-
Drugs 2007Abdominal cramping and pain is a frequent problem in the adult population of Western countries, with an estimated prevalence of < or =30%. Hyoscine butylbromide... (Review)
Review
Abdominal cramping and pain is a frequent problem in the adult population of Western countries, with an estimated prevalence of < or =30%. Hyoscine butylbromide (scopolamine butylbromide) [Buscopan/Buscapina] is an antispasmodic 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 <1%. However, because of its high tissue affinity for muscarinic receptors, hyoscine butylbromide remains available at the site of action in the intestine and exerts a local spasmolytic effect.Ten placebo-controlled studies have evaluated the efficacy and safety of oral or rectal hyoscine butylbromide. Hyoscine butylbromide was considered beneficial in all of these trials, which supports its use in the treatment of abdominal pain caused by cramping. Hyoscine butylbromide is barely absorbed and detectable in the blood and does not penetrate the blood-brain barrier, and is, therefore, generally well tolerated. Few adverse events have been reported; in particular, no significant increases in the incidence of anticholinergic-related adverse effects have been observed. In summary, hyoscine butylbromide appears to be a valuable treatment option for patients with symptoms of abdominal pain or discomfort associated with cramping.
Topics: Animals; Butylscopolammonium Bromide; Clinical Trials as Topic; Colic; Humans; Molecular Structure; Muscarinic Antagonists; Parasympatholytics; Treatment Outcome
PubMed: 17547475
DOI: 10.2165/00003495-200767090-00007 -
PloS One 2022First-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...
Study protocol for the BUSCopan in LABor (BUSCLAB) study: A randomized placebo-controlled trial investigating the effect of butylscopolamine bromide to prevent prolonged labor.
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.
Topics: Pregnancy; Female; Humans; Butylscopolammonium Bromide; Oxytocin; Bromides; Labor, Obstetric; Delivery, Obstetric; Randomized Controlled Trials as Topic
PubMed: 36327275
DOI: 10.1371/journal.pone.0276613 -
Journal of Veterinary Pharmacology and... Dec 2018The oral tablet formulation of butylscopolamine, which is available without prescription, is commonly used by trainers of racing greyhounds to treat functional urethral...
The oral tablet formulation of butylscopolamine, which is available without prescription, is commonly used by trainers of racing greyhounds to treat functional urethral obstruction. As medication control of butylscopolamine is therefore required for such use to ensure the integrity of greyhound racing, an administration study was performed in six greyhounds to determine the pharmacokinetics of orally administered butylscopolamine. A single dose of one 10 mg butylscopolamine tablet was administered orally to simulate this use in greyhound racing. Blood, urine and faeces were collected at regular intervals from the greyhounds for up to 9 days and butylscopolamine concentrations determined. There was some, but very limited, absorption of butylscopolamine, with rapid elimination from plasma with a mean half-life of 2 hr. Urine concentrations initially declined in a similar manner to the plasma pharmacokinetics but then entered a much longer half-life of approximately 50 hr. Faecal concentrations declined to very low levels between 48 and 120 hr. The use of orally administered butylscopolamine for functional urethral obstruction in greyhounds is unjustified due to this very limited drug absorption. Medication control of butylscopolamine's antispasmodic effect on the digestive tract is possible by setting screening limits based on the urinary and faecal drug levels as determined in this study.
Topics: Administration, Oral; Animals; Butylscopolammonium Bromide; Dogs; Female; Half-Life; Male
PubMed: 30076627
DOI: 10.1111/jvp.12701 -
JAMA Oct 2021Death rattle, defined as noisy breathing caused by the presence of mucus in the respiratory tract, is relatively common among dying patients. Although clinical... (Randomized Controlled Trial)
Randomized Controlled Trial
IMPORTANCE
Death rattle, defined as noisy breathing caused by the presence of mucus in the respiratory tract, is relatively common among dying patients. Although clinical guidelines recommend anticholinergic drugs to reduce the death rattle after nonpharmacological measures fail, evidence regarding their efficacy is lacking. Given that anticholinergics only decrease mucus production, it is unknown whether prophylactic application may be more appropriate.
OBJECTIVE
To determine whether administration of prophylactic scopolamine butylbromide reduces the death rattle.
DESIGN, SETTING, AND PARTICIPANTS
A multicenter, randomized, double-blind, placebo-controlled trial was performed in 6 hospices in the Netherlands. Patients with a life expectancy of 3 or more days who were admitted to the participating hospices were asked to give advance informed consent from April 10, 2017, through December 31, 2019. When the dying phase was recognized, patients fulfilling the eligibility criteria were randomized. Of the 229 patients who provided advance informed consent, 162 were ultimately randomized. The date of final follow-up was January 31, 2020.
INTERVENTIONS
Administration of subcutaneous scopolamine butylbromide, 20 mg four times a day (n = 79), or placebo (n = 78).
MAIN OUTCOMES AND MEASURES
The primary outcome was the occurrence of a grade 2 or higher death rattle as defined by Back (range, 0-3; 0, no rattle; 3, rattle audible standing in the door opening) measured at 2 consecutive time points with a 4-hour interval. Secondary outcomes included the time between recognizing the dying phase and the onset of a death rattle and anticholinergic adverse events.
RESULTS
Among 162 patients who were randomized, 157 patients (97%; median age, 76 years [IQR, 66-84 years]; 56% women) were included in the primary analyses. A death rattle occurred in 10 patients (13%) in the scopolamine group compared with 21 patients (27%) in the placebo group (difference, 14%; 95% CI, 2%-27%, P = .02). Regarding secondary outcomes, an analysis of the time to death rattle yielded a subdistribution hazard ratio (HR) of 0.44 (95% CI, 0.20-0.92; P = .03; cumulative incidence at 48 hours: 8% in the scopolamine group vs 17% in the placebo group). In the scopolamine vs placebo groups, restlessness occurred in 22 of 79 patients (28%) vs 18 of 78 (23%), dry mouth in 8 of 79 (10%) vs 12 of 78 (15%), and urinary retention in 6 of 26 (23%) vs 3 of 18 (17%), respectively.
CONCLUSIONS AND RELEVANCE
Among patients near the end of life, prophylactic subcutaneous scopolamine butylbromide, compared with placebo, significantly reduced the occurrence of the death rattle.
TRIAL REGISTRATION
trialregister.nl Identifier: NTR6264.
Topics: Aged; Aged, 80 and over; Butylscopolammonium Bromide; Cholinergic Antagonists; Confidence Intervals; Death; Double-Blind Method; Drug Administration Schedule; Female; Hospice Care; Humans; Incidence; Informed Consent; Injections, Subcutaneous; Life Expectancy; Male; Middle Aged; Netherlands; Placebos; Proportional Hazards Models; Respiratory Sounds; Treatment Outcome
PubMed: 34609452
DOI: 10.1001/jama.2021.14785 -
Naunyn-Schmiedebergs Archiv Fur... 1951
Topics: Autonomic Agents; Butylscopolammonium Bromide; Ganglia; Ganglia, Autonomic; Scopolamine Derivatives
PubMed: 14934141
DOI: No ID Found -
The Analyst Mar 2020It is not a simple task to develop techniques for analyzing tricyclic quaternary ammonium alkaloids (TCQAAs) because of the relative polarity and alkalinity of the... (Review)
Review
It is not a simple task to develop techniques for analyzing tricyclic quaternary ammonium alkaloids (TCQAAs) because of the relative polarity and alkalinity of the latter. Moreover, less volatility of these alkaloids prevents the establishment of direct GC methods. Hyoscine N Butyl Bromide (HNBB) is one of the most frequently used antispasmodic TCQAAs. There are many therapeutic uses of HNBB other than in antispasmodic activity. It may be used as an analgesic and local cervical antispasmodic drug in maternity labor. A variety of analytical techniques (colorimetric, spectrophotometric, chromatographic, electrophoretic, and electrochemical techniques) have been reported for HNBB analysis. Moreover, two stability-indicating chromatographic methods have also been developed for the drug. Many multistep colorimetric techniques have been developed for HNBB analysis on two main bases; charge-complex formation and the reduction properties of the drug. No spectrofluorometric methods have been reported for HNBB measurement. Many chromatographic methods have been mentioned for HNBB analysis. However, most of them are quite low in terms of sensitivity because of the low ultraviolet (UV) absorbance character of the drug. Therefore, testing the drug by using other detectors, such as refractive index or corona charged aerosol detectors, is strongly recommended. The most sensitive methods are liquid chromatography-mass spectrometry (LC-MS/MS) and ultra-performance liquid chromatography-electrospray ionization-tandem mass spectrometry (UPLC-ESI-MS/MS) techniques since they can detect as low as 1 ng mL-1 and 0.03 ng mL-1, respectively. Determination of the drug by thin-layer chromatography (TLC) is possible only with the use of a reversed-phase TLC plate because of the high polarity of HNBB. A few electrophoresis techniques and many electrochemical methods have also been reported. Two accelerated stability studies were performed for HNBB using LC/MS and high-performance liquid chromatography-ultraviolet (HPLC-UV) methods. The time of the stability study and the presence of mefenamic acid greatly affect the percentage of drug degradation. As a general observation by comparing those two stability methods, strict guidelines for performing stability studies are strongly recommended. Further evaluation of the greenness of all analytical methods for the drug is highly recommended for the choice of more eco-friendly techniques for the safety of the environment.
Topics: Butylscopolammonium Bromide; Chemistry Techniques, Analytical; Humans
PubMed: 32049090
DOI: 10.1039/d0an00076k -
JAMA Oct 2021
Topics: Butylscopolammonium Bromide; Hydrocarbons, Brominated; Muscarinic Antagonists
PubMed: 34609471
DOI: 10.1001/jama.2021.9846 -
British Journal of Anaesthesia Dec 2013Catheter-related bladder discomfort (CRBD) secondary to intraoperative catheterization of urinary bladder is one of the most distressing symptoms during recovery from... (Randomized Controlled Trial)
Randomized Controlled Trial
BACKGROUND
Catheter-related bladder discomfort (CRBD) secondary to intraoperative catheterization of urinary bladder is one of the most distressing symptoms during recovery from anaesthesia. Butylscopolamine, a peripheral antimuscarinic agent, is effective for relieving the pain, which is because of smooth muscle contraction. The aim of this study was to assess the efficacy and safety profiles of butylscopolamine in treating CRBD after urological surgeries.
METHODS
Adult male patients undergoing urological surgery requiring urinary bladder catheterization intraoperatively were enrolled. Induction and maintenance of anaesthesia were standardized. Patients were randomized into two groups after complaining of CRBD in the post-anaesthesia care unit. The control group (n=29) received normal saline and the butylscopolamine group (n=28) was administered butylscopolamine 20 mg i.v. The severity of CRBD, postoperative pain, and adverse effects were assessed at baseline, 20 min, 1, 2, and 6 h after administration of the study drug.
RESULTS
The severity of CRBD observed in the butylscopolamine group was significantly lower than that of the control group at 1, 2, and 6 h after administration of the study drug [59 (12), 50 (16), 40 (21) in the control group vs 41 (22), 32 (25), 23 (18) in the butylscopolamine group, P<0.01]. Rescue analgesics were required less in the butylscopolamine group than in the control group (P=0.001). Adverse events were comparable between the two groups.
CONCLUSION
Butylscopolamine 20 mg administered i.v. after complaining CRBD during recovery reduced both the severity of CRBD and the need for rescue analgesics without adverse effects in patients undergoing urologic surgeries.
Topics: Adult; Aged; Blood Pressure; Butylscopolammonium Bromide; Double-Blind Method; Dysuria; Heart Rate; Humans; Intraoperative Care; Male; Middle Aged; Muscarinic Antagonists; Pain Measurement; Pain, Postoperative; Postoperative Care; Prospective Studies; Treatment Outcome; Urinary Catheterization; Urologic Surgical Procedures, Male; Young Adult
PubMed: 23869107
DOI: 10.1093/bja/aet249 -
Legal Medicine (Tokyo, Japan) May 2006A 40-year-old man experienced cardiopulmonary arrest after intramuscular injection of 20 mg of butylscopolamine bromide. No pathological changes were found at autopsy,...
A 40-year-old man experienced cardiopulmonary arrest after intramuscular injection of 20 mg of butylscopolamine bromide. No pathological changes were found at autopsy, and 1.19 microg/mL of butylscopolamine bromide was detected in his serum. Since he had taken no other drugs, his severe symptoms were thought to have been caused by an anaphylactic reaction to butylscopolamine bromide. Butylscopolamine bromide has been used for many years worldwide, and is considered to be a safe drug, with no reports of severe side effects following intramuscular injection. Since an anaphylactic reaction may not be related to a particular medication, the possibility of such a severe reaction must be considered, even during administration of an ostensibly safe drug such as butylscopolamine bromide.
Topics: Adult; Anaphylaxis; Butylscopolammonium Bromide; Death, Sudden; Drug Hypersensitivity; Heart Arrest; Humans; Injections, Intramuscular; Male; Parasympatholytics
PubMed: 16413812
DOI: 10.1016/j.legalmed.2005.11.001 -
Nuclear Medicine Communications Jan 2008To determine the effect of N-butylscopolamine (buscopan) on intestinal uptake of 18F-FDG.
PURPOSE
To determine the effect of N-butylscopolamine (buscopan) on intestinal uptake of 18F-FDG.
METHODS
Seventy-two oncology patients were prospectively studied and 36 patients received 20 mg of N-butylscopolamine intravenously. All patients were imaged with a Siemens PET scanner. After a 4-h fast, patients were injected with FDG and then scanned 1 h post-injection. Two experienced observers interpreted all studies independently. Scans were scored visually, grading 18F-FDG bowel uptake (0-3) and the influence of bowel uptake to a lack of confidence in scan reporting (0-3). For semi-quantitative comparison, the ratio of radiotracer uptake in the bowel to mean liver (B/L) was obtained.
RESULTS
All results were in favour of N-butylscopolamine. For the qualitative data, a Mann-Whitney test was used. Results for contribution of bowel uptake to lack of confidence in reporting scores, showed P=0.0001 for observer 1, and P=0.002 for observer 2; for degree of uptake in bowel scores, observer 1 results gave a value of P=0.0001 and observer 2 P=0.001. For agreement of uptake scores, Kappa index showed 'moderate' agreement between observers for the control group and 'fair' agreement for the N-butylscopolamine group. For contribution of bowel uptake to lack of confidence scores, there was 'very good' agreement for the control group and 'fair' agreement for the N-butylscopolamine group. The semi-quantitative effect of N-butylscopolamine on bowel-to-liver ratio was determined using an unrelated t-test that produced significance at the level of P<0.001.
CONCLUSION
This study showed that administration of N-butylscopolamine can reduce artefacts in the bowel during 18F-FDG PET, and can potentially improve accuracy of 18F-FDG PET reporting.
Topics: Adult; Aged; Aged, 80 and over; Butylscopolammonium Bromide; Contrast Media; Female; Fluorodeoxyglucose F18; Humans; Image Enhancement; Intestinal Absorption; Intestinal Mucosa; Intestines; Male; Middle Aged; Muscarinic Antagonists; Positron-Emission Tomography; Radiopharmaceuticals
PubMed: 18049092
DOI: 10.1097/MNM.0b013e3282f1d706