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Scopolamine (Systemic)

Pronunciation

Pronunciation

(skoe POL a meen)

Index Terms

  • Hyoscine Butylbromide
  • Scopolamine Base
  • Scopolamine Butylbromide
  • Scopolamine Hydrobromide

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Patch 72 Hour, Transdermal:

Transderm-Scop (1.5 MG): 1 MG/3DAYS (1 ea, 4 ea, 10 ea, 24 ea)

Solution, Injection, as hydrobromide:

Generic: 0.4 mg/mL (1 mL)

Brand Names: U.S.

  • Transderm-Scop (1.5 MG)

Pharmacologic Category

  • Anticholinergic Agent

Pharmacology

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)

Absorption

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

Distribution

Vd: Butylbromide: 128 L

Metabolism

Hepatic

Excretion

Urine (<10%, as parent drug and metabolites); IV: butylbromide: Urine (42% to 61%, half as parent drug); feces (28% to 37%)

Onset of Action

Oral, IM: 0.5 to 1 hour; IV: 10 minutes; Transdermal: 6 to 8 hours

Time to Peak

Hydrobromide: IM: ~20 minutes, SubQ: ~15 minutes; Butylbromide: Oral: ~2 hours; Scopolamine base: Transdermal: 24 hours

Duration of Action

IM: 4 to 6 hours; IV: 2 hours; Transdermal: 72 hours

Half-Life Elimination

Butylbromide: ~5 to 11 hours; Hydrobromide: ~1 to 4 hours; Scopolamine base: 9.5 hours

Protein Binding

Butylbromide: ~4% (albumin)

Use: Labeled Indications

Scopolamine base: Transdermal: Prevention of nausea/vomiting associated with motion sickness and recovery from anesthesia and surgery

Scopolamine hydrobromide: Injection: Preoperative medication to produce amnesia, sedation, tranquilization, antiemetic effects, and decrease salivary and respiratory secretions

Scopolamine butylbromide [Canadian product]: Oral/injection: Treatment of smooth muscle spasm of the genitourinary or gastrointestinal tract; injection may also be used prior to radiological/diagnostic procedures to prevent spasm

Use: Unlabeled

Scopolamine base: Transdermal: Breakthrough treatment of nausea and vomiting associated with chemotherapy

Contraindications

Transdermal, oral: Hypersensitivity to scopolamine, other belladonna alkaloids, or any component of the formulation; narrow-angle glaucoma

Injection: Hypersensitivity to scopolamine, other belladonna alkaloids, or any component of the formulation; narrow-angle glaucoma; chronic lung disease (repeated administration)

Canadian labeling: Additional contraindications (not in U.S. labeling):

Oral: Glaucoma, megacolon, myasthenia gravis, obstructive prostatic hypertrophy

Injection:

Hyoscine butylbromide: Untreated narrow-angle glaucoma; megacolon, prostatic hypertrophy with urinary retention; stenotic lesions of the GI tract; myasthenia gravis; tachycardia, angina, or heart failure; IM administration in patients receiving anticoagulant therapy

Scopolamine hydrobromide: Glaucoma or predisposition to narrow-angle glaucoma; paralytic ileus; prostatic hypertrophy; pyloric obstruction; tachycardia secondary to cardiac insufficiency or thyrotoxicosis

Dosing: Adult

Note: Scopolamine injection is no longer available in the US.

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

Scopolamine base:

Preoperative: Transdermal patch: Apply 1 patch to hairless area behind ear the night before surgery or 1 hour prior to cesarean section (apply no sooner than 1 hour before surgery to minimize newborn exposure); remove 24 hours after surgery

Motion sickness: Transdermal patch: Apply 1 patch to hairless area behind the ear at least 4 hours prior to exposure and every 3 days as needed; effective if applied as soon as 2 to 3 hours before anticipated need, best if 12 hours before

Chemotherapy-induced nausea and vomiting, breakthrough (off-label use): Apply 1 patch every 72 hours (NCCN Antiemesis guidelines v.1.2012)

Scopolamine hydrobromide:

Antiemetic: SubQ: 0.6 to 1 mg

Preoperative: IM, IV, SubQ: 0.3 to 0.65 mg

Sedation, tranquilization: IM, IV, SubQ:

U.S. labeling: 0.6 mg 3 to 4 times/day

Canadian labeling: 0.3 to 0.6 mg 3 to 4 times/day

Scopolamine butylbromide [Canadian product]: Gastrointestinal/genitourinary spasm:

Oral: Acute therapy: 10 to 20 mg daily (1 to 2 tablets); prolonged therapy: 10 mg (1 tablet) 3 to 5 times/day; maximum: 60 mg/day

IM, IV, SubQ: 10 to 20 mg; maximum: 100 mg/day

Dosing: Geriatric

Lower dosages may be required. Refer to adult dosing.

Dosing: Pediatric

Note: Scopolamine injection is no longer available in the US.

Scopolamine hydrobromide:

Antiemetic: SubQ: 0.006 mg/kg

Preoperative: IM, IV, SubQ:

Children 6 months to 3 years: 0.1 to 0.15 mg

Children 3 to 6 years: 0.2-0.3 mg

Dosing: Renal Impairment

No dosage adjustment provided in manufacturer’s labeling. However, caution is recommended due to increased risks of adverse effects.

Dosing: Hepatic Impairment

No dosage adjustment provided in manufacturer’s labeling. However, caution is recommended due to increased risks of adverse effects.

Reconstitution

Solution for injection:

IM: Butylbromide: No dilution required.

IV:

Butylbromide: No dilution is necessary prior to injection.

Hydrobromide: Dilute with an equal volume of sterile water.

Administration

Note: Butylbromide or hydrobromide may be administered by IM, IV, or SubQ injection.

IM: Butylbromide: Intramuscular injections should be administered 10-15 minutes prior to radiological/diagnostic procedures.

IV:

Butylbromide: No dilution is necessary prior to injection; inject at a rate of 1 mL/minute

Hydrobromide: Dilute with an equal volume of sterile water and administer by direct IV; inject over 2-3 minutes

Oral: Tablet should be swallowed whole and taken with a full glass of water.

Transdermal: Apply to hairless area of skin behind the ear. Wash hands before and after applying the disc to avoid drug contact with eyes. Do not use any patch that has been damaged, cut, or manipulated in any way. 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. Dispose of used or unused patches in the trash out of reach from children and pets.

Compatibility

Butylbromide injection: Stable in D5W, NS, D10W, LR, Ringer's solution.

Hydrobromide injection: Avoid acid solutions.

Storage

Solution for injection:

Butylbromide [Canadian product]: Store at room temperature. Do not freeze. Protect from light and heat. Stable in D5W, D10W, NS, Ringer's solution, and LR for up to 8 hours.

Hydrobromide: Store at room temperature of 20°C to 25°C (68°F to 77°F). Protect from light. Avoid acid solutions; hydrolysis occurs at pH <3.

Tablet [Canadian product]: Store at room temperature. Protect from light and heat.

Transdermal system: Store at 20°C to 25°C (68°F to 77°F).

Drug Interactions

AbobotulinumtoxinA: Anticholinergic Agents may enhance the anticholinergic effect of AbobotulinumtoxinA. Monitor therapy

Acetylcholinesterase Inhibitors: Anticholinergic Agents may diminish the therapeutic effect of Acetylcholinesterase Inhibitors. Acetylcholinesterase Inhibitors may diminish the therapeutic effect of Anticholinergic Agents. Monitor therapy

Aclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Avoid combination

Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Monitor therapy

Analgesics (Opioid): CNS Depressants may enhance the CNS depressant effect of Analgesics (Opioid). Management: Avoid concomitant use of opioid analgesics 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. Consider therapy modification

Anticholinergic Agents: May enhance the adverse/toxic effect of other Anticholinergic Agents. Monitor therapy

Azelastine (Nasal): CNS Depressants may enhance the CNS depressant effect of Azelastine (Nasal). Avoid combination

Blonanserin: CNS Depressants may enhance the CNS depressant effect of Blonanserin. Consider therapy modification

Brimonidine (Topical): May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

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 patches (Butrans brand) at 5 mcg/hr in adults when used with other CNS depressants. Consider therapy modification

Cannabis: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Chloral Betaine: May enhance the adverse/toxic effect of Anticholinergic Agents. Monitor therapy

Chlorphenesin Carbamate: May enhance the adverse/toxic effect of CNS Depressants. Monitor therapy

Cimetropium: Anticholinergic Agents may enhance the anticholinergic effect of Cimetropium. Avoid combination

CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Monitor therapy

Dimethindene (Systemic): May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Doxylamine: May enhance the CNS depressant effect of CNS Depressants. Management: The manufacturer of Diclegis (doxylamine/pyridoxine), intended for use in pregnancy, specifically states that use with other CNS depressants is not recommended. Monitor therapy

Dronabinol: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Droperidol: May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (e.g., opioids, barbiturates) with concomitant use. Consider therapy modification

Eluxadoline: Anticholinergic Agents may enhance the constipating effect of Eluxadoline. Avoid combination

Flunitrazepam: CNS Depressants may enhance the CNS depressant effect of Flunitrazepam. Consider therapy modification

Gastrointestinal Agents (Prokinetic): Anticholinergic Agents may diminish the therapeutic effect of Gastrointestinal Agents (Prokinetic). Monitor therapy

Glucagon: Anticholinergic Agents may enhance the adverse/toxic effect of Glucagon. Specifically, the risk of gastrointestinal adverse effects may be increased. Avoid combination

Glycopyrrolate (Oral Inhalation): Anticholinergic Agents may enhance the anticholinergic effect of Glycopyrrolate (Oral Inhalation). Avoid combination

HYDROcodone: CNS Depressants may enhance the CNS depressant effect of HYDROcodone. Management: Avoid concomitant use of hydrocodone 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. Consider therapy modification

HydrOXYzine: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Ipratropium (Oral Inhalation): May enhance the anticholinergic effect of Anticholinergic Agents. Avoid combination

Itopride: Anticholinergic Agents may diminish the therapeutic effect of Itopride. Monitor therapy

Kava Kava: May enhance the adverse/toxic effect of CNS Depressants. Monitor therapy

Levosulpiride: Anticholinergic Agents may diminish the therapeutic effect of Levosulpiride. Avoid combination

Lofexidine: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Magnesium Sulfate: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Methotrimeprazine: May enhance the CNS depressant effect of CNS Depressants. CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Management: Reduce adult dose of CNS depressant agents by 50% with initiation of concomitant methotrimeprazine therapy. Further CNS depressant dosage adjustments should be initiated only after clinically effective methotrimeprazine dose is established. Consider therapy modification

MetyroSINE: CNS Depressants may enhance the sedative effect of MetyroSINE. Monitor therapy

Mianserin: May enhance the anticholinergic effect of Anticholinergic Agents. Monitor therapy

Minocycline: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Mirabegron: Anticholinergic Agents may enhance the adverse/toxic effect of Mirabegron. Monitor therapy

Mirtazapine: CNS Depressants may enhance the CNS depressant effect of Mirtazapine. Monitor therapy

Nabilone: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

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. Avoid combination

OnabotulinumtoxinA: Anticholinergic Agents may enhance the anticholinergic effect of OnabotulinumtoxinA. Monitor therapy

Orphenadrine: CNS Depressants may enhance the CNS depressant effect of Orphenadrine. Avoid combination

Oxatomide: May enhance the anticholinergic effect of Anticholinergic Agents. Avoid combination

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. Consider therapy modification

Paraldehyde: CNS Depressants may enhance the CNS depressant effect of Paraldehyde. Avoid combination

Perampanel: May enhance the CNS depressant effect of CNS Depressants. Management: Patients taking perampanel with any other drug that has CNS depressant activities should avoid complex and high-risk activities, particularly those such as driving that require alertness and coordination, until they have experience using the combination. Consider therapy modification

Piribedil [INT]: CNS Depressants may enhance the CNS depressant effect of Piribedil [INT]. 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. Avoid combination

Pramipexole: CNS Depressants may enhance the sedative effect of Pramipexole. Monitor therapy

Pramlintide: May enhance the anticholinergic effect of Anticholinergic Agents. These effects are specific to the GI tract. Consider therapy modification

Ramosetron: Anticholinergic Agents may enhance the constipating effect of Ramosetron. Monitor therapy

RimabotulinumtoxinB: Anticholinergic Agents may enhance the anticholinergic effect of RimabotulinumtoxinB. Monitor therapy

ROPINIRole: CNS Depressants may enhance the sedative effect of ROPINIRole. Monitor therapy

Rotigotine: CNS Depressants may enhance the sedative effect of Rotigotine. Monitor therapy

Rufinamide: May enhance the adverse/toxic effect of CNS Depressants. Specifically, sleepiness and dizziness may be enhanced. Monitor therapy

Secretin: Anticholinergic Agents may diminish the therapeutic effect of Secretin. Management: Avoid using drugs with substantial anticholinergic effects in patients receiving secretin whenever possible. If such agents must be used in combination, monitor closely for a diminished response to secretin. Consider therapy modification

Selective Serotonin Reuptake Inhibitors: CNS Depressants may enhance the adverse/toxic effect of Selective Serotonin Reuptake Inhibitors. Specifically, the risk of psychomotor impairment may be enhanced. Monitor therapy

Sodium Oxybate: May enhance the CNS depressant effect of CNS Depressants. Management: Consider alternatives to combined use. When combined use is needed, consider minimizing doses of one or more drugs. Use of sodium oxybate with alcohol or sedative hypnotics is contraindicated. 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. Consider therapy modification

Tapentadol: May enhance the CNS depressant effect of CNS Depressants. Management: Avoid concomitant use of tapentadol 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. Consider therapy modification

Tetrahydrocannabinol: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Thalidomide: CNS Depressants may enhance the CNS depressant effect of Thalidomide. Avoid combination

Thiazide and Thiazide-Like Diuretics: Anticholinergic Agents may increase the serum concentration of Thiazide and Thiazide-Like Diuretics. Monitor therapy

Tiotropium: Anticholinergic Agents may enhance the anticholinergic effect of Tiotropium. Avoid combination

Topiramate: Anticholinergic Agents may enhance the adverse/toxic effect of Topiramate. Monitor therapy

Trimeprazine: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Umeclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Avoid combination

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. Consider therapy modification

Test Interactions

Interferes with gastric secretion test

Adverse Reactions

Frequency not defined.

Cardiovascular: Bradycardia, flushing, orthostatic hypotension, tachycardia

Central nervous system: Amnesia, ataxia, confusion, disorientation, dizziness, drowsiness, fatigue, headache, heat intolerance, irritability, restlessness, sedation

Dermatologic: Dyshidrotic eczema, erythema, hypohidrosis, pruritus, skin rash (including drug eruption), urticaria, xeroderma

Endocrine & metabolic: Increased thirst

Gastrointestinal: Constipation, diarrhea, dysphagia, nausea, vomiting, xerostomia

Genitourinary: Dysuria, urinary retention

Hypersensitivity: Angioedema, hypersensitivity reaction

Neuromuscular & skeletal: Tremor, weakness

Ophthalmic: angle-closure glaucoma, blurred vision, conjunctival infection, cycloplegia, decreased accommodation, eye pain (intraocular), eye pruritus, mydriasis, photophobia, retinal pigment changes, xerophthalmia

Respiratory: Dry nose, dry throat, dyspnea

<1% (Limited to important or life-threatening): Agitation, anaphylaxis, anaphylactic shock, delusions, hallucination, paranoia, toxic psychosis (acute)

Warnings/Precautions

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.

• CNS effects: May cause drowsiness and/or blurred vision, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).

• Idiosyncratic reaction: Idiosyncratic reactions may rarely occur; patients may experience acute toxic psychosis, agitation, confusion, delusions, hallucinations, paranoid behavior, and rambling speech.

• Visual disturbances: Discontinue if patient reports unusual visual disturbances or pain within the eye.

• Withdrawal: Adverse events (including dizziness, headache, nausea, vomiting) may occur following abrupt discontinuation of large doses or in patients with Parkinson’s disease; adverse events may also occur following removal of the transdermal patch although symptoms may not appear until ≥24 hours after removal.

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 of the transdermal product in patients with open-angle glaucoma may necessitate adjustments in glaucoma therapy.

• Hepatic impairment: Use with caution in patients with hepatic impairment; adverse CNS effects occur more often in these patients.

• 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.

• Psychosis: Use with caution in patients with a history of psychosis; may exacerbate condition.

• Renal impairment: Use with caution in patients with renal impairment; adverse CNS effects occur more often in these patients.

• 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.

Concurrent drug therapy issues:

• Sedatives: Effects with other sedative drugs or ethanol may be potentiated.

Special populations:

• Pediatric: Use with caution in infants and children since they may be more susceptible to adverse effects.

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.

Monitoring Parameters

Body temperature, heart rate, urinary output, intraocular pressure

Pregnancy Risk Factor

C

Pregnancy Considerations

Adverse events were observed in some animal reproduction studies. Scopolamine crosses the placenta; may cause respiratory depression and/or neonatal hemorrhage when used during pregnancy. Transdermal scopolamine has been used as an adjunct to epidural anesthesia for cesarean delivery without adverse CNS effects on the newborn. Parenteral administration does not increase the duration of labor or affect uterine contractions. Except when used prior to cesarean section, use during pregnancy only if the benefit to the mother outweighs the potential risk to the fetus.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience dizziness, fatigue, dry mouth, sensitivity to light, pharyngitis, agitation, or injection site irritation. Have patient report immediately to prescriber confusion, difficult urination, vision changes, eye pain, severe eye irritation, enlarged pupils, mood changes, difficulty speaking, hallucinations, memory impairment, severe abdominal pain, severe vomiting, or severe nausea (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.

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