Subutex

High Dose Buprenorphine

Most BP readers will already know a bit about Buprenorphine, probably in its guise as the drug contained in Temgesic™ - that little analgesic all the Scots rave about! However, Subutex is not the same. It is made up of higher doses of buprenorphine (0.4, 2 and 8mg), compared to Temgesic (0.2mg). The concept of using a higher dosage of buprenorphine as a form of drug treatment (substitution therapy) for people dependent on opiates has proved very encouraging in studies held throughout the US and Europe and quite a few people in the UK have already started treatment on Subutex. In France it is the main form of substitution therapy, with 75 000 people being prescribed Subutex as opposed to just 9 000 prescribed Methadone.

But Subutex has some particular qualities, which may not make it suitable for some of us but could prove just the thing for others. As the French users have found out with Subutex and the British users with Methadone, to assume all drug users needs are the same just because they use opiates and so prescribe one drug almost exclusively, is a mistake - and it is the drug users that ultimately pay. So, aside from useless Government drug policies, we should applaud the continuation of research for new substitution treatments and Subutex will undoubtedly prove a help to many.
So, What is it and What Does it Do?

Buprenorphine was discovered in1968 and by 1978, it was shown a potentially useful substitution agent for those opiate dependent. It is a semi-synthetic opioid molecule, which is derived from one of opium's components - Thebaine. It resembles morphine but it acts as a partial agonist. Now, to fully understand this, we need to take a small detour into the world of agonists, partial agonists, and antagonists.

All opiates are catagorised according to the way they interact and bind with specific receptor subtypes in your brain. The main opioid receptors are designated the symbols µ, s, d, andk but it is the µ receptor that concerns us here. The µ receptor is believed to be responsible for most of the analgesic or pain relieving effects (including euphoria) of opiates. Now the opiates or opioids that appear to have an affinity with for the µ receptor can be divided into 3 main classes.

A full agonist like heroin, methadone or morphine, binds to your µ receptor producing such effects as euphoria and pain relief. An antagonist on the other hand like naloxone or naltraxone, will also bind to the µ receptor with at least the same strength as an agonist but they have no actual activity and so produce minimal effects. But, they can displace or push out any agonists that have already bound to the receptor, which literally means, any opiates found will be ditched and replaced by the antagonist. This is why drugs like naltrexone can set you off into instant withdrawals and any additional opiates you use will have no effect (gross maybe but handy when you overdose on an opiate or need naltraxone detox treatment!).
On the other hand, a partial agonist like buprenorphine can exhibit both agonist and antagonist properties. Once buprenorphine binds to your µ receptor, it will produce some euphoric effects. However, once bound it will also stop the action of any subsequently administered opiate, so if you use (opiates) on top, it won't work. Although buprenorphine also displaces any opiates you may have in your system (like an antagonist), the subsequent withdrawal effects are far less severe than may be the case with a full agonist like naltraxone.

As a Substitution Therapy?

Most UK users are on Methadone. This has been prescribed as a blanket treatment for all drug users with an opiate problem and sadly, or rather obviously, it is not going to work for everyone. Subutex is definitely a treatment worth considering but it will only really suit particular needs. You really ought to understand the drug itself and to analyze what you really want out of a substitution treatment. With Subutex, you'd be wise to ask yourself (continued) whether you really want to come off gear permanently or are you are looking for a drug to keep you from being sick while you still use here and there. If you are ready to stop using all opiates, need a bit of incentive and are ready to do it now, then Subutex might just be the thing. One thing worth mentioning though is that Subutex will not stop the effects of other drugs and, as has been the case in France, many users have turned to benzos and alcohol and crack in order to still get a buzz. That can be a messy road to go down so consider your options.

Choosing Subutex

Buprenorphine is taken under the tongue (sublingual) and takes up to 10 minutes to be absorbed (peaking within 1-1.5 hours). Because of the withdrawal effects that can be induced by taking Subutex, it is not recommended to jump off a high dose of methadone onto Subutex. The usual procedure is to try and reduce your methadone to around 30 - 40mg (less if you can) and then make the changeover. You still may experience some 'discomfort' (- Drs famous last words) but with a reasonable dose of buprenorphine, you should start to feel better quite quickly. Coming off shorter acting drugs like heroin or morphine onto Subutex is much less traumatic however with little or even no withdrawals but it is still wise to get your dose down as low as possible. It is an opiate so it will make you feel better if you're hanging out and a dose of Subutex greater than 8mg will stop the effects of heroin altogether.

The effects of an 8-32mg Subutex tablet is considered roughly equal to approx 60mg methadone. The usual doses given out are between 24mg - 32mg and these doses appear to have a longer duration than methadone - lasting up to 48 hours after administration. This is great news for those of us who don't relish the long trek to the clinic/chemist everyday.

Once stabilised on Subutex it should entail a much less strict regime than most methadone programmes which has got to be good news! The really interesting thing about Subutex is that it can be a much easier way off coming off opiates. If you are on methadone or have a habit on other opiates, once you manage the changeover to Subutex it can be one of the better options when coming off the opiates altogether. Methadone is famous for its difficult withdrawals (although it can be done very carefully) and we all know how hard heroin can be. But coming off Subutex/buprenorphine, the withdrawals are considered relatively mild so this may make it a good option for those detoxing.

High dose buprenorphine can be used as both a withdrawal and a maintenance treatment and has benefits with its alternate day dosing. It is less addictive and less likely

to trigger fatal overdoses because it does not suppress breathing as much as heroin or methadone. If you are on methadone and still use heroin then Subutex is probably not the best option. Fiddling about with heroin so that Subutex doesn't make you hang out can be very complicated and really isn't worth the hassle. But if you are ready to give up the opiates, need a little incentive, and don't think you will end up supplementing with benzos etc, then buprenorphine/Subutex could be a good option for you.

NOTE: As of 1998, buprenorphine was not recommended for pregnant women although there has been studies done to suggest withdrawal effects on the baby are less than those of methadone. Please check this out with a specialist doctor experienced in buprenorphine drug therapy or ring us at Black Poppy and we will do some investigating for you.

Available on the NHS and cost around £20 for a pack of 7x 8mg tablets. Legal category: POM Further information available from Schering-Plough. All references available from Black Poppy 0208 968 3452

The Pro's
Easier to withdraw from than other opiates.
Provides an incentive to stop using opiates because other opiates won't work.
No more methadone!
Attending the clinic less often as dosage can last up to 48 hours.
More room for self-dosing (for those poor folk on supervised consumption)
Stops withdrawals
Safer than methadone, respiratory failure on Subutex alone is rare.
Minimal euphoric effects compared to methadone so you won't feel that haze some of us do.
8-32mg Subutex produces a ceiling effect

The Cons
Doesn't help with the psychological aspects of using
If you're already on methadone you need to reduce your dose (to approx 30-40mg) before transferring to Subutex
If you use opiates on top of Subutex, they won't work.
May lead to increased usage of benzos, alcohol, or crack in search of a buzz.
Will cause withdrawals
If you have an accident and need pain relief you may not be able to have an opiate-based painkiller or an opiate antagonist may be used first. (others painkilling methods are available).
Unwise to take Subutex with alcohol, medications containing alcohol and use cautiously with other central nervous system depressants.

SIDE EFFECTS: Frequently noted; - Constipation, headaches, insomnia, sweating, nausea, fainting, dizziness hepatic necrosis (if you have problems with your liver be sure to raise this with, preferably, your liver doctor. Depression has also been noted.