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Pronunciation
(hye oh SYE a meen)
Generic Available (U.S.)
Yes: Excludes chewable/disintegrating, dispersible, and variable release tablets, and injection
Index Terms
Brand Names: U.S.
Brand Names: Canada
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Oral: Adjunctive therapy for peptic ulcers, irritable bowel, neurogenic bladder/bowel; treatment of infant colic, GI tract disorders caused by spasm; to reduce rigidity, tremors, sialorrhea, and hyperhidrosis associated with parkinsonism; as a drying agent in acute rhinitis
Injection: Preoperative antimuscarinic to reduce secretions and block cardiac vagal inhibitory reflexes; to improve radiologic visibility of the kidneys; symptomatic relief of biliary and renal colic; reduce GI motility to facilitate diagnostic procedures (ie, endoscopy, hypotonic duodenography); reduce pain and hypersecretion in pancreatitis, certain cases of partial heart block associated with vagal activity; reversal of neuromuscular blockade
Pregnancy Risk Factor
C
Pregnancy Considerations
Crosses the placenta, effects to the fetus not known; use during pregnancy only if clearly needed.
Lactation
Enters breast milk/not recommended
Breast-Feeding Considerations
Excreted in breast milk in trace amounts. May also suppress lactation. Breast-feeding is not recommended.
Contraindications
Hypersensitivity to belladonna alkaloids or any component of the formulation; glaucoma; obstructive uropathy; myasthenia gravis; obstructive GI tract disease, paralytic ileus, intestinal atony of elderly or debilitated patients, severe ulcerative colitis, toxic megacolon complicating ulcerative colitis; unstable cardiovascular status in acute hemorrhage, myocardial ischemia
Warnings/Precautions
Concerns related to adverse effect:
• 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).
• Diarrhea: May be a sign of incomplete intestinal obstruction, treatment should be discontinued if this occurs.
• Heat prostration: May occur in the presence of increased environmental temperature; use caution in hot weather and/or exercise.
• Psychosis: Has been reported in patients with an extreme sensitivity to anticholinergic effects.
Disease-related concerns:
• Cardiovascular disease: Use with caution in patients with coronary artery disease, tachyarrhythmias, heart failure, or hypertension; evaluate tachycardia prior to administration.
• Hiatal hernia: Use with caution in patients with hiatal hernia with reflux esophagitis.
• Hyperthyroidism: Use with caution in patients with hyperthyroidism.
• Neuropathy: Use with caution in patients with autonomic neuropathy.
• Prostatic hyperplasia: Use with caution in patients with prostatic hyperplasia.
• Renal impairment: Use with caution in patients with renal impairment.
Special populations:
• Elderly: Avoid long-term use in this age group due to anticholinergic adverse effects and uncertain effectiveness (Beers Criteria). May severely impair memory function (especially in those patients with previous memory problems).
• Pediatrics: Use with caution in children with spastic paralysis.
Dosage form specific issues:
• Phenylalanine: NuLev™ contains phenylalanine.
Adverse Reactions
Frequency not defined.
Cardiovascular: Palpitation, tachycardia
Central nervous system: Ataxia, dizziness, drowsiness, headache, insomnia, mental confusion/excitement, nervousness, speech disorder
Dermatologic: Urticaria
Endocrine & metabolic: Lactation suppression
Gastrointestinal: Bloating, constipation, dry mouth, loss of taste, nausea, vomiting
Genitourinary: Impotence, urinary hesitancy, urinary retention
Neuromuscular & skeletal: Weakness
Ocular: Blurred vision, cycloplegia, increased ocular tension, mydriasis
Miscellaneous: Allergic reactions, sweating decreased
Metabolism/Transport Effects
None known.
Drug Interactions
AbobotulinumtoxinA: Anticholinergic Agents may enhance the anticholinergic effect of AbobotulinumtoxinA. Risk C: Monitor therapy
Acetylcholinesterase Inhibitors (Central): Anticholinergics may diminish the therapeutic effect of Acetylcholinesterase Inhibitors (Central). Acetylcholinesterase Inhibitors (Central) may diminish the therapeutic effect of Anticholinergics. If the anticholinergic action is a side effect of the agent, the result may be beneficial. Risk C: Monitor therapy
Anticholinergics: May enhance the adverse/toxic effect of other Anticholinergics. Exceptions: Levocabastine (Nasal); Paliperidone. Risk C: Monitor therapy
Cannabinoids: Anticholinergic Agents may enhance the tachycardic effect of Cannabinoids. Risk C: Monitor therapy
OnabotulinumtoxinA: Anticholinergic Agents may enhance the anticholinergic effect of OnabotulinumtoxinA. Risk C: Monitor therapy
Potassium Chloride: Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Chloride. Risk D: Consider therapy modification
Pramlintide: May enhance the anticholinergic effect of Anticholinergics. These effects are specific to the GI tract. Risk D: Consider therapy modification
RimabotulinumtoxinB: Anticholinergic Agents may enhance the anticholinergic effect of RimabotulinumtoxinB. Risk C: Monitor therapy
Secretin: Anticholinergic Agents may diminish the therapeutic effect of Secretin. Risk D: Consider therapy modification
Storage
Store at controlled room temperature.
Mechanism of Action
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
Pharmacodynamics/Kinetics
Onset of action: 2-3 minutes
Duration: 4-6 hours
Absorption: Well absorbed
Distribution: Crosses placenta; small amounts enter breast milk
Protein binding: 50%
Metabolism: Hepatic
Half-life elimination: 3-5 hours
Excretion: Urine
Dosage
Oral: Children: Gastrointestinal disorders: Dose as listed, based on age and weight (kg) using 0.125 mg/mL drops; repeat dose every 4 hours as needed:
Children <2 years:
3.4 kg: 4 drops; maximum: 24 drops/24 hours
5 kg: 5 drops; maximum: 30 drops/24 hours
7 kg: 6 drops; maximum: 36 drops/24 hours
10 kg: 8 drops; maximum: 48 drops/24 hours
Oral, S.L.:
Children 2-12 years: Gastrointestinal disorders: Dose as listed, based on age and weight (kg); repeat dose every 4 hours as needed:
10 kg: 0.031-0.033 mg; maximum: 0.75 mg/24 hours
20 kg: 0.0625 mg; maximum: 0.75 mg/24 hours
40 kg: 0.0938 mg; maximum: 0.75 mg/24 hours
50 kg: 0.125 mg; maximum: 0.75 mg/24 hours
Children >12 years and Adults: Gastrointestinal disorders: 0.125-0.25 mg every 4 hours or as needed (before meals or food); maximum: 1.5 mg/24 hours
Oral (timed release): Children >12 years and Adults: Gastrointestinal disorders: 0.375-0.75 mg every 12 hours; maximum: 1.5 mg/24 hours
I.M., I.V., SubQ: Children >12 years and Adults: Gastrointestinal disorders: 0.25-0.5 mg; may repeat as needed up to 4 times/day, at 4-hour intervals
I.V.: Children >2 year and Adults: I.V.: Preanesthesia: 5 mcg/kg given 30-60 minutes prior to induction of anesthesia or at the time preoperative narcotics or sedatives are administered
I.V.: Adults: Diagnostic procedures: 0.25-0.5 mg given 5-10 minutes prior to procedure
To reduce drug-induced bradycardia during surgery: 0.125 mg; repeat as needed
To reverse neuromuscular blockade: 0.2 mg for every 1 mg neostigmine (or the physostigmine/pyridostigmine equivalent)
Administration: Oral
Oral: Tablets should be administered before meals or food.
Levbid®: Tablets are scored and may be broken in half for dose titration; do not crush or chew.
Levsin/SL®: Tablets may be used sublingually, chewed, or swallowed whole.
Symax® SL: Tablets may be used sublingually or swallowed whole.
Administration: I.M.
May be administered without dilution.
Administration: I.V.
Inject over at least 1 minute. May be administered without dilution.
Administration: I.V. Detail
May be administered undiluted.
Dietary Considerations
Should be taken before meals or food
Patient Education
Take before meals. Do not crush or chew extended release form; swallow whole. You may experience dizziness, blurred vision, dry mouth, photosensitivity, decreased ability to sweat, or impotence (temporary). Report excessive and persistent anticholinergic effects (blurred vision, headache, flushing, tachycardia, nervousness, constipation, dizziness, insomnia, mental confusion or excitement, dry mouth, altered taste perception, dysphagia, palpitations, bradycardia, urinary hesitancy or retention, impotence, decreased sweating).
Geriatric Considerations
Avoid long-term use; the potential for toxic reactions is higher than the potential benefit, elderly are particularly prone to CNS side effects of anticholinergics (eg, confusion, delirium, hallucinations). Side effects often occur before clinical response is obtained.
This medication is considered to be potentially inappropriate in this patient population (Beers Criteria severity: High).
Dental Health: Effects on Dental Treatment
Key adverse event(s) related to dental treatment: Xerostomia (normal salivary flow resumes upon discontinuation).
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
May cause drowsiness; may rarely cause restlessness, amnesia, or delirium
Mental Health: Effects on Psychiatric Treatment
Concurrent use with psychotropics may produce additive sedation and dry mouth
Nursing: Physical Assessment/Monitoring
Assess potential for interactions with any drugs that may add to anticholinergic effects. I.V./I.M.: Have patient void before administration. Monitor for excessive dryness of eyes, nose, mouth, or throat.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Elixir, oral, as sulfate: 0.125 mg/5 mL (473 mL)
Hyosyne: 0.125 mg/5 mL (473 mL) [contains ethanol 20%, sodium benzoate; orange-lemon flavor]
Injection, solution, as sulfate:
Levsin®: 0.5 mg/mL (1 mL)
Solution, oral, as sulfate [drops]: 0.125 mg/mL (15 mL)
Hyosyne: 0.125 mg/mL (15 mL) [contains ethanol 5%, sodium benzoate; orange-lemon flavor]
Tablet, oral, as sulfate: 0.125 mg
Levsin®: 0.125 mg
Tablet, sublingual, as sulfate: 0.125 mg
HyoMax®-SL: 0.125 mg [peppermint flavor]
Levsin®/SL: 0.125 mg
Oscimin: 0.125 mg [peppermint flavor]
Symax® SL: 0.125 mg
Tablet, chewable/disintegrating, oral, as sulfate:
HyoMax™-FT: 0.125 mg [mint flavor]
NuLev®: 0.125 mg [peppermint flavor]
Oscimin: 0.125 mg [peppermint flavor]
Symax® FasTab: 0.125 mg [mint flavor]
Tablet, dispersible, oral, as sulfate:
Oscimin: 0.125 mg [peppermint flavor]
Tablet, extended release, oral, as sulfate: 0.375 mg
Levbid®: 0.375 mg
Oscimin: 0.375 mg
Tablet, orally disintegrating, oral, as sulfate: 0.125 mg
Anaspaz®: 0.125 mg [scored]
Tablet, sustained release, oral, as sulfate: 0.375 mg
HyoMax® -SR: 0.375 mg [scored]
Symax® SR: 0.375 mg
Tablet, variable release, oral:
HyoMax™-DT: Hyoscyamine sulfate 0.125 mg [immediate release] and hyoscyamine sulfate 0.25 mg [sustained release]
Symax® DuoTab: Hyoscyamine sulfate 0.125 mg [immediate release] and hyoscyamine sulfate 0.25 mg [sustained release]
Pricing: U.S. (www.drugstore.com)
Sublingual (HyoMax-SL)
0.125 mg (100): $79.99
Sublingual (Hyoscyamine Sulfate)
0.125 mg (30): $26.99
Sublingual (Levsin/SL)
0.13 mg (100): $140.99
Sublingual (Symax-SL)
0.125 mg (30): $98.70
Tablet, 12-hour (HyoMax-SR)
0.375 mg (100): $145.99
Tablet, 12-hour (Hyoscyamine Sulfate CR)
0.375 mg (30): $37.99
Tablet, 12-hour (Levbid)
0.38 mg (30): $73.49
Tablet, controlled release (Symax Duotab)
0.375 mg (30): $73.99
Tablet, orally-disintegrating (Anaspaz)
0.125 mg (100): $35.92
Tablet, orally-disintegrating (Hyoscyamine Sulfate)
0.125 mg (100): $82.99
Tablets (Hyoscyamine Sulfate)
0.125 mg (30): $31.99
Tablets (Levsin)
0.13 mg (90): $112.99
References
Boyson SJ, “Bethanechol for Anticholinergic Side Effects,” Ann Neurol, 1988, 23(4):422-3.
Shutt LE and Bowes JB, “Atropine and Hyoscine,” Anaesthesia, 1979, 34(5):476-90.
International Brand Names
Lexi-Comp.com
Last full review/revision January 2012
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