Comparative Pharmacology
Head-to-head clinical analysis: NALOXONE versus REVIA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: NALOXONE versus REVIA.
NALOXONE 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 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.
0.4-2 mg IV/IM/SC, may repeat every 2-3 minutes; if no response after 10 mg, reconsider diagnosis.
50 mg orally once daily
None Documented
None Documented
60-90 minutes in adults; shorter in neonates (3 hours); prolonged in hepatic impairment (up to 2-3 hours).
Clinical Note
moderateNaloxone + Teriflunomide
"The metabolism of Teriflunomide can be decreased when combined with Naloxone."
Clinical Note
moderateNaloxone + Sulfisoxazole
"The metabolism of Sulfisoxazole can be decreased when combined with Naloxone."
Clinical Note
moderateNaloxone + Erythromycin
"The metabolism of Erythromycin can be decreased when combined with Naloxone."
Clinical Note
moderateNaloxone + Cyclosporine
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: ~70% as metabolites (naloxone-3-glucuronide, naloxone-3-sulfate) and <2% unchanged; biliary/fecal: ~25% primarily as conjugated metabolites.
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
"The metabolism of Cyclosporine can be decreased when combined with Naloxone."