NAME THAT DRUG
VINNETTE BATISTE, MD, QUEST DIAGNOSTICS Pain Game: The Substitute Player
During the 1970s, this drug was used in low doses as a post-operative pain medication, and in the mid-to-late 1970s, its use as a treatment for drug addiction began.
T
he published isolation of morphine in 1805 permited precise drug dos- ing for the first time, and morphine
quickly became a “cure-all” drug as it was un- matched in its ability to treat pain during the 19th century. However, the widespread use of morphine elicited serious consequences including drug addiction and opioid toxic- ity. As a result, the medical and scientific communities were charged with the task of developing new compounds for the treat- ment of pain that lack these addictive and toxic properties. Tis month’s mystery drug, a derivative of thebaine, was synthesized in the continual effort to develop an analgesic compound as potent and effective as mor- phine, but which minimized the unwanted side effects and abuse potential. Tis semisynthetic drug was first discov-
ered in the mid-1960s by a British-owned pharmaceutical and consumer products com- pany that was founded in the early-1800s and merged, a century later, with a famous mus- tard company. During the 1970s, this drug was used in low doses as a post-operative pain medication, and in the mid-to-late 1970s, its use as a treatment for drug addiction began. Te drug was initially controlled in Sched- ule II under the Controlled Substances Act (CSA) during its research and development period in the United States. Since 1980, a high dose, non-injectable formulation of the drug has been utilized internationally for the treatment of opioid dependency. In 1985, an injectable formulation was approved in the United States for the treatment of moderate to severe pain, and its presumed low potential for abuse and diversion ultimately lead to a Schedule V assignment. It was not until 2002 that all formulations of the drug were placed in Schedule III of the CSA, a decision reached largely on the recommendation from the Department of Health and Human Services (DHHS). Subsequently, two products were approved in the United States for the office-
60 datia focus
based treatment of opioid dependence. Te availability of this treatment at doctors’ offices has proven effective and safe for detoxifica- tion, stabilization and long-term treatment in opioid-dependent individuals. Neverthe- less, widespread access of the drug led to increased abuse in the United States, which is supported by previous reports of diversion and illicit use internationally. Emergency de- partment visits involving the drug increased significantly from approximately 3,000 in 2005 to more than 30,000 in 2010, accord- ing to a 2013 Drug Abuse Warning Network (DAWN) report. Tis opioid drug is subject to extensive
metabolism in the liver following ingestion, making oral delivery challenging. As a result, sublingual (under the tongue), intranasal and injectable formulations are available. Tis drug is highly bound to proteins in the blood and possesses a half-life of 24-60 hours. It also shares a common metabolic pathway with many other drugs, which can lead to either inhibition or induction of metabolism depending on the co-administered drug. For example, studies have documented increases in blood concentrations of the drug when co-ingested with the antifungal, ketoconazole, and certain foods—such as grapefruit juice— are known to inhibit the metabolism of drugs that share this metabolic pathway. Te drug is a partial agonist at the recep-
tor responsible for the typical opioid effects of euphoria, pin-point pupils, sedation and central nervous system (CNS) depression; and is also an antagonist at a different recep- tor where the classical opioid antagonists (e.g. naloxone and naltrexone) exert their effects. Commonly reported side effects of the drug include flu- or cold-like symptoms, headaches, nausea, vomiting, constipa- tion, sweating, insomnia and changes in mood. When compared to other opioid compounds, the drug has demonstrated low physical dependence, is beter tolerated in
summer 2014
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