Celecoxib (cel-e-cox′ib) Celebrex
Classifications: ANALGESIC, NONSTEROIDAL ANTI-INFLAMMMATORY DRUG (NSAID); CYCLOOXYGENASE-2 (COX-2) INHIBITOR; ANTI-INFLAMMATORY
Therapeutic: ANALGESIC, NSAID; COX-2 INHIBITOR; ANTIINFLAMMATORY; ANTIRHEUMATIC
Pregnancy Category: C first and second trimester; D third trimester
ACTION & THERAPEUTIC EFFECT
Although an NSAID, unlike ibuprofen celecoxib
inhibits prostaglandin synthesis by inhibiting cyclooxygenase- 2 (COX-2), but
does not inhibit cyclooxygenase-1 (COX-1). Exhibits anti-inflammatory, analgesic, and antipyretic activities. Reduces
or eliminates the pain of rheumatoid
and osteoarthritis.
Relief of S&S of osteoarthritis and rheumatoid
arthritis. Treatment of acute pain and primary dysmenorrhea; ankylosing
spondylitis, juvenile rheumatoid arthritis.
Hypersensitivity to celecoxib, salicylate, or sulfonamide;
asthmatic patients with aspirin triad; GI bleeding; advanced renal disease;
development of S&S of renal impairment due to drug; severe hepatic
impairment; development of S&S of hepatic impairment due to drug; anemia; pain
from CABG surgery; pregnancy (category D third trimester); lactation.
Patients who are CYP2C9 poor metabolizers;
patients who weigh less than 50 kg; mild or moderate hepatic impairment; elevated
LTFs; renal insufficiency; prior history of GI bleeding or peptic ulcer
disease; alcoholics; asthmatics; bone marrow suppression; CVA; PVD; fluid
retention and/or HF; known risks for cardiovascular disease; kidney disease; hypertension;
fluid retention; older adults; pregnancy (category C first and second
trimester); children with systemic-onset juvenile rheumatoid arthritis younger
than 2 y.
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Celecoxib (Celebrex) Uses, Dosage, Side Effects |
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Osteoarthritis/Arthritis/ Ankylosing Spondylitis
Adult: PO 100 mg b.i.d. or 200 mg daily
Adult: PO 100–200 mg b.i.d.
Adult: PO 400 mg 1st dose, then 200 mg same day if needed, then 200 mg
b.i.d. prn
Juvenile Rheumatoid Arthritis
Adolescent/Child (2
y and older, weight greater than 25 kg): PO 100 mg
b.i.d. Child (2 y and
older, weight 10–25 kg): PO
50 mg b.i.d.
Hepatic Dosage Adjustment
Child-Pugh class B:
Reduce dose by 50%
Pharmacogenetic Dosage Adjustment
Poor CYP2C9
metabolizers: Start with
½ normal dose
- Give 2 h before/after magnesiumor aluminum-containing
antacids.
- Store in tightly closed container and protect
from light.
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.
Drug: May diminish effectiveness of ACE INHIBITORS; fluconazole
increases celecoxib concentrations;
may increase lithium concentrations; may increase INR in older
patients on warfarin.
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.
Black Box Warning
Celecoxib may
increase the risk of serious, potentially fatal thrombosis, (e.g., MI and
stroke) and GI adverse events (e.g., bleeding, ulceration, and perforation).
Assessment & Drug Effects
- Monitor for S&S of GI bleeding that may
occur suddenly and without warning, especially in older patients.
- Monitor for development of thrombotic events
even in those with no prior history of cardiovascular problems.
- 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.
- Monitor lab tests: Periodic Hct and Hgb, LFTs,
BUN and creatinine, and serum electrolytes.
Patient & Family Education
- Seek immediate medical attention for any of the
following: Chest pain, shortness of breath, sudden weakness, slurring of speech
or other S&S of a stroke.
- Promptly report any of the following: Unexplained
weight gain, edema, skin rash.
- Stop taking celecoxib and promptly report to
prescriber if any of the following occurs: S&S of liver dysfunction
including nausea, fatigue, lethargy, itching, jaundice, abdominal pain, and
flu-like symptoms; S&S of GI ulceration including black, tarry stools and upper
GI distress.
- Avoid using celecoxib during the third trimester
of pregnancy.
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