September/October 2007
Volume 3, Issue 5

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Suboxone and Drug Dependency

An Original Contribution by Sareta Coubarous, D.O.

In 2000, The Drug Addiction Treatment Act (DATA) was passed by Congress for hospital use in specially licensed clinics, and the in-office treatment of opioid dependence. Under DATA 2000, the approval of the first opioid medication to treat opioid dependence in an office setting was passed.

Suboxone® C-III (buprenorphine HCI/naloxone HCI dehydrate sublingual tablets), combines a partial opioid agonist, buprenorphine, and an opioid antagonist, naloxone, in a 4:1 buprenorphine: naloxone ratio. Buprenorphine is the primary active compound which reduces opioid cravings, withdrawal symptoms, and blocks other opioids’ effects by binding to the mu receptor. By binding to the mu receptors, Buprenorphine discourages the use of nonprescribed opioids. The naloxone component will precipitate opioid withdrawal if suboxone is crushed or injected, and is included to help discourage diversion and misuse.

Opioid dependence is a serious disease which has plagued the medical community for many reasons. Not only does dependence cause a burden on the lives of the patients, it causes a burden on health care and law enforcement. Until now, Methadone clinics have been the source of outpatient treatment of the opioid dependence of heroin. In-office treatment of prescription opioids with Suboxone offers patients privacy, convenience, and confidentiality.

Opioid tolerance is the need to take additional medication in order to get the same effect because the same amounts of medications have less effect. Some common characteristics of opioid tolerance includes taking larger amounts of opioids for longer periods of time; change in behavior to use, obtain, and recover from opioid use; the use of the drug despite negative consequences; disregard of work, social, or have access to the opioid use; going through withdrawal when the opioid is stopped abruptly, and having the need to relieve withdrawal symptoms with other medications.

How Does Suboxone Work?

When opioids are released in the bloodstream they cross the brain barrier and attach to mu receptors. This initiates the opioid’s effect. Dopamine is released into an area of the brain called the nucleus accumbens, when opioids bind at the mu receptors, and stimulates its release. When there is increased dopamine activity in the nucleus accumbens, euphoria and other pleasurable sensations are experienced. Mu receptors can become tolerant after chronic use of an opioid, which can produce physical dependence. The brain alters it response to opioids after chronic use of escalating doses. The hallmark of physical dependence is the emergence of opioid-specific withdrawal symptoms when opioid levels in the bloodstream decline. When there is a decline in the opioid concentrations in the brain, the opioid molecules leave the mu receptors, and therefore become unoccupied. As more mu receptors become unoccupied, the brain releases excessive norepinephrine, which the patient experiences as clinical symptoms of opioid withdrawal.

Suboxone is taken sublingually and the buprenorphine component travels to the brain, where it binds to the mu receptors, and reinitiates opioid activity in the brain. Because buprenorphine is a partial agonist, there is less production of euphoria than a full opioid agonist, but is still capable of suppressing withdrawal and cravings.

Buprenorphine has a high affinity for the mu receptor and therefore inhibits it from being displaced by other opioids. Once most receptors are filled with the Suboxone, withdrawal and sensations of cravings are controlled.

Buprenorphine has a slow dissociation from the mu receptor, and therefore can prolong its therapeutic effect for up to 2 to 3 days, depending on dose. As a partial agonist, Buprenorphine has lower intrinsic activity than full opioid agonists, which results in less euphoria. This lowers the potential for abuse and produces less physical dependence. In order to help limit diversion and misuse of Suboxone, naloxone is combined to attenuate the effects of buprenorphine, and precipitate withdrawal in an individual dependent on a full opioid agonist. When taken sublingually, Naloxone has no clinically significant effect.

The use of Suboxone in the office setting to treat opioid dependence is advancement for improving treatment confidentiality, treatment convenience, and limits diversion and misuse. As a prescription medication, Suboxone can be dispensed for take home use for induction of withdrawal from the full opioid and maintenance from its dependence. It allows patients the convenience of not having to be treated at a clinic on a daily basis, and to be able to not interrupt the daily activities of productive patients.

The most common side effects of Suboxone reported are headache, withdrawal syndrome, nausea, insomnia, hypotension, positional dizziness, and sweating which subside after a few weeks. In comparison to full agonists which lower breathing as more of the drug is taken, Suboxone has a “ceiling effect” which makes death unlikely from an overdose from lowering breathing. This ceiling effect is appropriate when buprenorphine is used alone where there is no greater effect observed on subjective or physiologic measures. Patients taking Suboxone while also taking other sedatives, especially benzodiazepines, will add to the sedating effects of the other drug, and the combination maybe dangerous. Crushing Suboxone and mixing it with benzodiazepines for injection has caused deaths. Patients being treated with buprenorphine should not use alcohol, antidepressants, tranquilizers, or sedatives except under strict direction of a physician.

Because physical dependence is only part of the picture of opioid dependence, treatment works best when medical treatment with Suboxone is combined with counseling. Combining Suboxone treatment with counseling may increase success because patients are able to focus on their counseling and recovery, and are not distracted by cravings and withdrawal symptoms. Suboxone may be used for a few weeks, while others may need it for months or even years. There is a higher risk of relapse with short-term treatment since patients may not have had enough time to learn how to deal with the emotional and behavioral aspects of dependence.§