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Pronunciation |
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(skoe
POL a
meen) |

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U.S. Brand
Names |
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Isopto® Hyoscine Ophthalmic;
Scopace® Tablet; Transderm Scop®
Patch |

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Generic
Available |
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Yes |

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Synonyms |
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Hyoscine; Scopolamine Hydrobromide |

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Pharmacological Index |
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Anticholinergic Agent |

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Use |
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Preoperative medication to produce amnesia and decrease salivary and
respiratory secretions; to produce cycloplegia and mydriasis; treatment of
iridocyclitis; prevention of motion sickness; prevention of nausea/vomiting
associated with anesthesia or opiate analgesia (patch); symptomatic treatment of
postencephalitic parkinsonism and paralysis agitans (oral); inhibits excessive
motility and hypertonus of the gastrointestinal tract in such conditions as the
irritable colon syndrome, mild dysentery, diverticulitis, pylorospasm, and
cardiospasm; it may also prevent motion sickness (oral) |

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Pregnancy Risk
Factor |
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C |

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Contraindications |
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Hypersensitivity to scopolamine or any component; narrow-angle glaucoma;
acute hemorrhage, gastrointestinal or genitourinary obstruction, thyrotoxicosis,
tachycardia secondary to cardiac insufficiency, paralytic
ileus |

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Warnings/Precautions |
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Use with caution with hepatic or renal impairment since adverse CNS effects
occur more often in these patients; use with caution in infants and children
since they may be more susceptible to adverse effects of scopolamine; use with
caution in patients with GI obstruction; anticholinergic agents are not well
tolerated in the elderly and their use should be avoided when
possible |

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Adverse
Reactions |
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Ophthalmic:
>10%: Ocular: Blurred vision, photophobia
1% to 10%:
Ocular: Local irritation, increased intraocular pressure
Respiratory: Congestion
<1%: Vascular congestion, edema, drowsiness, eczematoid dermatitis,
follicular conjunctivitis, exudate
Systemic:
>10%:
Dermatologic: Dry skin
Gastrointestinal: Constipation, xerostomia, dry throat
Local: Irritation at injection site
Respiratory: Dry nose
Miscellaneous: Diaphoresis (decreased)
1% to 10%:
Dermatologic: Increased sensitivity to light
Endocrine & metabolic: Decreased flow of breast milk
Gastrointestinal: Dysphagia
<1%: Orthostatic hypotension, ventricular fibrillation, tachycardia,
palpitations, confusion, drowsiness, headache, loss of memory, ataxia, fatigue,
rash, bloated feeling, nausea, vomiting, dysuria, weakness, increased
intraocular pain, blurred vision
Note: Systemic adverse effects have been reported following
ophthalmic administration |

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Overdosage/Toxicology |
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Symptoms of overdose include dilated pupils, flushed skin, tachycardia,
hypertension, EKG abnormalities, CNS manifestations resemble acute psychosis;
CNS depression, circulatory collapse, respiratory failure, and death can occur
Pure scopolamine intoxication is extremely rare. However, for a scopolamine
overdose with severe life-threatening symptoms, physostigmine 1-2 mg (0.5 mg or
0.02 mg/kg for children) S.C. or I.V. slowly should be given to reverse the
toxic effects. |

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Drug
Interactions |
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Decreased effect of acetaminophen, levodopa, ketoconazole, digoxin,
riboflavin, potassium chloride in wax matrix preparations
Increased toxicity: Additive adverse effects with other anticholinergic
agents; GI absorption of the following drugs may be affected: acetaminophen,
levodopa, ketoconazole, digoxin, riboflavin, potassium chloride wax-matrix
preparations |

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Stability |
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Avoid acid solutions, because hydrolysis occurs at pH <3; physically
compatible when mixed in the same syringe with atropine, butorphanol,
chlorpromazine, dimenhydrinate, diphenhydramine, droperidol, fentanyl,
glycopyrrolate, hydromorphone, hydroxyzine, meperidine, metoclopramide,
morphine, pentazocine, pentobarbital, perphenazine, prochlorperazine, promazine,
promethazine, or thiopental |

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Mechanism of
Action |
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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 |

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Pharmacodynamics/Kinetics |
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Onset of effect: Oral, I.M.: 0.5-1 hour; I.V.: 10 minutes
Duration of effect: Oral, I.M.: 4-6 hours; I.V.: 2 hours
Peak effect: 20-60 minutes; it may take 3-7 days for full recovery
Absorption: Well absorbed by all routes of administration
Protein binding: Reversibly bound to plasma proteins
Metabolism: In the liver
Elimination: In urine |

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Usual Dosage |
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Preoperatively:
Children: I.M., S.C.: 6 mcg/kg/dose (maximum: 0.3 mg/dose) or 0.2
mg/m2 may be repeated every 6-8 hours or alternatively:
4-7 months: 0.1 mg
7 months to 3 years: 0.15 mg
3-8 years: 0.2 mg
8-12 years: 0.3 mg
Adults:
I.M., I.V., S.C.: 0.3-0.65 mg; may be repeated every 4-6 hours
Transdermal patch: Apply 2.5 cm2 patch to hairless area behind ear
the night before surgery (the patch should be applied no sooner than 1 hour
before surgery for best results)
Motion sickness: Transdermal: Children >12 years and Adults: Apply 1 disc
behind the ear at least 4 hours prior to exposure and every 3 days as needed;
effective if applied as soon as 2-3 hours before anticipated need, best if 12
hours before
Ophthalmic:
Refraction:
Children: Instill 1 drop of 0.25% to eye(s) twice daily for 2 days before
procedure
Adults: Instill 1-2 drops of 0.25% to eye(s) 1 hour before procedure
Iridocyclitis:
Children: Instill 1 drop of 0.25% to eye(s) up to 3 times/day
Adults: Instill 1-2 drops of 0.25% to eye(s) up to 4 times/day
Oral: 0.4 to 0.8 mg as a range; the dosage may be cautiously increased in
parkinsonism and spastic states. |

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Mental Health: Effects
on Mental Status |
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May cause drowsiness; may rarely cause confusion or
amnesia |

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Mental Health:
Effects on Psychiatric
Treatment |
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May decrease the effects of levodopa; concurrent use with psychotropics may
produce additive sedation of anticholinergic side effects (dry
mouth) |

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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |

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Dental Health:
Effects on Dental Treatment |
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>10% of patients medicated with scopolamine patch (Transderm
Scop®) will experience significant dry mouth. This will
disappear with cessation of drug therapy. |

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Patient
Information |
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Take as directed (see below). You may experience drowsiness, confusion,
impaired judgment, or vision changes (use caution when driving or engaging in
tasks requiring alertness until response to drug is known); dry mouth, nausea,
or vomiting (small frequent meals, frequent mouth care, chewing gum, or sucking
lozenges may help); orthostatic hypotension (use caution when climbing stairs
and when rising from lying or sitting position); constipation (increased
exercise, fluid, or dietary fiber may reduce constipation, if not effective
consult prescriber); increased sensitivity to heat and decreased perspiration
(avoid extremes of heat, reduce exercise in hot weather); decreased milk if
breast-feeding. Report hot, dry, flushed skin; blurred vision or vision changes;
difficulty swallowing; chest pain, palpitations, or rapid heartbeat; painful or
difficult urination; increased confusion, depression, or loss of memory; rapid
or difficult respirations; muscle weakness or tremors; or eye pain.
Ophthalmic: Instill as often as recommended. Wash hands before using. Sit or
lie down, open eye, look at ceiling, and instill prescribed amount of solution.
Do not blink for 30 seconds, close eye and roll eye in all directions, and apply
gentle pressure to inner corner of eye for 1-2 minutes. Do not let tip of
applicator touch eye or contaminate tip of applicator. Temporary stinging or
blurred vision may occur.
Pregnancy precautions: Inform prescriber if you are or intend to be
pregnant. |

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Nursing
Implications |
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Topical disc is programmed to deliver in vivo 0.5 mg over 3 days;
wash hands before and after applying the disc to avoid drug contact with
eyes |

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Dosage Forms |
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Disc, transdermal: 1.5 mg/disc (4's)
Injection, as hydrobromide: 0.3 mg/mL (1 mL); 0.4 mg/mL (0.5 mL, 1 mL); 0.86
mg/mL (0.5 mL); 1 mg/mL (1 mL)
Solution, ophthalmic, as hydrobromide: 0.25% (5 mL, 15 mL)
Tablet: 0.4 mg |

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References |
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Bernstein S and Leff R,
"Toxic Psychosis From Sleeping Medicines Containing Scopolamine," N Engl J
Med, 1967, 277(12):638-9.
Clissold SP and Heel RC,
"Transdermal Hyoscine (Scopolamine). A Preliminary Review of Its Pharmacodynamic Properties and Therapeutic Efficacy,"
Drugs, 1985, 29(3):189-207.
Feinberg M,
"The Problems of Anticholinergic Adverse Effects in Older Patients," Drugs
Aging, 1993, 3(4):335-48.
Grunberg SM and Hesketh PJ, "Control of Chemotherapy-Induced Emesis," N
Engl J Med, 1993, 329(24):1790-6.
Hesketh PJ,
"Treatment of Chemotherapy-Induced Emesis in the 1990s: Impact of the 5-HT3 Receptor Antagonists,"
Support Care Cancer, 1994, 2(5):286-92.
Hooper RG, Conner CS, and Rumack BH,
"Acute Poisoning From Over-The-Counter Sleep Preparations," JACEP, 1979,
8(3):98-100.
Hughes SS and Zaloga GP, "Scopolamine Anisocaria," Ann Emerg Med,
1989, 18(4):423-4.
Osterholm RK and Camoriano JK, "Transdermal Scopolamine Psychosis,"
JAMA, 1982, 247(22):3081.
Tavorath R and Hesketh PJ,
"Drug Treatment of Chemotherapy-Induced Delayed Emesis," Drugs, 1996,
52(5):639-48.
Tortorice PV and O'Connell MB,
"Management of Chemotherapy-Induced Nausea and Vomiting,"
Pharmacotherapy, 1990, 10(2):129-45. |

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