Comparative Pharmacology
Head-to-head clinical analysis: OXYCONTIN versus ZOHYDRO ER.
Peer-Reviewed Evidence
Head-to-head clinical analysis: OXYCONTIN versus ZOHYDRO ER.
OXYCONTIN vs ZOHYDRO ER
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Oxycodone is a full opioid agonist with relative selectivity for the mu-opioid receptor, although it can bind to other opioid receptors at higher doses. The principal therapeutic action of oxycodone is analgesia. Like all full opioid agonists, there is no ceiling effect for analgesia with oxycodone. Clinically, dosage is titrated to provide adequate analgesia and may be limited by adverse reactions, including respiratory and CNS depression.
Zohydro ER is a pure opioid agonist with relative selectivity for mu-opioid receptors, although it can interact with other opioid receptors at higher doses. Its primary therapeutic action is analgesia via binding to mu-opioid receptors in the central nervous system, leading to activation of descending inhibitory pathways and modulation of pain perception.
10 mg orally every 12 hours; titrate based on pain severity and prior opioid exposure.
Initial: 20 mg orally every 24 hours; titrate in increments of 10-20 mg every 3-7 days as needed; maximum dose 200 mg every 24 hours.
None Documented
None Documented
4.5-5.0 hours (immediate-release); controlled-release OXYCONTIN has an apparent half-life of 4.5-8.7 hours. Terminal half-life is ~3.5-4 hours for immediate-release, reflecting context-sensitive elimination.
Terminal elimination half-life is approximately 10.6 hours (range 8-17 hours) due to extended-release formulation; immediate-release hydromorphone half-life is 2-3 hours. Clinically, steady-state is achieved after 3-5 days of dosing.
Primarily renal (90% as metabolites, 10% unchanged). Also biliary/fecal (10%).
Primarily renal excretion of hydromorphone-3-glucuronide (H3G, ~60%), unchanged hydromorphone (~15%), and other conjugates. Fecal excretion accounts for ~25%.
Category C
Category C
Opioid Analgesic
Opioid Analgesic