Opium preparations

In the mid-nineteenth century, it was the custom for doctors to frequently prescribe morphine (first isolated from opium by Friedrich Serturner in 1806) and other opium preparations. Morphine did not have a major impact on medical practice until the invention of the hypodermic needle in 1840. Soldiers illness was recognized after the Civil War when more than 50,000 veterans became dependent on morphine as a result of treatment for combat injuries (Musto 1987). The public also had ready access to opium and purified drugs in grocery stores and pharmacies. Medicinal mixtures and nostrums, usually unlabelled as to contents, often contained opium or morphine. By the end of the century, many physicians had come to recognize that chronic use of morphine was a disorder (morphinism), although others in society... 

Babies bom to opioid-addicted women also exhibit withdrawal signs, but because of the slower metabolism of opioids in the newborn, the withdrawal signs are more protracted. The babies are often treated with the opium preparation paregoric to reduce withdrawal signs. 

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 preparations have taken many forms during history. 

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 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 ... 

Chemical/Pharmaceutical/Other Class Paregoric is an opium preparation. It is composed of several alkaloids, including anhydrous morphine (9.5% or more) and smaller amounts of codeine and papaverine... 

Paregoric is well absorbed from the gastrointestinal tract. Peak serum levels are detectable 1 h after ingestion. Opium preparations are metabolized in... 

Morphine (21a) was first isolated by Sertumer in 1806, followed by codeine (21b) in 1832 by Robiquet and then the non-morphine alkaloid, papaverine by Merck in 1848, all from crude opium preparations. With the invention of the hypodermic needle and the availability of the purified alkaloids, the benefits and problems associated with these compounds (and their synthetic derivative, heroin) rapidly became apparent, leading to the search for potent dmgs without the abuse potential of the morphinoids. With the exception of the semi-synthetic compound, buprenorphine (22), which is approximately 25-50 times more potent than morphine and has a lower addiction potential, none of the compounds made to date from modifications around the phenanthrene stmcture of morphine have exceeded the pain control properties without a concomitant addiction potential. An interesting compound, whose structure is based on that of morphine is pentazocine (Talwin ) (23). This has about 30% of the efficacy of morphine, but has a much lower incidence of abuse and does in fact cause withdrawal... 

Examples are cough syrups containing codeine diphenoxylate preparations opium preparations 100 mg/mL and antidiarrheal and analgesics. Some examples are cough preparations containing not more than 200 mg of codeine per 100 mL or per 100 g (Robitussin AC), Phenergan with codeine. 

Although the term anesthesia was not used until the mid-1800 s, many herbal and alcoholic remedies had been used for thousands of years to duU sensation and relieve pain. Records from 1500 b.C.e. describe the use of inhaled opium preparations, and... 

Stahl and Jork [229 c] have critically compared the numerous solvents already quoted in the literature, with a view to introducing TLC into pharmacopoeia procedures and to identifying crude opium and opium preparations. 

As clearly seen from Fig. 154, solvent selection can be adapted to the particular problem. Thus papaverine and narcotine can be distinguished with neutral solvents which contain benzene as chief component (Nos. I—VI). Morphine and narceine can be separated only in basic solvent mixtures (Nos. X—XIV). If one has no desire to carry out multiple development, solvents X and XIV offer the best separation chance for the 6 alkaloids mentioned, whether in a mixture together or in opium preparations. 

Thebaine is devoid of analgaesic activity and is in some respects antagonistic and can also cause convulsions. It is not used medicinally by itself and, although it is present in opium preparations, the low levels mean that it only exerts a weak antagonistic effect on morphine. 

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