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Pronunciation |
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(or
FEN a
dreen) |
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U.S. Brand
Names |
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Norflex™ |
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Generic
Available |
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Yes |
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Synonyms |
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Orphenadrine Citrate |
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Pharmacological Index |
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Anti-Parkinson's Agent (Anticholinergic); Skeletal Muscle
Relaxant |
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Use |
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Treatment of muscle spasm associated with acute painful musculoskeletal
conditions; supportive therapy in tetanus |
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Pregnancy Risk
Factor |
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C |
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Contraindications |
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Glaucoma, GI obstruction, cardiospasm, myasthenia gravis, hypersensitivity to
orphenadrine or any component |
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Warnings/Precautions |
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Use with caution in patients with CHF or cardiac arrhythmias; some products
contain sulfites |
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Adverse
Reactions |
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>10%:
Central nervous system: Drowsiness, dizziness
Ocular: Blurred vision
1% to 10%:
Cardiovascular: Flushing of face, tachycardia, syncope
Dermatologic: Rash
Gastrointestinal: Nausea, vomiting, constipation
Genitourinary: Decreased urination
Neuromuscular & skeletal: Weakness
Ocular: Nystagmus, increased intraocular pressure
Respiratory: Nasal congestion
<1%: Hallucinations, aplastic anemia |
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Overdosage/Toxicology |
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Symptoms of overdose include blurred vision, tachycardia, confusion,
seizures, respiratory arrest, dysrhythmias
There is no specific treatment for an antihistamine overdose, however, most
of its clinical toxicity is due to anticholinergic effects. Anticholinesterase
inhibitors may be useful by reducing acetylcholinesterase. Anticholinesterase
inhibitors include physostigmine, neostigmine, pyridostigmine and edrophonium.
For anticholinergic overdose with severe life-threatening symptoms,
physostigmine 1-2 mg (0.5 mg or 0.02 mg/kg for children) I.V., slowly may be
given to reverse these effects. Lethal dose is 2-3 g; treatment is symptomatic.
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Drug
Interactions |
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CYP2B6, 2D6, and 3A3/4 enzyme substrate; CYP2B6 enzyme
inhibitor |
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Mechanism of
Action |
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Indirect skeletal muscle relaxant thought to work by central atropine-like
effects; has some euphorigenic and analgesic properties |
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Pharmacodynamics/Kinetics |
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Peak effect: Oral: Within 2-4 hours
Duration: 4-6 hours
Protein binding: 20%
Metabolism: Extensive
Half-life: 14-16 hours
Elimination: Primarily in urine (8% as unchanged drug) |
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Usual Dosage |
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Adults:
I.M., I.V.: 60 mg every 12 hours |
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Dietary
Considerations |
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Alcohol: Additive CNS effect, avoid use |
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|
Mental Health: Effects
on Mental Status |
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Drowsiness and dizziness are common; may rarely cause
hallucinations |
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Mental Health:
Effects on Psychiatric
Treatment |
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May rarely cause aplastic anemia; use caution with clozapine and
carbamazepine; has been used to treat tardive dyskinesia and augment typical
antipsychotics; clozapine is a better option; concurrent use with psychotropics
may produce additive sedation |
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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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The peripheral anticholinergic effects of orphenadrine may decrease or
inhibit salivary flow; normal salivation will return with cessation of drug
therapy |
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Patient
Information |
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Take exactly as directed. Do not increase dose or discontinue without
consulting prescriber. Do not chew or crush sustained release tablets. Do not
use alcohol, prescriptive or OTC antidepressants, sedatives, or pain medications
without consulting prescriber. You may experience drowsiness, dizziness,
lightheadedness (avoid driving or engaging in tasks requiring alertness until
response to drug is known); nausea or vomiting (small, frequent meals, frequent
mouth care, or sucking hard candy may help); constipation (increased dietary
fluids and fibers or increased exercise may help); or decreased urination (void
before taking medication). Report excessive drowsiness or mental agitation,
chest pain, skin rash, swelling of mouth/face, difficulty speaking, or vision
disturbances. 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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Do not crush sustained release drug product; raise bed rails, institute
safety measures, assist with ambulation |
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Dosage Forms |
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Injection, as citrate: 30 mg/mL (2 mL, 10 mL)
Tablet, as citrate: 100 mg
Tablet, as citrate, sustained release: 100 mg |
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References |
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Beech M, Hell C, and Nightingale P, "Central Anticholinergic Syndrome,"
Lancet, 1987, 1(8541):1089.
Boyson SJ, "Bethanechol for Anticholinergic Side Effects," Ann Neurol,
1988, 23(4):422-3.
Clarke B, Mair J, and Rudolf M, "Acute Poisoning With Orphenadrine,"
Lancet, 1985, 1(8442):1386.
Danze LK and Langdorf MI,
"Reversal of Orphenadrine-Induced Ventricular Tachycardia With Physostigmine,"
J Emerg Med, 1991, 9(6):453-7.
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