What Is Cocaine Used to Treat in Modern Medicine?

Cocaine is a FDA-approved local anesthetic used in nasal surgeries and diagnostic procedures. While widely known as an illegal drug, cocaine hydrochloride has a narrow but active role in modern medicine, specifically for numbing the mucous membranes inside the nose before surgery. It is the only local anesthetic that also constricts blood vessels, which makes it uniquely suited for procedures in the nose where both pain control and bleeding reduction matter.

The FDA-Approved Use

The sole approved indication for medical cocaine in the United States is local anesthesia of the mucous membranes during diagnostic procedures and surgeries on or through the nasal cavities in adults. It is sold under the brand name Goprelto, a 4% cocaine hydrochloride nasal solution that was first approved in 2017. The solution is a clear, green-colored liquid that comes in single-use bottles.

In practice, small cotton pledgets are soaked in the solution and placed against the nasal septum, two per nostril, for up to twenty minutes before a procedure begins. Each pledget delivers about 40 mg of cocaine hydrochloride, for a total dose of 160 mg across all four pledgets. After the pledgets are removed, the surgeon proceeds with the area numbed and blood vessels constricted.

This is used in ear, nose, and throat (ENT) procedures such as nasal septum repair, sinus surgery, and diagnostic nasal endoscopy. The dual effect of numbing tissue while simultaneously shrinking blood vessels means surgeons get a clearer, drier surgical field without needing to apply a separate vasoconstrictor. Other local anesthetics numb effectively but do nothing to control bleeding on their own.

Why Cocaine Works Differently Than Other Anesthetics

All local anesthetics work by blocking sodium channels in nerve cells. Sodium flowing through these channels is what allows a nerve to fire and send a pain signal to the brain. Cocaine blocks those channels reversibly, temporarily preventing nerves from transmitting pain. So far, this is the same mechanism as lidocaine or any other numbing agent.

What sets cocaine apart is a second action: it blocks the reabsorption of norepinephrine, a chemical your body uses to tighten blood vessels. When norepinephrine lingers around blood vessels longer than usual, those vessels constrict. The nasal lining is rich with blood vessels and bleeds easily during surgery, so this built-in vasoconstriction is genuinely useful. No other local anesthetic does both jobs at once. Research published in JAMA Otolaryngology confirmed that cocaine’s vasoconstrictive effect comes entirely from blocking norepinephrine reuptake rather than any direct action on the blood vessel walls themselves.

Cocaine also penetrates nasal tissue efficiently. Its molecular structure makes it highly lipid-soluble, meaning it passes through the mucous membrane about three times more readily than other molecules of similar size. This allows it to reach nerve endings quickly when applied topically.

How Hospitals Handle Medical Cocaine

Cocaine is a Schedule II controlled substance, the same classification as fentanyl and morphine. Hospitals that stock it follow strict security protocols. The drug must be stored in a vault or equivalent secure container, with access restricted to licensed pharmacists. Every unit is tracked through a perpetual inventory system maintained on hard copy, and any unused portions require two licensed staff members to witness and document disposal.

These requirements make medical cocaine more cumbersome to use than standard anesthetics. The regulatory burden is one reason many surgeons opt for alternatives like lidocaine combined with a separate vasoconstrictor such as oxymetazoline, even though the combination requires two drugs instead of one. Still, enough ENT surgeons find cocaine’s dual action valuable that it remains in active clinical use.

Dosage Limits and Safety

The commonly cited maximum safe dose for intranasal cocaine is 1.5 mg/kg of body weight, with most ENT surgeons staying under 200 mg total. These thresholds are based more on longstanding clinical practice than on formal dose-finding trials. The standard concentration used is 4%, meaning each milliliter contains 40 mg of cocaine hydrochloride.

An alternative preparation called Moffett’s solution combines cocaine with adrenaline and sodium bicarbonate, further enhancing vasoconstriction and tissue penetration. This mixture has a long history in British ENT practice and is still used in some surgical centers.

Medical cocaine is not used in eye surgery despite its historical roots there. In 1884, ophthalmologist Carl Koller demonstrated that cocaine could numb the eye for surgery, a breakthrough that launched the entire field of local anesthesia. However, cocaine causes damage to the corneal surface, and it is now explicitly contraindicated for ophthalmic use. People with allergies to ester-type local anesthetics are also unable to receive it.

What Cocaine Is Not Used For

Medical cocaine has no approved role in treating pain conditions, psychiatric disorders, or any chronic illness. Its use is limited to a single, brief application during a specific type of surgical procedure. It is not prescribed for home use, not dispensed through retail pharmacies, and not used as a substitute for other controlled substances.

The dopamine-blocking effect that makes cocaine highly addictive as a recreational drug is an unwanted side effect in the medical setting, not a therapeutic feature. At the low doses used topically during nasal procedures, systemic absorption is minimized, but the potential for cardiovascular effects like elevated heart rate and blood pressure is the reason dosing limits exist and patients are monitored throughout the procedure.