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) |
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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for PROFENAL (PROFENAL).
| Breastfeeding | Excreted in breast milk in low amounts; M/P ratio not established. Use with caution due to potential adverse effects on neonatal cardiovascular and renal systems. |
| 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. |
■ 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 |
Known hypersensitivity to PROFENAL or any NSAID; history of asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs; peri-operative pain in CABG surgery; advanced renal disease; pregnancy (third trimester).
| 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. |
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| 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. |