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Cyclobenzaprine

FLEXERIL

Pronunciation: sye-kloe-BEN-za-preen

Cyclobenzaprine ballicule: receptor binding, kinetics and half-life diagram
Mechanism of action: Cyclobenzaprine ballicule
Cyclobenzaprine FLEXERIL mascot mnemonic cartoon
Visual mnemonic: Cyclobenzaprine mascot
“Flexible Cycle bending”

What it isTricyclic-related central muscle relaxant with H1 and muscarinic antagonism; short-term treatment of acute muscle spasm.

Why this onePronounced sedation can make it useful when nighttime spasm dominates, unlike less sedating relaxants.

What limits itAnticholinergic effects, falls and next-day sedation limit it, especially in older adults. Avoid with MAOIs.

Cyclobenzaprine molecular structure (skeletal formula)
Molecular structure: Cyclobenzaprine

FDA-approved for

Off-label

FDA label

FDA dosingPopulationStartTargetMax
Muscle spasm, adjunct to rest/PT for acute musculoskeletal conditionsAdults5 mg TID5 mg TID10 mg TID

Renal Undefined

Hepatic Use less frequent dosing in hepatic impairment

Instructions

Available strengths

Contraindications

Adverse reactions

Pregnancy Undefined

Lactation Undefined

Cost

Cyclobenzaprine (FLEXERIL)
What pharmacies pay · NADAC 9/30/26
Strength#/mogeneric $/moCostPlus
5 mgtab90 TID$1.98offered
7.5 mgtab90 TID$23.66offered
10 mgtab90 TID$1.54offered

Generic entry1989

NO BOXED WARNINGS

Principal riskAnticholinergic burden and sedation

Classes and tags

Clinical profile

Therapeutic safety burden1 / 4
Overdose danger1 / 4
Weight-gain liability0 / 4
Sedation liability3 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism2 / 4
Embryofetal risk1 / 4

Legacy pregnancy categoryUnknown / historical label unavailable

Defining liabilityGenerally tolerated at therapeutic doses; clinically important risks are agent-specific and increase with interactions or organ impairment.

Serotonicity

This drug is routinely called serotonergic. By Gillman’s human-effect criteria it does not raise serotonin in the synapse.

Named as a serotonergic muscle relaxant in the opioid labels, but Gillman places it with the drugs unlikely to be dangerous with an MAOI, alongside amitriptyline. The label still contraindicates MAOIs (concurrently or within 14 days).

Gillman’s four human testsA measurable SERT affinity that fails all four is not clinical serotonicity.

Non-elevating actionNone recorded

Evidence confidenceHigh

Background: what serotonicity is · what is and is not an SRI · what counts as a relevant MAOI.

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Memory aids: interaction avatars

Cyclobenzaprine CYP1A2 substrate avatar mnemonic
CYP1A2 substrate

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