Medicinal reference book geotar. Active substance hyoscyamine butyl bromide of the drugs buscopan, hyoscine and spanil, instructions for use
Description
Detailed descriptionPharmacotherapeutic group: m-Cholinolytics Nosological classification (ICD-10): K25 Gastric ulcer K26 Duodenal ulcer K31.3 Pylorospasm, not classified elsewhere K59.8.1* Intestinal dyskinesia K81 Cholecystitis K82.8.0* Dyskinesia of the gallbladder and biliary tract K94 * Diagnosis of gastrointestinal diseases N23 Renal colic, unspecified N94.6 Dysmenorrhea, unspecified R10.4 Other and unspecified pain in the abdominal area
Detailed description
pharmachologic effect
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 automaticity of the sinus node and the functional activity of the AV node, relaxes the smooth muscles of the gastrointestinal tract, biliary and urinary tracts, 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.
Contraindications
Hypersensitivity (including to other belladonna alkaloids), angle-closure glaucoma, myasthenia gravis, megacolon, children under 6 years of age.
Use during pregnancy and breastfeeding
Possibly if the expected effect of therapy exceeds the potential risk to the fetus or child.
Side effects
From the nervous system and sensory organs: drowsiness, amnesia, impaired accommodation, increased eye sensitivity to light, exacerbation of glaucoma.
From the gastrointestinal tract: dryness of the mucous membrane of the mouth and pharynx, constipation, nausea and vomiting.
Allergic reactions: skin manifestations, anaphylaxis with episodes of difficulty breathing.
Others: dry skin, redness of the skin, tachycardia, difficulty urinating, decreased sweating.
Interaction
Enhances the m-anticholinergic effect of tricyclic antidepressants (including amitriptyline, clomipramine, imipramine), H 1 -antihistamines, quinidine, amantadine, disopyramide, and other m-anticholinergics (including ipratropium bromide, tiotropium bromide). The combined use of hyoscine butyl bromide and dopamine antagonists (for example, metoclopramide) leads to a weakening of the effect of both drugs on the gastrointestinal tract. Hyoscine butylbromide increases the risk of beta-adrenergic-induced tachycardia.
Overdose
Symptoms: dilated pupils and lack of reaction to light, dry mucous membranes, hoarseness, difficulty swallowing, tachycardia, hyperthermia, skin flushing, impaired consciousness, hallucinations, convulsions, followed by depression of the central nervous system, respiratory arrest, intestinal and bladder paresis.
Treatment: gastric lavage with activated charcoal and then with 15% magnesium sulfate, forced diuresis, repeated administration of physostigmine (every 0.5–1 hour) or galantamine (every 1–2 hours), to eliminate intestinal paresis and tachycardia, it is possible to administer neostigmine methyl sulfate, with moderate agitation and mild convulsions - magnesium sulfate; in severe cases - sodium oxybate, oxygen therapy, mechanical ventilation; for difficulty urinating - catheterization of the bladder. For patients with glaucoma, instillation of pilocarpine; if necessary, systemic administration of cholinomimetics is possible.
For quotation: The value of hyoscine butylbromide in the treatment of abdominal pain // RMZh. 2012. No. 35. S. 1718
Literature Review Abstract L.A. Samuels and meta-analysis by A.C. Ford et al.
L.A. Samuels (Samuels L.A. Pharmacotherapy update: Hyoscine Butylbromide in the treatment of abdominal spasms // Clinical Medicine: Therapeutics. 2009. Vol. 1. P. 647-665) begins a review of the literature on the importance of hyoscine butylbromide in the treatment of abdominal spasmodic pain, with the statement that abdominal pain is one of the most common reasons for seeking medical help after headaches, back pain and dizziness. Abdominal pain can be a symptom of both transient and self-resolving disorders, and life-threatening conditions requiring immediate medical intervention. Establishing the correct diagnosis when interpreting abdominal pain can be very difficult, since various diseases are hidden behind it, which is the task of general practitioners, surgeons, internists, emergency medicine specialists, pediatricians, gastroenterologists, urologists, and gynecologists.
Hyoscine butylbromide (or scopalamine-N-butylbromide, N-butylscopolammonium bromide and butylscopolamine) according to the mechanism of its therapeutic effect is a neurotropic antispasmodic.
Acetylcholine (ACCh) 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 releases ACh into the ganglion, and it acts on the nicotinic receptors of the postganglionic neurons. The postganglionic neuron then releases ACh to excite muscarinic receptors in the target organ. Several types of muscarinic receptors are known; from the point of view of the mechanism of action of hyoscine butyl bromide, the most interesting are the M3 receptors located in the smooth muscles of blood vessels, bronchi and the gastrointestinal tract (GIT), as well as various glands of the respiratory system and GIT. 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 muscles of the iris, where they are involved in accommodation and control pupil size. 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 smooth muscle receptors, eliminates spasm of smooth muscles of the gastrointestinal tract and genitourinary tract, and also reduces the motility of these organs. Secondly, hyoscine butylbromide is a non-competitive blocker of nicotinic receptors, due to which an antisecretory effect is realized, which is manifested by a decrease in the secretion of the digestive glands. The action of Buscopan is realized throughout the gastrointestinal tract, including its upper and lower sections. Therefore, it is prescribed for spasms that occur in various parts of the gastrointestinal tract, for biliary colic, cystitis, urethritis and primary dysmenorrhea. Hyoscine butyl bromide is used to prevent gastrointestinal spasms before diagnostic studies (X-ray, endoscopic retrograde cholangiopancreatography, colonoscopy).
Hyoscine butyl bromide is a quaternary ammonium compound; its molecule is polarized and maintains polarity regardless of the pH of the environment. In this regard, when administered orally, the drug is insignificantly absorbed (8%), and systemic bioavailability is less than 1%. Despite the low blood levels that are recorded transiently, hyoscine butyl bromide and/or its metabolites are detected 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 provides a summary of studies of hyoscine butyl bromide for abdominal colic and irritable bowel syndrome (IBS), renal colic, dysmenorrhea, as well as its potential in childbirth and diagnostic procedures.
Abdominal pain
(“nonspecific colic”) and IBS
The basis for the prescription of hyoscine butyl bromide for nonspecific colicky abdominal pain is its antimuscarinic effect. Clinically, this effect is manifested by relaxation of the smooth muscles of the gastrointestinal tract with a decrease or disappearance of the spasm felt by the patient. This effect was objectively demonstrated in a study of the electrical and biomechanical activity of the stomach: intravenous administration of 20 mg of hyoscine butyl bromide led to a decrease in the mechanical motility index by 50.9%, and an electrical motility index decreased by 36.5%.
Efficacy and safety of hyoscine butyl bromide at a dose of 10 mg 3 times a day. in comparison with paracetamol 500 mg 3 times / day, their combination and placebo were studied for recurrent crampy abdominal pain. 1637 patients (after placebo for 1 week) were randomized into 4 groups depending on treatment, which lasted 3 weeks. Pain severity (as measured by visual analogue scale (VAS) and verbal rating scale) was statistically significantly reduced in all treatment groups compared to placebo. Treatment was well tolerated in all groups, and the incidence of side effects did not differ significantly between groups (including placebo).
G.N. Tytgat has published reviews of the literature regarding the use of oral and parenteral hyoscine butyl bromide for the treatment of cramping abdominal pain and other clinical indications. The first of these analyzed 10 placebo-controlled studies that examined the effectiveness and safety of oral and rectal administration of hyoscine. The effectiveness of the drug has been established in all studies, which is considered by the authors as evidence in support of the use of the drug for abdominal pain associated with cramps.
The second review provides evidence on the use of GBB for the treatment of colic/spasm; to improve diagnostic testing; for parenteral administration for the treatment of biliary and renal colic, spasms of the genitourinary tract; as well as during childbirth and as palliative treatment. The author concluded that hyoscine butylbromide is fast-acting and highly effective and well tolerated, which supports its use in a range of indications related to acute abdominal cramps, labor and delivery for palliative care, and diagnostic and therapeutic abdominal procedures. which can be difficult with spastic contractions.
The effect of hyoscine butylbromide has also been studied for abdominal pain caused by a functional disorder. A double-blind, randomized, parallel-group comparative study was conducted, which included 712 patients with IBS. Patients for 4 weeks. hyoscine butyl bromide + paracetamol, hyoscine butyl bromide, paracetamol or placebo were prescribed. The VAS was used to assess symptoms. By the end of treatment, more than 75% of patients in the hyoscine butyl bromide group experienced symptom relief. There was a statistically significant decrease in the intensity of abdominal pain in the hyoscine butyl bromide group compared to placebo and paracetamol.
Renal colic
L.A. Samuels cites 6 studies involving 755 patients that evaluated hyoscine butyl bromide as an adjunctive pain reliever (along with morphine and indomethacin) compared with placebo, nonsteroidal anti-inflammatory drugs (NSAIDs), and other antispasmodics. It was concluded that hyoscine butylbromide 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 prescribing NSAIDs.
Dysmenorrhea
L.A. Samuels reviews 2 studies using hyoscine butyl bromide for primary and secondary dysmenorrhea. In the first double-blind crossover study of 120 women, hyoscine butylbromide and paracetamol were compared with lysine clonixinate and proprinox and placebo. Both treatment groups showed a significant reduction in subjective pain ratings compared to placebo. A long-term, open-label study examined the combined use of lysine clonixinate and hyoscine butyl bromide during 3 consecutive menstrual cycles in 30 women. Women initially reported very severe (10.7%), severe (42.9%) or moderate (46.4%) pain. By the end of the study, moderate pain persisted in only 1 patient.
Childbirth
Some authors have studied the effects of hyoscine butyl bromide as a labor accelerator, with the argument that if labor pain cannot be safely eliminated, then labor duration (and therefore labor pain) may be safely reduced. The use of hyoscine butyl bromide led to a statistically and clinically significant reduction 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 tests
procedures
In 3 studies, the effectiveness of hyoscine butylbromide compared with placebo (2 studies; 208 patients) and glucagon (1 study; 100 patients) was assessed during sigmoidoscopy and/or colonoscopy. When compared with placebo, a reduction in the duration of the procedure was proven in the group receiving hyoscine butyl bromide. Comparison with glucagon favored the latter for facilitating the endoscopic procedure.
There is evidence that intramuscular administration of hyoscine butyl bromide improves image quality in abdominal magnetic resonance imaging. Magnetic resonance imaging of the liver and pancreas was found to be slightly better when gastrointestinal motility was reduced by hyoscine butyl bromide.
IBS is one of the functional disorders of the gastrointestinal tract, which has enormous medical and social significance. Internists and gastroenterologists most often select drug treatment for abdominal pain in IBS. In this regard, the systematic review and meta-analysis of A.C. is of great interest. Ford, N.J. Talley, B.M. Spiegel et al. .
IBS is characterized by abdominal pain and discomfort and is associated with changes in bowel habits and frequency. According to epidemiological studies, the incidence of IBS in the population ranges from 5 to 20%. The exact cause of IBS remains unknown, although a number of pathological mechanisms have been proposed. Impaired gastrointestinal motility leads to changes in the nature and frequency of stool in some patients. Smooth muscle spasm, visceral hypersensitivity and features of 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 had a well-defined mechanism of action to normalize motility in IBS were banned due to their serious side effects. Traditionally, IBS patients have been advised to increase their intake of dietary fiber, which is thought to have a beneficial effect on intestinal transit time. To relieve pain and a feeling of fullness in the abdomen, various antispasmodics are used. Peppermint oil, according to several studies, also has an antispasmodic effect and is an over-the-counter remedy for IBS.
Data from clinical studies on the effectiveness of treatment for IBS are usually contradictory; it can be difficult to objectively assess the superiority of one of the compared treatment methods. The findings from systematic reviews were also mixed. Various approaches underlie recommendations for the treatment of patients with IBS.
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), the Cochrane Register of Controlled Trials (2007): studies in adult patients with IBS compared fiber, antispasmodics and peppermint oil with placebo or no treatment.
The purpose of the systematic review was to determine the effectiveness of fiber, antispasmodics, and peppermint oil in the treatment of IBS. From 615 literary 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 assessed the effectiveness of fiber, antispasmodics, and peppermint oil compared with placebo or no treatment in relieving core symptoms of IBS or abdominal pain after treatment. The duration of treatment was 4 weeks when fiber was prescribed. up to 4 months, antispasmodics - from 1 week. up to 6 months, mint oil - from 4 weeks. up to 3 months The secondary result is to determine the effectiveness depending on the type of fiber or antispasmodic drug and the safety of therapy. Treatment effect was expressed as a relative risk, with an estimate of the 95% confidence interval for core symptoms of IBS or abdominal pain persisting with fiber, antispasmodics, and peppermint oil.
In 12 studies of 591 patients, 155 (52%) of 300 people given fiber had symptoms that persisted after treatment, compared with 168 (57%) of 291 people given a placebo or low-fiber diet. Thus, the relative risk of persistent symptoms was 0.87 (95% CI 0.76-1.00, p = 0.05), the number of patients who needed to be treated (with fiber to prevent the 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 of 197 patients (26%) remained symptomatic compared with 127 (65%) of 195 placebo-treated patients. The relative risk of symptom persistence with peppermint oil was 0.43 (95% CI 0.32–0.59).
Of greatest interest is the 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 included studies of otilonium, hyoscine butyl bromide, pinaverium, trimebutine, alverine and mebeverine.
Overall, 350 (39%) of 905 patients treated with antispasmodics had persistent IBS symptoms, compared with 485 (56%) of 873 in the placebo group: relative risk was 0.68 (95% CI 0.57-0.81). . The number of patients needed to treat to prevent persistent IBS symptoms was 5 (95% CI 4-9).
When analyzing specific antispasmodic drugs, the best performance indicators were found to be otilonium and hyoscine. In 4 studies of otilonium (435 patients), IBS symptoms persisted in 111 (51%) of 216 patients receiving an antispasmodic, compared with 155 (71%) of 219 receiving placebo: relative risk was 0.55 (95% CI 0. 31-0.97), and the number of patients required for treatment is 4.5 (3.0-10.0). In 3 studies (426 patients) with hyoscine, persistence of IBS symptoms was detected in 63 (29%) of 215 patients compared with 97 (46%) of 211 receiving placebo. The relative risk of persistent IBS symptoms was calculated as 0.63 (95% CI 0.51–0.78). It was with the use of hyoscine butylbromide that the lowest indicator of the number of patients who needed to be treated to prevent the persistence of symptoms in 1 patient was obtained - 3.5 (2.0-25.0).
Some characteristics of the hyoscine butyl bromide studies 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 that the drug was well tolerated. As recommended by the authors of the systematic review, it makes sense for a general practitioner considering treatment of IBS with antispasmodics to start with hyoscine butylbromide as first-line therapy, with other antispasmodics in mind only if such treatment fails.
3 studies using trimebutine (140 patients) were analyzed. In 28 patients (40%) of 70 who used trimebutine, the main symptoms of IBS and abdominal pain persisted, compared with 27 (39%) 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 treating the main symptoms of IBS.
According to data from 13 studies (1379 patients), conclusions were drawn about adverse events while taking antispasmodics. A total of 101 patients (14%) of 704 reported adverse events when taking antispasmodics, compared with 62 (9%) of 675 patients in the placebo group. None of the studies reported serious adverse events. The most common symptoms were dry mouth, dizziness, and blurred vision. The relative risk of 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 butylbromide has a dual effect - antispasmodic and antisecretory. Demonstrated its effectiveness in spasmodic abdominal pain, biliary colic, esophageal spasms, IBS. Its effect has been proven “outside the gastrointestinal tract” - for renal colic, dysmenorrhea, and childbirth. Hyoscine butyl bromide improves the quality of diagnostic tests such as magnetic resonance imaging, and eliminates pain and spasm during colonoscopy and sigmoidoscopy.
Abstract prepared by Ph.D. ON THE. 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.
5. Schafer E., Ewe K. The treatment of irritable colon. Efficacy and tolerance of buscopan plus, buscopan, paracetamol and placebo in ambulatory patients with irritable colon // Fortschr Med. 1990. Vol. 108 (25). R. 488-492.
6. Saunders B.P., Elsby B., Boswell A.M., Atkin W., Williams C.B. Intravenous antispasmodic and patient-controlled analgesia are of benefit for screening flexible sigmoidoscopy // Gastrointest Endosc. 1995. Vol. 42(2). R. 123-127.
7. Wagner M., Klessen C., Rief M. et al. High-resolution T2-weightedabdominal magnetic resonance imaging using respiratory triggering: impact of butylscopolamine on image quality // Acta Radiol. 2008. Vol. 49(4). R. 376-382.
Analogs of the drug hyoscine butyl bromide are presented, in accordance with medical terminology, called “synonyms” - drugs that are interchangeable in their effects on the body, containing one or more identical active ingredients. When selecting synonyms, consider not only their cost, but also the country of production and the reputation of the manufacturer.
Description of the drug
Hyoscine butyl bromide- M-cholinergic receptor blocker. Reduces the tone of smooth muscles of internal organs, reduces their contractile activity. Causes a decrease in the secretion of exocrine glands. Increases heart rate. Causes mydriasis, paralysis of accommodation, increases intraocular pressure.List of analogues
Note! The list contains synonyms of Hyoscine butylbromide, which have a similar composition, so you can choose a replacement yourself, taking into account the form and dose of the medicine prescribed by your doctor. Give preference to manufacturers from the USA, Japan, Western Europe, as well as well-known companies from Eastern Europe: KRKA, Gedeon Richter, Actavis, Egis, Lek, Hexal, Teva, Zentiva.
Reviews
Below are the results of surveys of site visitors about the drug hyoscine butyl bromide. They reflect the personal feelings of the respondents and cannot be used as an official recommendation for treatment with this drug. We strongly recommend that you consult a qualified healthcare professional to determine a personalized course of treatment.Visitor survey results
Visitor Performance Report
Visitor Report of Side Effects
Information has not yet been providedTwo visitors reported cost estimates
| Participants | % | ||
|---|---|---|---|
| Dear | 2 | 100.0% | |
Two visitors reported frequency of intake per day
How often should I take Hyoscine butylbromide?Most respondents most often take this drug 3 times a day. The report shows how often other survey participants take this drug.
One visitor reported an expiration date
How long does it take to take Hyoscine butylbromide to feel an improvement in the patient’s condition?In most cases, survey participants felt an improvement in their condition after 1 day. But this may not correspond to the period after which you will begin to improve. Check with your doctor for how long you need to take this medicine. The table below shows the results of the survey on the initiation of effective action.
| Participants | % | ||
|---|---|---|---|
| 1 day | 1 | 100.0% | |
Visitor report on reception time
Information has not yet been providedEight visitors reported the patient's age
Visitor reviews
There are no reviews |
Official instructions for use
There are contraindications! Read the instructions before useBUSKOPAN
| Features and Benefits |
Registration number:
P N014393/01Trade patent name: Buscopan
MNI or group name: Hyoscine butyl bromide
Dosage form:
film-coated tabletsCompound:
1 tablet contains 10 mg hyoscine butyl bromideExcipients: calcium hydrogen phosphate anhydrous (calcium hydrogen phosphate) 33 mg; dried corn starch 30 mg; soluble starch (hydrolyzed potato starch) 2 mg; colloidal silicon dioxide 4 mg; tartaric acid 0.5 mg; stearic acid 0.5 mg.
Shell: povidone (polyvinylpyrrolidone) 0.505 mg; sucrose 41.182 mg; talc 23.671 mg; gum arabic (acacia gum) 2.761 mg; titanium dioxide 1.802 mg; macrogol 6000 (polyethylene glycol) 0.055 mg; carnauba wax 0.012 mg; white wax (white beeswax) 0.012 mg.
Description: White, round, biconvex tablets, sugar-coated. The smell is almost imperceptible
Pharmacological group: m-anticholinergic
ATX Code:А03ВВ01
Pharmacological properties
It has a local antispasmodic effect on the smooth muscles of internal organs (gastrointestinal tract, biliary tract, urinary tract), reduces the secretion of the digestive glands. The local antispasmodic effect is explained by the ganglion-blocking and antimuscarinic activity of the drug. Being a quaternary ammonium derivative, Hyoscine butyl bromide does not penetrate the blood-brain barrier, therefore there is no anticholinergic effect on the central nervous system.Pharmacokinetics
Being a quaternary ammonium derivative and having a high polarity, Hyoscine butyl bromide is slightly absorbed from the gastrointestinal tract. After oral administration, absorption of the drug is 8%. The average absolute bioavailability is less than 1%. After a single oral administration of hyoscine butyl bromide in doses of 20-400 mg, mean peak plasma concentrations were reached after approximately 2 hours and ranged from 0.11 to 2.04 ng/ml. Hyoscine butyl bromide, due to its high affinity for muscarinic and nicotinic receptors, is distributed mainly in the muscle cells of the abdominal and pelvic organs, as well as in the intramural ganglia of the abdominal organs. The connection with plasma proteins (albumin) is low and amounts to about 4.4%. It was found that the drug (at a concentration of 1 mmol) in vitro interacts with the transport of choline (1.4 nmol) in the epithelial cells of the human placenta.
The terminal half-life of the drug after a single oral dose of 100-400 mg ranged from 6.2 to 10.6 hours. Metabolism is carried out mainly by hydrolysis of the ester bond. After oral administration, excretion of the drug occurs in feces and urine. After oral administration of the drug: renal elimination is from 2 to 5%, elimination through the intestines is 90%. Renal excretion of hyoscine butyl bromide metabolites is less than 0.1% of the dose. After oral administration of the drug in doses of 100-400 mg, the average clearance values range from 881 to 1420 l/min, while the corresponding volumes of distribution for the same dose range vary from 6.13 to 11.3 x 10 5 l, which may be explained low systemic bioavailability.
Metabolites excreted in the urine weakly bind to muscarinic receptors, so they are not active and do not have pharmacological properties.
Indications for use
Renal colic, biliary colic, spastic dyskinesia of the biliary tract and gallbladder, cholecystitis, intestinal colic, pylorospasm, peptic ulcer of the stomach and duodenum in the acute phase (as part of complex therapy), algodismenorrhea.Contraindications
Hypersensitivity to hyoscine butyl bromide or any other component of the drug. Myasthenia gravis, megacolon.Children under 6 years old.
Pregnancy, lactation period.
A buscopan tablet contains 41.2 mg of sucrose. The maximum recommended daily dose (10 tablets) contains 411.8 mg of sucrose. Patients with rare hereditary disorders (fructose intolerance), such as glucose-galactose malabsorption or sucrase-isomaltase deficiency, should not take the drug.
Carefully
The drug should be prescribed with caution in the following clinical situations: suspected intestinal obstruction (including pyloric stenosis); obstruction of the urinary tract (including benign prostatic hyperplasia), tachyarrhythmias (including atrial fibrillation), angle-closure glaucoma.
In cases where abdominal pain of unknown origin continues or worsens, or when symptoms such as fever, nausea, vomiting, changes in stool consistency and frequency of bowel movements, abdominal tenderness, low blood pressure, fainting, or blood in the stool are simultaneously observed, immediate attention should be given to seek medical advice.
Fertility, pregnancy and lactation
Data on the use of the drug during pregnancy and on the penetration of the drug and its metabolites into breast milk are limited.
There have been no studies on the effect of the drug on fertility.
As a precautionary measure, use of the drug during pregnancy and lactation is not recommended.
Directions for use and doses
Inside.Unless otherwise prescribed by your doctor, the following dosage regimen is recommended:
Adults and children over 6 years of age: 1-2 tablets 3-5 times a day with water.
The drug should not be used daily for more than 3 days without consulting a doctor.
Side effects
Many of the listed undesirable effects may be associated with the anticholinergic properties of the drug. Anticholinergic side effects are usually mild and self-limiting.
From the immune system:
Anaphylactic shock, anaphylactic reactions, shortness of breath, skin reactions (eg, urticaria, rash, erythema, pruritus) and other manifestations of hypersensitivity
From the cardiovascular system:
Tachycardia
From the digestive system:
Dry mouth
For the skin and subcutaneous tissues:
Dyshidrotic eczema
The information on the page was verified by physician-therapist E.I. Vasilyeva.
Included in the preparations
ATX:A.03.B.B.01 Hyoscine butyl bromide
Pharmacodynamics:Blocks m-cholinergic receptors, reducing the stimulating effect of acetylcholine: reduces the secretion of lacrimal, bronchial, sweat, gastric glands, as well as the exocrine activity of the pancreas. As an antispasmodic, it reduces the tone of the bile ducts and gallbladder, the gastrointestinal tract, while simultaneously increasing the tone of the sphincters. Improves atrioventricular conduction, causes tachycardia. It impedes the outflow of intraocular fluid, increases intraocular pressure, and provokes paralysis of accommodation.
Pharmacokinetics:After oral administration on an empty stomach, up to 8% is absorbed in the gastrointestinal tract. The maximum concentration in blood plasma is achieved after 2 hours, 5 minutes after intravenous administration. Plasma protein binding is 4.4%.
Metabolism in the liver.
The half-life is 6 hours. Elimination in feces and kidneys.
Indications:Used to treat gastric and duodenal ulcers. Used for cholelithiasis, biliary and renal colic, spasm of smooth muscles of the gastrointestinal tract, acute pancreatitis, dysmenorrhea, hemorrhoids and anal fissure.
XI.K20-K31.K25 Stomach ulcer
XI.K20-K31.K26 Duodenal ulcer
XI.K20-K31.K31.3 Pylorospasm, not elsewhere classified
XI.K80-K87.K80 Gallstone disease [cholelithiasis]
XI.K80-K87.K81.0 Acute cholecystitis
XI.K80-K87.K81.1 Chronic cholecystitis
XI.K80-K87.K82.8 Other specified gallbladder diseases
XIV.N20-N23.N23 Renal colic, unspecified
XIV.N80-N98.N94.5 Secondary dysmenorrhea
XIV.N80-N98.N94.4 Primary dysmenorrhea
XVIII.R10-R19.R10.4 Other and unspecified abdominal pain
XI.K55-K63.K60.2 Anal fissure, unspecified
XI.K94.K94* Diagnosis of gastrointestinal diseases
XIV.N80-N98.N94.6 Dysmenorrhea, unspecified
Contraindications:Keratoconus, synechiae of the iris, closed-angle and open-angle glaucoma, individual intolerance.
Carefully:Coronary heart disease, polyneuropathy, hypertension, diaphragmatic hernia, hypersensitivity.
Pregnancy and lactation:FDA Recommendations - category C. Use with caution during pregnancy and lactation in cases where the expected benefit outweighs the risk to the fetus and newborn. With long-term use, it suppresses lactation.
Directions for use and dosage:Use in children
Intravenously slowly, for emergency indications: 0.3-0.6 mg/kg up to 12 years of age. The maximum daily dose is 1.5 mg/kg body weight.
From 12 years: intravenously slowly, intramuscularly or subcutaneously, 20-40 mg (1-2 ampoules).
Inside in children over 6 years of age, adult doses are used.
Adults
Orally, 10-20 mg 3-5 times a day.
Rectally, 1-2 suppositories (10-20 mg) 3 times a day.
Intravenously slowly, subcutaneously, intramuscularly, 20-40 mg (1-2 ampoules).
Highest daily dose: 100 mg.
Highest single dose: 40 mg.
Side effects:Central and peripheral nervous system : dizziness, drowsiness, hallucinations, impaired tactile sensitivity.
The cardiovascular system : tachycardia.
Digestive system : dry mouth, constipation.
Sense organs: mydriasis, paralysis of accommodation, photophobia.
Urinary system : urinary retention.
Allergic reactions.
Overdose:Motor and speech agitation, blurred vision, drowsiness, unsteadiness of gait, hallucinations, depression of the respiratory center.
Treatment. Administration of physostigmine (intravenously from 0.5 to 2 mg at a rate of up to 1 mg/min, not more than 5 mg per day) or neostigmine methyl sulfate (intramuscularly 1 mg every 2-3 hours, intravenously - up to 2 mg).
Interaction:Antacids containing aluminum or calcium carbonate reduce the absorption of the drug in the gastrointestinal tract. It is recommended to maintain an interval of at least 1 hour.
When used simultaneously with phenylephrine, the development of arterial hypertension is possible.
Reduces the concentration of levodopa in the blood plasma, reduces or eliminates the effect of anticholinesterase drugs and m-cholinomimetics. Concomitant use with atropine increases side effects.
Special instructions:Using the drug in conditions of elevated air temperature can cause heat stroke.
Instructions
