Suboxone Treatment and Abuse Potential

 History of Suboxone

Suboxone was initially marketed by the British company Reckitt Benckiser as a pain reliever for chronic pain.

It proved to be very effective in small doses; however, because of its special mechanism of action, it did not produce as robust of a euphoria as other opioid medications and was believed to possess relatively less abuse liability.

The standard of care at that time to assist with recovery from heroin addiction was methadone, but methadone—itself a full opioid receptor agonist—also carried a risk of abuse and addiction. Researchers found Suboxone was also an excellent candidate for opioid replacement therapy(a drug that can be used to stabilize someone in physical withdrawal from opioid drugs as people attempt to quit using). Suboxone became an FDA approved treatment for opioid addiction in 2002.^1,2

The United States Drug Enforcement Agency lists Suboxone as a Schedule III drug, meaning that it is believed to have a moderate to low potential for dependence and can only be prescribed by a waivered physician approved by the DEA and the Substance Abuse and Mental Health Services Administration (SAMHSA) to provide office based buprenorphine treatment for opioid use disorder.²

How Suboxone Works

Suboxone’s combination formulation is particularly suited to treating addiction to opioids such as morphine, heroin, oxycodone, and other prescription painkillers. Two other medications, methadone and naltrexone, are also approved for use in treating opioid dependence; however, Suboxone is quite different than these drugs.¹

Suboxone is combination pharmaceutical that contains two drugs:^1,2,3

• Buprenorphine—a long-acting partial opioid agonist.
• Naloxone—an opioid receptor antagonist.

As a partial opioid agonist, buprenorphine binds to opioid receptors, but elicits less of an effect than would be experienced with full agonist drugs, such as oxycodone, morphine, or heroin. Thus:

• When people take Suboxone, they may experience some degree of standard opioid effects—such as pain relief—but not to the same extent as with a full opioid agonist.
• Buprenorphine can mitigate some withdrawal effects and cravings related to the narcotic drug without an associated, highly reinforcing euphoria.
• Buprenorphine has high-affinity opioid receptor binding properties and relatively long duration of action;² therefore, even if one took heroin after taking Suboxone, heroin would be competing with buprenorphine for a limited number of mu-opioid receptor binding sites while buprenorphine remains active.
• In addition, taking buprenorphine also results in what is commonly called a ceiling effect, such that if one continues to take more Suboxone, the effects will plateau.¹ One study showed that single doses of buprenorphine 70 times higher than the recommend pain relieving dose were well tolerated by nondependent subjects.⁴
• Taking additional Suboxone will not allow the person to get higher on the drug, potentially decreasing its abuse liability. The inherent effects ceiling also increases its safety profile by making it more difficult to overdose on Suboxone.¹

Naloxone is an opioid antagonist, meaning it binds to and prevents activation of opioid receptors. When Suboxone is taken as directed and dissolved under the tongue:

• The naloxone component is not well absorbed into the bloodstream of the person taking it.
• However, if an individual were to grind up or dissolve Suboxone in liquid and inject it into the bloodstream directly, the naloxone activity predominates—immediately locking on to the opioid receptors in the brain and knocking out any opioid drugs attached to the receptors.
• This will trigger an immediate opioid withdrawal syndrome (in people with physical dependence on opioid drugs) that will result in the person becoming ill.
• The addition of naloxone is designed to keep people from intentionally misusing Suboxone to get high.¹

Common Side Effects of Suboxone

Like other opioid pharmaceuticals, Suboxone has some known side effects, including:^1,5

• Hepatitis (especially with needle use).
• Liver damage.
• Respiratory depression and increased overdose risk (especially if used simultaneously with other respiratory depressing substances.^5,6

Other symptoms of  buprenorphine toxicity or overdose (particularly in connection with polysubstance use with alcohol, benzodiazepines, and other sedatives) include:⁵

• Profound sleepiness.
• Confusion.
• Slowed reflexes.
• Markedly uncoordinated movements.
• Blurred vision.
• Slurred speech.
• Respiratory depression.
• Loss of consciousness.

Can a Person Abuse or Become Addicted to Suboxone?

Despite a relatively lower abuse liability than many full opioid agonist drugs of abuse, there are reports of illegal sales of Suboxone on the street as well as a 500% increase in the number of emergency department visits related to Suboxone use between 2006 and 2011.² Numbers like these indicate that there could be an increasing trend, even if it is a minor trend, for Suboxone abuse. Even though Suboxone is formulated to deter abuse, the evidence suggests that Suboxone misuse does occur.

Evidence exists for the illicit diversion and misuse of buprenorphine and Suboxone. Even if initially obtained as a prescription, this is a form of abuse that also opens the door for mixing with other drugs, such as alcohol or benzodiazepines. In instances of polysubstance misuse, it appears that benzodiazepines are commonly used in conjunction with Suboxone— a combination that could prove quite dangerous as it increases the risks of respiratory depression related overdose, which can be fatal.^1,2

Other signs that someone might be abusing Suboxone include:

• Mixing Suboxone with other drugs such as alcohol.
• Loss of interest in regular activities.
• Dishonesty and secrecy regarding the person’s use of Suboxone.
• Sudden changes in mood.
• Taking larger doses of Suboxone or taking it more frequently than prescribed.
• Using Suboxone without having a prescription.
• Buying Suboxone illegally.
• Spending increasing amounts of time trying to get Suboxone.
• Declining academic or work performance.
• Negative consequences in personal relationships as a result of using Suboxone.
• Wanting to, but being unable to stop using the drug.
• Getting angry when people mention that use of the drug might be too frequent.
• Changes in physical appearance, such as being disheveled or changes in one’s grooming habits.
• Changes in one’s presentation, such as slurred speech, extremely slow patterns of thinking or responding, or significant memory issues.

Differentiating between Addiction and Physical Dependence

The terms addiction and dependence are often used interchangeably; however, there is a real distinction between having a physical dependence on a specific drug and being addicted to the drug.  Moreover, a great number of individuals develop a physical dependence to drugs they are taking for legitimate therapeutic. A person can develop a physical dependence on a particular medication but not manifest other compulsive patterns of misuse that characterize addiction.

Addiction refers to a chronic condition that is characterized by compulsive use of substances despite suffering negative consequences related to such use.

Even those who use Suboxone therapeutically will most likely develop some magnitude of physical dependence on the drug, depending on the amount taken and length of use; however, with its effects ceiling and abuse-deterrent inclusion of naloxone, it may be less likely to motivate diversion and compulsive misuse than other prescription opioid medications.^3,6

Withdrawal from Suboxone

If a person being treated with Suboxone demonstrates recurrent symptoms of withdrawal, it could suggest that the person is being inadequately managed with the medication or is misusing it. Under normal treatment conditions, an individual should not experience significant withdrawal symptoms. Skipped doses and/or injecting Suboxone may lead to the onset of acute opioid withdrawal.

The following physical effects can occur from withdrawal from Suboxone:⁵

• Anxiety.
• Cravings.
• Sweating.
• Chills.
• Vomiting.
• Diarrhea.
• Aches and pains.
• Muscle cramps.
• Insomnia.

Getting off Suboxone

There are specific concerns and issues regarding discontinuation of the drug, and anyone who is going to attempt to discontinue Suboxone use should do so under the supervision of a physician. A person should not try to discontinue the drug alone due to the potential withdrawal effects and other unforeseen medical issues that may arise, such as increased physical pain that was controlled by using the drug. Physicians are best equipped to handle these issues.

• Typically, a physician will initiate a medical detox procedure and taper the dose slowly so the person can adjust.
• Should discontinuation be prompted because of compulsive misuse, additional substance abuse treatment maybe warranted.
• As the person successfully begins a transition to living without the drug, support groups can be beneficial to help with long-term recovery.

In cases where Suboxone abuse occurs in conjunction with other substances, such as alcohol, other detox measures may need to be implemented, as the combined withdrawal syndrome may be additionally severe or complicated. A comprehensive medical detox ensures that the individual can safely withdraw from all substances of abuse.

Conclusions

Discontinuing Suboxone is similar to discontinuing other opioid drugs; however, there are some specific issues with Suboxone abuse that can complicate the situation. Substance abuse treatment can help people be successful in their efforts to discontinue using Suboxone, whether their use of the drug stems from attempts to discontinue other opiate drugs or whether their use of Suboxone itself represents a substance use disorder.

References

1. SAMHSA (2019). Buprenorphine.
2. DEA (2019). Buprenorphine.
3. Velander, J. (2019). Suboxone: Rationale, Science, Misconceptions. The Ochsner Journal, 18(1): 23-29.
4. Walsh, SL., Preston, KL, et al. (1994). Clinical Pharmacology of Buprenorphine Ceiling Effects at High Doses. Clinical Pharmacology and Therapeutics, 55(5):589-90.
5. Suboxone. (2019). What is Suboxone Film?
6. Whelan, P. & Remski, K. (2012). Buprenorphine vs methadone treatment: A review of evidence in both developed and developing worlds. Journal of Neurosciences in Rural Practice, 3(1):45-50.