Look Up > Drugs > Orphenadrine
Orphenadrine
Pronunciation
U.S. Brand Names
Generic Available
Synonyms
Pharmacological Index
Use
Pregnancy Risk Factor
Contraindications
Warnings/Precautions
Adverse Reactions
Overdosage/Toxicology
Drug Interactions
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Dietary Considerations
Mental Health: Effects on Mental Status
Mental Health: Effects on Psychiatric Treatment
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Patient Information
Nursing Implications
Dosage Forms
References

Pronunciation
(or FEN a dreen)

U.S. Brand Names
Norflex™

Generic Available

Yes


Synonyms
Orphenadrine Citrate

Pharmacological Index

Anti-Parkinson's Agent (Anticholinergic); Skeletal Muscle Relaxant


Use

Treatment of muscle spasm associated with acute painful musculoskeletal conditions; supportive therapy in tetanus


Pregnancy Risk Factor

C


Contraindications

Glaucoma, GI obstruction, cardiospasm, myasthenia gravis, hypersensitivity to orphenadrine or any component


Warnings/Precautions

Use with caution in patients with CHF or cardiac arrhythmias; some products contain sulfites


Adverse Reactions

>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


Overdosage/Toxicology

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.


Drug Interactions

CYP2B6, 2D6, and 3A3/4 enzyme substrate; CYP2B6 enzyme inhibitor


Mechanism of Action

Indirect skeletal muscle relaxant thought to work by central atropine-like effects; has some euphorigenic and analgesic properties


Pharmacodynamics/Kinetics

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)


Usual Dosage

Adults:

I.M., I.V.: 60 mg every 12 hours


Dietary Considerations

Alcohol: Additive CNS effect, avoid use


Mental Health: Effects on Mental Status

Drowsiness and dizziness are common; may rarely cause hallucinations


Mental Health: Effects on Psychiatric Treatment

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


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions


Dental Health: Effects on Dental Treatment

The peripheral anticholinergic effects of orphenadrine may decrease or inhibit salivary flow; normal salivation will return with cessation of drug therapy


Patient Information

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.


Nursing Implications

Do not crush sustained release drug product; raise bed rails, institute safety measures, assist with ambulation


Dosage Forms

Injection, as citrate: 30 mg/mL (2 mL, 10 mL)

Tablet, as citrate: 100 mg

Tablet, as citrate, sustained release: 100 mg


References

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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