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Naloxone, Naltrexone, and Buprenorphine: What are They and Which is Right For You?

The recent opioid crisis in America has led to lots of attention on more effective forms of treatment for addiction. The recent rise in popularity of medication-assisted treatment (MAT) using methadone, buprenorphine, and naltrexone has been among the most talked-about forms of treatment for opioid addiction. However, what’s the difference between these medications and how are they used most effectively?

Naloxone and Naltrexone

Naloxone and naltrexone are both opioid antagonists that work to block the effects of opioids in the brain, but they have different uses. Naloxone is a short-acting drug that acts immediately to reverse the effects of opioid overdose. Naloxone is available to households, businesses, and medical facilities especially in American communities that have been hardest hit by the opioid epidemic. Naloxone works by binding to the opioid receptors in the brain, kicking out any existing opioids. This causes an immediate opioids withdrawal, which may be life-saving for someone who is overdosing on heroin or other opioid painkillers.

Naltrexone

Naltrexone is also an opioid antagonist that binds to the opioid receptors in the same way. The only notable difference is that naltrexone lasts longer than naloxone. Whereas naloxone is used primarily for the emergency treatment of an acute opioid overdose, naltrexone is used a long-term treatment after opioid detox. Marketed under the brand names of Vivitrol® and ReVia®, naltrexone helps prevent alcohol and opioid relapses by diminishing the enjoyment of using these substances. Naltrexone does not reduce the impairment effects of alcohol, but it does block the “buzz” that encourages more drinking. Naltrexone also does not stop nor reduce the intoxicating effects of alcohol on coordination, response time, and other physical impairments. It also does not cause a severe physical response to drinking, so you will not get sick if you drink while taking naltrexone. For individuals in recovery from opioid addiction, naltrexone is a long-term medication that helps maintain abstinence by reducing cravings. Naltrexone also works by binding to the opioid receptors in the brain, thereby blocking the euphoric and analgesic effects of opioids like heroin and narcotic painkillers. Naltrexone works very similarly for opioid addicts as it does for alcoholics, namely in the way it helps to reduce cravings and blocks the pleasurable effects of each substance. Naltrexone is not a narcotic medication, and it is not addictive, but it may cause some side effects like:

  • nausea and vomiting
  • dizziness
  • muscle cramps
  • insomnia
  • bruising, tenderness, or swelling at injection site (injectable forms of naltrexone)

Naltrexone is generally considered to be a very safe option for opioid and alcohol addiction treatment, but there is one serious risk associated with recovering opioid addicts. Regardless of the prior dosage or tolerance to opioids, if you have been taking naltrexone for treatment, your opioid tolerance has changed significantly. Attempting to use previous dosages of heroin or opioid painkillers drastically increases the risk of overdose, coma, or death. Further, attempts to take large amounts of opioids while on naltrexone can quickly lead to coma or death. Although naltrexone blocks the pleasurable effects of opioids, it cannot prevent respiratory depression caused by these drugs. So, large quantities of opioids won’t get you high, but they increase your chance of serious injury or death from respiratory depression. Although naltrexone is an effective form of treatment for opioid and alcohol dependence, individuals receiving it should also participate in a recovery program or regular counseling.

Buprenorphine

Buprenorphine was developed as an improvement to methadone, as it has added safety measures that set it apart from the full opioid agonist formulation. Buprenorphine, like methadone, is a long-lasting fully synthetic opioid that has a half-life of 24 to 60 hours. The most significant characteristic of buprenorphine is that it is a not a full opioid agonist like methadone. Buprenorphine is a partial agonist because it:

  1. fully binds to opioid receptors in the brain, blocking all other opioids from affecting
  2. has a ceiling in its effects, limiting the degree to which a user can feel euphoria and other effects of opioids

The ceiling effect of buprenorphine means that larger amounts of it will not result in a more intense euphoria or high. There is no limit to how high a user can feel when taking any other opioid, including methadone. Most buprenorphine formulations include naloxone, an opioid antagonist, as an added safety measure to prevent tampering. The naloxone in buprenorphine is inactive unless someone injects the medication. Only through intravenous administration would the naloxone in buprenorphine become active. Although thoughtful, this safety measure is far less effective than buprenorphine’s ability to block all other opioids. Today, buprenorphine is used to ease opioid withdrawal symptoms during detox, and in medication-assisted treatment (MAT) for opioid addiction treatment with counseling or recovery program participation. Since buprenorphine binds so strongly to opioid receptors in the brain, other opioids are rendered useless for their analgesic and euphoric effects. However, that does not mean there are no risks with buprenorphine treatment. Even though buprenorphine’s effects have a ceiling, attempting to take other opioids while taking it increases the risk of respiratory depression, coma, or death. Trying to override buprenorphine’s blocking effects will only result in respiratory depression because, like naltrexone, buprenorphine blocks the pleasurable effects of other opioids. Buprenorphine is effective because it splits the difference between the greatest struggle of addicts and that of addiction treatment professionals; binding to opioid receptors in the brain while avoiding the peaks and troughs of problem opioids like painkillers and heroin. Another beneficial use of buprenorphine is for opioid detox One of the most dangerous parts of opioid detox is the persistent cravings that addicts endure. With the painful symptoms, cravings push many addicts to relapse before or shortly after completion of opioids detox. The benefit of buprenorphine during this process allows addicts to withdraw comfortably because:

  • buprenorphine is an opioid that binds strongly to opioid receptors, thereby eliminating withdrawal symptoms
  • since buprenorphine binds to opioid receptors, addicts do not experience cravings for opioids during the detox process
  • as the body expels problem opioids during detox, buprenorphine doses are adjusted to address the severity of withdrawal symptoms, then reduced as the detox nears conclusion

Using buprenorphine during opioid detox help addicts to overcome one of the things they most fervently avid in getting sober; the pain and discomfort of withdrawal.

Maintenance Or Abstinence

When it comes to your recovery from opioid addiction, there are many options available, but all options fall under one of two paths;

  1. Abstinence options can include naltrexone or not, and may involve various types of addiction treatment ranging from short-term to long-term, counseling or outpatient to residential or inpatient treatment
  2. Maintenance options include MAT using buprenorphine or methadone

Although buprenorphine is common for opioid detox, addicts do not have to remain on the medication into their recovery. Any addict’s recovery from opioid addiction should involve counseling as a minimum form of recovery support. Long-term treatment with naltrexone has been approved for opioid addiction since 1984 and has since been formulated in several administrations from a once-daily oral tablet to a once-monthly intramuscular injection. While the path to recovery from opioid addiction is personal, the difference between treatment with naltrexone and buprenorphine contains a significant factor. Naltrexone allows the brain to recover its natural balance and function and buprenorphine maintains the opioid-dependent brain function. Each person is unique and should pursue the recovery course that will be most effective. However, many recovering opioid addicts find that naltrexone treatment is a very effective tool in remaining abstinent from further opioid abuse, with commitment and external support from sources like healthy family members, counselors or therapists, and sober groups and sponsors. Naltrexone and buprenorphine are both viable and effective options for opioid addiction treatment, but each takes a very different approach; buprenorphine medication-assisted treatment provides a safer way to maintain opioids in the brain and naltrexone supports abstinence from opioids. No matter which route of recovery is determined to be best, support and commitment are required elements in a long-term and successful recovery.