Cocaine has been used as a painkiller, a surgical anesthetic, a pick-me-up tonic, a toothache remedy, a soft drink ingredient, and a treatment for depression. Its history stretches from ancient Andean civilizations chewing coca leaves for endurance to a modern FDA-approved nasal spray used in operating rooms today. In between, it was one of the most widely marketed substances in the Western world, sold freely in pharmacies, wines, and beverages before laws caught up with its addictive potential.
Coca Leaves and Physical Endurance
Long before cocaine was isolated as a chemical, indigenous Andean communities chewed the leaves of the coca plant for centuries to boost physical performance at high altitude. The leaves triggered biochemical changes in how the body burned fuel during exercise, shifting energy production toward fat burning rather than relying solely on glucose. This gave sustained energy over long periods of physical labor, which was critical for people living and working thousands of feet above sea level. The effects were not about short bursts of power but about endurance, helping users function at a steady level during prolonged activity.
Freud and the “Wonder Drug” Era
Cocaine entered Western medicine largely through Sigmund Freud, who published an enthusiastic paper in 1884 documenting its stimulant and mood-elevating effects. Freud showed that cocaine had dose-dependent effects on mood, grip strength, and perception. He was so convinced of its potential that he treated a morphine-addicted friend with it, believing cocaine could cure the addiction.
Freud’s promotion, combined with earlier accounts from South America, set off a wave of medical enthusiasm. Doctors began prescribing cocaine for toothaches, headaches, digestive problems, nerve pain, and melancholy (what we’d now call depression). For a brief window in the late 1800s, cocaine was considered a legitimate treatment for an enormous range of complaints, both physical and psychological.
The First Local Anesthetic
The most lasting medical contribution of cocaine came in 1884 when Carl Koller, a young ophthalmologist in Vienna, placed a cocaine solution on the surface of the eye and discovered it completely numbed the tissue. This was the birth of local anesthesia. Before Koller’s discovery, surgery on sensitive areas like the eye was performed with the patient fully conscious and in tremendous pain, or under dangerous general anesthesia. Cocaine changed that, and its numbing properties quickly became the foundation for an entire class of anesthetic drugs that followed, many of which are still in use.
Tonics, Wines, and Coca-Cola
Outside the doctor’s office, cocaine became a commercial juggernaut. Vin Mariani, a French wine infused with coca leaves, was the most popular tonic drink of the 19th century. It contained about 15.7% alcohol and up to 300 milligrams of cocaine per liter. Over 2,000 physicians endorsed it in writing. Advertisements claimed it nourished, strengthened, and sustained the body, and that it was “well adapted for children, persons in delicate health, and convalescents.” It was marketed for anemia, lung problems, asthma, digestive issues, nervous depression, and general debility.
Coca-Cola, launched in 1886, originally contained an estimated nine milligrams of cocaine per glass, a small amount compared to a recreational dose of 50 to 75 milligrams, but enough to contribute a mild stimulant effect. The company removed fresh coca leaves from the formula in 1903. Other products were even more brazen. Lloyd Manufacturing Company sold “Cocaine Toothache Drops” in 1885, advertising them as an “instantaneous cure” with packaging clearly aimed at families.
How Regulation Shut It Down
The Harrison Narcotic Act of 1914 was the turning point. It classified cocaine alongside opium-based drugs and required registration and record-keeping for anyone distributing it. While it didn’t immediately make cocaine illegal in a criminal sense, enforcement quickly tightened. By 1919, court rulings confirmed that physicians could not prescribe cocaine simply to maintain an addict’s habit. The Treasury Department’s Prohibition Unit aggressively pursued doctors and pharmacists who continued to supply users, effectively severing the legal supply chain. Within a few years, cocaine went from a pharmacy staple to a controlled substance.
Cocaine in Modern Medicine
Cocaine never fully left the operating room. In January 2020, the FDA approved a 4% cocaine hydrochloride nasal spray as a Schedule II drug for a narrow set of uses: numbing the mucous membranes of the mouth, throat, and nasal passages. Each milliliter of the 4% solution contains 40 milligrams of cocaine hydrochloride.
It remains the most commonly used preparation among ear, nose, and throat surgeons for diagnostic and surgical nasal procedures. The reason is that cocaine is uniquely suited to this job. It simultaneously numbs tissue and constricts blood vessels, reducing bleeding and giving surgeons a clear view during endoscopic procedures. No other single drug does both. It is also used off-label to temporarily control nosebleeds before cauterization or packing, and to ease the insertion of tubes through the nose into the airway or stomach.
Systemic absorption is a real concern. When cocaine enters the bloodstream through nasal tissue, it blocks the reuptake of several chemical messengers in the nervous system, causing them to accumulate. This can increase heart rate, blood pressure, and the heart’s demand for oxygen, which is why its use is tightly controlled and limited to clinical settings with monitoring.