Hyoscine N-butyl Bromide Research Articles

Effects of timepidium bromide, hyoscine-N-butylbromide and atropine on the isolated guinea pig gallbladder and sphincter of Oddi.

Effects of timepidium bromide (TB), hyoscine-N-butylbromide (HB) and atropine (Atr) were studied on the isolated guinea pig gallbladder and sphincter of Oddi. In the isolated gallbladder, the contraction induced by methacholine was competitively antagonized with TB, HB and Atr: pA2 values for TB, HB and Atr were 8.44, 7.55 and 9.11, respectively. Contraction of gallbladder after field stimulation at 5 Hz was also inhibited by TB, HB and Atr as well as by tetrodotoxin (TTX). On the other hand, TB had no significant influence on the electrically evoked (30 Hz) contraction which remained after treatment with TTX. It was estimated that the inhibitory activity of TB on the contraction of gallbladder was 1/5-1/6 that of Atr and 7 times as potent as HB. In the isolated sphincter of Oddi, TB, HB and Atr reduced the perfusion pressure increased by acetylcholine (ACh), the activity of TB being 1/4 that of Atr and 3 times of HB. The contractile responses to field stimulation (5 Hz) were also inhibited by TB, HB and Atr. The inhibitory activity of TB was 1/5 that of Atr and 12 times of HB. It was also demonstrated that TB produced no significant effect on the noradrenaline (Nor)-induced contraction and isoproterenol (Iso)-induced relaxation in the gallbladder or Nor-induced increase of the perfusion pressure in the sphincter of Oddi. It is suggested that TB acts on the gallbladder and sphincter of Oddi by virtue of its anticholinergic activity.

Effects of Timepidium Bromide, Hyoscine-N-Butylbromide and Atropine on the Isolated Guinea Pig Gallbladder and Sphincter of Oddi

Effects of timepidium bromide (TB), hyoscine-N-butylbromide (HB) and atropine (Atr) were studied on the isolated guinea pig gallbladder and sphincter of Oddi. In the isolated gallbladder, the contraction induced by methacholine was competitively antagonized with TB, HB and Atr: pA2 values for TB, HB and Atr were 8.44, 7.55 and 9.11, respectively. Contraction of gallbladder after field stimulation at 5 Hz was also inhibited by TB, HB and Atr as well as by tetrodotoxin (TTX). On the other hand, TB had no significant influence on the electrically evoked (30 Hz) contraction which remained after treatment with TTX. It was estimated that the inhibitory activity of TB on the contraction of gallbladder was 1/5-1/6 that of Atr and 7 times as potent as HB. In the isolated sphincter of Oddi, TB, HB and Atr reduced the perfusion pressure increased by acetylcholine (ACh), the activity of TB being 1/4 that of Atr and 3 times of HB. The contractile responses to field stimulation (5 Hz) were also inhibited by TB, HB and Atr. The inhibitory activity of TB was 1/5 that of Atr and 12 times of HB. It was also demonstrated that TB produced no significant effect on the noradrenaline (Nor)-induced contraction and isoproterenol (Iso)-induced relaxation in the gallbladder or Nor-induced increase of the perfusion pressure in the sphincter of Oddi. It is suggested that TB acts on the gallbladder and sphincter of Oddi by virtue of its anticholinergic activity.

A Double-Blind Comparative Study of the Inhibitory Effect of Intraduodenally Administered Hyoscine-N-Butylbromide on Human Duodenal Motility

In a double-blind crossover study hyoscine-N-butylbromide (HBB) was compared with placebo in its inhibitory effect on duodenal motility stimulated by metoclopramide. Measurements were made both by the balloon technique and the open-tipped tube method with pressure transducer. 20 mg or 50 mg HBB or placebo were instilled in random sequence into the intestinal tract of 12 healthy volunteers. The frequency of Type II waves was determined in each experiment after administration of the test substance following prior metoclopramide stimulation. This frequency was used as the inhibitory index for each drug. The test substance was administered 15 minutes before a second stimulation. A four-way analysis of variance (mixed model) was applied to the calculated number of waves per period. Subjects were required to respond equally to stimulation with increased motility on both trial days as evidenced by a minimal difference in the averages following the first stimulation on each trial day and before application of the test substance. The frequency of Type II waves after 20 mg and 50 mg HBB was reduced in a statistically significant manner in each case when compared with placebo. The probabilities of error were p less than 0-05 and p less than 0-025.

Detection and grading of oesophageal varices by fibre-optic endoscopy and barium swallow with and without Buscopan

Detection of oesophageal varices is important in the diagnosis of portal hypertension. We have, therefore, compared the results of fibre-optic endoscopy and barium swallow in 56 patients with chronic liver disease. Oesophageal varices were graded as small, moderate or gross by independent observers for each technique. In 12 patients varices were not detected by either method, and in six cases varices were detected by endoscopy when the barium swallow was negative. In 15 of the remaining 38 patients varices were found to be one grade larger at endoscopy than on barium swallow. Since it is possible that varices appear larger at endoscopy because of the Buscopan (hyoscine N-butyl bromide) used as a relaxant, we carried out barium examinations after Buscopan 20 mg i.v. in 23 of the patients. In eight cases varices were one grade larger after Buscopan than on the standard barium swallow, and in two were only detected after Buscopan had been given. Eight cases negative after Buscopan were also negative at endoscopy. Although emergency endoscopy has particular value in locating the site of bleeding in patients with portal hypertension and acute gastrointestinal haemorrhage, the results of the present study suggest that a barium meal with Buscopan is as accurate as endoscopy in the detection of oesophageal varices.

Effect of a New Anticholinergic Agent (SA-504) on Motility of the Gastrointestinal Tract and the Urinary Bladder in Cats

Effects of 1, l-dimethyl-5-methoxy-3-(dithien-2-ylmethylene) piperidinium bromide (SA-504) on the motility of gastrointestinal tract and of the urinary bladder were examined in cats. The inhibitory activity of SA-504 on the spontaneous motility of the stomach brought about by i.v. injection was nearly equal to that of hyoscine-N-butylbromide (HB), but approx. one-fourth of atropine sulfate (Atr). Intragastric administration of either SA-504 or HB produced obvious inhibition on the spontaneous motility of the stomach, while their potencies were less than one-tenth of Atr. The spasmolytic activity of SA-504 on the stomach contraction induced by vagal stimulation was almost equal to that of HB and approx. one-fourth that of Atr. In contrast to the effect on spontaneous motility of the stomach, all these compounds exhibited a somewhat weaker inhibitory action on the contraction of the stomach induced by stimulation. Both SA-504 and HB exhibited more potent inhibition on spontaneous movements of the jejunum and the sphincter of Oddi than on the stomach. On the contrary, the inhibitory potencies of Atr on the jejunum and the sphincter of Oddi did not differ much from those observed in the stomach. The inhibitory effects of these compounds on the contraction of the colon induced by pelvic nerve stimulation was similar to that in the case of stomach contraction induced by vagal stimulation. Inhibition of SA-504 on the spontaneous motility of the urinary bladder was weak and hardly any effect was observed even at a dose inhibiting the gastric motility. HB inhibited the motility of the urinary bladder under the influence of the same dose as that reduced the gastric motility. On the other hand, a significant effect was observed with Atr, the activity of which was as strong as on the motility of the stomach. Blockade by these compounds of the contraction of the urinary bladder induced by pelvic nerve stimulation required much higher doses than those required for reduction of spontaneous movements of the bladder. Among the compounds tested, the activity of Atr on the contraction of the urinary bladder was the weakest.

Genetic influences in drug responses of the eye and the heart.

1. Pupillary responses to locally applied phenylephrine and cardiac responses to intravenous hyoscine N-butylbromide have been studied in ten pairs each of healthy monovular and binovular twins aged between 24 and 60 years. 2. Under identical lighting conditions resting pupil diameters differed widely among individuals, being greater in female subjects and in those with larger irides and smaller with increasing age. 3. Monovular twins, but not binovular twins, showed significant concordance in iris diameter, initial pupil diameter, initial heart rate and responses to both drugs. The results suggest that these responses were dependent on the concordance of peripheral sympathetic and parasympathetic tone within each twin pair. 4. It is concluded that much of the variability in response to drugs acting on the autonomic nervous system is determined by physiological factors and that these are genetically influenced.