ROXILOX
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ROXILOX (ROXILOX).
Roxilox is a nonsteroidal anti-inflammatory drug (NSAID) that inhibits cyclooxygenase (COX-1 and COX-2) enzymes, reducing prostaglandin synthesis and thereby alleviating pain and inflammation.
| Metabolism | Hepatic via CYP2C9 and CYP3A4; undergoes glucuronidation. |
| Excretion | Renal (70-80% unchanged), biliary/fecal (15-20%), remainder metabolized |
| Half-life | Terminal elimination half-life 4.5 hours; prolonged to 18-24 hours in severe renal impairment (CrCl <30 mL/min) |
| Protein binding | ~95% bound to serum albumin |
| Volume of Distribution | 0.3-0.5 L/kg, consistent with distribution in extracellular fluid and moderate tissue penetration |
| Bioavailability | Oral: 60-70% due to moderate first-pass metabolism; IV: 100% |
| Onset of Action | Oral: 30-60 minutes; IV: immediate |
| Duration of Action | Oral: 6-8 hours; IV: 4-6 hours; prolonged in renal impairment |
10 mg orally once daily, with or without food.
| Dosage form | CAPSULE |
| Renal impairment | eGFR 30-89 mL/min: no adjustment; eGFR 15-29 mL/min: 5 mg once daily; eGFR <15 mL/min or dialysis: not recommended. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: 5 mg once daily; Child-Pugh C: not recommended. |
| Pediatric use | Not approved for use in patients <18 years of age; safety and efficacy not established. |
| Geriatric use | No initial dose adjustment required; monitor renal function and titrate cautiously due to age-related decline in GFR. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ROXILOX (ROXILOX).
| Breastfeeding | Excreted in human milk with M/P ratio of 0.8. Limited data; potential for adverse effects in breastfed infant (e.g., diarrhea, rash). Use with caution; monitor infant for symptoms. Alternative agents preferred. |
| Teratogenic Risk | First trimester: No adequate human studies; animal studies show increased risk of skeletal malformations at high doses. Second and third trimesters: Risk of fetal growth restriction and oligohydramnios due to potential uteroplacental vasoconstriction. Avoid unless maternal benefit outweighs risk. |
■ FDA Black Box Warning
Increased risk of serious cardiovascular thrombotic events, including myocardial infarction and stroke, which can be fatal. This risk may increase with duration of use and in patients with cardiovascular risk factors. Roxilox is contraindicated for treatment of perioperative pain in the setting of coronary artery bypass graft (CABG) surgery.
| Serious Effects |
Hypersensitivity to Roxilox or any NSAID; active gastrointestinal bleeding; history of asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs; in the setting of CABG surgery; severe heart failure; advanced renal disease.
| Precautions | Use lowest effective dose for shortest duration; caution in patients with history of gastrointestinal bleeding, renal impairment, fluid retention, hypertension, asthma, and in elderly; monitor renal function, hepatic function, and blood pressure. |
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| Fetal Monitoring |
| Monitor maternal blood pressure and renal function. Assess fetal growth and amniotic fluid volume via ultrasound every 4-6 weeks. Consider non-stress test or biophysical profile in third trimester if uteroplacental insufficiency suspected. |
| Fertility Effects | No adverse effects on fertility observed in animal studies. Human data insufficient; theoretical risk of hormonal disruption at high doses. |