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At least 19 recordsLinked to original sources

A comparison of N-butylscopolammonium bromide and butorphanol tartrate for analgesia using a balloon model of abdominal pain in ponies.

The analgesic effect of N-butylscopolammonium bromide (0.3 mg/kg) using a balloon-induced model of colic in ponies was evaluated and compared with butorphanol tartrate (0.1 mg/kg). Eight adult ponies were used and each received both treatments during the two different trials. The order in which the treatment was received was randomly assigned. At the start of each trial, moderate abdominal pain was induced by inflation of a balloon placed in the lumen of the caecum. The ponies were evaluated every 5 minutes, and a cumulative pain score (CPS) was assigned. Two baseline measurements were recorded, followed by the administration of one of the two treatments. Assessments were continued for 60 minutes, or until moderate abdominal pain returned. Three ponies out of 8 responded to treatment with butorphanol tartrate, while 6 out of 8 ponies responded to N-butylscopolammonium bromide. There were no statistical differences in the CPS or duration of drug action between treatments.

Abdominal Pain↗

[Ion-selective electrodes with a liquid membrane for determining N-butylscopolammonium bromide].

Two ion-selective electrodes with liquid membrane for N-butylscopolamonium bromide are described, with N-butylscopolamonium tetraphenylborate (I) and N-butylscopolamonium reineckate (II), respectively, solved in benzylic alcohol as electroactive material. These electrodes have a linear response in the concentration range of 10(-2)-10(-6) M N-butylscopolamonium bromide, with the detection limit of 10(-7) M for both electrodes. These electrodes were used with good results for quantitative assay by direct potentiometry of injectable solutions of N-butylscopolamonium bromide.

Butylscopolammonium Bromide↗

A comparison of N-butylscopolammonium and lidocaine for control of rectal pressure in horses.

In its FDA approved formulation, N-butylscopolammonium bromide (Buscopan Injectable Solution, Boehringer Ingelheim Vetmedica) is an anticholinergic spasmolytic agent indicated for management of abdominal pain associated with spasmodic colic, flatulent colic, and simple impactions in horses. Use of this drug ablates gastrointestinal peristalsis and rectal pressure. It ahs been suggested that N-butylscopolammonium bromide could be used to facilitate rectal examinations in horses. This study compared the effects of N-butylscopolammonium bromide versus lidocaine and a saline control on rectal pressure and the number of rectal strains during rectal examination. The results of this study indicate that this drug increases the quality and, presumably, the safety of rectal examinations in horses.

Abdominal Pain↗

[Action of some drugs on pressure profile of female urethra (author's transl)].

The action of certain drugs upon the urethra of clinically intact women was studied by measurement of the urethral profile. beta-adrenoreceptor stimulating and blocking agents, such as fenoterol, propanolol, as well as cholinergics, including carbachol and pyridostigmine, failed to exercise any effect on the urethral pressure profile. On the other hand, anticholinergics, such as atropine and N-butylscopolammonium-bromide, diazepam, and chlorpromazine, produced significant decrease in both maximum urethral pressure and maximum urethral closure pressure. N-butylscopolammonium-bromide and chlorpromazine also shortened the functional length of urethra. Drop of all parameters relating to the urethral pressure profile was observed to take place in response to application of succinylcholine. Phentolamine, an alpha-adrenoreceptor blocking agent, then was administered and caused further reduction of those parameters. The pressure values were elevated by ketamine. The above findings are discussed and compared to present concepts published in literature on medicamentous control of urethral function.

Adolescent↗

Assessment of potential selectivity of antispasmodics for the various sections of the gastrointestinal tract of the rat as a guideline for their clinical use.

Two spasmolytic drugs, N-butylscopolammonium bromide and octylonium bromide have been challenged against topical carbachol-induced contracture of gastric antrum, duodenum, jejunum, ileum, caecum, colon and rectum of the rat. Experimental data indicate that N-butylscopolammonium bromide, a competitive anticholinergic agent, is more effective on the upper than on the lower sections of the rat gastrointestinal tract. On the other hand octylonium bromide, which has been reported to have little if any competitive antimuscarinic properties at effective spasmolytic doses, showed a more composite spectrum of activity. Hexamethonium, a nicotinic cholinoceptor antagonist, was about equally effective in inhibiting carbachol-induced contractions of all the GIT sections under study. Data in the literature and our own findings do not support the use of competitive antimuscarinic drugs for the treatment of colonic hypermotility. In fact, at effective spasmolytic doses they are expected to produce a greater inhibition of motility of the upper sections of the GIT than at the colonic level.

Animals↗

Effects of spasmolytics on K+-induced contraction of rat intestine in vivo.

Eight spasmolytic drugs commonly used in the treatment of the irritable bowel syndrome were compared to verapamil with respect to their effects (all drugs injected i.v.) on the contraction of duodenum, ileum and colon induced by high K+ topical application in the anaesthetized rat. Verapamil greater than rociverine greater than papaverine greater than mebeverine greater than dicyclomine antagonized dose-dependently the contraction of duodenum and colon, the activity on duodenum being from 2 (rociverine) to 10 (verapamil) fold higher. Verapamil and rociverine, but not the other drugs mentioned above, were also active on ileum. N-Butylscopolammonium bromide, phloroglucinol and trimebutine were inactive against the contraction of the three intestinal tracts and prifinium bromide was inactive on duodenum and ileum, while it had remarkable activity on colon, unrelated to its antimuscarinic activity. The results are discussed briefly with reference to the pharmacological therapy of the irritable bowel syndrome.

Animals↗

Effects of rociverine and other spasmolytic agents on caerulein-induced delay in gastric emptying in the conscious rat.

Caerulein (C)-induced delay in gastric emptying (GE), due to pylorospasm, was used as an experimental model for a quantitative test of the activity of some spasmolytic drugs in conscious rats. Rociverine at doses of 10 and 15 mg kg-1 i.p., though not at higher doses, considerably reduced this delay. Of the other drugs tested only papaverine had this effect and to a lesser degree. Atropine, N-butylscopolammonium bromide and dicyclomine proved to be inactive or further reduced GE. The effect of spasmolytics on C pylorospasm seems to be the outcome of two actions possessed by the drugs in varying degree: on the one hand a pyloric sphincter relaxant action, which increases GE, and on the other a relaxant action on the smooth musculature of the stomach, which tends to reduce GE. The model used highlights the activity of the spasmolytics that act on pylorospasm at doses which per se do not cause a marked delay in GE.

Animals↗

In vivo rat bladder: a new model to screen spasmolytic compounds.

A model for in vivo screening of spasmolytic compounds of the rat urinary bladder has been developed. It is physiological, specific, and adaptable. A filling volume of the bladder of 0.6-1 ml proved to be optimal. Agonists such as acetylcholine, KCl and BaCl2 exerted almost identical spasmogenic effects on both the in vivo and the in vitro model (isolated rat bladder strip). Moreover, the antagonistic effects of atropine, N-butylscopolammonium bromide, or flavoxate hydrochloride were directly comparable between the two models. Intravenously administered atropine was shown to be effective immediately; after intragastric application the maximum effect can not be observed until after 9 min. The in vivo rat bladder model presented is proposed to be a suitable method for advanced screening of spasmolytic compounds to include their absorption, biotransformation, and excretion.

Acetylcholine↗

Effects of some drugs on ripening of uterine cervix in nonpregnant castrated and pregnant rats.

The stimulating effect of some drugs on the ripening of the uterine cervix in rats was studied by measuring the wet weight of the uterine cervix and by both light and electron microscopy in nonpregnant castrated and pregnant conditions. Since the light and electron microscopic findings after estrogen (E) administration to castrated rats were similar to those found in the uterine cervix of rats at the end of pregnancy, it was concluded that E (E2 greater than or equal to E3 greater than or equal to E1) plays a major role in the ripening mechanism. It was also found that DHA-S, progesterone and relaxin had stimulating effects on cervical ripening. Oxytocin and PG (PGE2 greater than PGF2 alpha) showed the ripening activity only in pregnant condition. Moreover, oxytocin, PGE2 and PGF2 alpha potentiated the estrogen action. The effects on the increase in wet weight of the uterine cervix and microscopic findings due to DHA-S were different from E in castrated rats. It is therefore postulated that the effect of DHA-S might be mainly due to the secondary increase in E converted from DHA-S in the ovary and, in addition, to a direct effect of this medicament on the uterine cervix. There was essentially no difference in ultrastructure between the cervix of control (nonpregnant, castrated or pregnant) rats and that of rats treated with HCG, isoxsuprine hydrochloride, dihydroergotoxine, diazepam or n-butylscopolammonium bromide.

Animals↗

Rociverine, a new antispasmodic agent with balanced neurotropic and myotropic activity.

A systematic study in vitro and in vivo of the antispasmodic agent 2-(diethylamino)-1-methylethyl cis-1-hydroxy (bicyclohexyl)-2-carboxylate (rociverine) showed that its activity is both antimuscarinic and directly muscle-relaxant. The antimuscarinic activity is weaker than that of atropine, N-butylscopolammonium bromide and dicyclomine whilst the direct muscle-relaxant activity is equal to or greater than that of papaverine. The peculiarly balanced ratio of the neurotropic and myotropic components ensures that the antispasmodic effect is the outcome of both, without one prevailing over the other. This not only rules out major atropine-like side-effects but renders rociverine potentially effective on spasm of the different viscera, of particular interest in viscera in which there is only minor involvement of cholinergic structures. The muscle-relaxant activity of rociverine is achieved by inhibiting the availability of Ca2+ at contraction site and not through an antiphosphodiesterasic mechanism, which might explain the absence of muscle-relaxant effects on the smooth musculature of the blood vessels.

Analgesia↗

[Membrane-selective electrodes for drug analysis. Note II].

Seven membrane-selective electrodes with PVC matrix and liquid-membrane for N-butylscopolamine with different electroactive materials are presented. These electrodes have a linear response in the concentration range of 10(-6) - 10(-2) M N-butylscopolamine bromide, with a detection limit between 4.58 x 10(-7)M and 1.09 x 10(-6)M. These electrodes were used with good results for quantitative assay by direct potentiometry and potentiometric titration of N-butylscopolamine bromide from pharmaceutical formulations. Recovery was between 95.50% and 99.20% for N-butylscopolamine bromide of injectable solutions.

Algorithms↗