Facts about Buprenorphine (Suboxone®) • In NZ buprenorphine is only available in Suboxone® which also contains naloxone. Some of the info here is relevant to buprenorphine (whether it contains naloxone or not) and some to Suboxone® specifically, hence the use of both terms. • Buprenorphine is a class C4 controlled drug used for short‐term opioid withdrawal/ detoxification or as an alternative to methadone for opioid substitution treatment. • Naloxone is the drug used to bring people out of overdose (in other words, Narcan). It's been added to buprenorphine to deter people from injecting. The naloxone has no effect when Suboxone® is used sublingually (under the tongue), but if injected the naloxone can put you into withdrawal. • Drugs that activate receptors in the brain are called agonists. Buprenorphine is a partial agonist meaning it binds to the opioid receptors but doesn't activate them as much as full agonists like methadone, heroin and morphine. • This produces what’s called a ‘ceiling effect’ in that after a certain dose the drug produces no more effect, but the effect it does produce lasts longer. • Buprenorphine also binds to the receptors more avidly than other opioids. If there are opioids already on the brain’s receptors, buprenorphine will 'kick them off' and bind in preference. • This is why it's so important that you are in moderate withdrawal before your first dose of Suboxone®. If you still have a significant amount of opioids in your system that are then kicked off and replaced by the buprenorphine, you'll feel the rapid loss of the opioid effect i.e. withdrawal. This is known as 'precipitated withdrawal' ‐ the rapid and intense onset of withdrawal symptoms caused by the medication. • Buprenorphine's ability to bind to the receptors means using other opioids on top won’t have the desired effect. • As with methadone, you do become dependent on buprenorphine. A missed dose on daily dispensing should not cause any substantial withdrawal symptoms because of the long lasting effect of buprenorphine though people on low doses may become uncomfortable. • Suboxone® currently comes as a lemon‐lime flavoured tablet in two dosages: 2 mg and 8 mg. You place the tablet under your tongue until it is Revision 00 December 2011 dissolved ‐ this can take 2 – 10 minutes. It will not have any effect if you swallow it. • The effects come on within 30 ‐ 60 minutes and the full effects after 1 ‐ 4 hours. The duration of effects varies according to the dose and the person taking it. In general, the higher the dose, the longer the effects. • As yet there’s little research available about pregnancy and Suboxone®. If you become pregnant whilst on Suboxone®, you’ll probably be transferred to methadone. (Suboxone® isn't registered for use in pregnancy in NZ.) Benefits of buprenorphine • It provides an alternative for people who experience intolerable effects from methadone or have adverse side effects including methadone‐ related Torsade de Pointes (heart arrhythmia). • Induction onto buprenorphine is more rapid than onto methadone. • It is safer than methadone in accidental poisonings (e.g. if taken by a child) because it is not active if swallowed and it has a ceiling effect on breathing rate. (However if a child does take buprenorphine this is still an emergency and medical help should be sought). How buprenorphine differs from methadone • Like methadone, buprenorphine is designed to stop withdrawals and reduce the craving to use but for some people it has some possible advantages such as: • A feeling of being more clear‐headed, less ‘cloudy’ than with methadone (though not everyone likes that clear‐headed feeling). • Buprenorphine is said to cause less sweating, constipation and sedation than methadone, but severe headaches are occasionally reported and moderate headaches are common during the first few days of induction. • Taking large doses of methadone can cause and has caused deaths; taking large doses of buprenorphine is much less likely to cause overdose and possible death if it’s the only thing you’re taking. However if you try to override the blockade effect by using higher doses of opiates then the risk of overdose is significantly increased. When the buprenorphine wears off, the effects of the other drugs kick in. 058.047 Page 1 of 2 • It doesn't have to be taken daily when used for ongoing treatment. • Loss of appetite • Nausea and vomiting (which usually stop after a few days) • Buprenorphine may have advantages over methadone when used for withdrawal Research has shown that people may be more likely to complete a detox if buprenorphine is used rather than methadone. Anecdotal reports from CADS clients who have previously used both buprenorphine and methadone to withdraw from opiates are that most prefer Suboxone® for withdrawal, though warn of post‐ withdrawal symptoms. • People experiencing significant side effects from Suboxone® may need to transfer to an alternative medication. Potential risks of buprenorphine Pain management • Buprenorphine interacts with other central nervous systems depressants including alcohol, benzos (Valium/diazepam, temazepam, Rohypnol, etc), antidepressants, and antipsychotics (mental health medications), so you need to tell the prescriber if you’re taking any of these. • Respiratory depression can occur if buprenorphine is combined with these depressants. There have been reported deaths of people who’ve injected buprenorphine and taken benzos. The risk of overdose is the same whether you're mixing methadone and other drugs, or buprenorphine with other drugs. • Suboxone® isn't designed for injecting which can be painful and can cause tissue and vein damage and blood clots (deep vein thrombosis). • Injecting buprenorphine that's been in someone's mouth (even if it's your own) can result in fungal endophthalmitis – an infection forms INSIDE the eye. This is a big deal, as the internal eye is mostly filled with fluid, and quickly turns into a giant abscess. Plus, the retina is a sensitive structure and can get damaged easily. • If you feel drowsy on buprenorphine it’s safest not to drive or operate machinery. Possible side effects Buprenorphine has a range of side effects similar to those of all opioids. Most side effects occur early in treatment, are mild and subside with time. They appear to be generally unrelated to buprenorphine dose, however nausea is more common with doses over eight milligrams, and dizziness occurs more commonly at high doses. • The most commonly reported side effects are: • Headaches which are very common early in treatment but usually settle down in a few days • Constipation • Abdominal pain (cramps) which usually settle down quickly • Skin rashes and itching (which usually stop after a few days) • You should carry an information card for emergency medical personnel telling them you are on Suboxone® because it changes the pain relief treatment options available to you. You'll receive one of these cards from CADS. • The blockade effect (especially at higher buprenorphine doses) means usual opioid pain‐relief medications such as morphine may not provide the same effect or relief. • If you end up in hospital unexpectedly and need pain relief, get the hospital staff to contact your prescriber who can provide the GP or hospital staff with guidance on pain management. • People requiring analgesia (pain relief) should preferably use non‐opioid analgesics such as paracetamol, aspirin, and NSAIDs/non‐steroidals Voltaren (diclofenac) and Nurofen (ibuprofen), as opioid medications are less effective. Speak to the doctor about other options for severe pain. • Hospitals may not stock Suboxone® so if you have any planned hospital admissions it’s important to tell your nurse, doctor or key worker so they can help arrange your medication for you. Effectiveness Buprenorphine has proven to be a safe medication, effective in keeping people in treatment and in preventing the use of illicit opiates, though not more effective than methadone. The differences in treatment outcomes for people using buprenorphine as compared to people using methadone are small. Please note: Suboxone® is not subsidised by Pharmac so people have to pay for it themselves. The cost can vary between pharmacies. A short‐term detox will cost at least $40; ongoing treatment will of course cost more. • Sleep problems (difficulty falling asleep and disturbed sleep) References: Ministry of Health. 2010. New Zealand Clinical Guidelines for the Use of Buprenorphine (with or without Naloxone) in the Treatment of Opioid Dependence. Wellington: Ministry of Health. • Tiredness or drowsiness (especially after a dose) which usually stops within days to weeks Verster Annette and Ernst Buning. 2005. Buprenorphine: Critical Questions Examined. Euro‐Methwork. The Netherlands. • Mood swings Revision 00 December 2011 058.047 Page 2 of 2