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Narcotics were among the earliest drugs used. Opium, a narcotic, was one of the most potent drugs of our ancient pharmacopeia, with a very long history of abuse. Narcotics, whether natural or synthetic, pharmacologically impact us by binding to specific narcotic receptor sites located in the central nervous system and in other tissues. There are several different classes of these receptors, such as the delta, kappa, and mu receptors. Further, there are respective subtypes to the various classes of receptors, each of which have a specific neurological response. Accordingly, as different natural or synthetic narcotics bind to different receptors they produce varying pharmacodynamic responses. One of the most profound pharmacological effects of most narcotics, both natural and synthetic, is analgesia; antidiarrheal and cough suppressant functions have also been utilized. Habitual use of these substances, unfortunately, can readily progress to dependence. Narcotic abuse has been one of the primary targets for developers of drug policies.

In the early 19th century, Friedrich W. Serturner, a German pharmacist, successfully isolated morphine, a constituent of the latex obtained from opium poppies (Papaver somniferum). This landmark scientific discovery opened up an entire new field of study, alkaloidal chemistry. Many other opiates, the various alkaloids derived from opium, were subsequently discovered; these include substances such as codeine, narceine, narcotine, papaverine, and thebaine. These opiates can also be synthesized. For example, codeine, although a natural opiate contained in opium, can be synthesized by methylation of the 3-hydroxy group of the morphine ring. Opioids are biochemical synthetics that produce similar effects to opiates. Heroin is a semisynthetic narcotic that was created in 1874 by C. R. Wright, a British chemist. Many other semisythetic narcotics, also known as semisynthetic opioids, were synthesized, such as hydromorphone, hydrcodone, oxymorphone, oxycodone, dihydrodesoxymorphine, nicomorphine, and nalbuphine. In addition to the semisynthetic narcotics there are many synthetic narcotics.

Substances

A vast array of synthetic narcotics, also known as synthetic opioids, has been created. These substances have similar action to morphine and other opiates and many exhibit cross-tolerance. Synthetic narcotics are usually created in a laboratory with the intent of producing a substance that will have the pharmacological properties of a narcotic but, hopefully, with less liability for abuse and dependence. Some of these synthetic narcotics are drugs such as meperdine (Demerol), methadone (Dolophine), and propoxyphene (Darvon).

The synthetic narcotics can be separated into several different families, each of which consists of several different drugs. The families of the synthetic narcotics include phenylpiperidines, diphenylpropylamine derivatives, benzomorphan derivatives, oripavine derivatives, anilidopiperidines, morphinan derivatives, and others.

Phenylpiperidines

The phenylpiperidine group of synthetic narcotics includes substances such as meperdine, ketobemidone, and prodine. Meperdine, which is a synthetic opium derivative, was first made in 1939 by O. Eisleb and O. Schaumann of I. G. Farbenindustric in Hoechst-am-Main, Germany; they referred to it as dolantin. Meperdine, also known as pethidine, was first thought to have less dependence potential than morphine; however, its addictive nature was soon recognized. Meperdine has a shorter duration of action compared to morphine, as well as having less pronounced antidiarrheal and antitussive effects. Meperdine has a short half-life, three to four hours, and it also has a toxic metabolite, normeperidine. Accordingly, it should only be used for acute dosing, not for chronic analgesia, and it should also be avoided in the elderly and patients in renal failure. Under the Controlled Substances Act (21 U.S. 801–8886) of the Comprehensive Drug Abuse Prevention and Control Act and its amendments, meperdine is listed as a Schedule II substance regulated by the Drug Enforcement Administration (DEA No. 9230).

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