cox 2 inhibitors
- Relief of signs and symptoms of osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, and juvenile rheumatoid arthritis.
- Management of acute pain including primary dysmenorrhea.
- Inhibits the enzyme COX-2. This enzyme is required for the synthesis of prostaglandins.
- Has analgesic, anti-inflammatory, and antipyretic properties.
- Decreased pain and inflammation caused by arthritis or spondylitis.
- Decreased pain.
Absorption: Bioavailability unknown.
Distribution: 97% bound to plasma proteins; extensive tissue distribution.
Metabolism and Excretion: Mostly metabolized by the hepatic CYP2C9 isoenzyme; the CYP2C9 enzyme system exhibits genetic polymorphism; poor metabolizers may have significantly ↑ celecoxib concentrations and an ↑ risk of adverse effects; <3% excreted unchanged in urine and feces.
Half-life: 11 hr.
TIME/ACTION PROFILE (pain reduction)
|PO||24–48 hr||unknown||12–24 hr†|
- Cross-sensitivity may exist with other NSAIDs, including aspirin;
- History of allergic-type reactions to sulfonamides;
- History of asthma, urticaria, or allergic-type reactions to aspirin or other NSAIDs, including the aspirin triad (asthma, nasal polyps, and severe hypersensitivity reactions to aspirin);
- Advanced renal disease;
- Severe hepatic dysfunction;
- Coronary artery bypass graft (CABG) surgery;
- OB: Should not be used in late pregnancy (may cause premature closure of the ductus arteriosus).
Use Cautiously in:
- Cardiovascular disease or risk factors for cardiovascular disease (may ↑ risk of serious cardiovascular thrombotic events, myocardial infarction, and stroke, especially with prolonged use or use of higher doses); avoid use in patients with recent MI or HF;
- Pre-existing renal disease, heart failure, liver dysfunction, concurrent diuretic, or ACE inhibitor therapy (↑ risk of renal impairment);
- Hypertension or fluid retention;
- Renal impairment (may precipitate acute renal failure);
- Serious dehydration (correct deficits before administering);
- Patients who are known or suspected to be poor CYP2C9 metabolizers (↓ initial dose by 50%);
- Pre-existing asthma;
- Pedi: Safety not established in children <2 yr or for longer than 6 mo;
- Geri: Concurrent therapy with corticosteroids or anticoagulants, long duration of NSAID therapy, history of smoking, alcoholism, geriatric patients, or poor general health status (↑ risk of GI bleeding);
- Lactation: Lactation.
Exercise Extreme Caution in:
History of ulcer disease or GI bleeding.
Adverse Reactions/Side Effects
CNS: dizziness, headache, insomnia
CV: HF, MYOCARDIAL INFARCTION, STROKE, THROMBOSIS, edema, hypertension
GI: GI BLEEDING, abdominal pain, diarrhea, dyspepsia, flatulence, nausea
Derm: EXFOLIATIVE DERMATITIS, STEVENS-JOHNSON SYNDROME, TOXIC EPIDERMAL NECROLYSIS, rash
F and E: hyperkalemia
* CAPITALS indicate life-threatening.
Underline indicate most frequent.
- CYP2C9 inhibitors may ↑ levels.
- May ↓ effectiveness of ACE inhibitors, thiazide diuretics, and furosemide.
- Fluconazole ↑ levels (use lowest recommended dosage).
- ↑ risk of bleeding with anticoagulants, aspirin, clopidogrel, ticagrelor, prasugrel, corticosteroids, fibrinolytics, SNRIs, or SSRIs.
- May ↑ serum lithium levels.
- Does not inhibit the cardioprotective effect of low-dose aspirin.
PO: (Adults) Osteoarthritis– 200 mg once daily or 100 mg twice daily. Rheumatoid arthritis– 100–200 mg twice daily. Ankylosing spondylitis– 200 mg once daily or 100 mg twice daily; dose may be ↑ after 6 wk to 400 mg daily. Acute pain, including dysmenorrhea– 400 mg initially, then a 200-mg dose if needed on the first day; then 200 mg twice daily as needed.
PO: (Adults) Moderate hepatic impairment (Child-Pugh Class B)– ↓ dose by 50%.
PO: (Children ≥2 yr, ≥10 kg–≤25 kg): Juvenile rheumatoid arthritis– 50 mg twice daily.
PO: (Children ≥2 yr, ≥25 kg): Juvenile rheumatoid arthritis– 100 mg twice daily.
Availability (generic available)
Capsules: 50 mg, 100 mg, 200 mg, 400 mg
Cost:100 mg $387.18/100, 200 mg $621.67/100, 400 mg $1,576.25/180
- Assess range of motion, degree of swelling, and pain in affected joints before and periodically throughout therapy.
- Assess patient for allergy to sulfonamides, aspirin, or NSAIDs. Patients with these allergies should not receive celecoxib.
- Assess patient for skin rash frequently during therapy. Discontinue at first sign of rash; may be life-threatening. Stevens-Johnson syndrome may develop. Treat symptomatically; may recur once treatment is stopped.
Lab Test Considerations: May cause ↑ AST and ALT levels.
- May cause hypophosphatemia, hyperkalemia, and ↑ BUN.
- Do not confuse with Celexa (citalopram) or Cerebyx (fosphenytoin).
- PO: May be administered without regard to meals. Capsules may be opened and sprinkled on applesauce and ingested immediately with water. Mixture may be stored in the refrigerator for up to 6 hr.
- Instruct patient to take celecoxib exactly as directed. Do not take more than prescribed dose. Increasing doses does not appear to increase effectiveness. Use lowest effective dose for shortest period of time.
- Advise patient to notify health care professional promptly if signs or symptoms of GI toxicity (abdominal pain, black stools), skin rash, unexplained weight gain, edema, or chest pain occurs. Patients should discontinue celecoxib and notify health care professional if signs and symptoms of hepatotoxicity (nausea, fatigue, lethargy, pruritus, jaundice, upper right quadrant tenderness, flu-like symptoms) occur.
- Advise patient to notify health care professional if pregnancy is planned or suspected.
- Reduction in joint pain in patients with osteoarthritis.
- Reduction in joint tenderness, pain, and joint swelling in patients with rheumatoid arthritis and juvenile rheumatoid arthritis.
- Decreased pain.
- Decreased pain with dysmenorrhea.
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