Drugs

, Volume 67, Issue 9, pp 1343–1357

Hyoscine Butylbromide

A Review of its Use in the Treatment of Abdominal Cramping and Pain
Review Article

Abstract

Abdominal cramping and pain is a frequent problem in the adult population of Western countries, with an estimated prevalence of ≤30%. Hyoscine butylbromide (scopolamine butylbromide) [Buscopan®/Buscapina®] is an antispas-modic drug indicated for the treatment of abdominal pain associated with cramps induced by gastrointestinal (GI) spasms. It was first registered in Germany in 1951 and marketed in 1952, and has since become available worldwide both as a prescription drug and as an over-the-counter medicine in many countries. This article reviews the pharmacology and pharmacokinetic profile of hyoscine butylbromide, and summarises efficacy and safety data from clinical trials of this drug for abdominal cramping and pain.

Pharmacological studies have revealed that hyoscine butylbromide is an anticholinergic drug with high affinity for muscarinic receptors located on the smooth-muscle cells of the GI tract. Its anticholinergic action exerts a smooth-muscle relaxing/spasmolytic effect. Blockade of the muscarinic receptors in the GI tract is the basis for its use in the treatment of abdominal pain secondary to cramping. Hyoscine butylbromide also binds to nicotinic receptors, which induces a ganglion-blocking effect.

Several pharmacokinetic studies in humans have consistently demonstrated the low systemic availability of hyoscine butylbromide after oral administration, with plasma concentrations of the drug generally being below the limit of quantitation. The bioavailability of hyoscine butylbromide, estimated from renal excretion, was generally <1%. However, because of its high tissue affinity for muscarinic receptors, hyoscine butylbromide remains available at the site of action in the intestine and exerts a local spasmolytic effect.

Ten placebo-controlled studies have evaluated the efficacy and safety of oral or rectal hyoscine butylbromide. Hyoscine butylbromide was considered beneficial in all of these trials, which supports its use in the treatment of abdominal pain caused by cramping. Hyoscine butylbromide is barely absorbed and detectable in the blood and does not penetrate the blood-brain barrier, and is, therefore, generally well tolerated. Few adverse events have been reported; in particular, no significant increases in the incidence of anticholinergic-related adverse effects have been observed.

In summary, hyoscine butylbromide appears to be a valuable treatment option for patients with symptoms of abdominal pain or discomfort associated with cramping.

References

  1. 1.
    Sandler RS, Stewart WF, Liberman JN, et al. Abdominal pain, bloating, and diarrhea in the United States: prevalence and impact. Dig Dis Sci 2000; 45: 1166–71PubMedCrossRefGoogle Scholar
  2. 2.
    Bommelaer G, Poynard T, Le Pen C, et al. Prevalence of irritable bowel syndrome (IBS) and variability of diagnostic criteria. Gastroenterol Clin Biol 2004; 28: 554–61PubMedCrossRefGoogle Scholar
  3. 3.
    Quigley EMM, Locke GR, Mueller-Lissner S, et al. Prevalence and management of abdominal cramping and pain: a multinational survey. Aliment Pharmacol Ther 2006; 24: 411–9PubMedCrossRefGoogle Scholar
  4. 4.
    Maxion-Bergemann S, Thielecke F, Abel F, et al. Costs of irritable bowel syndrome in the UK and US. Pharmacoeco-nomics 2006; 24: 21–37CrossRefGoogle Scholar
  5. 5.
    Simrén M, Brazier J, Coremans G, et al. Quality of life and illness costs in irritable bowel syndrome. Digestion 2004; 69: 254–61PubMedCrossRefGoogle Scholar
  6. 6.
    Gupta V, Moshiree B, Verne GN. Treatment of pain symptoms in irritable bowel syndrome patients. Drugs Today 2004; 40: 829–36PubMedCrossRefGoogle Scholar
  7. 7.
    Poynard T, Regimbeau C, Benhamou Y. Meta-analysis of smooth muscle relaxants in the treatment of irritable bowel syndrome. Aliment Pharmacol Ther 2001; 15: 355–61PubMedCrossRefGoogle Scholar
  8. 8.
    Jailwala J, Imperiale TF, Kroenke K. Pharmacologie treatment of the irritable bowel syndrome: a systematic review of randomized, controlled trials. Ann Intern Med 2000; 133: 136–47PubMedGoogle Scholar
  9. 9.
    Lesbros-Pantoflickova D, Michetti P, Fried M, et al. Meta-analysis: the treatment of irritable bowel syndrome. Aliment Pharmacol Ther 2004; 20: 1253–69PubMedCrossRefGoogle Scholar
  10. 10.
    Brandt LJ, Bjorkman D, Fennerty MB, et al. Systematic review on the management of irritable bowel syndrome in North America. Am J Gastroenterol 2002; 97: S7–26PubMedGoogle Scholar
  11. 11.
    Schoenfeld P. Efficacy of current drug therapies in irritable bowel syndrome: what works and does not work. Gastroenterol Clin North Am 2005; 34: 319–35, viiiPubMedCrossRefGoogle Scholar
  12. 12.
    Evangelista S. Quaternary ammonium derivatives as spasmolytics for irritable bowel syndrome. Curr Pharm Des 2004; 10: 3561–8PubMedCrossRefGoogle Scholar
  13. 13.
    Data on file, Boehringer Ingelheim GmbHGoogle Scholar
  14. 14.
    Pennefather JN, McCulloch MW, Rand MJ. Observations on the efficacy of oral hyoscine N-butyl bromide. J Pharm Pharmacol 1968; 20: 867–72PubMedCrossRefGoogle Scholar
  15. 15.
    Lecchini S, Del Tacca M, Soldani G, et al. The actions of atropine, tropenziline and N-butyl hyoscine bromide on the isolated distal colon of the guinea-pig: a comparison of their activities and mechanisms of action. J Pharm Pharmacol 1969; 21: 662–7PubMedCrossRefGoogle Scholar
  16. 16.
    Pomeroy AR, Rand MJ. Anticholinergic effects and passage through the intestinal wall of N-butylhyoscine bromide. J Pharm Pharmac 1969; 21: 180–7CrossRefGoogle Scholar
  17. 17.
    Maggi CA, Meli A. Assessment of potential selectivity of antispasmodics for the various sections of the gastrointestinal tract of the rat as a guideline for their clinical use. Arch Int Pharmacodyn Ther 1983; 262: 221–31PubMedGoogle Scholar
  18. 18.
    Bauer R, Gross E, Scarselli V, et al. On the differences of effect of atropine, scopolamine and some of their quaternary derivatives after subcutaneous and enterai administration with special reference to scopolamine-n-butylbromide [in German]. Arzneimittelforschung 1968; 18 (9): 1132–7PubMedGoogle Scholar
  19. 19.
    Sasaki D, Kido A, Yoshida Y. Effect of antispasmodic drugs on colonic motility: part I. Laboratory study of the dog. Int J Clin Pharmacol Ther Toxicol 1984; 22: 333–7PubMedGoogle Scholar
  20. 20.
    Sagrada A, Schiavone A, Cefala A, et al. N-butyl hyoscine exerts local spasmolytic effect in the small and large bowel of the conscious dog. Arch Int Pharmacodyn Ther 1987; 287: 237–47PubMedGoogle Scholar
  21. 21.
    Herxheimer A, Haefeli L. Human pharmacology of hyoscine butylbromide. Lancet 1966; 2: 418–21CrossRefGoogle Scholar
  22. 22.
    Schmid E, Bleichert A, Uberla K, et al. Investigations into the testing of oral antispasmodics as demonstrated by the effect of hyoscine-N-butylbromide on gastric motility. Drugs Made Ger 1968; 11: 153–63Google Scholar
  23. 23.
    Schmid E, Bleichert A, Uberla K, et al. Testing of orally administered spasmolytics demonstrated by the effect of hyoscine-N-butylbromide on gastric motility [in German]. Arzneimittelforschung 1968; 18 (11): 1449–53PubMedGoogle Scholar
  24. 24.
    Stacher G, Bergmann H, Havlik E, et al. Effects of oral cyclo-tropium bromide, hyoscine N-butylbromide and placebo on gastric emptying and antral motor activity in healthy man. Gut 1984; 25: 485–90PubMedCrossRefGoogle Scholar
  25. 25.
    Schmid E, Bleichert A, Kitzing J, et al. Inhibition of small intestine motility by orally administered hyoscine-N-butylbromide [in German]. Arzneimittelforschung 1969; 19 (6): 998–9PubMedGoogle Scholar
  26. 26.
    Schmid E, Ritter U. Effect of rectally applied hyoscin-N-butyl-bromide on small intestine motility [in German]. Arzneimittelforschung 1972; 22 (12): 2149–52PubMedGoogle Scholar
  27. 27.
    Miyoshi A, Suyama T, Kawamura I. A double-blind comparative study of the inhibitory effect of intraduodenally administered hyoscine-N-butylbromide on human duodenal motility. J Int Med Res 1977; 5: 223–32PubMedGoogle Scholar
  28. 28.
    Thompson DG, Wingate DL. Oral hyoscine butylbromide does not alter the pattern of small intestinal motor activity. Br J Pharmacol 1981; 72: 685–7PubMedCrossRefGoogle Scholar
  29. 29.
    Schäfer E, Ewe K. The treatment of irritable colon: efficacy and tolerance of buscopan plus, buscopan, paracetamol and placebo in ambulatory patients with irritable colon [in German]. Fortschr Med 1990; 108 (25): 488–92PubMedGoogle Scholar
  30. 30.
    Sánchez Martinez J, Goiz Durán I. Clinical assessment of the tolerability and the effect of IK-19 in tablet form on pain of spastic origin. Invest Med Int 1988; 15: 63–5Google Scholar
  31. 31.
    Nigam P, Kapoor KK, Rastog CK, et al. Different therapeutic regimens in irritable bowel syndrome. J Assoc Physicians India 1984; 32: 1041–4PubMedGoogle Scholar
  32. 32.
    Miyoshi A. A multi-centre, double-blind evaluation against placebo of the therapeutic effect of hyoscine-N-butylbromide in patients with abdominal pain. Pharmatherapeutica 1976; 1: 46–51Google Scholar
  33. 33.
    De Gregorio M, Damiani S, Gatta G. Antalgic properties of proxazole: double blind study in visceral algoplastic conditions. Panminerva Med 1969; 11: 436–40PubMedGoogle Scholar
  34. 34.
    Ritchie JA, Truelove SC. Treatment of irritable bowel syndrome with lorazepam, hyoscine butylbromide, and ispaghula husk. BMJ 1979; 1: 376–8PubMedCrossRefGoogle Scholar
  35. 35.
    Mueller-Lissner S, Tytgat GN, Paulo LG, et al. Placebo- and paracetamol-controlled study on the efficacy and tolerability of hyoscine butylbromide in the treatment of patients with recurrent crampy abdominal pain. Aliment Pharmacol Ther 2006; 23: 1741–8PubMedCrossRefGoogle Scholar
  36. 36.
    Navarro Martinez P. Statistical double-blind study on the therapeutic perference of chronic gastropathic subjects in acute crises [in Spanish]. Rev Med Suiza 1972; 4: 77–9Google Scholar
  37. 37.
    Metzger KH. The effect of anticholinergic agents on caudal intestinal sections: experimental investigations into motility [in German]. Aerztl Praxis 1979; 21: 923–4Google Scholar
  38. 38.
    Sieg H. Double blind test using hyoscine-N-butyl bromide (Buscopan) to reduce pain in ulcus ventriculi [in German]. Z Gastroenterol 1974; 12 (4): 235-8PubMedGoogle Scholar

Copyright information

© Adis Data Information BV 2007

Authors and Affiliations

  1. 1.Academisch Medisch CentrumAmsterdamThe Netherlands

Personalised recommendations