SEARCH · PubMed Health

Results for “Propantheline”

Explore indexed PubMed citations for clinical trials, systematic reviews and public health research. Read source abstracts and follow each citation to its original PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 19 recordsLinked to original sources

PubMed1977

The measurements of propantheline ion in biological fluids after administering propantheline bromide to man.

The measurement of propantheline ion has been accomplished in urine and plasma following administration of propantheline bromide to man. Trideuteropropantheline bromide is added to the biological fluid to act as a carrier and internal standard to quantify the propantheline ion using multiple ion monitoring. Methane was used as reactant gas but following the discovery of exchange of the trideuteromethyl group when using methane, ammonia was used for later analyses. The determination of propantheline ion in urine and plasma after administration of propantheline bromide to man is described.

Deuterium↗

PubMed1975

Effects of intravenous and oral propantheline and metoclopramide on ethanol absorption.

The separate effects of propantheline, atropine, and metoclopramide on ethanol absorption have been studied in man. Intravenous propantheline lowered blood ethanol levels after ingestion of a standard ethanol load. Oral propantheline, at dose levels currently recommended for therapeutic use, was without significant effect on ethanol tolerance, whereas the tolerance was reduced by oral atropine. Propantheline bromide tablets have been shown to undergo significant hydrolysis at alkaline pH in vitro. Metoclopramide, given intravenously and orally, significant elevated blood ethanol levels soon after ingestion of a standard ethanol load. It is suggested that when propantheline is selected as an anticholinergic for clinical use, there is need for greater awareness of the marked reduction in bioavailablity that results when the drug is administered at conventional therapeutic dosage by the oral as opposed to the intravenous route.

Administration, Oral↗

PubMed1978

Identification of some urinary metabolites of propantheline bromide in man.

The peak plasma concn. of total radioactivity occurred 6 h after a single oral dose of [carboxyl-14C; methyl-2H3] propantheline bromide was administered to a healthy man. At this time 10% of the dose was present in the total plasma volume. 2. A total of 71% dose of radioactivity was excreted in urine in 96 h after dosage, 59% dose being excreted in the first 24 h. About 5.3% of the orally administered propantheline bromide was excreted unchanged. 3. T.l.c. analysis and g.l.c.-mass spectrometry showed xanthanoic acid, hydroxyxanthanoic acid(s), and propantheline as urinary metabolites of the drug. 4. A glucuronide of xanthanoic acid, a hydroxylated propantheline and the (2-hydroxyethyl)diisopropylammonium ion were tentatively identified as urinary metabolites. Hydrolysis of propantheline and conjugation of the resulting xanthanoic acid appear to be the major routes of metabolism of this compound. 5. A mean elimination half-life of 9.2 h was obtained for the total radioactivity by pharmacokinetic analysis of plasma and urine levels of 14C.

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↗

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↗

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↗

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↗

PubMed1975

Propantheline bromide in massive upper gastrointestinal haemorrhage.

The effectiveness of the anticholinergic, propantheline bromide, administered parenterally in patients with upper gastro-intestinal bleeding has been investigated in a double-blind study. The basic material consisted of 99 patients. No differences were found between the group receiving propantheline bromide and the group receiving placebo in regard to clinical factors such as duration of intensive care, total hospital stay and surgical frequency. However, 21 patients under 50 years of age showed a significantly lower blood transfusion requirement with the use of propantheline bromide.

Adult↗

PubMed1975

Biopharmaceutic influences on the anticholinergic effects of propantheline.

With reduction of salivary flow rates as an index of anticholinergic response, 3 subjects manifested demonstrable effects shortly after ingestion of 15-mg doses of propantheline in conventional tablets. Ingestion of this dose i-mediately after a standardized breakfast substantially reduced the anticholinergic effects. In 1 subject, a dose-response relationship was noted after 15 mg and 30 mg doses under both fasting and fed conditions, but at each dose level the influence of food was clear. Administration of a 30-mg dose of propantheline in a commercially available "prolonged-acting" tablet induced little if any anticholinergic effects; in 2 subjects, marginal but fleeting indications of salivary suppression were noted about 4 hr after ingestion, while no effects were observed in the third subject (even after 2 "prolonged-acting" tablets).

Adult↗

PubMed1977

Bladder muscle contractility. Comparative effects and mechanisms of action of atropine, propantheline, flavoxate, and imipramine.

The anticholinergic and antispasmodic activity of atropine, propantheline, imipramine, and flavoxate were judged by each drug's ability to inhibit bethanechol chloride and barium chloride-induced canine detrusor contractions. In this in vitro model, atropine and propantheline are pure anticholinergic agents. Imipramine significantly decreases both bethanechol and barium-induced contractions, while flavoxate only minimally inhibits the response to either stimulant.

Animals↗

PubMed1979

A comparison between propantheline and imipramine on bladder and salivary gland function.

The effects of propantheline and imipramine on detrusor function and salivary gland secretion were studied in the dog. Both drugs caused a decrease in the rise of intravesical pressure following pelvic nerve stimulation in the anaesthetised dog. Propantheline had a profound effect on the salivary gland, whereas imipramine had very little effect on the volume of saliva produced after electrical stimulation of the chorda tympani. This suggests that the action of imipramine on the bladder is not anticholinergic. The significance for treatment of detrusor dysfunction is discussed.

Animals↗

PubMed1977

Double-blind evaluation of glucagon and propantheline bromide (pro-banthine) for hypotonic duodenography.

The hypotonic effect of glucagon (2 mg) and propantheline bromide (Pro-Banthine, 30 mg) on the upper gastrointestinal tract was compared in a double-blind study in 12 healthy volunteers and 36 patients. The solvent solution for the two drugs was used as a placebo. Both drugs and placebo were administered intramuscularly. The time of onset of the hypotonic effect was similar for both drugs, with maximum effect achieved 10 min after injection. Effects of glucagon dissapeared rapidly after 30 min, while Pro-Banthine still retained 50% of its maximum effect 2 1/2 hr after injection. Side effects of Pro-banthine were related to the long duration of the hypotonic effect (4-6 hr). A significant placebo effect on the duodenal C loop was observed. Glucagon appears to be the drug of choice since its hypotonic and hypomotile effects on the gastrointestinal tract are comparable to propantheline bromide while having the advantage of shorter duration and practically no side effects.

Adult↗

PubMed1977

Influence of food on the effect of propantheline and L-hyoscyamine on salivation.

The absorption of a quartenary (propantheline, 30 mg) and a tetiary (1-hyoscyamine, 0.8 mg) anticholinergic compound was studied in 8 healthy volunteers by measuring the effects on salivation. Both compounds were administered as rapidly disintegrating tablets, 1-hyoscyamine also in a slow-release formulation (Egazil Durules). The three preparations and placebo were administered under fasting conditions and with a standardized light meal using a randomized cross-over design. Salivation measurement were performed with a citric acid stimulation method every hour for 10 hours. In the fasting patient, all three anticholinergic test preparations decreased the salivation significantly. When taken with food, the effect of propantheline was almost abolished, while the effects of the 1-hyoscyamine preparations were uninfluenced. It was concluded that the clinical effects of proprantheline might be extremely varying depending how the drug is taken in relation to meals. In contrast the clinical effects of 1-hyoscyamine seem to be independent of food intake.

Adolescent↗

PubMed1978

Gastric antisecretory effects of propantheline bromide and metiamide in rhesus monkeys.

The effects of propantheline bromide (PB) and metiamide (M), two dissimilar classes of gastric secretory inhibitors, were studied in chronic gastric fistula rhesus monkeys. Basal and stimulated gastric secretory studies were conducted in conscious monkeys. Multiple s.c. injections of either histamine or pentagastrin were given hourly for four consecutive hours. One hour after the injection of the stimulants a constant plateau of gastric secretion was reached, and the test compounds were then administered as a single i.v. bolus dose. Propantheline bromide at doses of 0.03--0.3 mg/kg inhibited basal and pentagastrin stimulated gastric secretion, but had no effect on histamine stimulation. Total acid output paralleled inhibition of volume of secretion, while there was little or no effect on acid concentration. Metiamide at the doses of 1--10 mg/kg inhibited basal, pentagastrin and histamine stimulated gastric secretion. Metiamide was equally effective in inhibiting the volume of secretion and acid concentration. The scope of the gastric secretory inhibition in the rhesus monkey achieved with these pharmacological agents is very similar to man. These results suggest that the rhesus monkey is an important animal model for predicting clinically useful gastric secretory inhibitors.

Animals↗

PubMed1976

The use of intramuscular propantheline in the short bowel syndrome.

A patient is presented with the short bowel syndrome who because of massive diarrhea was unable to maintain fluid and electrolyte balance with the aid of the usual antidiarrhea drugs. Her bowel remnant consisted of approximately 155 cm of proximal jejunum. Intramuscular propantheline has allowed this patient to function normally for the past 36 months. Balance studies are presented to document the benefit of this drug. Propantheline's effectiveness is probably secondary to its marked slowing of intestinal motility.

Adult↗

PubMed1977

Propantheline as a diagnostic tool--a serious complication.

Propantheline bromide is a synthetic quaternary ammonium compound widely used in urologic patients to block the action of acetylcholine at the postganglionic nerve endings of the bladder's parasympathetic innervation. It is used clinically in a wide range of doses in ambulatory outpatients as well as hospitalized patients. To document its effects on the bladder, test doses are given with a cystometrogram documenting the dynamic changes. Herein we report a case of serious cardiac toxicity from a diagnostic test dose.

Aged↗