The Role of Opioid Blockers in Treatment of Opioid Use Disorder

By: Bonnie Nolan, PhD, Addiction Services Coordinator
Woodbridge Township Department of Health & Human Services

For centuries, there have been few options for the millions of people who have suffered from opiate and opioid use disorders. Although opiates are derived from opium, while opioids are synthetics such as heroin, this class of drug all bind to µ-opioid receptors and therefore exert similar effects, such as analgesia and, at higher doses, euphoria and dependence. In the 20th century, inpatient institutions, support groups such as Narcotics Anonymous, counseling by anyone from a sponsor to a licensed clinician, and the opioid methadone represented the full gamut of treatment options.
As we reached the new millennium, buprenorphine (aka Subutex) and its variant Suboxone (buprenorphine + naloxone, an opioid blocker), were introduced. This not only represented a novel treatment for opioid use disorders, but a novel mindset. Methadone had shown considerable efficacy when used as prescribed, but it is a burdensome treatment. Risk of overdose and diversion (selling or trading the dose for “street” drugs) necessitates close supervision, so patients have to show up at a dosing site daily, often for years. However, Suboxone and Subutex carry a much lower risk for overdose and diversion, so they can be prescribed as any prescription would be, albeit by a doctor who has obtained a special waiver. Patients can take these medications and get on with the business of rebuilding their lives and getting better. When methadone was the only medical option, patients suffered not only the inconvenience of the daily visit to the clinic, but the stigma that invariably accompanied that. Suboxone therapy offered patients a more dignified medical approach.
More recently, an entirely new therapy was introduced. Arguably the most important advance in the fight against opioid-related mortality to date, naltrexone and naloxone block opioid receptors so that drugs such as heroin cannot bind to them, thereby completely blocking all effects of opioids. There are absolutely no narcotic effects associated with opioid blockers. Naloxone can be used in an emergency situation (Narcan) where a person has overdosed on opioids. To understand the completely non-narcotic nature of opioid blockers, one need only observe a patient who has been treated with Narcan. The patient is shocked into reality and often quite confused and sick as a result of experiencing what is called “precipitated withdrawal.” This syndrome is well-known to people who have opioid use disorder, and any notion that drug use behavior becomes intentionally more risky as a result of what naïve persons call the “Narcan safety net” is misguided; patients do not relish the idea of overdose or Narcan.
Medical treatment following Narcan administration is critical. Narcan is a short-term opioid blocker. If a person has overdosed and the effects of Narcan wear off, opioids that are already in the patient’s bloodstream can bind to the now active receptors, and overdose will occur again. Furthermore, the patient may have additional supply of the drug that caused the overdose; obviously this can result in a repeated life-threatening situation.
Opioid blockers can also be used in pill form, taken daily. Vivitrol (injectable naltrexone) blocks the effects of all opioids and opiates, and is injected monthly. Perhaps most importantly, the receptor blockade curbs cravings for opioids. These cravings can be one of the biggest impediments to recovery; Vivitrol’s efficacy in stopping cravings is remarkable.
Research shows that relapse rates drop dramatically during Vivitrol treatment. Recommended term of Vivitrol treatment is generally six months to one year, but it varies by patient. Vivitrol is covered by most insurance, including Medicaid. There are no known long-term side effects, and short-term side effects are minor.
It is important to note that Vivitrol is intended for use while a person receives additional psychological therapy for substance use disorder. It is by no means a substitute for counseling. Patients should always seek counseling for substance use issues along with medical therapies.
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