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Percocet

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From Pharmacopedia
Oxycodone / Acetaminophen
Percocet, Endocet, Roxicet, Tylox, Primlev

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Summary
Common uses
Moderate to moderately severe acute pain0, Postoperative pain0, Cancer-related breakthrough pain (selected)0
Pharmacy
Starting dose
5 mg / 325 mg PO every 4-6 hours as needed; total acetaminophen <3 g/d
Preparations
Oxycodone/acetaminophen 2.5/325, 5/325, 7.5/325, 10/325 mg tablets; 5/325 mg/5 mL solution
US FDA Max
Acetaminophen 4 g/d absolute (3 g/d conservative); oxycodone titrated to effect
Pharmacology
Routes
Oral
Onset
10-30 minutes
Duration
4-6 hours
Half-life
Oxycodone 3-5 hours; acetaminophen 1-3 hours[2]
Bioavailability
~60-87% oxycodone (high and predictable, less CYP-genotype-dependent than codeine or hydrocodone); 85-98% acetaminophen[2]
Pregnancy
Limited use in pregnancy; chronic third-trimester opioid exposure produces neonatal opioid withdrawal syndrome and respiratory depression at delivery.[citation needed]
Legal status
Schedule II controlled substance in US. Acetaminophen content limited to ≤325 mg per dosage unit (FDA 2014)
Purported mechanism
Oxycodone is a semi-synthetic μ-opioid receptor agonist with high oral bioavailability; CYP3A4 N-demethylation and CYP2D6 O-demethylation (to oxymorphone) contribute to metabolism, but oxycodone itself is largely the analgesic, making it less CYP2D6-dependent than codeine or hydrocodone for efficacy. Acetaminophen adds central non-opioid analgesia.0 The combination is the most-prescribed opioid analgesic in the US for moderate-to-severe acute pain. CPIC PGx guidance addresses CYP2D6-driven exposure variation[1].

References

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  1. CPIC Guideline for CYP2D6, OPRM1, and COMT and Opioid Use, 2021. https://cpicpgx.org/guidelines/cpic-guideline-for-codeine-and-cyp2d6/
  2. 2.0 2.1 FDA Prescribing Information, Percocet (oxycodone HCl / acetaminophen), Endo, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/040330s015,040341s013,040434s003lbl.pdf