Yes

Anticholinergic Agent

Treatment of GI tract disorders caused by spasm, adjunctive therapy for peptic ulcers

C

Narrow-angle glaucoma, obstructive uropathy, obstructive GI tract disease, myasthenia gravis, known hypersensitivity to belladonna alkaloids

Use with caution in children with spastic paralysis; use with caution in elderly patients. Low doses cause a paradoxical decrease in heart rates. Some commercial products contain sodium metabisulfite, which can cause allergic-type reactions. May accumulate with multiple inhalational administration, particularly in the elderly. Heat prostration may occur in hot weather. Use with caution in patients with autonomic neuropathy, prostatic hypertrophy, hyperthyroidism, congestive heart failure, cardiac arrhythmias, chronic lung disease, biliary tract disease.

>10%:

Dermatologic: Dry skin

Gastrointestinal: Dry throat, xerostomia

Local: Irritation at injection site

Respiratory: Dry nose

Miscellaneous: Diaphoresis (decreased)

1% to 10%:

Dermatologic: Photosensitivity

Gastrointestinal: Constipation, dysphagia

Ocular: Blurred vision, mydriasis

<1%: Palpitations, orthostatic hypotension, headache, lightheadedness, memory loss, fatigue, delirium, restlessness, ataxia, rash, dysuria, tremor, increased intraocular pressure

Symptoms of overdose include dilated, unreactive pupils; blurred vision; hot, dry flushed skin; dryness of mucous membranes; difficulty in swallowing, foul breath, diminished or absent bowel sounds, urinary retention, tachycardia, hyperthermia, hypertension, increased respiratory rate

Anticholinergic toxicity is caused by strong binding of the drug to cholinergic receptors. Anticholinesterase inhibitors reduce acetylcholinesterase, the enzyme that breaks down acetylcholine and thereby allows acetylcholine to accumulate and compete for receptor binding with the offending anticholinergic. For anticholinergic 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 may be given to reverse these effects.

Decreased effect with antacids

Increased toxicity with amantadine, antimuscarinics, haloperidol, phenothiazines, TCAs, MAO inhibitors

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

Onset of effect: 2-3 minutes

Duration: 4-6 hours

Absorption: Oral: Absorbed well

Distribution: Crosses the placenta; small amounts appear in breast milk

Protein binding: 50%

Metabolism: In the liver

Half-life: 13% to 38%

Elimination: In urine

Children: Oral, S.L.: Dose as listed, based on age (y) and weight (kg). Repeat dose every 4 hours as needed:

Children <2 years:

2.3 kg:

12.5 mcg; maximum 75mcg/24 hours

3.4 kg:

16.7 mcg; maximum 100 mcg/24 hours

5 kg:

20.8 mcg; maximum 125 mcg/24 hours

7 kg:

25 mcg; maximum 150 mcg/24 hours

10 kg:

31.3-33.3 mcg; maximum 200 mcg/24 hours

15 kg:

45.8 mcg; maximum 275 mcg/24 hour

Children 2-10 years:

10 kg:

31.3-33.3 mcg; do not exceed 0.75 mg/24 hours

20 kg:

62.5 mcg; do not exceed 0.75 mg/24 hours

40 kg:

93.8 mcg; do not exceed 0.75 mg/24 hours

50 kg:

125 mcg; do not exceed 0.75 mg/24 hours

Adults:

Oral or S.L.: 0.125-0.25 mg 3-4 times/day before meals or food and at bedtime

Oral: 0.375-0.75 mg (timed release) every 12 hours

I.M., I.V., S.C.: 0.25-0.5 mg every 6 hours

Should be administered before meals or food

May cause drowsiness; may rarely cause restlessness, amnesia, or delirium

Concurrent use with psychotropics may produce additive sedation and dry mouth

No information available to require special precautions

>10% of patients experience dry mouth (normal salivary flow returns with cessation of drug therapy)

Take as directed before meals; do not increase dose and do not discontinue without consulting prescriber. Void before taking medication. You may experience dizziness or blurred vision (use caution when driving or engaging in tasks that require alertness until response to drug is known); dry mouth (sucking on lozenges may help); photosensitivity (wear dark glasses in bright sunlight); or impotence (temporary). Report chest pain or palpitations, or excessive and persistent anticholinergic effects (blurred vision, headache, flushing, tachycardia, nervousness, constipation, dizziness, insomnia, mental confusion or excitement, hyperthermia, dry mouth, altered taste perception, dysphagia, palpitations, bradycardia, urinary hesitancy or retention, impotence, decreased sweating). Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to be pregnant. Consult prescriber if breast-feeding.

Observe for tachycardia if patient has cardiac problems.

Capsule, as sulfate, timed release (Cystospaz-M®, Levsinex®): 0.375 mg

Elixir, as sulfate (Levsin®): 0.125 mg/5 mL with alcohol 20% (480 mL)

Injection, as sulfate (Levsin®): 0.5 mg/mL (1 mL, 10 mL)

Solution, oral (Gastrosed™, Levsin®): 0.125 mg/mL (15 mL)

Tablet, as sulfate:

Anaspaz®, Gastrosed™, Levsin®, Neoquess®: 0.125 mg

Cystospaz®: 0.15 mg

Extended release (Levbid®): 0.375 mg

Boyson SJ, "Bethanechol for Anticholinergic Side Effects," Ann Neurol, 1988, 23(4):422-3.

Rumack BH, "Anticholinergic Poisoning: Treatment With Physostigmine," Pediatrics, 1973, 52(3):449-51.

Shutt LE and Bowes JB, "Atropine and Hyoscine," Anaesthesia, 1979, 34(5):476-90.