Suboxone and the two drugs that comprise it, buprenorphine and naloxone, are used to treat opioid addiction, although they are both subject to abuse. You may have read about how naloxone has saved the lives of many young people suffering from heroin overdoses. The following Suboxone facts provide insights on these often misunderstood drugs. Learn the differences between buprenorphine and naloxone, how they work together and alone, side effects and more.
Is Subutex Still Available?
No. Subutex, a brand name of buprenorphine manufactured by Reckitt Benckiser Pharmaceuticals, was discontinued in 2011. This caused widespread confusion due to the misconception that it was withdrawn due to abuse potential or safety concerns. Administered as sublingual tablets, the drug was placed under the tongue and allowed to dissolve. When taken in prescribed doses, Subutex did not generate the same level of euphoria, drowsiness or central nervous system suppression as illicit opioids. In February 2015, the U.S. Food and Drug Administration (FDA) said Subutex was not withdrawn for reasons of safety or effectiveness. Currently, three buprenorphine/naloxone formulas and one buprenorphine formula have been approved by the FDA, although generic versions of Subutex may now be considered due to the 2015 findings.1,2
What Is Naloxone?
Naloxone, also called Narcan, is a drug formulated with buprenorphine in Suboxone to treat opioid addiction. On its own, it is a highly effective antidote indicated for the emergency treatment of known or suspected opioid overdose, as manifested by respiratory and or CNS depression. Although emergency medical personnel and hospitals have used naloxone for decades, it is being used with growing frequency by police departments and families of addicted individuals to reverse opioid overdose. For many years, it was available only as an injection. In late 2015, however, the FDA approved a nasal spray. This provides family members, caregivers and first responders with an easy-to-use, needle-free alternative to injectable naloxone. The opioid abuse epidemic sparked the enactment of legislation in many states to make naloxone widely available.3,4
What Is the Difference Between Buprenorphine and Naloxone?
To understand the differences, it helps to have a basic understanding of agonist and antagonist drugs. An agonist fully activates the opioid receptors in the brain, resulting in the desired opioid effects addicts seek in heroin, oxycodone, methadone, hydrocodone, morphine, opium and others. An antagonist is a drug that blocks opioids by attaching to the opioid receptors without activating them. Naltrexone and naloxone are both antagonists, and the latter is combined with buprenorphine in Suboxone, as well as used alone as an emergency intervention to reverse opioid overdose.5
Buprenorphine is a partial agonist, so while it activates the opioid receptors in the brain, it does so to a far less degree than a full agonist. It is an effective treatment for opioid addiction because it acts as an antagonist, blocking other opioids, while allowing some opioid effects to suppress withdrawal symptoms and cravings.5
What Are the Dangers of Taking Suboxone?
Suboxone can cause serious life-threatening breathing problems, overdose and death, especially when the film is injected intravenously. Injecting Suboxone film may cause serious withdrawal symptoms such as pain, cramps, vomiting, diarrhea, anxiety, sleep problems and cravings. Injecting it in combination with benzodiazepines or other medications acting on the CNS (e.g. sedatives, tranquilizers, or alcohol) is extremely dangerous. Drinking alcohol while taking Suboxone can lead to a loss of consciousness or death. Fatalities have been reported in individuals who were not opioid-dependent. Suboxone impacts the liver and is not recommended for individuals with severe hepatic impairment. It may be used with caution for maintenance treatment in those with moderate hepatic impairment who have initiated treatment with a buprenorphine product without naloxone. Even when administered properly, Suboxone is associated with a wide array of side effects — from common to serious.6
- Substance Abuse and Mental Health Services Administration website. https://www.samhsa.gov/medication-assisted-treatment/treatment/buprenorphine Updated May 31, 2016. Accessed February 9, 2017.
- Determination That SUBUTEX (Buprenorphine Hydrochloride) Sublingual Tablets, Equivalent 2 Milligrams Base and Equivalent 8 Milligrams Base, Were Not Withdrawn From Sale for Reasons of Safety or Effectiveness. Federal Register website. https://www.federalregister.gov/documents/2015/02/13/2015-03001/determination-that-subutex-buprenorphine-hydrochloride-sublingual-tablets-equivalent-2-milligrams Published February 13, 2015. Accessed February 9, 2017.
- What is naloxone? Project Lazarus website. http://projectlazarus.org/patients-families/what-naloxone Accessed February 9, 2017.
- FDA approves naloxone nasal spray to reverse opioid overdose. National Institute on Drug Abuse website. https://www.drugabuse.gov/news-events/news-releases/2015/11/fda-approves-naloxone-nasal-spray-to-reverse-opioid-overdose Published November 18, 2015. Accessed February 9, 2017.
- What’s this agonist/antagonist stuff? The National Alliance of Advocates for Buprenorphine Treatment website. https://www.naabt.org/faq_answers.cfm?ID=5 Accessed February 9, 2017.
- Opioid dependence FAQs. Suboxone website. http://www.suboxone.com/understanding-opioid-dependence/frequently-asked-questions Accessed February 9, 2017.