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Orphenadrine

NORFLEX

What it isAntimuscarinic, H1, and NMDA antagonist used for acute musculoskeletal spasm.

Why this oneUnlike purely sedating relaxants, it adds an NMDA-linked analgesic component, though efficacy evidence is weak.

What limits itAnticholinergic burden makes it poor for older adults. Overdose can be lethal through arrhythmia, seizure, and coma.

FDA-approved for

FDA label

FDA dosingPopulationStartTargetMax
Adjunct for acute painful musculoskeletal conditionsAdults1 tablet BID (one AM, one PM)1 tablet BID1 tablet BID

Renal Undefined

Hepatic Undefined

Instructions

Contraindications

Cautions

Adverse reactions

Pregnancy Pregnancy Category C; use only if clearly needed

Lactation Undefined

NO BOXED WARNINGS

Principal riskAnticholinergic burden; lethal in overdose

Cost, est. cash$10–$300/month

Generic entry1982

Classes and tags

Clinical profile

Therapeutic safety burden1 / 4
Overdose danger1 / 4
Weight-gain liability0 / 4
Sedation liability2 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism3 / 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.

Mechanism of action: Orphenadrine ballicule

Orphenadrine ballicule: receptor binding, kinetics and half-life diagram

Open Orphenadrine in the interactive console ↗

Memory aids: mascots and interaction avatars

Orphenadrine NORFLEX mascot mnemonic cartoon
“No reflex Orphan drain”
muscles → muscle relaxant
Orphenadrine CYP2B6 inhibitor avatar
CYP2B6 inhibitor (weak)

Open Orphenadrine in the interactive console ↗