History of Cocaine


(From the book Cocaine the Legend by Jorge Hurtado)

It was Vassili von Anrep, of the University of Wursburg, who first perceived in 1880 the anesthetic properties of cocaine. Later Karl Koller, an associate and friend of Sigmund Freud had the opportunity of using the anesthetic properties of the new substance in eyeball operations. It fulfilled all requirements of a medication long dreamed by surgeons – the ideal anesthetic – a drug that would effectively and reversibly block the pain impulses sent to the brain, keep the patient fully conscious without the dangers of chemical sleep and, more specifically, without causing defensive behavior.

Long before, in 1859, Albert Niemann at the University of Gottingen had succeeded, in isolating this substance contained in the leaves brought in from the mountains of the Andes, the coca leaves. Its active component was cocaine, the famous compound which was a major player in American history of the twentieth century and its famous war against drugs.

Thanks to this property of the derivative from the coca leaves, it is possible to apply a cocaine injection of 2% on the nerve of a diseased molar and remove it without having the patient suffer and be tortured by pain. The doctor was able to find a calm and passive subject on whom he could work at ease and carefully. We can imagine that the benefits were momentous in the history of buccal surgery. It marked the passing of the traumatic, painful, dangerous and primitive surgical methods to the painless surgery of the twentieth century, which permitted great advances in the medical sciences. The coca leaves and the miraculous substance against pain, cocaine, soon rose to the pinnacle of pharmacology and medicine.

Hundreds of pharmaceuticals based on this molecule were thrown into the market: 2% cocaine solutions for odontological and ophthalmological work, ocular surgery was a reality!. The anesthetic properties of cocaine were used to an advantage for making medications against birth pains, ointments for hemorrhoids, solutions to relieve dentition pains in infants, drops for earaches, in addition to the myriad of applications in all surgical cases of the various medical specialties: traumatology, abdominal surgery, gynecology, etc.

The big pharmaceutical companies, such as Merck, le Pharmacie Centrale de France, later on Parke Davis and so on, endevoured in its manufacturing

The Pharmacology Manual of Odillon Martin, published in 1913, dedicated 50 pages of the treatise (almost one quarter of it) to lists of indications for the use of cocaine.





(Former Chief Laboratorist of the School of Medicine of Paris)

EYE DROPS: Cocaine Chloride 10 cg Distilled Water 10 g
INTRA RACHIDIAL INJECTIONS Cocaine Chloride 10 cgBoiled Distilled Water 20 ccSterilize:
The solution to be applied must always be recently prepared, inject into the preferred site (See dispensing methods) 2 or 3 cc of the cocaine solution. Preparatory surgical anesthetic.

OINTMENTS Alcohol coca extract 1 gBenzoate pork fat or starch glycerol 5 gTo relieve continuous painful locations, fissures, sores,

.SUPPOSITORY Alcohol coca extract 1 g Cocoa Butter 4 g To relive the pain of anal fissures and hemorrhoids


In 1923, Richard Willstatter of the University of Munich succeeded in creating, the first synthetic cocaine molecule based on the coca leaf alkaloid molecule, named procaine. The new molecule also had the anesthetic and psycho-stimulating effects of cocaine, but it has a serious shortcoming: its anesthetic power was 50% below cocaine and had no hemostatic properties (which prevent bleeding). It was necessary to add vessel constricting substances, such as epinephrine to match the hemostatic properties of natural cocaine. The vessel constricting effect is important: it prolongs the anesthetic effect by preventing the rapid reabsorbtion of the drug, which is what happens when the neighboring blood vessels are normally dilated.

Shortly there after, other molecules, invariably superficial modifications of natural cocaine and having the same shortcoming: no vessel constricting or hemostatic properties, such as xylocaine, lidocaine, etc. made their entrance into the huge vademecum of modern anesthetics.

An so, like in the 1913 treatise of Odillon Martin, the cocaine molecule, with small variants and near the year 2000, continues to be the star of local anesthetics.Modern local anesthetics have bee achieved through slight variations of the natural cocaine molecule .

Thus, for instance, Novocaine, Tetracaine, etc., are tertiary amine esters of par-amino-benzoic acid instead of esters of benzoic acid or cocaine. Later on we will look into the current legal and multimillionaire aspects of this industry.