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Article Summary

Semi-Synthetic Narcotics

The following narcotics are among the more significant substances that have been derived from morphine, codeine, or thebaine contained in opium.


First synthesized from morphine in 1874, heroin was not extensively used in medicine until the early 1900s. Commercial production of the new pain remedy was first started in 1898. It initially received widespread acceptance from the medical profession, and physicians remained unaware of its addiction potential for years. The first comprehensive control of heroin occurred with the Harrison Narcotic Act of 1914. Today, heroin is an illicit substance having no medical utility in the United States. It is in Schedule I of the CSA.

Four foreign source areas produce the heroin available in the United States: South America (Colombia), Mexico, Southeast Asia (principally Burma), and Southwest Asia (principally Afghanistan). However, South America and Mexico supply most of the illicit heroin marketed in the United States. South American heroin is a high-purity powder primarily distributed to metropolitan areas on the East Coast. Heroin powder may vary in color from white to dark brown because of impurities left from the manufacturing process or the presence of additives. Mexican heroin, known as "black tar," is primarily available in the western United States. The color and consistency of black tar heroin result from the crude processing methods used to illicitly manufacture heroin in Mexico. Black tar heroin may be sticky like roofing tar or hard like coal, and its color may vary from dark brown to black.

Pure heroin is rarely sold on the street. A "bag" (slang for a small unit of heroin sold on the street) currently contains about 30 to 50 milligrams of powder, only a portion of which is heroin. The remainder could be sugar, starch, acetaminophen, procaine, benzocaine, or quinine, or any of numerous cutting agents for heroin. Traditionally, the purity of heroin in a bag ranged from 1 to 10 percent. More recently, heroin purity has ranged from about 10 to 70 percent. Black tar heroin is often sold in chunks weighing about an ounce. Its purity is generally less than South American heroin and it is most frequently smoked, or dissolved, diluted, and injected.

In the past, heroin in the United States was almost always injected, because this is the most practical and efficient way to administer low-purity heroin. However, the recent availability of higher purity heroin at relatively low cost has meant that a larger percentage of today's users are either snorting or smoking heroin, instead of injecting it. This trend was first captured in the 1999 National Household Survey on Drug Abuse, which revealed that 60 to 70 percent of people who used heroin for the first time from 1996 to 1998 never injected it. This trend has continued. Snorting or smoking heroin is more appealing to new users because it eliminates both the fear of acquiring syringe-borne diseases, such as HIV and hepatitis, as well as eliminating the social stigma attached to intravenous heroin use. Many new users of heroin mistakenly believe that smoking or snorting heroin is a safe technique for avoiding addiction. However, both the smoking and the snorting of heroin are directly linked to high incidences of dependence and addiction.

According to the 2003 National Survey on Drug Use and Health, during the latter half of the 1990s, heroin initiation rates rose to a level not reached since the 1970s. In 1974, there were an estimated 246,000 heroin initiates. Between 1988 and 1994, the annual number of new users ranged from 28,000 to 80,000. Between 1995 and 2001, the number of new heroin users was consistently greater than 100,000. Overall, approximately 3.7 million Americans reported using heroin at least once in their lifetime.


Hydromorphone (Dilaudid) is marketed in tablets (2, 4, and 8 mg), suppositories, oral solutions, and injectable formulations. All products are in Schedule II of the CSA. Its analgesic potency is from two to eight times that of morphine, but it is shorter acting and produces more sedation than morphine. Much sought after by narcotic addicts, hydromorphone is usually obtained by the abuser through fraudulent prescriptions or theft. The tablets are often dissolved and injected as a substitute for heroin. In September 2004 the FDA approved the use of Palladone (hydromorphone hydrochloride) for the management of persistent pain. This extended-release formulation could have the same risk of abuse as OxyContin.


Oxycodone is synthesized from thebaine. Like morphine and hydromorphone, oxycodone is used as an analgesic. It is effective orally and is marketed alone in 10, 20, 40, 80, and 160 mg controlled-release tablets (OxyContin), or 5 mg immediate-release capsules (OxyIR), or in combination products with aspirin (Percodan) or acetaminophen (Percocet) for the relief of pain. All oxycodone products are in Schedule II. Oxycodone is abused orally, or the tablets are crushed and sniffed or dissolved in water and injected. The use of oxycodone has increased significantly. In 1993, about 3.5 tons of oxycodone were manufactured for sale in the United States. In 2003, about 41 tons were manufactured.

Historically, oxycodone products have been popular drugs of abuse among the narcotic abusing population. In recent years, concern has grown among federal, state, and local officials about the dramatic increase in the illicit availability and abuse of OxyContin products. These products contain large amounts of oxycodone (10 to 160 mg) in a formulation intended for slow release over about a 12-hour period.

Abusers have learned that this slow-release mechanism can be easily circumvented by crushing the tablet and swallowing, snorting, or injecting the drug product for a more rapid and intense high. The criminal activity associated with illicitly obtaining and distributing this drug, as well as serious consequences of illicit use, including addiction and fatal overdose deaths, are of epidemic proportions in some areas of the United States.


Hydrocodone is structurally related to codeine but more closely related to morphine in its pharmacological profile. As a drug of abuse, it is equivalent to morphine with respect to subjective effects, opiate signs and symptoms, and "liking" scores. Hydrocodone is an effective cough suppressant and analgesic. It is most frequently prescribed in combination with acetaminophen (i.e., Vicodin, Lortab) but is also marketed in products with aspirin (Lortab ASA), ibuprofen (Vicoprofen) and antihistamines (Hycomine). All products currently marketed in the United States are either Schedule III combination products primarily intended for pain management or Schedule V antitussive medications often marketed in liquid formulations. The Schedule III products are currently under review at the Federal level to determine if an increase in regulatory control is warranted.

Hydrocodone products are the most frequently prescribed pharmaceutical opiates in the United States with over 111 million prescriptions dispensed in 2003. Despite their obvious utility in medical practice, hydrocodone products are among the most popular pharmaceutical drugs associated with drug diversion, trafficking, abuse, and addiction. In every geographical area in the country, the DEA has listed this drug as one of the most commonly diverted. Hydrocodone is the most frequently encountered opiate pharmaceutical in submissions of drug evidence to federal, state, and local forensic laboratories. Law enforcement has documented the diversion of millions of dosage units of hydrocodone by theft, doctor shopping, fraudulent prescriptions, bogus "call-in" prescriptions, and diversion by registrants and Internet fraud.

Hydrocodone products are associated with significant drug abuse. Hydrocodone was ranked 6th among all controlled substances in the 2002 Drug Abuse Warning Network (DAWN) emergency department (ED) data. Poison control data, DAWN medical examiner (ME) data, and other ME data indicate that hydrocodone deaths are numerous, widespread, and increasing in number. In addition, the hydrocodone acetaminophen combinations (accounting for about 80 % of all hydrocodone prescriptions) carry significant public health risk when taken in excess.

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