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Injection Buscopan hyoscine butylbromide pharmacology uses dose mechanism

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Buscopan injection dose mechanism pharmacokinetics contraindications adverse effects

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Injection Buscopan (Hyoscine Butylbromide) — Detailed Overview


1. Basic Identity

PropertyDetail
Generic nameHyoscine butylbromide (scopolamine butylbromide)
Brand nameBuscopan®
Drug classAnticholinergic / Antispasmodic
Chemical classQuaternary ammonium compound
WHO statusOn the WHO Essential Medicines List
Injection form20 mg/mL ampoule (1 mL = 20 mg)

2. Mechanism of Action

Buscopan is a parasympatholytic (antimuscarinic) agent with two key pharmacological actions:
  1. Muscarinic receptor blockade — Blocks M1–M5 muscarinic acetylcholine receptors on smooth muscle cells of the GI, biliary, and genitourinary tracts → prevents acetylcholine-mediated smooth muscle contraction → spasmolysis.
  2. Ganglionic blockade (nicotinic) — Also binds nicotinic receptors at parasympathetic ganglia in the visceral walls, amplifying its antispasmodic effect.
Critical distinction from scopolamine/hyoscine hydrobromide: The butyl-bromide group makes it a quaternary ammonium compound — permanently charged across the entire pH range. This prevents it from crossing the blood-brain barrier (BBB), so central anticholinergic effects (sedation, confusion, delirium) are essentially absent. This makes it the preferred antispasmodic in elderly patients where cognitive side effects must be avoided.
  • Maudsley Prescribing Guidelines, 15ed — "Hyoscine butylbromide is not thought to enter the CNS, so central anticholinergic adverse effects are rare."

3. Indications

Injectable form specifically:

  • Acute GI spasm — gastric, intestinal, and colonic colic
  • Renal colic — smooth muscle spasm in the ureter
  • Biliary colic — spasm of the common bile duct and gallbladder
  • Genitourinary spasm — bladder spasm
  • Endoscopy adjunct — IV Buscopan is used to abolish duodenal motility during upper GI endoscopy and during CT colonography/MRI, improving visualisation of the duodenum (2nd and 3rd parts), bowel wall detail, and reducing motion artefact in radiology
  • End-of-life / Palliative care — reduces death rattle (excessive respiratory secretions) in dying patients (equivalent efficacy to atropine and scopolamine in this setting)
  • IBS — as part of antispasmodic regimen

4. Pharmacokinetics

ParameterInjection (IV/IM/SC)
AbsorptionImmediate (IV), rapid (IM/SC)
DistributionRapidly distributed; does not cross BBB
Protein binding~4.4% bound to serum albumin
MetabolismHepatic; hydrolysis products and conjugates
EliminationRenal + biliary (fecal)
Half-life~5 hours
Bioavailability (oral)Very low (<1%) — hence parenteral form is more potent
After IV administration, hyoscine butylbromide is rapidly distributed to the target tissues (smooth muscle, ganglia).

5. Dose & Administration

RouteAdult DoseRate
IV10–20 mg (0.5–1 ampoule)1 mL/min
IM10–20 mgSlow injection
SC10–20 mgSlow injection
Max daily dose100 mg/day (5 ampoules)
  • Can be repeated if required
  • No dilution needed for the ampoule
  • IV is preferred for fastest onset in acute colic

6. Adverse Effects

Common (anticholinergic — peripheral):

  • Dry mouth (xerostomia)
  • Tachycardia ← most clinically important with injection
  • Urinary retention
  • Visual accommodation disturbances, mydriasis
  • Increased intraocular pressure
  • Decreased sweating / heat sensation (hypohidrosis)
  • Constipation

Uncommon/Rare:

  • Dizziness, flushing
  • Skin reactions (urticaria, rash, erythema, pruritus, angioedema)
  • Fixed drug eruptions
  • Anaphylaxis / anaphylactic shock (rare but potentially fatal — monitor for 30 min after injection)
  • Hypotension (especially with rapid IV injection)
Cardiac warning: Parenteral Buscopan can cause serious tachycardia and hypotension. More severe in patients with coronary artery disease, cardiac arrhythmias, hypertension, or mitral stenosis. Emergency resuscitation equipment must be available when giving IV.

7. Contraindications

ContraindicationReason
TachycardiaWorsens heart rate
Angle-closure glaucomaRaises intraocular pressure
Myasthenia gravisWorsens neuromuscular blockade
Megacolon / paralytic ileusReduces bowel motility further
Cardiac failure, anginaHemodynamic risk
Known hypersensitivity to hyoscine butylbromideAnaphylaxis risk
Prostatic hypertrophy / bladder neck obstructionUrinary retention risk
Pyloric stenosis

8. Drug Interactions

Interacting DrugEffect
TCAs (amitriptyline, etc.)↑ anticholinergic effects
Antihistamines (1st gen)↑ anticholinergic effects
Quinidine, disopyramide↑ anticholinergic effects
Amantadine↑ anticholinergic effects
Phenothiazines, butyrophenones↑ anticholinergic effects
MetoclopramideMutual antagonism — both lose GI motility effect
Beta-agonistsEnhanced tachycardia

9. Special Populations

PopulationGuidance
ElderlyPreferred over hyoscine hydrobromide (no CNS effects); use with caution for urinary retention
PregnancyUse only if clearly needed; limited data
Renal impairmentNo dose adjustment needed; dialysed
Hepatic impairmentUse with caution
ChildrenIV/IM use in children with caution; specialist guidance required

10. Overdose Management

  • Features: Exaggerated anticholinergic signs — tachycardia, urinary retention, hot dry skin, mydriasis, delirium (rare, since poor CNS penetration)
  • Antidote: Physostigmine (a reversible cholinesterase inhibitor that crosses the BBB) can be used to reverse severe anticholinergic toxidrome
  • Supportive care: catheterisation for urinary retention, cooling for hyperthermia

11. Key Clinical Pearls

  • Not to be confused with Hyoscine Hydrobromide (Kwells/Joy-rides for motion sickness) — that agent crosses the BBB and causes sedation/amnesia
  • For renal/biliary colic, IV Buscopan is often combined with an analgesic (e.g., diclofenac or morphine) for faster and more complete pain relief
  • During CT colonography and MRI enterography, IV Buscopan 20 mg reduces bowel peristalsis and improves image quality
  • In palliative care, SC infusion via syringe driver is commonly used for secretion control — equally effective as atropine and scopolamine
  • No significant CNS effects = safe to use in elderly, post-operative, and neurologically vulnerable patients

Sources: Maudsley Prescribing Guidelines in Psychiatry 15ed; Bailey & Love's Surgery 28ed; Grainger & Allison's Diagnostic Radiology; Miller's Anesthesia 10ed; Goldman-Cecil Medicine; Buscopan® Canadian Prescribing Information (Health Canada)
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