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Wednesday, July 23, 2025

Hyoscine hydrobromide


Generic Name
Hyoscine hydrobromide

Also Known As
Scopolamine hydrobromide
L-hyoscine hydrobromide

Brand Names
Kwells
Buscopan Hydrobromide
Scopoderm
Hyoscine Tabs
Travel Calm
Avalon Travel Sickness
Joy-Rides
Formulated as oral tablets, sublingual tablets, transdermal patches, injectable ampoules

Drug Class
Antimuscarinic agent
Belladonna alkaloid derivative
Parasympatholytic (cholinergic antagonist)

Mechanism of Action
Hyoscine hydrobromide competitively blocks muscarinic acetylcholine receptors, particularly M1 and M3 subtypes
It reduces the activity of the parasympathetic nervous system, leading to inhibition of smooth muscle contraction, glandular secretions, and vestibular input
In the central nervous system, it acts on the medullary vomiting center and vestibular nuclei to prevent motion-induced nausea and vomiting
It also reduces gastrointestinal spasms and secretions

Indications
Prevention and treatment of motion sickness (sea, air, or land)
Nausea and vomiting due to inner ear disturbances
Adjunct in anesthesia to reduce secretions and prevent bradycardia
Treatment of gastrointestinal, biliary, or genitourinary spasms
Palliative care for drooling (sialorrhea) and respiratory secretions
Control of extrapyramidal symptoms like drug-induced Parkinsonism (rare use)

Dosage and Administration

Adults – Oral Tablets
Typical dose: 300–600 micrograms 30 minutes before travel
May be repeated every 6–8 hours
Maximum: 1.2 mg/day
Used as a short-term treatment (≤48 hours) for motion sickness

Sublingual Tablets (e.g., Kwells)
Same dosing as above
Dissolve under the tongue for rapid effect

Transdermal Patch (Scopoderm)
Delivers 1.5 mg over 72 hours
Applied behind the ear at least 5–6 hours before travel
Replaced every 3 days as needed

Injectable Form
Used in palliative or perioperative care
Dose: 0.2–0.6 mg IM/IV/SC every 6–8 hours as required

Pediatric Use
Children ≥4 years (oral/sublingual): 150–300 micrograms before travel
Children <4 years: not recommended
Transdermal patches not approved for children

Geriatric Use
Start with lowest effective dose
Caution due to increased risk of confusion, hallucinations, anticholinergic burden

Pharmacokinetics
Onset:
– Oral: 30–60 minutes
– Sublingual: 20–30 minutes
– Patch: ~6 hours
Duration:
– Oral: ~6–8 hours
– Patch: up to 72 hours
Metabolized hepatically
Excreted renally
Crosses blood-brain barrier and placenta

Contraindications
Hypersensitivity to hyoscine or belladonna alkaloids
Angle-closure glaucoma
Prostatic hypertrophy with urinary retention
Pyloric stenosis
Myasthenia gravis
Tachyarrhythmia
Severe ulcerative colitis or intestinal obstruction
Children under 4 years (for oral/sublingual)

Warnings and Precautions
Use caution in elderly due to CNS effects and anticholinergic burden
May cause drowsiness, blurred vision, and impaired coordination – avoid driving or operating machinery
Worsening of narrow-angle glaucoma – monitor intraocular pressure
Exacerbation of urinary retention in patients with prostatic hypertrophy
Risk of heat stroke due to decreased sweating in hot environments
Cognitive impairment and confusion especially in older adults or those with underlying dementia
Abrupt withdrawal of transdermal patch can result in rebound symptoms
Transdermal formulation must be applied with clean hands and disposed of safely

Adverse Effects

Very Common
Drowsiness
Dry mouth
Blurred vision

Common
Dizziness
Nausea
Constipation
Mydriasis
Increased intraocular pressure
Urinary retention
Sedation

Uncommon
Disorientation
Confusion
Hallucinations
Agitation
Tachycardia
Skin reactions at patch site

Rare
Delirium (particularly in elderly or high doses)
Allergic reactions
Paralytic ileus

Pregnancy and Lactation

Pregnancy Category
Generally considered low risk when used intermittently for motion sickness
Avoid use near term due to potential neonatal CNS depression
Transdermal patch may be used under medical guidance

Lactation
Excreted in breast milk in small amounts
Potential for infant sedation and feeding difficulty
Caution advised during breastfeeding

Drug Interactions

Anticholinergic Burden
Additive effects with other anticholinergics (e.g., atropine, oxybutynin, tricyclic antidepressants)
Increased risk of dry mouth, urinary retention, cognitive effects

CNS Depressants
Additive sedation with alcohol, benzodiazepines, opioids, antihistamines
Avoid alcohol while using hyoscine

Glaucoma Medications
May antagonize cholinergic glaucoma therapies

Levodopa
May reduce absorption and therapeutic effect

Potassium Chloride
Risk of GI ulceration if delayed-release potassium tablets are used concomitantly due to delayed gastric emptying

Monoamine Oxidase Inhibitors (MAOIs)
Caution due to potential for additive anticholinergic and CNS effects

Monitoring Parameters
Evaluate for relief of nausea or spasm
Monitor for signs of CNS toxicity (confusion, hallucinations, restlessness) especially in elderly
Assess urinary output in patients with prostatic hypertrophy
Monitor intraocular pressure in glaucoma patients
Observe for local skin reactions in patch users

Counseling Points
Take 30 minutes before travel for best effect
Avoid driving, alcohol, or operating heavy machinery due to drowsiness
Do not cut or split transdermal patches
Dispose of used patches safely away from children and pets
Store away from heat and light
Use sugar-free gum or lozenges to relieve dry mouth
Report visual disturbances or confusion immediately

Comparative Notes

Hyoscine Hydrobromide vs Hyoscine Butylbromide
Hydrobromide crosses blood-brain barrier – used for CNS effects (nausea, motion sickness)
Butylbromide (e.g., Buscopan) is quaternary compound – does not cross BBB – used for GI spasms

Hyoscine vs Cinnarizine for Motion Sickness
Hyoscine is anticholinergic
Cinnarizine is antihistamine with calcium channel blocking effect
Both effective, but cinnarizine may be less sedating

Hyoscine vs Meclizine or Cyclizine
Meclizine and cyclizine are less anticholinergic
Better tolerated in elderly
Hyoscine more potent but more CNS adverse effects

Legal and Regulatory Status
OTC in many countries for motion sickness
Prescription-only for injection or in high-dose transdermal forms
Available under pharmacist supervision for pediatric use



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