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Treatment of urgency by instillation of emepronium bromide in the urinary bladder.

The possibility of a purely local action of intravesically instilled emepronium bromide (Cetiprin) was investigated. Subjective reports and simultaneous urethrocystometry were used to assess such effect. In order to ascertain the purely local nature of effect, the serum was analyzed for freely circulating emepronium ion at increasing intravesical concentrations. No adverse effects were found at the highest dosage (100 mg in 100 ml saline solution), and the concentrations in serum were very low or were not detectable. The seemingly promising influence on micturition frequency and urge prompted a double-blind study of 20 patients with chronic urgency. In ten of them 100 mg emepronium bromide in 100 ml saline solution was instilled intravesically, while the other ten received only the same volume of saline solution. The symptoms were relieved in eight of the ten patients given emepronium bromide. The observation time was one week. The therapeutic possibilities were further evaluated in 24 women with frequency and urgency with or without urge incontinence. Emepronium bromide was intravesically instilled in the mentioned concentration and, if the symptoms were not totally relieved, this was repeated at weekly intervals. The maximum number of instillations was four and the observation time after the final treatment was at least three weeks. Frequency and urgency disappeared in approximately 70% of the affected women, nocturia in 60%, but urge incontinence in only 30%. Both frequency and urgency therefore were therapeutically influenced by intravesical instillation of emepronium bromide.

Administration, Topical

A second look at emepronium bromide in urinary incontinence.

Response to oral and intramuscular emepronium bromide was assessed cystometrically in nine patients with urinary incontinence caused by an uninhibited bladder. Oral therapy had no effect, whereas intramuscular administration increased bladder capacity and significantly delayed the onset of bladder spasm and the desire to void. Plasma-propranolol response was delayed and concentrations were reduced after an oral 40 mg dose of propranolol in 3 patients who had received oral emepronium bromide. These results indicate that although oral emepronium bromide had some anticholinergic effect--i.e., in reducing gastrointestinal motility--absorption of an oral dose was not sufficient for the bladder to be affected.

Administration, Oral

[Comparison of emepronium bromide with intravesical administration of lidocaine gel in women with urge incontinence].

In the treatment of urge incontinence, drug therapy predominates. In a prospective randomised study on treatment of females with motor urge incontinence, intravesically administered lidocaine-gel and oral emepronium bromide were compared using clinical and urodynamic parameters. From 30 patients, 15 women were treated for 3 weeks with repeated intravesical lidocaine gel instillations whilst the other 15 had a peroral emepronium bromide medication. The intravesical lidocaine gel installation proved more efficient compared with peroral emepronium bromide therapy with regard to the parameters of imperative micturition, occurrence of detrusor contractions as well as number of urinary frequencies per diem. Intravesical application of lidocaine-gel is particularly indicated in patients with increased sensitivity against parasympathicolytics and anticholinergics.

Administration, Intravesical

Electron-capture GC determination of subnanogram amounts of emepronium bromide in serum.

Barium peroxide in an acidic medium was utilized to increase the sensitivity in the benzophenone method for the determination of the quaternary ammonium compound emepronium bromide. The method is comprised of ion-pair extraction, oxidation, and quantitative determination of benzophenone by electron-capture GC. By employing small extraction and reaction volumes, the method was used in the 0.2--8-ng/ml range with a relative standard deviation of 2.5% at the 1-ng/ml level. The application of the method to human serum samples after a single oral dose demonstrated that the elimination phase for emepronium in serum had a half-life of 7--11 hr.

Administration, Oral

An urodynamic study of emepronium bromide in bladder dysfunction.

The effect of emepronium bromide in 13 patients, most of whom had uninhibited bladders, has been studied urodynamically. Under the influence of this drug, the detrusor pressure and the urinary flow was reduced, and abdominal straining during during micturition was commonly recorded. The bladder capacity increased considerably, but all subjects developed residual urine. The effect of emepronium bromide on the bladder capacity seemed to last for a longer period than the effect on the detrusor pressure.

Child

Vesical instillation of emepronium bromide in defunctionalized postobstructive noncompliant bladder: an alternative to intestinal augmentation surgery?

A contracted noncompliant bladder is an infrequent but severe complication of cutaneous ureterostomy. Recently, we effected a significant increase in bladder capacity by long-term, gentle hydraulic dilation with saline solution plus an anticholinergic drug (emepronium bromide). Based on this experience, we suggest a conservative approach like this before electing a patient for bladder augmentation or permanent diversion for any child with vesical contracture.

Administration, Intravesical

Emepronium bromide (Cetiprin) as a postoperative spasmolytic agent in transvesical prostatectomy.

To find out whether Cetiprin reduces the vesical spasms seen after cystotomias, a double-blind investigation including 22 men was carried out. Eleven of the men were given 25 mg Cetiprin i.m. twice a day for 2 days after transvesical prostatectomy, then 200 mg orally 3 times a day the following 12 days. The rest of the men, 11 patients, received placebo. In the Cetiprin group 9 patients had no vesical spasm postoperatively, whereas 1 had moderate and 1 had severe spasms. Only 4 patients were without spasms in the control group, whereas 5 had moderate and 2 severe spasms. The postoperative reduction of the bladder volume were counteracted by Cetiprin. No significant influence on liver- or kidney function was seen with the dosages mentioned.

Aged

Organic cation uptake in vitro by the rabbit iris-ciliary body, renal cortex, and choroid plexus.

The uptake in vitro of radioactively labeled test substances was studied in tissues from albino rabbits. Choroid plexus, slices of outer renal cortex, and iris-ciliary body were incubated in a K-rich medium containing one of the cations 14C-Emepronium (Cetiprin), 14C-tetraethylammonium, 14C-choline, or 125I-o-iodobenzyltrimethylammonium and sometimes the anions 131I-o-iodohippurate and 125I-iodipamide. Choroid plexus and renal cortex accumulated all test substances, some to very high tissue-medium ratios. The iris-ciliary body preparation accumulated the anions well but the organic cations only weakly. The only convincing uptake was that of Emepronium. The affinity of this uptake system seemed to be similar to that in the kidney, half-saturating around 10(-4)M Emepronium.

Animals