ORUDIS

Clinical safety rating: caution

Comprehensive clinical and safety monograph for ORUDIS (ORUDIS).

How it works

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.

What the body does with it

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.

Classification & Brands

Dosing & administration

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.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for ORUDIS (ORUDIS).

Breastfeeding	Ketoprofen is excreted into human milk in very low amounts (M/P ratio approximately 0.2-0.4). Based on limited data, it is generally considered compatible with breastfeeding, but use lowest effective dose for shortest duration.
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.

Warnings & precautions

■ 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.

Side Effect Profile

Serious Effects

Absolute Contraindications

History of hypersensitivity to ketoprofen or aspirin/NSAIDs; perioperative pain in CABG surgery; active GI bleeding or peptic ulcer disease; severe renal impairment (CrCl <30 mL/min); hyperkalemia; third trimester of pregnancy; use with other NSAIDs including COX-2 inhibitors.

Clinical Precautions

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.

Clinical Tips & Counseling

Drug interactions

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ORUDIS

Clinical safety rating: caution

Comprehensive clinical and safety monograph for ORUDIS (ORUDIS).

How it works

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.

What the body does with it

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.

Classification & Brands

Dosing & administration

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.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for ORUDIS (ORUDIS).

Breastfeeding	Ketoprofen is excreted into human milk in very low amounts (M/P ratio approximately 0.2-0.4). Based on limited data, it is generally considered compatible with breastfeeding, but use lowest effective dose for shortest duration.
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.