Suboxone (Buprenorphine)

This page does not begin by offering any featured reading on this subject. The subject is Suboxone®, the first legal opioid substitution treatment available by prescription without attachment to a special clinic since the passage of the earliest anti-narcotics laws (e.g., the Harrison act). The Suboxone® product is actually just a sublingual formulation of an extremely high dose of buprenorphine, a partial-agonist opioid available in the U.S., at far lower does, as an injectable analgesic, which goes by the brand name Buprenex®, and is also available in generic form. The Suboxone® product is formulated for sublingual administration and is combined with the pure opioid antagonist naloxone, in an attempt to deter intravenous misuse of the product: sublingually absorbed naloxone is without signficant effect, but if it is injected, it will cause an immediate and extremely intense withdrawal reaction in opioid-dependent persons. Suboxone is available in tablets of 2 mg and 8 mg, and the effective dosage generally ranges from 8

mg to 32 mg per day. Because buprenorphine is a partial μ-agonist, is shows a ceiling effect: even at maximum receptor occupation, it will not produce the same intensity of effect that a full agonist (e.g., heroin, methadone, morphine) would at maximum receptor occupation. People who require methadone doses much higher than 40 mg/day probably won't be comfortable using Suboxone®.

First of all, those know who what Suboxone® is and immediately want practical details about obtaining and using it should go here. This page is going to discuss the pharmacology, sociology, and politics of buprenorphine. You will probably find it interesting reading, but if you are sick, it's obviously more imporant for you to get relief than it is for you to find interesting reading. So go to our Suboxone Resource Page first. Remember: Suboxone means that there is now no reason (no legal reason, anyway) why anyone has to be suffer withdrawal sickness again. That is an enormous sea-change, considering that expenditures in the war on the Bill of Rights (er, sorry, I meant the war on drugs) have been rising steadily since at least 1970, and really, since 1935; and the ability of physicians to prescribe opioid substitution treatment has been drastically circumscribed until now. The office-based prescribing of buprenorphine was made possible by the Drug Abuse Treatment Act of 2000 (DATA), which allows specially certified physicians to prescribe approved narcotics in Schedules III, IV, and V for the maintainence treatment of opioid dependence – not drugs in Schedule II, like methadone, morphine, or oxydocone. The catch was that the drug prescribed must be specifically approved by the FDA for maintainence, and no drugs that were not in Schedule II were approved until a few months ago.

Buprenorphine has been used to maintain opioid addicts in Europe for quite a number of years now; the idea of maintaining addicts on the drug is hardly a new one. Bringing the idea into America, however, has involved crossing many hurdles. The public needs to be convinced that any new "therapy" for addicts will, at a minimum, not give the addicts the effect they crave, that it will block the effects of opiates that addicts themselves decide to take whilst on the "treatment" drug, and, hopefully, that there will be a punitive aspect to the treatment as well, "disease model" notwithstanding. In the case of methadone, the public continues to believe these things – especially, the idea that methadone is without psychotropic effects – in spite of the fact that methadone is a Schedule II narcotic, right up there with morphine and Dilaudid®, and really doesn't differ in any substantive pharmacological way from those drugs. The so-called "blocking effect" of methadone is not at all like the blocking effect of, e.g., naltrexlone: what is meant by saying that a high dose of methadone "blocks" the effects of heroin is simply that the subject's tolerance is made so high that he or she will not be able to afford enough heroin to overcome it – too, with all binding sites saturated by methadone, there is a problem of kinetics/equilibrium involved in the attempt to displace methadone from those sites.

Some Political Comments

If you read the Drug Abuse Treatment Act (DATA) carefully, you will discover that it allows the individual States to forbid opioid substitution treatment any time following three years of the passage of the Act. The Act was passed in 2000, and the FDA held up approval of any drug intended for use under the Act until 2003. In other words, the "evaluation period" was already over before any treatment at all had taken place under the new law. This is obscene, evil beyond description, and therefore entirely in keeping with the values and motives of our government with respect to our massive addicted citizen population.
But what is unspeakably more vile is that DATA states that, any time after the three year "evaluation period," the DEA can, at its discretion, cancel authorization for office-based maintenance treatment, rendering DATA entirely null and void. Of particular importance is the fact that DATA can be repealed by the DEA (which is an executive agency, not a legislative one) without any legislative action at all being taken. Plainly put: if, in the opinion of the DEA, significant amounts of buprenorphine are being "diverted," or if it finds anything else about office-based maintenance upsetting, it may simply nullify the will of our elected representatives, making this treatment method illegal and condemning hundreds of thousands of addicts to agony, misery, despair, and death. Again, it can't be over-emphasized that the DEA can take this action at their whim, at any time following the three-year "evaluation period," which was already over before any medication had been approved for use under the new law, and before a single patient had actually been treated. Can it really be a coincidence that no drugs were approved for use under the Act until this three-year "evaluation period" was over?
Such a thought is not paranoid at all. Consider how much time passed between the approval of Viagra® and its appearance on pharmacy shelves. That period of time is measured in nanoseconds, not years. It seems that helping old white men achieve erections is far more important than the suffering of millions of subhuman "junkies." Given the current War on Freedom (er, sorry, I meant the war on drugs), it always seemed rather astounding that Suboxone® treatment was being contemplated at all. One would expect that the man appointed President by the once-venerable but now irredeemably corrupt Supreme Court would have preferred a policy of rounding up all addicts and plowing them into mass graves. After all, Mr. Bush has stated, with respect to addiction, "Punishment is treatment." And recall that supposedly "liberal" Republican Rudy Giuliani did his utmost to close down even the methadone clinics in New York City during his tenure as Mayor. Something is happening here, but you don't know what it is, do you, Mr. Jones?
Alas, heartsick as it may make one, Mr. Jones is beginning to put the pieces together.
Once the new law is seen in its full context – once it is clearly seen that this law was never allowed to actually become effective, due to the FDA's deliberate withholding of approval for Suboxone® until after the "evaluation period" had expired – the Congress' making such an uncharacteristically humane Act becomes far less baffling. For the DATA law had been a profound mystery: an Act whose wisdom and compassion were entirely at odds with the government's ongoing War on Certain Ordinary Citizens (excuse me, I meant "War on Drugs"), and its "harm augmentation" policy. But the DEA is now free to "evaluate" the DATA law without any actual information to base an evaluation on, and decide whether it likes the law or not. If it does not (and who could doubt the compassion of the DEA towards America's millions of addicted citizens?), it can simply repeal the Act, even though the Constitution forbids the Legislative Branch from delegating its powers to the Executive Branch. Our Senators and Representatives needn't dirty their hands with legislation that would send thousands of American citizens to their graves – a clerk in DEA Administrator Hutchinson's office can take that distasteful task off their hands.
Of course, while our nation is waging a War on the Constitution (pardon me, I meant "a War on Drugs"), we cannot allow our resolve to be weakened by technicalities. And the Constitution and the Bill of Rights inch closer and closer to being "technicalities" every day.

Unlike methadone, which, aside from its high oral bioavailability and long duration of action, isn't signficnalty different from morphine or hydromorphone (Dilaudid®), buprenorphine really does differ pharmacologically from full opioid agonists. It differs enough that it was only listed in Schedule V, until, having failed in their attempt to prohibit office-based maintainence outright, those in favor of the most miserable lives possible for addicts settled for having it moved up to Schedule III. Overnight, buprenorphine, one of the most benign drugs that exists, had become orders of magnitude more dangerous.