What is naltrexone?

Naltrexone is a medication approved for the treatment of opioid use disorder (opioid dependence). It blocks the μ (mu) opioid receptor in the brain, displacing most other opioids and rendering them basically inactive in that regard. If a person under treatment with naltrexone, takes an opioid (e.g. heroin, oxycodone, hydrocodone etc), the opioid ingested
cannot activate the μ opioid receptors and thus exert its actions to the body. The actions typically mediated by these receptors include the feeling of euphoria (“high”), analgesia (decreased perception of pain), respiratory depression, somnolence. In other words, the most rewarding and dangerous effects of opioids are blocked by naltrexone.

How is the medication administered?

Naltrexone is either administered orally (by mouth) in a tablet form or intramuscularly (muscle injection). The oral form has to be taken daily typically. The intramuscular form can be administered monthly as the medication is released slowly in the circulation for an extended period of time. The oral formulation is more affordable and easier to take. The major advantage of the intramuscular formulation is increased adherence to treatment, as the patient only has to remember to take his shot once per month and is thus protected from relapse for a more extended period of time.

How does naltrexone prevent a lapse from becoming a full-blown relapse?

If a person receiving naltrexone at the recommended dose decides to (unfortunately) use an opioid (e.g. heroin or oxycodone), they will likely not feel the effects of the opioid as the main relevant receptors at the brain are blocked by naltrexone. The body will deactivate the opioid ingested within a few or several hours (whereas naltrexone lasts for much longer in the body). Under the condition of ongoing treatment with naltrexone, the possibility of using again is much lower than otherwise, as our hypothetical person did not feel much after using an opioid once. So, why use an opioid again, if it feels as if they are taking an inactive substance? In other words, it is less likely that a lapse (a single time use event) will lead to a full-blown relapse (frequent, compulsive use with loss of control over the amount used and the time spent in the activity). People who are adherent to treatment with naltrexone are very well protected from a full-blown relapse and typically do very well. The treatment
typically fails after a patient stops being adherent to naltrexone and uses opioids restarting the vicious cycle of relapse.

Is naltrexone addictive?

No, naltrexone has no addiction potential whatsoever as it blocks the μ opioid receptor.
Naltrexone does not produce a euphoric sensation and there is no risk for abuse. In contrast, medications/substances that stimulate this receptor can have addictive properties.

What are the side effects of naltrexone?

Naltrexone is tolerated well when taken responsibly under the supervision of a knowledgeable physician. Of course, like any other medication, it can cause side effects. When initiating treatment (taking naltrexone for the first time), if a person is tolerant to
opioids (which happens following frequent, heavy use), naltrexone can induce opioid withdrawal symptoms. These symptoms would have happened anyways, once that person would quit taking opioids but with naltrexone they could be more intense and abrupt. This is why, naltrexone is only started after a person is already past the phase of opioid withdrawal (and never before that phase is over). Other side effects include nausea, dizziness, headaches, fatigue.Severe adverse effects are rare and include liver damage.

Under the hands of an experienced psychiatrist, this medication can be used safely and effectively. Also, it should be emphasized that the side effects of naltrexone are minuscule in comparison to the dire complications associated with continued opioid use (e.g. risk of overdose, respiratory depression and death, contracting Hepatitis C and HIV).

Is it OK to use other substances while taking naltrexone?

Abstinence from any and all substances is the goal when under treatment with naltrexone. Generally, this medication is supposed to increase the margin of safety of any opioid use as it renders them almost inactive (when comparing taking the same dose of an opioid in
the absence of naltrexone). However, definitely ongoing use of opioids is not safe in general and is not recommended. Also, using other substances such as alcohol and marijuana is not advisable, but probably taking naltrexone does not increase the risks associated with such use to a significant extent. In addition, interestingly naltrexone is also approved by the FDA for the treatment of alcohol use disorder (alcohol dependence/addiction) and appears to decrease the pleasure derived from alcohol use.

Regular urine drug screen testing may be recommended to monitor response to treatment and ensure its safety. If naltrexone is not working for you as evidenced by ongoing use of opioids, perhaps a different treatment plan should be implemented to assist you in your
recovery.

Is naltrexone administered by itself or additional treatments are provided concurrently?

Psychotherapy is a treatment provided simultaneously with naltrexone to support and assist our patients in their recovery from opioids as it has been shown to improve the outcomes of treatment with naltrexone. Active participation in psychotherapy is recommended based on most treatment protocols. In addition, any underlying psychiatric disorders (e.g. depression, anxiety) are also being addressed as indicated at the same time to achieve the best results.

What type of treatment does Dr. Panagopoulos offer for opioid use disorder (opioid addiction)?

Dr. Panagopoulos, a double-board certified addiction psychiatrist with significant related experience in the treatment of opioid use disorder, offers both medication management services regarding naltrexone as well as psychotherapy services in a compassionate and individualized manner adhering to the most up-to-date treatment guidelines. There is no room for shame and stigma in our clinic and treatment philosophy!

Thank you for your interest in mental health and in our services!

Feel free to contact us to schedule your complimentary meet-and-greet 10-minute appointment with Dr. Panagopoulos, if you reside in New York, Texas or California.

The content of this website is provided for educational/informational purposes only. It should not be used as a substitute for medical evaluation, diagnosis and treatment.