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PubMed1996

Urinary urge incontinence: randomised crossover trials of penthienate versus placebo and propantheline.

OBJECTIVE: To compare the efficacy of penthienate with that of propantheline and placebo for treatment of primary idiopathic detrusor instability. DESIGN: Two prospective, randomised, crossover trials (double-blind for penthienate versus placebo and non-blinded for penthienate versus propantheline). SETTING: Urology Clinic of Prince Henry Hospital, Sydney, NSW (an outpatient clinic of a tertiary referral hospital), in 1993-1994. PARTICIPANTS: Neurologically intact patients with urodynamically proven detrusor instability, urgency and urge incontinence, but no stress incontinence (20 participated in the penthienate/placebo trial and 23 in the penthienate/propanthelin trial). OUTCOME MEASURES: Cystometrography results before and after treatment; frequency and volumes of urine voided in weeks 1 and 4 of treatment; and patient scores for degree of continence, side effects, efficacy and acceptability of treatment. INTERVENTIONS: Penthienate (5 mg), propantheline (15 mg) or placebo (all three times a day) for 4 weeks. RESULTS: Penthienate produced significantly greater improvements than placebo in frequency (daytime, P = 0.002; and night-time, P = 0.02), incontinence scores (P = 0.002) and amplitude of unstable detrusor contractions, when present (P = 0.01), and significantly increased diurnal and nocturnal bladder capacity, both on cystometrography (P = 0.003) and by voiding-diary records (P < 0.001). It also increased residual urine volume over the baseline level, but not significantly. Side effects, especially dry mouth, were common with penthienate, and one patient developed urinary retention. Penthienate was significantly better than propantheline in improving cystometric capacity (P = 0.03), and reducing the amplitude of unstable detrusor contractions (P = 0.01), and was perceived as more effective by patients for frequency, nocturia and incontinence. CONCLUSIONS: Penthienate (5 mg three times a day) was objectively and subjectively significantly better than both placebo and propantheline (15 mg three times a day) for treatment of primary idiopathic detrusor instability.

Adult↗
PubMed1993

Propantheline prevention of mucositis from etoposide.

Mucosal toxicity is dose limiting for etoposide. This may be related to the direct effects of etoposide on the mucosa. Twelve patients receiving etoposide 1800 mg/m2 as part of a myeloablative pre-transplant regimen were randomized to receive propantheline 30 mg or placebo orally every 6 h for six doses. Mucositis was less frequent (2 of 6 vs 5 of 6) and less severe (p = 0.05) in the propantheline arm. There were no differences in tumor response or survival between the two groups. Propantheline is an anticholinergic that causes xerostomia by decreasing salivation. Propantheline may reduce the salivary excretion of etoposide and could reduce its toxic effects on the mucosa. Propantheline is effective in reducing the incidence and severity of mucositis in patients receiving high-dose etoposide.

Adult↗
PubMed1977

Biopharmaceutic factors that influence effects of anticholinergic drugs: comparison of propantheline, hexocyclium, and isopropamide.

The antisecretory (determined from salivary flow rates) and antimotility (determined from riboflavin absorption) effects of usually recommended doses of propantheline, hexocyclium, and isopropamide were compared in four adult volunteers. Both propantheline and hexocyclium significantly decreased salivary flow and increased riboflavin absorption. Although the usual dose of propantheline was about twice as effective as the usual dose of hexocyclium in suppressing salivary flow, these doses produced comparable effects on riboflavin absorption. Isopropamide had little or no effect on either the salivary flow rate or riboflavin absorption. Propantheline and hexocyclium elicited little effect on salivary flow when administered after a meal. Prolonged-release dosage forms of these drugs produced effects comparable to those produced by much smaller doses in conventional tablets and gave no indication of providing prolonged anticholinergic effects.

Adult↗
PubMed1980

Plasma levels and urinary excretion of orally administered propantheline bromide in man.

After a single oral dose of 30 or 60 mg of propantheline bromide peak plasma levels of the drug were reached within 2 h in six healthy men. Mean peak plasma concentrations were 20.6 and 53.1 ng/ml after 30 mg and 60 mg respectively. The mean apparent absorption and elimination half-lives after 30 mg dose were 0.22 and 1.57 h respectively, and similar half-lives were found at the higher dose level. There was a dose related change in plasma levels and AUCinfinity of the drug, and some 3% to 4% of the administered dose of propantheline bromide was excreted unchanged in urine at each dose level. Comparison of the plasma levels and urinary excretion of the drug with those seen after i.v. administration in an earlier study indicated an apparently low systemic availability of orally administered propantheline bromide. There was tentative evidence of a qualitative relationship between the oral dose administered, plasma concentrations and the effects of propantheline bromide on salivary excretion.

Administration, Oral↗
PubMed1998

Absorption behavior of orally administered drugs in rats treated with propantheline.

The effect of gastrointestinal (GI) transit rate on the absorption behavior of orally administered drugs was investigated using rats pretreated with propantheline. The propantheline-treatment reduced the transit rate in all segments to approximately 50%. The absorption behavior was examined for three model drugs with different absorption characteristics: theophylline as a highly absorbable drug without the first-pass elimination, ampicillin as a poorly absorbable one, and cephalexin as a highly absorbable one via carrier-mediated transport system. In the GI transit-retarded state, the Tmax of the plasma concentration-time curve was delayed in all the three drugs. However, the extent of bioavailability was not changed in theophylline and cephalexin. On the other hand, the extent of bioavailability of ampicillin was increased in rats pretreated with propantheline. This might be caused by the increased residence time in the absorption site, i.e., small intestine. These results were generally predicted by use of the convolution method based on the GI-Transit-Absorption Model, which was developed in our previous study, using the GI transit rate parameters in rats pretreated with propantheline. The analysis using this model could clarify that the substantial absorption site of cephalexin moved to the upper region of the small intestine by the reduction of the GI transit rate.

Ampicillin↗
PubMed1977

Effect of low-dose propantheline on food-stimulated gastric acid secretion: comparison with an "optimal effective dose" and interaction with cimetidine.

We evaluated the widely held notion that anticholinergic drugs must be used in near toxic doses to inhibit gastric acid secretion effectively. Nine patients with duodenal ulcer were studied after a low dose (15 mg) and after a near toxic dose (averaging 48 mg) of the anticholinergic, propantheline. Mean (+/- S.E.) inhibition of food-stimulated acid secretion was identical with the two doses of propantheline: 29 +/- 10 and 29 +/- 11 per cent, respectively. In addition, when 15 mg of propantheline was combined with the histamine H2-receptor antagonist, cimetidine, acid secretion was suppressed to a greater degree than with either drug alone. A low dose of propantheline is as effective as a near toxic dose in suppressing food-stimulated acid secretion and augments the inhibitory effect of cimetidine.

Adult↗
PubMed1983

Treatment of gastroduodenal ulcers with cimetidine in combination with low-dose propantheline.

Fifty-eight adult outpatients with endoscopically verified gastric, prepyloric or duodenal ulcers completed a double-blind trial of treatment with either cimetidine, 1 g daily, plus propantheline, 45 mg daily (group A) or cimetidine, 1 g daily, plus placebo (group B). After neither three nor six weeks of treatment was there any significant difference between the two groups with regard to ulcer healing or symptomatic relief. The ulcers of 22 (79%) of the 28 patients in group A and 25 (83%) of the 30 patients in group B were healed after six weeks, and 93% of the patients in both groups became painfree. We were thus not able to show any advantage in combining cimetidine treatment for ulcer healing with low-dose propantheline. In a small open trial the patients with healed ulcers received prophylactic treatment for 12 months with 1) cimetidine 800 mg daily, 2) cimetidine 400 mg at bedtime plus propantheline 45 mg daily or 3) propantheline 90 mg daily. No significant differences were found between the ulcer recurrence rates, but it cannot be excluded that a larger number of patients in each group might have yielded real differences.

Adolescent↗
PubMed1978

The influence of digoxin particle size on absorption of digoxin and the effect of propantheline and metoclopramide.

1 The influence of particle size on absorption of digoxin was studied in ten healthy volunteers who received 0.5 mg digoxin as two standard Lanoxin tablets, or tablets containing micronized digoxin or large particle size digoxin. Tablets were given 30 min after 15 mg propantheline, 10 mg metoclopramine or a placebo tablet, and following an overnight fast. 2 The overall mean cumulative 4 day urinary excretion of digoxin was significantly lower (P less than 0.01) after large particle size digoxin than after standard or micronized digoxin. Mean cumulative urinary excretion following large particle size digoxin was reduced when administered after metoclopramide and increased after propantheline, the difference between these two treatments being significant (P less than 0.05). There was a significantly lower (P less than 0.05) overall mean cumulative excretion following standard by comparison with micronized digoxin. However, by comparison with placebo, neither metoclopramide nor propantheline significantly altered mean cumulative excretion after standard or micronized digoxin. Propantheline and metoclopramide affect absorption of digoxin from formulations of large particle size and slow dissolution rate only.

Adult↗
PubMed1986

Pirenzepine and propantheline effects on esophageal pressure responses to bethanechol.

Pirenzepine is an antisecretory anticholinergic type drug that has recently been shown to be relatively free of usual anticholinergic side effects on esophageal smooth muscle. It has also been suggested that this drug might release some of the inhibitory control of the esophagus and allow increased muscle contractions. To test this hypothesis, we compared the response of the lower esophageal sphincter (LES) and esophageal peristaltic contractions to bethanechol in 12 healthy controls after background oral doses of placebo, pirenzepine (50 mg), and propantheline (30 mg). After baseline placebo, bethanechol (40 micrograms/kg subcutaneously) produced the expected significant increases in LES pressure and amplitude of peristaltic contractions. Maximal increases were 51.9 +/- 14.9 and 29.5 +/- 7.0%, respectively. Also as expected, propantheline inhibited the cholinergic stimulation from bethanechol, allowing only a 10.1 +/- 13.6% increase in LES pressure and a decrease in peristaltic contraction amplitudes (-44.1 +/- 5.0%) after bethanechol. After background pirenzepine, the responses to bethanechol were intermediate between the other two drugs. A significant increase (44.2 +/- 16.4%) in LES pressure occurred after bethanechol while no significant changes (6.9 +/- 5.8%) were noted in peristaltic amplitudes with this drug. Typical side effects of dry mouth were noted in six of the 12 subjects with propantheline and in only three subjects after pirenzepine. These studies once again confirm the absence of usual anticholinergic side effects with oral pirenzepine compared to oral propantheline in the doses studied. We could find no evidence for a release of cholinergic inhibition after pirenzepine administration.

Adult↗
PubMed1982

[Contact allergy due to the topical antiperspirant propantheline bromide (author's transl)].

After a treatment of 6 months with the antiperspirant Hydonan a contact dermatitis was found in the axillae of a 42 year-old soldier. Hydonan is a combination of 2 emphatic substances: aluminium hydrochloride and propantheline bromide. Aluminium hydrochloride is an adstringence substance, propantheline bromide is a topical active anticholinergic agent. As side-effect an irritation due to aluminium hydrochloride and a contact allergy due to propantheline bromide can occur. In our case there was a contact allergy to propantheline bromide 5% aq.

Adult↗
PubMedDate not supplied

The effect of antacid, metoclopramide, and propantheline on the bioavailability of metoprolol and atenolol.

Concomitant administration of antacid increased the maximum concentration (Cpmax) and the area under the plasma concentration-time curve (AUC) of 100 mg oral dose of metoprolol by 25 per cent (p less than 0.05) and 11 per cent (p less than 0.1) respectively. For atenolol the opposite effect was observed and Cpmax and AUC were decreased by 37 and 33 per cent respectively (p less than 0.02). In both cases the antacid did not affect the time-course of atenolol in the plasma or its bioavailability. Propantheline prolonged the absorption phase of atenolol and the time of peaking (tmax) was shifted from 2.1 to 4.5 h. Cpmax of atenolol was essentially unchanged by propantheline pretreatment while the AUC was increased by 36 per cent. It is concluded that the negative effect of the antacid on the bioavailability of atenolol is caused by a reduction in the in vivo dissolution rate due to increased gastric pH. The positive effect of propantheline might be due either to more efficient absorption of atenolol in the upper part of the intestine or more extensive dissolution of the drug as a result of prolonged contact with gastric juice or a combination of these factors.

Adult↗
PubMed1977

Prolongation of gastric emptying by oral propantheline.

The present study shows that a single oral recommended dose of propantheline bromide normally doubles the mean gastric half-emptying time in man. In a prospective, double-blind, randomized crossover design 13 normal subjects were given 30 mg propantheline or placebo 90 min before taking a 113m-indium-labeled liquid test meal, the volume of which was adjusted to body weight. The disappearance of radioisotope from the area of the stomach was determined by external gamma counting. After placebo the mean half-emptying time was 68 min and after propantheline it was 135 min (p less than 0.005). Although salivary flow decreased and pulse rate increased there were no visual disturbances. In studies already reported maximally tolerated oral doses of quaternary ammonium anticholinergic drugs have not consistently retarded gastric emptying in man.

Adult↗
PubMed1992

Pharmacokinetic interactions of cefprozil with food, propantheline, metoclopramide, and probenecid in healthy volunteers.

Cefprozil, a new oral cephalosporin antibiotic, is composed of cis and trans isomers in an approximate 90:10 ratio. The objectives of this study were: (1) to assess the effects of alterations in gastrointestinal motility by metoclopramide and propantheline on the pharmacokinetics of cis and trans isomers of cefprozil, and to compare them with the effects of food on the pharmacokinetics of cefprozil; (2) to assess the effects of inhibition of renal tubular secretion by probenecid on the pharmacokinetics of cefprozil isomers. In this four-way crossover study, 15 healthy male volunteers received a 1000-mg dose of cefprozil after fasting, pretreatment with metoclopramide or propantheline, after breakfast, or after probenecid in an incomplete, balanced block design. There was a 1-week washout period between each treatment. Blood and urine samples collected over a 24-hour period were assayed for the cis and trans isomers. The concentrations of the trans isomers were generally 1/10 of the cis isomer. The means and variances of the pharmacokinetic parameters of the cis and trans isomers of cefprozil were similar in fasting subjects and were affected in a parallel manner by food, metoclopramide, propantheline, and probenecid. The pharmacokinetics of the cis isomer under the fasting condition were as follows: maximum peak plasma concentration (Cmax), 14.0 +/- 2.7 micrograms/mL; median time to reach Cmax (tmax), 1.5 (range, 1.0-3.5) hours; half-life (t1/2), 1.24 +/- 0.27 hours; area under the concentration (AUC0-infinity), 47.3 +/- 7.7 micrograms.hour/mL; mean residence time after oral administration (MRTpo), 2.9 +/- 0.4 hours; CLR, 219 +/- 60 mL/minute; and Xu% (percent cumulative urinary excretion in 0-24 hours), 68.1 +/- 12.5.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMed1978

Enhancement of the gastrointestinal absorption of hydrochlorothiazide by propantheline.

Hydrochlorothiazide 75 mg was given twice p.o. to fasting subjects. In the second study they had been pretreated with propantheline 60 mg. Plasma and urine concentrations of hydrochlorothiazide were determined by GLC. Pretreatment with propantheline on average delayed the maximal plasma level of hct from 2.4 to 4.8 h (p less than 0.05); and the total urinary recovery of hydrochlorothiazide by 48 h was increased from 49.3 mg to 66.9 mg (p less than 0.005). It was concluded that propantheline increased substantially the absorption of the diuretic.

Adolescent↗
PubMed1982

Cimetidine or propantheline combined with antacid therapy for short-term treatment of duodenal ulcer.

Seventy-one patients with duodenal ulcer disease completed a 3- to 6-week controlled randomized trial in which cimetidine (1 g daily) was compared with an optimally effective dose of propantheline. Both groups had free access to an antacid suspension. There were no significant differences between the groups concerning ulcer healing, relief of ulcer symptoms, antacid consumption, or patient compliance. After 3 weeks of treatment, endoscopic examination revealed complete ulcer healing in 63% of the cimetidine and 47% of the propantheline treated patients. The corresponding figures after 6 weeks were 94% and 86%, respectively. After 12 weeks, ulcer recurrence was confirmed in 26% of the cimetidine- and 23% of the propantheline-treated patients. Except for the absence of anticholinergic adverse reactions, no significant advantages could be confirmed for combined cimetidine and antacid treatment.

Adult↗
PubMed1987

Subchronic toxicity of propantheline bromide administered in the feed to Fischer 344/N rats and B6C3F1 mice.

Propantheline bromide, a drug used for the treatment of peptic ulcers, was studied in male and female Fischer 344/N rats and B6C3F1 mice for subchronic toxicity. The drug was administered in the feed for 13 weeks at 0, 220, 670, 2000, 6000, and 24,000 ppm in both species. Propantheline bromide caused a decrease in weight gain at 24,000 ppm in male and female rats and at 6000 and 24,000 ppm in male and female mice. All rats survived the treatment. The top dose of 24,000 ppm was fatal to mice. Clinical signs of toxicity (dilated pupils and decreased gastrointestinal emptying), similar to the atropine-like effects of propantheline bromide in man, were seen in male and female rats at 24,000 ppm. Hyperplasia of the transitional epithelium of the urinary bladder was seen in high-dose male rats at the end of 13 weeks.

Administration, Oral↗
PubMed1989

Toxicity studies of amphetamine sulfate, ampicillin trihydrate, codeine, 8-methoxypsoralen, alpha-methyldopa, penicillin VK and propantheline bromide in rats and mice.

Thirteen-week toxicity studies in F344/N rats and B6C3F1 mice were conducted to determine general toxicity and target organ toxicity with amphetamine sulfate, ampicillin trihydrate, codeine, 8-methoxypsoralen, alpha-methyldopa sesquihydrate, penicillin VK, and propantheline bromide. This paper discusses the toxicity observed; use of the toxicity data to set dose levels for subsequent 2-year studies; and comparison of dose levels administered to rodents with doses used in the treatment of human disease. Drugs were administered orally in the feed or by gavage. The lowest doses in the 13-week studies were comparable to therapeutic doses in man on a mg/m2 (body surface area) basis or 5-10 times doses used in man on a mg/kg body weight basis. Little toxicity was seen at the low dose level with ampicillin, penicillin VK, 8-methoxypsoralen or propantheline bromide. At higher doses, target organ toxicity seen included the urinary bladder in male rats after propantheline bromide; the glandular stomach in rats and mice after penicillin VK; the liver and adrenals in rats after 8-methoxypsoralen; and the kidney in mice and rats after alpha-methyldopa. After amphetamine, codeine, or ampicillin administration, no target organ toxicity was seen in rats or mice, even at doses which caused body weight gain depression. The high doses chosen for subsequent 2-year studies were within 10 times human dose levels when compared on a mg/m2 body surface area.

Ampicillin↗
PubMed1980

Cystometric response to propantheline in detrusor hyperreflexia: therapeutic implications.

We studied 42 patients with urinary incontinence who demonstrated uninhibited detrusor contractions during cystometry. Each patient underwent urodynamic evaluation before and after the parenteral administration of propantheline bromide. Of these 42 patients 33 (79 per cent) had a positive response to propantheline: total abolition of uninhibited bladder contractions or 200 per cent increase in bladder capacity. Of these 33 patients 26 were treated with the oral drug and all but 1 had complete clinical response. Urinary retention occurred in half of the patients. These patients were managed with intermittent self-catheterization in addition to oral propantheline. None of the patients who failed to respond to the parenteral medication had a favorable response to the orally administered drug.

Administration, Oral↗