Comparative Pharmacology
Head-to-head clinical analysis: NALOXONE HYDROCHLORIDE versus REVIA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: NALOXONE HYDROCHLORIDE versus REVIA.
NALOXONE HYDROCHLORIDE vs REVIA
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Competitive antagonist at mu, kappa, and delta opioid receptors, reversing opioid-induced respiratory depression and analgesia.
Naltrexone is a mu-opioid receptor antagonist that competitively binds to opioid receptors, blocking the effects of endogenous and exogenous opioids. It also exhibits some antagonistic activity at kappa and delta opioid receptors.
0.4 mg to 2 mg intravenous, intramuscular, or subcutaneous every 2 to 3 minutes as needed for opioid reversal; may repeat until response achieved. For continuous infusion, 0.25-6.25 mg/hour IV.
50 mg orally once daily
None Documented
None Documented
Terminal elimination half-life is 1–1.5 hours in adults; shorter in neonates (approx. 3 hours due to immature clearance). Clinically, rapid decline limits duration of antagonism.
Terminal half-life of naltrexone is approximately 4 hours; its active metabolite, 6β-naltrexol, has a half-life of about 13 hours. Clinically, the prolonged blockade of opioid receptors (up to 72 hours after a single oral dose) is attributed to the metabolite's accumulation and high receptor affinity.
Primarily hepatic metabolism (glucuronidation) with renal excretion of metabolites. ~70% as naloxone-3-glucuronide in urine, <5% unchanged. Minor fecal elimination (<10%).
Renal: primarily as unchanged drug and glucuronide conjugates; fecal: minor; approximately 60% of a dose is excreted in urine within 48 hours (with about 20% as unchanged naltrexone and the rest as metabolites, mainly 6β-naltrexol).
Category A/B
Category C
Opioid Antagonist
Opioid Antagonist