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Pronunciation |
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(BENZ
troe
peen) |
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U.S. Brand
Names |
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Cogentin® |
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Generic
Available |
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Yes: Tablet |
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Canadian Brand
Names |
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PMS-Benztropine |
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Synonyms |
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Benztropine Mesylate |
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Pharmacological Index |
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Anticholinergic Agent; Anti-Parkinson's Agent
(Anticholinergic) |
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Use |
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Adjunctive treatment of Parkinson's disease; also used in treatment of
drug-induced extrapyramidal effects (except tardive
dyskinesia) |
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Pregnancy Risk
Factor |
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C |
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Contraindications |
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Children <3 years of age; hypersensitivity to benztropine or any component
of the formulation; pyloric or duodenal obstruction, stenosing peptic ulcers;
bladder neck obstructions; achalasia; myasthenia gravis |
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Warnings/Precautions |
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Use with caution in older children (dose has not been established). Use with
caution in hot weather or during exercise. May cause anhydrosis and
hyperthermia, which may be severe. The risk is increased in hot environments,
particularly in the elderly, alcoholics, patients with CNS disease, and those
with prolonged outdoor exposure.
May be associated with confusion or hallucinations (generally at higher
dosages). Intensification of symptoms or toxic psychosis may occur in patients
with mental disorders. Benztropine does not relieve symptoms of tardive
dyskinesia. |
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Adverse
Reactions |
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Cardiovascular: Tachycardia
Central nervous system: Confusion, disorientation, memory impairment, toxic
psychosis, visual hallucinations
Dermatologic: Rash
Endocrine & metabolic: Heat stroke, hyperthermia
Gastrointestinal: Xerostomia, nausea, vomiting, constipation, ileus
Genitourinary: Urinary retention, dysuria
Ocular: Blurred vision, mydriasis
Miscellaneous: Fever |
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Overdosage/Toxicology |
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Symptoms of overdose include CNS depression, confusion, nervousness,
hallucinations, dizziness, blurred vision, nausea, vomiting, hyperthermia
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. 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. |
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Drug
Interactions |
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Decreased effect: May increase gastric degradation of levodopa and decrease
the amount of levodopa absorbed by delaying gastric emptying; the opposite may
be true for digoxin
Therapeutic effects of cholinergic agents (tacrine, donepezil) and
neuroleptics may be antagonized
Increased toxicity: Central and/or peripheral anticholinergic syndrome can
occur when administered with amantadine, rimantadine, narcotic analgesics,
phenothiazines and other antipsychotics (especially with high anticholinergic
activity), tricyclic antidepressants, quinidine and some other antiarrhythmics,
and antihistamines |
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Mechanism of
Action |
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Possesses both anticholinergic and antihistaminic effects. In vitro
anticholinergic activity approximates that of atropine; in vivo it is
only about half as active as atropine. Animal data suggest its antihistaminic
activity and duration of action approach that of pyrilamine maleate. May also
inhibit the reuptake and storage of dopamine and thereby, prolong the action of
dopamine. |
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Pharmacodynamics/Kinetics |
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Onset of action: Oral: Within 1 hour; Parenteral: Within 15 minutes
Duration of action: 6-48 hours (wide range) |
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Usual Dosage |
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Use in children <3 years of age should be reserved for life-threatening
emergencies
Children >3 years: 0.02-0.05 mg/kg/dose 1-2 times/day
Adults: 1-4 mg/dose 1-2 times/day
Acute dystonia: Adults: I.M., I.V.: 1-2 mg
Parkinsonism: Oral:
Adults: 0.5-6 mg/day in 1-2 divided doses; if one dose is greater, administer
at bedtime; titrate dose in 0.5 mg increments at 5- to 6-day intervals
Elderly: Initial: 0.5 mg once or twice daily; increase by 0.5 mg as needed at
5-6 days; maximum: 4 mg/day |
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Dietary
Considerations |
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Alcohol: Additive CNS effects, avoid use |
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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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Dry mouth, nose, and throat very prevalent in patients taking this
drug |
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Patient
Information |
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Take exactly as directed; do not increase, decrease, or discontinue without
consulting prescriber. Take at the same time each day. Do not use alcohol and
all prescription or OTC sedatives or CNS depressants without consulting
prescriber. You may experience drowsiness, dizziness, confusion, and blurred
vision (use caution when driving, climbing stairs, or engaging in tasks
requiring alertness until response to drug is known); increased susceptibility
to heat stroke, decreased perspiration (use caution in hot weather - maintain
adequate fluids and reduce exercise activity); constipation (increased exercise,
fluids, or dietary fruit and fiber may help). Report unresolved nausea,
vomiting, or gastric disturbances; rapid or pounding heartbeat, chest pain or
palpitation; difficulty breathing; CNS changes (hallucination, loss of memory,
nervousness, etc); eye pain; prolonged fever; painful or difficult urination;
unresolved constipation; increased muscle spasticity or rigidity; skin rash; or
significant worsening of condition. Pregnancy/breast-feeding
precautions: Inform prescriber if you are or intend to be pregnant. Consult
prescriber if breast-feeding. |
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Nursing
Implications |
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No significant difference in onset of I.M. or I.V. injection, therefore,
there is usually no need to use the I.V. route. Improvement is sometimes
noticeable a few minutes after injection. |
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Dosage Forms |
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Injection, as mesylate: 1 mg/mL (2 mL)
Tablet, as mesylate: 0.5 mg, 1 mg, 2 mg |
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References |
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Catterson ML and Martin RL,
"Anticholinergic Toxicity Masquerading as Neuroleptic Malignant Syndrome: A Case Report and Review,"
Ann Clin Psychiatry, 1995, 6:267-9.
Erwin WG and Turco TF,
"Current Concepts in Clinical Therapeutics: Parkinson's Disease," Clin
Pharm, 1986, 5(9):742-53.
Fahy P, Arnold P, Curry SC, et al,
"Serial Serum Drug Concentrations and Prolonged Anticholinergic Toxicity After
Benztropine (Cogentin®)
Overdose," Am J Emerg Med, 1989, 7(2):199-202.
Feinberg M,
"The Problems of Anticholinergic Adverse Effects in Older Patients," Drugs
Aging, 1993, 3(4):335-48.
Goff DC, Arana GW, Greenblatt DJ, et al,
"The Effect of Benztropine on Haloperidol-Induced Dystonia, Clinical Efficacy and Pharmacokinetics: A Prospective, Double-Blind Trial,"
J Clin Psychopharmacol, 1991, 11(2):106-12.
Harper G, Dawes M, Azlin C, et al,
"Small Bowel Obstruction in a Child on an Antipsychotic," J Child Adolesc
Psychopharm, 1995, 5:81-4.
Mackie A and Hill HF,
"Prophylactic Benztropine for Antiemetic Precipitated Extrapyramidal Symptoms During Cancer Chemotherapy,"
J Pain Symptom Manage, 1989, 4(3):109-10.
McEvoy JP,
"The Clinical Use of Anticholinergic Drugs as Treatment for Extrapyramidal Side Effects of Neuroleptic Drugs,"
J Clin Psychopharmacol, 1983, 3(5):288-302.
Rosano TG, Meola JM, Wolf BC, et al,
"Benztropine Identification and Quantitation in a Suicidal Overdose," J Anal
Toxicol, 1994, 18(6):348-53.
Roth A, Akyol S, and Nelson JC,
"Delirium Associated With the Combination of a Neuroleptic, an SSRI, and Benztropine,"
J Clin Psychiatry, 1994, 55(11):492-5.
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