The value of hyoscine butylbromide in the treatment of abdominal pain. The active substance hyoscyamine butyl bromide of the preparations buscopan, hyoscine and spanil, instructions for use Contraindications to use
Pharmacological properties
M-cholinergic receptor blocker. Has an antispasmodic effect on smooth muscles internal organs, reduces the secretion of the digestive glands. Does not penetrate the BBB (because hyoscine butyl bromide is a quaternary ammonium derivative), therefore there is no anticholinergic effect on the central nervous system.Indications
- renal colic; - biliary colic; - spastic dyskinesia of the biliary tract and gallbladder; - cholecystitis; - intestinal colic; - pylorospasm; - peptic ulcer stomach and duodenum in the exacerbation phase (as part of complex therapy); - algodismenorrhea.Application
Adults and children over 6 years of age are prescribed orally 1-2 tablets 3-5 times / Tablets should be taken orally with water.Contraindications
- myasthenia gravis; - megacolon; - childhood up to 6 years old; - hypersensitivity to the components of the drug.Side effects
Side effect associated with the anticholinergic effect of the drug: dry mouth, dryness skin, tachycardia; possible retention of urine (usually mild and resolved on its own). Allergic reactions: in rare cases - skin manifestations, anaphylaxis with episodes of shortness of breath.special instructions
The drug is prescribed with caution if intestinal obstruction is suspected (including pyloric stenosis), with obstruction urinary tract (including prostate adenoma), with a tendency to tachyarrhythmias (including atrial fibrillation), angle-closure glaucoma. Buscopan tablet contains 41.2 mg sucrose. The maximum recommended daily dose contains 411.8 mg sucrose.Interaction
Buscopan® can enhance the anticholinergic effect of tricyclic antidepressants, antihistamines, quinidine, amantadine, disopyramide, anticholinergic drugs (for example, tiotropium bromide, ipratropium bromide). The simultaneous use of Buscopan and dopamine antagonists (for example, metoclopramide) leads to a weakening of the effect on the gastrointestinal tract of both drugs. Buscopan® may increase tachycardia caused by beta-agonists.Overdose
Currently, cases of overdose of Buscopan® have not been described, therefore the following symptoms and recommendations are theoretical. Symptoms: anticholinergic effects are possible - urinary retention, dry mouth, skin redness, tachycardia, suppression of gastrointestinal motility, transient visual impairment. Treatment: the use of cholinomimetics is indicated. For glaucoma, pilocarpine (in the form of eye drops). If necessary, cholinomimetics are prescribed for systemic use (for example, neostigmine is administered intramuscularly or intravenously at a dose of 0.5-2.5 mg); cardiovascular complications are treated according to the usual therapeutic guidelines; carry out supportive and symptomatic therapy; with paralysis of the respiratory muscles - intubation and mechanical ventilation; with urinary retention - bladder catheterization.Storage conditions
The drug should be stored out of the reach of children at a temperature not exceeding 25 ° C. The shelf life is 5 years.Temporarily unavailable
Active substance
Hyoscine butylbromide
pharmachologic effect
Spasmolytic, m-anticholinergic.
Blocks m-cholinergic receptors. Causes atropine-like effects: pupil dilation, accommodation paralysis, increased intraocular pressure, increased heart rate, acceleration of sinoatrial and AV conduction, stimulates the automatism of the sinus node and the functional activity of the AV node, relaxes the smooth muscles of the gastrointestinal tract, bile and urinary tract, uterus, bronchi, slows down peristalsis , reduces the secretion of excretory glands (salivary, mucous, sweat).
After oral administration, it is poorly absorbed from the gastrointestinal tract. Protein binding is low.
Mode of application
For adults: Adult patients receive the drug orally from 10 to 20 mg 3 to 5 times a day.
When using the drug in the form of suppositories, patients receive 1 to 2 suppositories 3 times a day.
The drug in parenteral form can be used for subcutaneous, intramuscular and intravenous administration from 20 to 40 mg.
For kids: Children receive the drug intravenously slowly and only for medical emergencies. For children under 12 years of age, the drug is used at a dosage of 0.3 to 0.6 mg per kg of body weight, if necessary, the dose of the drug can be increased to 15 mg per kg of body weight. Children over 12 years of age receive the drug from 20 to 40 mg.
Children aged 1 to 6 years - by mouth, 5-10 mg or rectally, 7.5 mg 3-5 times / day;
at the age of 1 year - by mouth 5 mg 2-3 times / day or rectally 7.5 mg up to 5 times / day.
Indications
Renal colic, ureteral spasms, biliary colic, hypermotor dyskinesia of the biliary tract and gallbladder, cholecystitis, intestinal colic, pylorospasm, gastric ulcer and duodenal ulcer in the acute phase (as part of complex therapy), dysmenorrhea.
Contraindications
Glaucoma, benign hyperplasia prostate gland, pyloric stenosis, tachyarrhythmias, megacolon, mechanical intestinal obstruction, acute pulmonary edema, severe cerebral atherosclerosis.
Side effects
- From the side nervous system and sense organs:
drowsiness, amnesia, violation of accommodation, increased sensitivity of the eyes to light, exacerbation of glaucoma.
- From the digestive tract:
dryness of the oral mucosa and pharynx, constipation, nausea and vomiting.
- Allergic reactions:
skin manifestations, anaphylaxis with episodes of shortness of breath.
Others: dry skin, redness of the skin, tachycardia, difficulty urinating, decreased sweating.
Release form
dragee 0.01 g - 20 pcs in a package;
rectal suppositories - 10 pcs in the package
ATTENTION!
The information on the page you are viewing was created for informational purposes only and does not in any way promote self-medication. The resource is intended to familiarize healthcare professionals with additional information about certain medicines, thereby increasing the level of their professionalism. Use of the drug " Hyoscine butyl bromide"without fail provides for a consultation with a specialist, as well as his recommendations on the method of application and dosage of your chosen medicine.
For citation:The value of hyoscine butylbromide in the treatment of abdominal pain. Breast cancer. 2012; 35: 1718.
Abstract of L.A. Literature Review Samuels and meta-analysis A.C. Ford et al.
L.A. Samuels (Samuels LA Pharmacotherapy update: Hyoscine Butylbromide in the treatment of abdominal spasms // Clinical Medicine: Therapeutics. 2009. Vol. 1. P. 647-665) begins a literature review on the value of hyoscine butylbromide in the treatment of abdominal spastic pain, with the statement the fact that abdominal pain is one of the most common reasons for seeking medical help after headache, back pain and dizziness. Abdominal pain can be a symptom of both transient and self-resolving disorders, and life-threatening conditions that require immediate medical attention. Establishing the correct diagnosis in the interpretation of abdominal pain can be very difficult as it hides various diseases, which is the task of doctors general practice, surgeons, internists, emergency therapy specialists, pediatricians, gastroenterologists, urologists, gynecologists.
Hyoscine butyl bromide (or scopalamine-N-butyl bromide, N-butyl scopolammonium bromide and butyl scopolamine) by the mechanism of its therapeutic effect is a neurotropic antispasmodic.
Acetylcholine (ACC) serves as the main neurotransmitter of the parasympathetic nervous system and acts on 2 types of receptors - muscarinic and nicotinic cholinergic. When stimulated, the preganglionic nerve secretes ACC into the ganglion, and it acts on the nicotinic receptors of postganglionic neurons. Then the postganglionic neuron secretes ACh to excite the muscarinic receptors of the target organ. Several types of muscarinic receptors are known; from the point of view of the mechanism of action of hyoscine butyl bromide, M3 receptors located in smooth muscles blood vessels, bronchi and gastrointestinal tract (GIT), as well as various glands of the respiratory system and gastrointestinal tract. Stimulation of these receptors leads to indirect vasodilation (due to the formation of nitric oxide), bronchoconstriction, increased gastrointestinal motility, and increased glandular secretion. M3 receptors are also found in the ciliary body and the muscles of the iris, where they participate in accommodation and control the size of the pupil. M2 and M3 receptors are found in the organs of the genitourinary system.
Hyoscine butyl bromide has a dual mechanism of action. Firstly, it blocks the action of ACh on muscarinic receptors of smooth muscles, eliminates spasm of smooth muscles of the gastrointestinal tract and urinary tract, and also reduces the motility of these organs. Secondly, hyoscine butyl bromide is a non-competitive blocker of nicotinic receptors, due to which the antisecretory effect is realized, which is manifested by a decrease in the secretion of the digestive glands. The action of Buscopan is realized on the entire gastrointestinal tract, including its upper and lower sections. Therefore, it is prescribed for spasm that occurs in various parts of the gastrointestinal tract, with biliary colic, cystitis, urethritis and primary dysmenorrhea. Hyoscine butyl bromide is used to prevent gastrointestinal spasms before diagnostic tests (X-ray, endoscopic retrograde cholangiopancreatography, colonoscopy).
Hyoscine butyl bromide is a quaternary ammonium compound, its molecule is polarized and retains polarity regardless of the pH of the medium. In this regard, when oral administration there is a slight absorption of the drug (8%), and the systemic bioavailability is less than 1%. Despite the low blood levels, which are recorded for a short time, hyoscine butyl bromide and / or its metabolites are found at the sites of action. When administered intravenously, the drug does not penetrate the blood-brain barrier and has low binding to plasma proteins.
L.A. Samuels presents a brief overview of studies of hyoscine butylbromide in abdominal nonspecific colic and irritable bowel syndrome (IBS). renal colic, dysmenorrhea, as well as its capabilities during childbirth and diagnostic procedures.
Abdominal pain
("Nonspecific colic") and IBS
At the heart of the appointment of butyl bromide hyoscine for nonspecific colicky abdominal pain is its antimuscarinic action. Clinically, this action is manifested by relaxation of the smooth muscles of the gastrointestinal tract with a decrease or disappearance of spasm that the patient feels. This effect was objectively demonstrated in a study of the electrical and biomechanical activity of the stomach: intravenous administration 20 mg of hyoscine butylbromide resulted in a 50.9% decrease in the mechanical motor index, while the electrical motor index decreased by 36.5%.
Efficacy and safety of hyoscine butyl bromide at a dose of 10 mg 3 r. / Day. in comparison with paracetamol 500 mg 3 r. / day, their combination and placebo were studied in recurrent spastic abdominal pain. 1637 patients (after placebo for 1 week) were randomized into 4 treatment groups, the duration of which was 3 weeks. Pain severity (according to the visual analogue scale (VAS) and the verbal rating scale) was statistically significantly reduced in all treatment groups compared with placebo. Treatment was well tolerated in all groups, frequency side effects did not differ significantly between groups (including placebo).
G.N. Tytgat has published literature reviews regarding the oral and parenteral use of hyoscine butylbromide for the treatment of abdominal cramping and other clinical indications. The first analyzed 10 placebo-controlled trials that examined the efficacy and safety of oral and rectal hyoscine. The effectiveness of the drug has been established in all studies, which is considered by the authors as evidence to support the use of the drug for abdominal pain associated with cramps.
The second review presents data on the use of GBD for the treatment of colic / spasm; to improve the performance of diagnostic studies; with parenteral administration for the treatment of biliary and renal colic, spasms of the genitourinary tract; as well as during childbirth and as palliative care. The author came to the conclusion that hyoscine butyl bromide is fast acting and highly effective with good tolerance, which supports its use in a number of indications associated with acute abdominal cramps, during childbirth for palliative treatment, as well as during diagnostic and therapeutic procedures in abdominal cavitywhich can be difficult with spastic contractions.
The effect of butyl bromide hyoscine has also been studied in abdominal pain caused by a functional disorder. This was a double-blind, randomized, parallel-group, comparative study that included 712 IBS patients. Patients within 4 weeks. were prescribed hyoscine butyl bromide + paracetamol, hyoscine butyl bromide, paracetamol, or placebo. The VAS was used to assess symptoms. By the end of treatment, more than 75% of patients in the hyoscine butylbromide group experienced symptom relief. There was a statistically significant decrease in the intensity of abdominal pain in the hyoscine butylbromide group compared with placebo and paracetamol.
Renal colic
L.A. Samuels cites 6 studies involving 755 patients evaluating hyoscine butyl bromide as an adjunctive pain reliever (along with morphine and indomethacin) compared to placebo, nonsteroidal anti-inflammatory drugs (NSAIDs) and other antispasmodics. It was concluded that hyoscine butyl bromide is effective in the treatment of renal colic, either alone or in combination with opioids and NSAIDs. It should be noted that the speed of onset and duration of the analgesic effect is better when NSAIDs are prescribed.
Dysmenorrhea
L.A. Samuels is reviewing 2 studies using hyoscine butylbromide in primary and secondary dysmenorrhea. In the first double-blind, cross-over study of 120 women, hyoscine butyl bromide and paracetamol were compared with lysine clonixinate and proprinox, as well as placebo. In both treatment groups, there was a significant decrease in subjective pain score compared with placebo. A long-term open-label study investigated the combined use of lysine clonixinate and hyoscine butyl bromide during 3 consecutive menstrual cycles in 30 women. The women initially had very severe (10.7%), severe (42.9%) or moderate (46.4%) pain. By the end of the study, only 1 patient had moderate pain.
Childbirth
Several authors have studied the effect of hyoscine butyl bromide as a labor-accelerating agent, citing the fact that if pain during labor cannot be relieved in a safe way, then it is possible to safely reduce the duration of labor (and therefore labor pain). The use of hyoscine butylbromide resulted in a statistically and clinically significant decrease in the period between drug administration and delivery in the absence of significant adverse reactions on the part of the mother or newborn.
Abdominal pain and discomfort during diagnostic
procedures
In 3 studies, the efficacy of hyoscine butyl bromide compared with placebo (2 studies; 208 patients) and glucagon (1 study; 100 patients) was assessed by sigmoidoscopy and / or colonoscopy. When compared with placebo, a decrease in the duration of the procedure was proved in the group receiving hyoscine butyl bromide. Comparison with glucagon was in favor of the latter for facilitating the endoscopic procedure.
There is evidence that intramuscular injection butyl bromide hyoscine improves image quality in abdominal magnetic resonance imaging. It was found that magnetic resonance imaging of the liver and pancreas is somewhat better with a decrease in the gastrointestinal motility of hyoscine with butyl bromide.
IBS is one of the functional disorders of the gastrointestinal tract, which is of great medical and social importance. Doctors-internists and gastroenterologists most often carry out the selection drug treatment abdominal pain in IBS. In this regard, a systematic review and meta-analysis by A.C. Ford, N.J. Talley, B.M. Spiegel et al. ...
IBS is characterized by abdominal pain and discomfort and is associated with changes in stool pattern and frequency. According to epidemiological studies, the incidence of IBS in the population ranges from 5 to 20%. The true cause of IBS remains unclear, although a number of pathological mechanisms have been suggested. Impaired gastrointestinal motility leads to a change in the nature and frequency of stools in some patients. Smooth muscle spasm, visceral hypersensitivity, and central pain perception underlie the most important symptom of IBS, abdominal pain.
There is no doubt that IBS is a chronic condition that is prone to recurrence, which requires effective, simple and safe treatments. Some drugs that have a well-defined mechanism of action to normalize motility in IBS have been banned because of their serious side effects. Traditionally, IBS patients have been advised to increase their intake of dietary fiber, which is believed to have a beneficial effect on intestinal transit time. Various antispasmodics are used to relieve pain and a feeling of fullness in the abdomen. Peppermint oil, according to a number of studies, also has antispasmodic effects and serves as an over-the-counter remedy for IBS.
Data clinical research on the effectiveness of treatment of IBS, as a rule, contradictory, it is difficult to objectively assess the superiority of one of the compared treatment methods. The findings of the systematic reviews were also mixed. Various approaches underlie the recommendations for the treatment of IBS patients.
A.C. Ford, N.J. Talley, B.M. Spiegel et al. undertook a literature review of Medline (1950 to April 2008) and Embase (1980 to April 2008), Cochrane Controlled Trials Registry (2007): Studies in adult IBS patients compared fiber, antispasmodics, and peppermint oil with placebo or no treatment.
The purpose of this systematic review is to determine the effectiveness of fiber, antispasmodics, and peppermint oil in treating IBS. Out of 615 literature sources, 35 controlled studies were selected for analysis: 9 of them - assessing the effectiveness of fiber, 19 - antispasmodics, 3 - fiber and antispasmodics, 4 - peppermint oil.
The primary outcome of the systematic review is the efficacy of fiber, antispasmodics, and peppermint oil versus placebo or no treatment in treating the underlying symptoms of IBS or abdominal pain after treatment. The duration of the course of treatment was from 4 weeks with the appointment of fiber. up to 4 months, antispasmodics - from 1 week. up to 6 months, peppermint oil - from 4 weeks. up to 3 months The secondary result is the determination of effectiveness depending on the type of fiber or antispasmodic drug and the safety of therapy. Treatment effect was expressed as a relative risk, with a 95% confidence interval estimate of the main symptoms of IBS or abdominal pain persisting with fiber, antispasmodics, and peppermint oil.
In 12 studies involving 591 patients, 155 (52%) of 300 people who received fiber remained symptomatic after treatment, compared with 168 patients (57%) of 291 people who received a placebo or a low-fiber diet. Thus, the relative risk of persisting symptoms was 0.87 (95% CI 0.76-1.00, p \u003d 0.05), the number of patients who needed to be treated (with fiber to prevent persistence of symptoms) reached 11 (95% CI 5-100). It is important to note that in a separate analysis of the effectiveness of such a source of fiber as bran, it was not possible to prove their effectiveness (relative risk was 1.02; 95% CI 0.82-1.27), in contrast to psyllium preparations as a source of fiber (0 , 78; 95% CI 0.63-0.96).
In an analysis of 4 studies (392 patients), 52 patients (26%) of 197 remained symptomatic, compared with 127 (65%) of 195 patients who received placebo. The relative risk of persisting symptoms with peppermint oil treatment was 0.43 (95% CI 0.32-0.59).
Of greatest interest is that part of the meta-analysis by A.C. Ford, N.J. Talley, B.M. Spiegel et al., Which evaluates the role of antispasmodic drugs in the treatment of IBS. A total of 22 studies of 12 different antispasmodic drugs were analyzed, which included 1778 patients. Of the drugs with antispasmodic properties currently available to domestic doctors, this review includes studies of otylonia, hyoscine butylbromide, pinaverium, trimebutin, alverin, and mebeverin.
Overall, 350 (39%) of 905 patients receiving antispasmodics retained symptoms of IBS compared with 485 (56%) of 873 in the placebo group: the relative risk was 0.68 (95% CI 0.57-0.81) ... The number of patients who need to be treated to prevent persistence of IBS symptoms was 5 (95% CI 4-9).
When analyzing specific antispasmodic drugs, the best indicators of effectiveness were found in otylonia and hyoscine. In 4 studies of otylonia (435 patients), symptoms of IBS persisted in 111 (51%) of 216 patients who received an antispasmodic, compared with 155 (71%) of 219 with placebo: the relative risk was 0.55 (95% CI 0, 31-0.97), and the number of patients required for treatment was 4.5 (3.0-10.0). In 3 studies (426 patients) with the use of hyoscine, persistence of IBS symptoms was detected in 63 (29%) of 215 patients compared to 97 (46%) of 211 who received placebo. The relative risk of persistence of IBS symptoms was calculated as 0.63 (95% CI 0.51-0.78). It is with the use of hyoscine butyl bromide that the most low rate the number of patients who need to be treated to prevent persistence of symptoms in 1 patient is 3.5 (2.0-25.0).
Some characteristics of the studies of hyoscine butyl bromide are presented in Table 1. The total number of patients in 3 studies exceeded 400, and in each of them hyoscine butyl bromide was significantly more effective than placebo. It should be noted that in 1 study the duration of hyoscine administration was 1 month, and in 2 others - 3 months, which indicates a good tolerability of the drug. According to the recommendations of the authors of the systematic review, it makes sense for a general practitioner planning to treat IBS with antispasmodics to start with hyoscine butylbromide as a first-line therapy, with other antispasmodics in mind only if such treatment fails.
We analyzed 3 studies using trimebutin (140 patients). In 28 patients (40%) out of 70 who used trimebutin, the main symptoms of IBS and abdominal pain remained, compared with 27 (39%) out of 70 patients on placebo. The calculated relative risk was 1.08 (95% CI 0.72-1.61), which did not confirm the effectiveness of trimebutine in the treatment of the main symptoms of IBS.
According to the data of 13 studies (1379 patients), conclusions were drawn about adverse events while taking antispasmodics. Only 101 patients (14%) out of 704 noted adverse events when taking antispasmodics compared with 62 (9%) of 675 patients in the placebo group. None of the papers reported serious adverse events. The most common were dry mouth, dizziness, blurred vision. The relative risk of developing adverse events was 1.62 (95% CI 1.05-2.50), the number of patients who could be harmed was 17.5 (7.0-217.0).
Thus, hyoscine butyl bromide has a dual effect - antispasmodic and antisecretory. Demonstrated its effectiveness in spastic abdominal pain, biliary colic, esophageal spasms, IBS. Its effect has been proven "outside the digestive tract" - in renal colic, dysmenorrhea, childbirth. Hyoscine butyl bromide improves the quality of diagnostic tests such as magnetic resonance imaging and relieves pain and spasm during colonoscopy and sigmoidoscopy.
The abstract was prepared by Ph.D. ON. Lyutov 1 Moscow State Medical University named after I.M. Sechenov
Literature
1. Americo M.F., Miranda J.R., Cora L.A. ,. Romeiro F.G. Electrical and mechanical effects of hyoscine butylbromide on the human stomach: a non-invasive approach // Physiol Meas. 2009. Vol. 30 (4). R. 363-370.
2. Mueller-Lissner S., Tytgat G.N., Paulo L.G. et al. Placebo- and paracetamol controlled study on the efficacy and tolerability of hyoscine butylbromide in the treatment of patients with recurrent crampy abdominal pain // Aliment Pharmacol Ther. 2006. Vol. 23 (12). R. 1741-1718.
3. Tytgat G.N. Hyoscine butylbromide: a review of its use in the treatment of abdominal cramping and pain // Drugs. 2007. Vol. 67 (9). R. 1343-1357.
4. Tytgat G.N. Hyoscine butylbromide - a review on its parenteral use in acute abdominal spasm and as an aid in abdominal diagnostic and therapeutic procedures // Curr Med Res Opin. 2008.
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Hyoscine butyl bromide (synonyms butylscopolamine, hyoscine-N-butyl bromide; English butylscopolamine, lat. hyoscine butylbromide) — medicinal product, M-anticholinergic, antispasmodic, used in gastroenterology to relieve pain and discomfort in the abdomen.
Hyoscine butyl bromide is a chemical compound
-9-Butyl-7- (3-hydroxy-1-oxo-2-phenylpropoxy) -9-methyl-3-oxa-9-azonium-tricyclononane bromide. Empirical formula C 21 H 30 BrNO 4. Hyoscine butyl bromide is a semi-synthetic derivative of hyoscyamine - an alkaloid contained in belladonna (belladonna), henbane, dope, scopolia. It has the form of a white crystalline powder, easily soluble in water, soluble in alcohol. The molecular weight of hyoscine butyl bromide is 440.38.
Hyoscine butyl bromide - international non-proprietary name drug
Hyoscine butyl bromide is a semi-synthetic peripheral neurotropic antispasmodic (Minushkin O.N. et al.).Hyoscine butyl bromide has a pronounced antispasmodic effect on M-cholinergic receptors of smooth muscles, does not pass through the blood-brain barrier and does not central action... Not addictive.
At the same time, it was found that with a single admission, hyoscine butyl bromide has the greatest antispasmodic activity in a short period of time. This is most likely due to its double antispasmodic effect by selective binding to muscarinic receptors located on the smooth muscles of the gastrointestinal tract, and by a parallel ganglion blocking action, which causes a rapid onset of the clinical effect (Belousova L.N. et al.):
Decrease in the power level (in% compared to the initial level) in various parts of the gastrointestinal tract on an empty stomach after a single dose of an antispasmodic drug. It is seen that butyl bromide hyoscine acts more efficiently
The use of hyoscine butylbromide in pregnant and lactating mothers
Hyoscine butylbromide is not recommended for pregnant women, women planning to become pregnant, and breastfeeding mothers. Professional medical publications concerning the use of hyoscine butyl bromide in the therapy of the gastrointestinal tract
- Belousova L.N., Baryshnikova N.V., Zhuravleva M.S. and other Comparative characteristics of antispasmodic drugs according to peripheral electrogastroenterography // Farmateka. - 2012. - No. 13.
- Minushkin O. N., Maslovsky L. V. Diagnostics and treatment of functional disorders of the biliary tract // BC. Gastroenterology. - 2010. - Volume 18. - No. 4.
general information
Trade names of drugs with active ingredient hyoscine butyl bromide, registered in the countries of the former USSR: Hyoscin, Spazmobru, Spanil and others.Hyoscine butylbromide has contraindications, side effects and application features, consultation with a specialist is required.