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Hyoscine

(British Approved Name)

Drug Nomenclature

International Nonproprietary Names (INNs) in main languages (French, Latin, Russian, and Spanish):

Synonyms: Escopolamina; Hyoscin; Hyoscinum; Hyoskiini; Scopolamine; Scopolaminum; Skopolamiini; Skopolamin
BAN: Hyoscine
Chemical name: (-)-(1S,3s,5R,6R,7S,8s)-6,7-Epoxy-3[(S)-tropoyloxy] tropane
Molecular formula: C17H21NO4 =303.4
CAS: 51-34-3
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 colourless crystals. M.p. 66° to 70°. Soluble in water freely soluble in alcohol.

Hyoscine Butylbromide

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
CAS: 149-64-4
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 in dichlorometh-ane sparingly soluble in dehydrated alcohol. A 5% solution in water has a pH of 5.5 to 6.5.

Hyoscine Hydrobromide

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 the 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 labelling information.

Pharmacopoeias. In China, Europe, Japan, and US.

European Pharmacopoeia, 6th ed. (Hyoscine Hydrobromide). A white or almost white, efflorescent, crystalline powder or colourless 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). Colourless or white crystals, or white granular powder. Is odourless 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.

Hyoscine Methobromide

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
CAS: 155-41-9

Pharmacopoeias. In US.

The United States Pharmacopeia 31, 2008 (Methscopolamine Bromide). Store in airtight containers. Protect from light.

Hyoscine Methonitrate

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
CAS: 6106-46-3

Adverse Effects, Treatment, and Precautions

As for Atropine Sulfate. 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 in a similar manner to atropine. However, hyoscine does not stimulate the medullary centres 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 in patients with impaired liver, or kidney function, as adverse CNS effects have been stated to be more likely in these patients. There have been rare reports of an increase in frequency of seizures in epileptic patients.

The quaternary derivatives, such as the butylbromide, methobromide, or methonitrate, do not readily cross the blood-brain barrier, so central effects are rare.

Abuse. 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 referred to as cacao sabanero) has been blown into the victim’s face or given in drinks, chocolate, or chewing gum.

Breast feeding. 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 breast-feeding mothers, and that therefore it may be considered to be usually compatible with breast feeding.

Effects on the eyes. ANISOCORIA. Although bilateral mydriasis has occurred with the use of transdermal hyoscine, 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 instillation of hyoscine eye drops.

Effects on the oesophagus. A patient developed pain on swallowing after 4 days of treatment with hyoscine. Endoscopy showed oesophageal ulceration, which healed completely after 8 weeks of esomeprazole treatment.

Effects on the skin. Contact dermatitis occurred in 16 men being treated for seasickness with transdermal hyoscine for 6 weeks to 15 months.

Porphyria. Hyoscine butylbromide has been associated with acute attacks of porphyria and is considered unsafe in porphyric patients.

Pregnancy. 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.

Withdrawal. A withdrawal syndrome of dizziness and nausea can occur in patients who have used transdermal hyoscine patches for several days hypersalivation and diarrhoea has 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 for a few days.

Interactions

As for antimuscarinics in general (see Atropine Sulfate).

The sedative effect of hyoscine may be enhanced by alcohol or other CNS depressants.

Pharmacokinetics

Hyoscine is readily absorbed from the gastrointestinal tract after oral doses of the hydrobromide. It is almost entirely metabolised, probably in the liver 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 the butylbromide or methobromide, are poorly absorbed from the gastrointestinal tract and do not readily pass the blood-brain barrier.

Uses and Administration

Hyoscine is a tertiary amine antimuscarinic with central and peripheral actions (see Action of Antimuscarinics). 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 also a tertiary amine, whereas hyoscine butylbromide, hyoscine methobromide, and hyoscine methonitrate are quaternary ammonium derivatives.

Hyoscine and hyoscine hydrobromide are used in the management of motion sickness and other forms of nausea and vomiting hyoscine hydrobromide is also given as a premedicant in anaesthesia, and to produce mydriasis and cycloplegia. Hyoscine butylbromide and other quaternary ammonium derivatives are used in conditions associated with visceral spasms. Hyoscine methobromide has also been employed as an adjunct in the treatment of peptic ulcer disease. Other hyoscine salts or derivatives that have been used include hyoscine borate, hyoscine hydrochloride, and hyoscine oxide hydrobromide. See under headings below for details of dosage and administration of hyoscine and its salts in specific indications.

Anaesthesia. The role of antimuscarinics, including hyoscine, in anaesthesia is discussed under Atropine. For the use of hyoscine in the prevention of postoperative nausea and vomiting, see below.

For premedication hyoscine hydrobromide is injected subcuta-neously or intramuscularly in doses of 200 to 600 micrograms, usually with papaveretum about half to one hour before induction of general anaesthesia. In the UK, a dose of 15 micrograms/kg is licensed in children (the BNFC suggests that this dose is appropriate from 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.

Anoxic seizures. For mention of the use of transdermal hyoscine as an alternative to atropine in the management of reflex anoxic seizures in children.

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 butylbromide 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. See also Palliative Care, below. References.

Cardiac disorders. 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 thereby reduce the autonomic imbalance seen in patients with these conditions._ Improved exercise tolerance has been reported after 1 week of treatment with transdermal hyoscine in a small open study in 14 patients with mild to moderate heart failure.

Depression. Rapid reductions in severity of depression were seen after intravenous hyoscine hydrobromide 4 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.

Dysmenorrhoea. Hyoscine as the butylbromide or hydrobromide has been used for its antispasmodic action in the treatment of dysmenorrhoea, but the BNF considers that antispas-modics do not generally provide significant relief.

Eye disorders. 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 useful for patients who are hypersensitive to atropine.

Gastrointestinal disorders. Hyoscine has been used as an antispasmodic to relieve the pain of smooth muscle spasm 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 by mouth for gastrointestinal spasms. As an adjunct in the treatment of peptic ulcer disease hyoscine methobromide has been licensed in the USA in a dose of 2.5 mg half an hour before meals and 2.5 to 5 mg at bedtime. Hyoscine may also be useful as an antispasmodic in diagnostic procedures of the gastrointestinal tract.

The antiemetic effect of hyoscine is discussed under Nausea and Vomiting, below.

Hyperhidrosis. Adverse effects of antimuscarinics given orally generally preclude their use by this route for the management of hyperhidrosis, but some, such as hyoscine, have been applied topically as alternatives to aluminium salts. Hyoscine hydrobromide applied as a 3% cream was successful in reducing 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. The use of transdermal or injectable hyoscine was reported to be effective for the control of 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 the prevention of motion sickness and is one of the principal drugs used. It may be given orally for short-term protection or by transdermal patch for a prolonged duration of 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 10 years, 150 to 300 micrograms. Children aged 3 to 4 years may be given 75 micrograms 20 minutes before a journey, repeated if necessary to a maximum total dose of 150 micrograms in 24 hours. Hyoscine is also given via a transdermal patch which is placed behind the ear and supplies 1 mg over 3 days. The patch is licensed in the UK for adults and children aged 10 years and over and should be applied 5 to 6 hours before travelling or on the preceding evening and removed at the end of the j ourney.

An intranasal formulation of hyoscine hydrobromide has been investigated for the treatment and prevention of motion sickness. Transdermal hyoscine has been used in adults and children for the prevention of 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 in the management of motion sickness and postoperative nausea and vomiting are discussed on p. 1700. References.

Palliative care. 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 3 times daily. Hyoscine butylbromide is also used in palliative care in the treatment of 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, but it can produce both sedation and agitation there is no clear evidence favouring one antimuscarinic over another.

Urinary incontinence. Antimuscarinics have been used in the management of urge incontinence butthe incidence of adverse effects can be high. Results of a small study suggested that transdermal hyoscine might be of benefit in females with detrusor instability.

Vertigo. Hyoscine has a long history of use in the management of vertigo, although other drugs are now preferred.

Preparations

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.

Proprietary Preparations

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

Chile: Buscapina

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

Greece: Buscopan

Hong Kong: Buscopalamin Buscopan Busopin Copan Dhacopan Hysopan Scopoderm TTS Vidaspan

Hungary: Buscopan

India: Buscopan Hyospan

Indonesia: Buscopan Gitas Hyscopan Scobutrin Scopamin Spashi Spasmolit

Ireland: Buscopan Kwells

Italy: Buscopan Transcop

Japan: Buscopan

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

Portugal: Buscopan

Russia: Buscopan

South Africa: Buscopan Hyospasmol Scopaject Scopex

Singapore: Buscopan Colospan Dhacopan Fucon Hyomide Spasmoliv Vacopan

Spain: Buscapina Vorigeno

Sweden: Buscopan Scopoderm

Switzerland: Buscopan

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

Multi-ingredient

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

Ireland: Feminax

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

Sweden: Spasmofen

Switzerland: Nardyl

Thailand: Amcopan Plus Buscopan Plus Donnatal Pacopan Spasgone Unigan

Turkey: Buscopan Compositum Molit Plus Skopolin Spazmol Plus Tanko-Buskas Tranko-Buskas

UK: Feminax

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

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