WYGESIC
Clinical safety rating: caution
Comprehensive clinical and safety monograph for WYGESIC (WYGESIC).
WYGESIC (ibuprofen and hydrocodone) combines a nonsteroidal anti-inflammatory drug (ibuprofen) that inhibits cyclooxygenase (COX-1 and COX-2) enzymes, reducing prostaglandin synthesis, and a narcotic analgesic (hydrocodone) that acts as a mu-opioid receptor agonist.
| Metabolism | Hydrocodone is metabolized primarily via CYP2D6 and CYP3A4 mediated O-demethylation and N-demethylation to hydromorphone and norhydrocodone, respectively. Ibuprofen is metabolized via CYP2C9 and CYP2C8. |
| Excretion | Primarily renal: 90% as unchanged drug and glucuronide conjugate; <5% fecal. |
| Half-life | 3–4 hours in healthy adults; prolonged to 5–6 hours in moderate renal impairment (CrCl 30–50 mL/min) and >11 hours in severe renal impairment (CrCl <30 mL/min). |
| Protein binding | 20–25% bound to albumin. |
| Volume of Distribution | 3.0–4.7 L/kg; indicates extensive tissue distribution. |
| Bioavailability | Oral: 50–70% (first-pass effect); rectal: 50–60%; intravenous: 100%. |
| Onset of Action | Oral: 30–60 minutes; rectal: 60–90 minutes; intravenous: 5–10 minutes. |
| Duration of Action | Oral/rectal: 4–6 hours; intravenous: 3–5 hours; prolonged in hepatic or renal impairment. |
1-2 tablets (paracetamol 325 mg / tramadol 37.5 mg) orally every 4-6 hours as needed for pain, not to exceed 8 tablets per day.
| Dosage form | TABLET |
| Renal impairment | CrCl ≥30 mL/min: no adjustment; CrCl <30 mL/min: extend dosing interval to every 12 hours, maximum 4 tablets per day. Not recommended for CrCl <10 mL/min. |
| Liver impairment | Child-Pugh Class A: no adjustment; Child-Pugh Class B: extend interval to every 12 hours; Child-Pugh Class C: avoid use. |
| Pediatric use | Weight ≥50 kg: same as adult; weight 36-49 kg: 1 tablet (paracetamol 325 mg / tramadol 37.5 mg) every 4-6 hours, max 4 tablets daily. Not recommended for weight <36 kg. |
| Geriatric use | Patients >75 years: initial dose 1 tablet every 6 hours; maximum 4 tablets per day. Use with caution due to increased risk of respiratory depression and falls. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for WYGESIC (WYGESIC).
| Breastfeeding | Excreted into breast milk; relative infant dose approximately 2-4% of maternal weight-adjusted dose. M/P ratio not established. Use with caution; monitor infant for sedation and poor feeding. Consider benefits vs. risks. |
| Teratogenic Risk | First trimester: Limited human data; animal studies show no consistent teratogenicity. Second and third trimesters: Prolonged use may cause neonatal withdrawal; high doses near term associated with respiratory depression in neonate. FDA Pregnancy Category C. |
| Fetal Monitoring |
■ FDA Black Box Warning
Risk of addiction, abuse, and misuse; life-threatening respiratory depression; accidental ingestion of even one dose of hydrocodone, especially by children, can result in fatal overdose; neonatal opioid withdrawal syndrome; cytochrome P450 3A4 interaction; risks from concomitant use with benzodiazepines or other CNS depressants; risk of cardiovascular thrombotic events (ibuprofen); serious gastrointestinal adverse events including bleeding, ulceration, and perforation.
| Serious Effects |
["Hypersensitivity to hydrocodone, ibuprofen, or any component of the product","Significant respiratory depression","Acute or severe bronchial asthma in an unmonitored setting or in absence of resuscitative equipment","Known or suspected gastrointestinal obstruction, including paralytic ileus","History of asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs","In the setting of coronary artery bypass graft (CABG) surgery"]
| Precautions | ["Addiction, abuse, and misuse","Life-threatening respiratory depression","Accidental ingestion","Neonatal opioid withdrawal syndrome","Cytochrome P450 3A4 interaction","Risks from concomitant use with benzodiazepines or other CNS depressants","Risk of cardiovascular thrombotic events (NSAIDs)","Gastrointestinal bleeding, ulceration, and perforation","Hypertension and heart failure","Renal toxicity","Anaphylactoid reactions","Serious skin reactions","Drug abuse and dependence","Driving and operating machinery"] |
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| Monitor maternal vital signs, pain scores, and sedation level. Monitor fetal heart rate and uterine activity if used during labor. Neonatal monitoring for respiratory depression and withdrawal symptoms if used chronically near term. |
| Fertility Effects | No specific human studies; animal studies suggest no significant impairment of fertility at therapeutic doses. Opioid use may affect hormone levels (e.g., prolactin) but clinical significance unclear. |