Comparative Pharmacology
Head-to-head clinical analysis: NALTREXONE versus REVEX.
Peer-Reviewed Evidence
Head-to-head clinical analysis: NALTREXONE versus REVEX.
NALTREXONE vs REVEX
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Naltrexone is a pure opioid antagonist that competitively binds to μ-opioid receptors, blocking the effects of endogenous and exogenous opioids. It also antagonizes κ- and δ-opioid receptors to a lesser extent.
Nalmefene is an opioid antagonist that competitively binds to mu, delta, and kappa opioid receptors, reversing or preventing opioid effects.
Oral: 50 mg once daily for opioid dependence; 25 mg initially for first dose to minimize adverse effects. Intramuscular: 380 mg every 4 weeks for alcohol dependence.
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
Clinical Note
moderateMethylnaltrexone + Fesoterodine
"The serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Methylnaltrexone."
Clinical Note
moderateNaltrexone + Methadone
"The therapeutic efficacy of Methadone can be decreased when used in combination with Naltrexone."
Clinical Note
moderateNaltrexone + Dabigatran etexilate
"The serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Naltrexone."
Clinical Note
moderateNaltrexone: 3.9–10.3 hours; active metabolite 6β-naltrexol: 12.9 hours. Context: Trough levels of 6β-naltrexol sustain receptor blockade for 24–48 h.
Terminal elimination half-life: 2.4-4.2 hours in adults; prolonged in renal impairment (up to 50 hours).
Primarily renal (60% as metabolites, including 6β-naltrexol; <2% unchanged) and biliary/fecal (30%).
Renal: 60% as unchanged drug and metabolites; fecal: 40% via biliary elimination.
Category A/B
Category C
Opioid Antagonist
Opioid Antagonist
Naltrexone + Sufentanil
"The therapeutic efficacy of Sufentanil can be decreased when used in combination with Naltrexone."