“It’s rotten!”, her dad said. I exclaimed, “Really was it?!” My mom was lamenting to me about having her tooth extracted as an adolescent. The tooth wasn’t rotten, but it had a hole, and it was cheaper to pull it than to fill it.”it was $10 dollars to pull it and $100 dollars to fill it…so there went my tooth”, she said. I was already drunk with laughter after she described the dentist placing his foot on her shoulders and pressing her head back with one hand, while he attempted to yank the tooth out with the other. Then, I sobered up when I vaguely heard the mention of the application of cocaine to her gums. I roared with laughter again when she slumped her body down, and waved side-to-side in an attempt to depict the feeling of euphoria it gave her. I yelled out, “cocaine”?! She wasn’t sure if it was cocaine, or if that’s just what they called it. I said, “it had to be…I didn’t know they used cocaine in dentistry?!” So naturally, I had to research the matter and write an article about it.

History of Medicinal Use

Cocaine comes from the leaves of the plant Erythroxylon Coca. The Inca of Peru had long known of the beneficial effects of the dried leaves; which they chewed to decrease fatigue and reduce appetite during long treks. A Spanish Jesuit by the name of Bernabe Cobo, in 1653, wrote that toothaches can be alleviated by chewing the leaves. Then In 1862, German Chemist Albert Niemann isolated the compound responsible for the “numbing sensation” from the leaves, and named it “cocaine”.

Shortly thereafter, Dr. Carl Koller identified cocaine as a topical local anesthetic. Many had been aware that it numbed the tongue (this is why people “taste” illicit looking powders to determine whether they are  cocaine or not), but it wasn’t until Dr. Koller made a solution of cocaine and tested it in a frogs eye, was it elucidated that cocaine can be used to perform previously painful impossible eye surgery. When dropped in the eye of the frog, he was able to touch the cornea with the head of a needle, without the frog so much as blinking or even flinching. He went on to test the cocaine solution in the eye of a rabbit, a dog, and then himself.

Dr. Koller reported his finding at the Congress of Ophthalmology in Heidelberg, on September 15, 1884. Soon thereafter, Dr. William Stewart-Halsted and Dr. Richard John Hall purchased a 4% cocaine solution from Park Davies (the company that  extracted and distributed cocaine in the USA) and subcutaneously injected it as a local anesthetic into the gums and showed that it blocked nerve sensation, without causing the patient to become drowsy or loose consciousness. Thus the use of cocaine in dentistry was born. Tooth extractions could now be performed with ease.

Undesired Effects

Cocaine also causes feelings of euphoria, and many dentists witnessed this affect in their patients. The 4% cocaine hydrochloride solution proved to be too potent, and needed to be diluted. Dr, Halsted and Dr. Hall experimented on themselves with doses and ended up becoming addicted. They started behaving erratically, both socially and professionally. Chronic Cocaine use can cause seizures, panic disorders, and psychosis. Many dentists became addicted and some — like Dr. Halsted,  even died from it. Death is a result of cocaine’s affect on the cardiovascular system, leading ultimately to heart attack or stroke. For this reason, an alternative to the use of cocaine  was sought.

In 1905, Procaine (brand name: Novocain) was introduced. It had the same local anesthetic effect without the addictive property. Later came a new generation of local anesthetic, such as, lidocaine, prilocaine, and articaine; which are still used in dentistry today. 

Pharmacology of Cocaine

There are three alkaloids extracted from coca leaves: ecgonine, tropine, and hygiene. Ecogonine is the active compound from which we get cocaine. Cocaine is an ester of benzoic acid and methyl-ecognine. It blocks nerve conduction primarily by inhibiting neuronal sodium permeability. It also causes local vasoconstriction due to inhibition of local norepinephrine reuptake at adrenergic neurons. Euphoria is due to inhibition of dopamine re-uptake in the central synapses. 

Cocaine is highly toxic due to its inability to be metabolized, inability to develop tolerance, and high ability to become addictive. Even after chronic use, low doses can cause death.  Thus, use has been limited to a topical anesthetic and vasoconstrictor (1-10 %  solution) in surgical procedures involving the nose, throat, larynx, and lower respiratory passages; to control blood loss in these highly vascularized areas.