CELEBREX
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CELEBREX (CELEBREX).
Celecoxib is a nonsteroidal anti-inflammatory drug (NSAID) that inhibits cyclooxygenase-2 (COX-2) selectively, thereby reducing the synthesis of prostaglandins involved in inflammation, pain, and fever. It does not significantly inhibit COX-1 at therapeutic concentrations.
| Metabolism | Primarily metabolized by cytochrome P450 enzyme 2C9 (CYP2C9) with minor involvement of CYP3A4. Metabolites include inactive hydroxycelecoxib and carboxycelecoxib. Elimination occurs via urine and feces. |
| Excretion | Primarily hepatic metabolism via CYP2C9; approximately 27% of dose excreted in urine as unchanged drug and metabolites, with about 3% as unchanged celecoxib; 57-70% excreted in feces as metabolites. |
| Half-life | Terminal elimination half-life is approximately 11 hours (range 8-12 hours) in healthy adults; in elderly patients (≥65 years), half-life is prolonged to ~18 hours; in patients with mild-to-moderate hepatic impairment, half-life increased by 2-fold. |
| Protein binding | Approximately 97% bound to albumin; primarily to albumin with minor binding to α1-acid glycoprotein. |
| Volume of Distribution | Apparent volume of distribution at steady state (Vdss) is approximately 400 L (5.7 L/kg for a 70 kg adult), indicating extensive tissue distribution. |
| Bioavailability | Absolute bioavailability after oral administration is not available (not available as intravenous formulation); relative bioavailability compared to oral solution is approximately 100% for capsules; absorption is delayed by high-fat meal (Tmax increased by 1-2 hours, Cmax decreased by about 20%). |
| Onset of Action | Oral: Analgesic effect begins within 1-2 hours; anti-inflammatory effect may require several days to weeks of regular dosing. |
| Duration of Action | Approximately 12-24 hours for pain relief with once or twice daily dosing; sustained anti-inflammatory effect with continued dosing. |
| Molecular Weight | 381.38 |
100-200 mg orally twice daily; for acute pain or primary dysmenorrhea, 400 mg initially followed by 200 mg twice daily as needed.
| Dosage form | CAPSULE |
| Renal impairment | GFR <30 mL/min: reduce dose by 50%; maximum dose 200 mg/day. Not recommended in severe renal impairment (GFR <15 mL/min) or on dialysis. |
| Liver impairment | Child-Pugh Class A: no adjustment. Child-Pugh Class B: reduce dose by 50%; maximum dose 100 mg/day. Class C: contraindicated. |
| Pediatric use | For juvenile rheumatoid arthritis (age >=2 years): weight >=10 kg and <=25 kg: 50 mg twice daily; weight >25 kg: 100 mg twice daily. |
| Geriatric use | Patients >=65 years: initiate at lowest recommended dose (100 mg/day); may increase to 200 mg/day if needed. Monitor renal function and for GI bleeding. |
| 1st trimester | Avoid use; associated with increased risk of cardiovascular malformations and spontaneous abortion. NSAIDs are generally not recommended in the first trimester unless absolutely necessary. |
| 2nd trimester | Use with caution; may cause oligohydramnios and premature closure of ductus arteriosus. Avoid if possible. |
| 3rd trimester | Contraindicated; risk of premature closure of ductus arteriosus, oligohydramnios, and neonatal renal impairment. |
Clinical note
Comprehensive clinical and safety monograph for CELEBREX (CELEBREX).
| Placental transfer | Celecoxib crosses the placenta in humans. Cord blood concentrations are approximately 20-40% of maternal plasma concentrations. |
| Breastfeeding | Celecoxib is excreted into breast milk in small amounts (relative infant dose approximately 0.3-3% of weight-adjusted maternal dose). Compatible with breastfeeding but monitor infant for potential adverse effects such as gastrointestinal disturbances or rash. Avoid in nursing mothers with known sensitivity to NSAIDs. |
■ FDA Black Box Warning
["Increased risk of serious cardiovascular thrombotic events, including myocardial infarction and stroke, which can be fatal. This risk increases with duration of use and in patients with cardiovascular risk factors.","Celecoxib is contraindicated for treatment of perioperative pain in the setting of coronary artery bypass graft (CABG) surgery.","Increased risk of serious gastrointestinal adverse events including bleeding, ulceration, and perforation of the stomach or intestines, which can be fatal."]
| Serious Effects |
Hypersensitivity to celecoxib or sulfonamidesHistory of asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDsCoronary artery bypass graft (CABG) surgeryThird trimester of pregnancy
| Precautions | Cardiovascular thrombotic events: Use lowest effective dose for shortest duration., Gastrointestinal effects: History of peptic ulcer disease or GI bleeding increases risk., Hypertension: Can lead to new-onset hypertension or worsening of pre-existing hypertension., Renal effects: Monitor renal function in patients with pre-existing renal disease, heart failure, liver dysfunction, or those taking diuretics or ACE inhibitors., Anaphylactoid reactions: Avoid in patients with aspirin triad (aspirin sensitivity, nasal polyps, asthma)., Hepatic effects: Monitor liver enzymes; discontinue if signs of hepatic injury occur., Hematologic effects: May inhibit platelet aggregation but not to the same degree as aspirin; monitor for bleeding., Fluid retention and edema: Use with caution in patients with heart failure or hypertension., Pregnancy: Avoid in third trimester due to risk of premature closure of ductus arteriosus., Skin reactions: Serious skin adverse events such as Stevens-Johnson syndrome can occur. |
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| Lactation Rating | L2 (Safer) |
| Teratogenic Risk | Celecoxib (Celebrex) is contraindicated in the third trimester due to risk of premature closure of the ductus arteriosus and oligohydramnios. In first and second trimesters, use is not recommended unless clearly necessary; limited data show possible increased risk of cardiac defects and gastroschisis. NSAIDs are generally associated with increased risk of miscarriage and malformations. |
| Fetal Monitoring | Monitor maternal renal function, blood pressure, and signs of bleeding. For prolonged use beyond 48 hours, fetal ultrasound to assess amniotic fluid volume and ductus arteriosus patency is recommended, especially in third trimester. |
| Fertility Effects | Celecoxib may impair female fertility by interfering with prostaglandin-mediated follicular rupture (luteinized unruptured follicle syndrome). This effect is reversible upon discontinuation. Limited data on male fertility; theoretical risk due to prostaglandin inhibition but no significant adverse effects reported. |
| Food/Dietary | No significant food interactions. Take with food or milk to minimize gastrointestinal upset. Avoid alcohol due to increased risk of GI bleeding. |
| Clinical Pearls | Celecoxib is a COX-2 selective NSAID with lower GI bleeding risk than non-selective NSAIDs, but does not reduce cardiovascular risk. Use lowest effective dose for shortest duration. Contraindicated in sulfonamide allergy, aspirin-sensitive asthma, and CABG perioperative pain. Monitor renal function in elderly, volume-depleted patients, and those on ACE inhibitors, ARBs, or diuretics. |
| Patient Advice | Take with food or milk to reduce stomach upset. · Avoid alcohol while taking celecoxib. · Do not take with other NSAIDs like ibuprofen, naproxen, or aspirin unless directed by your doctor. · Report signs of GI bleeding: black/tarry stools, vomit that looks like coffee grounds, severe stomach pain. · Celecoxib may increase risk of heart attack or stroke; seek emergency if chest pain, shortness of breath, or weakness on one side of body occurs. · If you have sulfa allergy, inform your doctor before taking celecoxib. · Do not use if you are pregnant, especially in the third trimester, unless specifically directed by your doctor. |