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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

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

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

An objective comparison of the effects of parenterally administered drugs in patients suffering from detrusor instability.

Cystometric changes produced by 3 parenterally administered drugs, flavoxate hydrochloride, emepronium bromide and imipramine hydrochloride, have been evaluated in 15 female patients with detrusor instability. Each patient was given 2 of the 3 drugs and cystometric recordings were done 10 and 30 minutes after the administration of each drug. Emepronium bromide was found to be the only drug to cause a significant improvement in bladder capacity and reduction in detrusor pressure.

Adult

Uropharmacology: VII. Ganglionic stimulating and blocking agents.

A classification of the various ganglionic stimulants and blockers is presented, and their pharmacologic effects on the urinary bladder and urethra are discussed. Ganglionic stimulating drugs are of considerable interest in investigational work but are not presently used therapeutically. Ganglionic blockers include hexamethonium, tetraethylammonium, mecamylamine emepronium, pentolinium, chlorisondamine, and pemipidine. Of the numerous ganglionic blocking drugs that have appeared on the therapeutic scene, only mecamylamine, pentolinium, and trimethaphan are currently official.

Animals