AdultPediatricDosage Forms & Strengths tablet 50mg microspheres for IM injection 380mg Opioid Dependence Prevention of relapse after opioid detoxification; to be used only after patient has been opioid-free for 7-10 days and after negative naloxone challenge (no symptom withdrawal after naloxone administration) PO: 25 mg initially, then observation for 1 hr, then 50 mg once daily starting on day 2; flexible dosing regimens can be employed to accommodate patient convenience or ensure compliance IM: 380 mg in gluteal muscle every 4 weeks for maintenance of abstinence Alcohol Dependence Treatment in patients who have been able to abstain from alcohol in outpatient settings before treatment initiation PO: 50 mg once daily for ≤12 weeks IM: 380 mg in gluteal muscle every 4 weeks for maintenance of abstinence Dosing Considerations Administer only as a deep intramuscular gluteal injection only Hepatitis (Orphan) Orphan designation for treatment of autoimmune hepatitis Sponsor TaiwanJ Pharmaceuticals Co., Ltd, Room 204 A, Bldg 53; 195 Chung Hsing Rd., Sec 4; Chutung, Hsinchu, Taiwan Postherpetic Neuralgia (Orphan) Orphan designation for treatment of postherpetic neuralgia Sponsor Allodynic Therapeutics, LLC; 1785 NE 123rd Street; North Miami, FL 33181-2537 Safety and efficacy not established Crohn Disease (Orphan) Treatment in pediatric patients Orphan indication sponsor Jill P Smith, MD, Pennsylvania State University, 500 University Drive, Hershey, PA 17033 Interaction CheckerEnter a drug name and naltrexoneNo Results No Interactions Found Interactions FoundContraindicatedSerious - Use AlternativeSignificant - Monitor CloselyMinorAll Interactions Sort By: SeverityName Contraindicated (0)Serious - Use Alternative (3)bremelanotidebremelanotide will decrease the level or effect of naltrexone by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid using bremelanotide with an orally administered naltrexone-containing product that is intended to treat alcohol and opioid addiction due to the potential for naltrexone treatment failure.naldemedinenaldemedine, naltrexone. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Potential for additive opioid receptor anatagonism and increased risk of opioid withdrawal.naloxegolnaloxegol, naltrexone. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration; potential for additive effect of opioid receptor anatagonism and increased risk of opioid withdrawal.Monitor Closely (5)acamprosatenaltrexone increases levels of acamprosate by unspecified interaction mechanism. Use Caution/Monitor. No dosage adjustment is needed.apalutamideapalutamide will decrease the level or effect of naltrexone by increasing elimination. Use Caution/Monitor. Apalutamide induces UGT and may decrease systemic exposure of drugs that are UGT substrates.dronabinolnaltrexone increases effects of dronabinol by Other (see comment). Use Caution/Monitor. Comment: Naltrexone may enhance therapeutic effects of cannabinoids. .lofexidinelofexidine will decrease the level or effect of naltrexone by unknown mechanism. Modify Therapy/Monitor Closely. Coadministration of lofexidine with oral naltrexone resulted in statistically significant differences in the steady-state pharmacokinetics of naltrexone. The efficacy of oral naltrexone may be reduced if administered within 2 hours of taking lofexidine. Interaction not expected with other naltrexone routes of administration.nabilonenaltrexone increases effects of nabilone by Other (see comment). Use Caution/Monitor. Comment: Naltrexone may enhance therapeutic effects of cannabinoids. .Minor (0)acamprosateMonitor Closely (1)naltrexone increases levels of acamprosate by unspecified interaction mechanism. Use Caution/Monitor. No dosage adjustment is needed.apalutamideMonitor Closely (1)apalutamide will decrease the level or effect of naltrexone by increasing elimination. Use Caution/Monitor. Apalutamide induces UGT and may decrease systemic exposure of drugs that are UGT substrates.bremelanotideSerious - Use Alternative (1)bremelanotide will decrease the level or effect of naltrexone by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid using bremelanotide with an orally administered naltrexone-containing product that is intended to treat alcohol and opioid addiction due to the potential for naltrexone treatment failure.dronabinolMonitor Closely (1)naltrexone increases effects of dronabinol by Other (see comment). Use Caution/Monitor. Comment: Naltrexone may enhance therapeutic effects of cannabinoids. .lofexidineMonitor Closely (1)lofexidine will decrease the level or effect of naltrexone by unknown mechanism. Modify Therapy/Monitor Closely. Coadministration of lofexidine with oral naltrexone resulted in statistically significant differences in the steady-state pharmacokinetics of naltrexone. The efficacy of oral naltrexone may be reduced if administered within 2 hours of taking lofexidine. Interaction not expected with other naltrexone routes of administration.nabiloneMonitor Closely (1)naltrexone increases effects of nabilone by Other (see comment). Use Caution/Monitor. Comment: Naltrexone may enhance therapeutic effects of cannabinoids. .naldemedineSerious - Use Alternative (1)naldemedine, naltrexone. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Potential for additive opioid receptor anatagonism and increased risk of opioid withdrawal.naloxegolSerious - Use Alternative (1)naloxegol, naltrexone. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration; potential for additive effect of opioid receptor anatagonism and increased risk of opioid withdrawal. >10% Injection site reaction (69%; includes bruising, induration, nodules, pain, pruritus, swelling, tenderness) Nausea (33%) Headache (25%) Decreased appetite (14%) Insomnia (14%) Vomiting (14%) Diarrhea (13%) Dizziness (13%) Upper respiratory tract infection (URTI) (13%) Anxiety (12%) Arthralgia (12%) Increased creatine phosphokinase (11%) Pharyngitis (11%) 1-10% Depression (8%) Muscle cramps (8%) Back pain (6%) Rash (6%) Dry mouth (5%) Somnolence (4%) Increased aspartate aminotransferase (AST) (2%) <1% Alopecia Dyspnea Edema Hepatocellular injury Increased systolic and diastolic blood pressures Liver function abnormalities Labored breathing Nonspecific electrocardiographic (ECG) changes Opiate withdrawal (mild to severe signs and symptoms, including drug craving, confusion, drowsiness, visual hallucinations, abdominal pain, vomiting, diarrhea) Palpitation Phlebitis Tachycardia Postmarketing Reports Hypersensitivity reactions, including anaphylaxis Contraindications 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 Cautions 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 Emergency treatment of opioid overdose At initial and subsequent naltrexone injections discuss with patient and caregiver the availability of naloxone for the emergency treatment of opioid overdose Inform patients and caregivers of options for obtaining naloxone as permitted by individual state naloxone dispensing and prescribing requirements or guidelines (eg, by prescription, directly from a pharmacist, or as part of a community-based program); strongly consider prescribing naloxone for emergency treatment of opioid overdose Educate patients and caregivers on how to recognize signs and symptoms of an opioid overdose and, if naloxone is prescribed, how to treat with naloxone; emphasize importance of calling 911 or getting emergency medical help in all cases of known or suspected opioid overdose, even if naloxone is administered Pregnancy 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 Untreated opioid addiction in pregnancy is associated with adverse obstetrical outcomes such as low birth weight, preterm birth, and fetal death; in addition, untreated opioid addiction often results in continued or relapsing illicit opioid use Published studies have demonstrated that alcohol is associated with fetal harm including growth restriction, facial abnormalities, central nervous system abnormalities, behavioral disorders, and impaired intellectual development Lactation The drug and metabolites, are present in human milk; there are no data on effects on breastfed infant or on milk production Developmental health benefits of breastfeeding should be considered along with mother’s clinical need for naltrexone and any potential adverse effects on breastfed infant from drug or mother’s underlying maternal conditionPregnancy Categories A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk. B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available. Mechanism of Action Opioid competitive receptor antagonist; shows highest affinity for mu receptors; congener of oxymorphone Absorption 96% absorbed from gastrointestinal tract, but because of first-pass metabolism, only 5-40% reaches systemic circulation Bioavailability: 5-40% Onset: 15-30 min Duration: 24 hr Peak plasma time: PO tablet, 1 hr; PO solution, 0.6 hr Peak plasma concentration (50-mg dose): Naltrexone, 10.6-13.7 ng/mL; 6-β-naltrexol, 109-139 ng/mL Distribution Protein bound: 21-28% Vd: 1350 L Metabolism Metabolized in liver Metabolites: 6-β-naltrexol (major), 2-hydroxy-3-methoxy-6-β-naltrexol (HMN), 2-hydroxy-3-metho-xynaltrexone, noroxymorphone, 3-methoxy-6-β-naltrexol Elimination Half-life: PO, 4 hr; 6-β-naltrexol, 13 hr; IM and 6-β-naltrexol and IM: 5-10 days Excretion: Urine (mainly) IM Administration Administer IM as gluteal injection, alternating buttocks for each subsequent injection Drug must be prepared and administered by a healthcare provider BRAND FORM. UNIT PRICE PILL IMAGE naltrexone oral- 50 mg tabletnaltrexone oral- 50 mg tabletnaltrexone oral- 50 mg tabletnaltrexone oral- 50 mg tabletnaltrexone oral- 50 mg tabletCopyright © 2010 First DataBank, Inc.Print Patient Educationnaltrexone oral NALTREXONE HCL - ORAL (nal-TREX-one hye-droe-KLOR-ide) COMMON BRAND NAME(S): Revia USES: This medication is used to prevent people who have been addicted to certain drugs (opiates) from taking them again. It is used as part of a complete treatment program for drug abuse (such as compliance monitoring, counseling, behavioral contract, lifestyle changes). This medication must not be used in people currently taking opiates, including methadone. Doing so can cause sudden withdrawal symptoms.Naltrexone belongs to a class of drugs known as opiate antagonists. It works in the brain to prevent opiate effects (such as feelings of well-being, pain relief). It also decreases the desire to take opiates.Ask your doctor or pharmacist if you should have naloxone available to treat opioid overdose. Teach your family or household members about the signs of an opioid overdose and how to treat it.This medication is also used to treat alcohol abuse. It can help people drink less alcohol or stop drinking altogether. It also decreases the desire to drink alcohol when used with a treatment program that includes counseling, support, and lifestyle changes. HOW TO USE: Take this medication by mouth with or without food, usually 50 milligrams once daily or as directed by your doctor. This medication may be given as part of a program where a health care professional will watch you take the medication. In this case, your doctor may order a higher dose (100-150 milligrams) to be taken every 2-3 days to make it easier to schedule clinic visits. Naltrexone may be taken with food or antacids if stomach upset occurs.A urine test should be done to check for recent opiate drug use. Your doctor may give you another medication (naloxone challenge test) to check for opiate use. Do not use any opiates for at least 7 days before starting naltrexone. You may need to stop certain opiate drugs (such as methadone) 10 to 14 days before starting naltrexone.Dosage is based on your medical condition and response to treatment. Your doctor may start you at a lower dose and monitor you for any side effects or withdrawal symptoms before increasing your dose. Take this medication as directed. Do