ORUVAIL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ORUVAIL (ORUVAIL).
Nonsteroidal anti-inflammatory drug (NSAID) that inhibits cyclooxygenase (COX-1 and COX-2), thereby reducing prostaglandin synthesis, leading to decreased inflammation, pain, and fever.
| Metabolism | Primarily hepatic via CYP2C9; undergoes extensive first-pass metabolism. Major metabolites include hydroxylated and carboxylated derivatives. |
| Excretion | Primarily renal excretion of metabolites (60-80%) with less than 1% unchanged drug; biliary/fecal excretion accounts for 20-40%. |
| Half-life | 5-9 hours (terminal elimination half-life); in elderly or renal impairment, may extend up to 20 hours; clinical context: dosing adjustments recommended in renal impairment. |
| Protein binding | 99% bound primarily to albumin. |
| Volume of Distribution | 0.1-0.2 L/kg; indicates low tissue distribution consistent with extensive protein binding. |
| Bioavailability | Oral: 80-100% (immediate-release); topical: approximately 5% systemic absorption. |
| Onset of Action | Oral: 1-2 hours (analgesic effect); topical: 2-4 hours. |
| Duration of Action | Oral: 6-8 hours; topical: 8-12 hours; clinical notes: duration may be prolonged with extended-release formulations. |
100 to 200 mg orally twice daily
| Dosage form | CAPSULE, EXTENDED RELEASE |
| Renal impairment | GFR 30-89 mL/min: no adjustment; GFR <30 mL/min: contraindicated |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B or C: contraindicated |
| Pediatric use | Not recommended for use in pediatric patients |
| Geriatric use | Initiate at lowest effective dose (100 mg/day); monitor renal function and gastrointestinal bleeding risk |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ORUVAIL (ORUVAIL).
| Breastfeeding | Minimal excretion in breast milk (M/P ratio not reported). Use with caution; may cause adverse effects in neonates. Consider alternative analgesics. |
| Teratogenic Risk | First trimester: Avoid; associated with increased risk of cardiac defects and gastroschisis (OR 1.21-3.08). Second trimester: Caution; NSAIDs may cause oligohydramnios. Third trimester: Contraindicated; risk of premature ductus arteriosus closure and persistent pulmonary hypertension. |
| Fetal Monitoring |
■ FDA Black Box Warning
Nonsteroidal anti-inflammatory drugs (NSAIDs) cause an increased risk of serious cardiovascular thrombotic events, including myocardial infarction and stroke, which can be fatal. This risk may increase with duration of use. Patients with cardiovascular disease or risk factors for cardiovascular disease may be at greater risk. Oruvail is contraindicated for the treatment of peri-operative pain in the setting of coronary artery bypass graft (CABG) surgery.
| Serious Effects |
Hypersensitivity to ketoprofen or any component of the formulation; history of asthma, urticaria, or other allergic-type reactions after taking aspirin or other NSAIDs; peri-operative pain in the setting of coronary artery bypass graft (CABG) surgery; advanced renal disease; active GI bleeding or ulceration.
| Precautions | Cardiovascular thrombotic events; gastrointestinal bleeding, ulceration, and perforation; hypertension; congestive heart failure; renal toxicity; anaphylactoid reactions; serious skin reactions; hematologic toxicity; use with caution in patients with asthma, pre-existing renal impairment, or hepatic impairment. |
Loading safety data…
| Monitor fetal echocardiography if used in 1st trimester. Ultrasound for amniotic fluid volume if used >48 hours after 20 weeks. Monitor ductus arteriosus with Doppler in 3rd trimester. |
| Fertility Effects | Reversible inhibition of ovulation due to prostaglandin synthesis inhibition. May delay follicular rupture. Impact on male fertility not established. |