Naltrexone and Opioid Use Disorder

It’s not often you come across a medication that seems to work for many patient problems, but naltrexone is one of those medications. My staff and I have been working closely with providers to help patients utilize naltrexone for pain, inflammation, autoimmune conditions, depression, anxiety, and long covid symptoms. It wasn’t until recently that we started working with patients utilizing tiny doses of naltrexone to help them transition off of opioids.

If you have read or listened to the news, the opioid epidemic continues to roll on. The CDC website has data on the opioid crisis, and the one statistic that jumps out is that 760,000 people have died since 1999 from a drug overdose. The number of drug overdose deaths increased by nearly 30% from 2019 to 2020, and almost 75% of the 91,799 drug overdose deaths in 2020 involved an opioid. The problem continues to march on without many solutions to the problem.

Not all deaths are from legitimate prescriptions, as in the late 1990s. We are currently dealing with deaths due to synthetic opioids, particularly those involving illicitly manufactured fentanyl. Fentanyl finds itself in combination with heroin, counterfeit medications, and cocaine. The problem with fentanyl is that it takes a minimal amount to be lethal and can easily be combined into these other illicit dosage forms.

It seems like a lot of doom and gloom regarding opioids and the current situation in our country. Still, I want to provide some hope to those taking opioids for conditions they might have been prescribed for many years ago and may wish for a different option.

Opioid Use Disorder, defined by the CDC as a substance use disorder, is a problematic pattern of opioid use that causes significant impairment or distress. OUD is a treatable, chronic disease. A diagnosis of OUD is based on specific criteria, such as unsuccessful efforts to cut down or control use leading to failure to fulfill obligations at work, school, or home, among other measures. It can even lead to overdose and death. In 2020, an estimated 2.7 million people ages 12 or older reported having an OUD.

Historically, patients wanting to get off opioids could do so with methadone or buprenorphine. Both are good options, and once transitioned to these medications, the risk of overdose goes down significantly. The drawbacks are they need to be prescribed by a provider with a special license for buprenorphine and in a clinic setting with methadone. Another downside is that now the patient can develop a dependence on these medications.

Naltrexone has been used at higher doses to block the opioid receptor 24 hours a day, not allowing the opioid to stimulate the receptor, producing a euphoric feeling or sedation—the amounts used for this type of treatment range from 50 to 200mg per day. The downsides of this treatment option are that the patient has to stop the opioid before starting treatment, and patients describe a feeling of being “flat” or dysphoric while on this treatment option.

All 3 of these options are helpful for patients in their quest to end their dependence on opioids. 

Now I am going to propose another option.  In my practice, we have been helping patients transition away from opioids with the use of ultra-low-dose naltrexone (ULDN). In previous articles, I have talked about the use of low-dose naltrexone (LDN), which are doses ranging from 0.5mg to 10mg per day. ULDN utilizes 1 to 50 micrograms or 0.001 to 0.05mg doses. Achieving these tiny doses is done by making a suspension that can be drawn up by the patient and taken orally. Making a 1mcg capsule would be extremely difficult, and the suspension makes it more accurate and adjustable as needed while the dose is slowly increased.

When utilizing ULDN, these low doses improve the effectiveness of the opioid so that the patient will need less, a benefit that could be used for any patient taking an opioid. Ultimately, less drug with the same effect is a win/win for the patient. 

The protocol involves weekly increases of the ULDN while simultaneously decreasing the opioid by about 10% each week until the patient is entirely off the medication. After the opioid has been removed, naltrexone is titrated upwards until the desired effect (pain relief) is achieved. Some chronic pain patients may require additional medication to bridge the pain gap until the LDN provides pain relief.

The pharmacy has worked with five patients on transitioning them off their opioid medication. Three patients have been long-term opioid patients taking them for 13 to 15 years. We also have three patients that are in the transition phase. The database is not extensive, but knowing how difficult it is to help get patients off opioids should be considered a success.

Why do I think this protocol has been effective? First, you need to have a motivated patient to get off opioids. Without having that, this will be exponentially more difficult. Secondly, having LDN as the medication to transition to is an excellent option as it helps patients in so many ways, so it’s not just getting the patient to discontinue the opioid but also having a backup to replace it. 

Lastly, as I mentioned when talking about other treatment options, the patients often feel “flat” or like something is missing, which I think is the dopamine spike they would get from taking the opioid. Dopamine, our reward neurotransmitter, spikes when we do something that rewards us. Not having a dopamine spike leaves a person feeling empty. When a person takes LDN, they get a dopamine increase, which is replaced for those patients making the transition a little less painful.

The article provides a lot of information that I hope you didn’t find too technical but ultimately valuable for you or a loved one. Transitioning a person off opioids is no easy task. Still, from my experience with a small group of patients, this protocol has made it less painful, and I hope to share it with as many people as possible to help patients leave opioids in the dust.

If you or a loved one takes an opioid and wants to explore an alternative option for pain management or is just looking to stop taking the opioid, call the pharmacy @ 701-483-4858 to schedule a consultation. Please visit my website at www.irsfeldpharmacy.com to find this and other archived articles in the blog section and a link to listen to my podcast, specifically episode 13, which covers this topic (or click link below for podcast). Until next time, be vigilant about your health!!