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Naltrexone

ReVia

Opioid AntagonistGeneric availableTDM data

DESCRIPTION Naltrexone hydrochloride, an opioid antagonist, are a synthetic congener of oxymorphone with no opioid agonist properties. Naltrexone differs in structure from oxymorphone in that the methyl group on the nitrogen atom is replaced by a cyclopropylmethyl group. Naltrexone hydrochloride is also related to the potent opioid antagonist, naloxone, or n-allylnoroxymorphone. The chemical name for naltrexone hydrochloride is Morphinan-6-one, 17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxy-, hydrochloride, (5a)-. The structural formula is as follows: C 20 H 23 NO 4 ∙HCl Molecular Weight: 377.86 Naltrexone hydrochloride is a white, crystalline compound. The hydrochloride salt is soluble in water to the extent of about 100 mg/mL. Naltrexone Hydrochloride Tablets USP are available in scored film-coated tablets containing 50 mg of naltrexone hydrochloride. Naltrexone Hydrochloride Tablets USP also contain: carnauba wax powder, colloidal silicon dioxide, croscarmellose sodium, hypromellose, hydroxypropyl cellulose, lactose anhydrous, magnesium stearate, microcrystalline cellulose, polyethylene glycol, titanium dioxide and yellow iron oxide.

Compare Naltrexone

FDA-Approved Indications

  • Alcohol dependence (adults)
  • Opioid use disorder — opioid blockade after detoxification (adults)

Common Off-Label Uses

  • Opioid use disorder
  • Self-injurious behavior
  • Impulse control disorders

What Sets This Drug Apart

  • Opioid antagonist (mu/delta/kappa) FDA-approved for both alcohol use disorder AND opioid use disorder — dual indication is distinctive
  • Available as oral 50 mg daily or extended-release IM injection 380 mg monthly (Vivitrol) — monthly injection eliminates daily adherence burden
  • For opioid use disorder: patients MUST be fully detoxified (7-10 days opioid-free) before starting, or precipitated withdrawal occurs
  • Boxed warning for hepatotoxicity at doses above 50 mg/day; baseline and periodic LFTs essential
  • Blocks opioid analgesia — medical alert bracelet recommended; pre-surgical planning required; naltrexone must be discontinued before opioid-based anesthesia