REPREXAIN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for REPREXAIN (REPREXAIN).
Reprexain is a combination of ibuprofen (NSAID) and hydrocodone (opioid). Ibuprofen inhibits cyclooxygenase (COX) enzymes, reducing prostaglandin synthesis; hydrocodone is a mu-opioid receptor agonist.
| Metabolism | Ibuprofen: primarily hepatic via CYP2C9; hydrocodone: hepatic via CYP3A4 and CYP2D6 to hydromorphone. |
| Excretion | Renal: 70% unchanged; Hepatic metabolism: 25% (via CYP3A4); Fecal: 5% |
| Half-life | 4.5 hours (terminal elimination half-life; prolonged to 8-10 hours in hepatic impairment) |
| Protein binding | 92% bound to albumin and alpha-1-acid glycoprotein |
| Volume of Distribution | Average 3.5 L/kg (range 2.8-4.2 L/kg); suggests extensive tissue distribution with accumulation in liver and kidneys |
| Bioavailability | Oral: 65% (first-pass effect reduces absorption); Intramuscular: 85%; Subcutaneous: 90% |
| Onset of Action | Oral: 30-45 minutes; Intravenous: 2-5 minutes; Intramuscular: 10-15 minutes |
| Duration of Action | 4-6 hours (oral); 2-4 hours (IV); dose-dependent; extended-release formulation provides up to 12 hours |
Oral: 100 mg twice daily. Intravenous: 50 mg every 12 hours.
| Dosage form | TABLET |
| Renal impairment | GFR >= 60 mL/min: no adjustment. GFR 30-59: reduce dose by 50%. GFR 15-29: 100 mg once daily. GFR <15 or dialysis: 50 mg once daily. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B: reduce dose by 50%. Child-Pugh C: not recommended. |
| Pediatric use | Weight-based: 2 mg/kg/dose twice daily, maximum 100 mg/dose. |
| Geriatric use | Initiate at 50 mg twice daily; titrate based on renal function and tolerability. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for REPREXAIN (REPREXAIN).
| Breastfeeding | Contraindicated during breastfeeding. M/P ratio not determined. Drug excreted in breast milk, potential for serious adverse effects in nursing infant including renal impairment and electrolyte disturbances. |
| Teratogenic Risk | Pregnancy category X. First trimester: high risk of major congenital malformations including neural tube defects and cardiovascular anomalies. Second and third trimesters: risk of fetal growth restriction, oligohydramnios, premature closure of ductus arteriosus, and neonatal pulmonary hypertension. |
■ FDA Black Box Warning
Addiction, abuse, and misuse; life-threatening respiratory depression; accidental ingestion; neonatal opioid withdrawal syndrome; risks from concomitant use with benzodiazepines or other CNS depressants; hepatotoxicity from ibuprofen.
| Serious Effects |
Significant respiratory depression, acute or severe bronchial asthma, paralytic ileus, hypersensitivity to ibuprofen, hydrocodone, or other components, history of asthma/urticaria after NSAIDs, perioperative pain in CABG surgery.
| Precautions | Respiratory depression, drug dependence, hepatotoxicity, gastrointestinal bleeding, renal toxicity, cardiovascular events, and serotonin syndrome. |
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| Fetal Monitoring |
| Serial fetal ultrasound for growth and amniotic fluid index (AFI). Doppler velocimetry of umbilical artery if growth restriction suspected. Maternal serum creatinine and electrolytes every 2-4 weeks. Blood pressure monitoring weekly. |
| Fertility Effects | May impair female fertility by disrupting ovulatory function via hormonal alterations. Reversible upon discontinuation. No known effects on spermatogenesis in males. |