. Flavoxate, under these experimental conditions exerts little anticholinergic, antispasmodis, or local anesthetic activity. Imipramine and oxybutynin thus demonstrate a number of smooth muscle effects by which their therapeutic actions may be exerted. The mechanisms of action of flavoxate remain obscure.

Anesthetics, Local↗
PubMed1980

The effect of flavoxate on uninhibited detrusor contractions and urinary incontinence in the elderly.

The effect of flavoxate, a smooth muscle relaxant, was investigated in 6 elderly patients with uninhibited detrusor contractions associated with urinary incontinence. Cystometry was done initially to confirm the diagnosis, immediately after an intravenous injection of 100 mg. flavoxate and after 200 mg. flavoxate orally 4 times daily for 7 days. No consistent drug effect could be detected cystometrically and incontinence was unchanged clinically.

Aged↗
PubMed1995

Flavoxate treatment of micturition disorders accompanying benign prostatic hypertrophy: a double-blind placebo-controlled multicenter investigation.

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.

Aged↗
PubMedDate not supplied

A review of flavoxate hydrochloride in the treatment of urge incontinence.

This article provides a review of the use of flavoxate hydrochloride in the treatment of urge incontinence. It outlines the pharmacology, mode of action, toxicology and pharmacokinetic studies which have been carried out, and then reviews the clinical studies, including those involving patients with benign prostatic hypertrophy. The effects of dosages of 600-1200 mg/day are compared, particularly regarding safety and tolerability factors. Finally, alternative therapies to flavoxate hydrochloride (alpha-adrenergic receptor blockers, oxybutinin chloride, terodiline hydrochloride, emepronium bromide and imipramine) are summarized. The article is written in the knowledge of recent evidence which indicates that flavoxate hydrochloride exhibits only weak anticholinergic activity on receptors involved in the control of the lower urinary tract.

Flavonoids↗
PubMedDate not supplied

Treatment of urgency and urge incontinence with flavoxate in the People's Republic of China.

Flavoxate is a smooth muscle relaxant widely used to treat urgency and urge incontinence. It has been used in an unblinded, uncontrolled clinical trial in 14 urology departments in universities and major hospitals in the People's Republic of China involving 361 patients with urgency/incontinence of various types. Patients were given 200 mg three times daily, orally, for 2 weeks, although 33 patients received a daily dosage of 1200 mg. Frequency, urgency, dysuria, nocturia and incontinence were assessed and scored clinically prior to and after treatment. Three departments also included urodynamic investigations, e.g. monitoring of the end-residual volume. Results from 336 evaluable patients indicate that 228 (67%) were completely cured of urgency/incontinence symptoms, 66 (20%) were improved and 42 (13%) patients were unchanged. Flavoxate was also effective in 77.4% of patients refractory to previous anti-cholinergic treatment. Treatment did not increase the end-residual volume and adverse events occurred only in four (1.3%) patients, two (0.6%) of which discontinued the therapy. The 1200 mg dose produced a complete cure in 82% of patients and improvement in the remaining 18%, with no side-effects. In conclusion, flavoxate is an effective and well tolerated treatment for urgency/incontinence of various causes.

Adolescent↗
PubMed1987

Flavoxate, a drug with smooth muscle relaxing activity.

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.

Flavonoids↗
PubMed1975

Flavoxate, a potent phosphodiesterase inhibitor.

The c-AMP phosphodiesterase inhibiting properties of flavoxate and of its main metabolite i.e. 3-methylflavone-8-carboxylic acid (MFCA), were assayed in vitro and compared to those of theophylline. Flavoxate and MFCA are competitive phosphodiesterase inhibitors, and are 21 and respectively 5 times more potent than theophylline. The smooth muscle relaxing activity of flavoxate possibly relies on this enzymatic mechanism.

Animals↗
PubMedDate not supplied

Paradoxical effect of flavoxate on human uterine contractility in vivo.

Flavoxate's effect on uterine contractility was investigated in 20 women with histories of primary dysmenorrhea. After 100 mg of the smooth muscle relaxant was infected intravenously, intrauterine pressure was recorded continuously for 1--2 hours. Immediately after the injection, intrauterine pressure and the frequency of contractions increased for 5--15 minutes at all phases of the menstrual cycle. After the activating response, there was a reduction in both the frequency of contractions and uterine tonus below preinjection levels in some patients. The paradoxical effect of flavoxate on uterine motility may be caused by its relaxation of vascular smooth muscle, which results in increased blood flow and, consequently, increased oxygen supply to the myometrium.

Adolescent↗
PubMed1977

Bladder muscle contractility. Comparative effects and mechanisms of action of atropine, propantheline, flavoxate, and imipramine.

The anticholinergic and antispasmodic activity of atropine, propantheline, imipramine, and flavoxate were judged by each drug's ability to inhibit bethanechol chloride and barium chloride-induced canine detrusor contractions. In this in vitro model, atropine and propantheline are pure anticholinergic agents. Imipramine significantly decreases both bethanechol and barium-induced contractions, while flavoxate only minimally inhibits the response to either stimulant.

Animals↗
PubMed1991

Antispasmodic effects of flavoxate, MFCA, and REC 15/2053 on smooth muscle of human prostate and urinary bladder.

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.

Adenoma↗