VICOPROFEN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for VICOPROFEN (VICOPROFEN).
Hydrocodone is a mu-opioid receptor agonist that activates G-protein coupled opioid receptors, leading to analgesia; ibuprofen is a nonsteroidal anti-inflammatory drug (NSAID) that inhibits cyclooxygenase (COX-1 and COX-2), reducing prostaglandin synthesis.
| Metabolism | Hydrocodone is metabolized via CYP3A4 and CYP2D6; ibuprofen is primarily metabolized by CYP2C9. |
| Excretion | Hydrocodone: primarily renal (26% as unchanged drug and metabolites, including norhydrocodone, hydromorphone, and conjugates); less than 5% fecal. Ibuprofen: renal (50-60% as unchanged drug and metabolites, mainly conjugated with glucuronic acid; <10% unchanged); biliary/fecal (minor). |
| Half-life | Hydrocodone: 3.8-4.5 hours (immediate-release); clinical context: analgesic duration correlates with half-life, but may be prolonged in renal/hepatic impairment. Ibuprofen: 2-4 hours (immediate-release); clinical context: anti-inflammatory effect may outlast plasma half-life due to tissue distribution. |
| Protein binding | Hydrocodone: approximately 20-30% bound to plasma proteins (albumin). Ibuprofen: >99% bound to albumin. |
| Volume of Distribution | Hydrocodone: 3.3 L/kg (large Vd indicates extensive tissue distribution). Ibuprofen: 0.1-0.3 L/kg (low Vd reflects high protein binding and limited extravascular distribution). |
| Bioavailability | Oral: hydrocodone bioavailability 60-80% (due to first-pass metabolism); ibuprofen bioavailability 80-100% (rapid absorption). |
| Onset of Action | Oral: hydrocodone component analgesic onset within 20-30 minutes; ibuprofen component analgesic/anti-inflammatory onset within 30-60 minutes. |
| Duration of Action | Hydrocodone: analgesic effect lasts 4-6 hours. Ibuprofen: analgesic/anti-inflammatory effect lasts 4-6 hours. Clinical note: combination product VICOPROFEN is dosed every 4-6 hours as needed; hepatic or renal impairment may prolong effects. |
| Molecular Weight | Ibuprofen: 206.28 Da; Hydrocodone: 299.36 Da |
1 tablet (hydrocodone 5 mg / ibuprofen 200 mg) orally every 4 to 6 hours as needed for pain; maximum 5 tablets per day.
| Dosage form | TABLET |
| Renal impairment | Avoid use if CrCl <30 mL/min; for CrCl 30-59 mL/min, reduce dose frequency and avoid prolonged use due to ibuprofen component. |
| Liver impairment | Contraindicated in severe hepatic impairment (Child-Pugh class C); for moderate impairment (Child-Pugh class B), use with caution and consider dose reduction. |
| Pediatric use | Not recommended for use in pediatric patients (safety and efficacy not established). |
| Geriatric use | Use lowest effective dose for shortest duration; increased risk of GI bleeding and renal impairment; monitor renal function and avoid prolonged use. |
| 1st trimester | Avoid use, especially during organogenesis. NSAIDs are associated with increased risk of spontaneous abortion and cardiac malformations. |
| 2nd trimester | Use with caution; may cause oligohydramnios and premature closure of ductus arteriosus. Avoid if possible. |
| 3rd trimester | Contraindicated due to risk of premature closure of ductus arteriosus, oligohydramnios, and neonatal renal impairment. |
Clinical note
Comprehensive clinical and safety monograph for VICOPROFEN (VICOPROFEN).
| Placental transfer | Both ibuprofen and hydrocodone cross the placenta. Ibuprofen transfer is minimal; hydrocodone transfer is significant. |
| Breastfeeding | Ibuprofen and hydrocodone are excreted into breast milk in small amounts. Ibuprofen is considered compatible with breastfeeding; hydrocodone may cause infant sedation. Monitor infant for drowsiness and respiratory depression. Use lowest effective dose for shortest duration. |
■ FDA Black Box Warning
Risk of addiction, abuse, and misuse; life-threatening respiratory depression; accidental ingestion (especially in children) can be fatal; neonatal opioid withdrawal syndrome with prolonged use during pregnancy; risks from concomitant use with benzodiazepines or other CNS depressants (additive effects); hepatotoxicity from ibuprofen (NSAID).
| Serious Effects |
Known hypersensitivity to ibuprofen, hydrocodone, or any componentSignificant respiratory depressionAcute or severe bronchial asthma in an unmonitored settingGastrointestinal obstruction (e.g., paralytic ileus)Post-operative pain management in children after tonsillectomy/adenoidectomyIn the setting of coronary artery bypass graft (CABG) surgeryThird trimester of pregnancy
| Precautions | Addiction, abuse, and misuse; life-threatening respiratory depression; accidental ingestion; neonatal opioid withdrawal syndrome; risks with benzodiazepines or other CNS depressants; hepatotoxicity; cardiovascular thrombotic events; gastrointestinal bleeding; renal toxicity; hypertension; anaphylactoid reactions; serious skin reactions; use in patients with renal or hepatic impairment; pregnancy; lactation. |
| Food/Dietary |
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| Lactation Rating | L2 (Safer) |
| Teratogenic Risk | First trimester: NSAIDs associated with increased risk of miscarriage and cardiac defects. Second trimester: Potential for oligohydramnios and fetal renal dysfunction. Third trimester: Risk of premature closure of ductus arteriosus, oligohydramnios, and neonatal renal impairment. |
| Fetal Monitoring | Monitor fetal ultrasound for oligohydramnios and ductus arteriosus patency if used in second/third trimester. Assess maternal renal function, blood pressure, and signs of gastrointestinal bleeding. In neonates, monitor for respiratory depression and withdrawal symptoms. |
| Fertility Effects | NSAIDs may impair female fertility by inhibiting prostaglandin synthesis, potentially interfering with ovulation and implantation. Reversible upon discontinuation. Hydrocodone may cause hormonal disturbances with chronic use. |
| Avoid alcohol while taking Vicoprofen. Take with food or milk to reduce GI upset. Grapefruit juice may increase hydrocodone levels; avoid consuming large amounts. There are no other significant food interactions. |
| Clinical Pearls | Vicoprofen is a fixed-dose combination of hydrocodone bitartrate (an opioid agonist) and ibuprofen (an NSAID). It is indicated for short-term (generally <10 days) management of acute pain severe enough to require an opioid and for which alternative treatments are inadequate. The maximum daily dose is 5 tablets of 7.5 mg hydrocodone/200 mg ibuprofen, not to exceed 5 days due to ibuprofen-associated GI and renal risks. Monitor for respiratory depression, especially in opioid-naïve patients, and assess for signs of NSAID-related bleeding, renal impairment, or cardiovascular events. Abrupt discontinuation may precipitate withdrawal symptoms. Avoid co-prescription with other CNS depressants or NSAIDs. |
| Patient Advice | Take exactly as prescribed; do not increase dose or frequency without consulting your doctor. · Do not take with other products containing acetaminophen, NSAIDs (e.g., ibuprofen, naproxen), or opioids. · Avoid alcohol while taking this medication as it increases risk of liver damage, stomach bleeding, and respiratory depression. · May cause drowsiness or dizziness; do not drive or operate machinery until you know how this medication affects you. · Seek emergency medical attention if you experience difficulty breathing, chest pain, severe drowsiness, or signs of allergic reaction. · If you miss a dose, take it as soon as you remember. If it is near time for the next dose, skip the missed dose. Do not double the dose. · Do not stop taking abruptly without talking to your doctor; a gradual dose reduction may be needed to avoid withdrawal symptoms. · Store at room temperature away from moisture and heat. Keep out of reach of children. · Report any new or worsening pain, signs of stomach bleeding (vomit that looks like coffee grounds, black/tarry stools), or symptoms of kidney problems (e.g., change in urine output, swelling in legs/ankles). · This medication may cause constipation; increase fluid and fiber intake, and consider a stool softener if needed. |