ascorbic-acid has been researched along with Urinary-Bladder--Overactive* in 2 studies
1 trial(s) available for ascorbic-acid and Urinary-Bladder--Overactive
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Absorption, metabolism, and excretion of [14C]imidafenacin, a new compound for treatment of overactive bladder, after oral administration to healthy male subjects.
The absorption, metabolism, and excretion of imidafenacin [KRP-197/ONO-8025, 4-(2-methyl-1H-imidazol-1-yl)-2,2-diphenylbutanamide], a new antimuscarinic drug developed for treatment of overactive bladder, were assessed in six healthy male subjects after a single oral administration of 0.25 mg of [(14)C]imidafenacin (approximately 46 microCi). The highest radioactivity in the plasma was observed at 1.5 h after administration. The apparent terminal elimination half-life of the total radioactivity was 72 h. Approximately 65.6 and 29.4% of the administered radioactivity were recovered in the urine and feces, respectively, within 192 h after administration. The metabolite profiling by high-performance liquid chromatography-radiodetector and liquid chromatography/tandem mass spectrometry demonstrated that the main component of radioactivity was unchanged imidafenacin in the 2-h plasma. The N-glucuronide conjugate (M-9) was found as the major metabolite and the oxidized form of the 2-methylimidazole moiety (M-2) and the ring-cleavage form (M-4) were detected as the minor metabolites in the 2-h plasma, but M-4 was found to be the main component in the 12-h plasma. Unchanged imidafenacin, M-9, M-2, and other oxidized metabolites were excreted in the urine, but the unchanged imidafenacin and M-9 were not found in the feces. Two unique metabolites were found in the urine and feces, which were identified as the interchangeable cis- and trans-isomers of 4,5-dihydrodiol forms of the 2-methylimidazole moiety. These findings indicate that imidafenacin is rapidly and well absorbed (at least 65% of dose recovered in urine) after oral administration, circulates in human plasma as the unchanged form, its glucuronide, and other metabolites, and is then excreted in urine and feces as the oxidized metabolites of 2-methylimidazole moiety. Topics: Adult; Area Under Curve; Ascorbic Acid; Biotransformation; Chromatography, High Pressure Liquid; Feces; Glucuronides; Half-Life; Humans; Imidazoles; Intestinal Absorption; Magnetic Resonance Spectroscopy; Male; Mass Spectrometry; Middle Aged; Muscarinic Antagonists; Oxidation-Reduction; Urinary Bladder, Overactive | 2007 |
1 other study(ies) available for ascorbic-acid and Urinary-Bladder--Overactive
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Modification of rat detrusor muscle contraction by ascorbic acid and citric acid involving enhanced neurotransmitter release and Ca2+ influx.
Consumption of carbonated soft drinks is independently associated with the development of overactive bladder (OR 1.41, 95% Cl 1.02-1.95). We have shown previously that artificial sweeteners, present in carbonated soft drinks, enhanced detrusor muscle contraction. Other constituents of soft drinks are preservatives and antioxidants, we evaluated the effects of two of these, ascorbic acid and citric acid, on the contractile response of isolated rat bladder muscle strips.. Detrusor muscle strips were suspended in a perfusion organ bath. We determined the effect of ascorbic acid and citric acid on the contractile responses to electrical field stimulation (EFS) in the absence and presence of atropine, carbachol, alpha, beta methylene ATP, potassium and calcium.. Ascorbic acid and citric acid (10(-7) M to 10(-3) M) enhanced the contractile response to 10 Hz EFS compared to control (P < 0.01). The frequency and amplitude of spontaneous bladder contractions were enhanced in the presence of ascorbic acid and citric acid by 14%, 21%, 21%, and 11% respectively. Ascorbic acid 10(-4) M significantly increased the atropine resistant response to EFS 5 Hz by 37% (P < 0.01) and inhibited contraction in response to carbachol 10(-4) M by 24%, (P < 0.05). Both ascorbic acid 10(-4) M and citric acid 10(-5) M significantly enhanced maximum contractile responses to alpha, beta methylene ATP, KCI and calcium compared to control.. Ascorbic acid and citric acid augmented bladder muscle contraction possibly by enhanced Ca(2+) influx. Presynaptic neurotransmitter release was enhanced by ascorbic acid. Carbonated beverages containing preservatives may aggravate symptoms of OAB. Topics: Adenosine Triphosphate; Animals; Antioxidants; Ascorbic Acid; Atropine; Calcium Signaling; Carbachol; Cholinergic Agonists; Citric Acid; Dose-Response Relationship, Drug; Electric Stimulation; Female; Food Preservatives; In Vitro Techniques; Muscarinic Antagonists; Muscle Contraction; Perfusion; Potassium; Presynaptic Terminals; Rats; Rats, Wistar; Time Factors; Urinary Bladder; Urinary Bladder, Overactive | 2009 |