1 Name of Medicine
Hyoscine butylbromide.
2 Qualitative and Quantitative Composition
Hyoscine Butylbromide-AFT hyoscine butylbromide 20 mg/1 mL contains 20 mg hyoscine butylbromide per 1 mL ampoule.
For the full list of excipients, see Section 6.1 List of Excipients.
3 Pharmaceutical Form
Hyoscine Butylbromide-AFT hyoscine butylbromide 20 mg/1 mL is a clear and colourless solution for injection.
4.1 Therapeutic Indications
Spasm of the gastrointestinal tract, biliary spasm, renal spasm, diagnostic aid in radiology.
4.2 Dose and Method of Administration
1 or 2 ampoules (20 or 40 mg) by intramuscular or slow intravenous injection. A maximum daily dose of 100 mg should not be exceeded.
Hyoscine Butylbromide-AFT injection should not be administered on a continuous daily basis or for extended periods without investigating the cause of abdominal pain.
Product is for single use in one patient only. Discard any residue.
4.3 Contraindications
Hyoscine Butylbromide-AFT is contraindicated in patients with:
known hypersensitivity to hyoscine butylbromide or to any of the excipients of the product (excipients are listed under Section 6.1 List of Excipients);
mechanical stenosis in the gastrointestinal tract;
achalasia;
paralytic or obstructive ileus;
intestinal atony;
prostatic hypertrophy with urinary retention;
myasthenia gravis;
glaucoma;
pathological tachyarrhythmias;
megacolon.
Hyoscine butylbromide should not be given to patients with porphyria as, according to a single report, it has been said to exacerbate the disease.
By intramuscular injection, Hyoscine Butylbromide-AFT injections are contraindicated in patients being treated with anticoagulant drugs as intramuscular haematoma may occur. In these patients, intravenous routes may be used.
4.4 Special Warnings and Precautions for Use
In case severe, unexplained abdominal pain persists or worsens, or occurs together with symptoms like fever, nausea, vomiting, changes in bowel movements, abdominal tenderness, decreased blood pressure, fainting or blood in stool, medical advice should immediately be sought.
Hyoscine may cause drowsiness: patients so affected should not drive or operate machinery. Patients should abstain from alcohol. However, as a quaternary ammonium compound with low lipid solubility, hyoscine cannot cross the blood/brain barrier easily and only rarely causes the central nervous system side effects associated with atropine and hyoscine.
After parenteral administration of Hyoscine Butylbromide-AFT, patients with visual accommodation disturbances should not drive or operate machinery until vision has normalised.
Elevation of intraocular pressure may be produced by the administration of anticholinergic agents such as hyoscine in patients with undiagnosed and therefore untreated narrow-angle glaucoma. Patients should be advised to seek urgent ophthalmological advice if they develop a painful, red eye with loss of vision after an injection of Hyoscine Butylbromide-AFT.
Because of the potential risk of anticholinergic complications, caution should be used in patients prone to narrow angle glaucoma as well as in patients susceptible to intestinal or urinary outlet obstructions and in those inclined to tachyarrhythmia.
After parenteral administration, cases of anaphylaxis including episodes of shock have been observed. As with all drugs causing such reactions, patients receiving Hyoscine Butylbromide-AFT by injection should be kept under observation.
Patients with cardiac conditions who are undergoing parenteral treatment with Hyoscine Butylbromide-AFT ampoules should be monitored.
Hyoscine Butylbromide-AFT can cause tachycardia, hypotension and anaphylaxis, therefore use with caution in patients with cardiac conditions such as cardiac failure, coronary heart disease, cardiac arrhythmia or hypertension, and in cardiac surgery. Monitoring of these patients is advised. Emergency equipment and personnel trained in its use must be readily available.
Use in the elderly.
No data available.
Paediatric use.
No data available.
Effects on laboratory tests.
No data available.4.5 Interactions with Other Medicines and Other Forms of Interactions
The anticholinergic effects of drugs such as amantadine, tri- and tetracyclic antidepressants, quinidine, antihistamines, antipsychotics, disopyramide, phenothiazines, belladonna alkaloids, other anticholinergics (e.g. tiotropium, ipratropium, atropine-like compounds) and MAO inhibitors etc, together with the tachycardia induced by beta-sympathomimetics, can be potentiated by Hyoscine Butylbromide-AFT.
The concomitant administration of dopamine antagonists, such as metoclopramide, can reciprocally antagonise the effect on gastrointestinal tract motility.
4.6 Fertility, Pregnancy and Lactation
Effects on fertility.
No data available.
(Category B2)
There is limited data from the use of hyoscine butylbromide in pregnant women.
As a precautionary measure, it is preferable to avoid the use of Hyoscine Butylbromide-AFT during pregnancy.
There is insufficient information on the excretion of hyoscine and its metabolites in human milk. As a precautionary measure, it is preferable to avoid the use of Hyoscine Butylbromide-AFT during lactation.4.7 Effects on Ability to Drive and Use Machines
No studies on the effects on the ability to drive and use machines have been performed. However, patients should be advised that they may experience undesirable effects such as accommodation disorder or dizziness during treatment with Hyoscine Butylbromide-AFT injections. Therefore, caution should be recommended when driving a car or operating machinery. If patients experience accommodation disorder or dizziness, they should avoid potentially hazardous tasks such as driving or operating machinery.
4.8 Adverse Effects (Undesirable Effects)
Many of the listed adverse effects of Hyoscine Butylbromide-AFT can be attributed to its anticholinergic properties. Anticholinergic side effects of Hyoscine Butylbromide-AFT are generally mild and self-limited.
Immune system disorders.
Anaphylactic shock including fatal outcome, anaphylactic reactions, dyspnoea, skin reactions (e.g. urticaria, rash, erythema, pruritus) and other hypersensitivity reactions.
Eye disorders.
Accommodation disorders, mydriasis, increased intraocular pressure.
Cardiac disorders.
Tachycardia.
Vascular disorders.
Decreased blood pressure, dizziness and flushing.
Gastrointestinal disorders.
Dry mouth.
Skin and subcutaneous tissue disorders.
Dyshidrosis, abnormal sweating.
Renal and urinary disorders.
Impaired micturition. Urinary retention.
Nervous system disorders.
Very rarely in the national post marketing surveillance data base, there have been isolated reports following parenteral administration of coma, hallucinations, dystonia, confusion, agitation and dizziness from which the patient recovered after drug withdrawal and appropriate treatment. In very rare cases, dyspnoea has been reported.
Reporting suspected adverse effects.
Reporting suspected adverse reactions after registration of the medicinal product is important. It allows continued monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions at www.tga.gov.au/reporting-problems.4.9 Overdose
Symptoms.
Serious signs of poisoning have not been observed in man. In case of overdose, anticholinergic symptoms such as urinary retention, dry mouth, reddening of the skin, inhibition of gastrointestinal motility, tachycardia, drowsiness and transient visual disorders may occur.
Toxicity data from studies in animals after parenteral administration suggest that the following may be possible: shock, Cheyne-Stokes respiration, respiratory paralysis, clonic spasms, paralysis of striated muscle, coma, paralytic ileus, bladder atony.
Management.
After oral overdose, induce emesis, gastric lavage, activated charcoal followed by magnesium sulfate (15%). Supportive measures if necessary, should be instituted. Symptoms of overdosage may respond to parasympathomimetics. Ophthalmological advice should be sought urgently in cases of glaucoma. Pilocarpine may be administered locally in patients with glaucoma. Sympathomimetics may be used for circulatory support. For mental excitation, diazepam.
Cardiovascular complications as a result of using this medicine should be treated according to usual therapeutic principles. In case of respiratory paralysis, intubation and assisted respiration. Catheterisation may be required for urinary retention. In addition, appropriate supportive measures should be used as required.
For information of the management of overdose, contact the Poisons information Centre on 131126 (Australia).5 Pharmacological Properties
5.1 Pharmacodynamic Properties
Mechanism of action.
Hyoscine Butylbromide-AFT is a quaternary ammonium compound which, as an anticholinergic agent, has a ganglion blocking component. Due to its anticholinergic action, Hyoscine Butylbromide-AFT reduces the tone and peristalsis of smooth muscle in hollow organs with parasympathetic innervation. As a quaternary ammonium compound with low lipid solubility, it cannot pass the blood/brain barrier easily and only rarely causes the central nervous system side effects associated with atropine and hyoscine.
Hyoscine Butylbromide-AFT is a spasmolytic. The anticholinergic spasmolytic effect is based both on competitive inhibition of the parasympathetic activation of smooth muscle mediated through muscarinic receptors and, more markedly, through ganglionic blockade of neural transmission.
Hyoscine Butylbromide-AFT is a powerful smooth muscle relaxant, effective when given by mouth or by injection. In the recommended dosages, it relieves smooth muscle spasm rapidly. Undesirable 'atropine-like' side effects such as blurred vision, palpitation or dry mouth are rare.
Clinical trials.
No data available.
5.2 Pharmacokinetic Properties
Absorption.
Hyoscine butylbromide is poorly absorbed from the gastrointestinal tract and is rapidly distributed. The bioavailability of oral hyoscine butylbromide, as calculated from plasma levels, is reported to be 0.13%.
Distribution.
Upon oral administration hyoscine butylbromide concentrates especially in the tissue of the gastrointestinal tract, liver and kidneys. The high affinity of this agent to the tissue is reflected by the very short half-life, t-alpha of 3 minutes (distribution phase) of the blood levels, while the excretion rates are slow. Thus, in spite of the extremely low blood levels measurable over a short period of time, hyoscine butylbromide remains available at the site of action in the tissue in high concentrations.
5.3 Preclinical Safety Data
Genotoxicity.
No data available.
Carcinogenicity.
No data available.6 Pharmaceutical Particulars
6.1 List of Excipients
Sodium chloride, hydrochloric acid, water for injection.
6.2 Incompatibilities
Incompatibilities were either not assessed or not identified as part of the registration of this medicine.
6.3 Shelf Life
In Australia, information on the shelf life can be found on the public summary of the Australian Register of Therapeutic Goods (ARTG).
The expiry date can be found on the packaging.
6.4 Special Precautions for Storage
Store below 30°C. Protect from light.
6.5 Nature and Contents of Container
Hyoscine Butylbromide-AFT hyoscine butylbromide 20 mg/1 mL is supplied in 1 mL amber glass ampoule. Five ampoules are packaged a carton.
6.6 Special Precautions for Disposal
In Australia, any unused medicine or waste material should be disposed of in accordance with local requirements.
6.7 Physicochemical Properties
Chemical structure.
CAS number.
149-64-4.7 Medicine Schedule (Poisons Standard)
S4 - Prescription only medicine.
