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Pronunciation |
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(trye
heks ee FEN i
dil) |
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U.S. Brand
Names |
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Artane®; Trihexy® |
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Generic
Available |
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Yes: Tablet |
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Canadian Brand
Names |
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Apo®-Trihex; Novo-Hexidyl;
PMS-Trihexyphenidyl; Trihexyphen® |
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Synonyms |
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Benzhexol Hydrochloride; Trihexyphenidyl Hydrochloride |
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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; treatment of drug-induced
extrapyramidal effects |
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Pregnancy Risk
Factor |
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C |
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Contraindications |
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Hypersensitivity to trihexyphenidyl or any component; patients with
narrow-angle glaucoma; 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 hot weather or during exercise. Elderly patients require
strict dosage regulation. Use with caution in patients with tachycardia, cardiac
arrhythmias, hypertension, hypotension, prostatic hypertrophy or any tendency
toward urinary retention, liver or kidney disorders, and obstructive disease of
the GI or GU tract. May exacerbate mental symptoms when used to treat
extrapyramidal reactions. When given in large doses or to susceptible patients,
may cause weakness. Does not improve symptoms of tardive
dyskinesias. |
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Adverse
Reactions |
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Cardiovascular: Tachycardia
Central nervous system: Confusion, agitation, euphoria, drowsiness, headache,
dizziness, nervousness, delusions, hallucinations, paranoia
Dermatologic: Dry skin, increased sensitivity to light, rash
Gastrointestinal: Constipation, xerostomia, dry throat, ileus, nausea,
vomiting, parotitis
Genitourinary: Urinary retention
Neuromuscular & skeletal: Weakness
Ocular: Blurred vision, mydriasis, increase in intraocular pressure, glaucoma
Respiratory: Dry nose
Miscellaneous: Diaphoresis (decreased) |
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Overdosage/Toxicology |
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Symptoms of overdose include blurred vision, urinary retention, tachycardia
Anticholinergic toxicity is caused by strong binding of the drug to
cholinergic receptors. Anticholinesterase inhibitors reduce
acetylcholinesterase; 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 |
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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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Exerts a direct inhibitory effect on the parasympathetic nervous system. It
also has a relaxing effect on smooth musculature; exerted both directly on the
muscle itself and indirectly through parasympathetic nervous system (inhibitory
effect) |
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Pharmacodynamics/Kinetics |
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Peak effect: Within 1 hour
Half-life: 3.3-4.1 hours
Time to peak serum concentration: Within 1-1.5 hours
Elimination: Primarily in urine |
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Usual Dosage |
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Adults: Oral: Initial: 1-2 mg/day, increase by 2 mg increments at intervals
of 3-5 days; usual dose: 5-15 mg/day in 3-4 divided doses |
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Dietary
Considerations |
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Alcohol: Additive CNS effect, avoid use |
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Monitoring
Parameters |
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IOP monitoring and gonioscopic evaluations should be performed
periodically |
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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 experience significant dry mouth; normal salivary flow
will resume with cessation of drug therapy. Prolonged xerostomia may contribute
to development of caries, periodontal disease, oral candidiasis and
discomfort |
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Patient
Information |
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Take exactly as directed; with meals if GI upset occurs, before meals if dry
mouth occurs, after eating if drooling or if nausea occurs. Take at the same
time each day. Maintain adequate hydration (2-3 L/day of fluids unless
instructed to restrict fluid intake); void before taking medication. Do not use
alcohol and all prescription or OTC sedatives or CNS depressants without
consulting prescriber. You may experience drowsiness, confusion, or vision
changes (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); dry skin or nasal passages
(consult prescriber for appropriate relief). Report unresolved constipation,
chest pain or palpitations, difficulty breathing, CNS changes (hallucination,
loss of memory, nervousness, etc), painful or difficult urination, 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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Tolerated best if given in 3 daily doses and with food; high doses may be
divided into 4 doses, at meal times and at bedtime; patients may be switched to
sustained-action capsules when stabilized on conventional dosage
forms |
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Dosage Forms |
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Capsule, as hydrochloride, sustained release: 5 mg
Elixir, as hydrochloride: 2 mg/5 mL (480 mL)
Tablet, as hydrochloride: 2 mg, 5 mg |
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References |
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Feinberg M,
"The Problems of Anticholinergic Adverse Effects in Older Patients," Drugs
Aging, 1993, 3(4):335-48. |
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