(1) The drug is a favored agonist–antagonist used as part of a complete treatment plan to include counseling and psychosocial support in the effective management of opioid dependence. It is very valuable in such plans, especially since there are not enough addiction treatment centers to help all patients seeking treatment.
(2) The drug is an addictive treatment that amounts to "trading one substance for another." Since it contains a synthetic opiate, it has a street value for abuse. When a person is tapered off Suboxone but does not receive effective help to recover from the need to abuse drugs, he may return to drug abuse later since it does nothing to help a person stop craving the high of opiate abuse.
What Is Suboxone?
Buprenorphine is an opioid, a semi-synthetic derivative of thebaine. It is a mixed agonist–antagonist opioid receptor modulator that is used to treat opioid addiction in higher dosages, to control moderate acute pain in non-opioid-tolerant individuals in lower dosages and to control moderate chronic pain in even smaller doses. Since buprenorphine has the advantage of being a partial antagonist, it also negates the potential for life-threatening respiratory depression in cases of abuse.
And then enters Suboxone ...
In October 2002, the Food and Drug Administration (FDA) of the United States approved Suboxone for detoxification and long-term replacement therapy in opioid dependency. The drug is now used predominantly for this purpose -- in the treatment of those addicted to opioids, such as heroin and oxycodone.
Suboxone, a controlled substance, contains both buprenorphine (an opioid) and naloxone (blocks the effects of opiates) to deter the use of the substance by intravenous injection. Controlled trials in human subjects suggest that buprenorphine and naloxone at a 4:1 ratio will produce unpleasant withdrawal symptoms if taken intravenously by people who are addicted to opioids.
In addition to the form of a sublingual tablet, Suboxone is now marketed in the form of a sublingual film. The makers of Suboxone, Reckitt Benckiser, claim that the film has some advantages over the traditional tablet in that it dissolves faster and, unlike the tablet, adheres to the oral mucosa under the tongue, preventing it from being swallowed or falling out.
Also, patients favor its taste over the tablet, stating that "more than 71% of patients scored the taste as neutral or better"; that each film strip is individually wrapped in a compact unit-dose pouch that is child-resistant and easy to carry and that it is clinically interchangeable with the Suboxone tablet and can also be dosed once daily.
Reckitt Benckiser also states that the film discourages misuse and abuse, as the paper-thin film is more difficult to crush and snort. Also, a 10-digit code is printed on each pouch which helps facilitate medication counts and therefore serves to deter diversion into the illegal drug market
How Suboxone "Works"
Buprenorphine blocks the euphoric effects of drugs like heroin by binding to the same opiate receptors in the brain used by heroin. Thus, people who use buprenorphine are not able to get a "high" from their original drug of choice (heroin, morphine, OxyContin, etc.).
Furthermore, although buprenorphind and depression are not clinically related, brain chemicals affect mood. So buprenorphine can make people feel better as they detox from opiate addiction.
The idea behind adding naloxone to Suboxone is to create a drug that is less likely to be abused. In fact, the 4:1 ratio of buprenorphine to naloxone in Suboxone helps create a “ceiling effect” without producing significant signs of withdrawal after long periods of taking the drug. To explain this another way, at moderate doses, the euphoric effects of buprenorphine reach a plateau and no longer continue to increase with higher doses, known as the “ceiling effect.”
As an added effect, high doses of Suboxone can cause withdrawal symptoms. Thus, buprenorphine carries a lower risk of abuse, addiction, and side effects compared to full opioid agonists. Therefore, the DEA currently rates Suboxone as a Schedule III drug, having relatively low abuse and addiction potential.
Getting "High" on Suboxone
Because one of the main ingredients in Suboxone (buprenorphine) is an opioid, it can produce side effects such as euphoria. And, even though the maximum effects of buprenorphine are less than those of full agonists like heroin and methadone, drug abusers have learned to get high on Suboxone. How? By crushing the sublingual tablets and either snorting or injecting the extract, which gives an effect similar to equivalent doses of morphine or heroin.
People who choose to abuse Suboxone are likely to have abused opiates over a long period of time. They may simply abuse Suboxone as a way of preventing withdrawal symptoms from heroin or other opiate addiction, or they may wish to get high or simply be curious about the effect of the drug, based on surveys done in 2006.
If buprenorphine and methadone are abused together, the effects of both drugs are enhanced. This is another reason the buprenorphine contained in Suboxone may be attractive to people currently using methadone, inhibiting methadone maintenance effectiveness.
Some people may abuse buprenorphine in conjunction with even other substances to increase the effects. This can be dangerous. These substances include benzodiazepines such as Klonopin, sleeping pills such as Ambien, alcohol, tranquilizers, other opiate medications and some antidepressants.
Combining these drugs could cause extreme sedation and drowsiness, unconsciousness and death. This is especially true if patients use injection as their method of administration. The misuse of buprenorphine medications, especially when combined with benzodiazepines and other central nervous system depressants, can lead to respiratory depression and death.
Since the Suboxone formulation still has potential to produce an opioid agonist "high" if injected by non-dependent persons, this may provide some explanation to street reports indicating that the naloxone is an insufficient deterrent to injection of suboxone.
Is Suboxone addictive?
Federal regulators now acknowledge that some users seem to be injecting the crushed tablets to get high, so there exists a thriving street market for the drug. They conclude certain doctors seem to be prescribing the drugs outside of the bounds of good medical practices.
When taken other than prescribed (crushed, snorted or injected), a person may become addicted to Suboxone. However, the naloxone contained in Suboxone guards against abuse. The opiate antagonist does nothing when the drugs are taken as directed, but should a user crush and snort or inject the medication, it blocks the effects of the buprenorphine - and, in fact, sends the user into immediate withdrawal sickness while reversing the effects of the high, requiring medical help.
Deaths have been reported in 2009 and 2010 of a father and son in Maine, two young adults in Milwaukee, a Maryland teen and a Wisconsin prison inmate, all as a result of mixing this drug with alcohol or other drugs.
The Bottom Line
Almost any drug can be abused. For example, we could discuss the harmful effects of alcohol and the devastating statistics of its abuse. Alcohol is responsible in the world for 1.8 million deaths and results in disability in approximately 58.3 million people. And then, of course, there is naltrexone (Vivitrol), developed for treatment of alcohol dependence and now also used for opioid addiction. Some people even oppose the administration of Vivitrol, an expensive drug that runs about $1,100 a month, for the treatment of these addictions.
(M.T. Moreira, L.A. Smith, et al. (2009). "Social norms interventions to reduce alcohol misuse in university or college students." Cochrane Database of Systematic Reviews. 2009)
The key issue for treatment centers using Suboxone is the exacting monitoring of their patients. That has be so tough considering different lengths of treatment, proper effective doses, tolerance levels, and many other variables. That said, addicts will continually find new ways to abuse drugs, even those substances employed in detoxification and in long-term replacement therapy.
Just consider ...
* Without Suboxone, heroin addicts and prescription opioid addicts will continue to find their products on the street.
* Some who legally take Suboxone will still get high -- by abusing it or by mixing it in deadly cocktails with other substances.
* Others who are prescribed Suboxone will even sell it -- drug dealers sell any substance to make money. But, buyers will include addicts who are unable to get into a treatment center or people who purchase the substance to keep from experiencing withdrawal from not being able to attain illegal opiates.
When considered against the reality of having heroin addicts in our communities ...
who steal to finance their addictions,
who commit violent crimes while high,
who recklessly drive their autos while under the influence,
who ignore the proper care of their children and other loved ones,
who lose job after job until they settle for living on welfare for the rest of their lives, and
who ultimately influence the next generation of addicts,
the proper administration of Suboxone that includes counseling and psychosocial support in the effective management of opioid dependence gets my approval.
No treatment is perfect, and I realize everyone has their own reasons for either supporting the use of Suboxone or for wishing it were never formulated. And, that choice is the prerogative of all citizens who must live with the effects of a crippling drug epidemic. My only hope is that thorough research and study of the use of Suboxone leads people to a learned opinion, not a view based on hearsay and the inevitable examples of times when the drug didn't work as prescribed.
Isn't it our duty and our responsibility to be receptive to methods that change the overall sad state of affairs we find ourselves currently enduring? No perfect answer to opioid addiction exists. Maybe it is on the far horizon somewhere over the rainbow, but until we find better answers, we must work to save every life we can. That is a mighty tall order, but a challenge we must be willing to accept.
Laura McNicholas. "Clinical Guidelines for the Use of Buprenorphine in the Treatment of Opioid Addiction." Treatment Improvement Protocol (TIP) 40. US Department of Health and Human Services.
E.C. Strain, K. Stoller, S.L. Walsh SL. G.E. Bigelow. "Effects of buprenorphine versus buprenorphine/naloxone tablets in non-dependent opioid abusers". Psychopharmacology 148 (4) 2000.