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Medical Disclaimer: This information is for educational purposes only and is not a substitute for professional medical advice.
Other
Cocaine hydrochloride is an ester-type local anesthetic and vasoconstrictor. In clinical settings, it is primarily used for providing topical anesthesia of the mucous membranes during diagnostic and surgical procedures in the nasal cavities.
Name
Cocaine
Raw Name
COCAINE HYDROCHLORIDE
Category
Other
Salt Form
Hydrochloride
Drug Count
4
Variant Count
4
Last Verified
February 17, 2026
RxCUI
1995288, 1995293, 2272608
UNII
XH8T8T6WZH
About Cocaine
Cocaine hydrochloride is an ester-type local anesthetic and vasoconstrictor. In clinical settings, it is primarily used for providing topical anesthesia of the mucous membranes during diagnostic and surgical procedures in the nasal cavities.
Detailed information about Cocaine
This page is for informational purposes only and does not replace medical advice. Consult a qualified healthcare professional before using any medication containing Cocaine.
Historically, cocaine was the first local anesthetic discovered, revolutionizing surgery in the late 19th century. However, due to its high potential for addiction and systemic toxicity, its use has been largely supplanted by synthetic amide-type anesthetics like lidocaine. Today, it remains a Schedule II controlled substance in the United States, meaning it has a high potential for abuse but can be administered by a doctor for legitimate medical purposes under strict regulation. When used clinically, it is applied as a topical solution, allowing for localized numbing while simultaneously reducing bleeding at the surgical site through its unique vasoconstrictive properties.
At the molecular level, cocaine hydrochloride exerts its anesthetic effect by binding to and blocking voltage-gated sodium channels on the neuronal cell membrane. Under normal conditions, the influx of sodium ions through these channels is essential for the generation and conduction of nerve impulses (action potentials). By blocking these channels, cocaine prevents the initiation and transmission of pain signals from the site of application to the central nervous system. This results in a localized loss of sensation (anesthesia).
Distinctly from other local anesthetics, cocaine also acts as a potent inhibitor of the reuptake of catecholamines, specifically norepinephrine, dopamine, and serotonin. It binds to the transport proteins responsible for removing these neurotransmitters from the synaptic cleft (the space between nerve cells). By preventing their reuptake, cocaine causes an accumulation of these neurotransmitters, particularly norepinephrine, at the sympathetic nerve endings. This leads to prolonged and intensified stimulation of alpha- and beta-adrenergic receptors. The stimulation of alpha-adrenergic receptors in the blood vessels causes significant vasoconstriction, which is clinically useful for reducing operative bleeding and shrinking swollen mucous membranes. However, the accumulation of dopamine in the brain's reward pathways is what accounts for the drug's high potential for euphoria and subsequent addiction.
When applied topically to the nasal mucosa (the lining of the nose), cocaine hydrochloride is rapidly absorbed into the systemic circulation. The rate and extent of absorption depend on several factors, including the concentration of the solution, the total dose administered, the vascularity of the tissue, and the presence of inflammation. While its vasoconstrictive properties theoretically limit its own absorption by reducing blood flow to the area, significant systemic levels are still achieved. Peak plasma concentrations (Tmax) typically occur within 30 to 60 minutes after topical application.
Cocaine is highly lipophilic (fat-soluble), allowing it to cross the blood-brain barrier and the placenta easily. It has a volume of distribution of approximately 1.5 to 2.0 L/kg. It binds to plasma proteins, primarily alpha-1-acid glycoprotein and albumin, though the clinical significance of this binding is relatively low compared to other drugs.
Cocaine is primarily metabolized by hydrolytic pathways. The majority (about 90-95%) is metabolized by plasma pseudocholinesterase and hepatic esterases into two major inactive metabolites: benzoylecgonine and ecgonine methyl ester. A small fraction is metabolized by the cytochrome P450 system (specifically CYP3A4) into norcocaine, which is a pharmacologically active and potentially toxic metabolite. It is important to note that patients with a genetic deficiency in pseudocholinesterase are at a significantly higher risk for cocaine toxicity because they cannot break the drug down efficiently.
The plasma half-life of cocaine is relatively short, ranging from 0.7 to 1.5 hours. The metabolites, particularly benzoylecgonine, have a much longer half-life (approximately 5 to 8 hours) and are excreted primarily in the urine. Benzoylecgonine is the primary metabolite detected in standard drug screenings.
Cocaine hydrochloride is FDA-approved for the following indications:
Off-label use of cocaine is rare in modern medicine due to the availability of safer alternatives, though it was historically used in 'Brompton's Cocktail' for pain management in terminal illness—a practice now considered obsolete.
Cocaine hydrochloride is available only for professional use in the following forms:
> Important: Only your healthcare provider can determine if Cocaine is right for your specific condition. It is never for self-administration and is strictly regulated under federal law.
Dosage of cocaine hydrochloride must be individualized based on the specific procedure, the area to be anesthetized, and the patient's physical status. Healthcare providers aim to use the lowest effective dose to achieve adequate anesthesia and vasoconstriction while minimizing the risk of systemic toxicity.
Cocaine hydrochloride is generally not approved for use in pediatric patients. The safety and efficacy of modern formulations like Goprelto and Numbrino have not been established in individuals under the age of 18. Children are at a significantly higher risk for systemic toxicity and adverse cardiovascular effects due to their lower body mass and potentially different metabolic rates.
No specific dosage adjustments are typically provided for patients with renal impairment, as the parent drug is primarily metabolized by esterases in the blood and liver. However, since metabolites are excreted renally, caution is advised in patients with severe end-stage renal disease (ESRD).
Patients with significant hepatic impairment may have reduced levels of plasma cholinesterase and hepatic esterases. This can lead to a decreased rate of cocaine metabolism, resulting in higher and more prolonged plasma concentrations. Healthcare providers should use the lowest possible dose and monitor these patients closely for signs of systemic toxicity (e.g., increased heart rate, agitation).
Geriatric patients may be more sensitive to the cardiovascular and central nervous system effects of cocaine. Clinical studies suggest that lower doses should be considered, and vital signs must be monitored rigorously during and after the procedure.
Cocaine hydrochloride for medical use is only administered by trained healthcare professionals in a clinical or hospital setting. It is not available for home use or self-administration.
Because cocaine hydrochloride is administered as a one-time dose for a specific procedure by a healthcare professional, the concept of a 'missed dose' does not apply. If a procedure is delayed, the provider will determine if re-application is necessary based on the duration of the anesthetic effect.
Cocaine overdose in a clinical setting is a medical emergency. It usually results from accidental systemic absorption or rapid administration.
> Important: Follow your healthcare provider's dosing instructions. Do not attempt to obtain or use this medication outside of a supervised medical environment.
Because cocaine is applied topically to the nose, many of its common side effects are localized to the site of application or related to mild systemic absorption of its stimulant properties. These may include:
> Warning: Stop the procedure and call for emergency medical help immediately if you experience any of the following during or after receiving cocaine hydrochloride:
In a clinical setting, cocaine is used as a one-time or infrequent application. However, repeated or chronic exposure (as seen in misuse) leads to devastating long-term effects:
Cocaine hydrochloride carries a prominent FDA Black Box Warning regarding its potential for abuse and dependence.
Report any unusual symptoms to your healthcare provider immediately. If you are at home and experience chest pain or severe headache after a procedure involving cocaine, call 911.
Cocaine hydrochloride is a potent medication that requires careful screening of patients before use. Because it significantly stimulates the sympathetic nervous system, it can place undue stress on the heart and vascular system. Patients must disclose their full medical history, especially any history of heart disease, high blood pressure, or drug allergies, to their healthcare provider.
Cocaine hydrochloride has a high potential for abuse and may lead to severe psychological or physical dependence. Use of cocaine hydrochloride should be limited to the indicated medical procedures. Strict adherence to Schedule II regulations is required for storage, handling, and administration.
During and after the administration of cocaine hydrochloride, healthcare providers must perform the following:
Because cocaine can cause dizziness, anxiety, and potential 'rebound' fatigue as the drug wears off, patients should not drive or operate heavy machinery for at least 24 hours following the procedure. A responsible adult should be available to drive the patient home.
Alcohol should be strictly avoided before and for at least 24 to 48 hours after receiving cocaine hydrochloride. The combination of alcohol and cocaine leads to the formation of a unique metabolite in the liver called cocaethylene. Cocaethylene is more toxic to the heart and has a longer half-life than cocaine itself, significantly increasing the risk of sudden cardiac death.
In a clinical setting, cocaine is used as a single-dose application. There is no requirement for tapering when used appropriately for a medical procedure. However, if a patient has been using cocaine illicitly, sudden discontinuation can lead to a 'crash' characterized by severe depression, fatigue, and intense drug cravings.
> Important: Discuss all your medical conditions, especially heart or blood pressure issues, with your healthcare provider before starting any procedure involving Cocaine.
Certain medications should never be used in conjunction with cocaine hydrochloride due to the risk of fatal complications:
For each interaction, the primary mechanism is usually the additive effect on the sympathetic nervous system or the interference with neurotransmitter reuptake. Management involves avoiding the combination or rigorous monitoring of vital signs.
> Important: Tell your doctor about ALL medications, supplements, and herbal products you are taking, including over-the-counter cold medicines.
Cocaine hydrochloride must NEVER be used in the following circumstances:
These are conditions where the healthcare provider must perform a careful risk-benefit analysis before deciding to use cocaine:
Patients who are allergic to one ester-type anesthetic are frequently allergic to others in the same class. This is often due to the production of para-aminobenzoic acid (PABA) during the metabolism of these drugs. However, there is generally no cross-sensitivity between ester-type anesthetics (like cocaine) and amide-type anesthetics (like lidocaine or bupivacaine). Therefore, lidocaine is usually a safe alternative for patients with an ester allergy.
> Important: Your healthcare provider will evaluate your complete medical history, including any past reactions to numbing agents, before prescribing or using Cocaine.
Cocaine hydrochloride is classified as FDA Pregnancy Category C (under the old system) and carries significant risks under current labeling. There are no adequate and well-controlled studies in pregnant women. However, cocaine is a known potent vasoconstrictor that can significantly reduce uterine blood flow, potentially leading to fetal hypoxia (lack of oxygen).
Cocaine is known to pass into human breast milk. Due to the drug's high potency and the sensitivity of an infant's developing nervous and cardiovascular systems, breastfeeding is not recommended following the administration of cocaine. If a nursing mother receives cocaine for a procedure, she should 'pump and dump' her breast milk for at least 48 to 72 hours to ensure the drug and its metabolites have been cleared from her system.
As previously noted, cocaine hydrochloride is not approved for use in children under 18 years of age. The risk of systemic toxicity, seizures, and cardiovascular collapse is significantly higher in pediatric populations. Clinical trials for modern formulations like Goprelto and Numbrino were conducted exclusively in adults.
In clinical trials, elderly patients (65 years and older) did not show overall differences in safety or effectiveness compared to younger adults. However, because older adults are more likely to have underlying heart disease, reduced kidney function, or be taking multiple other medications (polypharmacy), they should be treated with the lowest effective dose. Monitoring of blood pressure and heart rhythm is particularly critical in this population to prevent falls or cardiac events.
While the primary metabolism of cocaine occurs in the blood via esterases, the metabolites are cleared by the kidneys. In patients with severe renal impairment or end-stage renal disease (ESRD), these metabolites can accumulate. While the metabolites are mostly inactive, their accumulation may have unknown effects. No specific dose adjustment is required, but clinical monitoring is advised.
Since a portion of cocaine metabolism occurs via hepatic esterases and the CYP3A4 system, patients with severe liver disease (Child-Pugh Class C) may experience slower clearance of the drug. This increases the risk of systemic toxicity. Healthcare providers should exercise caution and consider alternative anesthetics if the liver impairment is severe.
> Important: Special populations require individualized medical assessment. Always inform your doctor if you are pregnant, planning to become pregnant, or breastfeeding.
Cocaine hydrochloride is a unique pharmacological agent that serves two primary functions: local anesthesia and vasoconstriction.
| Parameter | Value |
|---|---|
| Bioavailability | 30% - 60% (Topical Nasal) |
| Protein Binding | ~90% (Alpha-1-acid glycoprotein) |
| Half-life | 0.7 - 1.5 hours |
| Tmax | 30 - 60 minutes |
| Metabolism | Plasma Pseudocholinesterase & Hepatic Esterases |
| Excretion | Renal (90-95% as metabolites) |
Cocaine is classified as an Ester-type Local Anesthetic. It is the parent compound from which many synthetic anesthetics were derived. Related medications include procaine (Novocain), tetracaine, and benzocaine. It is also classified as a CNS Stimulant and a Schedule II Controlled Substance.
Medications containing this ingredient
Common questions about Cocaine
In modern medicine, cocaine hydrochloride is used exclusively as a topical anesthetic and vasoconstrictor for procedures involving the nasal cavities. It is applied by healthcare professionals to numb the lining of the nose and reduce bleeding during surgeries or diagnostic exams, such as a nasal endoscopy. Unlike its illicit use, medical cocaine is a highly regulated, standardized solution (usually 4%) administered in a controlled clinical environment. It is particularly valued in ear, nose, and throat (ENT) surgery because it provides both numbing and a reduction in blood flow simultaneously. It is not used for systemic pain relief or as a general stimulant in clinical practice.
The most common side effects reported after the clinical use of cocaine hydrochloride include headache, a mild increase in blood pressure, and a faster heart rate. Some patients may also experience minor nosebleeds (epistaxis) once the medication wears off or a stinging sensation when the solution is first applied. Because it is a stimulant, some individuals may feel briefly anxious, jittery, or have trouble sleeping if the procedure is done late in the day. These effects are usually temporary and resolve within a few hours. However, healthcare providers monitor patients closely during administration to ensure these symptoms do not become severe.
No, you must strictly avoid alcohol for at least 24 to 48 hours after receiving cocaine hydrochloride. When alcohol and cocaine are both present in the body, the liver produces a unique substance called cocaethylene. Cocaethylene is significantly more toxic to the heart than cocaine alone and stays in the system much longer. This combination drastically increases the risk of dangerous heart rhythms, heart attack, and sudden cardiac death. Always wait until your doctor confirms that the medication has completely cleared your system before consuming any alcoholic beverages.
Cocaine is generally considered unsafe during pregnancy and should only be used if there is a life-threatening medical necessity where no other alternative exists. It is a potent vasoconstrictor that can reduce blood flow through the placenta, potentially depriving the fetus of oxygen and nutrients. Chronic illicit use is linked to severe complications like placental abruption and developmental issues, and while a single medical dose is different, the risk of uterine artery constriction remains. If you are pregnant or think you might be, it is vital to inform your surgeon or anesthesiologist before any procedure. They will likely choose a safer alternative, such as lidocaine.
When applied topically to the mucous membranes of the nose, cocaine hydrochloride begins to work very quickly, usually within 1 to 5 minutes. However, it takes about 10 to 20 minutes to reach its peak anesthetic and vasoconstrictive effect. This is why healthcare providers typically leave soaked cotton pledgets in the nose for about 20 minutes before starting a procedure. The numbing effect generally lasts for 30 to 60 minutes, which provides enough time for most diagnostic tests or minor surgical interventions. If the procedure lasts longer, the doctor may need to use additional or different types of anesthesia.
In a medical context, cocaine is administered as a single, one-time dose by a professional, so there is no ongoing 'taking' of the drug to stop. There are no withdrawal symptoms from a single clinical application used for a procedure. However, the FDA warns that cocaine has a very high potential for abuse and dependence. If someone has been using cocaine illicitly or chronically, stopping suddenly can cause a severe 'crash' involving extreme fatigue, depression, and intense cravings. For medical use, the drug is strictly controlled to prevent the possibility of developing such a dependence.
Since cocaine hydrochloride is only administered by a doctor during a specific medical procedure, it is impossible for a patient to 'miss a dose' in the traditional sense. You do not take this medication at home on a schedule. If your scheduled surgery or nasal exam is cancelled or delayed, the medication will simply not be administered. If you were supposed to have a procedure and it didn't happen, you don't need to do anything regarding the medication. Always follow the specific pre-operative and post-operative instructions provided by your surgical team.
A single medical application of cocaine for a nasal procedure will have no impact on your body weight. However, chronic illicit use of cocaine is well-known to cause significant weight loss. This occurs because cocaine is a powerful appetite suppressant and increases the body's metabolic rate. Chronic users often neglect nutrition, leading to severe malnutrition and a 'wasted' appearance. In a clinical setting, these effects are not observed due to the limited, localized, and one-time nature of the application. If you have concerns about weight changes, they are likely related to other factors or medications.
Cocaine has many dangerous drug interactions and should be used with extreme caution if you are taking other medicines. It is especially dangerous to combine with Monoamine Oxidase Inhibitors (MAOIs), beta-blockers, or certain antidepressants, as these can lead to life-threatening spikes in blood pressure or heart problems. Even over-the-counter decongestants can increase the stimulant effects of cocaine. You must provide your healthcare provider with a complete list of all prescriptions, over-the-counter drugs, and herbal supplements you use. This allows them to safely manage your anesthesia and choose the correct dosage.
Cocaine hydrochloride is available as a generic topical solution, but it is still strictly a Schedule II controlled substance. There are also brand-name versions, such as Goprelto and Numbrino, which have been specifically approved by the FDA in recent years with standardized concentrations and application instructions. Regardless of whether a brand-name or generic version is used, the medication is never sold to the public at pharmacies. It is only sold directly to hospitals and licensed medical clinics for use by professionals during procedures. You cannot get a prescription to take cocaine home.