Therapeutic Classification: antirheumatics
Pharmacologic Classification: cox 2 inhibitors
Absorption: Bioavailability unknown.
Distribution: Extensively distributed to tissues.
Protein Binding: 97%.
Metabolism/Excretion: Mostly metabolized by the liver via the CYP2C9 isoenzyme; the CYP2C9 isoenzyme 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.
Contraindicated in:
- Hypersensitivity;
- Cross-sensitivity may exist with other NSAIDs, including aspirin;
- History of allergic-type reactions to sulfonamides;
- History of 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 impairment;
- Coronary artery bypass graft (CABG) surgery;
- HF;
- OB: Avoid use after 30 wk gestation.
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;
- Renal impairment, hepatic impairment, dehydration, or concurrent diuretic, ACE inhibitor, or angiotensin receptor blocker therapy (↑ risk of renal impairment);
- History of long duration of NSAID use, smoking, alcohol use, advanced liver disease, coagulopathy, and poor general health (↑ risk of GI bleeding);
- Hypertension or fluid retention;
- Asthma;
- Patients who are known or suspected to be poor CYP2C9 metabolizers (↓ initial dose by 50%; in patients with juvenile rheumatoid arthritis, use alternative treatment);
- Asthma;
- OB: Use at or after 20 wk gestation may cause fetal or neonatal renal impairment; if treatment is necessary between 20 wk and 30 wk gestation, limit use to the lowest effective dose and shortest duration possible;
- Pedi: Safety not established in children <2 yr or for longer than 6 mo;
- Geri: ↑risk of GI bleeding and renal impairment in older adults.
Exercise Extreme Caution in:
Osteoarthritis
- PO (Adults ): 200 mg once daily or 100 mg twice daily. CYP2C9 poor metabolizers:↓ dose by 50%.
Hepatic Impairment
- PO (Adults ): Moderate hepatic impairment:↓ dose by 50%.
Rheumatoid Arthritis
- PO (Adults ): 100–200 mg twice daily (capsules). CYP2C9 poor metabolizers:↓ dose by 50%.
Hepatic Impairment
- PO (Adults ): Moderate hepatic impairment:↓ dose by 50%.
Ankylosing Spondylitis
- PO (Adults ): 200 mg once daily (capsules) or 100 mg twice daily (capsules); may ↑ dose after 6 wk to 400 mg/day. CYP2C9 poor metabolizers:↓ dose by 50%.
Hepatic Impairment
- PO (Adults ): Moderate hepatic impairment:↓ dose by 50%.
Juvenile Rheumatoid Arthritis
- PO (Children ≥2 yr, 10–25 kg): 50 mg twice daily (capsules).
- PO (Children ≥2 yr, ≥25 kg): 100 mg twice daily (capsules).
Hepatic Impairment
- PO (Children ≥2 yr): Moderate hepatic impairment:↓ dose by 50%.
Acute Pain or Primary Dysmenorrhea
- PO (Adults ): 400 mg initially, then a 200-mg dose if needed on the first day; then 200 mg twice daily as needed (capsules). CYP2C9 poor metabolizers:↓ dose by 50%.
Hepatic Impairment
- PO (Adults ): Moderate hepatic impairment:↓ dose by 50%.
Acute Treatment of Migraine
- PO (Adults ): 120 mg as a single dose (not to exceed 120 mg/24 hr). CYP2C9 poor metabolizers: 60 mg as a single dose (not to exceed 60 mg/24 hr).
Hepatic Impairment
- PO (Adults ): Moderate hepatic impairment: 60 mg as a single dose (not to exceed 60 mg/24 hr).
