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

(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.
References in periodicals archive ?
Theoretically celecoxib, on the other hand, should not alter renal function, due to its specificity, but it has been found to cause papillary necrosis in humans (17) due to COX2 inhibition, that it affects the glomerular filtration rate and therefore behaves like the majority of NSAIDS, in addition to modifying sodium elimination (13, 17).
[13] Pharmacologically, celecoxib acts via selective inhibition of COX-2 and, therefore, provides better safety profile with regards to GI complications compared with nonselective NSAIDs.
Celecoxib for the treatment of mild-tomoderate depression due to acute brucellosis: a double-blind, placebo-controlled, randomized trial.
Celecoxib, Etoricoxib, and Diclofenac Have Comparable Efficacy in Patients With Arthritic Conditions
In this study, we want to determine whether genistein influences conversion of celecoxib or not.
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].
Of these, 199 received CS, 199 received celecoxib, and 205 received placebo.
"Prescription-strength ibuprofen is under pressure--it has a high incidence of new-onset hypertension, particularly when compared to the more selective COX-2 inhibitor celecoxib. Before we did this study, many would have said it's the other way around," observed Dr.
In the on-treatment analysis, the ibuprofen group was significantly more likely to experience cardiovascular and all-cause mortality and renal events than were those on celecoxib (N Engl J Med.
PRECISION-ABPM, (3) a pre-specified four month substudy of the landmark PRECISION trial, (4) was designed to determine the blood pressure effects of the selective COX-2 inhibitor celecoxib compared to the non-selective NSAIDs naproxen and ibuprofen.
The researchers hypothesized that celecoxib, a common anti-inflammatory drug that selectively inhibits the pro-inflammatory enzyme COX-2, would improve stem cell survival and treatment outcomes for chronic wound therapy.