celecoxib, CeleBREX

 Indications

Relief of signs and symptoms of osteoarthritis, rheumatoid

arthritis, ankylosing spondylitis, and juvenile rheumatoid

arthritis. Management of acute pain including

primary dysmenorrhea.

Action

Inhibits the enzyme COX-2. This enzyme is required for

the synthesis of prostaglandins. Has analgesic, anti-inflammatory,

and antipyretic properties. Therapeutic

Effects: Decreased pain and inflammation caused by

arthritis or spondylitis. Decreased pain.

Pharmacokinetics

Absorption: Bioavailability unknown.

Distribution: 97% bound to plasma proteins; extensive

tissue distribution.

Metabolism and Excretion: Mostly metabolized

by the hepatic CYP2C9 isoenzyme; the CYP2C9 enzyme

system exhibits genetic polymorphism; poor metabolizers

may have significantlyqcelecoxib concentrations

and anqrisk of adverse effects; 3% excreted

unchanged in urine and feces.

Half-life: 11 hr. 

TIME/ACTION PROFILE (pain reduction)

ROUTE ONSET PEAK DURATION

PO 24–48 hr unknown 12–24 hr†

†After discontinuation.

Contraindications/Precautions

Contraindicated in: Hypersensitivity; Cross-sensitivity

may exist with other NSAIDs, including aspirin;

History of allergic-type reactions to sulfonamides; History

of asthma, urticaria, or allergic-type reactions to

aspirin or other NSAIDs, including the aspirin triad

(asthma, nasal polyps, and severe hypersensitivity reactions

to aspirin); Advanced renal disease; Severe hepatic

dysfunction; Coronary artery bypass graft (CABG)

surgery; OB: Should not be used in late pregnancy (may

cause premature closure of the ductus arteriosus).

Use Cautiously in: Cardiovascular disease or risk

factors for cardiovascular disease (mayqrisk of serious

cardiovascular thrombotic events, myocardial infarction,

and stroke, especially with prolonged use or

use of higher doses); avoid use in patients with recent

MI or HF; Pre-existing renal disease, heart failure, liver

dysfunction, concurrent diuretic, or ACE inhibitor therapy

(qrisk of renal impairment); Hypertension or fluid

retention; Renal impairment (may precipitate acute renal

failure); Serious dehydration (correct deficits before

administering); Patients who are known or suspected

to be poor CYP2C9 metabolizers (pinitial dose

by 50%); Pre-existing asthma; Pedi: Safety not established

in children 2 yr or for longer than 6 mo; Geri:

Concurrent therapy with corticosteroids or anticoagulants,

long duration of NSAID therapy, history of smoking,

alcoholism, geriatric patients, or poor general

health status (qrisk of GI bleeding); Lactation: Lactation.

Exercise Extreme Caution in: History of ulcer

disease or GI bleeding.

Adverse Reactions/Side Effects

CNS: dizziness, headache, insomnia. CV: HF, MYOCARDIAL

INFARCTION, STROKE, THROMBOSIS, edema, hypertension.

GI: GI BLEEDING, abdominal pain, diarrhea,

dyspepsia, flatulence, nausea. Derm: EXFOLIATIVE DERMATITIS,

STEVENS-JOHNSON SYNDROME, TOXIC EPIDERMAL

NECROLYSIS, rash. F and E: hyperkalemia.

Interactions

Drug-Drug: CYP2C9 inhibitors mayqlevels. Mayp

effectiveness of ACE inhibitors, thiazide diuretics,

and furosemide. Fluconazoleqlevels (use lowest

recommended dosage).qrisk of bleeding with anticoagulants,

aspirin, clopidogrel, ticagrelor, prasugrel,

corticosteroids, fibrinolytics, SNRIs, or

SSRIs. Mayqserum lithium levels. Does not inhibit

the cardioprotective effect of low-dose aspirin.

Route/Dosage

PO (Adults): Osteoarthritis—200 mg once daily or

100 mg twice daily. Rheumatoid arthritis—100–200 mg twice daily. Ankylosing spondylitis—200 mg once

daily or 100 mg twice daily; dose may beqafter 6 wk to

400 mg daily. Acute pain, including dysmenorrhea—

400 mg initially, then a 200-mg dose if needed on the

first day; then 200 mg twice daily as needed.

Hepatic Impairment

PO (Adults): Moderate hepatic impairment (Child-

Pugh Class B)—pdose by 50%.

PO (Children 2 yr, 10 kg–25 kg): Juvenile

rheumatoid arthritis—50 mg twice daily.

PO (Children 2 yr, 25 kg): Juvenile rheumatoid

arthritis—100 mg twice daily.

Availability (generic available)

Capsules: 50 mg, 100 mg, 200 mg, 400 mg. Cost: 100

mg $387.18/100, 200 mg $621.67/100, 400 mg

$1,576.25/180.