The Suboxone Ceiling Effect - Why Some People Need Methadone
Suboxone (buprenorphine) is a pretty great new drug, and for a lot of people, it's just a far preferable alternative to methadone and especially to naltrexone. When suboxone works well, withdrawal pains are largely avoided, and the eventual detox off of Suboxone is considered far less painful than for methadone.
Clients not seeking to taper off opiates at all are also well served by Suboxone, and it can work just like methadone as a drug for years of pain free opioid maintenance.
But Suboxone is not for everyone. Some people, especially people coming off of heavy use of short acting pain pills such as Oxycontin or hydrocodone, or heavy use of illicit opiates such as heroin – may find that even high doses of Suboxone do not offer them the replacement effects they need. For some people, even maximum doses won't keep withdrawal pains away – and that is because of the ceiling effect of the drug.
The Ceiling Effect
To understand why suboxone will work well for some people and not for others, it is helpful to understand the terms opiate agonist, opiate antagonist and partial opiate agonist.
All opiates work their magic in the brain by binding to neural receptors called opioid receptors. These receptors can be thought of as key holes, and drugs such as heroin (or any opiates) can be thought of as keys. When heroin floods the brain – these "keys" enter the receptors "the keyholes" and turn them on. Once these receptors are activated – all of the effects of the opiate are unleashed – and the user will feel euphoria, analgesia, etc. Basically, turning the key gets you high.
Drugs that activate these opiate receptors are called "Opiate Agonists". Opiate Agonists are straight forward keys for the keyholes.
Examples of opiate agonists include:
Opiate antagonists are sort of like broken keys for those opioid receptors in the brain. They fit in the opioid receptors but they do not turn them on – And significantly, while they sit in the receptor keyhole slots, other opioids cannot get in these keyholes to turn them on.
Opiate Antagonists include drugs such as Naloxone or Naltrexone, and they are used to help people overcome opiate addictions. When a person takes Naltrexone, for example, even if she were to take heroin afterwards, she would not get high. All of her opioid receptors would be filled with the opiate antagonist drug.
Partial Opiate Agonists
Suboxone belongs to a third class of drugs, called the partial agonists.
These partial agonists are "keys" very much like the agonists, and they do fit in the receptors and turn them on. They are called partial agonists, however, as they can only turn these receptors on partially.
Suboxone for example, will fit the opiate receptor key holes and will turn these on a little bit, producing some typical opiate effects and sensations. It is only a partial agonist though, as it has a fairly low ceiling – that is, at a certain point, taking more of the drug will not increase the effects felt. It can only turn the keys a small amount and once you fill all the key-holes, taking more of the drug won’t increase the effects.
Why is the Ceiling Effect Important?
The ceiling effect of Suboxone increases the safety of the medication but limits who will be able to use it.
The ceiling effect is good in some ways. It makes Suboxone less likely abused and far less easy to O.D. on – and because of this, Suboxone can usually be taken home, saving the client from regular or even daily trips to the methadone clinic.
The ceiling effect of Suboxone holds true for all effects – that is, after a certain point, taking more of the medication won’t increase any of the effects of the drug. Taking a higher dosage of Suboxone won't result in much intoxication, but it also won’t cause much risk of respiratory depression and possible overdose death.
After the Suboxone ceiling of effect has been reached – taking more Suboxone has no effect – it won't make you higher, and it also won't keep slowing your breathing like heroin or other opiates would.
But The Ceiling Limits its Use
Because of the ceiling effect, people with heavy opiate habits may not get enough out of Suboxone to keep withdrawal pains away.
Suboxone has "High Affinity" for opiate receptors. If you were, for example, to take high doses of heroin and Suboxone at the same time – the Suboxone would fill the opiate receptor "keyholes" and the heroin would have nowhere to go, and thus could not get you high. Suboxone has a higher affinity for the opiate receptors than other opiates do, and will win the fight to fill those key holes.
People with trying to overcome heavy drug habits may need more opiate receptor activation than Suboxone can give them – they may need a drug that can turn those opiate keyholes a little further just to keep the feelings of withdrawal away.
Unfortunately, if a person that wasn't getting enough relief from Suboxone tried to take another opiate at the same time – to get rid of their withdrawal pains, the Suboxone would be filling all of the opiate receptor "key-holes" and any additional opiates would have no effect.
If you had a heavy heroin habit and took some Suboxone – and still found that you were feeling withdrawal pains – taking more heroin at that point to chase those pains away would not work. The heroin would have no place in the brain to activate – all the keyholes would be filled with Suboxone.
Some People Will Probably Need Methadone
Most people prefer Suboxone to Methadone, but some people will not find the relief they need from suboxone, and will have to at least start off on Methadone.
Methadone has no ceiling effect. If you take more methadone you get a proportionally greater affect in the body. People that need more symptoms relief can take a slightly higher dose of methadone and find what they need.
In general, anyone needing more than 40mg of methadone daily will not find Suboxone effective.