Look Up > Drugs > Cyclobenzaprine
Cyclobenzaprine
Pronunciation
U.S. Brand Names
Generic Available
Canadian Brand Names
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
(sye kloe BEN za preen)

U.S. Brand Names
Flexeril®

Generic Available

Yes


Canadian Brand Names
Novo-Cycloprine

Synonyms
Cyclobenzaprine Hydrochloride

Pharmacological Index

Skeletal Muscle Relaxant


Use

Dental: Treatment of muscle spasm associated with acute temporomandibular joint pain

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


Pregnancy Risk Factor

B


Contraindications

Hypersensitivity to cyclobenzaprine or any component; do not use concomitantly or within 14 days of MAO inhibitors; hyperthyroidism, congestive heart failure, arrhythmias


Warnings/Precautions

Cyclobenzaprine shares the toxic potentials of the tricyclic antidepressants and the usual precautions of tricyclic antidepressant therapy should be observed; use with caution in patients with urinary hesitancy or angle-closure glaucoma


Adverse Reactions

>10%:

Central nervous system: Drowsiness, dizziness, lightheadedness

Gastrointestinal: Xerostomia

1% to 10%:

Cardiovascular: Edema of the face/lips, syncope

Gastrointestinal: Bloated feeling

Genitourinary: Problems in urinating, polyuria

Hepatic: Hepatitis

Neuromuscular & skeletal: Problems in speaking, muscle weakness

Ocular: Blurred vision

Otic: Tinnitus

<1%: Tachycardia, hypotension, arrhythmia, headache, fatigue, nervousness, confusion, ataxia, rash, dermatitis, dyspepsia, nausea, constipation, stomach cramps, unpleasant taste


Overdosage/Toxicology

Symptoms of overdose include troubled breathing, drowsiness, syncope, seizures, tachycardia, hallucinations, vomiting

Following initiation of essential overdose management, toxic symptoms should be treated. Ventricular arrhythmias often respond to systemic alkalinization (sodium bicarbonate 0.5-2 mEq/kg I.V.) and/or phenytoin 15-20 mg/kg (adults). Arrhythmias unresponsive to this therapy may respond to lidocaine 1 mg/kg I.V. followed by a titrated infusion. Physostigmine (1-2 mg I.V. slowly for adults or 0.5 mg I.V. slowly for children) may be indicated in reversing cardiac arrhythmias that are life-threatening. Seizures usually respond to diazepam I.V. boluses (5-10 mg for adults up to 30 mg or 0.25-0.4 mg/kg/dose for children up to 10 mg/dose). If seizures are unresponsive or recur, phenytoin or phenobarbital may be required.


Drug Interactions

CYP1A2, 2D6 and 3A3/4 enzyme substrate

Do not use concomitantly or within 14 days after MAO inhibitors

Because of similarities to the tricyclic antidepressants, may have additive toxicities

Anticholinergics: Because of cyclobenzaprine's anticholinergic action, use with caution in patients receiving these agents

Alcohol, barbiturates, and other CNS depressants: Effects may be enhanced by cyclobenzaprine


Mechanism of Action

Centrally acting skeletal muscle relaxant pharmacologically related to tricyclic antidepressants; reduces tonic somatic motor activity influencing both alpha and gamma motor neurons


Pharmacodynamics/Kinetics

Onset of action: Commonly occurs within 1 hour

Duration: 8 to >24 hours

Absorption: Oral: Completely

Metabolism: Hepatic; may undergo enterohepatic recycling

Time to peak serum concentration: Within 3-8 hours

Elimination: Renally as inactive metabolites and in feces (via bile) as unchanged drug


Usual Dosage

Oral: Note: Do not use longer than 2-3 weeks

Adults: 20-40 mg/day in 2-4 divided doses; maximum dose: 60 mg/day


Dietary Considerations

No data reported


Mental Health: Effects on Mental Status

Drowsiness and dizziness are common; may cause nervousness or confusion


Mental Health: Effects on Psychiatric Treatment

Contraindicated with MAOIs or within 14 days of MAOI; concurrent use with psychotropics may exacerbate the dry mouth and sedation commonly seen with cyclobenzaprine


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions


Dental Health: Effects on Dental Treatment

>10% of patient experience dry mouth


Patient Information

Take exactly as directed. Do not increase dose or discontinue without consulting prescriber. 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 that require alertness until response to drug is known); or urinary retention (void before taking medication). Report excessive drowsiness or mental agitation, chest pain, skin rash, swelling of mouth/face, difficulty speaking, ringing in ears, or blurred vision. Breast-feeding precautions: Breast-feeding is not recommended.


Nursing Implications

Raise bed rails, institute safety measures, assist with ambulation


Dosage Forms

Tablet, as hydrochloride: 10 mg


References

Ambre JJ, "Cyclobenzaprine Overdose," Ann Intern Med, 1985, 102(4):559-60.

Heckerling PS, Bartow TJ, "Paradoxical Diaphoresis in Cyclobenzaprine Poisoning," Ann Intern Med, 1984, 101(6):881.

Hucker HB, Stauffer SC, Albert KS, et al, "Plasma Levels and Bioavailability of Cyclobenzaprine in Human Subjects," J Clin Pharmacol, 1977, 17(11-12):719-27.

Linden CH, Mitchiner JC, Lindzon RD, et al, "Cyclobenzaprine Overdosage," J Toxicol Clin Toxicol, 1983, 20(3):281-8.

Theoharides TC, Harris RS, and Weckstein D, "Neuroleptic Malignant-Like Syndrome Due to Cyclobenzaprine?" J Clin Psychopharmacol, 1995, 15(1):79-81.


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