Opella Healthcare


Opella Healthcare
Full Prescribing Info
Tablet: 1 sugar coated (s.c.) tablet contains 10 mg Hyoscine-N-butylbromide.
Excipients: dibasic calcium phosphate, maize starch, starch soluble, aerosil 200, tartaric acid, stearic acid, polyvidone, saccharose, talc, acacia, titanium dioxide, polyethylene glycol 6000, carnauba wax, beeswax white.
Injection: Each mL contains: Hyoscine-N-butylbromide 20 mg.
Excipients: sodium chloride, water for injection.
Pharmacology: The active ingredient in Buscopan is Hyoscine-N-butylbromide, a known antispasmodic substance. It relieves the pain by acting on the muscle spasm which causes the pain.
Hyoscine-N-butylbromide (BUSCOPAN) exerts a spasmolytic action on the smooth muscle of the gastro-intestinal, biliary and genito-urinary tracts. As a quaternary ammonium derivative, hyoscine butylbromide does not enter the central nervous system. Therefore, anticholinergic side effects at the central nervous system do not occur. Peripheral anticholinergic action results from a ganglion-blocking action within the visceral wall as well as from an anti-muscarinic activity.
Pharmacokinetics: Injection: Absorption and distribution: After intravenous administration hyoscine butylbromide is rapidly distributed (t½α = 4 min, t½β = 29 min) into the tissues. The volume of distribution (Vss) is 128 L (corresponding to approx. 1.7 L/kg). Because of its high affinity for muscarinic receptors and nicotinic receptors, hyoscine butylbromide is mainly distributed on muscle cells of the abdominal and pelvic area as well as in the intramural ganglia of the abdominal organs. Plasma protein binding (albumin) of hyoscine butylbromide is approximately 4.4%. Animal studies demonstrate that hyoscine butylbromide does not pass the blood-brain barrier, but no clinical data to this effect is available. Hyoscine butylbromide (1 mM) has been observed to interact with the choline transport (1.4 nM) in epithelial cells of human placenta in vitro.
Metabolism and elimination: The main metabolic pathway is the hydrolytic cleavage of the ester bond. The half-life of the terminal elimination phase (t½γ) is approximately 5 hours. The total clearance is 1.2 L/min. Clinical studies with radiolabeled hyoscine butylbromide show that after intravenous injection 42 to 61% of the radioactive dose is excreted renally and 28.3 to 37% faecally.
The portion of unchanged active ingredient excreted in the urine is approximately 50%. The metabolites excreted via the renal route bind poorly to the muscarinic receptors and are therefore not considered to contribute to the effect of the hyoscine butylbromide.
Toxicology: Injection: Acutely, hyoscine butylbromide has a low index of toxicity: oral LD50 values were 1000-3000 mg/kg in mice, 1040-3300 mg/kg in rats, and 600 mg/kg in dogs. Toxic signs were ataxia and decreased muscle tone, additionally, in mice tremor and convulsions, in dogs mydriasis, dry mucous membranes and tachycardia. Deaths from respiratory arrest occurred within 24 h. The intravenous LD50 values of hyoscine butylbromide were 10-23 mg/kg in mice and 18 mg/kg in rats. In repeated oral dose toxicity studies over 4 weeks, rats tolerated 500 mg/kg = "no observed adverse effect level (NOAEL)".
At 2000 mg/kg, by the action on parasympathetic ganglia of visceral area, hyoscine butylbromide paralysed the gastrointestinal function resulting in obstipation. Eleven out of 50 rats died.
Haematology and clinical chemistry results did not show dose-related variations.
Over 26 weeks, rats tolerated 200 mg/kg, while at 250 and 1000 mg/kg, the gastrointestinal function was depressed and deaths occurred. The NOAEL of the 39-week oral (capsule) dog study was 30 mg/kg. The majority of clinical findings was attributable to acute effects of hyoscine butylbromide at high dosages (200 mg/kg). No adverse histopathological findings were observed. A repeated intravenous dose of 1 mg/kg was well tolerated by rats in a 4-week study. At 3 mg/kg, convulsions occurred immediately after injection. Rats dosed with 9 mg/kg died from respiratory paralysis.
Dogs treated intravenously over 5 weeks at 2x1, 2x3 and 2x9 mg/kg, showed a dose-dependent mydriasis in all treated animals, in addition at 2x9 mg/kg, ataxia, salivation and decreased body weight and food intake were observed. The solutions were locally well tolerated.
After repeated i.m. injection, the dose of 10 mg/kg was systemically well tolerated, but lesions of muscles at the site of injection were distinctly increased if compared to control rats. At 60 and 120 mg/kg, mortality was high and local damages were dose-dependently increased.
Hyoscine butylbromide was neither embryotoxic nor teratogenic at oral doses of up to 200 mg/kg in the diet (rat) and 200 mg/kg by gavage or 50 mg/kg s.c. (rabbit). Fertility was not impaired at doses of up to 200 mg/kg p.o.
Like other cationic drugs, Hyoscine butylbromide interacts with the choline transport system of human placental epithelial cells in vitro. Transfer of Hyoscine butylbromide to the foetal compartment has not been proved.
In special studies concerning local tolerability, a repeated i.m. injection of 15 mg/kg Hyoscine-N-butylbromide (BUSCOPAN) over 28 days was studied in dogs and monkeys. Small focal necroses at the site of injection were seen only in dogs. Hyoscine-N-butylbromide (BUSCOPAN) was well tolerated in arteries and veins of the rabbit's ear. In vitro, 2 % hyoscine-N-butylbromide (BUSCOPAN) injectable solution showed no haemolytic action when mixed with 0.1 mL human blood.
Hyoscine butylbromide revealed no mutagenic or clastogenic potential in the Ames test, in the in vitro gene mutation assay in mammalian V79 cells (HPRT test) and in an in vitro chromosome aberration test in human peripheral lymphocytes. In vivo, Hyoscine butylbromide was negative in the rat bone marrow micronucleus assay.
There are no in vivo carcinogenicity studies.
Nevertheless, Hyoscine butylbromide did not show a tumorigenic potential in two oral 26-week-studies in rats given up to 1000 mg/kg.
Tablet: It is an antispasmodic used for gastrointestinal tract spasm, spasm and dyskinesia of the biliary system and genitourinary tract spasm.
Injection: Acute gastro-intestinal, biliary and genitourinary spasm, including biliary and renal colic. As an aid in diagnostic and therapeutic procedures, where spasm may be a problem, e.g. gastro-duodenal endoscopy, and in radiology.
Dosage/Direction for Use
Hyoscine-N-butylbromide (BUSCOPAN) should not be taken on a continuous daily basis or for extended periods without investigating the cause of abdominal pain.
Tablet: Unless otherwise prescribed by the physician, the following doses are recommended: Adults and children over 6 years: 1-2 sugar coated tablets 3-5 times daily.
The tablets should be swallowed whole with adequate fluid.
Injection: Adults and adolescents over 12 years: 1-2 ampoules of Hyoscine-N-butylbromide (BUSCOPAN) (20-40 mg) may be administered by slow intravenous, intramuscular or subcutaneous injection several times daily.
The maximum daily dose of 100 mg should not be exceeded.
Infants and children: In severe cases: 0.3-0.6 mg/kg bodyweight, to be administered by slow intravenous, intramuscular or subcutaneous injection several times daily.
The maximum daily dose of 1.5 mg/kg bodyweight should not be exceeded.
Symptoms: In the case of overdose, anticholinergic effects may be observed.
Therapy: If required, parasympathomimetic drugs should be administered.
Ophthalmological advice should be sought in cases of glaucoma urgently. Cardiovascular complications should be treated according to usual therapeutic principles. In case of respiratory paralysis: intubation, artificial respiration should be considered.
Catheterisation may be required for urinary retention. In addition, appropriate supportive measures should be used as required.
Hyoscine-N-butylbromide (Buscopan) is contraindicated in: patients who have demonstrated prior hypersensitivity to Hyoscine-N-butylbromide or any other component of the product; myasthenia gravis, mechanical stenosis in the gastrointestinal tract, paralytical or obstructive ileus, megacolon.
Tablet: In case of rare hereditary conditions that may be incompatible with an excipient of the product, the use of the product is contraindicated.
Injection: untreated narrow angle glaucoma, hypertrophy of the prostate with urinary retention, tachycardia.
By intramuscular injection, Hyoscine-N-butylbromide (BUSCOPAN) ampoules are contraindicated: in patients being treated with anticoagulant drugs since intramuscular haematoma may occur. In these patients, the subcutaneous or intravenous routes may be used.
Special Precautions
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, appropriate diagnostic measures are needed to investigate the etiology of the symptoms.
Because of 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.
Tablet: One sugar coated tablet of 10 mg contains 41.2 mg sucrose, resulting in 411.8 mg sucrose per maximum recommended daily dose. Patients with the hereditary condition of fructose intolerance should not take this medicine. Abdominal cramps may be temporary or signal the presence of a more serious problem. Consult the doctor if the pain is severe or does not improve within 48 hours of taking Hyoscine-N-butylbromide (Buscopan).
Injection: Elevation of intraocular pressure may be produced by the administration of anticholinergic agents such as Hyoscine-N-butylbromide (BUSCOPAN) in patients with undiagnosed and therefore untreated narrow angle glaucoma. Therefore, patients should seek urgent ophthalmological advice in case they should develop a painful, red eye with loss of vision after the injection of Hyoscine-N-butylbromide (BUSCOPAN).
After parenteral administration of Hyoscine-N-butylbromide (BUSCOPAN), cases of anaphylaxis including episodes of shock have been observed. As with all drugs causing such reactions, patients receiving Hyoscine-N-butylbromide (BUSCOPAN) by injection should be kept under observation.
Caution is needed in patients with cardiac conditions submitted to parenteral treatment with Buscopan. Monitoring of these patients is advised.
Effects on ability to drive and use machines: No studies on the effects on the ability to drive and use machines have been performed.
Injection: However, patients should be advised that they may experience undesirable effects such as accommodation disorder or dizziness during treatment with Hyoscine-N-butylbromide (BUSCOPAN) ampoules. 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.
Use In Pregnancy & Lactation
There is limited data from the use of Hyoscine butylbromide in pregnant women.
Animal studies do not indicate direct or indirect harmful effects with respect to reproductive toxicity (see Pharmacology: Toxicology under Actions).
There is insufficient information on the excretion of Hyoscine-N-butylbromide (BUSCOPAN) and its metabolites in human milk.
As a precautionary measure, it is preferable to avoid the use of Hyoscine-N-butylbromide (BUSCOPAN) during pregnancy and lactation.
No studies on the effects on human fertility have been conducted (see Pharmacology: Toxicology under Actions).
Side Effects
Many of the listed undesirable effects can be assigned to the anticholinergic properties of Hyoscine-N-butylbromide (BUSCOPAN).
Anticholinergic side effects of Hyoscine-N-butylbromide (BUSCOPAN) 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.
Cardiac disorders: Tachycardia.
Gastrointestinal disorders: Dry mouth.
Skin and subcutaneous tissue disorders: Dyshidrosis.
Renal and urinary disorders: Urinary retention.
Injection: Eye disorders: Accommodation disorders, mydriasis, increased intraocular pressure.
Vascular disorders: Blood pressure decreased, dizziness, flushing.
Drug Interactions
The anticholinergic effect of drugs such as tri- and tetracyclic antidepressants, antihistamines, antipsychotics, quinidine, amantadine, disopyramide and other anticholinergics (e.g. tiotropium, ipratropium, atropine-like compounds) may be intensified by Hyoscine-N-butylbromide (BUSCOPAN).
Concomitant treatment with dopamine antagonists such as metoclopramide may result in diminution of the effects of both drugs on the gastrointestinal tract.
The tachycardic effects of beta-adrenergic agents may be enhanced by Hyoscine-N-butylbromide (BUSCOPAN).
Tablet: Tell the physician if the patient begins to take any other medicine while taking Hyoscine-N-butylbromide (Buscopan).
Store at temperatures not exceeding 30°C.
MIMS Class
ATC Classification
A03BB01 - butylscopolamine ; Belongs to the class of belladonna alkaloids, semisynthetic, quaternary ammonium compounds. Used in the treatment of functional gastrointestinal disorders.
Sugar-coated tab 10 mg x 4's, 120's. Inj (amp) 20 mg/mL x 10's.
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