Hyoscine butylbromide

Hyoscine butylbromide
Clinical data
Trade names Buscopan
Pregnancy
category
Routes of
administration		 By mouth, rectal, intravenous
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability <1%
Protein binding Low
Biological half-life 5 hours
Excretion Renal (50%) and fecal
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
ChEMBL
ECHA InfoCard 100.005.223
Chemical and physical data
Formula C21H30NO4+
Molar mass 360.467 g/mol
3D model (JSmol)
 NYesY (what is this?)  (verify)

Hyoscine butylbromide, also known as scopolamine butylbromide[1] and sold under the brandname Buscopan,[2] is a medication used to treat crampy abdominal pain, esophageal spasms, renal colic, and bladder spasms.[2][3] It is also used to improve respiratory secretions at the end of life.[4] Hyoscine butylbromide can be taken by mouth, injection into a muscle, or into a vein.[2]

Side effects may include sleepiness, vision changes, triggering of glaucoma, and severe allergies.[2] Sleepiness however, is uncommon.[5] It is unclear if it is safe in pregnancy.[2] It is an anticholinergic agent,[2] which does not have much effect on the brain.[6]

It is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system.[7] It is not available in the United States.[8] The wholesale cost in the developing world is 0.004 to 0.11 USD per pill as of 2014.[9] It is manufactured from hyoscine which occurs naturally in the plant deadly nightshade.[10]

Medical uses

A package of injectable buscopan

Hyoscine butylbromide is effective in treating crampy abdominal pain.[11]

Hyoscine butylbromide is effective in reducing the duration of the first stage of labour, and it is not associated with any obvious adverse outcomes in mother or neonate.[12]

It is also used during abdominal or pelvic MRI or CT scans to improve the quality of pictures.[13]

Side effects

As little of the medication crosses the blood brain barrier it has less effects on the brain and therefore has reduced occurrence of the centrally-mediated effects (such as delusions, somnolence, and inhibition of motor-functions) which hinder the usefulness of some other anticholinergic drugs.[6] Hyoscine butylbromide is still capable of impacting the chemoreceptor trigger zone due to the lack of a well-developed blood-brain-barrier in the medulla oblongata, which potentiates the antiemetic effects that it produces via local action on the smooth muscle of the gastrointestinal tract.[14]

Pharmacology

It is a quaternary ammonium compound and a semisynthetic derivative of hyoscine hydrobromide (scopolamine). The attachment of the butyl-bromide moiety effectively prevents the movement of this drug across the blood–brain barrier, effectively minimising undesirable central nervous system side effects associated with scopolamine/hyoscine.

Abuse

Hyoscine butylbromide is not centrally active and has a low incidence of abuse.

References

  1. ↑ Juo, Pei-Show (2001). Concise Dictionary of Biomedicine and Molecular Biology. (2nd ed.). Hoboken: CRC Press. p. 570. ISBN 9781420041309.
  2. 1 2 3 4 5 6 "Buscopan Tablets and Ampoules". Therapeutic Goods Administration, Australia. 8 November 2010. Retrieved 22 October 2013.
  3. ↑ Hamilton, Richart (2015). Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition. Jones & Bartlett Learning. p. 270. ISBN 9781284057560.
  4. ↑ Paice, Judith (2015). Care of the Imminently Dying. Oxford University Press. p. 43. ISBN 9780190244309.
  5. ↑ Handbook of Palliative Care (3rd ed.). New York: Wiley. 2012. p. 570. ISBN 9781118426814.
  6. 1 2 Hanks, Geoffrey (2011). Oxford textbook of palliative medicine (4th ed.). Oxford [etc.]: Oxford University Press. p. 805. ISBN 9780199693146.
  7. ↑ "WHO Model List of Essential Medicines (19th List)" (PDF). World Health Organization. April 2015. Retrieved 8 December 2016.
  8. ↑ Territo, editor, Dennis A. Casciato ; associate editor, Mary C. (2012). Manual of clinical oncology (7th ed.). Philadelphia: Wolters Kluwer/Lippincott Williams & Wilkins Health. p. 146. ISBN 9781451115604.
  9. ↑ "Hyoscine Butylbromide". International Drug Price Indicator Guide. Retrieved 4 December 2015.
  10. ↑ Twycross, Robert (2003). Introducing palliative care (4th ed.). Oxford: Radcliffe Medical Press. p. 172. ISBN 9781857759150.
  11. ↑ Tytgat, G. N. (2007). "Hyoscine Butylbromide: A Review of its Use in the Treatment of Abdominal Cramping and Pain". Drugs. 67 (9): 1343–1357. PMID 17547475. doi:10.2165/00003495-200767090-00007.
  12. ↑ Samuels, L. A.; Christie, L.; Roberts-Gittens, B.; Fletcher, H.; Frederick, J. (2007). "The effect of hyoscine butylbromide on the first stage of labour in term pregnancies". BJOG. 114 (12): 1542–1546. PMID 17903230. doi:10.1111/j.1471-0528.2007.01497.x.
  13. ↑ "Hyoscine butylbromide (Buscopan®)" (PDF). UK: Guy's and St Thomas' NHS Foundation Trust. July 2014. Retrieved 16 June 2016.
  14. ↑ Paul Glare, Jeanna Miller, Tanya Nikolova, and Roma Tickoo (12 September 2011). "Treating nausea and vomiting in palliative care: a review". Clinical Intervention of Aging. PMC 3180521 Freely accessible.
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