Scopolamine is available in different formulations. The most commonly used is butyl-scopolamine available by the brand name of Buscopan. It is indicated for the symptomatic treatment of abdominal cramps, intestinal and esophageal spasm, ureteric colic, and bladder spasm.

Scopolamine (Buscopan) Uses:

• Scopolamine base:

  • Transdermal: To prevent nausea/vomiting associated with motion sickness and recovery from anesthesia and surgery (other than cesarean section).

• Scopolamine hydrobromide [Canadian product]:

  • Injection: Adjunct to anesthesia to produce sedation and amnesia.

• Scopolamine butylbromide [Canadian product]:

  • Oral/injection:
    • Treatment of smooth muscle spasm of the genitourinary or GI tract;
    • The injection may also be used before radiological/diagnostic procedures to prevent spasm.

Scopolamine Dose in Adults

Note: Scopolamine (hyoscine) hydrobromide should not be interchanged with scopolamine butylbromide formulations. Dosages are not equal.

Scopolamine base:

• Preoperative:

  • Transdermal patch: Apply 1 patch to the hairless area behind the ear the night before surgery; remove 24 hours after surgery.

• Motion sickness:

  • Transdermal patch: Apply 1 patch to the hairless area behind the ear at least 4 hours prior to exposure and every 3 days as required.

Scopolamine hydrobromide [Canadian product]:

• Dose for Sedation and amnesia:

  • IM, IV, SubQ: 0.3 to 0.6 mg 3 to 4 times/day

Scopolamine butylbromide [Canadian product]:

• Dose in Gastrointestinal and genitourinary spasm:

  • Oral: Acute therapy: 10 to 20 mg/day; prolonged therapy: 10 mg 3 to 5 times/day; maximum: 60 mg/day
  • IM, IV, SubQ: 10 to 20 mg; maximum: 100 mg/day

Scopolamine Dose in Childrens

Scopolamine (Buscopan) dose as an antiemetic Preoperatively:

• Children:

  • Scopolamine hydrobromide: IM, IV, SubQ:
    • 6 mcg/kg/dose (maximum dose: 0.3 mg/dose);
    • The dose may be repeated every 6 to 8 hours.

Scopolamine (Buscopan) dose for Motion sickness: Limited data available:

• Adolescents:

  • Scopolamine base: Transdermal:
    • Apply 1 disc behind the ear at least 4 hours before exposure every 3 days as required.

Pregnancy Risk Factor C

• Scopolamine crosses over the placenta.
• Pregnant females suffering from severe preeclampsia should not use transdermal patches.
• Eclamptic seizures have been reported following IV and IM use.

Scopolamine use during breastfeeding:

• Breast milk contains Scopolamine.
• According to the manufacturer the decision about whether to continue or stop breastfeeding during therapy should be made based on the risks of infant exposure, the benefits to the infant and the benefits to the mother.
• According to the Academy of Breastfeeding Medicine, scopolamine is safe during the perioperative period. However, scopolamine can cause maternal sedation, which could adversely affect milk supply, and may lead to increased risk of scopolamine-related complications.

Scopolamine (Buscopan) Dose in Kidney Disease:

• There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).
• However, use cautiously because of increased risks of adverse effects.

Scopolamine (Buscopan) Dose in Liver disease:

• There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).
• However, use cautiously because of increased risks of adverse effects.

Common Side Effects of Scopolamine (Buscopan):

• Central nervous system:

  • Drowsiness
  • Dizziness

• Gastrointestinal:

  • Xerostomia

Less Common Side Effects of Scopolamine (Buscopan):

• Central Nervous System:

  • Agitation
  • Confusion

• Ophthalmic:

  • Visual Impairment
  • Mydriasis

• Respiratory:

  • Pharyngitis

Side effects of Scopolamine (Buscopan) - frequency of side effects not defined:

• Gastrointestinal:

  • Decreased gastrointestinal motility

• Genitourinary:

  • Urinary retention

• Ophthalmic:

  • Blurred vision

Contraindications to Scopolamine (Buscopan):

Injection:

• Hyoscine butylbromide [Canadian Product]:
  • Hypersensitivity to hyoscine bromide, atropinics or any component of this formulation
  • Untreated narrow-angle, untreated glaucoma
  • megacolon,
  • Prostatic hypertrophy and urinary retention
  • stenotic lesions, or mechanical stenosis in the GI tract
  • myasthenia gravis;
  • Tachycardia
  • Angina
  • heart failure;
  • Paralytic or obstructive intestinal ileus
  • Anticoagulant therapy patients may require IM administration
• Scopolamine hydrobromide [Canadian Product]:
  • Hypersensitivity to scopolamine and any component of the formulation
  • Predisposition to narrow-angle or glaucoma
  • paralytic ileus;
  • Prostatic hypertrophy
  • pyloric obstruction
  • Tachycardia caused by cardiac insufficiency, thyrotoxicosis

Oral [Canadian Product]:

• Hypersensitivity to hyoscine butylbromide, atropine, or any component of the formulation;
• glaucoma,
• megacolon,
• myasthenia gravis,
• Obstructive prostatic hypertrophy

Transdermal

• Hypersensitivity to scopolamine, other belladonna alkaloids, or any component of the formulation;
• Glaucoma with narrow angles

Warnings and precautions

• Anaphylaxis

  • Parenteral administration has been associated with anaphylaxis, including episodes of shock. Look out for signs and symptoms of hypersensitivity.
  • Hypersensitivity reactions may be more common in patients with asthma or allergies.

• Bradycardia (paradoxical):

  • Vagal mimetic effects may occur at lower doses (0.1 mg); these effects could be caused by an increase in vagal tone, resulting in paradoxical bradycardia.

• CNS effects

  • This may cause blurred or drowsy vision and/or drowsiness, which can lead to impairment of physical or mental capabilities.
  • Patients should be warned about tasks that require mental alertness, such as operating machinery or driving.

• Reaction idiosyncratic:

  • Rarely, patients will experience idiosyncratic symptoms. Patients may experience agitation, confusion and hallucinations.

• Visual disturbances:

  • If the patient experiences unusual visual disturbances or pain in the eye, discontinue treatment.

• Withdrawal

  • If large doses are abruptly stopped or in Parkinson's patients, adverse events such as dizziness, headaches, nausea, vomiting, and other symptoms may occur.
  • Negative events can also occur after the removal of the transdermal patches, although symptoms may not manifest until 24 hours later.

• Cardiovascular disease

  • Patients with heart disease, tachyarrhythmias or heart failure should be cautious. Before administering, evaluate for tachycardia.

• Gastrointestinal (GI) obstruction:

  • Patients with GI obstruction should be cautious. Avoid continuous (daily or prolonged) use of this medication without evaluating the cause of abdominal pain.
  • Patients should be directed to report persistent or worsening stomach pain, with or without any other symptoms (eg nausea/vomiting irregular bowel movements bloody stool, hypotension).

• Genitourinary (GU), disease/obstruction

  • Patients with GU obstruction, prostate hyperplasia, and urinary retention should be cautious.
  • Avoid continuous (daily), prolonged, or indefinite use of the GU tract for smooth muscle spasm.

• Glaucoma:

  • Patients with open-angle glaucoma should be cautious when using transdermal products. It may raise intraocular pressure. Adjust glaucoma therapy as necessary.

• Hepatic impairment

  • Patients with hepatic impairment should be cautious; adverse CNS effects are more common in these patients.

• Hiatal hernia

  • Patients with hiatal hernia and reflux esophagitis should be treated with caution.

• Hyperthyroidism:

  • Patients with hyperthyroidism should be cautious; they may be at greater risk of developing arrhythmias.

• Psychosis:

  • Patients with a history or psychosis should be cautious. It may make the condition worse.

• Renal impairment

  • Patients with kidney impairment should be cautious; adverse CNS effects are more common in these patients.

• Seizure disorders:

  • Patients with seizure disorders should be cautious. It may make the condition worse.

• Ulcerative colitis

  • Patients with ulcerative colitis should be cautious. It may cause or aggravate toxic megacolon.

Monitoring parameters:

• Body temperature,
• heart rate,
• urinary output,
• intraocular pressure

How to administer Scopolamine (Buscopan)?

Notification 

• IM, IV or SubQ injections are available for butylbromide [Canadian Product] and hydrobromide (Canadian Product].

IM: Butylbromide

• Before radiological or diagnostic procedures, intramuscular injections must be given between 10 and 15 minutes.

IV: Butylbromide

• Do not dilute before injecting; only 1 mL per minute is sufficient
• Before injecting Hydrobromide, there is no need to dilute it.

Oral [Canadian Product]:

• Take the tablet whole with a glass of water.

Transdermal

• Apply the cream to the area behind the ears.
• Only wear one patch at a given time. Remove the first and place a new patch behind each ear.
• To avoid drug contact with the eyes, use hand hygiene prior to and after you apply the patch.
• Do not trim the patch.
• The topical patch contains 1 mg for 3 days.
• Do not remove the patch after it has been applied (motion sickness).
• The patch should be removed 24 hrs after surgery if it is used for nausea or vomiting.
• Discard the damaged patch and replace it with a new one.
• After removing the patch, fold it in half and stick the sticky side together.

Mechanism of action of Scopolamine (Buscopan):

• It inhibits the action of Acetylcholine in parasympathetic sites of smooth muscle, secretory and the CNS.
• It increases cardiac output, dries out secretions, antagonizes serotonin, and causes blockade at the cardiac SA node of muscarinic receptors.
• At usual recommended doses it is parasympatholytic (ie blocks vagal activity, increasing heart rate).

The onset of action:

• Butylbromide: Injection:
  • ≤15 minutes.
• Hydrobromide: Injection:
  • ~15 minutes.
• Scopolamine base: Transdermal:
  • 6 to 8 hours.

Duration:

• Hydrobromide: Injection:
  • ~4 hours.
• Scopolamine base: Transdermal:
  • 72 hours.

Absorption:

• Butylbromide: Oral:
  • Quaternary salts are poorly absorbed (local concentrations in the GI tract following oral dosing may be high).
• Hydrobromide: IM, SubQ:
  • Rapid.

Protein binding:

• Butylbromide: ~4% (albumin).

Metabolism: Hepatic.

Bioavailability:

• Butylbromide: Oral: 8%.

Half-life elimination:

• Butylbromide: Terminal:
  • IV: ~5 hours;
  • Oral: ~6 to 11 hours.
• Hydrobromide:
  • Injection: ~1 to 3.5 hours.
• Scopolamine base:
  • Transdermal: 9.5 hours.

Time to peak:

• Butylbromide:
  • Oral:2 hours.
• Hydrobromide:
  •  IM: ~20 minutes;
  • IV: ~5 minutes;
  • SubQ: ~15 minutes.
• Scopolamine base:
  • Transdermal: 24 hours.

Excretion:

• Butylbromide: IV:
  • Urine (42% to 61% [half as parent drug]),
  • feces (28% to 37%).
• Hydrobromide: Injection:
  • Urine (variable; as parent drug and metabolites).
• Scopolamine base: Transdermal: Urine (<10%, as parent drug and metabolites).

International Brand Names of Scopolamine:

• Transderm Scop (1.5 MG)
• Ariel TDDS
• Belloid
• Boro-Scopal
• Bupasmol
• Buscapina
• Buscopan
• Buscopina
• Buscotica
• Butyl
• Cifespasma
• Colospan
• Copan
• Dhacopan
• Dormi
• Escapin
• Espasmotab
• Gascosin
• Gastride
• Hayospan
• Higan
• Hyomide
• Hyospasmol
• Kimite
• Kimite Pad
• Kimite Patch
• Kwells
• Labinpina
• Modul
• Scoburen
• Scolmin
• Scopamin
• Scopma
• Scopoderm
• Scopoderm TTS
• Scopolamine Dispersa
• Setacol
• Soonway
• Spashi
• Stomica
• Vacopan
• Vellios

Scopolamine Brand Names Pakistan: