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Drug overview for NALTREX (naltrexone hcl):
Generic name: naltrexone HCl
Drug class: Opioid Antagonists
Therapeutic class: Analgesic, Anti-inflammatory or Antipyretic
Naltrexone is an opioid antagonist.
No enhanced Uses information available for this drug.
Generic name: naltrexone HCl
Drug class: Opioid Antagonists
Therapeutic class: Analgesic, Anti-inflammatory or Antipyretic
Naltrexone is an opioid antagonist.
No enhanced Uses information available for this drug.
DRUG IMAGES
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The following indications for NALTREX (naltrexone hcl) have been approved by the FDA:
Indications:
None.
Professional Synonyms:
None.
Indications:
None.
Professional Synonyms:
None.
The following dosing information is available for NALTREX (naltrexone hcl):
Dosage of oral naltrexone is expressed in terms of the hydrochloride salt; dosage of the extended-release IM injection is expressed in terms of naltrexone. The following dosage recommendations are usual dosages recommended by the manufacturer; alternative flexible dosing schedules in which the dose and/or frequency of administration of the drug are altered in an attempt to improve compliance have also been suggested.
After opioid detoxification, patients are likely to have reduced tolerance to opioids. As the blockade of exogenous opioids produced by naltrexone decreases and eventually dissipates completely, patients who have been treated with naltrexone may respond to lower doses of opioids than previously used. This could result in potentially life-threatening opioid overdose (e.g., respiratory compromise or arrest, circulatory collapse) if the patient uses previously tolerated doses of opioids.
Cases of overdosage with fatal outcomes have been reported after patients discontinued treatment with naltrexone.
The possibility also exists that patients who are treated with naltrexone could overcome the potent opioid blockade effect of naltrexone; the plasma concentration of exogenous opioids attained immediately following their acute administration may be sufficient to overcome the competitive receptor blockade. This poses a potential risk to individuals who attempt, on their own, to overcome the blockade by administering large amounts of exogenous opioids. Any attempts by a patient to overcome the antagonistic activity of naltrexone is especially dangerous and may lead to life-threatening opioid intoxication or fatal overdose.
Inform patients that they may be more sensitive to opioids, even at lower doses, after naltrexone 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. Also inform patients of the serious consequences of trying to overcome the opioid blockade.
Because of the risks for opioid overdose, discuss with the patient and caregiver the importance of having access to naloxone for the emergency treatment of opioid overdose. Educate patients and caregivers on how to recognize the signs and symptoms of an opioid overdose and how to treat with naloxone. Emphasize the importance of calling 911 or seeking emergency medical help in all cases of known or suspected opioid overdose, even if naloxone is administered.
After opioid detoxification, patients are likely to have reduced tolerance to opioids. As the blockade of exogenous opioids produced by naltrexone decreases and eventually dissipates completely, patients who have been treated with naltrexone may respond to lower doses of opioids than previously used. This could result in potentially life-threatening opioid overdose (e.g., respiratory compromise or arrest, circulatory collapse) if the patient uses previously tolerated doses of opioids.
Cases of overdosage with fatal outcomes have been reported after patients discontinued treatment with naltrexone.
The possibility also exists that patients who are treated with naltrexone could overcome the potent opioid blockade effect of naltrexone; the plasma concentration of exogenous opioids attained immediately following their acute administration may be sufficient to overcome the competitive receptor blockade. This poses a potential risk to individuals who attempt, on their own, to overcome the blockade by administering large amounts of exogenous opioids. Any attempts by a patient to overcome the antagonistic activity of naltrexone is especially dangerous and may lead to life-threatening opioid intoxication or fatal overdose.
Inform patients that they may be more sensitive to opioids, even at lower doses, after naltrexone 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. Also inform patients of the serious consequences of trying to overcome the opioid blockade.
Because of the risks for opioid overdose, discuss with the patient and caregiver the importance of having access to naloxone for the emergency treatment of opioid overdose. Educate patients and caregivers on how to recognize the signs and symptoms of an opioid overdose and how to treat with naloxone. Emphasize the importance of calling 911 or seeking emergency medical help in all cases of known or suspected opioid overdose, even if naloxone is administered.
Administer naltrexone orally or by IM injection. Do not administer the parenteral preparation by IV or subcutaneous injection. Therapy may be initiated with the parenteral preparation; it is not necessary to initiate therapy with oral naltrexone and then switch to parenteral preparation.
No dosing information available.
No generic dosing information available.
The following drug interaction information is available for NALTREX (naltrexone hcl):
There are 1 contraindications.
These drug combinations generally should not be dispensed or administered to the same patient. A manufacturer label warning that indicates the contraindication warrants inclusion of a drug combination in this category, regardless of clinical evidence or lack of clinical evidence to support the contraindication.
| Drug Interaction | Drug Names |
|---|---|
| Opioid Antagonists/Opioid Analgesics SEVERITY LEVEL: 1-Contraindicated Drug Combination: This drug combination is contraindicated and generally should not be dispensed or administered to the same patient. MECHANISM OF ACTION: Naltrexone, nalmefene, and samidorphan are opioid antagonists and thus inhibit the effects of opioid analgesics.(1-3) CLINICAL EFFECTS: Concurrent administration or the administration of naltrexone within 7-10 days of opioids may induce acute abstinence syndrome or exacerbate a pre-existing subclinical abstinence syndrome.(1,4) Patients taking naltrexone may not experience beneficial effects of opioid-containing medications.(4) Samidorphan can precipitate opioid withdrawal in patients who are dependent on opioids. In patients who use opioids, delay initiation of samidorphan for a minimum of 7 days after last use of short-acting opioids and 14 days after last use of long-acting opioids.(3) Concurrent use of nalmefene tablets with opioid agonists may prevent the beneficial effects of the opioid.(2) PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: The manufacturer of naltrexone states that the administration of naltrexone concurrently with opioids or to patients dependent on opioids is contraindicated.(1,4) Patients previously dependent on short-acting opioids should be opioid-free for a minimum of seven to ten days before beginning naltrexone therapy. Patients previously on buprenorphine or methadone may be vulnerable to withdrawal symptoms for as long as 2 weeks.(1,4) The manufacturer of naltrexone states that the naloxone challenge test, described in the naltrexone prescribing information, can be administered to determine if patients are opioid free.(1) The manufacturer of samidorphan states the concurrent use of samidorphan in patients using opioids or undergoing acute opioid withdrawal is contraindicated. Prior to initiating samidorphan, there should be at least a 7-day opioid free interval from the last use of short-acting opioids, and at least a 14-day opioid free interval from the last use of long-acting opioids.(3) The UK manufacturer of nalmefene tablets (for reduction of alcohol consumption) states the concurrent use of opioid analgesics is contraindicated.(2) Suspend the use of nalmefene tablets for 7 days prior to the anticipated use of opioids (e.g., elective surgery).(2) DISCUSSION: A double-blind, randomized, placebo-control study evaluated pain relief and side effects of 35 opioid-naive patients undergoing cesarean section. All patients received spinal anesthesia (bupivacaine and morphine) and were randomized to also receive placebo, naltrexone 3 mg, or naltrexone 6 mg. Patients treated with naltrexone experienced shorter duration of pain relief (not statistically significant), however incidence of opioid-induced side effects was reduced. Patients in the naltrexone 6 mg group had lower rates of pruritus, vomiting, and somnolence (all statistically significant) compared to the placebo group.(5) In a double-blind, randomized, placebo-control trial ten recreational opioid users were studied to determine the effects of hydromorphone (4 mg and 16 mg), tramadol (87.5 mg, 175 mg, and 350 mg), and placebo after pretreatment with naltrexone (50 mg) or placebo. Results show that lower doses of hydromorphone and tramadol acted similar to placebo. Hydromorphone 16 mg alone caused euphoria and miosis which were blocked by naltrexone. Tramadol 350 mg produced a lower magnitude of euphoria and miosis compared to hydromorphone. Naltrexone partially diminished the euphoria caused by tramadol, while it enhanced some of the unpleasant monoaminergic effects (flushing, malaise, vomiting).(6) A case report describes a 28 year-old ex-heroin addict who was stable on methadone 100 mg daily and simultaneously stopped using heroin and began drinking alcohol. He was admitted to the hospital for alcohol detoxification and, by mistake, was given naltrexone 100 mg instead of methadone 100 mg. The patient experienced withdrawal symptoms including chills, agitation, muscle and abdominal pain, generalized piloerection, and dilated pupils. Treatment of withdrawal was titrated to treat symptoms and required administration 78 mg of parenteral hydromorphone, after which the patient experienced relief for the following six hours.(8) Intentional administration of an opioid antagonist, naloxone, with opioid analgesics has been performed with close monitoring to lower required opioid dose by inducing withdrawal. Three case reports describe patients who had improved pain relief on significantly reduced doses of opioid analgesics.(8) In a double-blind controlled trial, 267 trauma patients were randomized to receive 0.05 mg/kg intravenous morphine either alone or in combination with 5 mg naltrexone oral suspension. Evaluated endpoints include reduction of pain and incidence of side effects. Results indicate that ultra-low dose naltrexone does not alter opioid requirements for pain control, but does lower incidence of nausea [2 (1.16%) vs 16 (11.6%), p<0.001].(9) |
ACETAMIN-CAFF-DIHYDROCODEINE, ACETAMINOPHEN-CODEINE, APADAZ, ASA-BUTALB-CAFFEINE-CODEINE, ASCOMP WITH CODEINE, BELBUCA, BELLADONNA-OPIUM, BENZHYDROCODONE-ACETAMINOPHEN, BRIXADI, BUPRENORPHINE, BUPRENORPHINE HCL, BUPRENORPHINE-NALOXONE, BUTALB-ACETAMINOPH-CAFF-CODEIN, BUTORPHANOL TARTRATE, BUTRANS, CARISOPRODOL-ASPIRIN-CODEINE, CODEINE PHOSPHATE, CODEINE SULFATE, CONZIP, DEMEROL, DIHYDROCODEINE BITARTRATE, DILAUDID, DIPHENOXYLATE-ATROPINE, DISKETS, DSUVIA, DURAMORPH, ENDOCET, FENTANYL, FENTANYL CITRATE, FENTANYL CITRATE-0.9% NACL, FENTANYL CITRATE-D5W, FENTANYL CITRATE-STERILE WATER, FENTANYL CITRATE-WATER, FENTANYL-BUPIVACAINE-0.9% NACL, FENTANYL-BUPIVACAINE-NACL, FENTANYL-ROPIVACAINE-0.9% NACL, FENTANYL-ROPIVACAINE-NACL, FIORICET WITH CODEINE, HYCODAN, HYDROCODONE BITARTRATE, HYDROCODONE BITARTRATE ER, HYDROCODONE-ACETAMINOPHEN, HYDROCODONE-CHLORPHENIRAMNE ER, HYDROCODONE-HOMATROPINE MBR, HYDROCODONE-IBUPROFEN, HYDROMET, HYDROMORPHONE ER, HYDROMORPHONE HCL, HYDROMORPHONE HCL-0.9% NACL, HYDROMORPHONE HCL-D5W, HYDROMORPHONE HCL-NACL, HYDROMORPHONE HCL-WATER, HYSINGLA ER, INFUMORPH, LEVORPHANOL TARTRATE, LOMOTIL, MEPERIDINE HCL, MEPERIDINE HCL-0.9% NACL, METHADONE HCL, METHADONE HCL-0.9% NACL, METHADONE HCL-NACL, METHADONE INTENSOL, METHADOSE, MITIGO, MORPHINE SULFATE, MORPHINE SULFATE ER, MORPHINE SULFATE-0.9% NACL, MORPHINE SULFATE-NACL, MOTOFEN, MS CONTIN, NALBUPHINE HCL, NALOCET, NUCYNTA, NUCYNTA ER, OLINVYK, OPIUM TINCTURE, OXYCODONE HCL, OXYCODONE HCL ER, OXYCODONE HYDROCHLORIDE, OXYCODONE-ACETAMINOPHEN, OXYCONTIN, OXYMORPHONE HCL, OXYMORPHONE HCL ER, PENTAZOCINE-NALOXONE HCL, PERCOCET, PRIMLEV, PROLATE, PROMETHAZINE-CODEINE, QDOLO, REMIFENTANIL HCL, ROXICODONE, ROXYBOND, SUBLOCADE, SUBOXONE, SUFENTANIL CITRATE, TRAMADOL HCL, TRAMADOL HCL ER, TRAMADOL HCL-ACETAMINOPHEN, TREZIX, TUXARIN ER, ULTIVA, XTAMPZA ER, ZUBSOLV |
There are 0 severe interactions.
There are 0 moderate interactions.
The following contraindication information is available for NALTREX (naltrexone hcl):
Drug contraindication overview.
*Patients receiving opioid analgesics. *Patients with current physiologic opioid dependence, including those currently maintained on opiate agonists (e.g., methadone) or partial agonists (e.g., buprenorphine). *Patients in acute opioid withdrawal.
*Patients who have failed the naloxone challenge test or who have a positive urine screen for opioids. *Patients with known hypersensitivity to naltrexone or any components of the products. I
*Patients receiving opioid analgesics. *Patients with current physiologic opioid dependence, including those currently maintained on opiate agonists (e.g., methadone) or partial agonists (e.g., buprenorphine). *Patients in acute opioid withdrawal.
*Patients who have failed the naloxone challenge test or who have a positive urine screen for opioids. *Patients with known hypersensitivity to naltrexone or any components of the products. I
There are 3 contraindications.
Absolute contraindication.
| Contraindication List |
|---|
| Acute hepatic failure |
| Opioid use last 4 hours in narcotic-dependent patient |
| Opioid withdrawal symptoms |
There are 4 severe contraindications.
Adequate patient monitoring is recommended for safer drug use.
| Severe List |
|---|
| Acute hepatitis |
| Depression |
| Eosinophilic pneumonia |
| Suicidal ideation |
There are 0 moderate contraindications.
The following adverse reaction information is available for NALTREX (naltrexone hcl):
Adverse reaction overview.
The most common adverse effects in patients with opioid use disorder receiving naltrexone extended-release injectable suspension (incidence >=2% and at least twice as frequent as with placebo) include hepatic enzyme abnormalities, injection site pain, nasopharyngitis, insomnia, and toothache. The most common adverse effects in patients with opioid use disorder receiving naltrexone oral tablets (incidence >=10%) include difficulty sleeping, anxiety, nervousness, abdominal pain/cramps, nausea and/or vomiting, low energy, joint and muscle pain, and headache. The most common adverse effects in patients with alcohol use disorder receiving naltrexone extended-release injectable suspension (incidence >=5% and at least twice as frequent as with placebo) include nausea, vomiting, injection site reactions (including induration, pruritus, nodules and swelling), muscle cramps, dizziness or syncope, somnolence or sedation, anorexia, and decreased appetite or other appetite disorders. The most common adverse effects in patients with alcohol use disorder receiving naltrexone oral tablets (incidence >=2%) include depression, nausea, headache, dizziness, nervousness, fatigue, insomnia, vomiting, anxiety, and somnolence.
The most common adverse effects in patients with opioid use disorder receiving naltrexone extended-release injectable suspension (incidence >=2% and at least twice as frequent as with placebo) include hepatic enzyme abnormalities, injection site pain, nasopharyngitis, insomnia, and toothache. The most common adverse effects in patients with opioid use disorder receiving naltrexone oral tablets (incidence >=10%) include difficulty sleeping, anxiety, nervousness, abdominal pain/cramps, nausea and/or vomiting, low energy, joint and muscle pain, and headache. The most common adverse effects in patients with alcohol use disorder receiving naltrexone extended-release injectable suspension (incidence >=5% and at least twice as frequent as with placebo) include nausea, vomiting, injection site reactions (including induration, pruritus, nodules and swelling), muscle cramps, dizziness or syncope, somnolence or sedation, anorexia, and decreased appetite or other appetite disorders. The most common adverse effects in patients with alcohol use disorder receiving naltrexone oral tablets (incidence >=2%) include depression, nausea, headache, dizziness, nervousness, fatigue, insomnia, vomiting, anxiety, and somnolence.
There are 30 severe adverse reactions.
| More Frequent | Less Frequent |
|---|---|
|
Allergic dermatitis Angioedema Skin rash |
None. |
| Rare/Very Rare |
|---|
|
Abnormal ECG Abnormal hepatic function tests Acute cognitive impairment Altered mental status Blurred vision Depression Drug-induced hepatitis Dyspnea Dysuria Earache Epistaxis Fever Gastrointestinal ulcer Hallucinations Hypertension Idiopathic thrombocytopenic purpura Increased urinary frequency Lymphadenopathy Mood changes Ocular inflammation Ocular irritation Ocular pain Phlebitis Pruritus of skin Sleep apnea Suicidal ideation Tinnitus |
There are 31 less severe adverse reactions.
| More Frequent | Less Frequent |
|---|---|
|
Abdominal pain with cramps Arthralgia Fatigue Headache disorder Insomnia Myalgia Nausea Symptoms of anxiety Vomiting |
Anorexia Chills Constipation Cough Diarrhea Dizziness Hoarseness Irritability Nasal congestion Nervousness Polydipsia Rhinorrhea Sinusitis Sneezing Sore throat Tachycardia |
| Rare/Very Rare |
|---|
|
Drowsy Edema Erectile dysfunction Muscle fasciculation Palpitations Tremor |
The following precautions are available for NALTREX (naltrexone hcl):
The safety and efficacy of naltrexone have not been established in pediatric patients younger than 18 years of age.
Contraindicated
Severe Precaution
Management or Monitoring Precaution
Contraindicated
| None |
Severe Precaution
| None |
Management or Monitoring Precaution
| None |
In reproduction studies in rats and rabbits, oral naltrexone increased the incidence of early fetal loss. There are no adequate and well-controlled studies of oral naltrexone use in pregnant women. Available data from published case series of naltrexone extended-release injectable suspension are insufficient to identify a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes.
Naltrexone should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Untreated opioid addiction in pregnancy is associated with adverse obstetrical outcomes, such as low birth weight, preterm birth, and fetal death, and 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, CNS abnormalities, behavioral disorders, and impaired intellectual development.
Naltrexone should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Untreated opioid addiction in pregnancy is associated with adverse obstetrical outcomes, such as low birth weight, preterm birth, and fetal death, and 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, CNS abnormalities, behavioral disorders, and impaired intellectual development.
Naltrexone and its major metabolite, 6beta-naltrexol, are present in human milk. There are no data on the effects of the drug on the breastfed infant or on milk production. Consider the developmental health benefits of breastfeeding along with the mother's clinical need for naltrexone and any potential adverse effects on the breastfed infant from naltrexone or the underlying maternal condition.
Clinical studies of naltrexone extended-release injectable suspension did not include sufficient numbers of patients 65 years of age and older to determine whether they respond differently from younger patients. In trials of alcohol-dependent patients, 2.6% of patients were over 65 years of age, and one patient was over 75 years of age.
No individuals older than 65 years of age were included in studies of opioid dependency. The pharmacokinetics of naltrexone have not been evaluated in the geriatric population. This drug is known to be substantially excreted by the kidney, and the risk of adverse reactions may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, it may be useful to monitor renal function in this population.
No individuals older than 65 years of age were included in studies of opioid dependency. The pharmacokinetics of naltrexone have not been evaluated in the geriatric population. This drug is known to be substantially excreted by the kidney, and the risk of adverse reactions may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, it may be useful to monitor renal function in this population.
The following prioritized warning is available for NALTREX (naltrexone hcl):
No warning message for this drug.
No warning message for this drug.
The following icd codes are available for NALTREX (naltrexone hcl)'s list of indications:
No ICD codes found for this drug.
No ICD codes found for this drug.
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