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Cyclobenzaprine

From Pharmacopedia
(Redirected from Flexeril)
Cyclobenzaprine
Flexeril (IR; brand discontinued in US, generic widely available), Amrix (ER)

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Pharmacy
Starting dose
IR 5 mg PO TID; titrate to 10 mg TID if needed. Amrix ER 15 mg PO once daily. Off-label insomnia / fibromyalgia: 5-10 mg PO at bedtime
Preparations
IR tablets 5, 7.5, 10 mg; Amrix ER capsules 15, 30 mg
US FDA Max
30 mg/day (IR or ER)
Common uses
Pharmacology
Routes
Oral
Onset
~1 hour
Duration
12-24 hours (IR); 24 hours (Amrix ER)
Half-life
18 hours (IR); 32-33 hours (ER)[1]
Bioavailability
~33-55% (IR); reduced by food[1]
Pregnancy
Limited human data.[citation needed]
Legal status
Rx-only in US. Not a controlled substance, distinguishing it from the carisoprodol alternative for muscle spasm[1]
Purported mechanism
Structurally a tricyclic compound closely related to amitriptyline but FDA-approved as a muscle relaxant rather than an antidepressant. Centrally-acting via brainstem and supraspinal sites, reducing tonic somatic motor activity through noradrenergic descending pathways; the spinal cord is not the primary site of action. Substantial anticholinergic, H1 antihistaminergic, and α1-adrenergic antagonist activity accounts for sedation, dry mouth, and orthostatic adverse effects.0 Serotonin syndrome risk applies through the tricyclic-class identity when combined with SSRIs, SNRIs, MAOIs, tramadol, or other serotonergic agents. FDA labeling restricts to short-term use (≤2-3 weeks); evidence for prolonged use is limited[1].
Pharmacopedia is intended for reference. Nothing here is advice. In an emergency call 911; US Poison Control 1-800-222-1222. See the full disclaimer.

References

  1. 1.0 1.1 1.2 1.3 FDA Prescribing Information, Flexeril (cyclobenzaprine hydrochloride), Merck/various, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/017821s048lbl.pdf