ORUDIS
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ORUDIS (ORUDIS).
Nonsteroidal anti-inflammatory drug (NSAID) that inhibits cyclooxygenase (COX-1 and COX-2), thereby reducing prostaglandin synthesis, leading to anti-inflammatory, analgesic, and antipyretic effects.
| Metabolism | Ketoprofen is extensively metabolized in the liver via glucuronidation, primarily by UDP-glucuronosyltransferases (UGTs), with minor involvement of CYP3A4 and CYP2C9. The major metabolite is ketoprofen glucuronide. |
| Excretion | Renal: ~60% as metabolites (glucuronides of ketoprofen and hydroxylated metabolites); fecal: ~30% (biliary excretion); unchanged drug: <1% in urine. |
| Half-life | Terminal half-life: ~1.5-2 hours for immediate-release; 30-50% increase in elderly due to reduced clearance. Clinical context: short half-life requires frequent dosing for sustained analgesia; no accumulation with q6-8h dosing. |
| Protein binding | High: ~99% bound to albumin. Drug is primarily bound to serum albumin, resulting in low free fraction. |
| Volume of Distribution | 0.1-0.2 L/kg. Small Vd indicates limited tissue distribution; primarily remains in plasma and extracellular fluid. Clinical meaning: loading doses not typically required; drug is not extensively distributed into tissues. |
| Bioavailability | Oral: ~90% (immediate-release). IM: ~100% (complete). Rectal: ~70-80%. Topical: ~1-5% systemically absorbed. |
| Onset of Action | Oral immediate-release: 30-60 min; IM: 15-30 min; IV: 5-10 min; Topical: 2-4 hours. Onset of analgesia correlates with peak plasma concentrations. |
| Duration of Action | Oral immediate-release: 4-6 hours; IM: 4-6 hours; IV: 4-6 hours; Topical: 4-6 hours. Duration is limited by half-life; extended-release not available. |
| Molecular Weight | 254.28 |
Oral: 50 mg three times daily or 75 mg twice daily; maximum 300 mg/day. Topical: Apply 2-4 g of gel or cream to affected area four times daily. Intramuscular: 50-100 mg every 4-6 hours; maximum 200 mg/day.
| Dosage form | CAPSULE |
| Renal impairment | GFR 30-89 mL/min: Reduce dose by 50% or extend interval. GFR <30 mL/min: Avoid use or use with caution, maximum dose 100 mg/day. |
| Liver impairment | Child-Pugh A: No adjustment. Child-Pugh B: Reduce dose by 50%. Child-Pugh C: Contraindicated. |
| Pediatric use | Not recommended for children under 12 years. For children ≥12 years: 50 mg twice daily with food; maximum 150 mg/day. |
| Geriatric use | Start at lowest effective dose (e.g., 25 mg twice daily), maximum 150 mg/day. Monitor renal function, gastrointestinal side effects, and bleeding risk. |
| 1st trimester | Avoid; associated with increased risk of congenital malformations, particularly cardiovascular and gastroschisis. |
| 2nd trimester | Avoid; risk of oligohydramnios and premature ductus arteriosus constriction. |
| 3rd trimester | Contraindicated; risk of premature closure of ductus arteriosus, oligohydramnios, and neonatal complications. |
Clinical note
Comprehensive clinical and safety monograph for ORUDIS (ORUDIS).
| Placental transfer | Ketoprofen crosses the placenta; fetal concentrations can reach 10-30% of maternal levels. Animal studies show significant transfer. |
| Breastfeeding | Ketoprofen (Orudis) is excreted into breast milk in low amounts. Due to potential adverse effects in neonates (e.g., renal impairment, gastrointestinal bleeding), caution is advised. Use only if clearly needed and monitor infant. |
■ 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. ORUDIS is contraindicated for treatment of perioperative pain in the setting of coronary artery bypass graft (CABG) surgery.
| Serious Effects |
History of hypersensitivity to ketoprofen or any NSAIDActive peptic ulcer disease or gastrointestinal bleedingSevere renal insufficiency (eGFR <30 mL/min/1.73m^2)Severe hepatic impairment (Child-Pugh class C)History of asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDsTreatment of perioperative pain in the setting of coronary artery bypass graft (CABG) surgery
| Precautions | Cardiovascular thrombotic risk; GI bleeding, ulceration, and perforation; hypertension; fluid retention; renal toxicity; hepatic toxicity; anaphylactoid reactions; serious skin reactions; hematologic toxicity; use in pregnancy (avoid in late pregnancy); inhibition of platelet function; use with caution in elderly and patients with prior GI disease. |
Loading safety data…
| Lactation Rating | L3 (Moderately Safe) or 'Caution' according to Hale's lactation risk categories. |
| Teratogenic Risk | Pregnancy Category C (1st and 2nd trimesters) and Category D (3rd trimester). Avoid use during 3rd trimester due to risk of premature closure of ductus arteriosus and oligohydramnios. Avoid use during 1st and 2nd trimesters unless clearly needed; risk of congenital malformations is low but cannot be excluded. |
| Fetal Monitoring | Monitor maternal renal function, blood pressure, and signs of bleeding. If used in pregnancy, monitor amniotic fluid index and ductus arteriosus via ultrasound if prolonged use. |
| Fertility Effects | May impair female fertility via inhibition of ovulation (reversible) and affect male fertility through prostaglandin-mediated effects on spermatogenesis; clinical significance is unclear. |
| Food/Dietary |
| Take with food or milk to minimize gastrointestinal irritation. Avoid alcohol. High-fat meals may delay absorption but do not affect extent. |
| Clinical Pearls | Orudis (ketoprofen) is a nonsteroidal anti-inflammatory drug (NSAID) with a short half-life (2-4 hours) and moderate COX-2 selectivity. It is more likely to cause gastrointestinal irritation than ibuprofen. Avoid in patients with aspirin-sensitive asthma. Maximum analgesic effect occurs at doses above 75 mg, but increasing dose increases toxicity. Use lowest effective dose for shortest duration. Renal function monitoring recommended in elderly, volume-depleted, or those on diuretics/ACE inhibitors. |
| Patient Advice | Take with food or milk to reduce stomach upset. · Avoid alcohol while taking this medication. · Do not take with other NSAIDs or aspirin without doctor approval. · Report signs of stomach bleeding: black/tarry stools, coffee-ground vomit. · May cause dizziness or drowsiness; avoid driving if affected. · Use sunscreen as this drug may increase sun sensitivity. · Do not use longer than prescribed without consulting doctor. |