Suboxone was designed to treat dependence and addiction to opioid drugs or narcotic drugs, including heroin, morphine, oxycodone, and drugs in this class. Other drugs like methadone used for opioid replacement therapy are more addictive than Suboxone and do not share its dual action.
Unlike other common drugs used for opioid replacement therapy; Suboxone combines the effects of two drugs into one medication. The two drugs are:
- Buprenorphine, the primary ingredient, is a partial opioid agonist.
- Naloxone, the secondary ingredient, is an opioid antagonist or opioid blocker.
Buprenorphine and Naloxone Combine to Fight Addiction and Dependence
According to Stahl’s Essential Psychopharmacology, partial opioid agonists (e.g., buprenorphine) produce an effect that is not as strong as their full opioid agonist counterparts produce (e.g., heroin and related drugs); however, partial opioid agonists bind to the same receptor sites as full opioid agonists do. So taking buprenorphine:
- Results in feeling similar sensations of pain relief or euphoria, but not to the same extent as one would experience with the use of a full opioid agonist
- Ends up tricking brain into experiencing the effect that a full opioid agonists, such as heroin, would produce as it locks right onto the same receptors in the brain that its full opioid agonist counterparts would occupy, allowing it to suppress both the cravings and withdrawal symptoms associated with the full opioid agonist if it is discontinued (see below)
- Protects against the effects of someone actually taking a full opioid agonist, such as heroin, following the administration of Suboxone because the buprenorphine is long-acting and binds to the receptor for nearly 24 hours; thus, taking any other narcotic drugs, such as morphine or heroin, would not produce any effects as these drugs now cannot bind onto those receptors
- Discourages abuse; ceiling effects for Suboxone indicate that once the Suboxone fully occupies the receptor sites, taking additional Suboxone does absolutely nothing (the person cannot experience getting higher from taking more Suboxone)
- Protects against overdose; ceiling effects also protect against the possibility of overdosing on Suboxone
The additional component of naloxone is designed to prevent abuse of Suboxone.
An opioid antagonist like naloxone fits perfectly onto the receptor sites for neurons that are sensitive to the effects of opioid drugs. Taking Suboxone as prescribed (in a tablet form that allows one to dissolve it under the tongue) results in the naloxone not being activated at all, and it does not enter the bloodstream at all. But if someone were to try to use the drug in a manner that is consistent with substance abuse, such as injecting it or grinding up into powder in an attempt to snort it, then the drug is activated. In this instance, it will knock out any existing drugs that are attached to the opioid receptors in the brain and lock onto those receptors, and immediately trigger an opioid withdrawal syndrome (see below) that will result in the person becoming extremely ill
The half-life for buprenorphine ranges from 24 to 42 hours, whereas the half-life for naloxone is reported to range from 2 to 12 hours.
Even though Suboxone is designed to be a drug that helps with recovery from opioid use and helps to treat addiction, it does have a potential for abuse and addiction itself, although this potential is much less than with full opioid agonists. According to the United States Drug Enforcement Agency Suboxone is rated in the Schedule III class, indicating that it has a moderate to low addiction potential and that it can only be legally obtained with a prescription.
As Suboxone is designed to deal with both substance use disorders and physical dependence, it is important to clarify how these terms differ and how they are related.
Physical Dependence vs. Addiction
The terms dependence and addiction are still often used to mean the same thing; however, the two terms do have different connotations. Addiction can occur with or without the presence of a physical dependence on the drug. Likewise, a person can develop a physical dependence on medication and not qualify for the diagnostic criteria of an addiction (now referred to as a substance use disorder).
Physical dependence is defined by having the presence of both tolerance and withdrawal. Tolerance refers to the notion that often occurs when a person takes a drug over a period of time. Taking a drug for any significant length of time offer results in the person needing a higher dose of the drug to get the same effects that they use to get at lower doses. Withdrawal is the result of either stopping the drug abruptly or significantly lowering the dosage. Withdrawal occurs when a person experiences a series of upsetting symptoms as a result of stopping the drug or lowering the dose significantly.
The presence of both tolerance and withdraw indicate that the person has developed a physical need to continue to take the drug in order to function normally. This need may not necessarily be a bad thing. Many people take narcotic pain medications to control serious chronic pain for a great many years. Just by taking these medications over that period of time, the person develops a physical dependence on the drug. However, the person may not be abusing the drug but instead taking the drug in order to function normally and taking it with medical supervision. Thus, while the person is physically dependent on the drug, by clinical standards the person is not addicted to the drug or does not have a substance use disorder.
Addiction refers to a disorder where the person engages in nonmedical use of the drug that results in a series of negative consequences. The person’s use of the drug is often compulsive, or the person is unable to control use and the consequences for using the drug affects life in a negative manner, such as via health problems, relationship problems, social problems, problems at work, legal problems, and so forth. Addiction may or may not include the symptoms of tolerance and withdrawal.
Thus, it is important to remember that everyone who uses Suboxone will most likely develop at least a low level physical dependence on the drug, depending on the amount taken and length of use; however, due to the chemical makeup of Suboxone becoming seriously addicted to it is rare. Suboxone abuse does, however, occur, and individuals abusing the drug may be subject to experiencing withdrawal symptoms as well.
Whether or not someone is coming off Suboxone due to abusing the drug or as a result of using the drug therapeutically for opioid addiction, the person will experience a physical withdrawal syndrome due to the properties of the buprenorphine in the drug.
Suboxone Withdrawal Timeline
If one were to immediately discontinue using Suboxone, withdrawal symptoms most likely would not occur immediately. This is because Suboxone has a relatively long half-life of about 36 hours, and withdrawal symptoms would not really kick in until the drug was out of the person’s system. The following scenario is based on the timeframe following the person’s last dose of Suboxone:
First 24-72 Hours: Withdrawal from buprenorphine (there is no withdrawal from naloxone) will be most intense in this time period and will peak in its intensity at around 72 hours since the last dose (however, individual differences may make this peak period shorter or longer). The symptoms most common during this phase include:
- Watery eyes
- Dilated pupils
Week 1: In the first week following discontinuation of Suboxone, people will often continue to feel joint pain, cramps, insomnia, mood swings, transient anxiety, malaise, and just all-around feelings of being uncomfortable and restless.
Week 2: During the second week, the physical pain and discomfort that were experienced in the acute withdrawal phase will typically abate; however, issues with depression, restlessness, and an overall loss of motivation may increase.
Weeks 3-4: By this time, the physical symptoms of withdrawal should be gone, but many people still experience feelings of depression, general malaise, restlessness, lack of motivation, and cravings for the drug.
For many, the early withdrawal symptoms are similar to a bad case of the flu. The acute symptoms usually peak within a few days as mentioned above; however, some people experienced prolonged psychological symptoms that can include things like:
- Mood swings, including depression
- Cravings for the drug
Withdrawal from Suboxone and other opioid drugs is not life-threatening; however, it certainly may feel that way to the individual. The longer withdrawal symptom profile occurring after a few short weeks is sometimes referred to as post-acute withdrawal syndrome (PAWS). Differences in individual psychological makeup, experience, and physiology are likely responsible for the length of PAWS. This syndrome can last for weeks to months, or even longer in some individuals, and can represent a period of extreme vulnerability to relapse for many.
Moreover, changes in the brain pathways that have occurred as a result of opioid addiction remain and render the individual vulnerable to relapse in the future. Unsupervised use of opioid drugs (even use supervised by a physician) by a person who used to struggle with opioid addiction can quickly result into a full-blown addiction that may even be worse than the original addiction. Therefore, if these individuals need to use narcotic medications for pain control or some other reason, usage must be closely supervised.
How to Get off the Drug
Discontinuing Suboxone is not much different than discontinuing any other opioid drug. There are specific concerns and issues regarding stopping the drug. 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. When an individual has a very low dosage of daily intake (e.g., 2 mg per day), the physician will generally withdraw the drug. During the detox/tapering portion, individuals should also begin therapy for substance use disorders. Once off Suboxone completely, individuals should continue to attend support groups or participate in another form of aftercare.
Some additional considerations are in order for anyone attempting to withdraw from Suboxone:
- Become educated regarding the withdrawal process.
- Maintain a balanced diet, eating nutritious foods and avoiding fatty foods, sugar, and starchy foods.
- Keep a regular sleep schedule and get plenty of sleep.
- Stay busy and aim to be productive.
- Keep social contacts available. Stay in contact with family and friends. Social support can be a major factor in getting off any type of drug or overcoming abuse or addiction issues.
- Ask for help when you need it. Many people want to maintain an air of toughness or independence; however, this is no time for one’s ego to get in the way of the recovery process.
- Stay patient and focused. It will take time to get through the withdrawal and treatment process.
- Get regular exercise.
- Some people find that learning to meditate helps them through the withdrawal process.
Suboxone withdrawal is similar to withdrawal from other opioid drugs. Thus, discontinuing Suboxone use is also similar to discontinuing the use of other narcotic drugs. Individuals who educate themselves about the process, receive support and understanding, and are prepared for issues with withdrawal can be successful in their efforts to discontinue using Suboxone.