There is one FDA-approved medication that contains cocaine: Goprelto, a 4% cocaine hydrochloride nasal solution made by Genus Lifesciences. It was approved on December 14, 2017, and is used exclusively as a local anesthetic during nasal surgery. All other cocaine hydrochloride products on the market are considered unapproved by the FDA and cannot legally be distributed across state lines without approval.
What Goprelto Is Used For
Goprelto is a topical anesthetic applied inside the nose before certain surgical and diagnostic procedures. Cocaine has a unique property that makes it useful in this narrow setting: it numbs tissue and shrinks blood vessels at the same time. Most local anesthetics only numb. To also control bleeding, surgeons typically need to combine a separate anesthetic with a separate vasoconstricting agent. Cocaine does both jobs in a single drug, which is why it has persisted in nasal surgery even as newer anesthetics have largely replaced it everywhere else.
The numbing works by blocking nerve signals in the tissue where it’s applied. The blood vessel constriction happens because cocaine prevents the body from clearing away certain chemical messengers (norepinephrine and dopamine) that keep blood vessels tight. It also triggers the release of endothelin-1, one of the body’s most powerful vessel-narrowing compounds, while simultaneously blocking nitric oxide, which normally relaxes vessels. The combined effect reduces bleeding in the surgical area.
How It’s Applied
Goprelto is never injected or swallowed. In the operating room, a clinician soaks small cotton or rayon pledgets (roughly half an inch by three inches) in the solution. Four pledgets absorb the full contents of one bottle: 4 mL of solution containing a total of 160 mg of cocaine hydrochloride, so each pledget holds about 40 mg. One or two soaked pledgets are placed into each nostril, left in place for up to 20 minutes, then removed before surgery begins. If a patient shows any sign of a reaction, the pledgets come out immediately.
Side Effects and Risks
In the Phase 3 clinical trial for Goprelto, the most common side effects were headache (3% of patients) and nosebleeds (1%). The more significant concern is cardiovascular. Cocaine raises blood pressure and heart rate, and those elevations can persist for 60 minutes or longer after the pledgets are removed.
The drug is not used in patients with uncontrolled high blood pressure, a history of heart attack, coronary artery disease, unstable angina, or heart failure. It can also lower the seizure threshold, meaning patients with a history of seizures face added risk. Other vasoconstrictors like epinephrine or phenylephrine should not be used alongside it because stacking those effects can dangerously spike blood pressure.
One study comparing topical cocaine to a lidocaine-plus-adrenaline combination during a type of tear duct surgery found that high blood pressure events were eight times more common in the cocaine group (16 patients versus 2). Blood loss was also about three times higher with cocaine. Patient comfort was similar in both groups, but the cardiovascular side effects made the lidocaine combination the better option for that particular procedure.
Why Cocaine Is Still a Controlled Substance With Medical Use
Cocaine is classified as a Schedule II substance under the Controlled Substances Act. That category is reserved for drugs with a high potential for abuse that also have an accepted medical use. Other Schedule II drugs include certain opioid painkillers and amphetamine-based medications for ADHD. The scheduling means Goprelto is subject to strict storage, tracking, and dispensing rules. You will never encounter it in a pharmacy or receive a prescription to take home. It is only used in supervised clinical settings.
Why Cocaine Isn’t Used More Widely
Cocaine was once the go-to local anesthetic across medicine. In the 1880s, an ophthalmologist named Carl Koller introduced it as the first effective local anesthetic for eye surgery, launching an era of regional anesthesia that replaced the need for general anesthesia in many procedures. It was widely used in dentistry and eye care for decades afterward.
Safer synthetic alternatives gradually replaced it almost everywhere. Lidocaine, procaine, and similar drugs can numb tissue without cocaine’s cardiovascular effects or abuse potential. Today, cocaine’s medical niche has shrunk to nasal procedures, where its dual action (numbing plus blood vessel constriction) in a single topical application still offers a practical advantage. Even in that setting, combinations of lidocaine with a separate vasoconstrictor are increasingly preferred, particularly for patients with any cardiovascular risk factors.
No Over-the-Counter Products Contain Cocaine
Despite persistent rumors, no cough syrup, throat lozenge, eye drop, or topical cream sold in the United States contains cocaine. The only legal source is an FDA-approved nasal solution used during surgery under direct medical supervision. If you’ve seen claims that certain consumer products contain cocaine, those claims are either outdated (some products did contain coca derivatives over a century ago) or simply false.