The active substance of hyoscyamine butylbromide preparations buscopan, hyoscine and spanil, instructions for use. Medicinal reference book geotar


For citation: The value of hyoscine butylbromide in treatment abdominal pain// RMJ. 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 significance of hyoscine butylbromide in the treatment of abdominal spastic pain by stating that abdominal pain is one of the most frequent occasions to apply for medical care after headache, 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. Establishment correct diagnosis when interpreting abdominal pain can be very difficult, as it hides various diseases, which is the task of doctors general practice, surgeons, internists, specialists emergency care, pediatricians, gastroenterologists, urologists, gynecologists.
Hyoscine butyl bromide (or scopalamine-N-butyl bromide, N-butylscopolammonium bromide and butylscopolamine) according to the mechanism of its therapeutic effect is a neurotropic antispasmodic.
Acetylcholine (ACCh) is 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 nicotinic receptors on postganglionic neurons. The postganglionic neuron then releases ACh to excite the target organ's muscarinic receptors. 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 are of greatest interest. blood vessels, bronchi and gastrointestinal tract (GIT), as well as various glands respiratory system and gastrointestinal tract. Stimulation of these receptors leads to mediated vasodilation (due to the formation of nitric oxide), bronchoconstriction, increased gastrointestinal motility, and increased secretion of glands. 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 butylbromide 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 an antisecretory effect is realized, which is manifested by a decrease in the secretion of the digestive glands. The action of Buscopan is implemented on the entire gastrointestinal tract, including its upper and lower divisions. Therefore, it is prescribed for spasm that occurs in various departments Gastrointestinal tract, with biliary colic, cystitis, urethritis and primary dysmenorrhea. Hyoscine butylbromide is used to prevent spasms of the gastrointestinal tract before diagnostic studies (X-ray, endoscopic retrograde cholangiopancreatography, colonoscopy).
Hyoscine butyl bromide is a quaternary ammonium compound, its molecule is polarized and retains its polarity regardless of the pH of the medium. In this regard, when oral administration there is a slight absorption of the drug (8%), and systemic bioavailability is less than 1%. In spite of low levels in the blood, 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 plasma protein binding.
L.A. Samuels presents short review 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
The basis of the appointment of hyoscine butylbromide for nonspecific colicky abdominal pain is its antimuscarinic effect. 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 the study of the electrical and biomechanical activity of the stomach: intravenous administration of 20 mg of hyoscine butylbromide led to a decrease in the mechanical motor index by 50.9%, and the electrical motor index decreased by 36.5%.
Efficacy and safety of hyoscine butylbromide at a dose of 10 mg 3 times a day. compared with paracetamol 500 mg 3 times a day, their combination and placebo have been studied in recurrent spastic abdominal pain. 1637 patients (after placebo for 1 week) were randomized into 4 groups depending on the treatment, the duration of which was 3 weeks. Pain severity (according to visual analog scale (VAS) and verbal rating scale) was statistically significantly reduced in all treatment groups compared to placebo. The treatment was well tolerated in all groups, the frequency side effects between groups (including placebo) did not differ significantly.
G.N. Tytgat has published reviews of the literature regarding oral and parenteral use of hyoscine butylbromide for the treatment of crampy abdominal pain and other clinical indications. The first of these analyzed 10 placebo-controlled studies that examined the efficacy and safety of oral and rectal administration of hyoscine. The effectiveness of the drug is 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 presents data on the use of GBB for the treatment of colic/spasm; to improve the conduct of diagnostic studies; at parenteral administration for the treatment of biliary and renal colic, spasms of the genitourinary tract; as well as in childbirth and as palliative care. The author came to the conclusion that hyoscine butylbromide has quick action and is highly effective with good tolerability, which supports its use in a number of indications associated with acute abdominal cramps, during childbirth for palliative care, as well as in diagnostic and medical procedures in abdominal cavity, which can be difficult with spastic contractions.
The effect of hyoscine butylbromide was also studied in abdominal pain caused by a functional disorder. Conducted double-blind randomized comparative study in parallel groups, which included 712 patients with IBS. Patients within 4 weeks. hyoscine butyl bromide + paracetamol, hyoscine butyl bromide, paracetamol or placebo were prescribed. 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 butylbromide group compared with placebo and paracetamol.
Renal colic
L.A. Samuels cites 6 studies involving 755 patients evaluating hyoscine butylbromide as an additional pain reliever (along with morphine and indomethacin) versus placebo, non-steroidal anti-inflammatory drugs (NSAIDs), and other antispasmodics. It was concluded that hyoscine butylbromide is effective in the treatment of renal colic as independent remedy or in combination with opioids and NSAIDs. It should be noted that the speed of onset and the duration of the analgesic effect are better when prescribing NSAIDs.
Dysmenorrhea
L.A. Samuels reviews 2 studies using hyoscine butyl bromide in 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, as well as with placebo. Both treatment groups showed a significant reduction in subjective pain score compared to placebo. A long-term, open-label study examined the combined use of lysine clonixinate and hyoscine butylbromide during 3 consecutive menstrual cycles in 30 women. 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
Some authors have studied the effect of hyoscine butylbromide as a means of accelerating labor, citing the fact that if pain in labor cannot be eliminated in a safe way, then it is possible to safely reduce the duration of labor (and therefore labor pain). The use of hyoscine butylbromide led to a statistically and clinically significant decrease in the period between drug administration and delivery in the absence of significant adverse reactions from the mother or the newborn.
Abdominal pain and discomfort during diagnostic tests
procedures
In 3 studies, the efficacy of hyoscine butylbromide versus placebo (2 studies; 208 patients) and glucagon (1 study; 100 patients) was evaluated by sigmoidoscopy and/or colonoscopy. When compared with placebo, a reduction in the duration of the procedure was proven in the group treated with hyoscine butyl bromide. Comparison with glucagon was in favor of the latter for facilitating the endoscopic procedure.
There is evidence that intramuscular injection hyoscine butylbromide improves image quality in magnetic resonance imaging of the abdomen. It has been found that magnetic resonance imaging of the liver and pancreas is somewhat better with a decrease in gastrointestinal peristalsis hyoscine butyl bromide.
IBS is one of the functional disorders of the gastrointestinal tract, which has a huge medical and social significance. Internists and gastroenterologists most often select drug treatment abdominal pain in IBS. In this regard, a systematic review and meta-analysis of 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 the nature and frequency of stools. According to epidemiological studies, the frequency of IBS in the population ranges from 5 to 20%. True reason IBS remains undetermined, although a number of pathological mechanisms have been suggested. Impaired motility of the gastrointestinal tract leads to a change in the nature and frequency of stools in some patients. Smooth muscle spasm, visceral hypersensitivity, and features of central pain perception underlie major symptom IBS - abdominal pain.
There is no doubt that IBS is chronic condition, which is prone to recurrence, which requires effective, simple and safe ways treatment. Some drugs that have a well-defined mechanism of action to normalize motor function in IBS have been banned because of their serious side effects. Traditionally, patients with IBS are advised to increase their intake dietary fiber, which are 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 has also been shown to have an antispasmodic effect and is an over-the-counter treatment for IBS, according to a number of studies.
Data clinical research on the effectiveness of the treatment of IBS, as a rule, are contradictory, it is difficult to objectively assess the superiority of one of the compared methods of treatment. The findings of systematic reviews have also been mixed. Various approaches underlie recommendations for the treatment of patients with IBS.
A.C. Ford, N.J. Talley, B.M. Spiegel et al. undertook an evaluation of literature data from 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 mint oil with placebo or no treatment.
The aim of the systematic review is 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 - to assess the effectiveness of fiber, 19 - antispasmodics, 3 - fiber and antispasmodics, 4 - mint oil.
The primary outcome of the systematic review is an assessment of the effectiveness of fiber, antispasmodics, and peppermint oil versus placebo or no treatment in reversing 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, mint oil - from 4 weeks. up to 3 months The secondary result is the determination of the effectiveness depending on the type of fiber or antispasmodic drug and the safety of therapy. The treatment effect was expressed as a relative risk with an estimate of 95 percent confidence interval the main symptoms of IBS or abdominal pain that persist with treatment with fiber, antispasmodics, and peppermint oil.
In 12 studies including 591 patients, 155 (52%) of 300 people who received fiber remained symptomatic after treatment compared with 168 (57%) of 291 people who received placebo or a diet with low content fiber. Thus, the relative risk of persisting 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 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 of A.C. Ford, N.J. Talley, B.M. Spiegel et al., which is devoted to assessing the role 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 currently available to domestic doctors with antispasmodic properties this review included studies on otilonium, hyoscine butylbromide, pinaverium, trimebutine, alverine, and mebeverine.
Overall, 350 (39%) of 905 patients treated with antispasmodics had 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 who needed to be treated to prevent persistence of IBS symptoms was 5 (95% CI 4-9).
When analyzing specific antispasmodic drugs best performance effectiveness were found in otilonium and hyoscine. In 4 studies of otilonium (435 patients), IBS symptoms persisted in 111 (51%) of 216 patients treated with an antispasmodic compared with 155 (71%) of 219 treated with placebo: the 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), 63 (29%) of 215 patients treated with hyoscine experienced persistence of IBS symptoms compared to 97 (46%) of 211 treated with 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 butylbromide that the most low rate the number of patients who need to be treated to prevent the persistence of symptoms in 1 patient is 3.5 (2.0-25.0).
Some characteristics of hyoscine butyl bromide studies are presented in Table 1. Total number patients in 3 studies exceeded 400, and in each of them hyoscine butylbromide 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. As recommended by the authors of the systematic review, it makes sense for a general practitioner who plans to treat IBS with antispasmodics to start with hyoscine butylbromide as first-line therapy, with other antispasmodics in mind only if such treatment fails.
Three studies were analyzed using trimebutine (140 patients). In 28 patients (40%) of 70 treated with trimebutine, the main symptoms of IBS and abdominal pain remained, compared with 27 (39%) of 70 patients treated with 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 13 studies (1379 patients), conclusions were drawn about adverse events while taking antispasmodics. A total of 101 patients (14%) of 704 reported adverse events with antispasmodics compared with 62 (9%) of 675 patients in the placebo group. None of the studies reported serious adverse events. The most common were dry mouth, dizziness, blurred vision. Relative risk of development 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 double effect - antispasmodic and antisecretory. Demonstrated its effectiveness in spastic abdominal pain, biliary colic, esophageal spasms, IBS. Its effect is proven "outside the gastrointestinal tract" - with renal colic, dysmenorrhea, childbirth. Hyoscine butylbromide improves the quality of such a diagnostic study 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.


Included in medications

ATH:

A.03.B.B.01 Hyoscine butyl bromide

Pharmacodynamics:

It blocks m-cholinergic receptors, reducing the stimulating effect of acetylcholine: it reduces the secretion of the lacrimal, bronchial, sweat, gastric glands, as well as the exocrine activity of the pancreas. How an antispasmodic reduces tone bile ducts and gallbladder, gastrointestinal tract, at the same time increases the tone of the sphincters. Improves atrioventricular conduction, causes tachycardia. Makes it harder to churn intraocular fluid, increases intraocular pressure, provokes accommodation paralysis.

Pharmacokinetics:

After oral administration on an empty stomach, up to 8% is absorbed in gastrointestinal tract. The maximum plasma concentration is reached after 2 hours, after 5 minutes - after intravenous administration. Communication with plasma proteins is 4.4%.

Metabolism in the liver.

The half-life is 6 hours. Elimination with faeces and kidneys.

Indications:

Used to treat stomach ulcers and duodenum. It is used for cholelithiasis, biliary and renal colic, spasm of smooth muscles of the gastrointestinal tract, acute pancreatitis, dysmenorrhea, hemorrhoids and fissure anus.

XI.K20-K31.K25 Gastric ulcer

XI.K20-K31.K26 Duodenal ulcer

XI.K20-K31.K31.3 Pylorospasm, not elsewhere classified

XI.K80-K87.K80 Cholelithiasis[cholelithiasis]

XI.K80-K87.K81.0 Acute cholecystitis

XI.K80-K87.K81.1 Chronic cholecystitis

XI.K80-K87.K82.8 Other specified diseases of the gallbladder

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 Fissure of anus, unspecified

XI.K94.K94* Diagnosis of diseases of the gastrointestinal tract

XIV.N80-N98.N94.6 Dysmenorrhea, unspecified

Contraindications:

Keratoconus, synechia of the iris, angle-closure and open-angle glaucoma, individual intolerance.

Carefully:

Ischemic heart disease, polyneuropathy, hypertonic disease, diaphragmatic hernia, hypersensitivity.

Pregnancy and lactation:

FDA Guidelines - category C. It is used with caution during pregnancy and lactation in cases where the intended benefit outweighs the risk to the fetus and newborn. At long-term use suppresses lactation.

Dosage and administration:

Use in children

Intravenously, slowly emergency indications: 0.3-0.6 mg/kg up to 12 years of age. Maximum daily dose is 1.5 mg/kg of body weight.

From 12 years: intravenously slowly, intramuscularly or subcutaneously, 20-40 mg (1-2 ampoules).

inside in children from 6 years of age, adult doses are used.

adults

Inside, 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.

Higher 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, accommodation paralysis, photophobia.

urinary system : urinary retention.

Allergic reactions.

Overdose:

Motor and speech excitation, blurred vision, drowsiness, unsteady gait, hallucinations, depression of the respiratory center.

Treatment. The introduction 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 at 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.

With simultaneous use with phenylephrine, arterial hypertension may develop.

Lowers the concentration of levodopa in blood plasma, reduces or eliminates the effect anticholinesterase agents and m-cholinomimetics. Simultaneous use with atropine enhances side effects.

Special instructions:

The use of the drug in conditions elevated temperature air can cause heat stroke.

Instructions

the basis of all medicines is a specific active ingredient. In addition to it, the composition of the drug includes additional compounds. They may have little or no effect. Today's article will tell you about what hyoscine butyl bromide is. You will learn about the method of its use and get acquainted with the preparations containing it.

General description of the active substance and its form of release

Hyoscine butylbromide belongs to the M-anticholinergics. It is in the form of a crystalline white powder. It is in this form that this substance is part of some drugs. The drug is able to have an antispasmodic effect on smooth muscle human body. It also has atropine-like effects (dilates pupils, speeds up the pulse, relaxes the muscles of the bronchi, uterus, Bladder slows down intestinal peristalsis).

Hyoscine butylbromide is available in the form of dragee tablets, as well as rectal suppositories. Less commonly, you can find a medication in the form of a solution for injection.

Hyoscine butyl bromide: trade name

As you already know, the described substance is active in some preparations. The most popular is Buscopan. The tablets contain the main component in the amount of 10 mg. Rectal suppositories are also popular. They contain 10 mg of a substance such as hyoscine butyl bromide. "Buscopan" is sold without a prescription and has a cost of 350 to 450 rubles.

Another medicine created on the basis of the described component is Neoskapan. It is less popular than the previous one. More often this tool is used for inpatient treatment in medical institutions. The drug is in the form of a solution for injection. It is administered intravenously or intramuscularly. One ampoule contains 20 mg active substance.

"Buscopan", "Neoscapan" and hyoscine butyl bromide are analogues in their composition and action.

Indications and contraindications: information from the annotation

The medicine is prescribed to patients suffering from the following pathologies:

  • spasms of the gastrointestinal tract;
  • renal, biliary and hepatic colic;
  • spasm of the genitourinary tract;
  • peptic ulcer stomach in the acute stage;
  • algomenorrhea and so on.

The drug is used to prepare patients for diagnostic and surgical interventions. It is included in the list of medicines used in premedication (to prepare for anesthesia).

It is forbidden to use hyoscine butylbromide on its own. An appointment for its use must be obtained from a doctor. You should also pay attention to contraindications before taking the medicine. These include the following states:

  • hypersensitivity and the possibility of allergies to components;
  • intestinal obstruction or suspicion of it;
  • adenoma prostate;
  • obstruction of the urinary tract;
  • tachycardia or arrhythmia;
  • diseases of the heart and blood vessels, manifested by depression or difficulty in breathing;
  • atherosclerosis of cerebral vessels.

The medication should not be used during pregnancy. But if necessary, the doctor can give such a recommendation. If therapy is required during lactation, then it is worth deciding on the temporary or complete cessation of breastfeeding.

Hyoscine butylbromide: instructions for use

The method of using the drug directly depends on its form of release. For outpatient treatment usually prescribe tablets and suppositories. In a hospital setting, the priority is the use of a solution for injection.

Adult patients and children from 6 years of age are prescribed from 30 to 100 mg of the active substance in the form of tablets. This portion should be divided into several doses. For one application, no more than 1 tablet should be consumed. Rectal suppositories administered 3 times a day, 1-2 suppositories. The maximum daily dose of the drug in this form is 60 mg.

In the form of injections and children under 6 years of age, the substance hyoscine butyl bromide is not recommended for use. In these situations, the medicine is taken in accordance with the doses prescribed by the doctor, and only on individual recommendations.

Finally

Antispasmodics are widely used in surgery, gynecology, urology, proctology and other branches of medicine. Prescribed drugs should be used in accordance with the instructions and recommendations of the doctor. If adverse reactions are detected, stop taking and consult a doctor. Hyoscine butylbromide has side effects in the form of drowsiness, tachycardia, irritability, dry mucous membranes, indigestion, and so on. Also during therapy may worsen chronic diseases. Take care of your health and stay healthy!

Structural formula

Russian name

Latin name of the substance Hyoscine butylbromide

Hyoscini butylbromidum ( genus. Hyoscini butylbromidi)

chemical name

9-Butyl-7-(3-hydroxy-1-oxo-2-phenylpropoxy)-9-methyl-3-oxa-9-azonium tricyclononane bromide

Gross formula

C 21 H 30 BrNO 4

Pharmacological group of the substance Hyoscine butylbromide

Nosological classification (ICD-10)

CAS code

149-64-4

Characteristics of the substance Hyoscine butylbromide

Semi-synthetic derivative of hyoscyamine, an alkaloid found in belladonna, henbane, dope, scopolia; quaternary ammonium compound. White crystalline powder, easily soluble in water, soluble in alcohol. Molecular weight - 440.38.

Pharmacology

pharmachologic effect- antispasmodic, m-anticholinergic.

Blocks m-cholinergic receptors. Causes atropine-like effects: dilated pupils, accommodation paralysis, increased intraocular pressure, increase in heart rate, acceleration of sinoatrial and AV conduction, stimulates the automatism of the sinus node and functional activity 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.

Application of the substance Hyoscine butylbromide

Spastic conditions of the gastrointestinal tract, biliary and genitourinary tract (renal colic, biliary colic, cholecystitis, intestinal colic, pylorospasm), spastic dyskinesia of the biliary tract and gallbladder, peptic ulcer of the stomach and duodenum in the acute phase (as part of complex therapy), algomenorrhea, endoscopic and functional diagnostic tests digestive organs (to relax smooth muscles).

Contraindications

Hypersensitivity (including to other belladonna alkaloids), angle-closure glaucoma, myasthenia gravis, megacolon, childhood up to 6 years old.

Application restrictions

Suspicion of intestinal obstruction(including pyloric stenosis), obstruction of the urinary tract (including prostate adenoma), a tendency to tachyarrhythmias (including tachyarrhythmia atrial fibrillation).

Use during pregnancy and lactation

Perhaps if the expected effect of therapy outweighs the potential risk to the fetus or child.

Side effects of the substance Hyoscine butylbromide

From the nervous system and sensory organs: drowsiness, amnesia, disturbance of accommodation, increased eye sensitivity to light, exacerbation of glaucoma.

From the digestive tract: dryness of the mucous membrane of the oral cavity and pharynx, constipation, nausea and vomiting.

Allergic reactions: skin manifestations, anaphylaxis with episodes of difficulty breathing.

Others: dryness 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, other m-anticholinergics (including ipratropium bromide, tiotropium bromide). Joint application hyoscine butylbromide and dopamine antagonists (for example, metoclopramide) leads to a weakening of the effect on the gastrointestinal tract of both drugs. Hyoscine butylbromide increases the risk of beta-adrenergic 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 CNS depression, respiratory arrest, intestinal and bladder paresis.

Treatment: gastric lavage with activated carbon and then with 15% magnesium sulfate, forced diuresis, repeated injections physostigmine (every 0.5-1 hour) or galanthamine (every 1-2 hours), to eliminate intestinal paresis and tachycardia, it is possible to administer neostigmine methyl sulfate, with moderate arousal and not severe convulsions- magnesium sulfate; in severe cases - sodium oxybate, oxygen therapy, mechanical ventilation; with difficulty urinating - catheterization of the bladder. Patients with glaucoma - instillation of pilocarpine, if necessary, systemic administration of cholinomimetics is possible.

Substance Precautions Hyoscine Butyl Bromide

It is necessary to take into account significant differences in individual sensitivity to hyoscine, incl. the possibility of arousal, hallucinations when taking normal doses in individual patients. The risk of side effects increases with age. It is forbidden to take alcohol during treatment. Avoid overheating when performing intense physical activity and in hot weather, as well as hot baths and saunas. During therapy, it is not recommended to drive vehicles and other activities that require increased speed reactions. Can be used to relieve dry mouth chewing gum no sugar, small pieces of ice, saliva substitutes. It should be borne in mind that dry mouth that persists for more than 2 weeks increases the risk of developing diseases of tooth enamel, gums, and fungal infections of the oral cavity. Cancellation of the drug should be carried out gradually (with rapid cancellation, nausea, sweating, dizziness may occur).

Description

Detailed description

Pharmacotherapeutic group: m-Cholinolytics Nosological classification (ICD-10): K25 Gastric ulcer K26 Duodenal ulcer K31.3 Pylorospasm, not elsewhere classified K59.8.1* Intestinal dyskinesia K81 Cholecystitis K82.8.0* Gallbladder dyskinesia and biliary tract K94* Diagnosis of diseases of the gastrointestinal tract N23 Renal colic, unspecified N94.6 Dysmenorrhea, unspecified R10.4 Other and unspecified abdominal pain

Detailed description

pharmachologic effect

Blocks m-cholinergic receptors. Causes atropine-like effects: dilated pupils, accommodation paralysis, increased intraocular pressure, increased heart rate, accelerated 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.

Contraindications

Hypersensitivity (including to other belladonna alkaloids), angle-closure glaucoma, myasthenia gravis, megacolon, children under 6 years of age.

Use during pregnancy and lactation

Perhaps if the expected effect of therapy outweighs the potential risk to the fetus or child.

Side effects

From the nervous system and sensory organs: drowsiness, amnesia, disturbance of accommodation, increased eye sensitivity to light, exacerbation of glaucoma.

From the digestive tract: dryness of the mucous membrane of the oral cavity 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.

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 butylbromide and dopamine antagonists (for example, metoclopramide) leads to a weakening of the effect on the gastrointestinal tract of both drugs. Hyoscine butylbromide increases the risk of beta-adrenergic 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 CNS depression, respiratory arrest, intestinal and bladder paresis.

Treatment: gastric lavage with activated charcoal and then with 15% magnesium sulfate, forced diuresis, repeated injections of physostigmine (every 0.5–1 h) or galanthamine (every 1–2 h), neostigmine methyl sulfate may be administered to eliminate intestinal paresis and tachycardia, with moderate arousal and not severe convulsions - magnesium sulfate; in severe cases - sodium oxybate, oxygen therapy, mechanical ventilation; with difficulty urinating - catheterization of the bladder. Patients with glaucoma - instillation of pilocarpine, if necessary, systemic administration of cholinomimetics is possible.

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