celecoxib


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celecoxib

 [sel″ĕ-kok´sib]
a nonsteroidal antiinflammatory drug of the cox-2 inhibitors group, administered orally for symptomatic treatment of arthritis.

celecoxib

Celebrex

Pharmacologic class: Nonsteroidal cyclooxygenase-2 (COX-2) inhibitor, nonsteroidal anti-inflammatory drug (NSAID)

Therapeutic class: Antirheumatic

Pregnancy risk category C

FDA Box Warning

• Drug may increase risk of serious cardiovascular thrombotic events, myocardial infarction, and stroke (which can be fatal). Risk may increase with duration of use, and may be greater in patients who have cardiovascular disease or risk factors for it.

• Drug is contraindicated for perioperative pain in setting of coronary artery bypass graft surgery.

• Drug increases risk of serious GI adverse events, including bleeding, ulcers, and stomach or intestinal perforation, which can be fatal. These events can occur at any time during therapy and without warning. Elderly patients are at greater risk.

Action

Exhibits anti-inflammatory, analgesic, and antipyretic action due to inhibition of COX-2 enzyme

Availability

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

Indications and dosages

Ankylosing spondylitis, osteoarthritis
Adults: 200 mg/day P.O. as a single dose or 100 mg P.O. b.i.d.

Rheumatoid arthritis

Adults: 100 to 200 mg P.O. b.i.d.

Adjunctive treatment in familial adenomatous polyposis to decrease the number of adenomatous colorectal polyps

Adults: 400 mg P.O. b.i.d.

Acute pain or primary dysmenorrhea
Adults: 400 mg P.O. once, plus one additional 200 mg-dose as needed on first day; then 200 mg b.i.d. as needed

Juvenile rheumatoid arthritis
Children age 2 and older weighing 10 to 25 kg (22 to 55 lb): 50 mg P.O. b.i.d.
Children age 2 and older weighing 25 kg or more: 100 mg P.O. b.i.d.

Dosage adjustment

• Hepatic impairment
• Patients weighing less than 50 kg (110 lb)

Contraindications

• Hypersensitivity to drug, sulfonamides, or other NSAIDs
• Advanced renal disease
• Severe hepatic impairment
• Sensitivity precipitated by aspirin
• Third trimester of pregnancy
• Breastfeeding

Precautions

Use cautiously in:
• renal insufficiency, hypertension
• history of asthma, urticaria, renal disease, hepatic dysfunction, heart failure
• patients on long-term NSAID therapy
• elderly patients
• pregnant patients in first or second trimester
• children younger than age 18 (safety not established).

Administration

• When administering doses higher than 200/mg daily, give with food or milk to improve drug absorption.

Adverse reactions

CNS: dizziness, drowsiness, headache, insomnia, fatigue, stroke

CV: angina, tachycardia, peripheral edema, myocardial infarction

EENT: ophthalmic effects, tinnitus, epistaxis, pharyngitis, rhinitis, sinusitis

GI: nausea, diarrhea, constipation, abdominal pain, dyspepsia, flatulence, dry mouth, GI bleeding

GU: menorrhagia, renal failure

Hematologic: eosinophilia, ecchymosis, neutropenia, leukopenia, pancytopenia, thrombocytopenia, agranulocytosis, granulocytopenia, aplastic anemia, bone marrow depression

Hepatic: hepatotoxicity

Metabolic: hyperchloremia, hypophosphatemia

Musculoskeletal: back pain, leg cramps

Respiratory: upper respiratory tract infection

Skin: rash

Other: anaphylaxis

Interactions

Drug-drug.Angiotensin-converting enzyme inhibitors, furosemide, thiazides: reduced celecoxib efficacy

Antacids containing aluminum and magnesium: decreased celecoxib blood level

Aspirin (regular doses): increased risk of GI bleeding and GI ulcers

Fluconazole, lithium: increased blood levels of these drugs

Warfarin: increased risk of bleeding

Drug-diagnostic tests.Alanine aminotransferase, aspartate aminotransferase, blood urea nitrogen: increased levels

Hematocrit, hemoglobin: decreased values

Drug-herbs.Dong quai, feverfew, garlic, ginger, horse chestnut, red clover: increased risk of bleeding

White willow: increased risk of GI ulcers

Drug-behaviors.Long-term alcohol use, smoking: GI irritation and bleeding

Patient monitoring

• Monitor CBC, electrolyte levels, creatinine clearance, occult fecal blood test, and liver function test results every 6 to 12 months.

Patient teaching

Advise patient to immediately report bloody stools, vomiting of blood, or signs or symptoms of liver damage (nausea, fatigue, lethargy, pruritus, yellowing of eyes or skin, tenderness in upper right abdomen, or flulike symptoms).
• Instruct patient to take drug with food or milk.
• Tell patient to avoid aspirin and other NSAIDs (such as ibuprofen and naproxen) during therapy.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, herbs, and behaviors mentioned above.

celecoxib

/cel·e·cox·ib/ (sel″ĕ-kok´sib) a nonsteroidal antiinflammatory drug that inhibits cyclooxygenase-1 activity, used for the treatment of osteoarthritis and rheumatoid arthritis.

celecoxib

(sĕl′ə-kŏk′sĭb)
n.
A nonsteroidal anti-inflammatory drug, C17H14F3N3O2S, that selectively inhibits the formation of prostaglandins and is used primarily to treat pain and other symptoms of osteoarthritis, rheumatoid arthritis, and other joint and musculoskeletal conditions.

celecoxib

[sel′ekok′sib]
a nonsteroidal antiinflammatory drug of the cox-2 inhibitors group, administered orally for symptomatic treatment of arthritis.
References in periodicals archive ?
Piroxicam, celecoxib and diclofenac sodium are clinically prescribed NSAIDs for osteoarthritis and rheumatoid arthritis as well as to treat severe pain, ankylosing spondylitis and acute pain in musculoskeletal condition and serious gout [25-27].
The analysis of pain scored revealed a significant improvement in all three groups compared with baseline at days 30, 91, and 182; but both the CS and the celecoxib group showed similar and a statistically greater reduction in pain compared with placebo after six months.
He presented the results of PRECISION-ABPM (Prospective Randomized Evaluation of Celecoxib Integrated Safety Versus Ibuprofen or Naproxen Ambulatory Blood Pressure Measurement).
Patients were randomised in a 1:1:1 fashion to receive celecoxib (100200 mg twice a day), ibuprofen (600800 mg three times a day), or naproxen (375500 mg twice a day) with matching placebos.
Celecoxib has a similar mechanism of action to other well-known anti-inflammatory drugs you might take for a headache, such as aspirin and ibuprofen, and doctors commonly prescribe it for pain relief.
The Adenoma Prevention with Celecoxib (APC) trial compared 2 doses of celecoxib (200 mg or 400 mg twice daily) with placebo for the prevention of colorectal adenomas.
The rate of hospitalization and renal events was significantly lower in the celecoxib group than in the ibuprofen group, but not lower than in the naproxen group.
Simply put, moderate-dose celecoxib did not confer a higher CVD risk compared to these two other NSAIDs and had fewer GI complications.
Experts said the trial found the use of either NSAIDS or celecoxib was associated with "only a low rate of the cardiovascular problems studied".
Adverse reactions in the gastrointestinal tract, kidney, and central nervous system caused by NSAIDs have been reduced using a new generation of NSAIDs, such as celecoxib and rofecoxib.
Celecoxib is effective in treating a number of common acute pain types, including acute tissue injury and postoperative pain.
Our study indicates that hypercholesterolemia results in elevation of homocysteine and C reactive protein while pretreatment with nimesulide was more effective than celecoxib in bringing down their concentrations to the baseline.