1 sugar-coated tablet contains 10 mg hyoscine-N-butylbromide.
Pharmacology: Properties: Buscopan exerts a spasmolytic action on the smooth muscle of the gastro-intestinal, biliary and genito-urinary tracts. As a quaternary ammonium derivative, hyoscine-N-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: Absorption: As a quaternary ammonium compound, hyoscine-N-butylbromide is highly polar and hence only partially absorbed following oral (8%) or rectal (3%) administration. After oral administration of single doses of hyoscine butylbromide in the range of 20 to 400 mg, mean peak plasma concentrations between 0.11 ng/mL and 2.04 ng/mL were found at approximately 2 hours. In the same dose range, the observed mean AUC0-tz-values varied from 0.37 to 10.7 ng h/mL. The median absolute bioavailabilities of different dosage forms, i.e. coated tablets, suppositoires and oral solution, containing 100 mg of hyoscine butylbromide each were found to be less than 1%.
Distribution: 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. Protein binding in the human plasma occurs at 8-13% and in a 4.4% human serum albumin solution at 3-11%. 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: Following oral administration of single doses in the range of 100 to 400 mg, the terminal elimination half-lives ranged from 6.2 to 10.6 hours. The main metabolic pathway is the hydrolytic cleavage of the ester bond. Orally administered hyoscine butylbromide is excreted in the faeces and in the urine. Studies in man show that 2 to 5% of radioactive doses is eliminated renally after oral, and 0.7 to 1.6% after rectal administration. Approximately 90% of recovered radioactivity can be found in the faeces after oral administration. The urinary excretion of hyoscine butylbromide is less than 0.1% of the dose. The mean apparent oral clearances after oral doses of 100 to 400 mg range from 881 to 1420 L/min, whereas the corresponding volumes of distribution for the same range vary from 6.13 to 11.3 x 105 L, probably due to very low systemic availability.
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.
Gastro-intestinal tract spasm, spasm and dyskinesia of the biliary system, genito-urinary tract spasm.
Unless otherwise prescribed by the physician, the following dosages are recommended: Sugar-coated tablets: Adults and children over 6 years: 3 - 5 times daily 1 - 2 s.c. tablets.
The tablets should be swallowed whole with adequate fluid.
Buscopan should not be taken on a continuous daily basis or for extended periods without investigating the cause of abdominal pain.
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.
Buscopan is contraindicated in: patients who have demonstrated prior hypersensitivity to hyoscine butylbromide or any other component of the product; myasthenia gravis; mechanical stenosis in the gastrointestinal tract; paralytical or obstructive ileus; megacolon.
In case of rare hereditary conditions that may be incompatible with an excipient of the product (please refer to Precautions) the use of the product is contraindicated.
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.
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.
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 rare hereditary condition of fructose intolerance should not take this medicine.
Effects on ability to drive and use machines: No studies on the effects on the ability to drive and use machines have been performed. Because of possible visual accommodation disturbances patients should not drive or operate machinery if affected.
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.
There is insufficient information on the excretion of Buscopan and its metabolites in human milk.
As a precautionary measure, it is preferable to avoid the use of Buscopan during pregnancy and lactation.
No studies on the effects on human fertility have been conducted.
Many of the listed undesirable effects can be assigned to the anticholinergic properties of Buscopan. Anticholinergic side effects of Buscopan are generally mild and self-limited.
Immune system disorders: Anaphylactic shock, 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.
The anticholinergic effect of drugs such as tri- and tetracyclic antidepressants, antihistamines, antipsychotics, quinidine, amantadine, disopyramide and other anticholinergics (eg. tiotropium, ipratropium, atropine-like compounds) may be intensified by 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 Buscopan.
A03BB01 - butylscopolamine ; Belongs to the class of belladonna alkaloids, semisynthetic, quaternary ammonium compounds. Used in the treatment of functional gastrointestinal disorders.
Sugar-coated tab (round, white, biconvex) 10 mg x 500's.