Suboxone: The Wonder Drug?

The 57-year-old woman is standing in the hall outside of the exam room. She is agitated. “I’m waiting for the doctor. I’m freezing! My back is killing me!” I note she is pale, unable to stand still, and has a sheen of perspiration on her forehead. She is in withdrawal. I get her a blanket and ask her to wait in her room. The pain clinic nurse is downstairs at the pharmacy getting the patient’s prescription for Suboxone for induction. Induction is the process of starting the patient on medication and finetuning the dose.

An hour later the patient is back in the hall calling me, “Thanks for the blanket!” She is smiling. Her color is back. She is clear eyed, calm, and collected. What happened? Suboxone. Suboxone is a combination of buprenorphine and naloxone that is used to treat opioid addiction. Buprenorphine is a partial agonist of the μ-opioid receptor with a high affinity and low rate of dissociation from the receptor. In English, the buprenorphine molecule sticks to the opioid receptor in the brain, but only partially activates it. Then it stays there for a long time, blocking it from opioids, before dissociating. What this means for the addict is that they get enough opioid receptor activation that they don’t get sick from withdrawal. They can function normally with less of the problematic effects of a full agonist like morphine or heroine.

The addition of naloxone, a

full opioid antagonist (blocker), keeps the Suboxone pills from being crushed and injected. Though naloxone has a strong effect when given parenterally (by injection), its effect when given by mouth is negligible because it is poorly absorbed sublingually. Suboxone disintegrating tablets are given under the tongue.

So, what is this wonder drug all about? In 2000, federal legislation (Drug Addiction Treatment Act of 2000) made office-based treatment of narcotic addiction with schedule III-V drugs legal. Until then, the only option for addicts was abstinence-based treatment or methadone clinics. The ever-increasing rates of drug overdose deaths in the United States showed this was not working. At first, only MDs specially approved by the Department of Health and Human Services could prescribe medications to treat addiction. In 2016, President Obama signed the Comprehensive Addiction and Recovery Act allowing nurse practitioners and physicians assistants to prescribe schedule III-V drugs for the treatment of addiction. Previously, they could prescribe these medications to treat pain but not to treat addiction.

What does this mean for the addict? For starters, Suboxone and similar drugs are now more widely available. Until recently, the only way for a heroin addict to keep from getting withdrawal sickness was to use more heroine. These patients were considered toxic to regular doctors because their disease lead to ever-increasing doses, seeking medications from multiple providers, decreasing levels of health, and ultimately death. Now that there is an option other than going cold turkey, the addict without some kind of pain diagnosis can get access to health care whereas before they would avoid it because of the stigma of being an addict. Because Suboxone is a partial agonist with high affinity to the μ-opioid receptor, it decreases the ‘high’ if the patient continues to use narcotics causing the patient to lose interest. It offers the benefit of allowing the addict to function in life, decreases the likelihood of death from respiratory depression, and increases the quality of life because there is no need for the addict to ride the wheel of withdrawal—drug seeking, using, running out, and then seeking again to the exclusion of every joy of life.

What happens when a person starts buprenorphine? After a largish battery of tests, the prospective recovering addict will be asked to abstain from narcotics before induction to Suboxone. How long before the first dose the addict has to abstain depends on the person’s addiction. Longer acting drugs like methadone could be 24 hours. Shorter acting drugs like morphine could be as little as six hours. The person should be in the early stages of withdrawal. The reason for this is the “partial” part of partial agonist. The buprenorphine molecule will muscle other narcotics off the receptor site where it was fully activating the receptor. Now, the higher affinity buprenorphine is sitting there doing half the work that the heroine was doing and this leads to symptoms of withdrawal. Giving a person a drug that puts them immediately into withdrawal will turn them off to it completely. You won’t see that person again. Higher success rates are tied with higher levels of symptoms of withdrawal before induction. Now instead of precipitated withdrawal, the person has relief from symptoms of withdrawal even if they are not getting high.

A person who has been successfully inducted to Suboxone therapy will find almost immediate relief. The terrible body aches, muscle pain, abdominal pain, depression, diarrhea, and cravings evaporate. Our patient might just have found a new way to live, free from the constant need to find more narcotics. She can focus on her life instead of her disease. Most of the clinic patients have jobs. They want desperately to be productive members of society for themselves and for their families. Buprenorphine therapy coupled with lifestyle interventions provided by mental health professionals, self-help groups like Narcotics Anonymous, and patient-initiated interventions (like taking a class or going back to school) are part of the success story of a growing number of recovering addicts.

What’s it like to come off Suboxone? Eh, probably a lot like getting off heroine. Same withdrawal profile or pretty close. Patients wanting to get off all narcotics, including Suboxone, can be weaned off gradually depending on their desired treatment goals. Someone facing a jail sentence or travel overseas that needs to detox from opioids quickly may be on a tapered dose of Suboxone for just a few days or weeks. Other people may decide that the burden of staying on Suboxone is worth not having to go through withdrawal and choose to stay on a maintenance dose for the rest of their life. The addiction specialist will help guide the patient through the decision process. Many patients decide to stay on the medication as a hedge against relapse since buprenorphine has a higher affinity for opioid receptors than street drugs. This coupled with the very slow rate of dissociation means that a person would have to stop the buprenorphine well in advance of restarting heroine or other opioid in order to get high.

What does this mean for health care? For one, at least some addicts who eschewed health care in the past can now get treatment for this disease. At some point, most addicts will desire to get off narcotics. Having a real treatment option available instead of a far-away methadone clinic or withdrawal will work to drive these patients into recovery. Another thing is that it’s possible that some of the stigma of addiction will be lifted, at least slowly, as treatment becomes available and success stories become commonplace. As the DEA and FDA work to get a handle on the 70,000 overdose deaths per year by educating doctors and enforcing distribution laws, these drugs will become harder to get. During the 12 months prior to July 2017, overdose deaths fell in 14 states for the first time during the opioid epidemic, according to the Centers for Disease Control and Prevention. In the rest of the nation, at least the numbers have leveled off. Greater access to Narcan (brand name of naloxone, one of the drugs in Suboxone), and more treatment options for addicts will hopefully drive these numbers lower over time. It’s not time to celebrate, but at least there is a glimmer of hope. The priority is to keep addicts alive until they can (or they are ready to) get treatment for their disease.