Crude opium

Estimation of Morphine in Opium. The problem of determining with reasonable accuracy the percentage of morphine in opium is of importance for the standardisation of medicinal opium, as a means of fixing the price of crude opium, and of controlling factory operations in the extraction of... 

As in the case of the steroids, introduction of additional nuclear substituents yields morphine analogs of increased potency. The more important of these are derived from one of the minor alkaloids that occur in opium. Thebaine (14), present in crude opium in about one-tenth the amount of morphine, exhibits a reactive internal diene system that is well known to undergo various addition reactions in a 1,4 manner (e.g., bromination). Thus, reaction with hydrogen peroxide in acid may be visualized to afford first the 14-hydroxy-6-hemiketal (15). Hydrolysis yields the isolated unsaturated ketone (16). Catalytic reduction... 

Morphine is a natural product. Morphine was isolated as a pure compound from crude opium, an exudate of the poppy, in 1804. Morphine is quite a complicated molecule. 

During the nineteenth century, chemists had a good deal of success in isolating and purifying natural products from plant sources. Morphine was isolated as a pure compound from crude opium in 1804. Quinine was isolated from the bark of the cinchona tree in 1820 and was initially employed as a fever reducer. However, its effectiveness against malaria was soon discovered and it found an alternative highly important medical use. Sodium salicylate was isolated from the bark of the willow tree in 1821 and was also shown to have analgesic, antipyretic, and antiinflammatory properties. It took an additional 76 years, until 1897, to synthesize the acetyl derivative, acetylsalicyclic acid, commonly known as aspirin. 

Crude opium has been used in the past as a sleep-inducer and in folk medicine for many purposes and smoked for the feeling of pleasure. The last use has lead to drug dependence and unpleasant withdrawal symptoms. 

Opium, the source of morphine, is obtained from the poppy, Papaver somnlferum and P album. After incision, the poppy seed pod exudes a white substance that turns into a brown gum that is crude opium. Opium contains many alkaloids, the principle one being morphine, which is present in a concentration of about 10%. Codeine is synthesized commercially from morphine. 

Diarrhea from almost any cause can be controlled with the opioid analgesics, but if diarrhea is associated with infection such use must not substitute for appropriate chemotherapy. Crude opium preparations (eg, paregoric) were used in the past to control diarrhea, but now synthetic surrogates with more selective gastrointestinal effects and few or no CNS effects, eg, diphenoxylate or loperamide, are used. Several preparations are available specifically for this purpose (see Chapter 62). 

Opium contains more than 20 distinct alkaloids. In 1806, Sertiirner reported the isolation of a pure substance in opium that he named morphine. The discovery of other alkaloids in opium quickly followed that of morphine (codeine by Robiquet in 1832 and papaverine by Merck in 1848). By the middle of the 19th century, the use of pure alkaloids rather than crude opium preparations began to spread throughout the medical world. 

The opium poppy is an annual. When the petals drop from the white flowers, the capsules are cut. The juice exudes and hardens, forming a brownish mass that is crude opium. It contains a total of about 20 narcotics, including morphine. 

The U.S. government passes the Narcotic Import and Export Act, which prohibits the import and sale of crude opium except for medical purposes. 

Even these numbers do not sufficiently reflect the scale of the cash flow derived from crude opium sales alone. It must be added... 

It was projected that the same networks established to bootleg liquor could just as easily smuggle and retail narcotics. By 1926, U.S. narcotics agent-on-the-scene in the Far East, Ralph Oyler, wrote back to his boss Levi Nutt, chief of the U.S. Narcotics Division, that the opium market had expanded so tremendously that Britain was "even taking shipments of crude opium from the... 

Morphine [MOR feen] is the major analgesic drug contained in crude opium and is the prototype agonist. Codeine [KOE deen] is present in lower concentrations and is inherently less potent. These drugs show a high affinity for p receptors, varying affinities for 8 and k receptors, and low affinity for o receptors. 

Codeine (2, R = CH3) occurs in the opium poppy along with morphine (2, R = H) but usually in much lower concentration. Because it is less toxic than morphine and because its side effects (including depression, etc) are less marked, it has found widespread use in the treatment of minor pain and much of the morphine found in crude opium is converted to codeine. The commercial conversion of morphine to codeine makes use of a variety of methylating agents, among which the most common are trimetliylphenylammonium salts. In excess of two hundred tons of codeine are consumed annually from production facilities scattered around the world. 

Crude opium tastes very bitter and contains more than twenty different drugs, of which the most important is morphine. Named for Morpheus, the Greek god of dreams, morphine was isolated... 

Yet narcotics have generated more fear and argument than any other class of drugs. The reason, of course, is their potential to cause addiction, a problem that was probably recognized even hy ancient peoples when the only form available was crude opium from poppies. 

The principal active ingredient in crude opium was isolated in 1806 by Friedrich Sertiimer, who tested pure morphine on himself and three young men. He observed that the drug caused cerebral depression and relieved toothache, and named it after Morpheus. ... 

Papaver somniferum (opium poppy) contains a variety of opioid and related alkaloids, including codeine, morphine, noscapine, papaverine, and thebaine. Crude opium is the air-dried latex obtained by incising the unripe capsules of P. somniferum. Paregoric is ammoniated tincture of opium (Scotch paregoric) or camphorated tincture of opium (English paregoric). The use of these formulations has largely been replaced by use of the purified compounds. 

The use of crude opium preparations is truly an ancient practice. There is evidence that opium was cultivated and used as long as 6,000 years ago by the Sumerian and Assyrian civilizations. The ancient Egyptians had discovered medical uses for opiates 3,500 years ago, as documented in the Therapeutic Papyrus of Thebes (Scott, 1969). Opium also was used for a variety of medical puiposes by the Greek and Roman civilizations. The great Greek physician Galen (a.d. 130-201) noted the following uses for opium ... 

Synonyms Crude opium Gum opium uc opium Raw opium Standardized opium powder... 

Nevertheless, long before the structure of morphine was realized, its analgesic properties were recognized and applied to medicine. Since morphine was in the pure form, it was far more effective than crude opium as an analgesic. But there was also a price to be paid—the increased risks of addiction, tolerance, and respiratory depression. 

Crude opium. Opium crudum, Pharm. Eur. has a morphine content of 12-16% whereas the pharmacopoeias require 10%. The alkaloids are bound to meconic acid, lactic acid, fumaric acid and sulphuric acid. Opium has a very characteristic smell and can be identified microscopically by the occurrence of characteristic fragments from the wall of the capsule. 

Crude opium is used as the starting material for the extraction of morphine (of which 80% is methylated to codeine), codeine and noscapine. Opium, according to the pharmacopoeia, is used for the preparation of opium tincture, which is an excellent remedy for the treatment of tropical diarrhoea. 

The following table shows the contents of various alkaloids in crude opium ... 

OPIUM FOR SMOKING (schandy, Chandu) Crude opium is extracted repeatedly with water, then fumigated and fermented for several months to get a product with a fine, peculiar aroma, which is smoked in special pipes. Daily dose is 5-15 g, corresponding to 0.5-1.5 g of morphine. 

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