Celecoxib

CELEBREX

Open Celecoxib in the interactive console ↗

What it isCOX-2-preferring NSAID; arthritis and acute pain.

Why this oneIt largely spares platelet COX-1 and causes less GI ulceration than nonselective NSAIDs, useful when bleeding risk matters.

What limits itCardiovascular and renal toxicity remain; CYP2C9 poor metabolism or inhibition raises exposure. Sulfonamide hypersensitivity warrants caution.

FDA-approved for

pain/arthritis (1998)

FDA label

Read the full label on DailyMed ↗

BOXED WARNING Serious CV thrombotic events (MI, stroke, may be fatal); contraindicated peri-CABG. Serious GI bleeding, ulceration, perforation (may be fatal).

FDA dosing	Population	Start	Target	Max
Osteoarthritis	Adult	200 mg QD or 100 mg BID	200 mg QD or 100 mg BID
Rheumatoid arthritis	Adult	100-200 mg BID	100-200 mg BID
Juvenile RA	Peds >=2 yr	50 mg BID (10-25 kg); 100 mg BID (>25 kg)	50-100 mg BID by weight
Ankylosing spondylitis	Adult	200 mg QD or 100 mg BID	200 mg/day	400 mg/day (trial if no effect at 6 wk)
Acute pain / primary dysmenorrhea	Adult	400 mg once, then 200 mg once if needed (day 1)	200 mg BID PRN

Renal Not recommended in severe renal insufficiency; avoid in advanced renal disease unless benefit outweighs risk

Hepatic Moderate (Child-Pugh B): reduce dose 50%; severe: not recommended

Instructions

May be given without regard to meals
Difficulty swallowing (incl. JRA): sprinkle capsule contents onto applesauce, ingest immediately with water
CYP2C9 poor metabolizers: start at half the lowest recommended dose (consider alternatives for JRA)

Contraindications

History of asthma, urticaria, or allergic-type reactions to aspirin or other NSAIDs
Setting of CABG surgery
Demonstrated allergic-type reactions to sulfonamides

Cautions

CV thrombotic events (MI, stroke)
GI bleeding, ulceration, perforation
Hepatotoxicity
Hypertension; heart failure and edema
Renal toxicity/hyperkalemia
Anaphylaxis; aspirin-sensitive asthma (contraindicated)
Serious skin reactions (SJS/TEN)/DRESS
Fetal toxicity 20-30 wk gestation
Anemia/hematologic toxicity

Adverse reactions

Abdominal pain
Diarrhea
Dyspepsia
Flatulence
Peripheral edema
Dizziness
Headache
Upper respiratory infection
Rash

Pregnancy Avoid at >=30 wk (premature ductus arteriosus closure); limit 20-30 wk (oligohydramnios/fetal renal dysfunction)

Lactation Low levels in breast milk (<1% weight-based infant dose); caution advised

⚠ BOXED WARNINGS

Cardiovascular thrombotic events
Gastrointestinal bleeding, ulceration and perforation

Cost, est. cash$4–$80/month

Generic entry2014

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4

Overdose danger3 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk3 / 4

Legacy pregnancy categoryMultiple / indication-, trimester- or formulation-dependent

Defining liabilityGI bleeding, kidney injury, hypertension and fluid retention; many agents increase lithium concentrations.

Mechanism of action: Celecoxib ballicule

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

Open Celecoxib in the interactive console ↗

Memory aids: mascots and interaction avatars

Celecoxib CELEBREX mascot mnemonic cartoon — **“2 Celebrating Cocks”**
Two roosters → COX-2 selective cue
“The N said... NSAID”

CYP2C9 substrate

Open Celecoxib in the interactive console ↗