Suboxone consists of two drugs; buprenorphine and naloxone. The naloxone is irrelevant if the addict uses the medication properly, but if the tablet is dissolved in water and injected the naloxone will cause instant withdrawal. When suboxone is used correctly, the naloxone is destroyed in the liver shortly after uptake from the intestines and has no therapeutic effect.

The first article defined the limitations of traditional treatment of narcotic addiction. With Suboxone, these limitations are avoided.

Suboxone consists of two drugs; buprenorphine and naloxone. The naloxone is irrelevant if the addict uses the medication properly, but if the tablet is dissolved in water and injected the naloxone will cause instant withdrawal. When suboxone is used correctly, the naloxone is destroyed in the liver shortly after uptake from the intestines and has no therapeutic effect.

Buprenorphine is the active substance; it is absorbed under the tongue (and throughout the mouth) but destroyed by the liver if swallowed. There is a formulation of buprenorphine without naloxone called subutex; I have used this formulation when the patient has apparent problems from naloxone, including headaches after dosing with suboxone.

I have also treated addicts who have had gastric bypass, where the first part of the intestine is bypassed and the stomach contents empty into a more distal part of the small intestine. In such cases the naloxone escapes 'first pass metabolism', the process with normal anatomy where the drug is taken up by the duodenum and transferred directly to the liver by the portal vein, where it is quickly and completely destroyed. After gastric bypass naloxone can be taken up by portions of the intestine that are not served by the portal system, causing blood levels of naloxone sufficient to cause brief, relatively mild withdrawal symptoms.

Buprenorphine has a 'ceiling effect'-the narcotic effect of the drug increases with increasing dose up to about one or two mg, but then the effect plateaus and higher amounts of buprenorphine do not increase narcosis. The average patient usually takes 12-24 mg of suboxone per day, and quickly becomes tolerant to the effects of buprenorphine (buprenorphine does have significant narcotic potency, but the potency usually pales in comparison to the degree of tolerance found in active opiate addicts).. The opiate receptors in the brain of the addict become completely bound up with buprenorphine, and the effects of any other opiate medication are blocked. Once the addict is tolerant to the correct dose of suboxone, the buprenorphine that is bound to their opiate receptors reduces cravings and prevents the effects-and so the use--of other opiates. Suboxone is very effective in preventing relapse; the 'choose to use' issue is effectively removed by the fact that use would require the addict to go through several days of withdrawal in order to remove the receptor blockade and allow other opiates to have an effect. Given addicts' attitudes toward withdrawal, the appeal of this 'choice' is quite low. The only real problem with suboxone treatment relates to specificity. With suboxone, the addict stays off opiates, but there is nothing to prevent the substitution of alcohol. On the other hand, naltrexone reduces alcohol cravings by blocking opiate receptors, and it is quite likely that suboxone, through its similar mechanism, will reduce alcohol cravings as well. Such an effect has been reported to me by a number of suboxone patients, but has not been reported in the literature at this point. The suboxone patients who move from one substance to another will likely require an approach that demands total sobriety. But for pure opiate lovers, other benefits of suboxone are that only mild (and possibly medicated) withdrawal is required to start treatment, the drug is usually covered by insurers, prescribing restrictions are minor, and there are fewer stigmas associated with maintenance than there are with methadone.

As I stated in part one of this article, I predict that suboxone will eventually be the standard treatment for opiate addiction, and will change the treatment approach for other substance addictions as well. My only reservation with this statement is that it is unclear how the current recovering community will respond to patients treated with suboxone. If suboxone patients are rejected by the recovering community, what will be the long-term outcome of their addictions when the substance is removed but the personalities and issues remain untreated? Is it a given that all addicts have a disease that requires group therapy? As things stand now, addicts maintained on suboxone are often referred for addiction counseling. But the exact message to deliver with counseling is debatable. In many ways, a patient maintained with suboxone becomes similar to a patient with hypertension treated for life with medication-the underlying problem persists, but the active disease is held in remission. If the uncontrolled use of opiates is effectively treated, is that enough? Should counseling be focused on removing the shame of having the disease of addiction, and on encouraging the treated addicts to get on with their normal lives? Or should we continue to see addiction as a consequence of a deeper problem or faulty character structure, which requires groups and meetings if one hopes to become 'normal'? Unfortunately the use of suboxone runs counter to successful adoption of sobriety through 12-step programs, which in the first step require acceptance of the fact that the addict is powerless over the substance-that there is no amount of will power that will allow the addict to control the deadly effects of the drug. By using suboxone the addict may develop the impression that he/she has control, particularly if suboxone becomes popular on the street for self-medication of withdrawal.

Before suboxone, the only option for opiate addicts was to lose a sufficient number of things-family, employment, freedom, health-to cause them to accept treatment and recovery. Only a small fraction of addicts recovered, and only after significant losses-and relapse rates were high. Suboxone is an amazing breakthrough; one that for the first time allows treatment of addicts early in the course of their illness, and that reliably induces remission in most patients. There are, however, some factors that have the potential to reduce the effectiveness of suboxone treatment. First, some insurers demand that the drug be used only short-term, in some cases for only three weeks! This requirement totally misses the nature of addiction, and ignores the known high relapse rate after short-term use of suboxone (and why wouldn't it be high?). Some physicians use the medication in this short-term way; hopefully the motivations for this ineffective treatment method are not related to the limits placed on the numbers of maintenance patients per physician. Other physicians will transfer their attitudes toward opiate agonists to the use of suboxone, and place constant downward pressure on the daily dose of suboxone. This approach is not appropriate with suboxone; the value of the drug requires adequate dosing to achieve the long half-life and repression of cravings.

At doses of less than 8 mg, suboxone becomes more similar to a pure agonist; one might as well be giving small doses of hydrocodone to prevent withdrawal. There is no reason beyond drug cost to reduce the dose, as tolerance is limited by the ceiling effect that occurs with relatively low doses. In other words, higher doses of suboxone do not result in eventual higher degrees of withdrawal. Another issue is that the medication is sometimes prescribed carelessly, without emphasizing the need to dose once per day. Patients left to their own devices will start using the medication multiple times per day as a 'prn' medication, and will remain in the same addiction behavior that brought them to treatment. Once per day dosing is important because it allows the addictive behavior to be extinguished over time. The frequent dosing does provide a distraction and placebo effect, and so initially patients will have an increase in anxiety when the dosing obsession is removed. But over time the anxiety will fade, and the huge void left by the removal of addictive obsession will allow the development of relationships and other positive character traits that were forced out by their addiction.

Given the time pressures and payment structures of modern medicine, suboxone may eventually replace residential treatment as a more reliable, less costly alternative. I believe that the time has come to replace the 'recovery' model with a new 'remission' model, which allows treatment of a much higher percentage of users at an earlier stage of disease. With time, will we find analogous agents that provide a low level of intoxication in return for receptor blockade? While not likely with alcohol, such an outcome is certainly within the bounds of imagination for cocaine, benzodiazepines, and barbiturates. While it is true that daily use of a partial agonist would represent a reversal from our current approach where all intoxicating substances are to be avoided, it is also true that the current approach has no bragging rights based on outcome. Finally, perhaps the adoption of a remission model will lessen the time until opiate and other addictions carry as much moral stigma as hypertension or diabetes-two other diseases that are generally treatable, but that require long-term use of medications.

Further Reference:

Suboxone for Opiate Painkiller Addiction: Are you Addicted

Pain Killer Addiction

Painkillers for Treating Pain and Inflammation

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