Hyoscine-N-ButylBromide - Uses, Indications, Contraindications, Warnings, and Side Effects

Overview

Hyoscine-N-butylbromide is an anticholinergic medication often referred to as Hyoscine butylbromide and Scopolamine butylbromide. It is chiefly used to treat pain, spasms, and cramping concerning organs involved in the digestive system. In addition, it is used as a drug therapy for irritable bowel syndrome and in a range of radiological studies.

Hyoscine butylbromide is an anticholinergic agent that does not influence the brain. The drug was designed and patented in 1950 and gained approval for its medical use in 1951. Moreover, it is incorporated in the list of essential medicines of the World Health Organization.

How Does Hyoscine-N-Butyl Bromide Work?

Hyoscine-n-butyl bromide is an anticholinergic drug that shows a high affinity towards the muscarinic receptors of the smooth muscles in the gastrointestinal tract. In other ways, Hyoscine butylbromide binds to nicotinic receptors, inducing a ganglion-blocking impact. As a result, blockade of the muscarinic receptors occurs. Therefore, it deploys a spasmolytic or relaxing action on the smooth muscles of the gastrointestinal (GI) tract, genito-urinary and biliary tracts.

Uses

• Stomach Cramps: As an antispasmodic agent, Hyoscine butylbromide is used to alleviate sharp pain and cramps in association with the stomach, intestine, and other parts of the digestive system. It is also used in relieving bladder cramps in case of kidney stones, menstrual cramps, and bowel cramps.

• Irritable Bowel Syndrome: Irritable bowel syndrome is an intestinal disorder with a combination of symptoms such as stomach pain, gas, constipation, cramping, and diarrhea. Hyoscine butylbromide is chiefly prescribed to treat these symptoms.

• Radiology Study: Under radiologic investigations, it can be used as the differential diagnosis of obstruction.

• Pyelography: Used in relieving pain during pyelography, an imaging technique of the urinary tract and system.

• To freeze the bowel motion in aspects of CT, MRI, and fluoroscopy.

• In diagnostic means like endoscopy.

Drug and Its Dosage

Route of Administration:

Oral, intramuscular, and intravenous injection.

Drug Form and Strength:

Tablet: Round, biconvex, white to off-white, 10 mg film-coated tablet.

Injection: Hyoscine butylbromide 20 mg/ml solution available for intramuscular (i.m) or intravenous (i.v) injection. It holds a clear, colorless solution free of visible particles with a pH of 3.7 to 5.5.

Drug Dosages

Medical healthcare professionals prescribe the drug form and dosage according to the patient's age and medical concerns with the severity of the condition.

Hyoscine butylbromide Tablet,

For Stomach Cramps:

• In adults- Two tablets of 10 mg are to be taken four times a day.

• In children of 12 years and above- Two 10 mg tablets four times a day.

• In children of six to 11 years- The usual recommended dose is one 10 mg tablet three times a day.

For Irritable Bowel Syndrome:

The initial recommended dosage is generally one 10 mg tablet three times daily. However, the dosage is then increased to two 10 mg tablets four times a day if required.

Note: It is not usually advised to take Hyoscine butylbromide tablets on a daily basis for a long span unless an actual investigation for stomach ache is done.

Hyoscine Butylbromide Injection,

The doctors will prescribe one Ampoule of 20 mg intramuscular or intravenous injection in the following cases. Repetition of the dose after half an hour is recommended if necessary.

• Acute spasm.

• Biliary or renal colic.

• Reduction of pain and spasm in pyelography.

• For differential diagnosis in radiography.

• Gastroduodenal endoscopy. The dosages might be frequently administered in aspects of endoscopy.

What Are the Precautions and Warnings of Hyoscine-N-Butyl Bromide?

• Pregnancy: Limited studies determine the use of Hyoscine butylbromide in the pregnancy period. However, it is not usually recommended as it might rarely result in an impaired fetal fluid sac. The medication is prescribed in terms of requisite to the mother predominantly than risks.

• Breastfeeding: The studies validating the use and its risk during breastfeeding are inadequate. Therefore, the discontinuation of either breastfeeding or the drug is advised to prevent the risks to the infant.

• In Children: Hyoscine butylbromide is intended to be used with extreme caution in children.

Specified Warnings:

• Driving and Occupational Work: Hyoscine-n-butylbromide medications are more likely to cause signs like drowsiness, tiredness, and blurred vision. So, one should have caution and not drive or do work requiring the most concentration.

• Anticoagulant Therapy: Hyoscine butylbromide intramuscular injection is not advised in individuals under anticoagulant (blood thinner) medication as a consequence of intramuscular hematoma. Intramuscular hematoma is an injury to the tissue with an accumulation of blood underneath the skin.

• Prostatic Enlargement: The medication should be used cautiously in men with prostatic enlargement since the drug influences the risk of urinary retention. So, water intake and output had better be monitored.

For Patients

When Are Stomach Cramps Serious?

People often feel uncomfortable, painful, and tight feelings in the stomach which is an obvious stomach cramp. However, the stomach cramps are not severe in most instances. But one must require medical attention if the stomach cramps persistently result in recurrences for more than a day. The pain seems to be from inside the abdomen or from the outer muscular linings, ranging from moderate to severe, with the requisite emergency care. So, the person encounters pain, stomach upset, nausea, diarrhea, fever, vomiting, and certain signs of dehydration.

What Are the Causes of Stomach Cramps?

Stomach cramps are attributable to the irritation, infection, or inflammation of the stomach and gastrointestinal tract. This can be due to a wide range of causes.

• Food poisoning.

• Stomach flu or viral gastroenteritis.

• Food intolerance.

• Food allergy.

How Hyoscine-N-Butylbromide Helps in Painful Stomach Cramps?

Hyoscine-n-butylbromide helps relieve abdominal pain, discomfort, and cramps by means of relaxing the digestive system. This is achieved by its anticholinergic action as it first binds and inhibits the muscarinic receptors in the gastrointestinal tract. Then, It diminishes the wave-like contractions of the smooth muscles and relieves the spasm of the organs involved in the digestive system.

Hyoscine-n-butyl bromide, as antispasmodic, reduces the spasm by smoothing the muscles concerning the stomach, digestive tract, intestine, urethra, and bladder. In addition to stomach cramps, it also treats bowel cramps and menstrual pain.

How to Take Hyoscine Butylbromide?

Hyoscine butylbromide exists in certain forms and dosages, though. Therefore, the doctors prescribe the drug on the basis of the severity, onset, and frequency of stomach cramps with the associated conditions. Subsequently, every individual possesses different effects of the drug. Therefore, one should take medicine as per the doctor’s advice and prescription labeled information.

Considerations Before Taking Hyoscine-N-Butylbromide:

• One should notify the doctor if one is allergic to Hyoscine-n-butylbromide or other ingredients.

• Food allergies should be informed priorly.

• Also, inform the doctor regarding the supplementary medicines, nutritional accompaniments, vitamins, and herbal supplements if taken or planned to take.

• Convey the doctor if one has other digestive system concerns like diarrhea, reflux disease, ulcerative colitis, severe constipation, enlarged bowel, or any blockage in the bowel system.

• In addition, tell the doctor in case of any general medical illnesses and diseases. Hence, certainly volunteer if one has prostate problems, fever, and high blood pressure.

• Tell the doctor if in case of myasthenia gravis, a condition of muscle weakness.

• Glaucoma and a rare form called acute angle closure glaucoma should be informed if they exist.

• Inform the doctors if in the case that one recently passed blood with the poo or pain while passing.

• Sickened feelings of nausea, vomiting or later events of food poisoning should be primed.

• Inform if one has an overactive thyroid.

• The doctor should know if one is pregnant, breastfeeding, or has any plans for pregnancy.

Directions to Take the Hyoscine-N-Butylbromide Tablet:

• One should read the manufacturer’s information leaflet of the pack as it contains precise insight.

• Hyoscine-n-butylbromide tablets are to be taken orally with or without food.

• Swallow the Hyoscine-n-butylbromide tablets with water.

• One should not crush or break the tablet. Also, do not indulge in chewing the tablet.

• Take the tablets according to the prescribed dosages. Also, take them concurrently every day.

• Do not halt or stop taking the medication unless the doctor utters it.

• Store the tablets in the cool, dry aspects away from direct heat and light.

• The medication should be stored away from the reach of children. Fill them in a safe, tight container that little ones cannot reach to safeguard them from poisoning.

• Cautions should be taken into account while driving or occupational work, as the medication can induce drowsiness.

• Drink adequate water to limit dehydration since the drug is attributable to diarrhea.

• In addition, call the doctor if there is no improvement or worsening of symptoms.

• Inform the doctor of any adverse side effects.

Directions for Hyoscine-N-ButylBromide Injection:

Doctors and other health care professionals give the Hyoscine-butylbromide injection, and strictly no one should do self-administration.

For IM

• Injection of undiluted solution into a large muscle mass.

For IV

• 20 mg/ml of solution is diluted with about 10 ml of normal saline.

• Then, it is injected gradually over three to five minutes.

• Compatible liquids are normal saline, sodium chloride, and five percent glucose.

• The solution should be stored at room temperature (below 25-degree celsius) with protection from moisture, heat, and light.

Dietetic Considerations

Drinking plenty of fluids is a must regimen to be coursed. In addition, ingesting a well-balanced nutritious diet paves the way for sound health. Avoid complex and spicy foods that are heavier on digestion. In contrast, have fruits, foods, and vegetables with stomach-soothing properties. The acronym BRAT says it all, bananas, rice (white), applesauce, and toast are so gentle on the stomach, preventing further upsets.

What if One Misses the Dose of Hyoscine-N-Butylbromide?

• Oral: If one halts taking the medication, there seems to be no further improvement. So, one should intake the missed dose right after the thought. In another way, one should skip the missed dose and proceed with the subsequent one if the time is nearly for this. So, do not indulge in taking a double dose to compensate for the missed doses.

• Injection: The injection is certainly given in hospital settings. However, one should seek the doctor if one misses out on the scheduled appointment for an injection.

What in Cases of Hyoscine-N-Butylbromide Overdose?

The medication is less likely to harm in cases of a drug overdose. Nevertheless, never take medications beyond the prescription. Also, seek out medical healthcare professionals at the earliest if the medication is taken in higher or increased doses.

Side effects

Side effects are less common in Hyoscine-n-butylbromide drug therapy.

• Dryness of mouth.

• Irregular heart rate.

• Difficulties with passing urine.

• Nausea.

• Diarrhea.

• Reduced blood pressure.

• Headache.

• Dizziness.

• Drowsy.

• Visual disturbances.

• Chest pain.

• Chest discomfort.

• Confusion.

• Constipation.

• Eyelid irritation.

For Doctors

Clinical Data of Hyoscine-N-Butylbromide

Generic name: Hyoscine-N-butylbromide.

Other names: Butylscopolamine bromide, Scopolamine butylbromide, and Hyoscine butylbromide.

Drug class: Anticholinergic, antimuscarinic antispasmodic.

Formula: C21H30BrNO4.

Molar mass: 440.378 g.mol-1.

Indications:

• Spasm and cramp relief of the gastrointestinal tract or genitourinary tract. So, abdominal cramps and pain.

• Symptomatic relief in irritable bowel syndrome (IBS).

• Endoscopy and radiological premedication.

Associated Conditions:

• Gastrointestinal spastic and hypermobility disorders.

• Menstrual distress in dysmenorrhea.

• Muscle spasm.

• Pain.

• Primary dysmenorrhea.

• Infantile hypertrophic pyloric stenosis.

• Urinary tract stiffness.

• Acute gastrointestinal spasms.

• Acute biliary spasm.

• Acute genitourinary spasm.

• Genitourinary smooth muscle spasm.

Associated Intervention:

• Analgesia.

• Smooth muscle relaxation before radiological-based therapy.

Pharmacology of Hyoscine-N-Butylbromide

Chemistry

Hyoscine-n-butyl bromide is the chemical derivative of Hyoscine. This is chemically regarded as alkaloid but was originally derived from plants of the Solanaceae family.

Mechanism of Action

The anticholinergic action of Hyoscine-n-butylbromide deploys relaxing or spasmolytic outcomes of the smooth muscles. Therefore, the Butylscopolamine bromide binds with muscarinic (M3) receptors in the GI tract. This, in turn, blocks and obviates the acetylcholine from binding to those receptors. In addition, Hyoscine butylbromide remains accessible at the site of action in the intestines and deploys a local spasmolytic effect. So, with the prevention of activation of the receptors, smooth muscle contraction is prevented. Therefore, inhibition of smooth muscle contraction alleviates pain and spasms from abdominal crampings. The Hyoscine plays an antagonist role in the following targets.

• Muscarinic acetylcholine receptor M3.

• Muscarinic acetylcholine receptor M2.

Pharmacodynamics

• Hyoscine butylbromide is a muscarinic antagonist.

• So, it inhibits and prevents acetylcholine-stimulated smooth muscle contraction in the gastrointestinal tract.

Absorption

• Hyoscine butylbromide is scarcely and partially absorbed, as it is highly polar, being a quaternary ammonium element.

• Hence, it is absorbed with oral 8 % and rectal 3 % of administration.

• The peak plasma concentration is attained in about 0.25 to two hours.

• Hyoscine butylbromide does not cross the blood-brain barrier, as per animal studies.

Distribution

• Scopolamine butylbromide possesses a high affinity for muscarinic and nicotinic receptors.

• Hence, it is primarily and widely distributed in the myocytes in the pelvic and abdominal aspects. And also it is distributed in the intramural ganglions.

• The binding of Hyoscine butylbromide with plasma protein is about 4.4 percent.

Metabolism

• The metabolism of Hyoscine butylbromide is through the hydrolytic disintegration of ester bonds.

• The metabolites are not to be as markedly active.

Elimination

• Hyoscine butylbromide is chiefly eliminated in the feces and secondary in the urine following an oral administration.

• The bioavailability was estimated at <1% from renal excretion.

Adverse Effects

The uncommon adverse events with the anticholinergic properties of Hyoscine-N-butylbromide include the following.

• Cardiac events: Tachycardia.

• Gastrointestinal disorders: Dry mouth.

• Skin and subcutaneous disorders: Unusual sweating and skin reactions like pruritus and urticaria.

In addition, it includes rare events of urinary retention. And immune system disorders such as anaphylaxis, shock, dyspnea, and other hypersensitivity reactions have not yet been estimated from the available studies.

Note: Intravenous injection of Hyoscine butylbromide should be administered gradually with care as it may rarely lead to an abrupt decline in blood pressure and, thus, shock.

Contraindications and Warnings

• Hypersensitivity to the active component or any other ingredient.

• Prostate hypertrophy and urinary retention.

• Mechanical stenosis in GIT.

• Paralytic ileus or obstructive ileus.

• Megacolon.

• Tachycardia.

• Myasthenia gravis.

• People under anticoagulant drugs. Intramuscular injection of Hyoscine butylbromide in people with anticoagulant drugs would result in an intramuscular hematoma.

Special Considerations

• Myasthenia Gravis: It may have certain theoretical risks which result as a consequence of the anticholinergic mechanism of the drug. Nevertheless, the most significant number of people experience no issues since the Hyoscine-n-butylbromide acts on the receptors of the autonomic system while not on skeletal muscles.

• Paralytic Ileus: Hyoscine-N-butylbromide might worsen the condition. However, this would not result in long-term consequences because of the short course of action.

• Prostatism: Hyoscine-N-butylbromide can influence the detrusor muscles and so potentially precipitate acute retention. But, this does not seem to be a complication as of its short duration of action.

• Intestinal Obstruction: Hyoscine butylbromide is not recommended in cases of intestinal obstruction as it might deteriorate.

• Cardiovascular Illnesses: Caution and considerations should be taken while prescribing Hyoscine butylbromide to individuals with cardiovascular concerns since it may provoke events such as tachycardia, decreased blood pressure, vertigo, dizziness, and dyspnea. And so, heart functions must be monitored accordingly.

• Porphyria: The drug prescription in cases of porphyria is considered safe and sound now.

Drug Interactions

The anticholinergic effects of antihistamines, antidepressants, antipsychotics, quinidine, and other anticholinergics may be intensified by Hyoscine butylbromide. In addition, Hyoscine butyl bromide holds several drug interactions, while a few are described below.

• Interaction with Benzodiazepines: 1, 2 Benzodiazepines might influence the central nervous system depressant effect of Hyoscine butylbromide.

• Interaction with Adenosine: A combination of Hyoscine butylbromide and Adenosine results in an increase in the risk and severity of tachycardia.

• Interaction with Dopamine Antagonists: Dopamine antagonists like Metoclopramide in conjugation treatment with Hyoscine butylbromide might result in declining effects of both drugs in the gastrointestinal tract.

• Interaction with Beta-Adrenergic Agents: With Hyoscine butylbromide, the tachycardic effects of beta-adrenergic agents get enhanced.

Clinical Trials Affirming the Efficacy of Hyoscine-N-Butylbromide

Aim of the Clinical Trial:

To validate the safety and efficacy of Hyoscine butylbromide for abdominal pain in association with crampings on a demand basis.

Description:

The clinical trial is a placebo-controlled, randomized, double-blind, parallel-group pilot study for the safety and efficacy of 20 mg Hyoscine-n-butylbromide tablets used on a demand basis for intervention of self-reported painful abdominal crampings. One group was given the active drug Hyoscine butylbromide 20 mg, one to five tablets for one episode. At the same time, the other one was treated with a placebo with the same frequency of one to five tablets per episode. The intervention was accomplished for a phase of four weeks.

Results

In the end, Hyoscine butylbromide seems to be a valuable and effective treatment option for people with abdominal cramping and pain. Therefore, the drug was considered beneficial in trials. In addition, the Hyoscine butylbromide has been rarely absorbed and ascertained in the blood, so the drug has not penetrated the blood-brain barrier. Therefore, Hyoscine butylbromide is generally well-tolerated in the system where few adverse effects were reported.