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The abuse of prescription drugs has increased significantly, with the number of Americans who report abusing controlled prescription drugs more than doubling from 7.8 million to 16.3 million from 1992 to 2006. Examples of commonly used and abused prescription drugs include but are not limited to benzodiazepines (e.g., diazepam [Valium], clonazepam [Klonopin]), stimulants (e.g., methylphenidate [Ritalin], d-amphetamine), opioids (e.g., oxycodone, hydrocodone), and barbiturates (e.g., pentobarbital). In its 2007 report, the International Narcotics Control Board reported that the abuse and trafficking of prescription drugs is set to exceed other illicit drugs. The board noted that medications containing narcotic drugs and/or psychotropic substances have become a drug of first choice for many individuals, rather than being used as a substitute for the more conventional illicit drugs such as cocaine and heroin. This report also noted that many prescription drugs can produce effects similar to illicit drugs when taken in inappropriate quantities and without medical supervision.

Although abuse of prescription drugs has increased in general, the rise has been particularly striking among prescription opioids. As noted in a comprehensive 2003 review by James Zacny and colleagues from the College on Problems of Drug Dependence, data from the 2001 National Survey on Drug Abuse show that, out of a large number of different psychotherapeutic drug classes, opioids are the class with the greatest nonmedical use, abuse, and dependence. Examples of prescription opioids include morphine (both immediate-release and sustained release, e.g., MS-Contin), levorphanol (Levo-Dromoran), methadone, codeine (opioid constituent in Tylenol-3), hydrocodone (opioid constituent in Vicodin, Lortab), oxycodone (opioid constituent in Percodan, OxyContin), propoxyphene (opioid constituent in Darvon), fentanyl (Duragesic), and hydro-morphone (Dilaudid). These drugs generally are categorized as opioid analgesics, are typically prescribed for the treatment of acute or chronic pain, and are usually ingested orally in pill form. When used appropriately, these medications can be extremely effective in the medical management of pain, and the vast majority of patients receiving prescription opioids for pain management do not develop problematic or excessive use of the medications. However, like other opioid agonists, such as morphine and heroin, prescription opioid pills can be abused. In addition to oral administration, for example, many of these drugs can be crushed and self-administered via injection, inhalation, or snorting.

Opioid Effects

Most of these opioids, regardless of whether they are licit or illicit, primarily bind to the mu-opioid receptors in the nucleus accumbens in the brain and produce an increase in the concentration of dopamine. Effects of prescription opioids are similar to those seen with the larger class of opioid drugs (e.g., heroin) and include analgesia, drowsiness, euphoria, constipation, pupil constriction, clouding of mental function, and depression of the central nervous system and of cardiac activity at high doses. When opioid overdoses occur, they typically result from the respiratory-suppressing effects of opioids. In general, the severity or intensity of opioid effects depends mainly upon the amount or dose of drug and route of administration used.

With repeated use of any opioid, physiological tolerance may develop. Tolerance is typically identified by diminished sensitivity to the drug. For example, it eventually takes a larger amount of the drug to achieve the same effects that were experienced early on. High levels of tolerance can develop for the respiratory depression, analgesia, sedation, and euphoric effects of opioids. In contrast, little tolerance develops for the pupil constriction or constipation typically seen following opioid administration.

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