TL;DR – Suboxone can block the effects of opioids for approximately 24 to 72 hours depending on the dose and individual factors.
Suboxone is a long-acting, combination opioid medication used to treat opioid use disorder or OUD. Approved for this purpose by the FDA in 2002, Suboxone is composed of buprenorphine, a semi-synthetic opioid and naloxone, a rescue drug used for opioid overdose.
Naloxone is better known by its trade name Narcan, and it’s included in Suboxone to discourage intravenous abuse of the buprenorphine. If someone tries to abuse Suboxone by dissolving it in water for injection, the naloxone becomes active and prevents any high from the buprenorphine. If the individual is also physically opioid-dependent, the naloxone will cause an instant, extremely unpleasant, full-blown opioid withdrawal syndrome.
Regular opioid users know better than to inject Suboxone. For this reason, the medication is considered to be abuse-deterrent.
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How is Suboxone Taken?
Neither naloxone nor buprenorphine are active by mouth. Naloxone must be injected or given nasally to be active. Buprenorphine must be taken sublingually. This means it’s placed under the tongue and allowed to dissolve. From there it passes readily through the oral tissues and into the bloodstream.
The naloxone in Suboxone will remain inactive as long as the user doesn’t inject it.
The buprenorphine in Suboxone is also an opioid blocker in itself. This is because it has a higher affinity (ability to attach to the brain’s opioid receptors) than other opioids. This means it will block other opioids from attaching to the brain’s opioid receptors, mainly the one known as the mu receptor, for as long as four days.
Advantages of Suboxone
When used in opioid recovery treatment, Suboxone offers several advantages:
- It prevents or blocks a high from other opioids, such as heroin
- It relieves opioid withdrawal symptoms and reduces drug cravings without causing a high of its own
- It’s long-acting and requires only one dose per day
- It doesn’t require a daily visit to a clinic and is taken in the privacy of one’s home
- Regarding possible overdose, Suboxone is much safer than methadone
Understanding How Suboxone Works:
Partial and Full Opioid Agonists
As a group, all opioids work similarly in the brain by binding to and activating some or all of the opioid receptors located there. These substances fit into the receptors like a key in a lock. Four of the opioid receptors are known as the mu or MOR, the kappa or KOR, the DOR or delta receptor, and the NOR, the nociception receptor. There is also a fifth identified opioid receptor called the ORL-1.
Although all five have roles in the opioid effect, it’s the MOR that mostly is responsible for the euphoria so prized by opioid users.
To really understand how Suboxone works, you must first understand the principles of affinity and full and partial agonism. Not all opioids work the same in the brain even though all are opioids. Some are full agonists, which means they activate the brain’s opioid receptors completely. Examples of these are morphine and codeine (both natural opiates), heroin, oxycodone, oxymorphone, hydrocodone, methadone and fentanyl. These are the ones that cause the most profound euphoria, sometimes known as a rush, are highly sedating and are the most likely to be involved in overdoses.
Other opioids are partial agonists. This means they can activate the brain’s opioid receptors as well but only to a degree. These tend to cause much less euphoria, if any, and are less likely to be involved in a fatal overdose. These opioids also have a ceiling effect. Full agonist opioids do not. This means that taking more of a partial agonist opioid after a certain dosage level will not result in more effects.
Examples of partial agonist opioids are buprenorphine, nalbuphine (Nubain), butorphanol (Stadol), tramadol (Ultram) and pentazocine (Talwin). Although partial agonists are safer than full agonists, they may not be effective enough to relieve more severe pain. This means they’re often not the best choice for pain control, but it also means they’re quite useful for MAT or medication assisted treatment.
Affinity refers to a drug’s relative power to attach to the opioid receptors in the brain. Buprenorphine has an extremely high affinity. Naloxone’s is even higher. When buprenorphine is present on the brain’s opioid receptors, there will be a blocking effect that can persist for as long as four days from the last dose. This is because only one molecule can occupy an opioid receptor at a time. As long as the buprenorphine is sitting on the receptor, no opioid with a lower affinity can kick it off. And, buprenorphine can sit there for a very long time. This is how it blocks other opioids.
Note: attempting to overcome a buprenorphine or methadone blockade is very dangerous. Some opioid users taking Suboxone, desperate for a high, will ingest or inject very large doses of full agonist opioids. Although it’s possible to overcome a blockade in this way, the risk of a lethal overdose is very high, especially with very strong opioids like fentanyl.
The long-acting superpower of buprenorphine lies in its half-life. A drug’s half-life is a measurement of how long it takes the body to break down and eliminate half the dose of a drug taken. The half-life of most opioids is typically just a few hours. Buprenorphine’s is a whopping 24 to 70 hours, with an average of 38 hours. That’s a day and a half minimum just to break down half the dose! Buprenorphine is perfectly capable of blocking opioid receptors for up to four days from a single dose. Of the opioids, only methadone (and related compounds) rivals that kind of long-acting power.
There is another group of opioids known as antagonists. These are drugs that have an extremely high affinity for the opioid receptors but do not have an effect of their own. They simply occupy the opioid receptor and prevent other opioids from binding there. Examples are naloxone and naltrexone (Vivitrol). These antagonists can also immediately and dramatically reverse an overdose even when a fatal opioid dose has been taken, if given in time.
Disadvantages of Suboxone
There’s no question that Suboxone is an effective form of MAT for the treatment of opioid use disorder. However, like all drugs, it’s not perfect. There are some disadvantages.
The waiting period
Unlike the full agonist methadone, Suboxone can’t be taken until a person is well into the opioid withdrawal phase. By this time, at least 24 hours after the last dose of a full agonist opioid like fentanyl, withdrawal symptoms have set in and become very hard to tolerate.
There is vomiting, restless leg syndrome, diarrhea, sweating, feeling hot and then cold or both at the same time, severe stomach pain, headache and backache, bone and muscle pain, weakness, insomnia and anxiety. It’s hard to wait through all that for long. It’s really a lot to ask. Some people can’t or won’t do it.
But, if Suboxone is taken too soon, the buprenorphine can cause precipitated withdrawal or PW. This is a rapid intensification of the opioid withdrawal syndrome and much worse than the naturally occurring one. Avoiding PW is why there’s a waiting period for the induction of Suboxone. Should PW occur, it may be managed with very high doses of buprenorphine, but PW is best avoided to begin with.
Suboxone is addictive
The buprenorphine in Suboxone is addictive. Many patients report great difficulty in stopping this drug. This is why you must tell your doctor when you want to stop Suboxone. You’ll need a slow tapering schedule. Getting off Suboxone will take time. It’s not a race. It’s all right to take many months or even a year to taper off and finally stop. Just be aware that without the help from buprenorphine, you may find it much harder to maintain sobriety. You’ll need a strong support system. However, it can be done.
In case you’re wondering, Suboxone, taken as directed, has a good safety profile even when used long-term. If you need the medication to help you stay sober, there’s nothing wrong with that. If your dose isn’t preventing withdrawal symptoms and cravings, tell your doctor. It can be adjusted. Just don’t increase the dose on your own.
Live Free Recovery Services
When opioids are taken daily for any length of time exceeding a few weeks or so, sometimes less, changes in brain function occur. It’s these changes that make opioids so hard to quit. At this point, willpower is unlikely to be enough. This is the time to seek professional help. Most people will need this help to stop abusing opioids. You’re not alone. Help is closer than you think. Our counselors are available to take your call and discuss your individual treatment options with you. We work with you to get your life back on track for a happy drug-free future.