Hyoscine butylbromide, also known as scopolamine butylbromide
and sold under the brandname Buscopan among others,
[ is an anticholinergic medication used to treat crampy abdominal pain, esophageal spasms, renal colic, and ]bladder spasms
Overactive bladder (OAB) is a condition where there is a frequent feeling of needing to urinate to a degree that it negatively affects a person's life. The frequent need to urinate may occur during the day, at night, or both. If there is loss ...
. It is also used to improve respiratory secretions at the end of life End-of-life may refer to:
* End-of-life (product), a term used with respect to terminating the sale or support of goods and services
* End-of-life care, medical care for patients with terminal illnesses or conditions that have become advanced, prog ...
. Hyoscine butylbromide can be taken by mouth, injection into a muscle, or into a vein.
Side effects may include sleepiness, vision changes, dry mouth, rapid heart rate, triggering of glaucoma, and severe allergies. Sleepiness is uncommon. It is unclear if it is safe in pregnancy.[ It appears safe in breastfeeding. Greater care is recommended in those with heart problems.] It is an anticholinergic agent,[ which does not have much effect on the brain.]
Hyoscine butylbromide was patented in 1950, and approved for medical use in 1951. It is on the World Health Organization's List of Essential Medicines. It is not available in the United States, and a similar compound methscopolamine may be used instead. It is manufactured from hyoscine, which occurs naturally in the plant deadly nightshade
''Atropa belladonna'', commonly known as belladonna or deadly nightshade, is a toxic perennial herbaceous plant in the nightshade family Solanaceae, which also includes tomatoes, potatoes, and eggplant (aubergine). It is native to Europe, North ...
.
It is available in the United States only for the medical treatment of horses.
Medical uses
Hyoscine butylbromide is effective in treating crampy abdominal pain.
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.
It is also used during abdominal
The abdomen (colloquially called the belly, tummy, midriff, tucky or stomach) is the part of the body between the thorax (chest) and pelvis, in humans and in other vertebrates. The abdomen is the front part of the abdominal segment of the torso. ...
, pelvic MRI, virtual colonoscopy
Virtual colonoscopy (VC, also called CT colonography or CT pneumocolon) is the use of CT scanning or magnetic resonance imaging (MRI) to produce two- and three-dimensional images of the colon (large intestine), from the lowest part, the rectum, ...
, and double barium contrasted studies to improve the quality of pictures. Hyoscine butylbromide can reduce the peristaltic movement of the intestines and mucosal foldings, thus reducing the movement artifact of the images.
Side effects
Since little of the medication crosses the blood brain barrier, this drug has less effect on the brain and therefore causes a reduced occurrence of the centrally-mediated effects (such as delusions
A delusion is a false fixed belief that is not amenable to change in light of conflicting evidence. As a pathology, it is distinct from a belief based on false or incomplete information, confabulation, dogma, illusion, hallucination, or some o ...
, somnolence and inhibition of motor functions) which reduce the usefulness of some other anticholinergic drugs.
Hyoscine butylbromide is still capable of affecting the chemoreceptor trigger zone, due to the lack of a well-developed blood-brain barrier in the medulla oblongata
The medulla oblongata or simply medulla is a long stem-like structure which makes up the lower part of the brainstem. It is anterior and partially inferior to the cerebellum. It is a cone-shaped neuronal mass responsible for autonomic (involun ...
, which increases the antiemetic effect it produces via local action on the smooth muscle
Smooth muscle is an involuntary non-striated muscle, so-called because it has no sarcomeres and therefore no striations (''bands'' or ''stripes''). It is divided into two subgroups, single-unit and multiunit smooth muscle. Within single-unit mus ...
of the gastrointestinal tract
The gastrointestinal tract (GI tract, digestive tract, alimentary canal) is the tract or passageway of the digestive system that leads from the mouth to the anus. The GI tract contains all the major organ (biology), organs of the digestive syste ...
.
Other side effects include accommodation reflex disturbances, tachycardia, dry mouth, nausea; urinary retention, reduced blood pressure; dyshidrosis; Other symptoms are dizziness, flushing and immune system disorders (anaphylactic shock, potentially fatal); anaphylactic reactions; dyspnoea; skin reactions and other hypersensitivity reactions. Cautions should be taken for those with untreated glaucoma, heart failure, benign prostatic hypertrophy with urinary retention as hyoscine may exacerbates these conditions.
Pharmacology
Hyoscine butylbromide reduces smooth muscle contraction and the production of respiratory secretions. These are normally stimulated by the parasympathetic nervous system
The parasympathetic nervous system (PSNS) is one of the three divisions of the autonomic nervous system, the others being the sympathetic nervous system and the enteric nervous system. The enteric nervous system is sometimes considered part of ...
, via the neurotransmitter
A neurotransmitter is a signaling molecule secreted by a neuron to affect another cell across a synapse. The cell receiving the signal, any main body part or target cell, may be another neuron, but could also be a gland or muscle cell.
Neuro ...
acetylcholine
Acetylcholine (ACh) is an organic chemical that functions in the brain and body of many types of animals (including humans) as a neurotransmitter. Its name is derived from its chemical structure: it is an ester of acetic acid and choline. Part ...
. As an antimuscarinic, hyoscine butylbromide binds to muscarinic acetylcholine receptors, blocking their effect.
It is a quaternary ammonium compound
In chemistry, quaternary ammonium cations, also known as quats, are positively charged polyatomic ions of the structure , R being an alkyl group or an aryl group. Unlike the ammonium ion () and the primary, secondary, or tertiary ammonium catio ...
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
The blood–brain barrier (BBB) is a highly selective semipermeable membrane, semipermeable border of endothelium, endothelial cells that prevents solutes in the circulating blood from ''non-selectively'' crossing into the extracellular fluid of ...
, 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. In 2015, it was reported that prisoners at Wandsworth Prison
HM Prison Wandsworth is a Prison security categories in the United Kingdom, Category B men's prison at Wandsworth in the London Borough of Wandsworth, South West (London sub region), South West London, England. It is operated by His Majesty's Pri ...
and other UK prisons were smoking prescribed hyoscine butylbromide, releasing the potent hallucinogen scopolamine
Scopolamine, also known as hyoscine, or Devil's Breath, is a natural or synthetically produced tropane alkaloid and anticholinergic drug that is formally used as a medication for treating motion sickness and postoperative nausea and vomiting ...
. There have also been reports of abuse in Mashhad
Mashhad ( fa, مشهد, Mašhad ), also spelled Mashad, is the List of Iranian cities by population, second-most-populous city in Iran, located in the relatively remote north-east of the country about from Tehran. It serves as the capital of R ...
Central Prison in Iran.
See Also
* Hyoscine
*Hyoscyamine
Hyoscyamine (also known as daturine or duboisine) is a naturally occurring tropane alkaloid and plant toxin. It is a secondary metabolite found in certain plants of the family Solanaceae, including henbane, mandrake, angel's trumpets, jimsonweed ...
References
External links
*
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Muscarinic antagonists
Chemical substances for emergency medicine
Peripherally selective drugs
Carboxylate esters
Quaternary ammonium compounds
World Health Organization essential medicines
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