pharmacopeia
GET
/api/v1/drug/naltrexone
2D structure
(4R,4aS,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy-2,4,5,6,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7-one
SMILES C1CC1CN2CC[C@]34[C@@H]5C(=O)CC[C@]3([C@H]2CC6=C4C(=C(C=C6)O)O5)O
InChIKey DQCKKXVULJGBQN-XFWGSAIBSA-N

Mechanism of action

Sourced from openFDA

Mechanism-of-action class: Opioid Antagonists.

Opioid

Indications

Sourced from openFDA
  • Naltrexone hydrochloride tablets USP 50 mg is indicated in the treatment of alcohol dependence and for the blockade of the effects of exogenously administered opioids. Naltrexone hydrochloride tablets USP 50 mg has not been shown to provide any therapeutic benefit except as part of an appropriate plan of management for the addictions.ICD-10: F10.20

Contraindications

Sourced from openFDA
  • Naltrexone hydrochloride is contraindicated in Patients receiving opioid analgesics. Patients currently dependent on opioids, including those currently maintained on opiate agonists (e.g., methadone ) or partial agonists (e.g., buprenorphine) Patients in acute opioid withdrawal (see WARNINGS ).contraindicated

Dosage & administration

Sourced from openFDA

To reduce the risk of precipitated withdrawal in patients dependent on opioids, or exacerbation of a preexisting subclinical withdrawal syndrome, opioid-dependent patients, including those being treated for alcohol dependence, should be opioid-free (including tramadol) before starting naltrexone hydrochloride treatment. An opioid-free interval of a minimum of 7 to 10 days is recommended for patients previously dependent on short-acting opioids. Switching from Buprenorphine, Buprenorphine/Naloxone, or Methadone There are no systematically collected data that specifically address the switch from buprenorphine or methadone to naltrexone hydrochloride; however, review of postmarketing case reports have indicated that some patients may experience severe manifestations of precipitated withdrawal when being switched from opioid agonist therapy to opioid antagonist therapy (see WARNINGS ).Patients transitioning from buprenorphine or methadone may be vulnerable to precipitation of withdrawal symptoms for as long as 2 weeks. Healthcare providers should be prepared to manage withdrawal symptomatically with non-opioid medications. Treatment of Alcoholism A dose of 50 mg once daily is recommended for most patients The placebo-controlled studies that demonstrated the efficacy of naltrexone hydrochloride as an adjunctive treatment of alcoholism used a dose regimen of naltrexone hydrochloride 50 mg once daily for up to 12 weeks. Other dose regimens or durations of therapy were not evaluated in these trials.

Warnings & precautions

Sourced from openFDA

Vulnerability to Opioid Overdose After opioid detoxification, patients are likely to have reduced tolerance to opioids. As the blockade of exogenous opioids provided by naltrexone hydrochloride wanes and eventually dissipates completely, patients who have been treated with naltrexone hydrochloride may respond to lower doses of opioids than previously used, just as they would shortly after completing detoxification. This could result in potentially life-threatening opioid intoxication (respiratory compromise or arrest, circulatory collapse, etc.) if the patient uses previously tolerated doses of opioids. Cases of opioid overdose with fatal outcomes have been reported in patients after discontinuing treatment. Patients should be alerted that they may be more sensitive to opioids, even at lower doses, after naltrexone hydrochloride treatment is discontinued. It is important that patients inform family members, and the people closest to the patient of this increased sensitivity to opioids and the risk of overdose. (see PRECAUTIONS, Information for Patients ). There is also the possibility that a patient who is treated with naltrexone hydrochloride could overcome the opioid blockade effect of naltrexone hydrochloride. Although naltrexone hydrochloride is a potent antagonist , the blockade produced by naltrexone hydrochloride is surmountable. The plasma concentration of exogenous opioids attained immediately following their acute administration may be sufficient to overcome the competitive receptor blockade.

Adverse reactions

Sourced from openFDA

During two randomized, double-blind placebo-controlled 12 week trials to evaluate the efficacy of naltrexone hydrochloride as an adjunctive treatment of alcohol dependence, most patients tolerated naltrexone hydrochloride well. In these studies, a total of 93 patients received naltrexone hydrochloride at a dose of 50 mg once daily. Five of these patients discontinued naltrexone hydrochloride because of nausea. No serious adverse events were reported during these two trials. While extensive clinical studies evaluating the use of naltrexone hydrochloride in detoxified, formerly opioid-dependent individuals failed to identify any single, serious untoward risk of naltrexone hydrochloride use, placebo-controlled studies employing up to five-fold higher doses of naltrexone hydrochloride (up to 300 mg per day) than that recommended for use in opiate receptor blockade have shown that naltrexone hydrochloride causes hepatocellular injury in a substantial proportion of patients exposed at higher doses (see WARNINGS and PRECAUTIONS: Laboratory Tests ). Aside from this finding, and the risk of precipitated opioid withdrawal, available evidence does not incriminate naltrexone hydrochloride, used at any dose, as a cause of any other serious adverse reaction for the patient who is“opioid free.” It is critical to recognize that naltrexone hydrochloride can precipitate or exacerbate abstinence signs and symptoms in any individual who is not completely free of exogenous opioids.

Use in specific populations

Sourced from openFDA

Pregnancy:Teratogenic Effects Pregnancy Category C:- Naltrexone has been shown to increase the incidence of early fetal loss when given to rats at doses ≥ 30 mg/kg/day (180 mg/m 2 /day; 5 times the recommended therapeutic dose, based on body surface area) and to rabbits at oral doses ≥ 60 mg/kg/day (720 mg/m 2 /day; 18 times the recommended therapeutic dose, based on body surface area). There was no evidence of teratogenicity when naltrexone was administered orally to rats and rabbits during the period of major organogenesis at doses up to 200 mg/kg/day (32 and 65 times the recommended therapeutic dose, respectively, based on body surface area). Rats do not form appreciable quantities of the major human metabolite, 6-β-naltrexol; therefore, the potential reproductive toxicity of the metabolite in rats is not known. There are no adequate and well-controlled studies in pregnant women. Naltrexone hydrochloride should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Overdosage

Sourced from openFDA

There is limited clinical experience with naltrexone hydrochloride overdosage in humans. In one study, subjects who received 800 mg daily naltrexone hydrochloride for up to one week showed no evidence of toxicity. In the mouse, rat and guinea pig, the oral LD 50s were 1,100 to 1,550 mg/kg; 1,450 mg/kg; and 1,490 mg/kg; respectively. High doses of naltrexone hydrochloride (generally ≥ 1,000 mg/kg) produced salivation, depression/reduced activity, tremors, and convulsions. Mortalities in animals due to high-dose naltrexone hydrochloride administration usually were due to clonic-tonic convulsions and/or respiratory failure. Treatment of Overdosage In view of the lack of actual experience in the treatment of naltrexone hydrochloride overdose, patients should be treated symptomatically in a closely supervised environment. Physicians should contact a poison control center for the most up-to-date information.

Approval history

Sourced from openFDA
  • May 26, 1999ANDAANDA075274Elite Labs
  • Mar 22, 2002ANDAANDA076264Specgx Llc
  • Apr 13, 2006NDANDA021897Alkermes
  • Aug 17, 2011ANDAANDA091205Accord Hlthcare
  • Feb 24, 2012ANDAANDA090356Sun Pharm
  • Sep 10, 2014NDANDA200063Nalpropion
  • Jul 21, 2017ANDAANDA207905Chartwell

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
39,969 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Injection Site Reaction4,41611%
  2. 2Nausea4,17410%
  3. 3Injection Site Pain3,1577.9%
  4. 4Headache2,6616.7%
  5. 5Fatigue2,4556.1%
  6. 6Dizziness2,0945.2%
  7. 7Drug Ineffective2,0295.1%
  8. 8Feeling Abnormal2,0195.1%
  9. 9Alcoholism1,9554.9%
  10. 10Injection Site Mass1,9154.8%
  11. 11Pain1,8414.6%
  12. 12Vomiting1,7214.3%
  13. 13Insomnia1,6474.1%
  14. 14Malaise1,5974.0%
  15. 15Off Label Use1,5974.0%

Literature

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Recent PubMed references pinned to Naltrexone as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 533 ClinicalTrials.gov registrations naming Naltrexone as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Pharmacogenomics

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CPIC-curated drug–gene pairs for Naltrexone. Levels describe the strength of curated evidence and guideline status — never a recommendation to test or to adjust therapy.

Structural analogs

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Ranked by 2D fingerprint (Tanimoto) similarity over PubChem structures. Structural proximity only — not a claim of therapeutic equivalence.

Frequently asked questions

How does Naltrexone work?
Mechanism-of-action class: Opioid Antagonists.
What is Naltrexone used for?
According to FDA labeling, Naltrexone carries indications including: Naltrexone hydrochloride tablets USP 50 mg is indicated in the treatment of alcohol dependence and for the blockade of the effects of exogenously administered opioids. Naltrexone hydrochloride tablets USP 50 mg has not been shown to provide any therapeutic benefit except as part of an appropriate plan of management for the addictions.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Naltrexone?
Naltrexone is classified as Drugs used in alcohol dependence, Opioid Antagonist, Opioid Antagonists, Central Nervous System Stimulation, Pupillary Constriction.
What are the brand names for Naltrexone?
Naltrexone is marketed under brand names including Contrave, ReVia, Vivitrol.
What are the contraindications for Naltrexone?
Naltrexone labeling lists contraindications including: Naltrexone hydrochloride is contraindicated in Patients receiving opioid analgesics. Patients currently dependent on opioids, including those currently maintained on opiate agonists (e.g., methadone ) or partial agonists (e.g., buprenorphine) Patients in acute opioid withdrawal (see WARNINGS ).. Always consult the full prescribing information and a clinician.
Note. Data for naltrexone is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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