Comparative Pharmacology
Head-to-head clinical analysis: NALTREXONE versus REVIA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: NALTREXONE versus REVIA.
NALTREXONE vs REVIA
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.
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.
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.
50 mg orally once daily
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 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 renal (60% as metabolites, including 6β-naltrexol; <2% unchanged) and biliary/fecal (30%).
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
Naltrexone + Sufentanil
"The therapeutic efficacy of Sufentanil can be decreased when used in combination with Naltrexone."