Dosage guidance:
Dosing: Each transdermal patch delivers ~1 mg scopolamine base over 3 days.
Dosage form information: In Canada, additional formulations include parenteral and oral scopolamine butylbromide (also known as hyoscine butylbromide) as well as parenteral scopolamine hydrobromide (also known as hyoscine hydrobromide). Scopolamine butylbromide and scopolamine hydrobromide formulations are not equivalent and are not interchangeable on a milligram-to-milligram basis.
Clinical considerations: Parenteral scopolamine hydrobromide is approved in Canada for preoperative reduction of oropharyngeal secretions and as an adjunct to anesthesia for sedation and amnesia; however, these uses may no longer represent current clinical practice (Ref); refer to manufacturer's labeling for additional information. Scopolamine butylbromide salt is a quaternary derivative with fewer CNS effects compared with scopolamine hydrobromide and base (patch) formulations (Ref).
Gastrointestinal/genitourinary spasm:
Note: American College of Gastroenterology guidelines recommend against use of antispasmodics such as scopolamine for treatment of global symptoms of irritable bowel syndrome (IBS) (Ref).
Scopolamine (hyoscine) butylbromide [Canadian product]: Oral: 10 to 20 mg 3 to 5 times/day as needed; maximum: 60 mg/day (Ref). Note: When used for chronic symptom control, 10 mg 3 to 5 times/day as needed is recommended (Ref).
Scopolamine (hyoscine) butylbromide [Canadian product]: IM/IV/SUBQ: 10 to 20 mg once; if needed, may repeat at intervals of ≥30 minutes; maximum: 100 mg/day. Note: To avoid a potentially severe infusion reaction (ie, hypotension), a maximum rate of 20 mg/minute is preferred.
Malignant bowel obstruction, inoperable (off-label use):
Note: Decreases gastric secretions, nausea, and vomiting; often given as part of a combination regimen (eg, with analgesic, antiemetic, or corticosteroid) (Ref).
Scopolamine (hyoscine) butylbromide [Canadian product]: SUBQ : Initial: 20 mg once followed by 60 mg over 24 hours as a continuous SUBQ infusion (Ref).
Motion sickness, prevention:
Scopolamine base: Transdermal: Apply 1 patch (1 mg/3 days) behind ear at least 4 hours prior to required antiemetic effect for use up to 72 hours; if needed for >72 hours, remove old patch and place new one behind other ear. If symptoms are not adequately controlled with use of 1 patch, may consider using 2 patches (Ref).
Postoperative nausea and/or vomiting, prevention:
Scopolamine base: Transdermal: Apply 1 patch (1 mg/3 days) behind ear at least 1 to 2 hours prior to anesthesia or night before, and remove 24 hours after procedure (Ref).
Sialorrhea (alternative agent) (off-label use):
Note: May be used to control excessive salivation associated with neuromuscular disorders (eg, cerebral palsy, amyotrophic lateral sclerosis [ALS]) (Ref).
Scopolamine base: Transdermal: Apply 1 patch (1 mg/3 days) behind ear; after 3 days, remove old patch and place new one behind other ear (Ref).
Terminal airway secretions (death rattle) (off-label use) (alternative agent):
Note: Does not dry secretions already present and typically ineffective for lower respiratory tract secretions (Ref).
Scopolamine base: Transdermal: Apply 1 patch (1 mg/3 days) behind ear for up to 72 hours; if needed for >72 hours, remove old patch and place new one behind other ear (Ref).
Scopolamine (hyoscine) butylbromide [Canadian product]: Various regimens described; refer to local protocols. Example regimens include: SUBQ: 20 mg every 4 to 6 hours as needed. Alternatively, administer 20 mg once followed by a continuous SUBQ infusion of 20 to 60 mg over 24 hours (Ref).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
The renal dosing recommendations are based upon the best available evidence and clinical expertise. Senior Editorial Team: Bruce Mueller, PharmD, FCCP, FASN, FNKF; Jason A. Roberts, PhD, BPharm (Hons), B App Sc, FSHP, FISAC; Michael Heung, MD, MS.
Altered kidney function:
Oral: Scopolamine (hyoscine) butylbromide [Canadian product]: No dosage adjustment likely to be necessary due to limited systemic absorption (Ref).
Parenteral: Scopolamine (hyoscine) butylbromide [Canadian product]: There are no specific dosage adjustments provided in the manufacturer's labeling (has not been studied). Use with caution (~42% to 61% of a total dose is excreted in the urine) with frequent monitoring for adverse effects. If using for >48 hours in patients with eGFR <50 mL/minute/1.73 m2, consider reducing the dose or prolonging the dosing interval to prevent accumulation (Ref).
Transdermal: Scopolamine base: No dosage adjustment likely to be necessary (<10% of a total dose is excreted in the urine) (Ref). Use with caution and frequent monitoring in patients with severe kidney disease due to possible increased risk of CNS adverse effects (Ref).
Hemodialysis, intermittent (thrice weekly): Dialyzability unknown:
Oral: Scopolamine (hyoscine) butylbromide [Canadian product] : No dosage adjustment likely to be necessary due to limited systemic absorption (Ref).
Parenteral: Scopolamine (hyoscine) butylbromide [Canadian product] : There are no specific dosage adjustments provided in the manufacturer's labeling (has not been studied); use with caution (~42% to 61% of a total dose is excreted in the urine) with frequent monitoring for adverse effects. If using for >48 hours, consider reducing the dose or prolonging the dosing interval to prevent accumulation (Ref).
Transdermal: Scopolamine base: No dosage adjustment likely to be necessary (<10% of a total dose is excreted in the urine) (Ref). Use with caution with frequent monitoring for adverse effects due to possible increased risk of CNS adverse effects (manufacturer's labeling); a case of ventricular tachycardia has also been reported in a patient with end-stage kidney disease (ESKD) and concomitant hepatic dysfunction (Ref).
Peritoneal dialysis: Dialyzability unknown:
Oral: Scopolamine (hyoscine) butylbromide [Canadian product] : No dosage adjustment likely to be necessary due to limited systemic absorption (Ref).
Parenteral: Scopolamine (hyoscine) butylbromide [Canadian product] : There are no specific dosage adjustments provided in the manufacturer's labeling (has not been studied); use with caution (~42% to 61% of a total dose is excreted in the urine) with frequent monitoring for adverse effects. If using for >48 hours, consider reducing the dose or prolonging the dosing interval to prevent accumulation (Ref).
Transdermal: Scopolamine base: No dosage adjustment likely to be necessary (<10% of a total dose is excreted in the urine) (Ref). Use with caution with frequent monitoring for adverse effects due to possible increased risk of CNS adverse effects (Ref); a case of ventricular tachycardia has also been reported in a patient with ESKD and concomitant hepatic dysfunction (Ref).
CRRT:
Oral: Scopolamine (hyoscine) butylbromide [Canadian product] : No dosage adjustment likely to be necessary due to limited systemic absorption (Ref).
Parenteral: Scopolamine (hyoscine) butylbromide [Canadian product] : There are no specific dosage adjustments provided in the manufacturer's labeling (has not been studied); use with caution with frequent monitoring for adverse effects. If using for >48 hours, consider reducing the dose or prolonging the dosing interval to prevent accumulation (Ref).
Transdermal: Scopolamine base: No dosage adjustment likely to be necessary (Ref).
PIRRT (eg, sustained, low-efficiency diafiltration):
Oral: Scopolamine (hyoscine) butylbromide [Canadian product] : No dosage adjustment likely to be necessary due to limited systemic absorption (Ref).
Parenteral: Scopolamine (hyoscine) butylbromide [Canadian product] : There are no specific dosage adjustments provided in the manufacturer's labeling (has not been studied); use with caution with frequent monitoring for adverse effects. If using for >48 hours, consider reducing the dose or prolonging the dosing interval to prevent accumulation (Ref).
Transdermal: Scopolamine base: No dosage adjustment likely to be necessary (Ref).
There are no dosage adjustments provided in the manufacturer's labeling (has not been studied). However, caution is recommended due to increased risks of adverse effects.
Avoid use (Ref).
(For additional information see "Scopolamine (hyoscine): Pediatric drug information")
Dosage guidance:
Dosing: Dosing presented is for scopolamine (hyoscine) hydrobromide; it should not be interchanged with scopolamine butylbromide formulations. Transdermal patch is designed to deliver 1 mg over 3 days. Do not cut patch to obtain smaller increments; remove only portions of the backing required for the dose (eg, if 1/2 patch is needed, remove only 1/2 of the backing prior to application), cover with occlusive dressing to keep in place (Ref).
Chronic drooling: Limited data available: Children ≥3 years and Adolescents: Transdermal: Initial: Apply 1/4 patch every 3 days for 1 week; may titrate to effect (control of secretions) by increasing by 1/4 patch every 7 days as tolerated. Maximum dose: 1 patch applied every 3 days (Ref).
Dosing based on retrospective and prospective studies. In one study, patients weighing ≥10 kg with neurodisabilities and chronic drooling (n=85, median age: 4.9 years, range: 3 to 14.5 years) were randomized to receive glycopyrrolate or scopolamine patches. Medications were titrated to effect at weekly intervals. While both glycopyrrolate and scopolamine controlled secretions, scopolamine was associated with more adverse reactions such as skin reactions, gait disturbances, and hyperactivity (Ref). In another study, children with developmental delay and chronic drooling (n=10, ages: 5 to 18 years) received scopolamine patches or placebo for 2 weeks, followed by a 1 week washout and then scopolamine patches or placebo for 2 weeks. Doses were initiated at a full patch. Scopolamine showed a significant reduction in drooling. Adverse effects reported were pupil dilation, skin reactions, and increased oral mouthing behaviors (Ref).
Postoperative nausea and vomiting, prevention: Limited data available:
Children <2 years: Transdermal: Apply 1/4 patch the evening before surgery (Ref).
Children ≥2 to 6 years: Transdermal: Apply 1/2 patch the evening before surgery (Ref).
Children ≥6 to 12 years: Transdermal: Apply 1/2 to 1 patch the evening before surgery (Ref).
Children ≥12 years and Adolescents: Transdermal: Apply 1 patch the evening before surgery (Ref).
Dosing based on 2 small, placebo-controlled studies. In the first study, patients undergoing strabismus surgery received scopolamine (n=25, age: 5.7 ± 2.9 years) or placebo (n=25, age: 5.3 ± 2.7 years) the evening prior to surgery. Children <2 years of age received 1/4 patch and children 2 to 11 years of age received 1/2 patch. Patients receiving scopolamine experienced less vomiting (16% compared to 48%) and only experienced 1 episode of vomiting, compared to the placebo group which experienced 1 to 7 episodes of vomiting. No side effects were observed (Ref). In another study, patients undergoing abdominal surgery received scopolamine (n=20, ages: 6.3 to 14.1 years) or placebo (n=20, ages: 7.2 to 14.3 years) at the start of surgery. Scopolamine was associated with a significant reduction in nausea and vomiting compared to placebo. Dry mouth was more common in patients receiving scopolamine on days 2 and 3 post-op, and 1 patient reported hallucinations on day 3, thought to be caused by scopolamine (Ref).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
There are no dosage adjustments provided in the manufacturer's labeling. However, caution is recommended due to increased risks of adverse effects.
There are no dosage adjustments provided in the manufacturer's labeling. However, caution is recommended due to increased risks of adverse effects.
Scopolamine is associated with anticholinergic effects, including xerostomia (Ref), visual disturbances (eg, blurred vision, mydriasis) (Ref), and urinary retention (Ref) in adult and pediatric patients. Anticholinergic effects may contribute to nonadherence or discontinuation (Ref).
Mechanism: Related to the pharmacologic action. Directly related to antagonism of muscarinic receptors (Ref).
Onset: Rapid; visual disturbances occurred within 1 to 2 days of patch application (Ref).
Risk factors:
• Concurrent medications that cause anticholinergic adverse reactions (eg, antihistamines, meclizine, tricyclic antidepressants, muscle relaxants)
• Older patients (Ref)
• Pediatric patients (Ref)
CNS effects such as drowsiness and fatigue may occur with scopolamine (Ref).
Mechanism: Related to the pharmacologic action. Directly related to the antagonism of muscarinic receptors (Ref).
Risk factors:
• Concurrent alcohol or medications that cause CNS effects (eg, sedatives, hypnotics, opiates, anxiolytics)
• Older patients (Ref)
• Pediatric patients (Ref)
Scopolamine may cause psychiatric effects, including acute psychosis (ie, delusion, hallucination), amnesia/memory impairment, agitation, confusion, and speech disturbance in adult and pediatric patients (Ref). Psychiatric effects are rare and reversible with discontinuation; may take 1 to 2 days to resolve following discontinuation (Ref).
Mechanism: Dose-related; related to the pharmacologic action. Directly related to the antagonism of muscarinic receptors (Ref).
Onset: Rapid; abnormal behaviors and psychosis may begin within 1 to 3 days of patch application (Ref).
Risk factors:
• Higher doses (Ref)
• Cognitive impairment or dementia (Ref)
• Older patients (Ref)
• Pediatric patients (Ref)
Withdrawal symptoms following scopolamine discontinuation may include diaphoresis, dizziness, drowsiness, fatigue, headache, hypotension, and nausea in adult and pediatric patients (Ref). Resolution of symptoms occurs within several days to weeks (Ref).
Mechanism: Withdrawal; may be related to muscarinic receptor sensitization, leading to rebound overstimulation of the vestibular nuclei and reticular formation of the vomiting center with discontinuation (Ref).
Onset: Rapid; occurs within 18 to 72 hours after removal of the patch (Ref).
Risk factors:
• Prolonged use (≥3 days) (Ref)
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Adverse reactions reported with transdermal administration. Reported adverse reactions are for adults.
>10%:
Gastrointestinal: Xerostomia (29% to 67%) (table 1)
Drug (Scopolamine) |
Placebo |
Indication |
Number of Patients (Scopolamine) |
Number of Patients (Placebo) |
Comments |
---|---|---|---|---|---|
67% |
N/A |
Nausea and vomiting associated with motion sickness |
N/A |
N/A |
~2/3 |
29% |
16% |
Post-operative nausea and vomiting |
461 |
457 |
N/A |
Nervous system: Dizziness (12%) (table 2) , drowsiness (8% to 17%) (table 3)
Drug (Scopolamine) |
Placebo |
Indication |
Number of Patients (Scopolamine) |
Number of Patients (Placebo) |
---|---|---|---|---|
12% |
7% |
Post-operative nausea and vomiting |
461 |
457 |
Drug (Scopolamine) |
Placebo |
Indication |
Number of Patients (Scopolamine) |
Number of Patients (Placebo) |
Comments |
---|---|---|---|---|---|
17% |
N/A |
Nausea and vomiting associated with motion sickness |
N/A |
N/A |
<1/6 |
8% |
4% |
Post-operative nausea and vomiting |
461 |
457 |
N/A |
1% to 10%:
Nervous system: Agitation (6%) (table 4) , confusion (4%) (table 5)
Drug (Scopolamine) |
Placebo |
Indication |
Number of Patients (Scopolamine) |
Number of Patients (Placebo) |
---|---|---|---|---|
6% |
4% |
Post-operative nausea and vomiting |
461 |
457 |
Drug (Scopolamine) |
Placebo |
Indication |
Number of Patients (Scopolamine) |
Number of Patients (Placebo) |
---|---|---|---|---|
4% |
3% |
Post-operative nausea and vomiting |
461 |
457 |
Ophthalmic: Mydriasis (4%) (table 6) , visual impairment (5%) (table 7)
Drug (Scopolamine) |
Placebo |
Indication |
Number of Patients (Scopolamine) |
Number of Patients (Placebo) |
---|---|---|---|---|
4% |
0% |
Post-operative nausea and vomiting |
461 |
457 |
Drug (Scopolamine) |
Placebo |
Indication |
Number of Patients (Scopolamine) |
Number of Patients (Placebo) |
---|---|---|---|---|
5% |
3% |
Post-operative nausea and vomiting |
461 |
457 |
Respiratory: Pharyngitis (3%)
Postmarketing:
Cardiovascular: Hypotension (associated with withdrawal) (Manno 2015)
Dermatologic: Diaphoresis (associated with withdrawal) (Manno 2015), erythema of skin, skin irritation, skin rash
Gastrointestinal: Nausea (associated with withdrawal) (Manno 2015)
Genitourinary: Dysuria, urinary retention (Apfel 2010)
Local: Application-site burning
Nervous system: Acute psychosis (Seo 2009), amnesia (Cissold 1985), ataxia (Seo 2009), delirium (Lin 2014, Rozzini 1988), delusion (Seo 2009), disorientation (Seo 2009), disturbance in attention, fatigue (Clissold 1985), hallucination (Seo 2009), headache (Seo 2009), insomnia (Seo 2009), memory impairment (Seo 2009), paranoid ideation, restlessness (Seo 2009), seizure, speech disturbance, vertigo
Ophthalmic: Amblyopia, angle-closure glaucoma, blurred vision (Nachum 2006), dry eye syndrome, eye pruritus, eyelid pain (irritation), strabismus (Good 1996)
Injection:
Hyoscine butylbromide [Canadian product]: Hypersensitivity to hyoscine butylbromide, atropinics, or any component of the formulation; untreated narrow-angle glaucoma; megacolon, prostatic hypertrophy with urinary retention; stenotic lesions or mechanical stenosis of the GI tract; myasthenia gravis; tachycardia, angina, heart failure; paralytic or obstructive ileus; IM administration in patients receiving anticoagulant therapy.
Scopolamine hydrobromide [Canadian product]: Hypersensitivity to scopolamine or any component of the formulation; glaucoma or predisposition to narrow-angle glaucoma; paralytic ileus; prostatic hypertrophy; pyloric obstruction; tachycardia secondary to cardiac insufficiency or thyrotoxicosis.
Oral [Canadian product]: Hypersensitivity to hyoscine butylbromide, atropinics, or any component of the formulation; glaucoma, megacolon, mechanical stenosis in the GI tract, myasthenia gravis, obstructive prostatic hypertrophy, paralytic or obstructive ileus.
Transdermal: Hypersensitivity to scopolamine, other belladonna alkaloids, or any component of the formulation; narrow-angle glaucoma
Concerns related to adverse effects:
• Anaphylaxis: Anaphylaxis including episodes of shock has been reported following parenteral administration; observe for signs/symptoms of hypersensitivity following parenteral administration. Patients with a history of allergies or asthma may be at increased risk of hypersensitivity reactions.
• Bradycardia (paradoxical): Lower doses (0.1mg) may have vagal mimetic effects (eg, increase vagal tone causing paradoxical bradycardia); these effects are likely mediated by blockade of muscarinic receptors at the level of the brain.
Disease-related concerns:
• Cardiovascular disease: Use with caution in patients with coronary artery disease, tachyarrhythmias, heart failure, or hypertension; evaluate tachycardia prior to administration.
• Gastrointestinal (GI) obstruction: Use with caution in patients with GI obstruction; when used for the treatment of smooth muscle spasm of the GI tract avoid continuous (daily) or prolonged use without evaluating source of abdominal pain. Patients should be instructed to report persistent or worsening abdominal pain with or without other symptoms (eg, nausea/vomiting, irregular bowel movements, bloody stool, hypotension).
• Genitourinary (GU) disease/obstruction: Use with caution in patients with GU obstruction, prostatic hyperplasia, or urinary retention; when used for the treatment of smooth muscle spasm of the GU tract, avoid continuous (daily) or prolonged use without evaluating source of the spasm.
• Glaucoma: Use transdermal product with caution in patients with open-angle glaucoma; may increase intraocular pressure; adjust glaucoma therapy as necessary.
• Hepatic impairment: Use with caution in patients with hepatic impairment.
• Hiatal hernia: Use with caution in patients with hiatal hernia with reflux esophagitis.
• Hyperthyroidism: Use caution in patients with hyperthyroidism; may have increased risk for arrhythmias.
• Parkinson disease: Adverse events (including dizziness, headache, nausea, vomiting) may occur following abrupt discontinuation in patients with Parkinson disease.
• Psychosis: Use with caution in patients with a history of psychosis; may exacerbate condition.
• Renal impairment: Use with caution in patients with renal impairment.
• Seizure disorders: Use with caution in patients with a history of seizure disorder; may exacerbate condition.
• Ulcerative colitis: Use with caution in patients with ulcerative colitis; may precipitate/aggravate toxic megacolon.
Special populations:
• Pediatric: Use with caution in pediatric patients since they may be more susceptible to the anticholinergic, neurologic, and psychiatric adverse reactions of scopolamine.
Dosage form specific issues:
• Fructose: Tablets may contain sucrose; avoid use of tablets in patients who are fructose intolerant.
• Product interchangeability: Scopolamine (hyoscine) hydrobromide should not be interchanged with scopolamine butylbromide formulations; dosages are not equivalent.
• Transdermal patch: May contain conducting metal (eg, aluminum); remove patch prior to MRI.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Patch 72 Hour, Transdermal:
Transderm Scop (1.5 MG): 1 MG/3DAYS (4 ea [DSC])
Transderm-Scop: 1 MG/3DAYS (1 ea, 10 ea, 24 ea)
Generic: 1 MG/3DAYS (4 ea, 10 ea, 24 ea)
Yes
Patch, 72-hour (Scopolamine Transdermal)
1 mg/3days (per each): $22.97 - $24.28
Patch, 72-hour (Transderm-Scop Transdermal)
1 mg/3days (per each): $25.56
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution, Injection, as butylbromide:
Buscopan: 20 mg/mL (1 mL)
Generic: 20 mg/mL (1 mL)
Solution, Injection, as hydrobromide:
Generic: 0.4 mg/mL (1 mL); 0.6 mg/mL (1 mL)
Tablet, Oral, as butylbromide:
Buscopan: 10 mg [contains corn starch]
Generic: 10 mg
Note: Butylbromide [Canadian product] or hydrobromide [Canadian product] may be administered by IM, IV, or SubQ injection.
IM: Butylbromide: Intramuscular injections should be administered 10 to 15 minutes prior to radiological/diagnostic procedures.
IV:
Butylbromide: No dilution is necessary prior to injection; inject at a rate of 1 mL/minute
Hydrobromide: No dilution is necessary prior to injection.
Oral [Canadian product]: Tablet should be swallowed whole and taken with a full glass of water.
Transdermal: Apply to hairless area of skin behind the ear. Wear only one patch at a time; remove first patch and apply new patch behind the other ear. Wash hands before and after applying the patch to avoid drug contact with eyes. Do not cut the patch. Once patch has been affixed behind the ear, do not touch while being worn since pressure may cause scopolamine to release at the edge. Topical patch is programmed to deliver 1 mg over 3 days. Once applied, do not remove the patch for 3 full days (motion sickness). When used postoperatively for nausea/vomiting, the patch should be removed 24 hours after surgery. If patch becomes displaced, discard and apply a new patch. Once removed, fold the used patch in half with the sticky side together; dispose of used patches in the trash out of reach from children and pets.
Transdermal: Apply patch to hairless area behind 1 ear. Do not wear more than 1 patch at a time. Wash hands before and after application of disc to avoid drug contact with eyes. Transdermal patch is designed to deliver 1 mg over 3 days. Do not use any patch that has been damaged, cut, or manipulated in any way. If necessary to use smaller patch increments, do not cut patch; remove only portions of the backing required for the dose (eg, if 1/2 patch is needed, remove only 1/2 of the backing prior to application), cover with occlusive dressing to keep in place (Ref). If patch becomes displaced, discard and apply a new patch behind the other ear. Once removed, fold the used patch in half with the sticky side together; dispose of used patches in the trash out of reach from children and pets.
Gastrointestinal/genitourinary spasm (scopolamine butylbromide [Canadian product]): Treatment of abdominal spasms and pain and discomfort in the stomach, bowels, and biliary tract; prevention of spasm prior to radiological or diagnostic procedures. May also be used off label for management of pain associated with smooth muscle spasms in the urinary tract (Tytgat 2007).
Motion sickness, prevention (scopolamine base): Prevention of nausea and vomiting associated with motion sickness.
Postoperative nausea and/or vomiting, prevention (scopolamine base): Prevention of postoperative nausea and vomiting associated with recovery from anesthesia or opioid analgesia and surgery.
Malignant bowel obstruction, inoperable; Sialorrhea; Terminal airway secretions (death rattle)
Beers Criteria: Scopolamine is identified in the Beers Criteria as a potentially inappropriate medication to be avoided in patients 65 years and older (independent of diagnosis or condition) due to its highly anticholinergic properties and uncertain effectiveness as an antispasmodic (Beers Criteria [AGS 2023]).
Transdermal patch may contain conducting metal (eg, aluminum); remove patch prior to MRI.
None known.
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Acetylcholinesterase Inhibitors: May diminish the therapeutic effect of Anticholinergic Agents. Anticholinergic Agents may diminish the therapeutic effect of Acetylcholinesterase Inhibitors. Risk C: Monitor therapy
Aclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination
Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Risk C: Monitor therapy
Alizapride: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Amantadine: May enhance the anticholinergic effect of Anticholinergic Agents. Risk C: Monitor therapy
Anticholinergic Agents: May enhance the adverse/toxic effect of other Anticholinergic Agents. Risk C: Monitor therapy
Azelastine (Nasal): May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination
Blonanserin: CNS Depressants may enhance the CNS depressant effect of Blonanserin. Management: Use caution if coadministering blonanserin and CNS depressants; dose reduction of the other CNS depressant may be required. Strong CNS depressants should not be coadministered with blonanserin. Risk D: Consider therapy modification
Botulinum Toxin-Containing Products: May enhance the anticholinergic effect of Anticholinergic Agents. Risk C: Monitor therapy
Brexanolone: CNS Depressants may enhance the CNS depressant effect of Brexanolone. Risk C: Monitor therapy
Brimonidine (Topical): May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Bromopride: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Bromperidol: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination
Buprenorphine: CNS Depressants may enhance the CNS depressant effect of Buprenorphine. Management: Consider reduced doses of other CNS depressants, and avoiding such drugs in patients at high risk of buprenorphine overuse/self-injection. Initiate buprenorphine at lower doses in patients already receiving CNS depressants. Risk D: Consider therapy modification
Cannabinoid-Containing Products: Anticholinergic Agents may enhance the tachycardic effect of Cannabinoid-Containing Products. Risk C: Monitor therapy
Cannabinoid-Containing Products: CNS Depressants may enhance the CNS depressant effect of Cannabinoid-Containing Products. Risk C: Monitor therapy
Chloral Betaine: May enhance the adverse/toxic effect of Anticholinergic Agents. Risk C: Monitor therapy
Chlormethiazole: May enhance the CNS depressant effect of CNS Depressants. Management: Monitor closely for evidence of excessive CNS depression. The chlormethiazole labeling states that an appropriately reduced dose should be used if such a combination must be used. Risk D: Consider therapy modification
Chlorphenesin Carbamate: May enhance the adverse/toxic effect of CNS Depressants. Risk C: Monitor therapy
Chlorprothixene: Anticholinergic Agents may enhance the anticholinergic effect of Chlorprothixene. Risk C: Monitor therapy
Cimetropium: Anticholinergic Agents may enhance the anticholinergic effect of Cimetropium. Risk X: Avoid combination
CloZAPine: Anticholinergic Agents may enhance the constipating effect of CloZAPine. Management: Consider alternatives to this combination whenever possible. If combined, monitor closely for signs and symptoms of gastrointestinal hypomotility and consider prophylactic laxative treatment. Risk D: Consider therapy modification
CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Risk C: Monitor therapy
Daridorexant: May enhance the CNS depressant effect of CNS Depressants. Management: Dose reduction of daridorexant and/or any other CNS depressant may be necessary. Use of daridorexant with alcohol is not recommended, and the use of daridorexant with any other drug to treat insomnia is not recommended. Risk D: Consider therapy modification
DexmedeTOMIDine: CNS Depressants may enhance the CNS depressant effect of DexmedeTOMIDine. Management: Monitor for increased CNS depression during coadministration of dexmedetomidine and CNS depressants, and consider dose reductions of either agent to avoid excessive CNS depression. Risk D: Consider therapy modification
Difelikefalin: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Dimethindene (Topical): May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Doxylamine: CNS Depressants may enhance the CNS depressant effect of Doxylamine. Risk C: Monitor therapy
DroPERidol: May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (eg, opioids, barbiturates) with concomitant use. Risk D: Consider therapy modification
Eluxadoline: Anticholinergic Agents may enhance the constipating effect of Eluxadoline. Risk X: Avoid combination
Esketamine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Flunarizine: CNS Depressants may enhance the CNS depressant effect of Flunarizine. Risk X: Avoid combination
Flunitrazepam: CNS Depressants may enhance the CNS depressant effect of Flunitrazepam. Management: Reduce the dose of CNS depressants when combined with flunitrazepam and monitor patients for evidence of CNS depression (eg, sedation, respiratory depression). Use non-CNS depressant alternatives when available. Risk D: Consider therapy modification
Gastrointestinal Agents (Prokinetic): Anticholinergic Agents may diminish the therapeutic effect of Gastrointestinal Agents (Prokinetic). Risk C: Monitor therapy
Glucagon: Anticholinergic Agents may enhance the adverse/toxic effect of Glucagon. Specifically, the risk of gastrointestinal adverse effects may be increased. Risk C: Monitor therapy
Glycopyrrolate (Oral Inhalation): Anticholinergic Agents may enhance the anticholinergic effect of Glycopyrrolate (Oral Inhalation). Risk X: Avoid combination
Glycopyrronium (Topical): May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination
HydrOXYzine: May enhance the CNS depressant effect of CNS Depressants. Management: Consider a decrease in the CNS depressant dose, as appropriate, when used together with hydroxyzine. Increase monitoring of signs/symptoms of CNS depression in any patient receiving hydroxyzine together with another CNS depressant. Risk D: Consider therapy modification
Ipratropium (Oral Inhalation): May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination
Itopride: Anticholinergic Agents may diminish the therapeutic effect of Itopride. Risk C: Monitor therapy
Ixabepilone: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Kava Kava: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Kratom: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination
Lemborexant: May enhance the CNS depressant effect of CNS Depressants. Management: Dosage adjustments of lemborexant and of concomitant CNS depressants may be necessary when administered together because of potentially additive CNS depressant effects. Close monitoring for CNS depressant effects is necessary. Risk D: Consider therapy modification
Levosulpiride: Anticholinergic Agents may diminish the therapeutic effect of Levosulpiride. Risk X: Avoid combination
Lisuride: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Lofexidine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Magnesium Sulfate: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Methotrimeprazine: CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants. Management: Reduce the usual dose of CNS depressants by 50% if starting methotrimeprazine until the dose of methotrimeprazine is stable. Monitor patient closely for evidence of CNS depression. Risk D: Consider therapy modification
Metoclopramide: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
MetyroSINE: CNS Depressants may enhance the sedative effect of MetyroSINE. Risk C: Monitor therapy
Mianserin: May enhance the anticholinergic effect of Anticholinergic Agents. Risk C: Monitor therapy
Minocycline (Systemic): May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Mirabegron: Anticholinergic Agents may enhance the adverse/toxic effect of Mirabegron. Risk C: Monitor therapy
Nabilone: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination
Nitroglycerin: Anticholinergic Agents may decrease the absorption of Nitroglycerin. Specifically, anticholinergic agents may decrease the dissolution of sublingual nitroglycerin tablets, possibly impairing or slowing nitroglycerin absorption. Risk C: Monitor therapy
Olopatadine (Nasal): May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination
Opioid Agonists: CNS Depressants may enhance the CNS depressant effect of Opioid Agonists. Management: Avoid concomitant use of opioid agonists and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Risk D: Consider therapy modification
Orphenadrine: CNS Depressants may enhance the CNS depressant effect of Orphenadrine. Risk X: Avoid combination
Oxatomide: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination
Oxomemazine: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination
Oxybate Salt Products: CNS Depressants may enhance the CNS depressant effect of Oxybate Salt Products. Management: Consider alternatives to this combination when possible. If combined, dose reduction or discontinuation of one or more CNS depressants (including the oxybate salt product) should be considered. Interrupt oxybate salt treatment during short-term opioid use Risk D: Consider therapy modification
OxyCODONE: CNS Depressants may enhance the CNS depressant effect of OxyCODONE. Management: Avoid concomitant use of oxycodone and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Risk D: Consider therapy modification
Paraldehyde: CNS Depressants may enhance the CNS depressant effect of Paraldehyde. Risk X: Avoid combination
Perampanel: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Piribedil: CNS Depressants may enhance the CNS depressant effect of Piribedil. Risk C: Monitor therapy
Potassium Chloride: Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Chloride. Management: Patients on drugs with substantial anticholinergic effects should avoid using any solid oral dosage form of potassium chloride. Risk X: Avoid combination
Potassium Citrate: Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Citrate. Management: Patients on drugs with substantial anticholinergic effects should avoid using any solid oral dosage form of potassium citrate. Risk X: Avoid combination
Pramipexole: CNS Depressants may enhance the sedative effect of Pramipexole. Risk C: Monitor therapy
Pramlintide: May enhance the anticholinergic effect of Anticholinergic Agents. These effects are specific to the GI tract. Risk X: Avoid combination
Procarbazine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Ramosetron: Anticholinergic Agents may enhance the constipating effect of Ramosetron. Risk C: Monitor therapy
Revefenacin: Anticholinergic Agents may enhance the anticholinergic effect of Revefenacin. Risk X: Avoid combination
Rivastigmine: Anticholinergic Agents may diminish the therapeutic effect of Rivastigmine. Rivastigmine may diminish the therapeutic effect of Anticholinergic Agents. Management: Use of rivastigmine with an anticholinergic agent is not recommended unless clinically necessary. If the combination is necessary, monitor for reduced anticholinergic effects. Risk D: Consider therapy modification
Ropeginterferon Alfa-2b: CNS Depressants may enhance the adverse/toxic effect of Ropeginterferon Alfa-2b. Specifically, the risk of neuropsychiatric adverse effects may be increased. Management: Avoid coadministration of ropeginterferon alfa-2b and other CNS depressants. If this combination cannot be avoided, monitor patients for neuropsychiatric adverse effects (eg, depression, suicidal ideation, aggression, mania). Risk D: Consider therapy modification
ROPINIRole: CNS Depressants may enhance the sedative effect of ROPINIRole. Risk C: Monitor therapy
Rotigotine: CNS Depressants may enhance the sedative effect of Rotigotine. Risk C: Monitor therapy
Rufinamide: May enhance the adverse/toxic effect of CNS Depressants. Specifically, sleepiness and dizziness may be enhanced. Risk C: Monitor therapy
Secretin: Anticholinergic Agents may diminish the therapeutic effect of Secretin. Management: Avoid concomitant use of anticholinergic agents and secretin. Discontinue anticholinergic agents at least 5 half-lives prior to administration of secretin. Risk D: Consider therapy modification
Suvorexant: CNS Depressants may enhance the CNS depressant effect of Suvorexant. Management: Dose reduction of suvorexant and/or any other CNS depressant may be necessary. Use of suvorexant with alcohol is not recommended, and the use of suvorexant with any other drug to treat insomnia is not recommended. Risk D: Consider therapy modification
Thalidomide: CNS Depressants may enhance the CNS depressant effect of Thalidomide. Risk X: Avoid combination
Thiazide and Thiazide-Like Diuretics: Anticholinergic Agents may increase the serum concentration of Thiazide and Thiazide-Like Diuretics. Risk C: Monitor therapy
Tiotropium: Anticholinergic Agents may enhance the anticholinergic effect of Tiotropium. Risk X: Avoid combination
Topiramate: Anticholinergic Agents may enhance the adverse/toxic effect of Topiramate. Risk C: Monitor therapy
Trimeprazine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Umeclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination
Valerian: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Zolpidem: CNS Depressants may enhance the CNS depressant effect of Zolpidem. Management: Reduce the Intermezzo brand sublingual zolpidem adult dose to 1.75 mg for men who are also receiving other CNS depressants. No such dose change is recommended for women. Avoid use with other CNS depressants at bedtime; avoid use with alcohol. Risk D: Consider therapy modification
Zuranolone: May enhance the CNS depressant effect of CNS Depressants. Management: Consider alternatives to the use of zuranolone with other CNS depressants or alcohol. If combined, consider a zuranolone dose reduction and monitor patients closely for increased CNS depressant effects. Risk D: Consider therapy modification
Scopolamine crosses the placenta.
When the transdermal patch is used to prevent nausea and vomiting associated with surgery, dose adjustments are required prior to cesarean delivery. Avoid use of transdermal patches in pregnant patients with severe preeclampsia; eclamptic seizures have been reported after IV and IM use.
Scopolamine is present in breast milk.
According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and benefits of treatment to the mother. The Academy of Breastfeeding Medicine (ABM) states that scopolamine used as an antiemetic in the perioperative period is likely safe; however, because scopolamine may cause maternal sedation and adversely affect milk supply with repeated doses, other agents may be preferred (ABM [Reece-Stremtan 2017]).
Body temperature, heart rate, urinary output, intraocular pressure, mental alertness.
Blocks the action of acetylcholine at parasympathetic sites in smooth muscle, secretory glands and the CNS; increases cardiac output, dries secretions, antagonizes histamine and serotonin; at usual recommended doses, causes blockade of muscarinic receptors at the cardiac SA-node and is parasympatholytic (ie, blocks vagal activity increasing heart rate)
Onset of action:
Butylbromide: Injection: ≤15 minutes.
Hydrobromide: Injection: ~15 minutes (Renner 2005).
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.
Distribution: Vd: Butylbromide: 128 L.
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 (Renner 2005).
Scopolamine base: Transdermal: 9.5 hours.
Time to peak:
Butylbromide: Oral: ~2 hours.
Hydrobromide: IM: ~20 minutes; IV: ~5 minutes; SubQ: ~15 minutes (Renner 2005).
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) (Renner 2005).
Scopolamine base: Transdermal: Urine (<10%, as parent drug and metabolites).
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