If you are taking an opioid drug like morphine or oxycodone, are addicted to an opioid drug, or are having withdrawal signs. Opioid drugs include heroin and prescription pain drugs like oxycodone and morphine. Memorial Sloan Kettering was founded in 1884, and today is a world leader in patient care, research, and educational programs.

Effect on body weight of bupropion sustained-release in patients with major depression treated for 52 weeks. Patients and practitioners are encouraged to report all side effects online to MEDWatch, FDA’s medical product safety reporting program for health care professionals, patients, and consumers or by calling FDA-1088. Naltrexone is one component of a comprehensive treatment plan, which includes counseling and other behavioral health therapies to provide patients with a whole-person approach. Naltrexone is not a recommended option for anyone younger than 18 years of age, or for patients experiencing other health conditions. 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.

Because endogenous opioids are involved in the brain reward system, it would be reasonable to hypothesize that naltrexone might produce anhedonic or dysphoric effects. Although some evidence from small, early trials suggested that patients with a history of opiate dependence might be susceptible to dysphoric effects in response to naltrexone (Crowley et al. 1985; Hollister et al. 1981), reports of such effects have been inconsistent. Most large clinical studies of recovering opioid-dependent individuals have not found naltrexone to have an adverse effect on mood (Greenstein et al. 1984; Malcolm et al. 1987; Miotto et al. 2002; Shufman et al. 1994).

Vivitrol, a naltrexone formulation for depot injection containing 380 mg of the medication per vial, is also available. Additionally, naltrexone subcutaneous implants that are surgically implanted are available. While these are manufactured in Australia, they are not authorized for use within Australia, but only for export. By 2009, naltrexone implants showed superior efficacy in the treatment of heroin dependence when compared to the oral form.


Peak concentrations of naltrexone are 19 to 44 μg/L after a single 100 mg oral dose and time to peak concentrations of naltrexone and 6β-naltrexol is within 1 hour. Linear increases in circulating naltrexone and 6β-naltrexol concentrations occur over an oral dose range of 50 to 200 mg. Naltrexone does not appear to be accumulated with repeated once-daily oral administration and there is no change in time to peak concentrations with repeated administration. Depression, suicidal ideation, and suicidal attempts have been reported in all groups when comparing Naltrekson, placebo, or controls undergoing treatment for alcoholism. Naltrekson should be considered as only one of many factors determining the success of treatment.

Further the study will investigate the effectiveness and safety of XR-NTX treatment given in a naturalistic setting as an alternative to OMT. The study period is 24 weeks, a subsequent 28 week follow up study and a 1 year post-treatment study. From the same participating sites, a control group of 150 subjects matched on age and gender and currently enrolled in the OMT program receiving daily treatment with either oral buprenorphine or buprenorphine-naloxone will be recruited.

Naltrexone HCL – Uses, Side Effects, and More

This enables the body to expend energy stores, namely, the adipose tissue in the human body. To lose weight, patients, simply put, need to decrease their calorie intake and increase their energy consumption through expanded physical activity. Various forms of extreme calorie reduction and extreme exercising have been found to be very effective. The problem is that very few obese/overweight people can adequately follow these diets and exercise routines, and even fewer people can sustain them over long periods of time. Thus, extreme dieting and exercise are efficacious in study conditions, but are not necessarily effective in practice or at the population level. According to one review, naltrexone and acamprosate have strong evidence and are recommended as treatment options for alcohol dependence in conjunction with behavioral therapy.


With some care to appropriate patient selection and with adequate knowledge of side effects and potential complications, the naltrexone–bupropion combination can be an effective tool for treatment of the obese patient. Occupancy of the opioid receptors in the brain by naltrexone has been studied using positron emission tomography . Naltrexone at a dose of 50 mg/day has been found to occupy approximately 90 to 95% of brain MORs and 20 to 35% of brain DORs. Naltrexone at a dose of 100 mg/day has been found to achieve 87% and 92% brain occupancy of the KOR in different studies. Per simulation, a lower dose of naltrexone of 25 mg/day might be expected to achieve around 60% brain occupancy of the KOR but still close to 90% occupancy of the MOR.

Special patient populations

Do not use alcohol/any opiates for at least 7 days before starting Naltrekson. You may need to stop certain opiate drugs 10 to 14 days before starting Naltrekson. Clinically significant weight loss with bupropion and bupropion naltrexone combination in 1 year. Clinically significant weight loss with bupropion and bupropion naltrexone combination in 6 months.

Never try to overcome the effects of the medication by taking large doses of narcotic drugs or alcohol. Doing so could result in dangerous effects, including coma and death. Ask your doctor before using any prescription or over-the-counter medicine to treat a cold, cough, diarrhea, or pain while taking Naltrekson oral. Clinicians are reminded that there is no completely reliable method for determining whether a patient has had an adequate opioid-free period. A naloxone challenge test may be helpful if there is any question of occult opioid dependence. If signs of opioid withdrawal are still observed following naloxone challenge, treatment with Naltrekson should not be attempted.

Other metabolites of naltrexone include 2-hydroxy-3-methoxy-6β-naltrexol and 2-hydroxy-3-methoxynaltrexone. Following their formation, the metabolites of naltrexone are further metabolized by conjugation with glucuronic acid to form glucuronides. Naltrexone is not metabolized by the cytochrome P450 system and has low potential early signs of liver damage from alcohol for drug interactions. Naltrexone blocks the effects of MOR agonists like morphine, heroin, and hydromorphone in humans via its MOR antagonism. Following a single 100 mg dose of naltrexone, the subjective and objective effects of heroin were blocked by 90% at 24 hours, with blockade then decreasing up to 72 hours.

  • Keep taking this drug as you have been told by your doctor or other health care provider, even if you feel well.
  • Five of these patients discontinued Naltrekson because of nausea.
  • There is no abuse and diversion potential with naltrexone.
  • No serious adverse events were reported during these two trials.
  • Do not drive, use machinery, or do anything that needs alertness until you can do it safely.

It is used as part of a complete treatment program for drug abuse . This medication must not be used in people currently taking opiates, including methadone. Despite these findings, naltrexone’s manufacturer and some health authorities have promoted the medicine as superior to methadone and buprenorphine since it is not an opioid and does not induce dependence.

Common and Serious Side Effects of Naltrexone

In a study of the duration of MOR blockade with naltrexone, the drug with a single 50 mg dose showed 91% blockade of brain carfentanil binding at 48 hours , 80% blockade at 72 hours , 46% blockade at 120 hours , and 30% blockade at 168 hours . The half-time of brain MOR blockade by naltrexone in this study was 72 to 108 hours (3.0 to 4.5 neurotoxic medications days). Based on these findings, doses of naltrexone of even less than 50 mg/day would be expected to achieve virtually complete brain MOR occupancy. Blockade of brain MORs with naltrexone is much longer-lasting than with other opioid antagonists like naloxone (half-time of ~1.7 hours intranasally) or nalmefene (half-time of ~29 hours).

In May 2017, United States Secretary of Health and Human Services Tom Price praised as the future of opioid addiction treatment after visiting the company’s plant in Ohio. His remarks set off sharp criticism with almost 700 experts in the field of substance use submitting a letter to Price cautioning him about Vivitrol’s “marketing tactics” and warning him that his comments “ignore widely accepted science”. The experts pointed out that Vivitrol’s competitors, buprenorphine and methadone, are “less expensive”, “more widely used”, and have been “rigorously studied”. Transaminase elevations occurred in 3 of 9 patients with Alzheimer’s Disease who received Naltrekson (at doses up to 300 mg/day) for 5 to 8 weeks in an open clinical trial.

A placebo controlled trial of bupropion for smoking cessation in schizophrenia. Bupropion SR vs placebo for weight loss in obese patients with depressive symptoms. During trials, myocardial infarction was observed.40 Bupropion has the potential to increase heart rate, which in turn may provoke arrhythmias.41 The naltrexone–bupropion combination should be used with great caution in this group of patients.

If you have questions about how to get or use naloxone, talk with your doctor or pharmacist. If you think there has been an opioid overdose, get medical care right away even if naloxone has been used. Naltrexone binds to the endorphin receptors in the body, and blocks the effects and feelings of alcohol. Naltrexone reduces alcohol cravings and the amount of alcohol consumed.

Generic Name: naltrexone

In a small number of people, mild opiate withdrawal symptoms may occur, including abdominal cramps, restlessness, bone/joint pain, muscle aches, and runny nose. If any of these effects last or get worse, tell your doctor or pharmacist promptly. 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. Do not increase your dose, take it more often, or stop taking it without your doctor’s approval.

Naltrexone for Opioid Use Disorder

It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved Naltrekson for the treatment of alcohol dependence. Naltrekson belongs to a class of drugs known as opiate antagonists. It is used as part of a complete treatment program for alcohol or opioid abuse (e.g., counseling, 12-step program, lifestyle changes). Naltrexone is metabolized in the liver mainly by dihydrodiol dehydrogenases into 6β-naltrexol (6β-hydroxynaltrexone). Levels of 6β-naltrexol are 10- to 30-fold higher than those of naltrexone with oral administration due to extensive first-pass metabolism.

For more information patients should talk to their practitioner or pharmacist. Patients should tell their practitioner about any side effects that are bothersome, or do not go away. When starting naltrexone for AUD, patients must not be physically dependent on alcohol or other substances.

Although no causal relationship with https://en.forexpulse.info/ is suspected, physicians should be aware that treatment with Naltrekson does not reduce the risk of suicide in these patients. A flexible approach to a dosing regimen may need to be employed in cases of supervised administration. Thus, patients may receive 50 mg of Naltrekson every weekday with a 100 mg dose on Saturday, 100 mg every other day, or 150 mg every third day. The degree of blockade produced by Naltrekson may be reduced by these extended dosing intervals. If you are giving this medication to yourself at home, learn all preparation and usage instructions from your health care professional. Before using, check this product visually for particles or discoloration.

A 2011 review found insufficient evidence to determine the effect of naltrexone taken by mouth in opioid dependence. While some do well with this formulation, it must be taken daily, and a person whose cravings become overwhelming can obtain opioid intoxication simply by skipping a dose. Due to this issue, the usefulness of oral naltrexone in opioid use disorders is limited by the low retention in treatment.

WP 3 is a health-economic study on the cost of XR-NTX treatment in study participants compared to treatment with buprenorphine or buprenorphine-naloxone in the controls. Registry-based information will be collected based on participants’ personal identity number . A dose of 50 mg once daily is recommended for most patients. The placebo-controlled studies that demonstrated the efficacy of Naltrekson as an adjunctive treatment of alcoholism used a dose regimen of Naltrekson 50 mg once daily for up to 12 weeks. Other dose regimens or durations of therapy were not evaluated in these trials.