Comparative Pharmacology
Head-to-head clinical analysis: NALTREXONE HYDROCHLORIDE versus REVEX.
Peer-Reviewed Evidence
Head-to-head clinical analysis: NALTREXONE HYDROCHLORIDE versus REVEX.
NALTREXONE HYDROCHLORIDE vs REVEX
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Competitive antagonist at mu, kappa, and delta opioid receptors, with highest affinity for mu receptors. Also acts as an antagonist at the toll-like receptor 4 (TLR4).
Nalmefene is an opioid antagonist that competitively binds to mu, delta, and kappa opioid receptors, reversing or preventing opioid effects.
50 mg orally once daily for opioid dependence; 25 mg orally once daily for alcohol dependence, may increase to 50 mg after one week.
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.
None Documented
None Documented
Terminal elimination half-life: ~4 hours for naltrexone; its major active metabolite, 6-β-naltrexol, has a half-life of ~13 hours. The longer half-life of the metabolite contributes to sustained receptor blockade.
Terminal elimination half-life: 2.4-4.2 hours in adults; prolonged in renal impairment (up to 50 hours).
Renal: primarily as unchanged drug (<2%) and metabolites (mainly 6-β-naltrexol, glucuronide conjugates); approximately 60% of dose excreted in urine (including metabolites) and about 30% in feces via biliary excretion.
Renal: 60% as unchanged drug and metabolites; fecal: 40% via biliary elimination.
Category A/B
Category C
Opioid Antagonist
Opioid Antagonist