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The action of tropane alkaloids at the cellular level is complex and is related to their molecular structure, particularly the methylated nitrogen at one end of the molecule (see tropane). This chemical structure is also found in the neurotransmitter acetylcholine, which transmits impulses between nerves in the brain and neuromuscular junctions. The anesthetic properties of tropane alkaloids may relate to their interference with acetylcholine, perhaps by competing with it at the synaptic junctions, thus blocking or inhibiting nerve impulses. It is interesting to note that the infamous tropane alkaloid cocaine, from the leaves of the coca shrub (Erythroxylum coca--Erythroxylaceae), is also a local anesthetic when injected into skin or muscle tissue. This property led to the discovery and synthesis of the more potent compound, novocain, widely used in dentistry
Incas of the South American Andes have used coca leaves since pre-Columbian times for religious and medicinal purposes. They chew coca leaves for its stimulant properties to ward off fatique and hunger, to enhance endurance in the high altitude Andes, and to promote a sense of well-being. Cocaine acts primarily by interfering with the reuptake of dopamine. Dopamine produces feelings of well-being when it is released from one transmitting brain neuron to another. After release, dopamine is normally pumped back into the original neuron. Cocaine prevents the reuptake of dopamine and therefore prolongs the feeling of well-being.
Spanish conquistadores tried to prohibit coca use until they realized that the Indians they enslaved would work harder if allowed to chew the leaves. Coca leaves were taken back to Europe by the Spanish and in 1860 cocaine was extracted and became a popular drug in Europe. It was a popular ingredient in some beverages and medicines in the United States, including Coca Cola; however, since 1904 federal law has prohibited the inclusion of cocaine in any beverage. The Coca Cola Company complied with this law, but was sued for misleading advertising because the name implied that the beverage contained coca products. As a result, coca leaves, with the cocaine removed, were used to flavor the syrup from which the soda is made. In 1914 cocaine was formally declared illegal by the Harrison Narcotics Act.
Cocaine is a 3-ring alkaloid that is most commonly taken as a hydrochloride salt known as "coke." Crystals of cocaine hydrochloride are ground into a fine powder. One method of taking this drug is to sniff (snort) a fine line of the powder. Since the hydrochloride salt decomposes at the temperature required to vaporize it, a method was developed to convert cocaine into the liberated "base" form. "Free-base" cocaine was typically produced by heating the hydrochloride in the volatile solvent ether; however, since ether is very flammable, this method is hazardous. Crack cocaine is produced by heating the hydrochoride in a solution of baking soda until the water evaporates. This type of base-cocaine makes a cracking sound when heated; hence the name crack cocaine. Both freebase and crack cocaine can be injected and, since they are unaffected by heat, can be smoked.
During the past century, many famous people in Europe and the United States took cocaine regularly. The fictional Sherlock Holmes character quite openly took cocaine in several of the stories in order to stimulate and clarify the mind. Cocaine addiction is associated with a number of health risks. If inhaled for long periods of time, it can cause damage to the inner surface of the nose. Cocaine users tend to increase the dosage to maintain the original highs, and continual use may eventually cause damage to neuroreceptors.
Depending on the dosages, several tropane alkaloids of Datura and Brugmansia (when absorbed together) may have synergistic properties resulting in extreme hallucinations, delirium and death. Since the alkaloids are fat soluble they are readily absorbed through the skin and mucous membranes. Volumes have been written about the uses and properties of Datura in the Middle Ages. Most of the uses involved the consumption of potions or concoctions made from various parts of the plant. The famous seventeenth century Dutch artist, David Teniers the Younger, made several paintings of witches preparing for their demonic orgy or sabbat. The scenes frequently depicted a witch being anointed while she straddled a broom for her flight into the sky. Clay tablets from Babylonian and Assyrian ruins indicate that Datura was used medically in ancient civilizations several thousand years ago. Greek and Roman physicians used Datura mixed with opium as a sedative and general anesthetic during surgery. In fact, the use of scopolamine (one of the alkaloids in Datura) plus morphine as an effective pain reliever and sleep inducer was common practice until the nineteenth century.
