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Pronunciation |
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(sye
kloe BEN za
preen) |
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U.S. Brand
Names |
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Flexeril® |
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Generic
Available |
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Yes |
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Canadian Brand
Names |
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Novo-Cycloprine |
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Synonyms |
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Cyclobenzaprine Hydrochloride |
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Pharmacological Index |
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Skeletal Muscle Relaxant |
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Use |
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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 |
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Pregnancy Risk
Factor |
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B |
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Contraindications |
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Hypersensitivity to cyclobenzaprine or any component; do not use
concomitantly or within 14 days of MAO inhibitors; hyperthyroidism, congestive
heart failure, arrhythmias |
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Warnings/Precautions |
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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 |
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Adverse
Reactions |
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>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 |
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Overdosage/Toxicology |
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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. |
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Drug
Interactions |
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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 |
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Mechanism of
Action |
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Centrally acting skeletal muscle relaxant pharmacologically related to
tricyclic antidepressants; reduces tonic somatic motor activity influencing both
alpha and gamma motor neurons |
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Pharmacodynamics/Kinetics |
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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 |
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Usual Dosage |
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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
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Dietary
Considerations |
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No data reported |
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Mental Health: Effects
on Mental Status |
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Drowsiness and dizziness are common; may cause nervousness or
confusion |
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Mental Health:
Effects on Psychiatric
Treatment |
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Contraindicated with MAOIs or within 14 days of MAOI; concurrent use with
psychotropics may exacerbate the dry mouth and sedation commonly seen with
cyclobenzaprine |
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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 patient experience dry mouth |
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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 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. |
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Nursing
Implications |
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Raise bed rails, institute safety measures, assist with
ambulation |
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Dosage Forms |
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Tablet, as hydrochloride: 10 mg |
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References |
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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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