Comparative Pharmacology
Head-to-head clinical analysis: REVEX versus REVIA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: REVEX versus REVIA.
REVEX vs REVIA
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Nalmefene is an opioid antagonist that competitively binds to mu, delta, and kappa opioid receptors, reversing or preventing opioid effects.
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.
0.5 mg to 1 mg intravenous, intramuscular, or subcutaneous, repeated every 2 to 5 minutes as needed, up to a maximum of 2 mg total dose per episode.
50 mg orally once daily
None Documented
None Documented
Terminal elimination half-life: 2.4-4.2 hours in adults; prolonged in renal impairment (up to 50 hours).
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.
Renal: 60% as unchanged drug and metabolites; fecal: 40% via biliary elimination.
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 C
Category C
Opioid Antagonist
Opioid Antagonist