Effects of beta-adrenergic stimulation on the acutely obstructed ureter in dogs.
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The objective of the present study was to evaluate the effects of a selective beta(3)-adrenoceptor agonist, (R, R)-5-[2-[[2-(3-chlorophenyl)-2-hydroxyethyl]-amino]propyl]-1, 3-benzodioxole-2,2-dicarboxylate (CL 316243), on the acutely obstructed ureter in anesthetized dogs. After a complete ureteral obstruction produced by the inflation of a balloon catheter placed within the left lower ureter, the intraluminal ureteral pressure gradually rose to reach a plateau of approximately 52.5 mm Hg. Intravenous administration of isoproterenol (a nonselective beta-adrenoceptor agonist; 10 microg/kg) and CL 316243 (1 microg/kg) significantly decreased this elevated ureteral pressure (by 74.1 and 77.2%, respectively), with the reduction more sustained with CL 316243 than with isoproterenol. In addition, under both isoproterenol and CL 316243, urine flow (which had been interrupted by the balloon) was resumed, resulting in further sustained decreases in ureteral pressure. The mean blood pressure decreased and heart rate increased after the administration of both drugs, but these changes were greater in the isoproterenol group than in the CL 316243 group. In contrast, i.v. administration of butylscopolamine (an anticholinergic agent; 1000 microg/kg) had no evident effects on ureteral pressure or on urine flow. The increase in left kidney weight seen after ureteral obstruction was suppressed by CL 316243. We conclude that the selective beta(3)-adrenoceptor agonist tested appears to be more useful than isoproterenol for reducing ureteral pressure above the obstructed site and for promoting ureteral relaxation and increasing urine flow around the point of obstruction in dogs. (+info)
The influence of commonly prescribed synthetic drugs for peptic ulcer on the pharmacokinetic fate of glycyrrhizin from Shaoyao-Gancao-tang.
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The influence of synthetic drugs prescribed for peptic ulcer on the pharmacokinetic fate of glycyrrhizin (GL) from Shaoyao-Gancao-tang (SGT, a traditional Chinese formulation, Shakuyaku-Kanzo-to in Japanese) was investigated in rats. Co-administration of histamine H2-receptor antagonist (cimetidine) and anticholinergic drug (scopolamine butyl bromide) with SGT didn't influence the area under the plasma concentration-time curves (AUC) of glycyrrhetic acid (GA), an active metabolite derived from GL in SGT. The AUC of GA from SGT were significantly reduced by co-administration of synthetic drugs commonly used for peptic ulcer in a triple therapy (OAM), a combination of a proton pump inhibitor (omeprazole) and two antibiotics (amoxicillin and metronidazole). We found that the reduction of AUC in OAM treatment was due to the antibacterial effect of amoxicillin and metronidazole on intestinal bacteria in rat which lead to the decrease of GL-hydrolysis activity. The present study suggests that it may not be a proper way to use triple therapy containing antibiotics simultaneously with SGT for healing of chronic ulcers. (+info)
Safety and efficacy of glucagon as a premedication for upper gastrointestinal endoscopy--a comparative study with butyl scopolamine bromide.
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BACKGROUND: Glucagon inhibits digestive motility and is used for endoscopic premedication; however, its effect on cardiopulmonary function during endoscopy has not yet been fully investigated. AIM: To clarify the efficacy and safety of glucagon compared with butyl scopolamine bromide as upper gastrointestinal endoscopy premedication. METHODS: Two hundred and forty consecutive patients over 40 years of age, referred for upper gastrointestinal endoscopy, without any complications, were studied. These patients were randomly premedicated with butyl scopolamine bromide (SC group) or glucagon (G group). Time course changes in blood pressure, arterial oxygen saturation, heart rate and the number of retching episodes during endoscopy were examined. The efficacy of glucose tablets after upper gastrointestinal endoscopy to prevent hypoglycaemia caused by glucagon was evaluated. Cardiopulmonary parameters were also examined in 77 complicated patients with glucagon premedication (GC group). RESULTS: A continuous increase in heart rate during upper gastrointestinal endoscopy was observed in the SC group, but not in the G and GC groups. Blood pressure, arterial oxygen saturation and number of retching episodes were not different between the groups. Hypoglycaemia-related symptoms were frequent in the G group without glucose tablets, but were prevented by the administration of glucose. CONCLUSIONS: Glucagon has a weaker effect on cardiopulmonary function during upper gastrointestinal endoscopy than butyl scopolamine bromide. Glucose administration prevents hypoglycaemia-related symptoms caused by glucagon. (+info)
Identification of the biomechanical factors associated with the perception of distension in the human esophagus.
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Current techniques used to investigate the mechanisms responsible for the sensory responses to distension of the human esophagus provide limited information because the degree of circumferential stretch required to determine tension can only be inferred. We used impedance planimetry to measure the cross-sectional area during esophageal distension to ascertain the degree of stretch and tension that initiated motor and sensory responses. Hyoscine-N-butyl bromide (HBB), a cholinergic muscarinic receptor blocker, was also used to alter esophageal tension during distension. Motor activity was initiated at a lower degree of stretch and tension than that which initiated sensory awareness; both increased directly with increasing distension. HBB reduced both esophageal motility and tension during distension without altering the relationship between sensation intensity and cross-sectional area. Esophageal stretch, rather than tension, thus appears to be the major factor influencing sensory responses to esophageal distension. (+info)
Sensory and biomechanical responses to ramp-controlled distension of the human duodenum.
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The aim of this study was to develop a new method for investigation of the relationship among the mechanical stimulus, the biomechanical properties, and the visceral perception evoked by volume/ramp-controlled distension in the human duodenum in vivo. An impedance planimetric probe for balloon distension was placed in the third part of the duodenum in seven healthy volunteers. Distension of the duodenum was done at infusion rates of 10, 25, and 50 ml/min. The pump was reversed when level 7 was reached on a visual analog scale ranging from 0 to 10. Distensions were done with and without the administration of the antimuscarinic drug butylscopolamine. The total circumferential tension (T(total)) and the passive circumferential tension (T(passive)) were determined from the distension tests without and with the administration of butylscopolamine, respectively. T(total) and T(passive) showed an exponential behavior as a function of strain (a measure of deformation). The active circumferential tension (T(active)) was computed as T(total)-T(passive) and showed a bell-shaped behavior as a function of strain. At low distension intensities, the intensity of sensation at 10 ml/min was significantly higher than that obtained at 25 and 50 ml/min. The coefficient of variation at the pain threshold for circumferential strain (average 4.34) was closer to zero compared with those for volume (8.72), pressure (31.22), and circumferential tension (31.55). This suggests that the mechanoreceptors in the gastrointestinal wall depend primarily on circumferential strain. The stimulus-response functions provided evidence for the existence of low- and high-threshold mechanoreceptors in the human duodenum. Furthermore, the data suggest that high-threshold receptors are nonadapting. (+info)
Towards evidence based emergency medicine: best BETs from the Manchester Royal Infirmary. Buscopan (hyoscine butylbromide) in abdominal colic.
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A short cut review was carried out to establish whether buscopan (hyoscine butylbromide) is better than analgesics at controlling pain in abdominal colic. A total of 31 papers were found using the reported search, of which none presented any evidence to answer the clinical question. It is concluded that there is no evidence available to answer this question. Further research is needed. (+info)
Effect of diazepam and hyoscine butylbromide on response to secretin and cholecystokinin-pancreozymin in man.
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Ten subjects received secretin and cholecystokinin or, in duplicate tests, the two hormones together with either diazepam or diazepam plus hyoscine butylbromide in order to determine whether these drugs, which are often used during retrograde endoscopic cannulation of the pancreatic duct, affect pancreatic and biliary secretion in response to the hormones. Diazepam with hyoscine butylbromide reduced the secretion of trypsin into the duodenum and delayed the appearance of both trypsin and bilirubin in duodenal aspirate. These effects must be taken into account when interpreting pancreatic and biliary responses measured during direct cannulation of the pancreatic duct. (+info)
Assessment of the anticholinergic effect of the new antihistamine mizolastine in healthy subjects.
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1. Twelve healthy subjects were enrolled in a double-blind placebo controlled cross-over study in order to assess the possible anticholinergic effects of four doses of a new antihistamine compound, mizolastine, compared with hyoscine butylbromide (HBB) used as a reference anticholinergic drug. 2. Although mizolastine, a potent and selective H1-receptor blocker has no affinity for muscarinic receptors and does not antagonize the effects of carbachol in rodents, a study was initiated to investigate its effects on various effectors possessing muscarinic receptors (eye, heart, sweat gland, salivary gland). 3. HBB (40 mg, s.c.) impaired accommodation, decreased salivary flow and inhibited cardiac sinus arrhythmia. Pupil diameter and maximum constriction speed, carbachol-induced skin sweating and Valsalva ratio were unaffected. 4. Mizolastine (5, 10, 20, 40 mg p.o.) did not affect any parameter at any time point, demonstrating a lack of anticholinergic effect. (+info)