Cocine

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Cocine

Method of action: Antigout, Anti-Inflammatory

Treatment option: Gout, Fits, Behcet Syndrome

Medically reviewed

Marina Burgos

Last updated on 22/12/2025

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

Overview of Cocine

Here is a quick overview of the essential facts about the substance known as Cocine.

Property Description
Active ingredient Cocaine (INN)
Form Typically, Hydrochloride Salt (white crystalline powder/solution)
Pharmacological class Local Anesthetic and CNS Stimulant
Common use Topical Anesthesia for mucous membranes
Origin Natural Product extracted from the Erythroxylum coca plant

What Kind of Substance is Cocine?

Cocine (Cocaine, the accepted International Nonproprietary Name or INN) is a tropane alkaloid, a complex molecule that occurs naturally in the leaves of the South American coca plant (Erythroxylum coca). This natural product is refined for strictly controlled pharmaceutical use, primarily utilized as the hydrochloride salt. In the medical context, it is formally classified as a local anesthetic with properties that also affect the central nervous system (CNS).

Cocine has a unique combination of effects on the body. Its identity as a naturally sourced compound, clinically recognized for its dual action, distinguishes it from fully synthetic numbing agents.


What is the Approved Medical Use of Cocine?

Cocine's official therapeutic purpose is highly specific: it is approved for use by healthcare professionals as a topical local anesthetic. It is applied directly to induce numbness for minor surgical or diagnostic procedures involving the mucous membranes of the nose, mouth, and throat.

A key, differentiating property is that Cocine is the only commonly used local anesthetic that also acts as a potent vasoconstrictor (a substance that narrows blood vessels). This clinically advantageous dual function is often preferred in specific surgical scenarios, as the vasoconstriction helps reduce bleeding and subsequent absorption of the drug into the body, improving the efficiency and safety of the local anesthetic effect.

Regulatory References

  1. MedlinePlus

What side effects are possible with Cocine?

Possible side effects and safety information

The officially documented safety profile for Cocine is structurally defined by its potential for systemic adverse effects, which involve the Cardiovascular System and the Central Nervous System (CNS), even with approved topical use. Government regulatory documents formally classify the likelihood and severity of these reactions.

Changes in heart rate and blood pressure are commonly classified systemic effects. For instance, Hypertension (High Blood Pressure) is typically designated as a Very Common adverse reaction, while Tachycardia (Increased Heart Rate) and Headache are classified as Common effects based on regulatory data.

Regulatory documents highlight several events as Serious Adverse Reactions. These include Seizures (due to the drug lowering the convulsive threshold), severe Ventricular Arrhythmias, Acute Myocardial Infarction, and Respiratory Failure. Furthermore, official labeling includes a mandated warning regarding the potential for Abuse and Dependence.

Safety restrictions are documented for specific populations and conditions. Use is generally not recommended in individuals with a history of Cardiovascular Risk Factors, such as uncontrolled hypertension or coronary artery disease. Older adults may also exhibit increased susceptibility to cardiovascular adverse events. Additionally, regulatory guidance recommends that use be avoided in cases of severe Hepatic Impairment due to potential increased systemic exposure. Systemic effects, such as increases in blood pressure and heart rate, have been documented to persist for an hour or longer after the topical application device is removed.

Overdose and Emergency Response

The official regulatory profile for Cocine overdose describes a sequence of systemic effects, primarily involving the Central Nervous System (CNS) and the Cardiovascular System. Manifestations typically begin with signs of CNS excitement, including restlessness, confusion, anxiety, and tremors, coupled with cardiovascular signs such as tachycardia and hypertension. This stage can progress rapidly to severe outcomes, including massive clonic-tonic convulsions, loss of consciousness, and a pyrogenic effect (rise in body temperature).

Immediate medical help must be sought if signs of severe toxicity, such as convulsions, irregular respiration, or collapse, are observed. Regulators emphasize that resuscitative equipment and drugs should be immediately available due to the risk of life-threatening events, including ventricular arrhythmias, myocardial infarction, and ultimately, respiratory arrest.

There is no specific antidote documented in official labeling for Cocine overdose. Treatment focuses on supportive and symptomatic management, which may include the intravenous administration of short-acting barbiturates or diazepam to control severe CNS excitation. Patients with renal impairment or geriatric patients may be more susceptible to cardiovascular adverse events, requiring continuous monitoring of vital signs and ECG during management.

Therapeutic Uses of Cocine

What Cocine Treats: Main Uses and Benefits

Cocine (Cocaine Hydrochloride) is a medication generally used in specific clinical settings to provide targeted symptomatic relief and procedural support, focusing on two key therapeutic domains. The solution is commonly used to help with both local anesthesia and vasoconstriction of accessible mucous membranes prior to surgery.

It is relevant in clinical scenarios requiring temporary assistance in managing acute procedural sensory discomfort and superficial bleeding. This medication is applied across domains where short-term symptom management is appropriate, relevant in clinical settings that involve acute or disruptive symptom patterns within the accessible mucous membranes.

“The support provided by this medication is focused on easing the overall burden of symptoms related to physical discomfort during these specific clinical interventions.”


Easing Acute Procedural Pain and Discomfort

This medication is applied to address procedural sensory discomfort by providing effective, localized numbing. It is relevant in situations where symptoms related to physical discomfort and sensitivity arise from the manipulation of mucous membranes. This benefit may contribute to improved comfort during periods of heightened symptoms associated with necessary examinations and treatments.

Supporting Procedures by Reducing Bleeding

Beyond pain relief, Cocine is considered relevant in clinical scenarios requiring control over superficial bleeding. Its unique properties may assist in restricting small blood vessels at the application site, thereby managing and reducing minor surface bleeding. This action provides supportive relief in several ways: it helps establish a clear procedural field and assists with maintaining functional stability during the procedure.

Quick Fact: Relief for Procedural Discomfort
Cocine is considered relevant because it supports both symptomatic relief and control of localized bleeding, a dual action applicable in contexts where supportive management of discomfort and hemostasis is needed.

Eligibility and Restrictions for Use

Who Can and Cannot Use Cocine?

This section describes the official population eligibility rules for Cocine (Cocaine Hydrochloride) as defined by regulatory authorities.

Eligibility Status Description (Official Regulatory Labeling)
Populations Allowed Adults requiring topical anesthesia of accessible mucous membranes (oral, laryngeal, and nasal cavities).
Populations Contraindicated Patients with known hypersensitivity to the drug or other ester-based anesthetics; patients with Epilepsy; or those with Hereditary pseudocholinesterase deficiency [FDA Label].
Conditions Requiring Avoidance Recent or active history of uncontrolled hypertension, unstable angina, myocardial infarction, coronary artery disease, or congestive heart failure [FDA Label].

Age-Related Eligibility

Use in the Pediatric population (children) is not established, as safety and efficacy data are insufficient. The medicine should not be administered to children or the elderly due to increased susceptibility to cardiovascular effects [UK SmPC].

Conditional Use

Use is restricted or requires caution in patients with renal impairment or sepsis in the application area. Application to damaged nasal mucosa is prohibited [FDA Label]. For pregnancy, use is restricted to cases where it is clearly needed. Breastfeeding is not recommended, and milk should be discarded for 48 hours following treatment [FDA Label].

What should I know about interactions with other medicines?

Interactions with other medicines and products

Official regulatory labeling for approved medicinal products containing cocaine hydrochloride (used as a topical local anesthetic for mucous membranes) documents specific and clinically significant interactions, primarily related to the drug’s cardiovascular and central nervous system effects.

Interaction Scope and Classification

The primary concern in regulatory documents is the concurrent use of the drug with agents that share its physiological effects or interfere with its metabolism. Specific interacting medicinal products and substance categories are explicitly listed to guide appropriate prescribing and use. Interactions are generally classified by the resulting constraint on co-administration.

Interaction Classification Description/Product Category
Exposure-Increasing Agents Medicines like disulfiram, which significantly increase the drug’s plasma exposure (AUC and C max) by several-fold, necessitating avoidance of co-administration.
Pharmacodynamic Additivity Co-administration with other vasoconstrictor agents, such as epinephrine and phenylephrine, is explicitly advised to be avoided due to the documented risk of myocardial ischemia, heart attack, and ventricular arrhythmias.
Metabolism-Related Factors Reduced clearance and increased exposure may occur in patients with decreased plasma cholinesterase activity. The official label notes that this population-specific factor can affect the drug's metabolism and resultant systemic levels.

These official regulatory statements establish clear restrictions for use, mandating that co-administration with other vasoconstrictors is generally avoided, and if unavoidable, prolonged vital sign and electrocardiogram (ECG) monitoring is required. The avoidance of certain enzyme inhibitors that increase drug exposure is a key restriction. The overall profile, as structured by government authorities, is defined by these critical cardiovascular and exposure-related constraints.

Mechanism of Action

Cocine functions primarily as a triple monoamine reuptake inhibitor. Its main biological targets are the presynaptic plasma membrane transporters for dopamine (DAT), norepinephrine (NET), and serotonin (SERT). Cocine binds to and blocks the reuptake site of these transporters, preventing the clearance of the respective monoamines from the synaptic cleft.

This interaction results in an acute and substantial increase in the extracellular concentration of dopamine, norepinephrine, and serotonin, prolonging and enhancing their signaling at postsynaptic receptors. In the central nervous system, particularly the mesolimbic pathway, the elevated dopamine levels lead to over-activation of downstream neuronal circuits, notably those involving the D1- and D2-family dopamine receptors.

At the system level, the enhanced adrenergic and dopaminergic signaling modulates central nervous system activity, motor function, and cardiovascular regulation. The agent also exhibits a distinct mechanism as a voltage-gated sodium channel inhibitor, leading to blockade of action potential propagation in neuronal and cardiac tissue.

Dosage and Administration Information

How Cocine is Used: Official Administration Guidelines

Cocine (Cocaine Hydrochloride Topical Solution) is intended for restricted use, administered exclusively in a medically supervised setting for acute procedural needs. Its use is limited to a single application by or under the direct supervision of a trained healthcare professional, such as in a clinic or hospital setting.

The medicine is strictly for topical use on accessible mucous membranes, primarily within the nasal cavities. It is not for injection or ophthalmic use.


Administration and Dosing Principles

Feature Official Usage Instruction
Route & Method Topical administration via cottonoid pledgets soaked in the solution.
Dosing Limit The total dose for any single procedure must not exceed 160 mg or 3 mg/kg of the patient’s body weight, whichever is lower.
Frequency Single-dose application only; a second dose is not to be administered within 24 hours.
Application Duration Pledgets are left in place for up to 20 minutes for the anesthetic effect to occur.

Clinical practice involves using the lowest dosage required for effective anesthesia. The procedural structure involves saturating the pledgets and placing a maximum of two in each nasal cavity. The administration constraints also mandate that the solution must not be applied to damaged nasal mucosa.

Population-Specific Use

Dosing requires modification for specific patient groups. Reduced doses are required for geriatric or acutely ill patients. Furthermore, use is generally avoided or not recommended in patients with known hepatic impairment. Safety and effectiveness are not established for pediatric patients, and reduced dosages must be used if administration occurs.

Recent Clinical Evidence

Research Evidence / Overview of Studies for Cocine

This overview summarizes the structure and nature of the research that has been conducted on Cocine (Cocaine Hydrochloride) for its approved medical use, based on information reported in regulatory and scientific literature. This text describes what research has been done and what remains uncertain, without providing any medical guidance or therapeutic claims.

Evidence for Topical Anesthesia in Procedures on Mucous Membranes

The formal evidence base for Cocine primarily consists of randomized controlled trials (RCTs)—the type of research regulators rely on for evaluating a substance. These trials, often designed as double-blind, placebo-controlled studies, was studied for its use in procedures involving the mucous membranes, such as those in the nasal cavity. The research focused on adult patients (aged 18 or older) in settings where the medication was studied for topical application prior to procedures.

Studies explored outcomes related to physical discomfort by using standardized scales to monitor patient-reported pain intensity and by conducting objective tests to measure changes in sensation following application. The research also documented the systemic concentrations of the substance in the body after topical use; studies report these absorption measurements for context.

Evaluating Dual-Action Outcomes in Trials

The research has placed a strong emphasis on the substance's dual characteristics. Trials research examined not only the anesthetic effect (numbing) but also the physical occurrence of vasoconstriction (narrowing of blood vessels) at the application site. Researchers examined this effect because vasoconstriction is relevant to the control of surface bleeding and visibility during medical interventions. Some comparative trials have been conducted where Cocine was observed in studies alongside alternative combinations. Findings indicated that in these comparison scenarios, the patterns of patient comfort outcomes may vary depending on the specific procedural setting and the alternative regimen being studied.

Study Duration: Acute and Long-Term Follow-up Data

Because Cocine is a substance used in research exploring short-term symptom changes specifically during a medical procedure, the available efficacy evidence is acute and procedural in nature. The research provides limited insight into the state of symptoms or effects beyond this very short procedural window, and long-term effects are not fully established.

Frequently Asked Questions (FAQ)

Common questions about Cocine (FAQ)

Q: What is the proper way to store Cocine, including any temperature or security rules?

Official product information emphasizes that this medication must be stored securely to prevent theft or diversion, in line with controlled substance regulations. Official guidance specifies storing the product at controlled room temperature, defined as 20° to 25°C (68° to 77°F). Freezing of the solution should also be avoided.


Q: What is the official approved purpose of Cocine medication?

The FDA has approved Cocine (cocaine hydrochloride) for a very specific therapeutic purpose: to provide local anesthesia (numbness) of the mucous membranes. It is only indicated for use in adults to prepare the nasal cavities for certain diagnostic procedures and surgeries.


Q: Can I use Cocine if I am pregnant or breastfeeding?

Official regulatory documents address the use of this product during pregnancy and breastfeeding. During pregnancy, it is generally restricted to cases where a healthcare professional determines that it is clearly needed. For breastfeeding, use is not recommended; official guidance indicates that if the medication is administered, breast milk should be discarded for 48 hours afterward due to the potential for serious adverse reactions in the infant.


Q: Can I receive a second dose of Cocine if the first one wasn't enough?

According to the official prescribing information, Cocine is for single-dose application only during a medical procedure. The product label specifies that a second dose is not administered to the patient within 24 hours of the first dose.


Q: What is the color, shape, and consistency of the Cocine solution?

Official regulatory documents describe the appearance of the medication. The Cocine nasal solution is supplied as a clear, green-colored liquid in a single-unit bottle, which is administered by a healthcare professional.


Q: What is the current FDA risk rating or controlled substance schedule for Cocine?

The official label notes that Cocine contains cocaine and is therefore classified as a Schedule II controlled substance by the Drug Enforcement Administration (DEA). This specific scheduling reflects its high potential for abuse and is why its use is restricted to medical supervision.

How should Cocine be stored and disposed of?

How to Store and Dispose of Cocine?

As a highly regulated controlled substance, the storage and disposal of Cocine (cocaine hydrochloride) is governed by specific requirements from regulatory bodies.

Storage and Handling

  • Secure Storage: The drug must be stored securely to prevent theft, diversion, and unauthorized access, consistent with controlled substance regulations.
  • Environment: Storage areas must maintain acceptable temperature and environmental conditions to assure the drug's quality, identity, and strength are preserved.
  • Child Safety: All medication must be kept out of the sight and reach of children to prevent accidental ingestion.

Disposal Instructions

  • Take-Back Programs: The preferred method for disposal is to use a drug take-back program or mail-back envelope, if available.
  • Household Disposal: If a take-back option is not readily available, the medication must be mixed with an unpalatable substance (such as dirt, cat litter, or used coffee grounds), placed in a sealed container, and discarded in the trash.
  • Flushing: Consult official guidelines, as some controlled substances are recommended for flushing down the toilet when take-back options are unavailable and immediate disposal is necessary to prevent harm.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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