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, 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.

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 studies digestive organs (to relax smooth muscles).

Contraindications

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

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 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 hour) or galanthamine (every 1-2 hours), 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.

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 usual doses in individual patients. Risk side effects increases in old 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).

Hyoscine butylbromide (Hyoscine butylbromide) - instructions for use, description, pharmacological action, indications for use, dosage and method of administration, contraindications, side effects.

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. Used for cholelithiasis, biliary and renal colic, spasm smooth muscle 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 application with atropine enhances side effects.

Special instructions:

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

Instructions

Hyoscyamine butyl bromide - active substance, which is considered a plant alkaloid, representing an ammonium compound found in the following representatives of the flora: belladonna, scopolia, as well as henbane and dope. When extracted from the plant, this compound forms a crystalline powder. white color, which is easily soluble in water and alcohol.

pharmachologic effect

The active substance hyoscine butylbromide is found in some medicines ah, which have an m-anticholinergic effect, as well as some antispasmodic effects.

This plant compound blocks the so-called m-cholinergic receptors. Preparations containing this substance have atropine-like effects, which is expressed in the form of pupil dilation, accommodation paralysis joins, intraocular pressure may increase slightly, tachycardia occurs, and AV conduction increases.

It also relaxes smooth muscle fibers. digestive tract, as well as the biliary tract and urinary tract, uterus, bronchi, in addition to this, hyoscine butylbromide slows down peristaltic processes, reduces the secretory function of the sweat, salivary and mucous glands.

During internal use preparations containing this plant alkaloid in its composition, it is poorly absorbed from the digestive tract, in addition, it has low binding to plasma proteins.

Indications for use

I will list when the means, including butylbromide in the composition of hyoscine, are indicated for use:

With spastic conditions of the gastrointestinal tract, as well as the biliary tract and genitourinary, such as intestinal, biliary and renal colic, with cholecystitis;
With spastic biliary dyskinesia;
With peptic ulcer occurring directly in the acute phase;
An effective remedy for algomenorrhea (painful menstruation).

When conducting endoscopic examination digestive tract to relax the muscles.

Contraindications for use

Among the contraindications are hypersensitivity to hyoscine butylbromide, as well as to other alkaloids of belladonna, in addition, with angle-closure glaucoma, the agent is not used, as well as up to the age of six and with the so-called megacolon ( pathological increase large intestine).

Among the restrictions on the use of hyoscine butylbromide preparations, one can note the suspicion of the presence of intestinal obstruction; blockage urinary tract, including with prostate adenoma; at cardiac pathology, in particular with the so-called atrial tachyarrhythmia.

Application and dosage

Medicines containing this substance can be used orally, and they are also administered rectally, while the dosage medication selected by a qualified doctor individually.

Adults and children over the age of six are usually prescribed the drug at a dosage of 10 to 20 milligrams three to five times a day. Rectally, the drug is used in the same dose, which is equivalent to one or two suppositories up to three times a day.

Side effects

I will list what are possible side effects in response to the use of drugs containing the active substance hyoscine butylbromide: there is some drowsiness, amnesia (memory loss), accommodation disturbance, glaucoma, increased eye sensitivity to bright light, dryness of the pharynx and oral cavity is added, constipation is noted, in addition, nausea and vomiting.

Others are possible unwanted manifestations as allergic reactions dermatological nature, such as itching, rash, redness and swelling skin, anaphylactic conditions with difficulty in breathing are not excluded. In addition, there is a decrease in sweating, dry skin, as well as tachycardia.

Overdose

In case of overdose, there will be the following symptoms: dilated pupils, dry mucous membranes, lack of reaction to light, difficulty swallowing, convulsions, tachycardia, hyperthermia joins, impaired consciousness, hallucinations, CNS depression are not excluded, in addition, respiratory arrest, as well as paresis Bladder and intestines.

In this case, the patient is next treatment: first of all, the stomach should be washed, after which the patient is given activated charcoal and magnesium sulfate, forced diuresis is prescribed, physostigmine is administered every hour or galantamine.

To eliminate intestinal paresis, as well as tachycardia, the patient is prescribed neostigmine methyl sulfate, magnesium sulfate is indicated for convulsions, in addition, mechanical ventilation is effective, and so on.

Preparations containing hyoscine butylbromide

The active substance hyoscine butylbromide is found in medication Buscopan, Hyoscin, and Spaniel. Listed medications are produced by the pharmaceutical industry in the form of tablets, which are coated on top with a thin shell, in addition, there are rectal suppositories and a solution that is recommended for use for injection.

Conclusion

The use of products containing this plant alkaloid should be carried out on the recommendation qualified specialist. The patient should independently study the instructions for the use of the prescribed drug.

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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, 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.

Contraindications

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

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 side nervous system and sense 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: 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, 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 h) or galanthamine (every 1–2 h), 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.


The analogues of the drug hyoscine butylbromide are presented, in accordance with medical terminology, called "synonyms" - drugs that are interchangeable in terms of effects on the body, containing one or more of the same active substances. When choosing synonyms, consider not only their cost, but also the country of origin and the reputation of the manufacturer.

Description of the drug

Hyoscine butyl bromide- Blocker of m-cholinergic receptors. Decreases smooth muscle tone internal organs, reduces them 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 for Hyoscine butylbromide that have similar composition, so you can choose a replacement yourself, taking into account the form and dose of the medicine prescribed by the doctor. Give preference to manufacturers from the USA, Japan, Western Europe, as well as well-known companies from of Eastern Europe: Krka, Gedeon Richter, Actavis, Egis, Lek, Geksal, Teva, Zentiva.


Reviews

Below are the results of surveys of visitors to the site about the drug hyoscine butylbromide. They reflect the personal feelings of the respondents and cannot be used as official recommendation during treatment with this drug. We strongly recommend contacting a qualified medical specialist for a personalized treatment plan.

Visitor survey results

Visitor Performance Report

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Members%
Expensive1 100.0%

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Two visitors reported frequency of intake per day

How often should I take Hyoscine Butyl Bromide?
Most of the respondents most often take this drug 3 times a day. The report shows how often the other participants in the survey take this drug.
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One visitor reported a start 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 improve. Talk to your doctor about how long you need to take this medicine. The table below shows the results of the survey on the beginning of an effective action.
Members%
1 day1 100.0%

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Official instructions for use

There are contraindications! Before use, read the instructions

BUSCOPAN

Features and Benefits

Registration number:

P N014393/01
Trade proprietary name: Buscopan
PIM or grouping name: Hyoscine butyl bromide

Dosage form:

coated tablets

Compound:

1 tablet contains 10 mg hyoscine butyl bromide
Excipients: anhydrous calcium hydrogen phosphate (calcium hydrogen phosphate) 33 mg; dried corn starch 30 mg; soluble starch (hydrolyzed potato starch) 2 mg; silicon dioxide colloidal 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 sugar-coated tablets. The smell is almost imperceptible
Pharmacological group: m-anticholinergic
ATC code: A03BB01

Pharmacological properties

It has a local antispasmodic effect on the smooth muscles of the internal organs (gastrointestinal tract, biliary tract, urinary tract), reduces the secretion of the digestive glands. The local antispasmodic effect is explained by the ganglioblocking and antimuscarinic activity of the drug. Being a quaternary ammonium derivative, Hyoscine butylbromide does not penetrate the blood-brain barrier, so there is no anticholinergic effect on the central nervous system.
Pharmacokinetics
Being a quaternary ammonium derivative and having a high polarity, Hyoscine butylbromide is slightly absorbed in the gastrointestinal tract. After oral administration, the absorption of the drug is 8%. The average absolute bioavailability is less than 1%. After a single oral dose of hyoscine butylbromide at doses of 20-400 mg, mean peak plasma concentrations were reached after about 2 hours and ranged from 0.11 to 2.04 ng/mL. Hyoscine butylbromide, due to its high affinity for muscarinic and nicotinic receptors, is distributed mainly in muscle cells bodies abdominal cavity and small pelvis, as well as in the intramural ganglia of the abdominal organs. Communication with plasma proteins (albumin) is low and is 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 epithelial cells human placenta.
The terminal half-life of the drug after a single oral administration in doses 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, the excretion of the drug occurs with feces and urine. After using the drug inside: renal elimination is from 2 to 5%, elimination through the intestine - 90%. Renal excretion of hyoscine butylbromide metabolites is less than 0.1% of the dose. After taking the drug orally in doses of 100-400 mg, the average clearance values ​​are 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 can be explained by low systemic bioavailability.
Metabolites excreted in the urine bind poorly to muscarinic receptors, so they are not active and do not have pharmacological properties.

Indications for use

Renal colic, biliary colic, spastic biliary dyskinesia and gallbladder, cholecystitis, intestinal colic, pylorospasm, peptic ulcer stomach and duodenum in the acute phase (as part of complex therapy), algomenorrhea.

Contraindications

Hypersensitivity to hyoscine butylbromide or any other component of the drug. Myasthenia gravis, megacolon.
Children under 6 years old.
Pregnancy, lactation.
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 used with caution in the following clinical situations: suspicion of intestinal obstruction(including pyloric stenosis); urinary tract obstruction (including benign hyperplasia prostate), 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, decreased blood pressure, fainting or blood in the stool, you should seek immediate medical attention medical advice.
Fertility, pregnancy and lactation
Data on the use of the drug during pregnancy and the penetration of the drug and its metabolites into breast milk limited.
Studies on the effect of the drug on fertility have not been conducted.
As a precautionary measure, the use of the drug during pregnancy and lactation is not recommended.

Dosage and administration

inside.
Unless otherwise prescribed by a doctor, it is recommended next mode dosing:
Adults and children over 6 years: 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 unwanted effects may be related to the anticholinergic properties of the drug. Anticholinergic side effects are usually mild and self-limiting.
From the immune system:
Anaphylactic shock, anaphylactic reactions, dyspnoea, skin reactions(eg, urticaria, rash, erythema, pruritus) and other manifestations of hypersensitivity
From the side of the cardiovascular system:
Tachycardia
From the digestive system:
Dry mouth
From the skin and subcutaneous tissues:
Dyshidrotic eczema

The information on the page was verified by the therapist Vasilyeva E.I.

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