PROFENAL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for PROFENAL (PROFENAL).
Nonsteroidal anti-inflammatory drug (NSAID) that inhibits cyclooxygenase (COX-1 and COX-2) enzymes, reducing prostaglandin synthesis, thereby exerting analgesic, anti-inflammatory, and antipyretic effects.
| Metabolism | Primarily metabolized in the liver via glucuronidation and hydroxylation, with minor involvement of cytochrome P450 enzymes (CYP2C9). |
| Excretion | Primarily renal (approximately 70% as metabolites, <5% unchanged), biliary/fecal (30%) |
| Half-life | 6-8 hours (terminal); requires dosing every 6-8 hours to maintain therapeutic levels |
| Protein binding | 99% bound, primarily to albumin |
| Volume of Distribution | 0.1-0.2 L/kg; low Vd indicates limited extravascular distribution |
| Bioavailability | Oral: 80-90%; Topical: 2-5% (systemic); IV: 100% |
| Onset of Action | Oral: 1-2 hours; Topical: 1-2 hours; IV: immediate |
| Duration of Action | Oral: 6-8 hours; Topical: 6-8 hours; IV: 4-6 hours (clinical effect varies with pain intensity) |
| Molecular Weight | 295.34 |
600 mg orally every 6 to 8 hours as needed for pain; or 1000 mg orally every 6 to 8 hours for antipyresis; maximum single dose 1000 mg, maximum daily dose 4000 mg.
| Dosage form | SOLUTION/DROPS |
| Renal impairment | CrCl 30-60 mL/min: 600 mg every 12 hours; CrCl 15-29 mL/min: 600 mg every 24 hours; CrCl <15 mL/min: 600 mg every 48 hours; hemodialysis: 600 mg every 48 hours. |
| Liver impairment | Child-Pugh Class A: no adjustment; Child-Pugh Class B: reduce dose by 50%; Child-Pugh Class C: contraindicated. |
| Pediatric use | 10-15 mg/kg per dose orally every 6-8 hours; maximum 60 mg/kg/day, not to exceed 2400 mg/day. |
| Geriatric use | Initial dose: 600 mg orally every 8 hours, titrate to response; use minimum effective dose; monitor renal function; maximum daily dose 3000 mg. |
| 1st trimester | Use is contraindicated due to risk of teratogenicity; NSAIDs are associated with cardiac defects and gastroschisis. Avoid in first trimester. |
| 2nd trimester | Use only if clearly needed and benefit outweighs risk; may cause oligohydramnios and fetal renal dysfunction. Short-term use if necessary. |
| 3rd trimester | Contraindicated due to risk of premature closure of ductus arteriosus, oligohydramnios, and neonatal pulmonary hypertension. Avoid in third trimester. |
Clinical note
Comprehensive clinical and safety monograph for PROFENAL (PROFENAL).
| Placental transfer | NSAIDs cross placenta via passive diffusion; extent depends on drug properties. Protein binding >99% limits transfer, but fetal levels can reach 10-20% of maternal. Documented transfer in animal models and some human studies. |
| Breastfeeding | Limited human data; NSAIDs are excreted in breast milk in low amounts. Risk to infant is low with short-term use, but long-term use not recommended due to potential for adverse effects. Monitor infant for gastrointestinal disturbance. |
■ FDA Black Box Warning
NSAIDs may increase the risk of serious cardiovascular thrombotic events, myocardial infarction, and stroke, which can be fatal. Risk increases with duration of use and in patients with cardiovascular risk factors. Contraindicated for treatment of peri-operative pain in coronary artery bypass graft (CABG) surgery.
| Serious Effects |
Hypersensitivity to PROFENAL or any NSAIDHistory of asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDsActive peptic ulcer disease or gastrointestinal bleedingSevere uncontrolled heart failureTreatment of perioperative pain in the setting of coronary artery bypass graft (CABG) surgeryAdvanced renal disease or renal impairment (CrCl <30 mL/min)Third trimester of pregnancy
| Precautions | Risk of serious gastrointestinal adverse events including bleeding, ulceration, and perforation; cardiovascular risk; renal toxicity; hypertension; fluid retention; hypersensitivity reactions; hepatic impairment; asthma exacerbation; use with caution in elderly. |
| Food/Dietary | Avoid alcohol as it increases risk of gastrointestinal bleeding. Taking with food or milk can decrease gastric irritation. No specific foods contraindicated, but a balanced diet is recommended. |
Loading safety data…
| Lactation Rating | L2 (Limited Data - Probably Compatible) |
| Teratogenic Risk | Pregnancy Category C. First trimester: Risk of spontaneous abortion and congenital malformations (e.g., cardiac defects) associated with NSAID use. Second trimester: Avoid due to potential fetal renal impairment and oligohydramnios. Third trimester: Contraindicated due to risk of premature closure of ductus arteriosus and persistent pulmonary hypertension. |
| Fetal Monitoring | Monitor fetal echocardiography if used in second trimester. Ultrasound for amniotic fluid index. Fetal ductus arteriosus assessment if third trimester exposure. Maternal renal function and blood pressure monitoring. |
| Fertility Effects | May impair female fertility via inhibition of prostaglandin synthesis affecting ovulation. Reversible upon discontinuation. No known male fertility effects. |
| Clinical Pearls | PROFENAL (ketoprofen) is a nonsteroidal anti-inflammatory drug (NSAID) with potent analgesic, anti-inflammatory, and antipyretic properties. It has a short half-life (1.5-2 hours) and is highly protein-bound (99%). Use with caution in patients with impaired renal function, as it reduces prostaglandin-mediated renal blood flow. Avoid concomitant use with other NSAIDs or anticoagulants due to increased bleeding risk. Monitor for gastrointestinal ulcers and bleeding, especially in elderly or those with prior GI history. May cause photosensitivity; advise sun protection. |
| Patient Advice | Take with food or milk to reduce stomach upset. · Do not drink alcohol while taking this medication. · Report any signs of stomach bleeding, such as black stools or vomiting blood. · Avoid prolonged sun exposure; use sunscreen and protective clothing. · Do not take with other NSAIDs or pain relievers like ibuprofen or aspirin. · Inform your doctor if you have kidney disease, high blood pressure, or a history of stomach ulcers. · Contact your doctor if you experience swelling, rapid weight gain, or shortness of breath. |