Important note: Information in this article was accurate in 2005. The state of the art may have changed since the publication date.AIDS Community Research Initiative of America (ACRIA) - Spring 2005
Many heroin users who want to and are ready to stop using may not be aware that there is a pharmaceutical alternative to methadone that can help them achieve their goal. Buprenorphine, a drug that's a derivative of opium, was approved in 2002 by the Food and Drug Administration to treat opioid addiction. Injectable buprenorphine has been available for many years to help manage pain under the brand name Buprenex.
Buprenorphine for the treatment of opioid addiction comes in two formulations - Subutex, which contains only buprenorphine, and Suboxone, which is a combination product that includes both buprenorphine and naloxone, a drug that causes very quick opiate detoxification. Both formulations come in tablets that contain 2 or 8 mg of buprenorphine. Suboxone tablets also contain 0.5 or 2 mg of naxolone. The naloxone in Suboxone makes you experience withdrawal if you were to crush the tablets for injection. You put the tablets under your tongue, and they dissolve in a few minutes. Buprenorphine doesn't work if it's chewed or swallowed, which is a plus if you live with or are around children.
Buprenorphine blocks the effects of heroin and prevents both withdrawal symptoms and cravings. If you aren't a regular opioid user, buprenorphine gives you a minor high - much less than either heroin or methadone. If you use heroin while taking buprenorphine, you won't get the high that you'd normally expect. In fact, in high doses, buprenorphine is extremely unpleasant to take if you're on heroin, methadone, or another opiate because combining the drugs causes severe withdrawal symptoms.
Buprenorphine begins to work a half-hour to an hour after it's taken, and the effect lasts anywhere from one to three days, depending on the dose and the individual. The standard dose ranges from 4 to 32 mg/day. Starting doses might begin at 2-4 mg and are often stabilized at 12-24 mg a day.
Buprenorphine has what's called a "ceiling effect." Once you're taking a certain amount of the drug, higher doses don't produce a greater effect. Because of this, people aren't likely to need their dose increased above 32 mg. This makes it much more difficult to overdose on buprenorphine than on heroin, methadone, or other opiates. So, while buprenorphine works similarly to methadone, it is considered safer. It also has a much lower street value. Some people choose to switch from methadone to buprenorphine as maintenance therapy.
Buprenorphine has been widely used in other countries for many years. In France, for example, about 80,000 people have used it in primary care, resulting in a decrease in heroin overdose and an improvement in health and social function. A French study published in AIDS in 2000 found that individuals on buprenorphine maintenance were more likely to adhere to their HIV medications and were able to keep their viral loads low. While experience with buprenorphine in the U.S. is comparatively limited, studies and experience with buprenorphine in France and other countries suggest that it is safe and has a positive impact on HIV adherence and viral load suppression.
The initial side effects of buprenorphine are similar to those of other opiates and may include headache, nausea, vomiting and constipation, though if you are moving from heroin to buprenorphine you may have no side effects. When you start buprenorphine it is very important that you have been away from heroin, methadone and all other opioids long enough to be feeling moderate withdrawal symptoms - at least 8 hours with heroin and 24 or more hours with methadone. Otherwise you will be thrown abruptly into withdrawal and feel miserable.
HIV medications such as the protease inhibitors Norvir, Kaletra, Crixivan, Invirase, and Fortovase and the non-nucleoside Rescriptor may increase buprenorphine blood levels and, therefore, its effects. The other non-nucleosides, Sustiva and Viramune, may decrease buprenorphine levels. These particular interactions don't appear to be dangerous, but buprenorphine dose adjustments may be necessary. Other drugs that aren't specific to HIV may also interact with buprenorphine.
Several overdoses have been reported in France when buprenorphine was injected with a benzodiazepine like Xanax.
Unlike methadone, you don't have to go to a specialized clinic to receive buprenorphine. It can be prescribed by your doctor, provided that she or he has been certified through an eight-hour training and has a permit to administer buprenorphine. Each approved doctor in private practice and any facility with an approved doctor on site can provide buprenorphine to a maximum of 30 people - although there is lobbying to increase these limits. The availability of buprenorphine in an office setting may help integrate substance use treatment into primary care, helping people who are wary of the restrictive, infantilizing atmosphere of some methadone clinics take advantage of this option. However, many doctors in private practice don't have experience in addiction issues or the capability to provide supportive services for drug users.
If you're interested in exploring this option, talk to your healthcare provider to see if buprenorphine treatment is appropriate for you.
Donna M. Kaminski is Associate Director of Treatment Education at ACRIA.
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