Importance of pharmacological and physicochemical properties for tolerance of antimuscarinic drugs in the treatment of detrusor instability and detrusor hyperreflexia--chances for improvement of therapy.

Background: Antimuscarinic side-effects are relatively frequent problems in oral pharmacotherapy of detrusor instability and neurogenic dysfunction of the urinary bladder. Results of recent clinical trials demonstrate differences in tolerance between antimuscarinic drugs. It is the purpose of this paper to relate the available clinical data to the pharmacological and physicochemical properties of the different antimuscarinic drugs, in order to discuss the reasons for this enhanced tolerance and to make possible modes for improvement of antimuscarinic therapy plainly visible.

Effect of Trospium Chloride on Duodenal Motility during Upper Gastrointestinal Endoscopy: A Randomised, Double-Blind, Placebo-Controlled Trial.

In a placebo-controlled, double-blind study the effects of depressing duodenal motility by administration of intravenous trospium chloride during gastroduodenoscopy were studied in 72 patients randomised to receive trospium chloride or saline (controls). Intravenous trospium chloride 1.2mg stopped the visible contractile activity of the duodenum as assessed by 3 independent observers during videoendoscopy within 76 seconds (median).

Influences of trospium chloride and oxybutynin on quantitative EEG in healthy volunteers.

Trospium chloride and oxybutynin are two antimuscarinergic agents used in the treatment of unstable bladder, urge incontinence, combined stress urge incontinence and detrusor hyperreflexia. The possibility that these two drugs produce changes in central nervous electrical activity was examined in an open, prospective, phase I study involving 12 volunteers. Quantitative evaluation of the multichannel electroencephalogram obtained from young healthy volunteers showed statistically significant decreases in alpha and beta 1 activity after oxybutynin, but not after intravenous or oral administration of trospium chloride.

Ulcer relapse rates following initial treatment with bismuth subnitrate as compared with cimetidine respectively.

As part of an open clinical trial, 18 out of 23 (78%) patients were treated with bismuth subnitrate (3 x 700 mg/d) and 15 out of 25 (60%) patients were treated with cimetidine (1 x 800 mg/d) to cure peptic ulcers linked with H. pylori, as ascertained following an endoscopic examination. All patients underwent continued observation after complete healing on completion of four weeks of acute treatment.

A study relating to bioavailability and renal elimination of bismuth after oral administration of basic bismuth nitrate.

The extent to which bismuth is absorbed following single and multiple oral administration of basic bismuth nitrate was investigated in healthy male subjects. The blood concentration of bismuth and the amounts excreted in urine and feces were determined. The results show that only a small fraction of the administered bismuth dose given in this form is absorbed.