Comparative Pharmacology
Head-to-head clinical analysis: NALOXONE versus VIVITROL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: NALOXONE versus VIVITROL.
NALOXONE vs VIVITROL
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, as the active moiety of VIVITROL, is a competitive antagonist at opioid receptors (mu, kappa, and delta), blocking the euphoric effects of alcohol and opioids. It also modulates the hypothalamic-pituitary-adrenal axis and dopamine pathways implicated in alcohol craving.
0.4-2 mg IV/IM/SC, may repeat every 2-3 minutes; if no response after 10 mg, reconsider diagnosis.
380 mg intramuscularly every 4 weeks, alternating gluteal injections.
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
Naltrexone terminal half-life: 4-13 hours (mean 9.7 h). Active metabolite 6-β-naltrexol: 10-15 hours. Clinically, naltrexone concentrations are sustained for ~30 days after IM injection.
Renal: ~70% as metabolites (naloxone-3-glucuronide, naloxone-3-sulfate) and <2% unchanged; biliary/fecal: ~25% primarily as conjugated metabolites.
Naltrexol (6-β-naltrexol) and naltrexone: primarily renal (60-70% as metabolites, <5% as unchanged drug); biliary/fecal (minor route, <10%).
Category A/B
Category C
Opioid Antagonist
Opioid Antagonist
"The metabolism of Cyclosporine can be decreased when combined with Naloxone."