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| Buprenorphine: An Excerpt from "Drugs of Abuse" |
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by Michael Palladini, RPh MBA - June 17, 2011
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DRUGS OF ABUSE: "FROM DOCTORS TO DEALERS, USERS AND HEALERS"
Buprenorphine is a semi-synthetic opiate, which also has the distinction of being a partial agonist and antagonist, meaning that the drug will have an opiate-like effect on mu receptors, but also has an antagonistic or blocking effect as well. This dual effect is unique to buprenorphine and has led to its use as an analgesic as well as a medicine to treat an opiate dependence. The analgesic has been marketed as Buprenex® in the parenteral (IV) form, and Suboxone® and Subutex® for use in opiate addiction treatment. Suboxone® and Subutex® are available as sublingual tablets that are dissolved in the mouth, under the tongue. The drug is metabolized considerably when used orally, and does not reach appropriate and effective bloodstream levels. Suboxone and Subutex have recently been made available as a sublingual film, which is dissolved under the tongue in a similar manner as the tablet. The film supposedly dissolves faster than the tablet, and is less bitter tasting. The individual packaging is more convenient, difficult to open to prevent accidental ingestion, and contains an imprinted code for tracking purposes. Buprenorphine is a derivative of thebaine, an alkaloid of the opium plant. The partial agonist quality of buprenorphine means that when it binds to a receptor, it is less likely to cause a response that a full agonist such as morphine or codeine. It also has a high affinity, or bonding ability, to the receptors, and prevents other opiates from exerting their effects. This less than full effect on the opiate receptors, coupled with its chemical bonding capability makes buprenorphine useful in preventing the use of other opiates, thus a powerful tool in treating an opiate addicted individual.
 
Suboxone 2mg Film Suboxone 8mg Tablet
Buprenorphine has a long elimination half life due to its high affinity for receptors, which is in the range of 20-73 hours, being highly dependent on individual variables. The use of buprenorphine for opiate dependence treatment became possible in the U.S. with the passage of the Drug Addiction Treatment Act of 2000 that made it possible for doctors to treat opiate addiction by prescribing opiates themselves, a practice that had been illegal for most of the twentieth century. Buprenorphine is available as Subutex® which contains buprenorphine in the strengths 2mg and 8mg. It is also available as Suboxone®, which contains 2mg and 8mg buprenorphine in combination with the opiate antagonist drug naloxone in a 4:1 ratio (buprenorphine 8mg: naloxone 2mg). The inclusion of naloxone in the drug preparation is to discourage the IV use of the drug, as the naloxone will provide additional opiate blockade at the receptor sites if injected, but is not effective when used as intended, sublingually. The maximum daily dose of buprenorphine is 32mg, which is also a “ceiling dose,” as the drug exerts no additional effects above this dosage. Due to its perceived safety profile and less potential for causing an overdose, buprenorphine is classified as a Schedule III drug under the Controlled Substance Act. It can therefore be prescribed via telephone by a physician and refilled at a pharmacy. This designation has made buprenorphine a much more convenient medication to use in the treatment of opiate dependence.
Buprenorphine has developed into a recreational drug regardless, and is typically sought and used by opiate users when the drug of choice is unavailable, or when one wishes to attempt to stop using opiates on their own. The partial agonist nature of the drug gives it a long onset of action time frame, which is close to 2 hours, and a long time to peak effects if taken sublingually as directed. These characteristics make buprenorphine an unlikely drug of choice for an opiate user looking for a “high.” Buprenorphine will produce effects of analgesia and a sense of euphoria in an individual with low opiate tolerance. Crushing and sniffing, in addition to injecting, is also practiced by those with a higher tolerance. The increased use of buprenorphine for opiate addiction treatment has led to an illicit market in the U.S. Bupes, subbies, oranges, stop signs, or subs sell for $10 to $15 per 8mg tablet on the street.
Michael Palladini, RPh MBA CAC resides in Beaver, Pa with wife Erin and three sons Michael, Noah and John. He received a BS in Pharmacy from Medical College of Virginia and a Master’s in Business Administration at Robert Morris University. Michael received his Certification in Addiction Counseling from Pa Certification Board. His current position is Director of Client Services for Express Med Pharmacy Services, a long term care pharmacy in Monaca, Pa. He is also employed as group therapist for outpatient services with Drug and Alcohol Services of Beaver Valley, Pa.
Michael is the founder of Three Suns Publishing, a sole proprietorship developed to educate and inform all interested parties in the area of drug addiction. He recently published “Drugs of Abuse: From Doctors to Dealers, Users and Healers.” His website and blog can be viewed at www.drugsofabuse.net.
The viewpoint expressed in this article is the opinion of the author and is not necessarily the viewpoint of the owners or employees at Healthcare Staffing Innovations, LLC.
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