A Drug for a Drug

It is perhaps ironic that the opioid epidemic that everyone is worried about is something that we have the most ability to address. The main pharmacological treatment (i.e., treating with drugs) for opioid addiction is known as Medication-Assisted Treatment or MAT. The rationale for MAT is use other opioids to reduce cravings, highs, and withdrawal from the standard opioid substances. However, from my limited reading of the conversation around these treatments, there appears to be a stigma against it, essentially saying, “You can’t treat drug addiction with more drugs!” That is understandable. If you’re unfamiliar with how the brain reward pathways or the MAT drugs work, then it is a bit unbelievable that giving people more opioids will help them to stop abusing opioids. However, we have definitive evidence that they reduce opioid abuse, so why not use them in our armamentarium?

Methadone is one of the oldest and most well-known of the drugs for MAT. Its long half-life and slow opioid receptor activation reduces the risk of withdrawal and cravings while also preventing any highs. When I first learned of this drug in Pharm school, I was flabbergasted by its mile-long list of both drug interactions and adverse effects, the most prominent one being QT prolongation and Torsades de pointes. QT prolongation?! You mean we risk stopping someone’s heart?! But through some discussion and more reading, it’s not as scary as the texts make it out to be. For one thing, QT prolongation is rare, and clinicians can just order regular EKGs. It is also appears to be safe when used long-term.

The main role of methadone is to help addicts taper off the opioids by taking a lower and lower dose over time, a sort of reverse tolerance. Remember, if you stop opioids cold turkey, you risk the dreaded withdrawal symptoms: the low mood, shaking, flu-like symptoms, sweating, and anxiety.  Methadone helps prevent that. But also recall that methadone is an opioid, so addiction and overdose is still a concern. Initially, people on methadone maintenance treatment must go to a methadone clinic every day for their dose until they are determined to be stable enough to take multiple doses at home. On a side note, methadone can also be used for pain control, and it’s an attractive one because of its lower addictive potential. However, like with all opioids, long-term effectiveness is unknown.

A medication that may be more comfortable to use is buprenorphine, or the brand Suboxone (plus Subutex and others). It is also an opioid, but importantly is a partial agonist. So it binds to the opioid receptors, but causes much less of a high, even less than methadone. It also reduces withdrawals and cravings like methadone. It has a ceiling effect, so that even at a high dose, there is no effect. Thus preventing overdose. Some may be tempted to crush buprenorphine and snort or inject it. To counter that, the manufacturers also include naloxone (an opioid antagonist) in its formulation to block any possible high.

Finally, there are naloxone and naltrexone, the opioid receptor antagonists. Naloxone is shorter-acting and works faster. It must be injected to rapidly reverse opioid overdose and prevent any highs. However, since it is short-acting, it is only used for emergencies. You may have read the high praise regarding its ability to save lives and that reputation is well-deserved. Naltrexone works the same way, but is longer-acting. It can be used in the same way as methadone and buprenorphine for MAT; however, the largest downside is that it does not reduce cravings, which to me would make it very difficult to use. We know how powerful cravings can be.

Alas, these treatments aren’t magic bullets. For buprenorphine, the relapse rate is 90%. However, this is after buprenorphine is discontinued. And remember! Relapses are not the failures we imagine them to be. Sure, we don’t want them to happen, especially for those who have lost tolerance to opioids. But on the whole, they are unfortunate episodes like in other chronic disease. Would you give up on a diabetic because their A1C went above 7.0%?

Summary: There are evidence-based pharmacological treatments for addiction. We shouldn’t shun them out of fear.

Disclaimer: This post is meant to be a general overview of pharmacological treatments of opioid addiction and not specific medical advice. Please consult with a health care professional before deciding on a course of therapy.

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