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At least 19 recordsLinked to original sources

PubMed1983

A comparison between the combination emepronium bromide/flavoxate and emepronium bromide in the treatment of detrusor instability.

Emepronium bromide and flavoxate have both and separately been used with success in the treatment of detrusor instability. In this study we have combined the two drugs emepronium bromide and flavoxate and compared the results with emepronium bromide. 20 consecutive patients with an uninhibited bladder, 12 men and 8 women, were randomly allocated to treatment with either emepronium bromide/flavoxate or emepronium bromide. In this trial we found that treatment with the combination is significantly better than treatment with emepronium bromide only.

Adult↗

PubMed1985

Ion pair formation and gastrointestinal absorption of emepronium.

Ion pair forming agents were evaluated in vitro for their ability to form lipophilic ion pairs with the quaternary ammonium compound emepronium and in vivo to enhance its gastrointestinal absorption. A 5- to 100-fold excess of trichloroacetate (TCA), diethylhexylphosphate (DEHPA), heptafluorobutyrate (HFBA), sodium lauryl sulphate (SLS), bromide or chloride all increased the extractability of the emepronium ion into methylene chloride. The additive with the most marked effect on the apparent partition coefficient of emepronium (Kapp) was SLS. At emepronium 10(-4) M, Kapp increased from a basal value of 0.1 to 368 with a 100-fold molar excess. However, the increased partitioning to methylene chloride was not reflected in an increased gastrointestinal absorption of the emepronium ion when this was given orally to mice. When intestinal juice, instead of distilled water or buffer, was used as the aqueous phase, the partition coefficient was markedly higher (Kapp approximately 2) but it was significantly less influenced by addition of sodium lauryl sulphate (Kapp approximately 6). The preexisting positive influence of the intestinal juice on the lipophilic character of emepronium and the rather limited additive effect of agents that form lipophilic complexes with emepronium, lead to the conclusion that the ion pair concept is not a suitable approach to enhance the gastrointestinal absorption of this drug.

Animals↗

PubMed1985

Pharmacokinetics and pharmacodynamics of emepronium bromide (Cetiprin) after intravenous administration in man.

Intravenous doses of 1, 5, 10 and 15 mg of emepronium bromide were given to three healthy volunteers. Emepronium serum concentration declined in a triexponential manner with half-lives between 2.2-3.0 min., 1.0-1.6 hours and 5.1-13 hours, respectively. The initial dilution space (volume of the central compartment) varied between 4.1-7.5 l. The area under the serum concentration time curve increased linearly with dose, indicating constancy of total serum clearance (range: 24-38 l/hr) with dose. The renal clearance of emepronium varied with serum concentration; secretion in addition to glomerular filtration was evident. Tubular secretion of emepronium was half-saturated at serum concentrations of approximately 50 nmol/l. No obvious drug-related effect on blood pressure was noted, whereas salivary secretion decreased and heart rate increased with 10-15% at emepronium serum concentrations of about 200 nmol/l. ECG recordings were without abnormalities after slow intravenous injections of emepronium bromide in doses of up to 15 mg. Since no adverse effects were noted, intravenous administration of emepronium bromide may be an alternative in situations where the drug is now used intramuscularly e.g. severe tenesmus in the urinary bladder.

Administration, Oral↗

PubMed1978

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↗

PubMed1987

Gastrointestinal transit rate-related absorption of emepronium: a study in mice.

The gastrointestinal (GI) absorption in mice of the anticholinergic quaternary ammonium compound emepronium, assessed by the urinary excretion of radioactivity and unchanged drug, increased from 1% to 7% and from 0.5% to 5%, respectively, in the dose range 0.1 to 40 mg/kg, whereafter a plateau was reached. Changes in the metabolism were evident at doses exceeding 80 mg/kg when 80% of the radioactivity was excreted as unchanged emepronium, as compared to 50% at lower doses. No dose-dependent urinary excretion of radioactivity was detected following intravenous injection. The increase in the fraction of the dose excreted in the urine after oral administration therefore cannot be easily explained by a dose-dependent metabolism or renal excretion. However, a relationship was seen between the reduced gastrointestinal motility, produced by increasing doses of the drug, and the increased bioavailability. Atropine sulphate given subcutaneously (1-50 mg/kg) more than doubled the urinary recovery of a small pharmacologically inactive oral dose of emepronium (5 mg/kg) and thus confirmed the transit rate-dependent absorption of emepronium. The superimposed effect of the pharmacological action on the GI transit rate, derived from the inherent property of an anticholinergic drug, may be of special significance for a drug with a low degree of absorption and a high variability, such as has been observed in clinical trials with the quaternary drug emepronium (Cetiprin).

Animals↗

PubMed1988

Relationship between gastric emptying and serum concentrations of emepronium in dogs and human volunteers.

Clinical trials with increased dosages, relative to the standard regimen, of the anticholinergic drug emepronium (Cetiprin Novum) resulted in a clear improvement in micturition- and urodynamic parameters in urinary incontinent patients. In the present study possible effects on the gastric emptying were tested in dogs and in human volunteers. In dogs a wide dose range of emepronium (5-100 mg/kg p.o.) was used to establish a relationship between serum concentration and effect on the gastric emptying. Gastric emptying was slightly decreased after 25 mg/kg (peak conc. of emepronium about 100 micrograms/l) and markedly decreased after 50 mg/kg (500 micrograms/l) and 100 mg/kg (5000 micrograms/l). In the volunteers no effect of emepronium on gastric emptying was observed, either after 200 mg q.i.d. or after 400 mg q.i.d. (about 3 and 6 mg/kg q.i.d.), which resulted in peak serum concentrations of 100-300 micrograms/l).

Adult↗

PubMed1977

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↗

PubMed1991

[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↗

PubMed1982

The lack of effect of intramuscular emepronium bromide for urinary incontinence.

Six elderly volunteers (4 men and 2 women), suffering from urinary incontinence due to small capacity, hyper-reflexic bladders, were assessed cystometrically 1/2 h, 1 h and 4 h after an intramuscular injection of emepronium bromide (Cetiprin). The dose given was sufficient to raise serum levels of emepronium to approximately 10 times those that could be reached with an oral dose. Analysis of the results showed that there was no significant difference in the state of the bladder at any time. The study confirms that emepronium bromide is ineffective in increasing bladder capacity in subjects with small, hyper-reflexic bladders. It has no value, therefore, in the management of urinary incontinence in elderly patients with this condition.

Aged↗

PubMed1976

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↗

PubMed1987

The effect of parenteral emepronium bromide (Cetiprin) on postoperative vesical tenesms after transurethral resection of the prostate. A randomized, placebo-controlled study.

Sixty patients were randomized to treatment with either emepronium bromide (Cetiprin) 25 mg t.i.d. or placebo, both medications administered intramuscularly, after transurethral resection of the prostate. Postoperatively, the number of episodes with vesical tenesms and the need for adjuvant analgesic medication were registered. No significant differences in the number of episodes with vesical tenesms or the need for adjuvant analgesic medication were found between the patients treated with emepronium bromide and those treated with placebo.

Aged↗

PubMed1976

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↗

PubMed1982

Urinary incontinence in old age. A controlled clinical trial of emepronium bromide.

The effect of the anticholinergic agent, emepronium bromide (Cetiprin), was studied in a double blind crossover study of a group of elderly patients with urinary incontinence and uninhibited bladder contractions during cystometry. There was no statistically significant difference between the subjective effect of emepronium bromide and that of placebo, and no change in the cystometric parameters. The overall subjective cure or improvement rate was 79%. The effect of anticholinergic drugs in the treatment of urinary incontinence in elderly patients with uninhibited bladder contractions might to some extent be due to an improvement in the patients' understanding and acceptance of the bladder disorders.

Aged↗

PubMed1983

Emepronium bromide and flavoxate hydrochloride in the treatment of urinary incontinence associated with detrusor instability in elderly women.

A 4-week randomised, double-blind, cross-over study is described which compared the effects of a combination of emepronium bromide and flavoxate hydrochloride with placebo on incontinence and cystometrogram findings in 20 female patients aged 59 to 88 years. All patients initially had detrusor instability demonstrated on cystometrography: 14 patients completed the study; on placebo 10 still had unstable bladders and on active drugs seven were unstable. The number of wettings over a 48-h period before the study commenced and at the end each course of tablets showed no significant differences; also the patients' opinions about the effect on their incontinence indicated that the majority had the same opinion of each course. Active drugs significantly increased residual urine but did not significantly alter the values obtained for maximum cystometric capacity or effective cystometric capacity (the latter volume being maximum cystometric capacity minus the residual urine). No correlation was found, on either course of treatment, between the change to detrusor stability and the amount of improvement in incontinence. Some side effects are described. Despite evidence of a pharmacological effect on the bladder and patients' opinions tending to favour the active combination, nonetheless the main results of this small study do not suggest that the combination of emepronium bromide and flavoxate hydrochloride is an effective treatment of urinary incontinence associated with detrusor instability in elderly women.

Aged↗

PubMed1988

Terodiline, emepronium bromide or placebo for treatment of female detrusor overactivity? A randomised, double-blind, cross-over study.

In a randomised, double-blind study, 20 women with idiopathic detrusor instability and associated symptoms were treated with terodiline 25 mg bd, placebo, and emepronium bromide 200 mg tds--each drug being given for 3 weeks with placebo as wash-out period before cross-over. The results were evaluated according to drug preference, frequency charts and elimination of detrusor instability on cystometry. Serum levels of both drugs were monitored as control of tablet intake. The preference for terodiline to placebo was statistically significant: 14/3 women (P less than 0.05), and the majority of women (12/4) preferred terodiline to emepronium. Terodiline also gave a small but significant reduction in 24 h micturition frequency and eliminated detrusor instability in almost 50% of the patients (P less than 0.05). Side effects were frequent but mild in all three treatment periods. It was concluded that terodiline offers an alternative in the treatment of female detrusor instability.

Adult↗

PubMed1987

Species differences in the intestinal excretion of emepronium.

A substantial proportion of a parenteral dose of emepronium given to dogs is excreted via the gastrointestinal tract by biliary excretion and by excretion through the intestinal mucosa (Hallén et al. 1979). In the present paper the different routes of elimination were further investigated in mouse and man and compared to the dog. The disposition of emepronium-derived radioactivity (14C) in the three species showed that about 45% was excreted via urine and 55% via faeces. The proportion of the faecal excretion of 14C that could be referred to the intestinal route differed between the species and was about 20% in man, 60% in the mouse and most pronounced, 80%, in the dog.

Aged↗

PubMed1982

Oesophageal stricture associated with emepronium bromide therapy.

Emepronium bromide, a drug used to control urinary frequency, has been reported as causing oesophageal ulceration but not stricture formation. This paper presents 3 cases in which the use of emepronium bromide preceded development of an oesophageal stricture and suggests that the drug played a causative role.

Aged↗

PubMed1984

Effect of emepronium bromide (Cetiprin) on symptoms and urinary bladder function after transurethral resection of the prostate. A double-blind randomized trial.

75 patients were randomized to be treated with either emepronium bromide (Cetiprin) 200 mg 4 times a day or placebo after transurethral resection of the prostate. The patients were evaluated urodynamically pre- and postoperatively, and further evaluated by micturition symptom charts. No significant differences in symptoms or objective findings were found between the patients treated with emepronium bromide and those treated with placebo.

Aged↗