CELECOXIB

CELECOXIB (cel-e-cox'ib) Celebrex Classifications: analgesic, nsaid; cyclooxygenase-2 (cox-2) inhibitor; antiinflammatory; Therapeutic: analgesic, nsaid; cyclooxygenase-2 (cox-2) inhibitor; antiinflammatory Pregnancy Category: C first and second trimester; D third trimester

Availability

100 mg, 200 mg, 400 mg capsules

Action

Although an NSAID, unlike ibuprofen celecoxib inhibits prostaglandin synthesis by inhibiting cyclooxygenase-2 (COX-2), but does not inhibit cyclooxygenase-1 (COX-1).

Therapeutic Effect

Exhibits antiinflammatory, analgesic, and antipyretic activities. Reduces or eliminates the pain of rheumatoid and osteoarthritis.

Uses

Relief of S&S of osteoarthritis and rheumatoid arthritis. Treatment of acute pain and primary dysmenorrhea. Reduction of polyp formation in familial adenomatous polyposis (FAP), ankylosing spondylitis, juvenile rheumatoid arthritis.

Contraindications

Severe hepatic impairment; hypersensitivity to celecoxib, salicylate, or sulfonamide; asthmatic patients with aspirin triad; advanced renal disease; concurrent use of diuretics and ACE inhibitors; anemia; pain from CABG surgery; pregnancy (category C in first and second trimesters and category D in third trimester); children <18 y; lactation.

Cautious Use

Patients who are P450 2C9 poor metabolizers; patients who weigh <50 kg; mild or moderate hepatic impairment; renal insufficiency; aspirin use; prior history of GI bleeding or peptic ulcer disease; alcoholics; concurrent use of anticoagulants; asthmatics; bone marrow suppression; CVA; PVD; elevated liver function tests; heart failure; kidney disease; hypertension; fluid retention.

Route & Dosage

Arthritis Adult: PO 100–200 mg b.i.d. or 200 mg q.d. Acute Pain, Dysmenorrhea Adult: PO 400 mg 1st dose, then 200 mg same day if needed, then 200 mg b.i.d. prn FAP Adult: PO 400 mg b.i.d. Juvenile Rheumatoid Arthritis Adolescents/Child (>2 y, >25 kg): PO 100 mg b.i.d. Child (>2 y, 10–25 kg): PO 50 mg b.i.d.

Administration

Oral

• Give 2 h before/after magnesium or aluminum-containing antacids.
• Store in tightly closed container and protect from light.

Adverse Effects (≥1%)

Body as a Whole: Back pain, peripheral edema. Increased risk of cardiovascular events. GI: Abdominal pain, diarrhea, dyspepsia, flatulence, nausea. CNS: Dizziness, headache, insomnia. Respiratory: Pharyngitis, rhinitis, sinusitis, URI. Skin: Rash.

Interactions

Drug: May diminish effectiveness of ace inhibitors; fluconazole increases celecoxib concentrations; may increase lithium concentrations; may increase INR in older patients on warfarin.

Pharmacokinetics

Peak: 3 h. Distribution: 97% protein bound; crosses placenta. Metabolism: In liver by CYP2C9. Elimination: Primarily in feces (57%), 27% in urine. Half-Life: 11.2 h.

Nursing Implications

Assessment & Drug Effects

• Therapeutic effectiveness is indicated by relief of joint pain.
• Lab tests: Periodically monitor Hct and Hgb, liver functions, BUN and creatinine, and serum electrolytes.
• Monitor closely lithium levels when the two drugs are given concurrently.
• Monitor closely PT/INR when used concurrently with warfarin.
• Monitor for fluid retention and edema especially in those with a history of hypertension or CHF.

Patient & Family Education

• Avoid using celecoxib during the third trimester of pregnancy.
• Promptly report any of the following: unexplained weight gain, edema, skin rash.
• Stop taking celecoxib and promptly report to physician if any of the following occurs: S&S of liver dysfunction including nausea, fatigue, lethargy, itching, jaundice, abdominal pain, and flulike symptoms; S&S of GI ulceration including black, tarry stools and upper GI distress.

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Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug