(In relation to the Buprenorphine/Naloxone Combination product(Suboxone®))
Naloxone is present in Suboxone to discourage misuse, only. It serves no other purpose.
Because of reports of misuse of buprenorphine by injection in other countries, the buprenorphine/naloxone combination was developed for the U.S. market. This combination was thought to decrease the potential for diversion and misuse of buprenorphine because, if injected, the naloxone should precipitate withdrawal in a patients already physically dependent on other opioids.
Sublingually, naloxone has a relatively low bioavailability while buprenorphine has good sublingual bioavailability.
Both have poor bioavailability through the GI tract. Taken sublingually, as directed, naloxone is clinically insignificant and has virtually no effect. (Except in rare cases of an allergic reaction or naloxone hypersensitivity.)
The safety and efficacy profile of sublingual buprenorphine/naloxone appears to be equivalent to that of buprenorphine alone (Harris et al. 2000).
Clinical Guidelines for the Use of Buprenorphine in the Treatment of Opioid Addiction
A Treatment Improvement Protocol TIP40 TIP 40, U.S. DEPARTMENT OF HEALTH AND HUMAN SERVICES, Substance Abuse and Mental Health Services Administration, Center for Substance Abuse Treatment
www.samhsa.gov, page 23
FDA. Full Prescribing information on Subutex® (buprenorphine)/Suboxone® (buprenorphine/naloxone)
naloxone: Brand name: Narcan. An opioid antagonist, similar to naltrexone, that works by blocking opioid receptors in the brain, thereby blocking the effects of opioid agonists (e.g., heroin, morphine). Naloxone has poor bioavailability when taken sublingually. Naloxone has a high afinity to the mu opioid receptor, yet not as high of an affinity as buprenorphine, at the mu receptor. source: http://www.naabt.org/glossary.cfm#N
In the absence of narcotics or agonistic effects of other narcotic antagonists it exhibits essentially no pharmacologic activity. Naloxone has not been shown to produce tolerance nor to cause physical or psychological dependence.
In the presence of physical dependence on narcotics Naloxone will produce withdrawal symptoms.
Studies and science concerning naloxone: http://www.biomedsearch.com/searchlist.html?query_txt=naloxone&s.x=15&s.y=6
To suppress the debilitating symptoms of cravings and withdrawal, enabling the patient to engage in therapy, counseling and support, so they can implement positive long-term changes in their lives which develops into the new healthy patterns of behavior necessary to achieve sustained addiction remission. - explain -