Hyoscine, also known as scopolamine, is a natural alkaloid found in certain plants, including the nightshade family members (Solanaceae). It has antimuscarinic properties, which block the action of acetylcholine, a neurotransmitter in the parasympathetic nervous system.
Hyoscine has various medical uses, including:
- Motion Sickness: It is commonly used to prevent motion sickness and nausea.
- Gastrointestinal Disorders: Hyoscine can relieve irritable bowel syndrome (IBS) symptoms, including abdominal cramps and spasms.
- Anesthesia: It is sometimes used with other medications to induce relaxation and reduce salivation in surgical and anesthetic procedures.
- Dizziness and Vertigo: Hyoscine may be prescribed to alleviate dizziness and vertigo associated with certain inner ear disorders.
- Parkinson’s Disease: In some cases, hyoscine is used to manage symptoms of Parkinson’s disease.
- Ophthalmology: Hyoscine can be used to dilate the pupils for eye examinations.
Hyoscine can have side effects, including dry mouth, blurred vision, and constipation. As with any medication, it should be used under the supervision of a healthcare professional, and the dosage and duration of use should be carefully monitored.
Hyoscine is readily absorbed from the gastrointestinal tract after oral doses of the hydrobromide. It is almost entirely metabolized, probably in the liver, and only a small proportion of an oral dose is excreted unchanged in the urine. It crosses the blood-brain barrier and has been stated to cross the placenta. Hyoscine is also well absorbed after application to the skin.
The quaternary derivatives, such as butyl bromide or methobromide, are poorly absorbed from the gastrointestinal tract and do not readily pass the blood-brain barrier.
Adverse Effects, Treatment, and Precautions
In contrast to atropine, hyoscine produces central depression at therapeutic doses, and symptoms include drowsiness and fatigue. Toxic doses of hyoscine produce stimulation of the CNS similar to atropine. However, hyoscine does not stimulate the medullary centers and, therefore, does not produce the increases in respiration rate or blood pressure seen with atropine.
Hyoscine may produce CNS stimulation rather than depression at therapeutic doses if used in the presence of pain without opioid analgesics. Symptoms include excitement, restlessness, hallucinations, or delirium. Patients who experience drowsiness should not drive or operate machinery. Caution has been advised in elderly patients and patients with impaired liver or kidney function, as adverse CNS effects are more likely in these patients. There have been rare reports of increased frequency of seizures in epileptic patients.
The quaternary derivatives, such as butyl bromide, methyl bromide, or methonitrate, do not readily cross the blood-brain barrier, so central effects are rare.
Hyoscine has been used by criminals to incapacitate and produce anterograde amnesia in their victims in crimes such as drug-facilitated rape (‘date rape’), robbery, and kidnapping. In some countries in South America, there has been a particular problem with the use of powders or extracts of plants containing hyoscine for such crimes. A powder, known locally as burundanga, prepared from the borrachero or borracchio tree (also called cacao sabanero) has been blown into the victim’s face or given in drinks, chocolate, or chewing gum.
The American Academy of Pediatrics states that there have been no reports of any clinical effect on the infant associated with the use of hyoscine by breastfeeding mothers. Therefore, it may be considered to be usually compatible with breastfeeding.
Effects on the Eyes
Anisocoria. Although bilateral mydriasis has occurred with the use of transdermal hyoscine, the development of a unilateral fixed dilated pupil (anisocoria) may be due to contamination of a finger with hyoscine in handling the device and then rubbing the eye. Similarly, anisocoria has been attributed to ocular contamination after handling broken hyoscine methobromide tablets.
STRAB/SMUS. Strabismus developed in a 4-year-old boy during treatment with transdermal hyoscine patches for drooling. The strabismus resolved shortly after stopping hyoscine.
Effects on Mental Function
There have been reports of psychotic reactions associated with the transdermal use of hyoscine. Psychotic reactions have also occurred after the instillation of hyoscine eye drops.
Effects on the Esophagus
A patient developed pain on swallowing after four days of treatment with hyoscine. Endoscopy showed oesophageal ulceration, which healed completely after eight weeks of esomeprazole treatment.
Effects on the Skin
Contact dermatitis occurred in 16 men treated for seasickness with transdermal hyoscine for six weeks to 15 months.
Hyoscine butyl bromide has been associated with acute porphyria attacks and is considered unsafe in porphyric patients.
There was a report of hyoscine toxicity in a neonate born to a mother who had received a total of 1.8 mg of hyoscine in divided doses with pethidine and levorphanol before delivery. The neonate was lethargic, barrel-chested, and had a heart rate of 200 beats/minute. Symptoms subsided when physostigmine 100 micrograms was given intramuscularly.
A withdrawal syndrome of dizziness and nausea can occur in patients who have used transdermal hyoscine patches for several days; hypersalivation and diarrhea have also been described. In reported cases, transdermal hyoscine had been used continuously for 7 or 10 days to prevent motion sickness. Symptoms usually begin 2 or 3 days after the last patch has been removed and may last a few days.
As for antimuscarinics in general (see Atropine Sulfate).
The sedative effect of hyoscine may be enhanced by alcohol or other CNS depressants.
Uses and Administration
Hyoscine is a tertiary amine antimuscarinic with central and peripheral actions. It is a more powerful suppressant of salivation than atropine and usually slows rather than increases heart rate, especially in low doses. Its central action differs from that of atropine in that it depresses the cerebral cortex and produces drowsiness and amnesia. Hyoscine hydrobromide is a tertiary amine, whereas hyoscine butyl bromide, hyoscine methobromide, and hyoscine methonitrate are quaternary ammonium derivatives.
Hyoscine and hyoscine hydrobromide are used to manage motion sickness and other forms of nausea and vomiting. Hyoscine hydrobromide is also given as a premedicant in anesthesia to produce mydriasis and cycloplegia. Hyoscine butyl bromide and other quaternary ammonium derivatives are used in conditions associated with visceral spasms. Hyoscine metho-bromide has also been employed as an adjunct in treating peptic ulcer disease. Other hyoscine salts or derivatives that have been used include hyoscine borate, hyoscine hydrochloride, and hyoscine oxide hydrobromide.
The role of antimuscarinics, including hyoscine, in anesthesia is discussed under atropine.
For premedication, hyoscine hydrobromide is injected subcutaneously or intramuscularly in doses of 200 to 600 micrograms, usually with papaveretum about half to one hour before induction of general anesthesia. In the UK, a dose of 15 micrograms/kg is licensed in children (the BNFC suggests that this dose is appropriate for 1 to 12 years of age; older children may be given the adult dose). If necessary for acute use, the same doses may be given by intravenous injection.
Biliary and Renal Colic
Hyoscine has been used as an adjunct to opioid analgesics for symptomatic relief of biliary or renal colic, although the evidence for such use is weak. Hyoscine butyl bromide 20 mg is given by intramuscular or slow intravenous injection; this may be repeated after 30 minutes if necessary to a maximum daily dose of 100 mg.
Although hyoscine is not one of the conventional therapies for heart failure or myocardial infarction, low-dose transdermal hyoscine can increase cardiac vagal activity and reduce the autonomic imbalance seen in patients with these conditions._ Improved exercise tolerance has been reported after one week of treatment with transdermal hyoscine in a small open study in 14 patients with mild to moderate heart failure.
Rapid reductions in the severity of depression were seen after intravenous hyoscine hydrobromide, four micrograms/kg, was given to patients with major depressive disorders or bipolar disorders (see depression). Repeat doses showed more benefit than single doses. Clinical effects persisted beyond the treatment period, which led the authors to conclude the effects were not due to anticholinergic euphoria. While noting that the optimal schedule and potential long-term use of hyoscine as an antidepressant needed further study, they also concluded that hyoscine could be a relatively safe and well-tolerated intervention for achieving a rapid initial antidepressant response.
Hyoscine as the butyl bromide or hydrobromide has been used for its antispasmodic action in treating dysmenorrhoea, but the BNF considers that antispasmodics do not generally provide significant relief.
Hyoscine hydrobromide is used in the eye for its mydriatic and cycloplegic actions, usually in a concentration of 0.25%. It has a faster onset and shorter duration of action than atropine, although the effects may still persist for up to 3 to 7 days. It may be helpful for patients who are hypersensitive to atropine.
Hyoscine has been used as an antispasmodic to relieve the pain of smooth muscle spasms associated with the gastrointestinal tract. In such conditions, the licensed UK dose is 20 mg of hyoscine butylbromide intramuscularly or by slow intravenous injection, repeated after 30 minutes if necessary, up to a maximum of 100 mg daily; alternatively, 20 mg may be given orally four times daily. In irritable bowel syndrome, the recommended oral starting dose is 10 mg three times daily, which may be increased to 20 mg four times daily if necessary. Children aged 6 to 12 years may be given 10 mg three times daily orally for gastrointestinal spasms. As an adjunct in treating peptic ulcer disease, hyoscine methobromide has been licensed in the USA at 2.5 mg half an hour before meals and 2.5 to 5 mg at bedtime. Hyoscine may also be helpful as an antispasmodic in diagnostic procedures of the gastrointestinal tract.
Adverse effects of oral antimuscarinics generally preclude their use by this route to manage hyperhidrosis. However, hyoscine has been applied topically as an alternative to aluminum salts. Hyoscine hydrobromide applied as a 3% cream successfully reduced gustatory sweating, consisting of flushing and sweating over the right mandible during eating, in a patient who had previously undergone surgical excision of the right submandibular salivary gland. Transdermal or injectable hyoscine was reported to be effective for controlling opioid-associated sweating in 2 patients receiving palliative care (see also below for other uses of hyoscine in palliative care).
Nausea and Vomiting
Hyoscine is an effective agent in preventing motion sickness and is one of the principal drugs used. It may be given orally for short-term protection or by the transdermal patch for prolonged action. In the UK, a usual oral dose of hyoscine hydrobromide is 300 micrograms taken 30 minutes before a journey, followed by 300 micrograms every 6 hours if required, up to a maximum of 3 doses in 24 hours. Children aged 4 to 10 years may be given 75 to 150 micrograms, and those over ten years, 150 to 300 micrograms. Children aged 3 to 4 years may be given 75 micrograms 20 minutes before a journey, repeated to a maximum dose of 150 micrograms in 24 hours if necessary. Hyoscine is also given via a transdermal patch placed behind the ear and supplies 1 mg over three days. The patch is licensed in the UK for adults and children aged ten years and over and should be applied 5 to 6 hours before traveling or on the preceding evening and removed at the end of the journey.
An intranasal formulation of hyoscine hydrobromide has been investigated to treat and prevent motion sickness. Transdermal hyoscine has been used in adults and children to prevent postoperative nausea and vomiting. Hyoscine hydrobromide has also been given by intravenous, subcutaneous, or intramuscular injection for its antiemetic effect in a usual dose of 300 to 600 micrograms. The other drugs used to manage motion sickness and postoperative nausea and vomiting are discussed on p. 1700. References.
The BNF includes doses for hyoscine in palliative care. Hyoscine hydrobromide is used in palliative care to reduce excessive respiratory secretions. A dose of 400 to 600 micrograms may be given by subcutaneous injection every 4 to 8 hours. Alternatively, 0.6 to 2.4 mg may be given over 24 hours by continuous subcutaneous infusion. In younger patients, the BNFC suggests a dose of 10 micrograms/kg (up to a maximum of 600 micrograms) by subcutaneous or intravenous injection every 4 to 8 hours. Alternatively, 1.5 to 2.5 micrograms/kg per hour may be given by continuous subcutaneous or intravenous infusion. Care should be taken to avoid the discomfort of a dry mouth. Hyoscine may also be given as a transdermal patch in some countries.
Hyoscine hydrobromide may be given sublingually for the pain of bowel colic in a dose of 300 micrograms three times daily. Hyoscine butyl bromide is also used in palliative care to treat bowel colic. However, it may not be adequate for the control of respiratory secretion. It is given as a subcutaneous infusion in a dose of 20 to 60 mg every 24 hours. A single subcutaneous dose of 20 mg, reviewed after 30 minutes, has been suggested if it is tried for excessive respiratory secretion. The use of hyoscine in palliative care has been reviewed. Hyoscine hydrobromide may be more effective than glycopyrronium bromide in drying secretions and has a rapid onset of action. However, it can produce both sedation and agitation; no clear evidence favors one antimuscarinic over another.
Antimuscarinics have been used to manage urge incontinence, but the incidence of adverse effects can be high. Results of a small study suggested that transdermal hyoscine might benefit females with detrusor instability.
Hyoscine has a long history of use in managing vertigo, although other drugs are now preferred.
(British Approved Name)
International Nonproprietary Names (INNs) in main languages (French, Latin, Russian, and Spanish):
Synonyms: Escopolamina; Hyoscin; Hyoscinum; Hyoskiini; Scopolamine; Scopolaminum; Skopolamiini; Skopolamin
Chemical name: (-)-(1S,3s,5R,6R,7S,8s)-6,7-Epoxy-3[(S)-tropoyloxy] tropane
Molecular formula: C17H21NO4 =303.4
ATC code: A04AD01; N05CM05; S01FA02
Read code: y03Rs; y07je
Note. The following terms have been used as ‘street names’ or slang names for various forms of hyoscine: Burundanga.
Pharmacopoeias. In Europe.
European Pharmacopoeia, 6th ed. (Hyoscine). A white or almost white crystalline powder or colorless crystals. M.p. 66° to 70°. Soluble in water, freely soluble in alcohol.
Synonyms: N-Butylscopolammonium Bromide; Butylscopolamine Bromide; Butylscopolaminii Bromidum; Butylscopolamonii Bromidum; Butylskopolaminium-bromid; Escopolamina, butilbromuro de; Hioscino butilbromidas; Hioszcin-butilbromid; Hyoscinbutylbromid; Hyoscine-N-butyl Bromide; Hyoscini Butylbromidum; Hyoskiinibutyylibromidi; Scopolamine N-Butyl Bromide; Scopolamine Butylbromide; Scopolamini Butylbromidum; Scopolomini Butylbromidum; Skopolamino butilbromidas; Szkopolamin-butilbromid
BAN: Hyoscine Butylbromide [BANM]
Chemical name: (-)-(1S,3s,5R,6R,7S,8r)-6,7-Epoxy-8-butyl-3-[(S)-tropoyloxy]tropanium bromide
Molecular formula: C21H30BrNO4 =440.4
Read code: y01OV; y07jc; y07jd
Pharmacopoeias. In China, Europe, and Japan.
European Pharmacopoeia, 6th ed. (Hyoscine Butylbromide). A white or almost white crystalline powder. Freely soluble in water and dichloromethane sparingly soluble in dehydrated alcohol. A 5% solution in water has a pH of 5.5 to 6.5.
Synonyms: Bromhidrato de Escopolamina; Escopolamina, hidrobromuro de; Hioscino hidrobromidas; Hioszcin-hidrobromid; Hyoscinhydrobromid; Hyoscini Hydrobromidum; Hyoskiinihydrobromidi; Ioscina Bromidrato; Scopolamine Bromhydrate; Scopolamine Hydrobromide; Scopolamini Hydrobromidum; Scopolamini Hydrobromidum Trihydricum; Skopolamiinihydrobromidi; Skopolamin-bromid trihydrát; Skopolaminhydrobromid; Skopolamino hidrobromidas; Szkopolamin-butilbromid
BAN: Hyoscine Hydrobromide [BANM]
Chemical name: (-)-(1S,3s,5R,6R,7S)-6,7-Epoxytropan-3-yl (S)-tropate hydrobromide trihydrate
Molecular formula: C17H21NO4,HBr,3H2O =438.3
CAS: 114-49-8 (anhydrous hyoscine hydrobromide); 6533-68-2 (hyoscine hydrobromide trihydrate)
ATC code: A04AD01; N05CM05; S01FA02
Read code: y00HA [Cns]; y00lv [Eye]; y08E2 [Anaesthesia]; y03Il; y07dV
Note. HYO is a code approved by BP 2008 for use on single unit doses of eye drops containing hyoscine hydrobromide where the individual container may be too small to bear all the appropriate labeling information.
Pharmacopoeias. In China, Europe, Japan, and the US.
European Pharmacopoeia, 6th ed. (Hyoscine Hydrobromide). A white or almost white, efflorescent, crystalline powder or colorless crystals. Freely soluble in water, soluble in alcohol. A 5% solution in water has a pH of 4.0 to 5.5. Store in well-filled, airtight containers of small capacity. Protect from light.
The United States Pharmacopeia 31, 2008 (Scopolamine Hydrobromide). Colorless or white crystals or white granular powder, odorless and slightly efflorescent in dry air. Soluble 1 in 1.5 of water and 1 in 20 of alcohol, slightly soluble in chloroform, insoluble in ether. pH of a 5% solution in water is between 4.0 and 5.5. Store in airtight containers. Protect from light.
Synonyms: Epoxymethamine Bromide; Escopolamina, metilbromuro de; Hyoscine Methylbromide; Methscopolamine Bromide; Scopolamine Methobromide; Scopolamine Methylbromide
BAN: Hyoscine Methobromide
Chemical name: (-)-(1S,3s,5R,6R,7S)-6,7-Epoxy-8-methyl-3-[(S)-tropoyloxy]tropanium bromide
Molecular formula: C18H24BrNO4 =398.3
Pharmacopoeias. In US.
The United States Pharmacopeia 31, 2008 (Methscopolamine Bromide). Store in airtight containers. Protect from light.
Synonyms: Escopolamina, metilnitrato de; Hyoscine Methylnitrate; Methscopolamine Nitrate; Methylhyoscini Nitras; Methylscopolamine Nitrate; Methylscopolamini Nitras; Metylskopolaminnitrat; Metyyliskopolamiininitraatti; Scopolamine Methonitrate; Scopolamine Methylnitrate
BAN: Hyoscine Methonitrate [BANM]
Chemical name: (-)-(1S,3s,5R,6R,7S)-6,7-Epoxy-8-methyl-3-[(S)-tropoyloxy]tropanium nitrate
Molecular formula: C18H24N2O7 =380.4
British Pharmacopoeia 2008: Hyoscine Butylbromide Injection; Hyoscine Butylbromide Tablets; Hyoscine Eye Drops; Hyoscine Injection; Hyoscine Tablets
The United States Pharmacopeia 31, 2008: Methscopolamine Bromide Tablets; Scopolamine Hydrobromide Injection; Scopolamine Hydrobromide Ophthalmic Ointment; Scopolamine Hydrobromide Ophthalmic Solution; Scopolamine Hydrobromide Tablets.
Argentina: Buscapina Cifespasmo Colobolina Luar-G Pasmodina Rupe-N
Australia: Buscopan Kwells Setacol Travacalm HO
Austria: Buscopan Scopoderm
Belgium: Aspasmine Buscopan
Brazil: Buscopan Hiospan Uni Hioscin
Canada: Buscopan Transderm-V
Czech Republic: Buscolysin Buscopan
Denmark: Buscopan Scopoderm
Finland: Buscopan Scopoderm
France: Scoburen Scopoderm TTS
Germany: Boro-Scopol BS Carino BS-ratiopharm Buscolysin Buscopan Scopoderm TTS Spasman scop Spasmowern
Hong Kong: Buscopalamin Buscopan Busopin Copan Dhacopan Hysopan Scopoderm TTS Vidaspan
India: Buscopan Hyospan
Indonesia: Buscopan Gitas Hyscopan Scobutrin Scopamin Spashi Spasmolit
Ireland: Buscopan Kwells
Italy: Buscopan Transcop
Malaysia: Buscopan Colospan Dhacopan Fucon Hyomide Spasmoliv Vacopan Vascopan
Mexico: Alpin Biomesina Bipasmin Bipasmin N Brolamina Buscapina Busina Busprina-S Butiral Cryopina Espacil Excosine-S Grafin Hiosinotil Hiosultrina Lemophar Liliam Selpiran-S Serralpina
The Netherlands: Buscopan Scopoderm TTS
Norway: Buscopan Scopoderm
New Zealand: Buscopan Gastro-Soothe Scopoderm TTS
Philippines: Ascopen Buscomed Buscopan Busopin Gastride Rotomide Scolmin Spasmosan
Poland: Buscolysin Buscopan Scopolan
South Africa: Buscopan Hyospasmol Scopaject Scopex
Singapore: Buscopan Colospan Dhacopan Fucon Hyomide Spasmoliv Vacopan
Spain: Buscapina Vorigeno
Sweden: Buscopan Scopoderm
Thailand: Amcopan Antispa Bacotan Buscono Buscopan Butyl Cencopan Eralga Higan Hy-Spa Hybutyl Hyosmed Hyospan Hyostan Hyozin Hytic Kanin Myspa Scopas Spalox Spascopan Spasgone-H Spatab U-Oscine Uricine Vacopan Vescopolamine
Turkey: Buscopan Butopan Molit Spazmol
United Arab Emirates: Scopinal
UK: Buscopan Joy-Rides Kwells Scopoderm TTS
USA: Famine Scopace Transderm Scop
Venezuela: Buscapina Hiocin
Argentina: 6 Copin Buscapina Compositum Buscapina CompositumN Buscapina Fern Cavodan Cifespasmo Compuesto Colobolina D Dislembral Espasmo Biotenk Gastrolina Compuesta Ibu-Buscapina Lisalgil Compuesto Luar-G Compositum Novopasmil Compuesto Pasmodina Compuesta Rupe-N Compuesto
Australia:: Donnagel Donnalix Donnatab Travacalm
Austria: Buscopamol Buscopan Compositum Modiscop
Belgium: Buscopan Compositum Spasma
Brazil: Algexin Analverin Composto Analverin Plus Binospan Bioscina Composta Buscopan Composto Buscopan Plus Buscoveran Composto Butilamin Disbuspan Dorspan Ductopan Espasmodid Composto Hioariston Hiospan Composto Inib-Dor Kindpasm Neocopan Sedabel Tropinal Uzara Vagoplex Veratropan Composto
Chile: Algion Buscapina Compositum Dolcopin Kordinol Compuesto Novalona
Germany: Buscopan Plus
Greece: Buscopan Plus Spasmo-Apotel
Hong Kong: Epilon Unigan Virulex Forte
Indonesia: Aludonna Buscopan Plus Gitas Plus Procolic Scopamin Plus Spashi Plus Spaslic Unthecol
Italy: Buscopan Compositum Spasmeridan
Mexico: Algosfar Anadil Benfol Biomesina Compuesta Bipasmin Compuesto Bipasmin Compuesto N Bipasmin Compuesto NF Buscapina Compositum Buscapina Compositum N Busconet Busepan Busprina Colepren Donodol Compuesto Escapin-N Espacil Compuesto Espasmogress Hiosinotil Compuesto Hiosultrina Infafren Compuesto Neo-Pasmonal Ortran Pasmodil Pirobutil Precicol Prestodol Compuesto Retodol Compositum Selpiran Selpiran Compuesto Serralpina Compuesta Viladol Plus
Philippines: Buscopan Plus
Poland: Scopolan Compositum Vegantalgin H
Portugal: Buscopan Compositum N
Spain: Buscapina Compositum Midriati Nolotil Compositum Oragalin Espasmolitico Psico Blocan
Thailand: Amcopan Plus Buscopan Plus Donnatal Pacopan Spasgone Unigan
Turkey: Buscopan Compositum Molit Plus Skopolin Spazmol Plus Tanko-Buskas Tranko-Buskas
USA: Accuhist LA AeroHist Plus AeroKid AH-chew Alkabel AllePak AlleRx Antispasmodic Elixir Barbidonnat Bellahist-D Bellatal Chlor-Mes Chlor-Mes D CPM PSE MSC CPM/PE/MSC DA Chewable DA II Dallergy Dehistine Dexphen M Don-natal DriHist Dura-Vent/DA Durahist Durahist D Ex-Histine Extendryl Extendryl DM Extendryl PEM Hista-Vent DA Histatab D Histor-D Time-celles Hyosophen Mescolor Murocoll-2 Nacon NoHistPlus Norel DM Omnihist LA Famine FQ Kit Pannaz PCM Prehist D PSE MSC Ralix Redur-PCM Relcof PSE Rescon-MX Ryneze Stahist Susano Xiral
Venezuela: Brugesina Buscapina Compositum Buscapina Plus Butilamina Compuesta Diezol Compuesto Fenopol Hioscinol Compuesto Sarifan Compuesto Vuscobras