Article

Hyoscine Butylbromide

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Abstract

Abdominal cramping and pain is a frequent problem in the adult population of Western countries, with an estimated prevalence of ≤30%. Hyoscine butylbromide (scopolamine butylbromide) [Buscopan®/Buscapina®] is an antispas-modic drug indicated for the treatment of abdominal pain associated with cramps induced by gastrointestinal (GI) spasms. It was first registered in Germany in 1951 and marketed in 1952, and has since become available worldwide both as a prescription drug and as an over-the-counter medicine in many countries. This article reviews the pharmacology and pharmacokinetic profile of hyoscine butylbromide, and summarises efficacy and safety data from clinical trials of this drug for abdominal cramping and pain. Pharmacological studies have revealed that hyoscine butylbromide is an anticholinergic drug with high affinity for muscarinic receptors located on the smooth-muscle cells of the GI tract. Its anticholinergic action exerts a smooth-muscle relaxing/spasmolytic effect. Blockade of the muscarinic receptors in the GI tract is the basis for its use in the treatment of abdominal pain secondary to cramping. Hyoscine butylbromide also binds to nicotinic receptors, which induces a ganglion-blocking effect. Several pharmacokinetic studies in humans have consistently demonstrated the low systemic availability of hyoscine butylbromide after oral administration, with plasma concentrations of the drug generally being below the limit of quantitation. The bioavailability of hyoscine butylbromide, estimated from renal excretion, was generally

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... The absorption of HBB after oral administration is about 8% and systemic bioavailability is 1%. Therefore, systemic anticholinergic effects are not expected when it is given orally [1,2]. It is rapidly distributed into tissues when given in IV form (t 1/2 = 29 min). ...
... In our study, HBB was administered in IV form, and in accordance with the literature, the frequency of side effects was low and there was no difference between the study and placebo groups in terms of side effects. The use of HBB in cases of nonspecific abdominal colic or abdominal pain is based on the smooth-muscle relaxation and resolution of spasms/cramps due to its antimuscarinic effects on the smooth muscles of the gastrointestinal tract [1,2,6]. Studies investigating the effect of HBB on abdominal cramping or abdominal pain have generally been conducted for diseases involving chronic abdominal cramping such as IBD or for nonspecific undiagnosed abdominal pain and with the oral or rectal form of the drug. ...
... Studies investigating the effect of HBB on abdominal cramping or abdominal pain have generally been conducted for diseases involving chronic abdominal cramping such as IBD or for nonspecific undiagnosed abdominal pain and with the oral or rectal form of the drug. In those studies, the effects of the drug on symptom intensity over a long period of time were measured, not the acute effects of the drug [2,11]. In most of those studies, oral HBB alone or in combination with paracetamol was shown to reduce cramping abdominal pain. ...
... Butilbrometo de hioscina (BBH) ou butilbrometo de escopolamina, geralmente vendido sob a marca comercial Buscopan ® , é um medicamento espasmódico, anticolinérgico, registrado pela primeira vez na Alemanha em 1951 e comercializado em 1952, sendo indicado para o tratamento da dor abdominal associada à cólicas induzidas por espasmos gastrintestinais (TYTGAT, 2007). ...
... Sua ação anticolinérgica exerce efeito relaxante e espasmolítico da musculatura lisa desta região. Assim, o bloqueio dos receptores muscarínicos no trato gastrointestinal corresponde à base para seu uso no tratamento da dor abdominal secundária às cólicas (TYTGAT, 2007 (CHENG et al., 2010). ...
... Como medida de precaução, você deve evitar o uso de Buscopan® durante a gravidez e a amamentação (BUSCOPAN, 2021). Além da falta de estudos durante o período de gravidez, o BBH também pode causar efeitos colaterais em baixa incidência (≤1,5%), baixa intensidade, autolimitantes e semelhantes aos provocados por outros medicamentos anticolinérgicos, como náuseas, constipação, boca seca, visão embaçada, taquicardia e retenção urinária (TYTGAT, 2007). Estes efeitos foram avaliados em algumas pesquisas, mas os resultados não foram apresentados aqui, pois este não é o tema da atual revisão integrativa. ...
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Introdução: O butilbrometo de hioscina (BBH) ou butilbrometo de escopolamina é um medicamento anticolinérgico e espasmódico, indicado para o tratamento da dor abdominal associada à cólicas induzidas por espasmos gastrintestinais. Estudos indicam que o BBH atue realizando uma inibição colinérgica de gânglios parassimpáticos da região abdominal e pélvica, aliviando os espasmos na musculatura lisa, atuando no plexo cérvico-uterino o que pode auxiliar na dilatação cervical no momento do parto. Objetivo: Realizar uma revisão integrativa de ensaios clínicos que analisaram os efeitos do BBH durante o primeiro estágio do trabalho de parto. Material e métodos: Foi realizada uma busca avançada de artigos científicos na base de dados Medical Literature Analysis and Retrieval System On-line (MEDLINE), utilizando os descritores “Brometo de butilescopolamônio” (Butylscopolammonium bromide), “Trabalho de parto” (Labor), “Primeira fase do trabalho de parto” (First labour stage) e “Dilatação cervical” (Cervical dilatation). Os artigos foram identificados, triados, elegidos e inclusos para elaboração da revisão integrativa. Resultados: A revisão integrativa foi composta por 11 ensaios clínicos publicados em artigos científicos que apresentaram resultados de duração de tempo total e do primeiro estágio do trabalho de parto e de taxa de dilatação cervical uterina. Conclusões: As pesquisas analisadas na atual revisão integrativa sugerem que 20 mg de BBH em uma paciente com dilatação cervical de aproximadamente 3 a 5 cm no, pode reduzir a duração do primeiro estágio do trabalho de parto, por meio de um aumento na taxa de dilatação cervical uterina.
... MDPI and/or the editor(s) disclaim responsibility for any injury to people or property resulting from any ideas, methods, instructions, or products referred to in the content. Hyoscine butylbromide (HBB; also known as butylscopolamine bromide or as scopolamine butylbromide) is a well-established anti-spasmodic medicine [9] that has also shown efficacy in a mouse model of dysmenorrhea [10]. A fixed-dose combination of HBB plus paracetamol (a.k.a. ...
... PLUS is an approved medication for the treatment of dysmenorrhea in at least 10 countries. While the effects of HBB and paracetamol against cramps and pain are well documented [9], the currently available evidence in the public domain underlying its use in dysmenorrhea is limited and rests on three open-label studies [11][12][13] followed by one randomized controlled trial [14]. Therefore, we have used data from a recently reported PBPS that had included many women using PLUS for the treatment of dysmenorrhea symptoms [15] to better characterize these women and the perceived treatment benefit. ...
... Therefore, no claims on absolute efficacy and safety should be derived from PBPS because randomized, controlled trials should address those. Presently, only limited data from controlled trials support the use of PLUS in the treatment of dysmenorrhea [14] but based on mechanistic plausibility [10] and the established efficacy and safety of HBB and paracetamol [9] as components of PLUS, at least 10 countries in Europe, Asia and Latin America have approved the use of PLUS for the treatment of dysmenorrhea. On the other hand, randomized controlled trials also have limitations: They have rigid inclusion and exclusion criteria often resulting in a group of participants that does not match those using the product in real life. ...
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Dysmenorrhea symptoms are frequent and often self-treated using non-prescription medicines. To further characterize women with dysmenorrhea using a combination of hyoscine butylbromide and paracetamol (PLUS) for self-management of their complaints, we performed a secondary analysis of a published pharmacy-based patient survey. 314 women (mean age 32.3 years) with dysmenorrhea reported a pain and cramps intensity of 7.45 ± 2.13 on a 0-10 Likert scale, which was reduced to 2.86 ± 1.81 upon treatment. Associated impairments of work/daily chores, leisure activities, and sleep were improved by 64.6%, 62.2% and 70.4%, respectively. The onset of symptom relief was within 60 min in 84.7%. Tolerability was rated as very good or good by 97.2%. These findings confirm the efficacy and tolerability data on PLUS from randomized controlled trials in a larger group of women conducting self-management of their dysmenorrhea.
... While OTC products differ in molecular targets, their functional targets are similar or at least largely overlapping. For instance, both HBB and PO have spasmolytic effects and are recommended for the treatment of IBS symptoms, but the former acts as a muscarinic receptor antagonist [7], and the latter by inhibiting Ca 2+ channels [8]. The effectiveness of HBB in the treatment of GI cramps and pain can be further improved by the addition of paracetamol (also known as acetaminophen) [9], and fixed-dose combinations of HBB plus paracetamol are available (PLUS). ...
... Randomized controlled trials are considered the gold standard of evidence generation in clinical medicine. HBB [7,9,[18][19][20][21][22][23][24], PLUS [9] and PO [8,25] have proven effectiveness in controlled trials, compared with a placebo for each of them. However, based on the trial setting and on the inclusion and exclusion criteria such randomized, controlled trials are not helpful to reflect real-world conditions in OTC settings where they are inherently dispensed without the involvement of a prescribing physician [26]. ...
... Moreover, 62-73% of users reported a reduction of at least 50%. This is well in agreement with the proven effectiveness of HBB [7], PLUS [9], and PO [8,25], all established in comparison to placebo in randomized controlled trials. However, these and other studies have also reported a markable placebo effect in the treatment of FGIDs. ...
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Functional gastrointestinal disorders (FGIDs), including irritable bowel syndrome (IBS), are frequently handled by self-management with over-the-counter (OTC) products such as hyoscine butylbromide (HBB), alone or in combination with paracetamol, and natural products such as peppermint oil. To obtain real-world information, we have performed an anonymous pharmacy-based patient survey among 1686 users of HBB, HBB + paracetamol, and peppermint oil. Based on the distinct but overlapping indications for the three OTC products, multiple logistic regression was applied to compare them in users reporting gastrointestinal cramps and pain, bloating, flatulence, or IBS as cardinal symptoms. All three treatments reduced symptoms and associated impairments of work/daily chores, leisure activities, and sleep by approximately 50%. Based on the four cardinal symptoms and the four dependent continuous variables of interest (change in intensity of symptoms and of the three impairment domains) a total of 16 logistic regression models were applied. HBB, HBB + paracetamol, and peppermint oil had similar reported overall effectiveness in those models. Gender, age, baseline symptom severity, and impairment in one of three domains had small and inconsistent effects on perceived treatment success. We provide evidence that HBB, HBB + paracetamol, and peppermint oil have comparable effectiveness in their approved indications under real-world conditions in an OTC setting.
... HBB acts mainly by binding to the muscarinic receptors on smooth muscle cells in different organs and is considered to belong to the family of the anticholinergic drugs (Tytgat, 2007). Thus, spasmolytic and relaxing influences on smooth muscle cells can be achieved by HBB. ...
... Thus, spasmolytic and relaxing influences on smooth muscle cells can be achieved by HBB. HBB is used to treat abdominal pain resulting from cramping by muscarinic receptors blockage and HBB can attach to nicotinic receptors and act as a ganglionic blocker (Tytgat, 2007). ...
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This paper reports a systematic review and meta-analysis of the effectiveness of hyoscine-N-butylbromide (HBB) administration in hysterosalpingography (HSG). Four electronic databases were searched for randomised controlled trials (RCTs) that compared HBB versus placebo or no intervention in infertile women undergoing HSG. Pain during and after HSG and different adverse events including nausea, vomiting, and dizziness were evaluated. Three RCTs with 335 patients were included. The analysis showed HBB was significantly effective in reducing pain during and after HSG (MD = −0.76 mm, 95% CI [−1.35, −0.17], p = 0.01) and (MD = −0.81 mm, 95% CI [−1.07, −0.56], p < 0.001), respectively. There were no significant differences in adverse events between HBB and control groups. The methodological evidence quality was high as evaluated by GRADEpro. In conclusion, this review provides good evidence that prior administration of HBB is effective in reducing induced pain during and after HSG with tolerable side effects.
... This equates to approximately 10-210 mg/day in adults. Systemic effects of hyoscine butylbromide are anticipated when oral doses reach ≥30 mg/kg [9,12]. ...
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Simple Summary High-resolution magnetic resonance imaging (MRI) is essential for detecting subtle pathologies in the bladder, but it can be affected by movement from peristalsis of the urinary, gastrointestinal, and reproductive systems. Spasmolytics such as buscolysin and glucagon help to reduce motion artifacts, potentially leading to clearer images. The aim of our study was to analyze and compare the properties, benefits, and side effects of these substances to improve patient preparation for bladder MRI exams. Although both substances have similarities, butylscopolamine is preferred due to its lower cost, with glucagon serving as an alternative for those with medical contraindications. We also reviewed recent studies on the use of spasmolytics in MRI of pelvic organs. Our findings indicate that the inconsistent results regarding the utility of spasmolytics highlight the need for further research to determine whether their application truly enhances MRI accuracy and quality for the examination and staging process. Abstract Accurate assessment of muscular layer infiltration of the urinary bladder wall is crucial for diagnostic precision and is significantly influenced, among other factors, by the elimination of motion artifacts. This review explores the potential benefits of using spasmolytic agents to achieve improved imaging results. Specifically, it examines two commonly available pharmaceutical preparations: butylscopolamine (buscolysin) and glucagon. The review highlights the similarities and differences between these agents and discusses the optimal methods of administration to enhance urinary bladder imaging. By addressing these factors, the article aims to provide insights into improving diagnostic accuracy in clinical practice.
... Capecitabine is a prodrug that is enzymatically converted to fluorouracil (antimetabolite [5,6]) in the tumor [7], where it inhibits DNA (Deoxyribo Nucleic Acid) synthesis [8,9] and slows growth of tumor tissue. Common side effects include abdominal pain [10], vomiting, diarrhea [11,12], weakness, and rashes. Other severe side effects include blood clotting problems [13,14], allergic reactions [15], heart problems such as cardiomyopathy [16,17], and low blood cell counts. ...
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Objective: An easy, quick, precise, active and reproducible Liquid Chromatography-Tandem Mass Spectrometry (LC-MS/MS) technique was developed for the bio-analytical method of Capecitabine and Docetaxel using D9-Capecitabine and D9-Docetaxel as Internal Standards (IS). Methods: This article summarizes the recent progress on bioanalytical LC-MS/MS methods using Symmetry C18 column (150x4.6 mm, 3.5µ) and an organic mobile phase of 0.1% formic acid and Acetonitrile in 80:20 v/v. Results: Analysis was carried out within 5 min over a good linear concentration range from 37.5ng/ml to 300ng/ml (r2= 0.9999±0.008) for Capecitabine and 10ng/ml to 80ng/ml (r2=0.9993±0.005) for Docetaxel. Accuracy, precision, recovery, matrix effect and stability results were found to be within suitable limits. Conclusion: The application denotes all the parameters of system suitability, specificity, linearity and accuracy are in good agreement with United States Food and Drug Administration (USFDA) guidelines and applied effectively for the investigation of pharmacokinetic studies in rats.
... Research has confirmed that drugs such as diphenoxylate [56,57], loperamide [58], in the treatment of diarrhea, hyoscine [59][60][61], and methocarbamol for abdominal cramps, ondansetron [62], and dimenhydrinate [63], for nausea and vomiting are effective in this period to help the patient and endure the effects of addiction withdrawal. Cyproheptadine drug is effective for the treatment of anorexia [64], and in parallel, for the prevention of migraine with the origin of an empty stomach, as well as the treatment of allergic complications (Scheme 4), [65]. ...
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Heterocyclic N-amine drugs, Abuse Drugs Biochemistry, Opium Methadone Buprenorphine. Naltrexone Naloxone Clonidine Diphenoxylate Harmaline Mitragynine Gabapentin Melatonin, Lorazepam Xanax Ondansetron Phenylephrin Diphenhydramine Voltaren Losartan-Hydrochlorothiazide Captopril Tetrazole Carbamate
... With these properties, MJ is a successful elicitor used for SMP including pharmaceuticals, nutraceuticals, and industrially important compounds in numerous plants (Kim et H. niger (black henbane), a member of the Solanaceae family, is a valuable medicinal plant species with high pharmacological activities due to its high content of tropane alkaloids (TAs), particularly scopolamine and hyoscyamine. TAs are among the most commonly used compounds in the formulation of medicines due to their hypnotic, antispasmodic, sedative, and anticholinergic effects (Tytgat et al., 2007;Thawabteh et al., 2019). In addition to TAs, Hyoscyamus niger also contains different groups of secondary metabolites including lignans, coumarinolignans, avonoids, glycerides, saponins, glycosides, and phenolics (Lunga et al., 2008). ...
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This research aimed to identify the influences of 24-epibrasinolide (EBL) and methyl jasmonate (MJ) applications on growth parameters and secondary metabolite syntheses in adventitious root and cell suspension cultures of Hyoscyamine niger . Therefore, EBL at different concentrations (0.5, 1, and 2 mg L − 1 ), individually and together with 1 mM MJ were implemented in root and cell suspension cultures. In root cultures, the optimum concentration for achieving the highest root growth parameters was found to be 2 mg L − 1 of EBL. On the other hand, in cell suspension cultures, the best cell growth was observed when 1 mg L − 1 of EBL was applied. In root cultures, the highest scopolamine and hyoscyamine amounts were obtained when 1 mM MJ was applied in combination with EBL at concentrations of 1 and 2 mg L − 1 , respectively. In cell cultures, 2 mg L − 1 EBL for scopolamine and 0.5 mg L − 1 EBL for hyoscyamine were found to be the best among all applications. Compared to the control, elicitor applications also stimulated phenolic production in both roots and cells, depending on their combinations and concentrations. Additionally, it was also found that the metabolite production performance of adventitious roots was higher than that of cells. In conclusion, it was suggested that the use of MJ and EBL could be a promising strategy for enhancing the accumulation of scopolamine, hyoscyamine, and phenolic substances in root and cell cultures of H. niger .
... The principal source of tropane alkaloids, particularly hyoscyamine and scopolamine, which are frequently used in folk medicine, is the hyoscyamus species. These substances act as an antispasmodic, a nervous system stimulant, and a treatment for stomach pain (Tytgat and Guido, 2007). Egypt. ...
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The development of biochemical from plant cells marks the beginning of a new phase in biotechnological research and increasing global demand for scopolamine. From this point, somatic calli of Egyptian henbane (Hyoscyamus muticus L.) were produced from leaf segments cultured on Murashige and Skoog (MS) medium containing various concentrations of Kin (0.5, 1, and 2 mg/l) or 2,4-D (1 and 2 mg/l). Immobilisation callus was conducted using various alginate treatments at 1.0, 1.5 and 2.0% combined with glycerol at 2, 3 and 4%. To complete gleization, two sources of calcium ions (CaCl 2 and Ca (NO 3) 2 .4H 2 O) were used at three concentrations 10, 20 and 30% or 1.5, 3 and 5%, respectively. The encapsulated somatic cell aggregates were cultured in liquid MS medium with 100, 200 and 300 mg/l of each tryptophan, glutamine and jasmine oil at 0.1, 0.2 and 0.3 % (v/v). The dried and fresh weights of immobilised cells were obtained after every two weeks of incubation for one month. The highest callus production (100%) was obtained on a medium containing 0.5 mg/l of Kin. While the medium containing 0.5 mg/l Kin plus 1 mg/l 2,4-D produced the highest percentage of somatic embryos (91.67%) with 147 embryos/g, this count produced a regeneration percentage of 39.27% (equivalent to 57.67 embryos/g). HPLC analysis revealed that the highest values of scopolamine and hyoscyamine (the major alkaloids) were obtained from applied tryptophan. When cells were treated with 100 mg/l of tryptophan, the medium contained 0.008 mg/ml of scopolamine and 0.09 mg/ml of hyoscyamine, respectively.
... 36 Other pharmacological studies have shown that this substance has a high dependence on muscarinic receptors in smooth muscle cells including in the digestive system and its anticholinergic activity has a muscle relaxant and spasmolytic effect. 37 The mechanism of action of hyoscine is competitive antagonism with acetylcholine in muscarinic receptors. 38 The parasympathetic branch in the uterus regulates contractile activity, increases angiogenesis and stimulates secretions from cervical glands, 39 therefore, hyoscine can reduce these activities. ...
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Although xylazine is widely used in domestic animals as a sedative, analgesic, and muscle relaxant, its side effects on the uterus prevent its utilization in pregnant animals or in embryo transfer. Although the effects of xylazine on increasing uterine contractions have been confirmed, no reliable report of fetal death due to xylazine administration has been published. Hyoscine is an anticholinergic medication that has antimuscarinic and antispasmodic effects in the uterine tissue of pregnant cattle during in vitro studies, therefore, we investigated if administration of xylazine in the last third of pregnancy could increase fetal death and if hyoscine could prevent its adverse effects. Twenty adult female rats, after mating with four adult male rats and confirming pregnancy, were randomly divided into two equal control and treatment groups. On the 18th day of pregnancy, the number of fetuses per rat was determined using ultrasonography. Rats in the treatment group received hyoscine (1 mg/kg, intraperitoneally) for 3 days. Subsequently, all rats were administered xylazine (10 mg/kg, intraperitoneally) for 3 days. On the 21st day of pregnancy, the number of living and dead fetuses was counted after laparotomy. Also, the weight and dimensions of the fetuses were measured. The results showed that although more fetuses lost their lives in the treatment group compared to the control group, the statistical difference in the percentage of fetal mortality in the two groups was not significant (p  0.05). In addition, the comparison of the mean weight, body length, and body width of living and dead fetuses in both groups showed that there was no statistically significant difference between these groups (p  0.05). It could be concluded that maternal xylazine intake in rats could cause about 18-25% of fetal mortality. However, the use of hyoscine to prevent fetal death induced by xylazine is not recommended.
... Hyoscine butylbromide binds to nicotinic receptors, which induces a ganglion-blocking effect. 18 However, there are many contraindications and adverse effects with using hyoscine butylbromide such as in patients with underlying cardiac disease. Furthermore, there has been no consensus on using IV hyoscine butylbromide for rectal cancer imaging. ...
Article
Backgrounds: Magnetic resonance imaging is the primary method for local staging in rectal cancer patients. Administration of intravenous (IV) hyoscine butylbromide is thought to improve accuracy, but there are contraindications and potential adverse effects. The aim was to assess the efficacy of IV hyoscine butylbromide on the accuracy of MRI rectal cancer staging of T2 and T3 rectal cancers. Methods: A retrospective cohort study was carried out on patients prospectively recorded on the Cabrini Monash colorectal neoplasia database. A total of 74 patients (53 males, 21 females) MRI pelvis and rectums with antispasmodics were performed at multiple centres in the pre-operative setting between 2010 and 2016. Each patient underwent total mesorectal excision of rectal cancer. The excision specimens were assessed and given a pathological TNM stage, which was considered the reference standard. Results: There was no statistically significant impact on the overall accuracy of MRI rectal cancer staging between patient groups who received IV hyoscine butylbromide and groups who did not receive IV hyoscine butylbromide. The accuracy of T2 and T3 staged rectal cancers was more likely to be correct (compared with T1 cancers) with the administration of IV hyoscine butylbromide. Still, there was no improvement in the accuracy of N-staging. Conclusion: Given the potential side effects and adverse outcomes of IV anti-spasmodic agents, department protocols may need to be re-assessed regarding the prescription of these medications for MRI rectal cancer staging.
... A possible influence on the fetal heart rate is likely to be caused by the temporary tachycardia experienced by the mother. Unlike scopolamine, butylscopolamine bromide does not cross the blood-brain barrier [26]. In line with this, although in vitro studies have demonstrated an interaction between butylscopolamine and the placental choline transport system, butylscopolamine bromide is not thought to cross the placenta [27]. ...
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Background First-time mothers are prone to prolonged labor, defined as the crossing of partograph alert or action lines. Prolonged labor may occur among as many as one out of five women, and is associated with a range of adverse birth outcomes. Oxytocin is the standard treatment for prolonged labor, but has a narrow therapeutic window, several adverse effects and limited efficacy. Despite poor evidence, labor wards often use antispasmodic agents to treat prolonged labor. The antispasmodic drug butylscopolamine bromide (Buscopan®) may shorten duration of labor, but studies on prevention of prolonged labor are lacking. In this randomized double-blind placebo-controlled clinical trial, we aim to evaluate the effect of butylscopolamine bromide on duration of labor in first-time mothers showing first signs of slow labor progress by crossing the World Health Organization partograph alert line. Methods and analysis The study is a single center study at Oslo University Hospital, Oslo, Norway. We will recruit 250 primiparous women with spontaneous labor start at term. Women are included in the first stage of labor if they show signs of slow labor progress, defined as the crossing of the partograph alert line with a cervical dilation between 3–9 cm. Participants are randomized 1:1 to either 20 mg intravenous butylscopolamine bromide or intravenous placebo (1 mL sodium chlorine 9 mg/mL). We considered a mean difference of 60 minutes in labor duration clinically relevant. The primary outcome is duration of labor from the provision of the investigational medicinal product to vaginal delivery. The secondary outcomes include change in labor pain, use of oxytocin augmentation, delivery mode, and maternal birth experience. The primary data for the statistical analysis will be the full analysis set and will occur on completion of the study as per the prespecified statistical analysis plan. The primary outcome will be analyzed using Weibull regression, and we will treat cesarean delivery as a censoring event.
... Hyoscine-N-butyl bromide prevents neural impulse conduction in pelvic-abdominal parasympathetic ganglia by binding to nicotinic receptors. [7,8] There are very few published researches on the effect of HnBB on pain perception during and after HSG. ...
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Background: A tubal patency test is essential in evaluating women with infertility. Hysterosalpingography (HSG) is the investigation of choice for assessing tubal patency. Objective: To evaluate the effect of intramuscular hyoscine-N-butyl bromide on tubal spasms and pain perception during hysterosalpingography. Methods: This randomized, controlled trial was conducted at the Radiology Departments and Infertility Clinics of four health institutions in Bayelsa State, Nigeria, between January 2021 and April 2022. Five hundred and twenty infertile women undergoing hysterosalpingography were randomized into two groups. Women in group I (control) received a placebo, while women in Group II (experimental) received 20 mg of intramuscular hyoscine-N-butyl bromide. Pain scores at different steps of the procedure were recorded. Results: The overall mean pain scores progressively decreased from contrast instillation (4.97 ± 2.08) through 30-minutes post-procedure (3.54 ± 1.54) to 24 hours post-procedure (1.96 ± 1.78). Pain scores at contrast instillation, 30 minutes and 24 hours after HSG were significantly lower in the hyoscine group compared to the placebo group (p = 0.001 each). There were significantly fewer women with tubal blockage in the hyoscine group compared to the placebo group [78 (30.0%) vs 131 (50.4%); p = 0.001]. Conclusion: Intramuscular hyoscine-N-butyl bromide before hysterosalpingography significantly reduces pain and tubal spasm during the procedure. Keywords: Diclofenac, Hyoscine-N-butyl bromide, Hysterosalpingography, Infertility, Pain, Tubal spasms.
... 8 Antispasmodics, analgesics, antacids, antidiarrheals, and laxatives are among frequently prescribed medications for the treatment of upper and lower abdominal pain in children. 9 Fixed-dose combination (FDC) drugs have proven advantages like synergistic effects, less risk of drug resistance, good tolerability, complementary mechanism of action, and cost effectiveness. Nevertheless, their safety needs to be established in real world settings. ...
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Background: The aim of this prospective, single-arm, open-label, multicenter study was to determine the safety and effectiveness of a fixed dose combination of paracetamol and the antispasmodic camylofin dihydrochloride in Indian children with acute colicky abdominal pain.Methods: A total of 197 children with acute colicky abdominal pain were enrolled to receive 2 teaspoons (10 mL) of the syrup thrice daily orally for 5 days per local label. Primary objective was to assess safety as incidence of adverse events (AEs) and change in the severity and frequency of AEs from baseline to end of treatment (EOT). Secondary objectives were effectiveness as evaluated by change in mean (standard deviation [SD]) pain intensity (based on the 100-mm visual analog scale [VAS]) and mean change in the frequency of daily pain episodes from baseline to EOT.Results: In all, 182 (92.4%) patients completed the study. Twenty AEs were reported in 17 patients (8.7%). All AEs were treatment-emergent and of non-serious type. Common AEs included anemia, vomiting, and constipation. At EOT, mean pain intensity significantly (p<0.0001) reduced to 3.3 (8.50) with a mean change of -61.5 (19.56) from baseline. Percentage change in mean intensity of pain from baseline to EOT visit was 94.9%. At EOT, the frequency of daily pain intensity significantly (p<0.0001) reduced to 1.7 (1.01) with a mean change of -3.5 (2.14) from baseline.Conclusions: A fixed-dose combination of camylofin dihydrochloride and paracetamol was effective and well tolerated and had a good safety profile in Indian children with acute colicky abdominal pain.
... Hyoscine is also an anticholinergic medication, which can have a synergistic effect with orphenadrine causing more bowel inertia. 15 Our patient was initially prescribed opiates for pain, which were stopped following presentation of obstructive symptoms. Neither the orthopaedic nor general surgery considered orphenadrine as culprit medication causing this patient's ileus. ...
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Background: Small bowel obstruction commonly presents to surgeons acutely. Adhesions and hernias are the commonest causes. However, medical ileus and gastroparesis are often overlooked. Case report: This article presents a case of an 82year-old woman on orthopaedic ward referred to the general surgeons with symptoms of small bowel obstruction: bilious vomiting and abdominal distension. Despite all conservative measures, symptoms did not improve. Oral contrast on cross-sectional imaging and gastrograffin follow-through consistently illustrated a transition point at the base of jejunum. No mass or mural lesion was seen. The patient was prescribed regular orphenadrine for cramps over her right periprosthetic femoral fracture. Surgical intervention was then considered on suspicion of adhesional small bowel obstruction. A day before the planned laparotomy, the general surgical team stopped orphenadrine as the last attempt to relieve her symptoms. Ceasing orphenadrine reversed her obstructive symptoms and signs within hours. Conclusion: Orphenadrine has a broad range of anticholinergic effects that is known to cause gastroparesis and ileus, which is often overlooked. This article discusses the learning points of this case and reviews literature regarding its pharmacologic effects.
... Hyoscine butylbromide was utilised for this indication more frequently than any other agent. The latter is largely considered a safe choice in elderly patients, due to it crossing the blood brain barrier in limited quantities, hence making central adverse effects unlikely [22]. Hyoscine hydrobromide was prescribed less frequently, but was still administered to 10% of patients. ...
Article
Background: Distressing symptoms are prevalent in patients with idiopathic Parkinson’s disease, yet little is known about symptom burden and subsequent pharmacological management at the end of life. Additionally, when oral administration of antiparkinsonian medications is no longer possible in dying patients it is becoming common place to initiate transdermal Rotigotine, despite a paucity of evidence to guide dosing. Objectives: To assess: (1) symptom prevalence from the use of anticipatory medicines in patients with idiopathic Parkinson’s disease, (2) the prescribing of antiparkinsonian medication at the end of life; and (3) the accuracy of conversion from oral antiparkinsonian medicines to transdermal Rotigotine and any associations between Rotigotine dosing and end of life symptoms. Methods: A retrospective case review was performed. One hundred consecutive patients with idiopathic Parkinson’s disease who died during an inpatient admission at a UK teaching hospital were assessed. Results: The most prevalent terminal symptoms were excess respiratory secretions (58%), pain (52%), agitation (51%), and fever (23%). The majority of patients were converted to transdermal Rotigotine (90%). Patients converted to a higher than equivalent dose of Rotigotine were more likely to be agitated (p<0.05), whilst those converted to a lower than equivalent dose were less likely to develop excess respiratory secretions (p<0.05). The prevalence of pain did not differ according to Rotigotine dosing. Conclusions: This study highlights for the first time use of anticipatory medications at the end of life in patients with idiopathic Parkinson’s disease and the prevalence of terminal symptoms. It also demonstrates the widespread use of Rotigotine patches, and that lower than equivalent doses may be better tolerated.
... It is methylphenidate's more active enantiomer. Common side effects anaphylaxis [11], seizures [12], Abd [13][14], and fever are all. It is not sure to note whether it is safe to use during pregnancy and breastfeeding. ...
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Aims: The present application is a Newly Validated Reverse Phase-High Performance Liquid Chromatography Method for the Assay of Dexmethylphenidate and Serdexmethylphenidate with PDA. Study design: Mentioned study is a quick, rapid, economical, precise, and accurate reverse phase- high performance liquid chromatographic method for estimating Dexmethylphenidate and Serdexmethylphenidate. Place and duration of study: The present assay was carried out at the Shree icon Pharma laboratories PVT.ltd, Vijayawada, AP, and India, from December 2020 to February 2021. Methodology: The stationary phase Agilent C18 column with dimensions of 150x4.6mm, 3.5 was used for chromatography and pH-2.5 ammonium acetate buffer with orthophosphoric acid: acetonitrile in a 50:50 ratio used as a buffer. The detection wavelength was 265nm, and the flow rate was 1mL/min. The strategy was justified according to ICH guidelines Results: Dexmethylphenidate and Serdexmethylphenidate had retention periods of 4.258 and 5.629 minutes, respectively. For the estimation of Dexmethylphenidate and Serdexmethylphenidate, the method has been validated for linearity, accuracy, precision, stability tests, and forced degradation studies including acid, base, hydrolysis, peroxide, and thermal degradation. By multiplying the quality six times, the system's suitability parameter was investigated, and they were well within reasonable limits. The regression coefficient of the two drugs was found to be 0.999 during the linearity study, which was performed at 10% to 150 percentage points. Precision results for Dexmethylphenidate and Serdexmethylphenidate were 0.54 and 1.24, respectively. The drugs were recovered at a rate of 98-102 percent, which is within the acceptable range. Conclusion: The validation results were found to be satisfactory. It was clear that the proposed method was suitable for routine quality control and analysis of pharmaceutical preparations.
... The mechanism of action of the anticholinergic drug HBB is through its competitive antagonism of acetylcholine at the muscarinic receptors. HBB also possesses central anticholinergic properties as it is a tertiary anticholinergic (Ali-Melkkilä, Kanto, & Iisalo, 1993;Corallo, Whitfield, & Wu, 2009;Renner, Oertel, & Kirch, 2005;Tytgat, 2007). ...
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Background: Buscopan is used to treat stomach cramps including those resulting from irritable bowel syndrome, bladder cramps, and pain related to menstruation. Its pregnancy category is determined as C. It has been shown in experimental animal studies that the drug has a negative effect on the embryo, but sufficient and well-controlled studies have not been conducted in humans. The aim of this study is to investigate effects of buscopan on the development of the neural tube (NT) in chick embryos. Methods: Sixty specific pathogen-free (SPF) fertilized eggs were used. SPF eggs were placed in an incubator and divided into six groups at 28 hr of incubation. Five different doses (low to high) of buscopan were injected sub-blastodermally. At the end of 48 hr, the embryos were evaluated morphologically and histopathologically. The argyrophilic nucleolar-organizing region (AgNOR) method was used in this study to determine the proliferation activity of cells in NT development in chick embryos. AgNOR number and total AgNOR area/nuclear area (TAA/NA) were detected for each embryo. Results: Depending on the dose, the embryo's crown-rump length and somite number decreased (p < .05). Significant differences were detected among all groups for mean AgNOR number (p < .05) and TAA/NA ratio (p < .05). Conclusions: Considering the average count of AgNOR cells and TAA/NA ratio, it was found that there was a decrease in cell division depending on the dose. It was determined that buscopan treatment on chick embryos adversely affected early nervous system and NT development. Keywords: birth defects; buscopan; chicken egg; histopathological; neural tube.
... It enhances cervical dilatation and effacement by reducing spasm of smooth muscles of female genital organs, particularly the cervicouterine plexus, through inhibition of cholinergic neurotransmission in the pelvic parasympathetic ganglia. 13 In 2013, a Cochrane Review concluded that antispasmodics can reduce the duration of the first stage of labor, increase the cervical dilatation rate, and reduce the total duration of labor. However, there is insufficient evidence to draw any conclusion regarding the safety of these drugs for both mother and baby. ...
Article
Objectives: The objective of the study is to evaluate the therapeutic effect of hyoscine N-butylbromide (HBB) in active phase of labor and its safety to mother and fetus. Methods: A systematic literature search was conducted on Cochrane Library, Pubmed, EMBASE, CINAHL, ClinicalTrials.gov and three databases in Chinese up to March 31, 2020. Randomized controlled trials (RCTs) of HBB administration during the active phase for shortening of spontaneous labor at term compared with placebo were included. Two reviewers assessed the methodological quality and data extraction independently. We calculated pooled risk ratios (RRs), mean differences (MDs) and 95% confidence intervals (CIs) using Review Manager 5.3 software. Intention-to-treat principles and random-effects model were adopted for analysis and pool results. Results: In total, 1448 women from 9 RCTs were included in the meta-analysis. The HBB group exhibited significantly decreased durations of active phase (MD -61.1 min; 95% CI: -87.7 to -34.4, I2 : 96%), the second stage (MD -2.0 min; 95% CI: -3.4 to -0.5, I2 : 62%), and third stage (MD -0.7 min; 95% CI: -1.1 to -0.3, I2 : 51%). Intravenous (IV) HBB group and intramuscularly (IM) HBB group were compared to the control group (MD -60.9 min; 95% CI -87.7 to -34.1, I2 : 96%). No significant differences were observed in Cesarean section, post-partum hemorrhage, instrumental labor, Apgar scores or any adverse effects. Conclusion: Hyoscine N-butylbromide had a significant effect of shortening the duration of the active phase of labor without adverse effects. We recommend a single dose of intravenous administrated HBB when a woman undergoes labor augmentation.
... These effects on the cardiovascular system cause untoward effects such as cardiac arrhythmia and fluctuation in blood pressure. 10 Some studies have indicated that cardiovascular complications, such as hypotension, arrhythmia, and tachycardia, increase with a massive dose of Hyoscine (≥40mg). 11 This is especially important when it comes to situations like difficult ERCP, in which second and even third dose of Hyoscine may be required. ...
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Purpose: To evaluate the efficacy and safety of low dose versus usual dose of Hyoscine during endoscopic retrograde cholangiopancreatography (ERCP). Patients and methods: This randomized, open-label clinical trial included 282 patients undergoing ERCP who had duodenal peristalsis interfering with cannulation. Patients were randomly divided into two groups: Group one and two received low (5 mg) and usual (10 mg) dose of Hyoscine, respectively. Cardiovascular service consultation was performed for all patients before entering the study and performing ERCP. Hyoscine was injected intravenously, and the spasmolytic effect of the drug was assessed while the papilla was in a completely enface view. The time interval between cessation of peristalsis and its further onset was recorded by the chronometer. Also, patient's heart rate and blood pressure were monitored during ERCP by digital monitoring. Results: The results showed no statistically significant differences in the mean duration of peristalsis, the duration of the antispasmodic activity and the time required to increase the heart rate between two groups (P=0.38, P=0.48, P=0.32, respectively). No significant differences were observed regarding the average of heart rate and mean arterial blood pressure (MAP) before drug administration between the two groups (P=0.182 and P=0.29, respectively), but after the drug administration, tachycardia and hypotension were significantly higher in the second group (P=0.007 and P=0.001, respectively). There was no statistically significant difference in the frequency of arrhythmia between two groups (P=0.08). The results also showed that tachycardia and hypotension occurred more frequently in men and elderly patients (P <0.05). Conclusion: A low dose of Hyoscine is as effective as the usual dose and its side effects such as alteration in blood pressure and heart rate are much fewer, especially in men and elderly patients.
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Camels are commonly administered butylscopolamine (BSA), an antimuscarinic quaternary ammonium derivative, to reduce spasms in the smooth muscles of their urinary and gastrointestinal tracts. However, its presence in body fluids after racing is prohibited by animal racing authorities. The current study aimed to conduct a pilot pharmacokinetic study of BSA in healthy camels. The goal was to obtain initial pharmacokinetic parameters and use these parameters to predict plasma concentrations from the dose and clearance. This will help advise on a withdrawal time for BSA administration before camel racing. The pharmacokinetics of BSA were evaluated in three healthy camels after a single intravenous dose of 0.2 mg/kg body weight. Sensitive liquid chromatography with tandem mass spectrometry was used for the quantification of BSA and the internal standard, ipratropium, in plasma. BSA concentration versus time data were best described by a two-compartment open model. The pharmacokinetic parameters (median and range) were as follows: terminal elimination half-life was 2.29 (1.48–2.46) h, plasma clearance was 1,018.5 (772.4–1,024.0) mL/h/kg, volume of distribution at steady state was 931.9 (700.0–1,068.7) mL/kg, Cmax was 443.9 (351.1–443.9) ng/mL, and Tmax was 0.5 (0.25–0.75) h. BSA’s irrelevant plasma concentration was estimated to be 20 ng/mL. Consequently, it can be concluded that plasma would not contain BSA at the screening level of 20 ng/mL at the usual dose of 0.2 mg/kg body weight 24 h before camel racing.
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The cholinergic system has been increasingly linked to the pathophysiology of mood disorders such as depression, with the potential involvement of nicotinic and/or muscarinic receptors. Conventional antidepressants usually require weeks of daily dosing to achieve a full antidepressant response. In contrast, clinical studies have shown that scopolamine, a nonselective muscarinic acetylcholine receptor antagonist, can induce potent and rapid antidepressant effects, requiring only a few days of treatment. This study aimed to examine the suitability of the unpredictable chronic mild stress (UCMS) model of depression to reproduce the above scopolamine antidepressant activity patterns. Rapid and sustained antidepressant-like effects were assessed by using the splash test, sucrose preference test (SPT), tail suspension test (TST), and forced swimming test (FST) in animals undergoing the UCMS procedure and stress-naïve C57BL/6J mice. Western Blotting was used to measure tropomyosin receptor kinase B (TrkB), mammalian target of rapamycin (mTOR), eukaryotic elongation factor (eEF2) and postsynaptic density protein 95 (PSD95) levels. Scopolamine induced antidepressant-like effects in a dose-dependent manner only after subchronic, but not single, administration in the UCMS model of depression in C57BL/6J mice without affecting locomotor activity. Specifically, scopolamine administered at a dose of 0.3 mg/kg for four consecutive days significantly reversed the UCMS-induced depressive-like behavior, such as apathy, anhedonia, and behavioral despair, while scopolamine, given at the same dose but only once, did not relieve the above symptoms. Scopolamine treatment was accompanied by eEF2 protein dephosphorylation and its subsequent reactivation in the prefrontal cortex (PFC). Subchronic administration of scopolamine is needed to ameliorate UCMS-induced depressive-like behavior. The suggested mechanism of scopolamine action covers eEF2 protein activity in the PFC.
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This study aimed to determine the effects of 24-epibrasinolide (EBL) and methyl jasmonate (MJ) treatments on growth parameters and secondary metabolite synthesis in adventitious root and cell suspension cultures of Hyoscyamus niger. Therefore, different concentrations (0.5, 1 and 2 mg L⁻¹) of EBL alone and combined with 224.3 mg L⁻¹ (1 mM) MJ were applied to root and cell suspension cultures. 2 mg L⁻¹ and 1 mg L⁻¹ EBL were determined as the treatments in which the highest values were obtained in terms of growth criteria in root and cell cultures, respectively. In root cultures, the highest scopolamine accumulation (2.57 mg g⁻¹) was obtained from the combination of 2 mg L⁻¹ EBL and MJ, while the highest value (0.66 mg g⁻¹) for hyoscyamine was observed in the roots treated with 1 mg L⁻¹ EBL and MJ. In cell cultures, 2 mg L⁻¹ EBL for scopolamine and 0.5 mg L⁻¹ EBL for hyoscyamine were found to be the best applications and calculated as 0.51 µg g⁻¹ and 0.28 µg g⁻¹, respectively. EBL and MJ treatments also stimulated total phenolic content (TPC). The highest TPC in root cultures was detected as 18.01 mg g⁻¹ with the combination of MJ while in cell cultures, maximum TPC was observed in cells applied with 2 mg L⁻¹ EBL and MJ as 11.56 mg g⁻¹. When EBL and MJ were applied to root and cell suspension cultures, significant changes occurred in the amount of phenolic compounds. Co-application of EBL and MJ significantly increased the amount of gallic acid, catechin, epicatechin, cinnamic acid and chlorogenic acid in root cultures. The application of 2 mg L⁻¹ EBL was determined as the most suitable application for gallic acid, catechin, epicatechin, p-coumaric acid, and caffeic acid in cell cultures. It was also found that the metabolite production performance of adventitious roots was higher than that of cells. In conclusion, it was suggested that the use of MJ and EBL may be a promising strategy to enhance the accumulation of scopolamine, hyoscyamine and phenolics in root and cell cultures of H. niger.
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Introduction The anti-cholinergic agent hyoscine-N-butylbromide (HBB) is used in gastrointestinal (GI) endoscopy to decrease motility and facilitate endoscopic procedures. Data from clinical studies to support this practice is limited especially for therapeutic procedures. Likewise, patterns of use among endoscopist are largely unclear. This study sought to assess usage of HBB among German-speaking endoscopists. Material and Methods We conducted an anonymous online survey among endoscopists in German-speaking countries. Results A total of 207 physicians participated in the survey. The majority (76.9%) were experienced endoscopists and 92.3% of respondents use HBB at least occasionally during procedures. The reported median stated frequency of HBB use varied greatly between different types of procedures and increased with the complexity of the procedure being performed. HBB was rarely used in diagnostic esophagogastroduodenoscopies (EGD) (median stated frequency 1% of procedures), while use frequency was significantly higher in EGD with endoscopic mucosal resection (EMR) (10%; p=0.002) and EGD with endoscopic submucosal dissection (ESD) (20%; p<0.001). Similarly, use frequency during diagnostic colonoscopy was lower (5%) compared to colonoscopy with EMR (20%, p=0.005) or ESD (42.5%, p<0.001). The highest use frequency was reported for ERCP (50%). The most frequently stated reason to use HBB was facilitation of the procedure (80.6%) followed by increasing diagnostic yield (58.3%). Conclusion German-speaking endoscopists commonly use HBB, most frequently to facilitate complex therapeutic procedures. Given there is almost no data supporting HBB use in therapeutic endoscopy, we suggest that more research is needed to evaluate benefits and risks of this practice.
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Introduction: Acute gastrointestinal cramping pain (GICP) is a debilitating condition that affects many people worldwide, significantly reducing their quality of life. As such, prompt treatment is crucial. Areas covered: This article will explore relevant literature from databases such as PubMed, Scopus, Google Scholar, Cochrane Library, and Web of Science. Additionally, we searched ClinicalTrials.gov and the WHO ICTRP database for the latest clinical trials. Expert opinion: Consensus dictates that antispasmodics such as hyoscine-N-butyl bromide and mebeverine should be the primary treatment for GICP. If these prove ineffective, patients can switch to an antispasmodic with a different mode of action or add acetaminophen/NSAIDs for more severe cases. Currently, several antispasmodics are undergoing clinical trials, including drotaverine, alverine, pinaverium, otilonium bromide, fenoverine, tiropramide, otilonium bromide, trimebutine, and peppermint oil. Well-designed head-to-head studies are necessary to evaluate current antispasmodics' safety, efficacy, pharmacokinetic, and pharmacoeconomics profiles. Recent studies have shown that fixed-dose combinations of antispasmodics + NSAIDs or two different antispasmodics can improve patient compliance and synergistically reduce GICP. Therefore, it is recommended that the global availability and accessibility of these products be enhanced.
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An axially chiral quaternary ammonium salt based on an ammonium‐centered spirocyclic scaffold was synthesized from readily available triphenylmethanol. Its enantiopure form was obtained by resolution from a diastereomeric mixture of the corresponding (R,R)‐tartrate salt. Application of this chiral quaternary ammonium salt in phase‐transfer catalytic asymmetric alkylation was also examined. image
Article
Purpose To assess whether administration of intramuscular (IM) glucagon improves T2-weighted image quality at multiparametric MRI (mpMRI) of the prostate. Materials and Methods In this Health Insurance Portability and Accountability Act-compliant single-center study, the authors retrospectively analyzed radiology reports from 3960 mpMRI examinations (2495 after exclusions) performed between September 2013 and September 2019 and performed outcome comparisons and semiquantitative image assessment of axial T2-weighted images from 120 consecutive mpMRI examinations performed between May 2015 and February 2016. Three experienced radiologists blinded to administration of IM glucagon assessed images using a five-point Likert scale (5 = no motion or blur) for overall image quality, anatomic delineation (prostate capsule, rectum, and lymph nodes), and identification of benign prostatic hyperplasia nodules. Wilcoxon rank sum and χ2 tests were used to assess quantitative parameters. Results The number of mpMRI radiology reports (599 examinations performed with glucagon; 1896, without glucagon) mentioning blur or motion were similar between groups (P = .82). Regression analysis of semiquantitative image quality assessments of T2-weighted images from mpMRI examinations (60 performed with glucagon; 60, without glucagon) demonstrated that images with glucagon were more likely to receive higher scores (4 or 5 rating) than those without glucagon only when the rectum (P = .001) and lymph nodes (P = .01) were evaluated, not when the prostatic capsule, benign prostatic hyperplasia nodules, or overall image quality was evaluated. No evidence of differences was found in identified Prostate Imaging Reporting and Data System (PI-RADS) lesions or targeted-biopsy Gleason scores. Conclusion Administration of IM glucagon did not improve T2-weighted image quality in prostate MRI examinations and showed similar PI-RADS scores and biopsy yields compared with examinations without glucagon. Keywords: MRI, Genital/Reproductive, Urinary, Prostate, Oncology, Observer Performance © RSNA, 2023 Online supplemental material is available for this article. See also commentary by Eberhardt in this issue.
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The mixture of Hyoscine N‐butyl bromide (HBB) and Ketoprofen (KTP) is commonly used for the handling of abdominal spasms and pain reliever. There are two challenges that restrict the simultaneous assessment of HBB and KTP in biological fluids and pharmaceuticals, the first issue is the difficulty of elution of HBB and the second one is the presence of KTP as a racemic mixture in all pharmaceutical formulations that obscure the appearance of it as a single peak. An ultra‐sensitive and highly efficient liquid chromatography–mass/mass spectrometric (LC–MS/MS) method is designed and validated for the first concurrent assessment of HBB and KTP in spiked human serum and urine, and pharmaceutical formulations. The estimated linearity ranges for HBB and KTP were respectively, 0.5 ‐ 500 ng/mL and 0.05‐500 ng/mL, with excellent correlation coefficients. Validation results showed that the value of relative standard deviations (RSDs) were less than 2 % for HBB and KTP. The mean extraction recoveries for HBB and KTP were respectively, 91.04 and 97.83 % in spasmofen® ampoules; 95.89 and 97.00 % in spiked serum; 97.31 and 95.63 in spiked urine. The presented innovative chromatographic approach was utilized for the measurement of trace amounts of coexisting pharmaceuticals in pharmacokinetics studies and routine therapeutic medication monitoring.
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Nowadays various analgesic medications are used for the management of acute and chronic pain. Among these opioid and non-steroidal anti-inflammatory drugs stand in the first line of therapy, however, prolonged administration of these substance is generally challenged by development of analgesic tolerance in patients. Therefore, it is highly valuable to find new pharmacological strategies for prolonged therapeutic procedures. In this respect, Taurine, a free amino acid, has been shown to induce significant analgesia at both spinal and peripheral levels through cholinergic mechanisms. In the present study, we used hot-plate analgesic test to investigate how taurine either as a single medication or in combination with sodium salicylate and morphine may affect both acute response to pain and development of analgesic tolerance. The effect of taurine was also tested on morphine withdrawal syndrome. Hyoscine butyl bromide was used to assess the role of muscarinic receptors in taurine-mediated effects. Finally, biochemical assay was done to reveal how the activity of brain acetylcholinesterase may change in relation with muscarinic receptor activity. Results indicated that acute administration of taurine-sodium salicylate combination causes more potent analgesia compared to the use of tau (but not SS alone) and this seems to be mediated via activity of muscarinic receptors in peripheral nervous system. Furthermore, the effect of this combination undergoes less analgesic tolerance during time. Combination of taurine and morphine is an effective strategy to attenuate both morphine analgesic tolerance and dependence and this also seems to depend on activity of muscarinic receptors, however through differential cellular mechanisms.
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Crohn's disease (CD) is a kind of inflammatory bowel disease (IBD) characterized by the chronic transmural inflammatory state of gastrointestinal tract that typically affects ileum, colon, and perineum. Although the precise etiology is unknown, the major risk aspects concerned with CD consist of several environmental factors, altered microbiota, unhealthy low fiber-high carbohydrate diet, and certain medicines like non-steroidal anti-inflammatory drugs. The disease has wide distribution and inflammation may affect the different areas of the alimentary tract in diverse people. In about 80 % of patients, only small bowel involvement is typically present, affecting distal ileum resulting in ileitis. In about 50 % patients, both ileum and colon are affected resulting in ileocolitis and in approximately 20 % patients, disease is limited to colonic portion. Perianal disease affects almost one-third of patients. As per the various genetic researches in the CD patients, various genetic mutations affect the body's immunological system that results in severe inflammatory state. The two major gene mutations which result in the pathological state of CD are autophagy-related 16-like 1 (ATG16L1) and nucleotide-binding oligomerization domain-containing protein 2 (NOD2/ Card15). The main techniques used for diagnosis of CD include the combination of pathological findings, endoscopic and radiographic findings demonstrating the disease features. The utmost preferred radiologic study for assessing the small bowel CD is abdominal computerized tomography (CT). The goal of current treatment strategies is to address symptomatic relief. Sequence of treatment includes induction therapy, followed by maintenance of remission. The currently used drugs that effectively can cause induction as well as maintain remission include 5-aminosalicylic acid, Tumor Necrosis Factor (TNF) inhibitors, immunomodulators and steroids. Treatment and management should be integrated with lifestyle and dietary amendments to prevent therapeutic failure and consideration of surgical intervention.
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Tropane alkaloids (TAs) are among the most valued chemical compounds known since pre-historic times. Poisonous plants from Solanaceae family ( Hyoscyamus niger, Datura, Atropa belladonna , Scopolia lurida, Mandragora officinarum, Duboisia ) and Erythroxylaceae ( Erythroxylum coca ) are rich sources of tropane alkaloids. These compounds possess the anticholinergic properties as they could block the neurotransmitter acetylcholine action in the central and peripheral nervous system by binding at either muscarinic and/or nicotinic receptors. Hence, they are of great clinical importance and are used as antiemetics, anesthetics, antispasmodics, bronchodilator and mydriatics. They also serve as the lead compounds to generate more effective drugs. Due to the important pharmacological action they are listed in the WHO list of essential medicines and are available in market with FDA approval. However, being anticholinergic in action, TA medication are under the suspicion of causing dementia and cognitive decline like other medications with anticholinergic action, interestingly which is incorrect. There are published reviews on chemistry, biosynthesis, pharmacology, safety concerns, biotechnological aspects of TAs but the detailed information on anticholinergic mechanism of action, clinical pharmacology, FDA approval and anticholinergic burden is lacking. Hence the present review tries to fill this lacuna by critically summarizing and discussing the above mentioned aspects. Graphical Abstract
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Background Hyoscine butylbromide (HBB) has been available for use as an antispasmodic since 1951 and is indicated for the treatment of abdominal pain associated with cramps. A previous review in 2007 summarized the evidence on the mode of action of HBB in vitro and in vivo in both animal and human studies. However, since then, novel publications have appeared within the literature and also our knowledge of what represents normal motility in humans has evolved. Purpose This review is the result of the collaboration between a basic scientist and clinicians with the aim of providing an updated overview of the mechanisms of action of HBB and its clinical efficacy to guide not only use in clinical practice, but also future research.
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Samenvatting In een placebogecontroleerde, multicenter, dubbelblind gerandomiseerde studie met 128 patiënten met bevestigde niersteenkolieken is onderzocht of placebo non-inferieur is aan continue infusie van butylscopolamine. De ene arm kreeg continue infusie van butylscopolamine, de andere arm placebo (zoutoplossing i.v.). De primaire uitkomstmaat was de hoeveelheid escapemedicatie in aantal toegediende doses. Het mediane aantal doses was in beide groepen één. Het aantal extra doses in de placebogroep was 0,05, met een 95% robuust BI van −0,38–0,47. De bovengrens van het BI bleef onder de gestelde non-inferioriteitsgrens van 0,5 ( p = 0,04). Er werden geen verschillen gezien tussen de groepen in secundaire uitkomstmaten. Placebo is non-inferieur aan butylscopolamine continue infusie ter pijnstilling bij patiënten met een niersteenkoliek. Op basis van dit onderzoek en eerdere studies blijkt continue infusie van butylscopolamine iv niet van meerwaarde te zijn bij de behandeling van patiënten met een niersteenkoliek.
Article
Study objective: To compare between oral diclofenac potassium alone versus a combination of it with hyoscine-N-butyl bromide (HBB) in reduction of pain in women undergoing office hysteroscopy. Design: Randomized, double-blind controlled trial. Setting: Kasralainy hospital (a tertiary hospital). Intervention: Sixty-Four patients undergoing office hysteroscopy were randomly divided into 2 groups (study group and placebo group) in the ratio of 1:1. Group 1 (study group = 32 participants) received two oral HBB tablets and one tablet of diclofenac potassium and group 2 (placebo group = 32 participants) received two oral placebo tablet similar in size, structure and color to buscopan in addition to the diclofenac tablet. The patient was given the drugs 30-60 min before the procedure. Results: There was statistically significant difference between the two groups in the pain score immediately during entry (p value = 0.001) and after 30 min of the procedure (p value = < 0.001). And there was a statistically significant difference as regards the side effects (gastric irritation) of the medications (p value = 0.04) between the women participating in the two groups. Conclusion: The combination of diclofenac potassium and HBB helps a lot in decreasing the pain and discomfort during and after performing office hysteroscopy but with more gastric side effects.
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Background: Cardiovascular effects for drugs such as hyoscine butylbromide are poorly documented in the literature, unlike atropine, which is considered the antimuscarinic of choice in the presence of intraoperative bradycardia. Aim: The aim of the study was to describe the dose-related cardiovascular effect of hyoscine butylbromide in patients between 18 and 65 years of age, with low perioperative risk undergoing elective surgery under general anaesthesia on an outpatient basis or hospitalised at our institution between 1 January and 31 May 2019. Methods: Descriptive, cross-sectional, retrospective study; 28 patients with low perioperative risk who underwent general anaesthesia were selected. Changes in heart rate and blood pressure were analysed during the first 6 minutes after the administration of hyoscine butylbromide. The data obtained was recorded in a Microsoft Excel database and analysed using the Excel analysis tool and IBM SPSS. Results: The average dose of 0.15mg/kg of hyoscine butylbromide achieved an increase in heart rate and mean arterial pressure in 96% and 92.8%, respectively, in the first 6 minutes after the administration. Significant changes in heart rate and blood pressure were obtained during the first 6 minutes at doses between 0.05mg/kg and 0.15mg/kg. Conclusion: Hyoscine butylbromide generates positive effects on the heart rate and blood pressure of patients under general anaesthesia, representing a possible alternative in the management of intraoperative bradycardia.
Chapter
The medicinally important species of the Solanaceae family belong to genera viz., Solanum, Atropa, Datura, Hyoscyamus, Nicotiana, etc. The active phytoalkaloids which are present in them are tropane, pyrrolidine–pyridine, and steroid alkaloids. Some of the pharmacologically potent alkaloids are scopolamine, atropine, hyoscyamine, nicotine, cocaine, solanidine, and solasodine. Tropane alkaloids, their semisynthetic, and synthetic derivatives are used as antispasmodic, antiemetic, mydriatic, and bronchodilator because of anticholinergic actions. Compounds with tropane nuclei bearing diester group on their structure without quaternary ammonium have shown local anesthetic and CNS stimulant actions. Nicotine is a pyrrolidine–pyridine alkaloid that acts on nicotinic receptors. Steroidal alkaloids like solasodine are poisonous and serve as starting material for the synthesis of steroidal hormones. This chapter describes general methods of extraction and isolation of alkaloids. The sources, classification, pharmacological actions, and structure–activity relationship of tropane alkaloids are illustrated with a special emphasis on chemical structure elucidation of atropine.
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Background and objective: Hyoscine-N-butyl bromide (HBB) and paracetamol (acetaminophen)are widely used in emergency departments for abdominal pain and cramps. However, there is not enough data on the efficacy, safety, and superiority of each other in treating acute gastroenteritis (AGE) related abdominal pain and cramps. In this study HBB and paracetamol were compared for the treatment of abdominal pain and cramps related to acute gastroenteritis. Materials and methods: The study was conducted in a tertiary university hospital emergency department as a prospective, randomized-controlled, and double-blind study. Intravenous (IV) 1000 mg paracetamol and IV 20 mg hyoscine-N-butyl bromide (HBB) were used to treat abdominal pain and cramps related to AGE. Visual analogue scale (VAS) was used to evaluate the degree of abdominal pain before and after treatment. Results: HBB and paracetamol groups consisted of 123 and 158 cases respectively. In both groups, it was observed that the VAS score gradually decreased from the 0th hour to the 1st and 2nd hours (p0.05). No severe side effects were observed in any of the patients. Conclusion: HBB and paracetamol were used for symptomatic treatment in AGE patients presenting with abdominal pain and cramps. A significant reduction in pain and cramps was achieved in both patient groups. There was no difference between the two drugs in terms of treatment efficacy and side effects. IMC J Med Sci 2022; 16(1): 009. DOI: https://doi.org/10.55010/imcjms.16.007 *Correspondence: Hasan Gümüşboğa, Department of Emergency, Şehitkamil State Hospital, Gaziantep, Turkey, Posta code: 27500; Email: profhasan@hotmail.com; ORCID:0000-0003-2097-7102.
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Background/aims: Endoscopic removal of bile duct stones has become the treatment of choice, which includes endoscopic sphincterotomy (EST) in the majority of cases, destroying at least partially the Oddi sphincter (OS). Loss of sphincter function in variable grade has been described, but changes in innervation are not known. Methods: Endoscopic manometry of OS was performed in 14 patients after EST with specialized perfused catheter. Pressure values were registered before and after 10 mg Buscapina injected intravenously. Results: Choledocho-duodenal pressure gradient was absent in all of 14 patients. Basal OS pressure was zero in 7 and conserved in normal range in the remaining 7. Phasic motor activity was registered in 11 patients and was absent in 3 patients. After 10 mg Buscapina intravenous injection, instead of habitual inhibition, increase in basal OS pressure and in frequency of phasic contractions was observed in 9 patients. This response was not related to age of patients, neither with time elapsed between the EST and manometry, nor the estimated size of papillotomy orifice. Duodenal peristalsis was invariably inhibited in all patients. Conclusions: EST destroys not only the smooth muscle of OS, also alters the innervation interrupting the duodeno-sphincteric nerve circuit. This finding questions the use of Buscapina or other anticholinergic agent as spasmolytic in patients after EST.
Article
Research Question To investigate the effect of adding an anti-spasmodic to an existing ultrasound-guided manual vacuum aspiration (USG-MVA) protocol to alleviate immediate post-procedure abdominal cramping pain in women treated for early pregnancy loss. Design : Double-blind, placebo-controlled, randomised control trial conducted between February 2018 and January 2020 in a university-affiliated tertiary hospital. 111 women were assigned to receive a 1ml intravenous injection containing either a 20mg hyoscine butylbromide (HBB) (n = 55) or saline (n =56) as a control immediately before the USG-MVA procedure. The primary outcome was whether adding a 20mg dose HBB to the current pain control regimen reduced abdominal pain. Secondary outcomes were vaginal pain, complications and side effects, women's pre- and post-procedure's psychological state, physiological stress (saliva alpha-amylase (sAA) and procedure pain control satisfaction. Two-way mixed ANOVA was used to evaluate for main effects and interactions. Results VAS abdominal pain scores in the HBB group were 16% lower immediately and 21% lower two hours postoperatively, though not statistically significant. Two-way ANOVA indicated that time (F (1,108) =83.41,p<0.001) was the only significant main effect for the reduction in abdominal pain post-procedure and vaginal pain score (F(1,108)=180.1, p<0.0001) but not drug received. No adverse events were reported. No significant difference was noted for psychological state, physiological stress and procedure pain control satisfaction between the two groups. Conclusions Anti-spasmodics can be helpful in the reduction of USG-MVA associated abdominal cramping pain, though our results showed HBB produced an insignificant decrease in abdominal pain score. Further studies with longer-acting or larger doses of anti-spasmodics are warranted.
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Introduction: Irritable bowel syndrome is a common functional gastrointestinal disorder in children, characterized by recurrent abdominal pain associated with altered bowel habits in terms of both frequency and consistency. According to change in stool consistency it is categorized into 4 subtypes. From the etiological perspective, it is a multifactorial functional disorder with both central (psychosocial) and peripheral factors (altered bowel sensitivity, motility and microbiota) implied in the genesis of the symptoms. Several treatment options, addressing each underlying pathophysiological mechanism have been proposed. However, since in most cases a combination of factors takes part in symptoms' generation, the overall treatment response rate is often unsatisfactory if a multidisciplinary is not pursued. Areas covered: The aim of this manuscript is to summarize the current pharmacotherapy in paediatric irritable bowel syndrome in order to aid clinicians in treating this challenging disorder. Expert opinion: Most evidence involving paediatric populations rely on open label or retrospective studies and/or are not specifically designed for irritable bowel syndrome but tend to generalise their results to mixed populations of children with functional gastrointestinal disorders. A high placebo response rate combined with poor patients' selection could account for the overall weak evidence supporting the use of pharmacological agents in paediatric irritable bowel syndrome. Given the multifaceted nature of the disorder, multidisciplinary approaches combining pharmacotherapy with alternative treatments is highly recommendable.
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A stability indicating method was developed and validated for the quantitative simultaneous estimation of hyoscine butylbromide (HBB) and paracetamol (PAR) in a combined dosage form by means of isocratic reverse-phase high-performance liquid chromatography (RP-HPLC). Separation was performed on a YMC C18 (250 × 4.6 mm, 5 μm) column using phosphate buffer–Methanol (60:40, v/v) in the isocratic elution regime at a flow rate of 1 mL/min. Quantification was achieved with UV detection at 210 nm. The retention time obtained for HBB was 9.509 min and that for PAR was 4.198 min in a continuous run up to 20 min. The detector response was found to be linear in a concentration range of 2.5 – 7.5 μg/mL for HBB and 125 – 375 μg/mL for PAR. The proposed method was validated as per ICH guidelines and shown to be specific, precise, linear, accurate, and robust. The samples were subjected to various accelerated stress conditions. The degradation products were well resolved at significantly different retention times. Thus, the proposed method can be applied successfully for the simultaneous estimation of PAR and HBB in combined pharmaceutical formulations and for their stability studies.
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Key points Recent animal and human physiology studies indicate that noradrenergic and muscarinic processes are key mechanisms that mediate pharyngeal muscle control during sleep. The noradrenergic agent reboxetine combined with the anti‐muscarinic hyoscine butylbromide has recently been shown to improve upper airway function during sleep in healthy individuals. However, whether these findings translate to the clinically relevant patient population of people with obstructive sleep apnoea (OSA), and the effects of the agents on OSA severity, are unknown. We found that reboxetine plus hyoscine butylbromide reduced OSA severity, including overnight hypoxaemia, via increases in pharyngeal muscle responsiveness, improvements in respiratory control and airway collapsibility without changing the respiratory arousal threshold. These findings provide mechanistic insight into the role of noradrenergic and anti‐muscarinic agents on upper airway stability and breathing during sleep and are important for pharmacotherapy development for OSA. Abstract The noradrenergic agent reboxetine combined with the anti‐muscarinic hyoscine butylbromide has recently been shown to improve upper airway function during sleep in healthy individuals. However, the effects of this drug combination on obstructive sleep apnoea (OSA) severity are unknown. Accordingly, this study aimed to determine if reboxetine plus hyoscine butylbromide reduces OSA severity. Secondary aims were to investigate the effects on key upper airway physiology and endotypic traits. Twelve people with OSA aged 52 ± 13 years, BMI = 30 ± 5 kg/m², completed a double‐blind, randomised, placebo‐controlled, crossover trial (ACTRN12617001326381). Two in‐laboratory sleep studies with nasal mask, pneumotachograph, epiglottic pressure sensor and bipolar fine‐wire electrodes into genioglossus and tensor palatini muscles were performed separated by approximately 1 week. Each participant received either reboxetine (4 mg) plus hyoscine butylbromide (20 mg), or placebo immediately prior to sleep. Polysomnography, upper airway physiology and endotypic estimates of OSA were compared between conditions. Reboxetine plus hyoscine butylbromide reduced the apnoea/hypopnoea index by (mean ± SD) 17 ± 17 events/h from 51 ± 30 to 33 ± 22 events/h (P = 0.005) and nadir oxygen saturation increased by 6 ± 5% from 82 ± 5 to 88 ± 2% (P = 0.002). The drug combination increased tonic genioglossus muscle responsiveness during non‐REM sleep (median [25th, 75th centiles]: −0.007 [−0.0004, −0.07] vs. −0.12 [−0.02, −0.40] %maxEMG/cmH2O, P = 0.02), lowered loop gain (0.43 ± 0.06 vs. 0.39 ± 0.07, P = 0.01), and improved airway collapsibility (90 [69, 95] vs. 93 [88, 96] %eupnoea, P = 0.02), without changing the arousal threshold (P = 0.39). These findings highlight the important role that noradrenergic and muscarinic processes have on upper airway function during sleep and the potential for pharmacotherapy to target these mechanisms to treat OSA.
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Background Bowel preparation before multiparametric MRI (mpMRI) of the prostate is performed widely, despite contradictory or no evidence for efficacy.PurposeTo investigate the value of hyoscine N-butylbromide (HBB), microenema (ME) and ‘dietary restrictions’ (DR) for artifact reduction and image quality (IQ) in mpMRI of the prostate.Study typeRetrospective.PopulationBetween 10/2018 and 02/2020 treatment-naïve men (median age, 64.9; range 39.8–87.3) who underwent mpMRI of the prostate were included. The total patient sample comprised of n = 180 patients, who received either HBB, ME, were instructed to adhere to DR, or received a combination of those measures prior to the MR scan.Field strength/sequenceT2-weighted imaging (T2w), diffusion-weighted imaging (DWI), and dynamic contrast-enhanced MRI (DCE-MRI) scanned on two 3T systems.AssessmentA radiologist specialized in urogenital imaging (R1) and a senior radiology resident (R2) visually assessed IQ parameters on transversal T2w, DWI and ADC maps on a 5-point Likert-like scale.Statistical testsGroup comparison between IQ parameters was performed on reader level using Kruskal–Wallis and Mann–Whitney U tests. Binary univariate logistic regression analysis was used to assess independent predictors of IQ. Interrater agreement was assessed using Intraclass Correlation Coefficient (ICC).Results‘DWI geometric distortion’ was significantly more pronounced in the HBB+/ME−/DR− (R1, 3.6 and R2, 4.0) as compared to the HBB−/ME+/DR− (R1, 4.2 and R2, 4.6) and HBB+/ME+/DR− (R1, 4.3 and R2, 4.7) cohort, respectively. Parameters ‘DWI IQ’ and ‘Whole MRI IQ’ were rated similarly by both readers. ME was a significant independent predictor of ‘good IQ’ for the whole MRI for R1 [b = 1.09, OR 2.98 (95% CI 1.29, 6.87)] and R2 [b = 1.01, OR 2.73 (95% CI 1.24, 6.04)], respectively.Data conclusionME seems to significantly improve image quality of DWI and the whole mpMRI image set of the prostate. HBB and DR did not have any benefit.
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In this paper we proposed a new approach for medical diagnosis which is based on the distance between interval valued intuitionstic fuzzy sets. We developed an interview chart with help of the interval fuzzy degrees. The formulation of interview chart is based on the relation between symptoms disease for stomach ache (Constipation, Appendicitis, Irritable Bowel syndrome (IBS)). Stomach ache is a common reason for medical visits. Now days many people have serious and non serious stomach ache. We also utilize the interval valued intuionistic fuzzy weighted to improve arithmetic average operator to aggregate fuzzy information from the symptoms. We also establish a measure based on distance between interval valued intuitionstic fuzzy sets for medical diagnosis. We use the methods to illustrate a numerical example which shows that patients suffer preferentially from constipation (type of stomach ache) which has been also presented graphically.
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Objective To review medical management of inoperable malignant bowel obstruction. Data Sources A literature review using PubMed and MEDLINE databases searching malignant bowel obstruction, etiology, types, pathophysiology, medical, antisecretory, anti-inflammatory, antiemetic drugs, analgesics, promotion of emptying, prevention of infection, anticholinergics, somatostatin analogs, gastric antisecretory drugs, prokinetic agents, glucocorticoid, opioid analgesics, antibiotics, enema, and adverse effects. Study Selection and Data Extraction Randomized or observational studies, cohorts, case reports, or reviews written in English between 1983 and November 2020 were evaluated. Data Synthesis Malignant bowel obstruction (MBO) commonly occurs in patients with advanced or recurrent malignancies and severely affects the quality of life and survival of patients. Its management remains complex and variable. Medical management is the cornerstone of MBO treatment, with the goal of reducing distressing symptoms and optimizing quality of life. Until now, there has been neither a standard clinical approach nor registered medications to treat patients with inoperable MBO. Relevance to Patient Care and Clinical Practice This review provides information on the etiology, type and pathophysiology, and medical treatment of MBO and related adverse reactions of the drugs commonly used, which can greatly assist clinicians in making clinical decisions when treating MBO. Conclusions Published research shows that medical management of MBO mainly consists of antisecretory, anti-inflammatory strategies, controlling vomiting and pain, promoting emptying, preventing infection, and combination therapy. Being knowledgeable about the most current treatment options, the related adverse effects, and the evidence supporting different practices is critical for clinicians to provide individualized medical therapy for MBO patients.
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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 < 0·05 and p < 0·025.
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Quality of life is reduced in patients with irritable bowel syndrome, and the costs for this disease are substantial to society. During a meeting in London, UK, the IBiS club reviewed the literature on these subjects. Drawbacks and advantages with existing instruments to assess quality of life and costs were discussed and the clinical and scientific relevance of the current knowledge was assessed. A summary from the meeting is presented in this paper.
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Quaternary ammonium derivatives such as cimetropium, n-butyl scopolammonium, otilonium and pinaverium bromide have been discovered and developed as potent spasmolytics of the gastrointestinal tract. Their pharmacological activity has been proven in both "in vivo" and "in vitro" studies of hypermotility. "In vitro" experiments showed that they possess antimuscarinic activity at nM level but only pinaverium and otilonium are endowed with calcium channel blocker properties. These latter compounds relaxed the gastrointestinal smooth muscle mainly through a specific inhibition of calcium ion influx through L-type voltage operated calcium channels. Molecular pharmacology trials have indicated that pinaverium and otilonium can bind specific subunits of the calcium channel in the external surface of the plasma membrane and in this way they block the machinery of the contraction. Recent evidence showed that otilonium is able to bind tachykinin NK(2) receptors and not only inhibits one of the major contractile agents but can reduce the activation of afferent nerves devoted to the passage of sensory signals from the periphery to the central nervous system. Thanks to their typical physico-chemical characteristics, they are poorly absorbed by the systemic circulation and generally remain in the gastrointestinal tract where they exert the muscle relaxant activity by a local activity. Some differences exists in the absorption among these compounds: both n-butyl scopolammonium and cimetropium are partially taken up in the bloodstream, pinaverium has a low absorption (8-10 %) but is endowed with an excellent hepato-biliary excretion and otilonium, which has the lowest absorption (3 %), is almost totally excreted by faeces. Quaternary ammonium derivatives are widely used for the treatment of irritable bowel syndrome and recent meta-analyses have supported their efficacy in this disease. Due to its therapeutic index, the use of n-butyl scopolammonium is more indicated to treat acute colics than a chronic disease such as irritable bowel syndrome. Taking into consideration the published trials carried out with validated methodology in irritable bowel syndrome, cimetropium and otilonium are the best demonstrated drugs for the improvement in global assessment, pain and abdominal distension.
Article
Aim: To update previous overviews of placebo-controlled double-blind trials assessing the efficacy and tolerance of smooth muscle relaxants in irritable bowel syndrome. METHODS AND TRIALS: A total of 23 randomized clinical trials were selected for meta-analyses of their efficacy and tolerance. Six drugs were analysed: cimetropium bromide (five trials), hyoscine butyl bromide (three trials), mebeverine (five trials), otilium bromide (four trials), pinaverium bromide (two trials) and trimebutine (four trials). The total number of patients included was 1888, of which 945 received an active drug and 943 a placebo. Results: The mean percentage of patients with global improvement was 38% in the placebo group (n=925) and 56% in the myorelaxant group (n=927), in favour of myorelaxants with a mean odds ratio of 2.13, P < 0.001 (95% CI: 1.77--2.58) and a mean risk difference of 22% P < 0.001 (95% CI: 13--32%). The percentage of patients with pain improvement was 41% in the placebo group (n=568) and 53% in the myorelaxant group (n=567): odds ratio 1.65, P < 0.001 (95% CI: 1.30--2.10) and risk difference 18%, P < 0.001 (95% CI: 7--28%). There was no significant difference for adverse events. Conclusion: Myorelaxants are superior to placebo in the management of irritable bowel syndrome.
Article
Purpose: To evaluate the efficacy of pharmacologic agents for the irritable bowel syndrome. Data Sources: Electronic literature search of MEDLINE (1966 to 1999), EMBASE (1980 to 1999), PsycINFO (1967 to 1999), and the Cochrane controlled trials registry and a manual search of references from bibliographies of identified articles. Study Selection: Randomized, double-blind, placebo-controlled, parallel, or crossover trials of a pharmacologic intervention for adult patients that reported outcomes of improvement in global or irritable bowel-specific symptoms. Data Extraction: Qualitative and quantitative data reported on study groups, interventions, treatment outcomes, and trial methodologic characteristics. Data Synthesis: 70 studies met the inclusion criteria. The most common medication classes were smooth-muscle relaxants (16 trials), bulking agents (13 trials), prokinetic agents (6 trials), psychotropic agents (7 trials), and loperamide (4 trials). The strongest evidence for efficacy was shown for smooth-muscle relaxants in patients with abdominal pain as the predominant symptom. Loperamide seems to reduce diarrhea but does not relieve abdominal pain. Although psychotropic agents were shown to produce global improvement, the evidence is based on a small number of studies of suboptimal quality. Psychotropic drugs, 5-hydroxytryptamine (5-HT)-receptor antagonists, peppermint oil, and Chinese herbal medicine require further study. Conclusions: Smooth-muscle relaxants are beneficial when abdominal pain is the predominant symptom. In contrast, the efficacy of bulking agents has not been established. Loperamide is effective for diarrhea. Evidence for use of psychotropic agents is inconclusive; more high-quality trials of longer duration are needed. Evidence for the efficacy of 5-HT-receptor antagonists seems favorable, although more studies are needed.
Article
The prevalence and impact of abdominal pain, bloating, and diarrhea in the adult US population are largely unknown. We conducted a national, cross-sectional, telephone survey of US households to provide estimates of the frequency, duration, severity, and impact of specific digestive symptoms during the previous month. A total of 2510 subjects completed interviews (70.7% response rate). Among the respondents, 1017 (40.5%) reported one or more digestive symptoms within the month before the interview, including abdominal pain or discomfort 21.8%, bloating or distension 15.9%, and diarrhea or loose stools 26.9%. Women were more likely than men to report abdominal pain or discomfort (24.4% vs 17.5%) and bloating or distension (19.2% vs 10.5%), but not diarrhea or loose stools (27.1% vs 26.7%). Symptoms were less common among those 60 years of age. More than 65% of respondents rated symptoms as moderate or severe in intensity, and the majority reported limitations in daily activities. We conclude that digestive symptoms are more common than previously recognized and have a significant impact.
Article
A double-blind controlled therapeutic trial of factorial design was used to study the therapeutic effects of lorazepam, hyoscine butylbromide, and ispaghula husk in 12 randomised blocks of eight patients with the irritable bowel syndrome (IBS). Each of the three agents caused a sustained symptomatic improvement in some of the patients, although only with ispaghula was the difference between the real and dummy preparation statistically significant. When the eight possible combinations of treatment were analysed none of the 12 patients who received only dummy preparations of the three agents had maintained any improvement over the three months of the trial. Seven patients improved among the 12 who received potent preparations of all three agents, and between four and six patients improved in the groups receiving one or two of the potent preparations. These therapeutic results, though far from perfect, show that the types of drug commonly used to treat IBS are of some value and may be additive in their effects. Similar combinations of other therapeutic agents may be more effective, but it will be possible to determine this only by carrying out factorial therapeutic trials.
Article
A double-blind, randomized parallel group trial comparison involving 712 patients with irritable bowel syndrome was performed. Over a treatment period of 4 weeks hyoscine-N-butylbromide (30 mg/day p.o.) plus paracetamol (1 500 mg/day p.o.), hyoscine-N-butylbromide (30 mg/day p.o.), paracetamol (1. 500 mg/day p.o.) or placebo (3 tablets/day p.o.) were administered. Patients kept a diary and entered a daily rating of their symptoms (visual analogue scale). At the end of the four weeks 81% of the patients in the Buscopan plus group were deemed "responder" (marked or some improvement in symptoms). In the Buscopan group 76%, in the paracetamol group 72% and in the placebo group 64% of the patients were responders. The differences between the Buscopan plus group and the placebo group, and between the Buscopan group and the placebo group were statistically significant. The daily rating on the analogue scale showed a statistically significant improvement in abdominal pain intensity in the Buscopan plus group versus the placebo group and in the Buscopan plus group versus the paracetamol group. Thirty-eight patients ( = 5%, no differences between the treatment groups) experienced adverse effects, that did not require treatment. Buscopan plus and Buscopan are suitable for the treatment of the irritable bowel syndromes.
Article
The spasmolytic activity of N-Butyl Hyoscine (NBH) (1) has been investigated in conscious dogs provided with ileal or colonic Thiry fistulas in which motility was stimulated by intraluminal distension. In ileal motility experiments, phasic motility index (PMI), intestinal tonus, contraction frequency and heart rate were monitored. Intravenous administration of NBH (10 to 100 micrograms/kg) depressed PMI (ED50 35.1 micrograms/kg) and the other motility parameters. Heart rate increases were observed at 100 micrograms/kg. Application of NBH directly into the fistula (300 to 3000 micrograms/kg) caused a long-lasting, potent inhibition (31-72%) of PMI; tonus and contraction frequency were only slightly affected, while heart rate was not altered. When NBH was administered into an ileal fistula adjacent to the one from which motility was recorded, changes of PMI and other parameters were observed only after a massive dose of the drug (10000 micrograms/kg). In colonic fistula experiments, intraluminal NBH administration (300 to 3000 micrograms/kg) depressed colonic motility (39-59%), without affecting heart rate. It is concluded that NBH present in the intestine, although poorly absorbed, exerts local spasmolytic action.
Article
The effects of N-butylhyoscine bromide (Buscopan) were examined on responses of guinea-pig isolated intestine to transmural stimulation and to peristalsis induced by raising the intraluminal pressure. The drug acted rapidly and in low concentration to abolish peristaltic activity and responses to transmural stimulation when applied to the serosal surface of the ileum, but from 100 to 1000 times the concentration was required when it was applied to the mucosal surface. The effects were more persistent after mucosal than after serosal application. N-Butylhyoscine bromide was bound to mucus and mucosal material, the ratio of free to bound drug being 2:1. The drug passed through portions of the intestinal wall containing Peyer's patches more rapidly than through portions containing no macroscopically visible lymphoid tissue. The rate of passage through Peyer's patches, but not through other portions, increased with increasing hydrostatic pressure. These findings help to explain why enterally administered N-butylhyoscine bromide exerts anti-cholinergic effects on the gut without producing systemic actions.
Article
Hyoscine N-butyl bromide (Buscopan) antagonized the spasmogenic action of acetylcholine on guinea-pig isolated ileum, having a pA2 of 7·8. The drug also had intestinal antispasmodic activity in the anaesthetized cat after either parenteral or enteral administration. With the enterally administered drug larger doses were required, but the effects were longer lasting. Enterally administered in conscious dogs the drug sometimes produced a small increase in heart rate.
Article
In the guinea-pig isolated distal colon, the order of anticholinergic activity is as follows: atropine > tropenziline bromide > N-butyl hyoscine bromide. The reduction in the responses to pelvic and transmural stimulation produced by tropenziline and N-butyl hyoscine bromide is due partly to their ganglion blocking activity. This effect also explains the reduction they cause in acetylcholine output on pelvic nerve and transmural stimulation. Since atropine also reduces acetylcholine release on pelvic nerve stimulation, it is suggested that muscarinic receptors of the parasympathetic ganglia are involved in transmission of pelvic nerve impulses.
Article
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.
Article
The inhibitory effect of five antispasmodic preparations, prifinium bromide, hyoscine butylbromide, propinox, trimebutine maleate and phloroglucinol + trimethyl-phloroglucinol on acetylcholine-induced contraction of the colon was investigated in anesthetized dogs. Prifinium bromide was most potent followed by hyoscine butylbromide. The other three preparations had no potent inhibitory effect even when given in a dose of 1000 micrograms/kg. The ED50 was 3.1 micrograms/kg for prifinium bromide and 12.3 micrograms/kg for hyoscine butylbromide; the prolonged time of action at ED50 was approximately 30 minutes for prifinium bromide and about 10 minutes for hyoscine butylbromide. From the dog experiments, it became clear that prifinium bromide and hyoscine butylbromide had a relatively potent antispasmodic effect on the colon.
Article
Cyclotropium bromide, a new antimuscarinic agent, inhibits gastrointestinal motility in animals at lower doses than those required to inhibit gastric acid secretion and salivation. In man, cyclotropium bromide suppresses fasting and meal stimulated colonic motility. This study investigated the effects of single oral doses of 60 mg cyclotropium bromide, 60 mg hyoscine N-butylbromide and placebo on gastric emptying and on antral motor activity. Twenty four healthy men (mean age 25 years) participated in three experiments one week apart. The drugs were administered, in random double blind fashion, 30 minutes before the ingestion of a semisolid test meal labelled with 74 MBq (2 mCi) 99mTc sulphur colloid. A gamma camera coupled to a computer monitored gastric emptying together with amplitude, frequency, and propagation velocity of antral contractions. Cyclotropium bromide and, to a lesser degree, hyoscine N-butylbromide delayed gastric emptying and reduced contraction amplitude, but did not affect frequency and propagation velocity of antral contractions. Cyclotropium bromide was significantly more active than hyoscine N-butylbromide; the effects of hyoscine N-butylbromide differed significantly from placebo. Antral contractile activity was present all the time. After cyclotropium bromide, there was a significant correlation between antral contraction amplitude and gastric emptying. No adverse side effects occurred with any one treatment. In conclusion, cyclotropium bromide markedly inhibits gastric emptying and reduces antral contraction amplitude.
Article
Continuous recording of proximal jejunal motility in conscious healthy subjects was made following ingestion of 200 mg hyoscine butylbromide (ten times the recommended therapeutic dosage). There was no detectable modification of fasting or postprandial motor activity, although the therapeutic potency of the standard intravenous dose was confirmed.
Article
To evaluate the efficacy of pharmacologic agents for the irritable bowel syndrome. Electronic literature search of MEDLINE (1966 to 1999), EMBASE (1980 to 1999), PsycINFO (1967 to 1999), and the Cochrane controlled trials registry and a manual search of references from bibliographies of identified articles. Randomized, double-blind, placebo-controlled, parallel, or crossover trials of a pharmacologic intervention for adult patients that reported outcomes of improvement in global or irritable bowel-specific symptoms. Qualitative and quantitative data reported on study groups, interventions, treatment outcomes, and trial methodologic characteristics. 70 studies met the inclusion criteria. The most common medication classes were smooth-muscle relaxants (16 trials), bulking agents (13 trials), prokinetic agents (6 trials), psychotropic agents (7 trials), and loperamide (4 trials). The strongest evidence for efficacy was shown for smooth-muscle relaxants in patients with abdominal pain as the predominant symptom. Loperamide seems to reduce diarrhea but does not relieve abdominal pain. Although psychotropic agents were shown to produce global improvement, the evidence is based on a small number of studies of suboptimal quality. Psychotropic drugs, 5-hydroxytryptamine (5-HT)-receptor antagonists, peppermint oil, and Chinese herbal medicine require further study. Smooth-muscle relaxants are beneficial when abdominal pain is the predominant symptom. In contrast, the efficacy of bulking agents has not been established. Loperamide is effective for diarrhea. Evidence for use of psychotropic agents is inconclusive; more high-quality trials of longer duration are needed. Evidence for the efficacy of 5-HT-receptor antagonists seems favorable, although more studies are needed.
Article
The main objectives of this study were to assess whether the use of different definitions of irritable bowel syndrome (IBS) could influence measurements of its prevalence and characterize the patient population fulfilling these different diagnostic criteria. A telephone survey was carried out by contacting 8,221 subjects aged >or=18 Years representative of the French population. A "screening" questionnaire based on three algorithms of IBS classification (Manning, with or without a notion of a minimal duration of symptoms, Rome I and Rome II) was used by specialised inquirers. Twenty three percent of the subjects interviewed stated that they had suffered from abdominal pain during the previous 12 Months. The prevalence of IBS considerably varied, depending on the diagnostic criteria used: 12% based on Manning criteria without reference to the duration of symptoms; 2.5% if the notion of duration of symptoms was added to the Manning criteria, and 2.1% and 1.1% based on the Rome I and Rome II criteria, respectively (the latter including the same notion of duration). In total, 212 subjects (2.6%) met at least one of the criteria including a minimal duration of symptoms, with a predominance for women (sex-ratio close to 2). The prevalence of IBS is strongly dependent on the classification algorithm employed. The requirement of a minimum duration of symptoms eliminates IBS in a large number of subjects complaining of abdominal disorders. Once these methodological variations were taken into account, the prevalence of IBS in France was found to be comparable to that published in international literature.
Article
Irritable bowel syndrome represents a common gastrointestinal disorder that significantly impacts patients' lives. It is defined by Rome II criteria and characterized by abdominal pain and bloating associated with changes in bowel habit. Visceral hypersensitivity is currently considered a biological marker for the disease. Current therapeutic treatments include the use of fiber supplements, antidiarrheal agents, laxatives, antispasmodics, tricyclic antidepressants and serotonergic agents. Through a proper understanding of the diagnostic criteria, pathophysiology and treatment options, this disorder can be treated effectively in many patients.
Article
To evaluate therapies available for the treatment of irritable bowel syndrome, and provide consensus recommendations for their use, a total of 51 double-blind clinical trials using bulking agents, prokinetics, antispasmodics, alosetron, tegaserod and antidepressants were selected. The quality of studies was assessed using 5-point scale. Meta-analyses were performed on all studies, and on 'high-quality studies'. The efficacy of fibre in the global irritable bowel syndrome symptoms relief (OR: 1.9; 95% CI:1.5-2.4) was lost after exclusion of low-quality trials (OR: 1.4; 95% CI: 1.0-2.0, P = 0.06). When excluding the low-quality trials, an improvement of global irritable bowel syndrome symptoms with all antispasmodics (OR: 2.1; 95% CI:1.8-2.9) was maintained only for octylonium bromide, but on the basis of only two studies. Antidepressants were effective (OR: 2.6, 95% CI: 1.9-3.5), even after exclusion of low-quality studies (OR: 1.9, 95% CI: 1.3-2.7). Alosetron (OR: 2.2; 95% CI: 1.9-2.6) and tegaserod (OR: 1.4; 95% CI: 1.2-1.5) showed a significant effect in women. We recommend the use of tegaserod for women with irritable bowel syndrome with constipation and alosetron for women with severe irritable bowel syndrome with diarrhoea. Antidepressants can be beneficial for irritable bowel syndrome with diarrhoea patients with severe symptoms. Loperamide can be recommended in painless diarrhoea. Evidence is weak to recommend the use of bulking agents in the treatment of irritable bowel syndrome with constipation.
Article
Based on current evidence, bulking agents are not more effective than placebo at improving global irritable bowel syndrome (IBS)symptoms, although they may increase stool frequency in large doses. Tricyclic antidepressants are more effective than placebo for patients with diarrhea-predominant IBS. Imodium is more effective than placebo at improving stool consistency and decreasing stool frequency in patients with IBS, and it may be an important component for treating diarrhea-predominant IBS. Antispasmodics agents available in the United States are not more effective than placebo for treating IBS, although the studies are small and poorly designed. There are no randomized controlled trials examining the efficacy of laxatives for managing IBS. Tegaserod is more effective than placebo at improving global IBS symptoms in women with nondiarrhea-predominant IBS. Alosetron is more effective than placebo in women with diarrhea-predominant IBS, although its use should be limited to patients who have failed conventional therapy because of its adverse event profile.
Article
Irritable bowel syndrome (IBS) is one of the most common functional gastrointestinal disorders, with an estimated prevalence rate in the general population of 10–15% in industrialised countries. Although IBS is not a life-threatening disease, it contributes significantly to a large segment of healthcare resource consumption. This review provides an overview of studies addressing the direct and indirect costs of IBS in the US and the UK. A systematic literature search was conducted in MEDLINE and the Cochrane library; additionally, all reference lists covering the years from 1960 to May 2004 were scanned. Twenty-four publications for the US and the UK, published between 1991 and 2003, were identified: 6 were excluded, 18 were included. Data for the UK, US and UK + US were reported in 5, 11 and 2 publications, respectively. Total direct cost estimates per patient per year ranged from US348toUS348 to US8750 (calculated for year 2002). The average number of days off work per year because of IBS was between 8.5 and 21.6; indirect costs ranged from US355toUS355 to US3344. The total costs and cost components of IBS are influenced by several factors: features of the investigated patient group (age, limitation to healthcare seekers or all IBS patients, comorbidity, severity of symptoms), database used, method of data collection (retrospective or prospective, varying cost components, time-point of data collection in relation to index-date of IBS diagnosis, method of cost calculation [incidence or prevalence based]) and different healthcare systems in the US and the UK. These factors led to the incomparability of published data, thus no comprehensive picture can be drawn of the total costs related to IBS in the UK and US. Data underline the magnitude of the economic impact of IBS in the UK and US, which is increased by a factor of 1.1–6.0, compared with matched non-IBS control groups. IBS contributes both direct and indirect costs to the total healthcare bill. Further studies should take influencial factors into account and report related data carefully in order to provide useful and comparable published cost data. Additionally, further research on the cost effectiveness of diagnostic procedures and therapies in IBS is required to define strategies to help IBS patients improve their quality of life and reduce related costs.
Article
To compare the efficacy and tolerability of oral hyoscine butylbromide (hereafter hyoscine) 10 mg t.d.s., paracetamol 500 mg t.d.s. and their fixed combination against placebo in patients with recurrent crampy abdominal pain. A total of 1637 patients were entered into a four-arm double-blind study. After a 1 week placebo run-in, they were randomized to 3 weeks of treatment with one of the four therapies with assessments after 1, 2 and 3 weeks. Pain intensity (Visual Analogue Scale) and pain frequency (Verbal Rating Scale) were self-assessed daily. Pain intensity on the Visual Analogue Scale decreased in all treatment groups; the adjusted mean changes from baseline were 2.3, 2.4 and 2.4 cm for the hyoscine, paracetamol and combination groups, respectively, compared with 1.9 cm for the placebo group (all P < 0.0001). The Verbal Rating Scale also showed a statistically significant decrease of 0.7, 0.7 and 0.7 in the hyoscine, paracetamol and combination groups compared with 0.5 in placebo (all P < 0.0001). All treatments were well tolerated: 16%, 14%, 17% and 11% of patients on hyoscine, paracetamol, combination and placebo reported at least one adverse event. Hyoscine, paracetamol and their fixed combination are effective in the treatment of recurrent crampy abdominal pain and well tolerated if used three times daily continuously for 3 weeks.
Article
Though functional gastrointestinal complaints are recognised as being common throughout the world, there have been few comparative studies of prevalence. To compare the prevalence and management of abdominal cramping/pain in nine countries. In a two-stage community survey, approximately 1000 subjects were interviewed in each of nine countries to establish the demographics of individuals with abdominal cramping/pain (stage 1) followed by market research-driven interviews with >or=200 sufferers per country (stage 2). 9042 subjects were interviewed in stage 1. Mexico (46%) and Brazil (43%) had the highest prevalence of abdominal cramping/pain; Japan the lowest (10%). Abdominal cramping/pain was more common in women (12-55%) than in men (7-38%). About 1717 subjects participated in stage 2; 65% were women and the average age at symptom onset was 29 years. The frequency of episodes differed between countries, being highest in the US (61% suffered at least once in a week). Sufferers in the US and Latin America reported a higher usage of medications (around 90%) than those in Europe (around 72%). In most countries over-the-counter drugs were principally used. Antispasmodic drugs were most popular in Latin America and Italy, antacids in Germany and the UK. Drug therapy decreased the duration of episodes (by up to 81% in Brazil). The community prevalence, severity, healthcare seeking and medication usage related to abdominal cramping/pain are high overall, but vary considerably between countries.