Disease relevance of flavoxate

• The effect of flavoxate on uninhibited detrusor contractions and urinary incontinence in the elderly [1].
• 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) [2].
• Forty patients, aged 51 to 79 years, with nocturia due to bladder instability, resorption of postural edema, or senile decay, were treated with rociverine or flavoxate to test the possibility of reducing or eliminating nocturnal voidings [3].
• 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 [4].
• By this token flavoxate is the agent of choice for therapy of disorders caused by smooth muscle spasms [5].

High impact information on flavoxate

• These results suggest that flavoxate caused muscle relaxation through the inhibition of L-type Ca(2+) channels in human detrusor [6].
• Of the investigated alternative drug regimens, the papaverine-like smooth muscle relaxant flavoxate was reported to be ineffective [7].
• 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 [2].
• REC 15/2053 showed only weak binding to [3H]nitrendipine sites (IC50 = 14 microM) and muscarinic receptors (IC50 = 18 microM), whereas flavoxate was slightly active only at muscarinic receptors (IC50 = 12.2 microM) [8].
• 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 [9].

Chemical compound and disease context of flavoxate

• A comparison of flavoxate, emepronium, propantheline and a placebo for the treatment of urinary incontinence due to bladder instability is made, the results are discussed and recommendations are made [10].

Biological context of flavoxate

• Pharmacokinetics of Flavoxate in man [11].
• Development of a high-performance liquid chromatographic method for bioequivalence study of flavoxate tablets [12].

Anatomical context of flavoxate

• 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 [13].
• Conformational evaluation and detailed (1)H and (13)C NMR assignments of flavoxate, a urinary tract antispasmodic agent [14].
• 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 [15].
• 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) [16].
• 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 [17].

Associations of flavoxate with other chemical compounds

• Comparative in vitro effects of imipramine, oxybutynin, and flavoxate on rabbit detrusor [13].
• In each of these experimental models rociverine was more effective than flavoxate [18].
• DATA SOURCES: MEDLINE (1966-December 1998) was searched for relevant publications using the following search terms: UI, UI in the elderly, treatment of UI, oxybutynin, flavoxate, vasopressin, quality of life in UI, and economic impact of UI [19].
• 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 [20].
• Tiropramide in general was more potent than reference agents such as papaverine or flavoxate and was active also after oral administration [21].

Analytical, diagnostic and therapeutic context of flavoxate

• 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 [1].
• Intravenous flavoxate suppressed both initial phasic, and later tonic, bladder contractions induced by electrical stimulation of the distal end of the pelvic nerve [16].
• The plasma levels, the urinary excretion and the biliary excretion of piperidinoethyl-3-methylflavone-8-carboxylate (flavoxate, F) were studied in rats after i.v. and after oral administration [22].
• Double-blind, placebo-controlled, cross-over study of flavoxate in the treatment of idiopathic detrusor instability [23].
• Finally, the synthesis and release of prostaglandins by urinary bladder muscle in vitro have been investigated before and after treatment with flavoxate [24].

References