Nonsteroidal Anti-inflammatory Drug (NSAID), COX-2
Relief of the signs and symptoms of osteoarthritis; relief of the signs and
symptoms of rheumatoid arthritis in adults
C (D after 34 weeks gestation or close to delivery)
In late pregnancy may cause premature closure of the ductus arteriosus. In
animal studies, celecoxib has been found to be excreted in milk; it is not known
whether celecoxib is excreted in human milk. Because many drugs are excreted in
milk, and the potential for serious adverse reactions exists, a decision should
be made whether to discontinue nursing or discontinue the drug, taking into
account the importance of the drug to the mother.
Hypersensitivity to celecoxib or any component, sulfonamides, aspirin, or
other nonsteroidal anti-inflammatory drugs (NSAIDs)
Gastrointestinal irritation, ulceration, bleeding, and perforation may occur
with NSAIDs (it is unclear whether celecoxib is associated with rates of these
events which are similar to nonselective NSAIDs). Use with caution in patients
with a history of GI disease (bleeding or ulcers), decreased renal function,
hepatic disease, congestive heart failure, hypertension, or asthma.
Anaphylactoid reactions may occur, even with no prior exposure to celecoxib. Use
caution in patients with known or suspected deficiency of cytochrome P-450
>10%: Central nervous system: Headache (15.8%)
2% to 10%:
Cardiovascular: Peripheral edema (2.1%)
Central nervous system: Insomnia (2.3%), dizziness (2%)
Dermatologic: Skin rash (2.2%)
Gastrointestinal: Dyspepsia (8.8%), diarrhea (5.6%), abdominal pain (4.1%),
nausea (3.5%), flatulence (2.2%)
Neuromuscular & skeletal: Back pain (2.8%)
Respiratory: Upper respiratory tract infection (8.1%), sinusitis (5%),
pharyngitis (2.3%), rhinitis (2%)
Miscellaneous: Accidental injury (2.9%)
0.1% to 2%:
Cardiovascular: Hypertension (aggravated), chest pain, myocardial infarction,
palpitation, tachycardia, facial edema, peripheral edema
Central nervous system: Migraine, vertigo, hypoesthesia, fatigue, fever,
pain, hypotonia, anxiety, depression, nervousness, somnolence
Dermatologic: Alopecia, dermatitis, photosensitivity, pruritus, rash
(maculopapular), rash (erythematous), dry skin, urticaria
Endocrine & metabolic: Hot flashes, diabetes mellitus, hyperglycemia,
hypercholesterolemia, breast pain, dysmenorrhea, menstrual disturbances,
Gastrointestinal: Constipation, tenesmus, diverticulitis, eructation,
esophagitis, gastroenteritis, vomiting, gastroesophageal reflux, hemorrhoids,
hiatal hernia, melena, stomatitis, anorexia, increased appetite, taste
disturbance, dry mouth, tooth disorder, weight gain
Genitourinary: Prostate disorder, vaginal bleeding, vaginitis, monilial
vaginitis, dysuria, cystitis, urinary frequency, incontinence, urinary tract
Hepatic: Elevated transaminases, increased alkaline phosphatase
Hematologic: Anemia, thrombocytopenia, ecchymosis
Neuromuscular & skeletal: Leg cramps, increased CPK, neck stiffness,
arthralgia, myalgia, bone disorder, fracture, synovitis, tendonitis, neuralgia,
paresthesia, neuropathy, weakness
Ocular: Glaucoma, blurred vision, cataract, conjunctivitis, eye pain
Otic: Deafness, tinnitus, earache, otitis media
Renal: Increased BUN, increased creatinine, albuminuria, hematuria, renal
Respiratory: Bronchitis, bronchospasm, cough, dyspnea, laryngitis, pneumonia,
Miscellaneous: Allergic reactions, flu-like syndrome, breast cancer, herpes
infection, bacterial infection, moniliasis, viral infection, increased
<0.1% (limited to severe): Congestive heart failure, ventricular
fibrillation, pulmonary embolism, syncope, cerebrovascular accident, gangrene,
thrombophlebitis, thrombocytopenia, ataxia, acute renal failure, intestinal
obstruction, pancreatitis, intestinal perforation, gastrointestinal bleeding,
colitis, esophageal perforation, sepsis, sudden death
Symptoms may include epigastric pain, drowsiness, lethargy, nausea, and
vomiting; gastrointestinal bleeding may occur. Rare manifestations include
hypertension, respiratory depression, coma, and acute renal failure.
Treatment is symptomatic and supportive; forced diuresis, hemodialysis and/or
urinary alkalinization may not be useful
Celecoxib may be a cytochrome oxidase P-450 isoenzyme 2C9 substrate and an
inhibitor of isoenzyme 2D6
Increased effect: Inhibitors of isoenzyme 2C9 may result in significant
increases in celecoxib concentrations. Coadministration of drugs by 2D6 may
result in increased serum concentrations of these agents. Fluconazole increases
celecoxib concentrations two-fold. Lithium concentrations may be increased by
celecoxib. Celecoxib may be used with low-dose aspirin, however rates of
gastrointestinal bleeding may be increased with coadministration. May increase
INR when used concurrently with warfarin (case reports).
Inhibits prostaglandin synthesis by decreasing the activity of the enzyme,
cyclooxygenase-2 (COX-2), which results in decreased formation of prostaglandin
precursors. Celecoxib does not inhibit cyclooxygenase-1 (COX-1) at therapeutic
Distribution: Vd (apparent): 400 L
Protein binding: 97% (albumin)
Metabolism: Metabolized by cytochrome P-450 isoenzyme 2C9 (CYP 2C9)
Bioavailability, absolute: Has not been determined
Half-life: 11 hours
Time to peak: 3 hours
Elimination: In urine as metabolites (<3% unchanged drug)
Rheumatoid arthritis: 100-200 mg twice daily
Dosing adjustment in renal impairment: No specific dosage adjustment
Dosing adjustment in hepatic impairment: Reduced dosage is
recommended (AUC may be increased by 40% to 180%)
Dosing adjustment for elderly: No specific adjustment is recommended.
However, the AUC in elderly patients may be increased by 50% as compared to
younger subjects. Use the lowest recommended dose in patients weighing <50
Peak concentrations are delayed and AUC is increased by 10% to 20% when taken
with a high-fat meal; celecoxib may be taken without regard to
|Mental Health: Effects
on Mental Status|
May cause dizziness and insomnia; may rarely, cause anxiety, depression,
nervousness, or somnolence
Effects on Psychiatric
Effects of benzodiazepines and antidepressants may be altered. Lithium
concentrations may be increased by celecoxib via decreased renal lithium
clearance; dose adjustment may be needed.
|Dental Health: Local
No information available to require special precautions
Effects on Dental Treatment|
Nonselective NSAIDs are known to reversibly decrease platelet aggregation via
mechanisms different than observed with aspirin. According to the manufacturer,
celecoxib, at single dose up to 800 mg and multiple doses of 600 mg twice daily,
had no effect on platelet aggregation or bleeding time. Comparative NSAIDs
(naproxen 500 mg twice daily, ibuprofen 800 mg three times daily or diclofenac
75 mg twice daily) significantly reduced platelet aggregation and prolonged the
Do not take more than recommended dose. May be taken with food to reduce GI
upset. Do not take with antacids. Avoid alcohol, aspirin, and OTC medication
unless approved by prescriber. You may experience dizziness, confusion, or
blurred vision (avoid driving or engaging in tasks requiring alertness until
response to drug is known); anorexia, nausea, vomiting, taste disturbance,
gastric distress (small frequent meals, frequent mouth care, sucking lozenges,
or chewing gum may help). GI bleeding, ulceration, or perforation can occur with
or without pain; it is unclear whether celecoxib has rates of these events which
are similar to nonselective NSAIDs. Stop taking medication and report
immediately stomach pain or cramping, unusual bleeding or bruising, or blood in
vomitus, stool, or urine. Report persistent insomnia; skin rash; unusual fatigue
or easy bruising or bleeding; muscle pain, tremors, or weakness; sudden weight
gain; changes in hearing (ringing in ears); changes in vision; changes in
urination pattern; or respiratory difficulty. Pregnancy/breast-feeding
precautions: Inform prescriber if you are or intend to be pregnant. Consult
prescriber if breast-feeding.
Capsule: 100 mg, 200 mg
Geis GS, et al,
"Efficacy and Safety of Celecoxib, A Specific COX-2 Inhibitor, in Patients With Rheumatoid Arthritis,"
Arthritis Rheum, 1998, 41(9 Suppl):S316:1699.
Karim A, et al,
"Celecoxib, A Specific COX-2 Inhibitor, Lacks Significant Drug-Drug Interactions With Methotrexate or Warfarin,"
Arthritis Rheum, 1998, 41(9 Suppl):S315:1698.
"Pain Management in Osteoarthritis: The Role of COX-2 Inhibitors," J
Rheumatol, 1997, 24(Suppl 49):20-4.
Lipsky PE and Isakson PC,
"Outcome of Specific COX-2 Inhibition in Rheumatoid Arthritis," J
Rheumatol, 1997, 24(Suppl 49):9-14.
Mengle-Gaw L, et al,
"A Study of the Platelet Effects of SC-58635, A Novel COX-2 Selective Inhibitor,"
Arthritis Rheum, 1998, 41(9 Suppl):S93:374.
Needleman P and Isakson PC, "The Discovery and Function of COX-2," J
Rheumatol, 1997, 24(Suppl 49):6-8.
Simon LS, et al,
"Preliminary Study of the Safety and Efficacy of SC-58635, A Novel Cyclo-oxygenase 2 Inhibitor: Efficacy and Safety in Two Placebo-Controlled Trials in Osteoarthritis and Rheumatoid Arthritis, and Studies of Gastrointestinal and Platelet Effects,"
Arthritis Rheum, 1998, 41:1591-1602.
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