Naltrexone

DEA Class; Rx

Common Brand Names; ReVia, Vivitrol, Depade

Opiate antagonist.
Used as an aid in relapse prevention in alcohol and/or opiate dependence; has been used as part of rapid and ultrarapid detoxification techniques.
Better bioavailability and longer duration of action than naloxone; will not prevent opiate withdrawal.

Indicated for the maintenance treatment of alcohol dependence.

Patients who are on opioid analgesics, are opioid-dependent (eg, opioid agonists [methadone], opioid partial agonists [buprenorphine]), are in acute opioid withdrawal, have positive urine test for opioids, or fail to pass naloxone challenge

Hypersensitivity

Administer as a deep intramuscular gluteal injection; inadvertent subcutaneous injection may increase likelihood of severe injection site reactions; the needles provided in the carton are customized needles

Depression, suicide, and suicidality cited in postmarketing reports; causal relation not demonstrated

Vulnerability to opioid overdose: Patients should be alerted that they may be more sensitive to opioids, even at lower doses, after discontinuance of naltrexone

Opioid withdrawal precipitated abruptly by administration of opioid antagonist to opioid-dependent patient may result in withdrawal syndrome severe enough to necessitate hospitalization (see Contraindications)

Risk of hepatotoxicity with increasing doses; dose related hepatocellular injury; discontinue therapy if signs/symptoms of acute hepatitis develop

Injection may cause severe injection-site reactions (eg, cellulitis, necrosis, hematoma); may be followed by pain, tenderness, induration, swelling, erythema, bruising, or pruritus; however, in some cases injection site reactions may be very severe andmay last for several weeks following administration

Injectable microspheres are for IM use only; inadvertent SC/IV administration may increase risk of severe injection-site reactions

Cases of eosinophilic pneumonia reported; consider in patients with symptoms of progressive hypoxia and dyspnea

Use caution in patients with hepatic failure or with bleeding disorder including thrombocytopenia and hemophilia, or patients taking anticoagulant therapy; beeding hematoma may occur from IM administration

Use caution in renal impairment or hepatic impairment

Patients should be opioid free for a minimum of 7-10 days before initiating therapy; a naltrexone challenge test recommended to confirm opioid-free status

The available data from published case series with use in pregnant women are insufficient to identify a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes

The drug and metabolites, are present in human milk; there are no data on effects on breastfed infant or on milk production