Alexander DeLuca, M.D.
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Buprenorphine for Combined Pain and Heroin Dependence

Alexander DeLuca, M.D., FASAM;  8/4/2001. Revisions as noted: 8/20/2003. Last minor edits & formatting: 2/22/2005. 
[Identifier: www.doctordeluca.com/Library/PsychoPharm/BuprenorphineGeneralComments.htm]
 
See also:
Office-Based Opiate Detoxification - An Open Letter to the FDA - DeLuca; 1998

[Print version]

Buprenorphine, formulated as ampoules containing 0.3 mg/cc (Buprenex), is approved for the treatment of moderate to severe pain. It is a partial agonist, and has a ceiling effect, so overdose is virtually impossible. It is, in my experience with 4 chronic pain patients who were also heroin addicts, THE drug of choice for this combination of problems. It must be used primarily for the treatment of pain; with secondary benefits to the pain patient/heroin addict of total relief from craving and decreased salience of heroin, makes it a truly wonderful medication.

[START: paragraph added 8/20/2003]

The pain/addict patients I treated with buprenorphine (n = 4) were all young, otherwise well, either working or students, who were finding their heroin use an intolerable financial and time drain, and who desperately wanted to stop using heroin, and who could not afford either the time or expense of inpatient treatment. They were all able to discontinue heroin use without discomfort on relatively low doses (see below) that also provided excellent analgesia. They expressed that they particularly liked buprenorphine because they felt "clear and alert" (these words used by several patients independently) with no "warm fuzzy" periods that they had experienced with methadone in the past. Finally, buprenorphine seems to produce a decreased salience for heroin - patients find themselves, quite suddenly, strikingly less interested in heroin and it's accompanying behavior and paraphernalia. This latter effect was highly appreciated and valued by my pain/dependence patients.
[END: paragraph added 8/20/2003]

In my (admittedly limited) experience, heroin dependent patients respond to  "pain" doses, generally in the range of 4-6 amps (1.2 - 1.8 mg/day) and experienced complete relief from craving and good analgesia. In the coming OBOT (Office Based Opioid Treatment) initiative, I think the smallest dose pill is 2 mg with a target of 8-16 mg (= 53 amps!!!) daily. Why it is felt such high doses are needed in heroin addicts I am not sure. Perhaps at those doses it is  a complete heroin blocker. One of my patients used heroin on top of his  4 amps per day and did "feel it" but the high was very attenuated and he really wasn't very interested in continuing to use and hasn't.

Buprenorphine can be used for detox in a number of interesting ways and induction can be very simple. It is easiest if the patient presents in withdrawal, but you can use this method even if if they have used recently. Start injecting buprenorphine IV, and it will induce withdrawal, but just keep pushing the buprenorphine and the patient passes quickly through the induced withdrawal and becomes suddenly comfortable. In a patient with chronic pain and heroin dependence, the dose required to produce comfort becomes the initial daily dose which is adjusted over several weeks to achieve optimal analgesia. If you were in an inpatient detoxification setting without concomitant chronic pain, this dose would represent the initial dose of an impending taper.

Buprenorphine withdrawal is usually relatively mild, so once stabilized, you can rapidly taper it to nothing, give  clonidine and valium if necessary for a few days, then induce them onto naltrexone maintenance as follows:

1. Preload with 0.2 of clonidine sublingually and 10mg of valium by mouth;

2. 60 - 90 minutes later administer 12.5 mg of naltrexone by mouth;

3. Cover any induced withdrawal with clonidine and valium;
 

4. Proceed to 25mg naltrexone the next day and 50mg on the next; and,
 

5. You're done!!

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Buprenorphine is not currently approve for use as a detoxification or substance abuse treatment agent, though its use for this purpose is taught in addiction medicine conferences, and it is rational. Dr. Maslansky (NY Hosp?) who has an OBOT clinic set up under research auspices has told me that he has been permitted to use buprenorphine only for detoxification to abstinence without naltrexone induction and maintenance, and that the relapse rate is tremendous under this mandated protocol. CSAT has approved OBOT, I believe, and we are now all awaiting approval from the FDA for approval of a pill formulation for sublingual or oral use.

Sublingual dosing using Buprenex  (ampoules) works fine. It is a bit unwieldy to hold three or more cc's in your mouth waiting for it to be absorbed, but patients tend to build a morning and evening ritual around it. You lose some effect relative to the parenteral route of administration, I think it's about 85% absorbed sublingually, but the doses are so low, who cares?  I suppose that if you were particularly upset by the thought of parenteral use, you could give the patient a 3 cc syringe and a large bore point to rule out anything but femoral IV injection and making IM injection painful. But most patients prefer the sublingual route - they are, after all, trying to get away from injecting and again, the "decreased salience effect" is a real feature of the drug, in my experience, as it often is with naltrexone.

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