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Narcotics of Natural Origin
The poppy plant, Papaver somniferum, is the source for non-synthetic narcotics. It was grown in the Mediterranean region as early as 5000 B.C., and has since been cultivated in a number of countries throughout the world. The milky fluid that seeps from incisions in the unripe seed pod of this poppy has, since ancient times, been scraped by hand and air-dried to produce what is known as opium. A more modern method of harvesting is by the industrial poppy straw process of extracting alkaloids from the mature dried plant. The extract may be in liquid, solid, or powder form, although most poppy straw concentrate available commercially is a fine brownish powder. More than 500 tons of opium or equivalents in poppy straw concentrate are legally imported into the United States annually for legitimate medical use.
There were no legal restrictions on the importation or use of opium until the early 1900s. In the United States, the unrestricted availability of opium, the influx of opium-smoking immigrants from East Asia, and the invention of the hypodermic needle contributed to the more severe variety of compulsive drug abuse seen at the turn of the 20th century. In those days, medicines often contained opium without any warning label. Today, there are state, federal, and international laws governing the production and distribution of narcotic substances.
Although opium is used in the form of paregoric to treat diarrhea, most opium imported into the United States is broken down into its alkaloid constituents. These alkaloids are divided into two distinct chemical classes, phenanthrenes and isoquinolines. The principal phenanthrenes are morphine, codeine, and thebaine, while the isoquinolines have no significant central nervous system effects and are not regulated under the CSA.
Morphine is the principal constituent of opium and ranges in concentration from 4 to 21 percent. Commercial opium is standardized to contain 10-percent morphine. In the United States, a small percentage of the morphine obtained from opium is used directly (about 20 tons); the remaining is converted to codeine and other derivatives (about 110 tons). Morphine is one of the most effective drugs known for the relief of severe pain and remains the standard against which new analgesics are measured. Like most narcotics, the use of morphine has increased significantly in recent years. Since 1998, there has been about a two-fold increase in the use of morphine products in the United States.
Morphine is marketed under generic and brand name products including MS-Contin?, Oramorph SR?, MSIR?, Roxanol?, Kadian?, and RMS?. Morphine is used parenterally (by injection) for preoperative sedation, as a supplement to anesthesia, and for analgesia. It is the drug of choice for relieving the pain of myocardial infarction and for its cardiovascular effects in the treatment of acute pulmonary edema. Traditionally, morphine was almost exclusively used by injection. Today, morphine is marketed in a variety of forms, including oral solutions, immediate and sustained-release tablets and capsules, suppositories, and injectable preparations. In addition, the availability of high-concentration morphine preparations (i.e., 20-mg/ml oral solutions, 25-mg/ml injectable solutions, and 200-mg sustained-release tablets) partially reflects the use of this substance for chronic pain management in opiate-tolerant patients.
Codeine is the most widely used, naturally occurring narcotic in medical treatment in the world. This alkaloid is found in opium in concentrations ranging from 0.7 to 2.5 percent. However, most codeine used in the United States is produced from morphine. Codeine is also the starting material for the production of two other narcotics, dihydrocodeine and hydrocodone. Codeine is medically prescribed for the relief of moderate pain and cough suppression. Compared to morphine, codeine produces less analgesia, sedation, and respiratory depression, and is usually taken orally. It is made into tablets either alone (Schedule II) or in combination with aspirin or acetaminophen (i.e., Tylenol with Codeine?, Schedule III). As a cough suppressant, codeine is found in a number of liquid preparations (these products are in Schedule V). Codeine is also used to a lesser extent as an injectable solution for the treatment of pain. Codeine products are diverted from legitimate sources and are encountered on the illicit market.
Thebaine, a minor constituent of opium, is controlled in Schedule II of the CSA as well as under international law. Although chemically similar to both morphine and codeine, thebaine produces stimulatory rather than depressant effects. Thebaine is not used therapeutically, but is converted into a variety of substances including oxycodone, oxymorphone, nalbuphine, naloxone, naltrexone, and buprenorphine. The United States ranks first in the world in thebaine utilization.
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