COCAINE, one of a series of "cocaines," alkaloids (q.v.) occurring in the leaves of coca (q.v.), a shrub indigenous to Bolivia and Peru, but now chiefly produced by cultivation in Java.
Cocaine crystallizes from alcohol in colourless prisms, melting at 98° C; it has a specific rotation and it is readily soluble in ordinary solvents except water. It is generally used in medicine as the hydrochloride but sometimes as the base, dis solved or suspended in oils or fats. It yields well-crystallized salts of which the hydrochloride, is the most important; this crystallizes from alcohol in short colourless prisms, melting at C, and having a specific rotation [a] —67.5°. On hydrolysis with mineral acids or baryta, cocaine breaks up into ecgonine (tropine carboxylic acid), benzoic acid and methyl alcohol, so that cocaine is closely related to atropine (q.v.). It was synthetized in 1923 by Willstatter and Bode.
All the "cocaines" are found to be derivatives of a simple base, ecgonine, which contains both a hydroxyl (•OH) and a carboxyl (COON) group, the latter being esterified with methyl alcohol and the former with an acid group—benzoic acid in the case of cocaine, and cinnamic or truxillic acid in the other natural "cocaines." In the process for the manufacture of cocaine the total alkaloids of Java coca leaves are hydrolysed to ecgonine, which is converted by esterification as described, so that most of the cocaine of commerce is a partially synthetic product.
Cocaine produces little or no action on the unbroken skin, but if it is injected subcutaneously, or applied to mucous mem branes such as those of the mouth, eye, nose, complete anaesthesia is produced so that slight operations can be carried out painlessly. A 5 or io% solution is sufficient to abolish pain and touch, but stronger solutions are required to abolish sensations of heat and cold. If cocaine be swallowed its anaesthetic properties act on the mucous membrane of the stomach; the sensation of hunger is deadened and, therefore, persons taking the drug by the mouth can go for a long period without feeling the want of food. The central nervous system is first stimulated and later depressed, the higher centres being affected first. Moderate doses increase the bodily and mental power and give a sense of calmness and hap piness ; fatigue is abolished. Long exhausting feats can be car ried out under the greater bodily power produced and the in habitants of Peru chew the coca leaves for this reason. A single large dose causes mental excitement, delirium, ataxy, with head ache and depression later.
Therapeutically, cocaine is very largely used by oculists to pro duce anaesthesia of the eye; it is also used to relieve pain locally in other parts such as the mouth, teeth, ear, larynx, etc. Wide spread anaesthesia may be produced by injecting cocaine into the spinal canal; thus an injection between the third and fourth lumbar vertebrae will produce anaesthesia of the lower limbs and of the trunk as far up as the umbilicus. Anaesthesia begins in the extremities and spreads upwards, recovery starts at the umbilicus and works downwards. A cocaine spray is often used to spray the throats of sensitive persons before making a laryn geal examination.
In Europe it is practically never used for its restorative effect, only for its anaesthetic effect : it is not a food, the good it does being only temporary. See DRUG ADDICTION and NOVOCAIN.