Morphine

General Information

Other Names: 4,5a-epoxy-17-methyl-7-morphinen-3,6a-diol, morfina, morphin, morphinium, morphium Substance type: opium alkaloid

History

Sometime around 1803 and 1804, Friedrich Wilhelm Adam Serturner (1783-1841), a pharmacist's assistant, first isolated morphine as the "sleep-inducing principle" in opium (cf. Papaver somniferum, opium alkaloids). This achievement was the most important "quantum leap" in the history of pharmacology and represents the beginning of the true chemical investigation of plants. Today, the Serturner Medal is still awarded for exceptional work in pharmaceutics. Morphine may also be present in Papaver decaisnei Hochst., Papaver dubium 1. [syn. Papaver modestum Jordan, Papaver obtusifolium Desf.], and Papaver hybridum 1. (Slavik and Slavikova 1980). Whether morphine occurs in Argemone mexicana and other Papaver species (Papaver spp.) is doubtful, while the idea that hops (Humulus lupulus) contains morphine is a figment of someone's imagination. Tiny traces of the substance have been found in hay and lettuce (cf. Lactuca virosa) (Amann and Zenk 1996, 19). Morphine has also been detected in the skin of Bufo marinus toads (cf. bufotenine) (Amann and Zenk 1996, 18). Since the time when morphine was first detected in breast milk, cow's milk, and human cerebrospinal fluid, it has been known that it is a natural endogenous neurotransmitter in higher vertebrates, including humans (Amann and Zenk 1996; Cardinale et al. 1987; Hazum et al. 1981). Morphine does not bind well to the encephalin receptors (to which the endorphins dock) but docks at the specific morphine (m) receptors (Hazum et al. 1981). It is most likely biosynthesized in the body from dopamine (Brossi 1991). Another closely related substance, codeine, is also endogenous in humans (Cardinale et al. 1987). Morphine is the best and strongest natural painkiller known. Its efficaciousness is surpassed only by that of the synthetic morphine analogs (heroin, fentanyl). Morphine is particularly well suited for treating chronic pain, such as in cancer therapy (Amann and Zenk 1996; Melzack 1991). Endogenous morphine constitutes the body's own pain medication: Studies on rats have shown that among animals who were suffering from arthritis, morphine concentrations in the spinal cord and urine were significantly elevated. Because of this, it is assumed today that the organism produces increased amounts of morphine in certain disease states. Consequently, endogenous morphine may serve to regulate pain in the organism. Morphine exists in animal and human tissue and is excreted in significant amounts in the urine. (Amann and Zenk 1996,24)

About 30 mg orally represents an effective dosage. Habitual morphine users may use as much as 1 g per day (Hirschfeld and Linsert 1930,255*): It is known that opium eaters experience a significant increase in sexual functions during the initial period of opium consumption. During opium inebriation, erotic images appear and may even include extraordinary sexual fantasies.... The effects of morphine are similar, where an increase in sexual excitability was observed following several weeks of taking 0.03 to 0.06 g per day. (Max Marcuse, 1923, Handworterbuch der Sexualwissenschaft [Handbook of Sexual Sciences] ) When used for sedation, in anesthesia, and for calming and antispasmodic purposes, pharmaceutical preparations of morphine hydrochloride and atropine sulfate or morphine hydrochloride and scopolamine hydrobromide are used-the final reminders of the recipes for the former soporific sponges. During the Golden Twenties, the use of morphine in Berlin society circles was depicted in numerous pictures and illustrations (e.g., by Paul Kamm) that appeared in magazines. These illustrations played a great role in creating the stereotype of the "Morphinist" (cf. Papaver somniferum), who also became the object of literary treatments (Bulgaka 1971; Mac From 1931). Even the life story of the man who first discovered the substance,

Friedrich Wilhelm Sertiirner, became the subject of a novel (Schumann-Ingolstadt n.d.). Heroin, a derivative of morphine, has also inspired a rich body of literature. One of the first of this was the novel Heroin, by Rudolf Brunngraber (1952*), which dealt with the role of heroin in Egypt during the Golden Twenties. Morphine was and still is a popular inebriant in the music scene (particularly that of jazz and rock). "Sister Morphine," a song by the Rolling Stones (Sticky Fingers, Virgin Records, 1971), is arguably the most famous hymn to the drug. Morphine, a crossover band that mixes elements of cool jazz and modern rock, took its name from the alkaloid, and one of its albums is titled Cure for Pain (Rykodisc, 1993).