Trade Names:Celebrex- Capsules 50 mg- Capsules 100 mg- Capsules 200 mg- Capsules 400 mg
Reduces inflammation, fever, and pain by inhibiting prostaglandin synthesis, primarily via inhibition of cyclooxygenase-2 (COX-2) isoenzyme.
C max is 705 ng/mL and T max is about 3 h after a single dose. Steady state is reached on or before day 5 with multiple dosing.Food
T max increased about 1 to 2 h and AUC increased 10% to 20% when taken with a high-fat meal.
Approximately 97% protein bound. Vd is about 400 L.
Metabolized in the liver via CYP2C9 to inactive metabolites.
Less than 3% is excreted unchanged in the urine and feces. About 57% is excreted in feces and 27% in urine. The half-life is about 11 h. Cl is about 500 mL/min.
AUC is about 40% lower in patients with a CrCl of 35 to 60 mL/min.Hepatic Function Impairment
AUC is increased about 40% in patients with mild impairment and 180% in patients with moderate impairment. Reduce dosage.Elderly
C max is 40% higher and AUC is 50% higher.Children
10 and 25 kg children are predicted to have 40% and 24% lower Cl, respectively, compared with a 70 kg adult.Race
AUC is about 40% higher in black vs white patients.
Relief of signs and symptoms of osteoarthritis (OA), rheumatoid arthritis (RA) in adults, and ankylosing spondylitis; management of acute pain in adults; treatment of primary dysmenorrhea; reduction of the number of adenomatous colorectal polyps in familial adenomatous polyposis (FAP), as an adjunct to usual care; relief of signs and symptoms of juvenile RA (JRA) in patients 2 yr of age and older.
Adjunctive therapy in the treatment of schizophrenia (inconclusive data); prevention of colorectal cancer; preterm labor.
Hypersensitivity to celecoxib, aspirin, or other NSAIDs; allergy to sulfonamides; previous allergic reactions following aspirin or other NSAID use (eg, asthma, hives, rash); treatment of perioperative pain in the setting of coronary artery bypass graft (CABG) surgery.
PO 400 mg initially followed by an additional 200 mg dose on day 1, if needed, then 200 mg twice daily as needed.Ankylosing SpondylitisAdults
PO 200 mg/day as a single dose or as 100 mg twice daily. If no response after 6 wk, attempt dosage increase to 400 mg/day; if no response after 6 wk at 400 mg/day, discontinue and consider alternate treatment.FAPAdults
PO 400 mg twice daily with food.JRAChildren 2 yr of age and older
PO Children weighing 10 to 25 kg (22 to 55 lb), 50 mg twice daily. Children weighing more than 25 kg (55 lb), 100 mg twice daily.OAAdults
PO 200 mg/day as a single dose or as 100 mg twice daily.RAAdults
PO 100 to 200 mg twice daily.Hepatic Function Impairment
Reduce dose by 50% in patients with moderate hepatic impairment. Not recommended in patients with severe hepatic impairment.Advanced Renal Function Impairment
Not recommended.Poor Metabolizers of CYP2C9 Substrates
Use with caution. Consider starting treatment at half the lowest recommended dose. In patients with JRA who are poor metabolizers, consider using alternative treatment.
Store at 59° to 86°F. The sprinkled capsule contents on applesauce are stable for up to 6 h in the refrigerator.
NSAIDs may diminish the antihypertensive effect of these drugs.Alcohol, corticosteroids, SSRIs (eg, fluoxetine)
May increase risk of GI bleeding.Antacids (containing aluminum or magnesium)
Coadministration may decrease celecoxib plasma levels.Aspirin
Coadministration may result in an increased rate of GI ulceration or other complications.Clopidogrel
Risk of hemorrhage may be increased.CYP2C9 and CYP2D6 inhibitors
There is a potential for drug interaction when coadministered with celecoxib.Diuretics
Patients taking thiazides or loop diuretics may have an impaired response to therapy. Risk of renal impairment may be increased.Fluconazole, voriconazole
Increase in celecoxib plasma concentration may occur.Heparin, low molecular weight heparin (eg, enoxaparin)
Risk of hemorrhagic adverse reactions may be increased. Monitor closely.Lithium
Mean steady-state lithium plasma levels increased about 17% when coadministered.Nonaspirin NSAIDs
Avoid concomitant use because of the potential for increased risk of adverse reactions.Warfarin
Monitor anticoagulant activity, particularly in the first few days, after initiating or changing celecoxib therapy in patients receiving warfarin or similar agents.
None well documented.
Hypertension (13%); aggravated hypertension, angina pectoris, coronary artery disorder, MI, palpitations, tachycardia (less than 2%); deep venous thrombosis, vasculitis (postmarketing).
Headache (16%); dizziness, insomnia (2%); anorexia, anxiety, depression, fatigue, migraine, nervousness, paresthesia, somnolence, vertigo (less than 2%); ageusia, anosmia, aseptic meningitis, fatal intracranial hemorrhage (postmarketing).
Rash (2%); alopecia, cellulitis, contact dermatitis, dermatitis, dry skin, erythematous rash, increased sweating, maculopapular rash, photosensitivity, pruritus, skin disorder, urticaria (less than 2%); erythema multiforme, exfoliative dermatitis, Stevens-Johnson syndrome, TEN (postmarketing).
Nasopharyngitis (6%); eye disorders, sinusitis (5%); rhinitis (2%); deafness, laryngitis, tinnitus (less than 2%).
Diarrhea (11%); dyspepsia (9%); upper abdominal pain (8%); abdominal pain, nausea (7%); vomiting (6%); gastroesophageal reflux (5%); flatulence (2%); constipation, diverticulitis, dry mouth, dysphagia, eructation, esophagitis, gastritis, gastroenteritis, hemorrhoids, hiatal hernia, increased appetite, melena, stomatitis, tenesmus (less than 2%).
Albuminuria, cystitis, dysuria, hematuria, micturition frequency, renal calculus (less than 2%); interstitial nephritis (postmarketing).
Anemia, ecchymosis, epistaxis, thrombocythemia (less than 2%); agranulocytosis, aplastic anemia, leukopenia, pancytopenia (postmarketing).
Abnormal hepatic function, elevated AST and ALT (less than 2%); hepatitis, jaundice, liver failure (postmarketing).
Hypercholesterolemia; hyperglycemia; hypokalemia; increased alkaline phosphatase, BUN, CPK, creatinine, and nonprotein nitrogen; weight gain (less than 2%); hypoglycemia, hyponatremia (postmarketing).
Arthralgia (7%); arthrosis, hypertonia, hypesthesia, leg cramps, myalgia, synovitis, tendonitis (less than 2%).
Upper respiratory tract infection (8%); cough (7%); dyspnea (3%); pharyngitis (2%); aggravated bronchospasm, bronchitis, bronchospasm, coughing, pneumonia (less than 2%).
Pyrexia (9%); injury and poisoning (6%); accidental injury, back pain (3%); peripheral edema (2%); aggravated allergy, allergic reaction, chest pain, cyst not otherwise specified, facial edema, flu-like symptoms, generalized edema, hot flushes, pain, peripheral pain (less than 2%); anaphylactoid reaction, angioedema (postmarketing).
May cause an increased risk of serious CV thrombotic events, MI, and stroke, which may be fatal. This risk may increase with duration of use. Patients with CV disease or risk factors for CV disease may be at higher risk. Celecoxib is contraindicated for the treatment of perioperative pain in the setting of CABG surgery.GI risk
NSAIDs, including celecoxib, caused an increase in serious GI adverse reactions, including bleeding, ulceration, and perforation of the stomach or intestines, which can be fatal. These reactions can occur at any time during use and without warning symptoms. Elderly patients are at higher risk for serious GI events.
Monitor BP closely during initiation and throughout therapy. Monitor CBC and chemistry profile periodically during long-term use. Monitor for signs and symptoms of GI bleeding. Monitor renal function in patients with advanced renal disease. Monitor liver function in patients with signs and symptoms of liver dysfunction. Monitor for the development of abnormal coagulation tests in patients with JRA.
Category C . Category D from 30 weeks' gestation onward. Because celecoxib may cause premature closure of the patent ductus arteriosus, avoid use in late pregnancy.
Excreted in breast milk.
Safety and efficacy not established in children younger than 2 yr of age or less than 10 kg (22 lb) with JRA. For other indications, safety and efficacy not established in patients younger than 18 yr of age.
There have been more spontaneous reports of fatal GI events and acute renal failure in elderly patients.
Severe anaphylactoid reactions and angioedema have occurred.
Not recommended in patients with advanced renal disease.
Not recommended in patients with severe hepatic impairment.
Use not recommended.
Use with caution in patients with preexisting asthma.
Fluid retention and edema have been observed. Use with caution.
Use with caution. Most spontaneous reports of fatal GI events are in debilitated patients.
Can cause serious skin reactions, which may be fatal (eg, Stevens-Johnson syndrome, TEN).
Celecoxib has not been shown to reduce the risk of GI cancer or the need for prophylactic colectomy or other FAP-related surgeries. Therefore, usual care of FAP patients should not be altered.
Use with extreme caution in patients with history of ulcer disease or GI bleeding.
Elevated liver enzymes may occur. Rare cases of severe hepatic reactions (eg, jaundice, hepatic failure) have occurred. Discontinue use if liver disease develops or if systematic manifestations occur (eg, eosinophilia, rash).
Use with caution. Can lead to onset of new hypertension or worsening of preexisting hypertension.
Long-term use of NSAIDs has resulted in renal papillary necrosis and other renal injury. Those at greater risk are patients with impaired renal function, heart failure, or liver dysfunction; those taking diuretics, angiotensin II receptor antagonists, or ACE inhibitors; and elderly patients.
Do not use in patients with a sulfa allergy.
Use with caution because of risk of serious adverse reactions, including DIC.
Acute renal failure, anaphylactoid reactions, coma, drowsiness, epigastric pain, GI bleeding, hypertension, lethargy, nausea, respiratory depression, vomiting.
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