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    Cocaine molecular structure

    Cocaine Stats & Data

    Coke Blow Snow Yayo Girl
    NPS DataHub
    MW339.82
    FormulaC17H22ClNO4
    CAS53-21-4
    IUPACmethyl (1~{S},2~{R},3~{S},5~{R})-3-benzoyloxy-8-methyl-8-azabicyclo[3.2.1]octane-2-carboxylate;hydrochloride
    SMILES[Cl-].COC(=O)C1C(OC(=O)c2ccccc2)CC2CCC1N2C.[H+]
    InChIKeyPIQVDUKEQYOJNR-OYEKJGGTSA-N
    Tropanes
    Psychoactive Class Stimulant
    Half-Life 0.7–1.5 hours

    Interaction Warnings

    stimulants

    When used in conjunction with other stimulants, the cardiovascular effects of cocaine such as increased heart rate become dangerously high. This is potentially fatal and severely increases the risk of cardiac arrest.

    depressants

    When used in conjunction with depressants such as opioids and benzodiazepines, the cardiovascular effects of the two classes begin to conflict as one increases the heart rate while the other decreases it. This is potentially fatal and can result in an extremely irregular heart rate leading onto cardiac arrest.

    mdma

    The neurotoxic effects of MDMA may be increased when combined with cocaine.

    nicotine

    Many cocaine users find that consumption of tobacco products during cocaine use enhances the euphoria because nicotine increases the levels of dopamine in the brain. This, however, may have undesirable consequences such as uncontrollable chain smoking during cocaine use (even users who do not smoke cigarettes have been known to chain smoke when using cocaine) in addition to the detrimental health effects and the additional strain on the cardiovascular system caused by tobacco.

    Pharmacology

    DrugBank
    Half-life 1 hour State Solid

    Description

    An alkaloid ester extracted from the leaves of plants including coca. It is a local anesthetic and vasoconstrictor and is clinically used for that purpose, particularly in the eye, ear, nose, and throat. It also has powerful central nervous system effects similar to the amphetamines and is a drug of abuse. Cocaine, like amphetamines, acts by multiple mechanisms on brain catecholaminergic neurons; the mechanism of its reinforcing effects is thought to involve inhibition of dopamine uptake.

    Mechanism of Action

    Cocaine produces anesthesia by inhibiting excitation of nerve endings or by blocking conduction in peripheral nerves. This is achieved by reversibly binding to and inactivating sodium channels. Sodium influx through these channels is necessary for the depolarization of nerve cell membranes and subsequent propagation of impulses along the course of the nerve. Cocaine is the only local anesthetic with vasoconstrictive properties. This is a result of its blockade of norepinephrine reuptake in the autonomic nervous system. Cocaine binds differentially to the dopamine, serotonin, and norepinephrine transport proteins and directly prevents the re-uptake of dopamine, serotonin, and norepinephrine into pre-synaptic neurons. Its effect on dopamine levels is most responsible for the addictive property of cocaine.

    Pharmacodynamics

    Cocaine is a local anesthetic indicated for the introduction of local (topical) anesthesia of accessible mucous membranes of the oral, laryngeal and nasal cavities.

    Metabolism

    Hepatic. Cocaine is metabolized to benzoylecgonine and ecgonine methyl ester, which are both excreted in the urine. In the presence of alcohol, a further active metabolite, cocaethylene is formed, and is more toxic then cocaine itself.

    Absorption

    Cocaine is absorbed from all sites of application, including mucous membranes and gastrointestinal mucosa. By oral or intra-nasal route, 60 to 80% of cocaine is absorbed.

    Toxicity

    Intense agitation, convulsions, hypertension, rhythm disturbance, coronary insufficiency, hyperthermia, rhabdomyolysis, and renal impairment. Oral mouse LD50 = 96 mg/kg

    Indication

    For the introduction of local (topical) anesthesia of accessible mucous membranes of the oral, laryngeal and nasal cavities.

    Receptor Profile

    Receptor Actions

    Inhibitors
    Serotonin-dopamine-norepinephrine reuptake inhibitor (SNDRI)
    Other
    Sodium channel blocker

    Receptor Binding

    Sodium-dependent dopamine transporter inhibitor
    Sodium-dependent noradrenaline transporter inhibitor
    Sodium channel protein inhibitor
    Sodium-dependent serotonin transporter inhibitor
    Muscarinic acetylcholine receptor M1 antagonist
    Muscarinic acetylcholine receptor M2 antagonist
    Sigma non-opioid intracellular receptor 1 agonist

    History & Culture

    6000 BCE–present

    Coca chewing dates back at least 8,000 years in South America, making it one of the oldest known psychoactive plant practices. The leaves were integral to Andean civilizations including the ancient Wari and Inca cultures, where they served both stimulant and medicinal purposes. Traditional consumption methods included chewing the dried leaves, drinking them as tea (known as "Mate de Coca"), or preparing them in a sachet wrapped around alkaline burnt ashes held against the inner cheek. The combination with alkaline substances such as lime or plant ash is essential for psychoactive effect, as this activates hydrolysis and produces the alkaloid ecgonine, which can then be absorbed by the body. Without these alkaline additives, coca leaves produce only a numbing effect on the tongue. Traditional applications centered on suppressing appetite, combating cold, and alleviating altitude sickness. When the Spanish arrived in South America, they initially banned coca but soon reversed course after recognizing its importance to indigenous labor, instead choosing to legalize and tax the substance. The word "cocaine" traces its etymology from the Quechua word "kúka," which passed through Spanish as "coca" and subsequently into French as "Cocaïne" before entering English.

    1855–1900

    The active alkaloid was first isolated from coca leaves in 1855 by German chemist Friedrich Gaedcke. The compound was later refined by Albert Niemann, who gave it the name "cocaine." During the late 1800s, cocaine gained significant popularity in Western medicine, primarily as a local anesthetic. Karl Koller's groundbreaking discovery of cocaine's anesthetic properties is regarded as the second most significant advance in the history of anesthesia. James Leonard Corning subsequently demonstrated its application in peridural anesthesia. Beyond medical applications, cocaine became a common ingredient in various commercial products during this period, including beverages and patent remedies. However, the compound's toxic effects and potential for abuse eventually drove the search for safer alternatives, and cocaine was gradually replaced in most medical contexts by synthetic local anesthetics with more favorable safety profiles.

    1900–1920

    Before the early 1900s, American newspapers primarily portrayed addiction as the main consequence of cocaine use, depicting typical users as upper or middle class White individuals. This characterization underwent a dramatic shift in the following years. In 1914, The New York Times published an article titled "Negro Cocaine 'Fiends' Are a New Southern Menace," which portrayed Black cocaine users as dangerous and possessing superhuman abilities to withstand normally fatal wounds. This racist narrative contributed to the social climate surrounding early drug legislation. The federal government instituted national drug labeling requirements for cocaine and cocaine-containing products through the Pure Food and Drug Act of 1906. The subsequent Harrison Narcotics Tax Act of 1914 established a regulatory and licensing regime rather than outright prohibition. Notably, the Harrison Act did not recognize addiction as a treatable medical condition, thereby outlawing the therapeutic use of cocaine, heroin, or morphine for individuals suffering from dependence.

    1970–present

    Prior to World War II, large-scale coca cultivation and cocaine production had expanded beyond South America to Taiwan (then known as Formosa) and Java in the Dutch East Indies (now Indonesia). The modern cocaine boom—characterized by a sharp rise in illegal production and trafficking—began in the late 1970s and peaked during the 1980s. From the 1980s onward, the cocaine trade became dominated by centralized, hierarchical drug cartels, most notably the Medellín and Cali organizations in Colombia, along with various successors and early factions of the FARC guerrilla group. By the early 2000s, this consolidated model fragmented into a diverse network of global trafficking links, enabling South American cocaine production to supply markets across Europe, Africa, Asia, and Oceania through multiple routes. In countries where cocaine is produced illegally, an intermediate product known as cocaine paste—referred to as "poor man's cocaine"—is frequently smoked in impoverished communities. This substance is favored in these areas primarily due to its low cost and greater accessibility compared to refined cocaine, though its use poses severe health risks. Cocaine production has also contributed substantially to environmental degradation; the United Nations Office on Drugs and Crime estimated that approximately 97,622 hectares of primary forest were cleared for coca cultivation between 2001 and 2004 in the Andean region alone, causing significant habitat destruction in areas recognized as biodiversity hotspots.

    Subjective Effect Notes

    physical: The physical effects of cocaine can be broken down into several components which progressively intensify proportional to dosage.

    cognitive: The cognitive effects of cocaine can be broken down into several components which progressively intensify proportional to dosage. The general head space of cocaine is described by many as one of extreme mental stimulation, increased focus, and powerful euphoria. It contains a large number of typical stimulant cognitive effects. Although negative side effects are usually mild at low to moderate dosages, they become increasingly likely to manifest themselves with higher amounts or extended usage. This particularly holds true during the offset of the experience.

    Effect Profile

    Curated + 777 Reports
    Stimulant 6.6

    Strong euphoria with moderate stimulation and anxiety/jitters, mild focus

    Stimulation / Energy×3
    76.2 4/20
    Euphoria / Mood Lift×2
    95.9 18/20
    Focus / Productivity×2
    52.3 3/20
    Anxiety / Jitters×1
    68.9 4/20
    Catalog Erowid

    User Experiences

    Euphoria "If you have a decent size shot of good quality meth that is diluted half water half dope you will prolly get an amazing rush." Bluelight
    Stimulation "The effect of that tiny bit was so intense I couldn't sleep for 3 days (I lay there at night eyes closed for 8+ hours strait, 2 nights in a row, totally awake, mind flying like crazy trying to sleep)." Bluelight
    Anxiety/jitters "my only source of info on this was the internet on my phone so i searched google for how to properly inject meth, how to shoot up, how to hit a vein, all that stuff but i couldnt find any type of..." Bluelight

    Duration Timeline

    Bluelight
    Onset Comeup Peak Offset After Effects
    Insufflated
    1-3 minutes
    4-10 minutes
    15-30 minutes
    30 minutes - 1.0 hours
    1-3 hours
    Total: 10-90 minutes hours
    Oral
    10-30 minutes
    15-30 minutes
    30 minutes - 1.0 hours
    30 minutes - 1.0 hours
    1-3 hours
    Total: 1-1.5 hours
    Intravenous
    0-0 minutes
    1-1 minutes
    4-15 minutes
    10-19 minutes
    1-3 hours
    Total: 1-1.5 hours
    Smoked
    0-0 minutes
    1-1 minutes
    3-4 minutes
    4-15 minutes
    1-3 hours
    Total: 1-1.5 hours

    Community Effects

    TripSit
    Positive
    euphoria visual enhancement energy
    Negative
    nausea vomiting anxiety paranoia insomnia confusion psychosis addiction

    Tolerance & Pharmacokinetics

    drugs.wiki
    Half-Life
    0.7–1.5 hours
    Addiction Potential
    High. Cocaine has strong reinforcing properties with rapid tolerance within sessions, intense craving, and a well-described withdrawal/comedown characterized by dysphoria, fatigue, hypersomnia/insomnia, and irritability.

    Tolerance Decay

    Full tolerance 6h Half tolerance 3d Baseline ~14d

    Marked acute tachyphylaxis within a session; compulsion to redose creates binge patterns. Subjective tolerance tends to decline substantially over 3–7 days and approaches baseline by ~1–2 weeks in many users. Numbers are approximate and reflect anecdotal/clinical synthesis rather than formal PK/PD studies.

    Cross-Tolerances

    Other stimulants (amphetamines, cathinones)
    30% ●○○

    Experience Report Analysis

    Erowid BlueLight
    665 Reports
    1991–2024 Date Range
    112 With Age Data
    32 Effects Detected

    Demographics

    Gender Distribution

    Age Distribution

    Reports Over Time

    Effect Analysis

    Erowid + Bluelight

    Effects aggregated from 715 experience reports (665 Erowid + 112 Bluelight)

    715 Reports
    136 Effects Detected
    43 Positive
    64 Adverse
    29 Neutral

    Effect Sentiment Distribution

    Confidence Distribution

    Positive Effects 43

    Euphoria 40.8% 90%
    Stimulation 39.0% 88%
    Thought Acceleration 36.0% 82%
    Sociability Enhancement 32.0% 86%
    Empathy 25.9% 85%
    Music Enhancement 16.0% 80%
    Tactile Enhancement 14.6% 70%
    Contentment 14.0% 81%
    Focus Enhancement 11.0% 85%
    Joy 10.0% 87%
    Body High 7.8% 83%
    Visual Clarity 6.0% 77%
    Clarity 6.0% 78%
    Libido Enhancement 6.0% 78%
    Orgasm Enhancement 6.0% 73%
    Color Enhancement 5.5% 90%
    Thought Deceleration 4.0% 80%
    Confidence Boost 4.0% 82%
    Pain Relief 3.4% 75%
    Introspection 3.3% 85%

    Adverse Effects 64

    Anxiety 38.7% 82%
    Body Load 24.0% 78%
    Tremor 22.0% 86%
    Confusion 19.7% 81%
    Dry Mouth 18.0% 79%
    Paranoid Ideation 16.0% 84%
    Insomnia 16.0% 87%
    Body Temperature Change 14.0% 79%
    Dizziness 12.0% 81%
    Fear 12.0% 85%
    Nausea 10.9% 77%
    Paranoia 10.0% 89%
    Dysphoria 10.0% 81%
    Panic 8.0% 85%
    Entity Imagery 8.0% 81%
    Thought Disorganization 8.0% 76%
    Depersonalization 8.0% 85%
    Increased Heart Rate 7.8% 70%
    Headache 7.2% 78%
    Sweating 6.6% 89%

    Dose-Response Correlation

    How effect frequency changes across dose levels

    View data table
    Effect Heavy (n=77)
    Euphoria 53.2%
    Anxiety 46.8%
    Stimulation 45.5%
    Music Enhancement 24.7%
    Tactile Enhancement 23.4%
    Empathy 22.1%
    Confusion 20.8%
    Sedation 18.2%
    Focus Enhancement 16.9%
    Visual Distortions 11.7%
    Body High 11.7%
    Increased Heart Rate 11.7%
    Hospital 11.7%
    Nausea 10.4%
    Auditory Effects 10.4%

    Subjective Effect Ontology

    Experience Reports

    Structured effect tags extracted from 777 Erowid & Bluelight experience reports using a controlled vocabulary of 220+ canonical effects across 15 domains.

    Auditory

    music enhancement 114 14.8%

    Cognitive

    confusion 141 19.4%

    Emotional

    euphoria 292 42.2% anxiety 277 37.8% empathy 185 24.0%

    Motor

    stimulation 279 41.9% sedation 110 14.6%

    7 unique effects extracted · Derived from Erowid & Bluelight reports

    Dose–Effect Mapping

    Experience Reports

    How reported effects shift across dose tiers, based on 665 experience reports.

    Limited tier coverage — most reports fall within the Heavy range. Effects at other dose levels may not be represented.

    Insufflated dose range: 500.0–2000.0 mg (median 1000.0 mg)
    Effect Heavy (n=77)
    euphoria
    53%
    anxiety
    47%
    stimulation
    46%
    music enhancement
    25%
    tactile enhancement
    23%
    empathy
    22%
    confusion
    21%
    sedation
    18%
    focus enhancement
    17%
    visual distortions
    12%
    body high
    12%
    increased heart rate
    12%
    hospital
    12%
    nausea
    10%
    auditory effects
    10%
    memory suppression
    9%
    dissociation
    9%
    jaw clenching
    9%
    sweating
    8%
    closed-eye visuals
    8%

    Showing top 20 of 32 effects

    Dosage Distribution

    Dose distribution from experience reports

    Median: 1000.0 mg IQR: 500.0–2000.0 mg n=79

    Real-World Dose Distribution

    62K Doses

    From 434 individual dose entries

    Insufflated (n=138)

    Median: 500.0mg 25th: 250.0mg 75th: 1000.0mg 90th: 2500.0mg
    mg/kg median: 8.616 mg/kg 75th: 18.718

    Intravenous (n=24)

    Median: 250.0mg 25th: 125.0mg 75th: 425.0mg 90th: 570.0mg
    mg/kg median: 2.876 mg/kg 75th: 6.484

    Oral (n=6)

    Median: 250.0mg 25th: 145.0mg 75th: 287.5mg 90th: 400.0mg
    mg/kg median: 3.556 mg/kg 75th: 3.556

    Smoked (n=7)

    Median: 100.0mg 25th: 87.5mg 75th: 493.75mg 90th: 880.0mg
    mg/kg median: 1.764 mg/kg 75th: 7.209

    Common Combinations

    Most co-occurring substances in experience reports

    Form / Preparation

    Most common forms and preparations reported

    Body-Weight Dosing

    Dose relative to body weight from reports with weight data

    Insufflated

    Median: 11.601 mg/kg IQR: 6.485–30.06 mg/kg n=75

    Intravenous

    Median: 3.243 mg/kg IQR: 2.32–6.485 mg/kg n=9

    Redose Patterns

    Redosing behavior across 533 reports

    10.5% Redosed
    1.1 Avg Doses
    40m Median Interval

    Legal Status

    Single Convention on Narcotic Drugs 1961 United Nations Convention Against Illicit Traffic in Narcotic Drugs and Psychotropic Substances
    Country Status Notes
    Australia Schedule 8 (Poisons Standard) Controlled drug requiring prescription for medical use. In Western Australia, the Misuse of Drugs Act 1981 specifies threshold quantities: 4.0 grams determines court of trial jurisdiction, 2.0 grams creates presumption of intent to supply, and 28.0 grams constitutes trafficking.
    Bolivia Coca leaf legal; refined cocaine prohibited Coca cultivation for traditional indigenous consumption is protected under the Bolivian Cato accord, which specifies allowable annual yields for farmers. Coca leaves may be chewed or consumed as tea. Production, distribution, and consumption of refined cocaine remain criminal offenses.
    Canada Controlled (prescription medical use permitted) Cocaine hydrochloride pharmaceutical preparations are available for legitimate medical purposes. Topical solutions have been marketed since the 1990s for clinical applications. Recreational possession, production, and distribution remain prohibited.
    Colombia Coca leaf legal; refined cocaine prohibited Cultivation of coca leaf is permitted for traditional consumption by indigenous populations. Manufacturing, trafficking, and recreational use of cocaine are prohibited under national drug control legislation.
    Peru Coca leaf legal; refined cocaine prohibited Traditional coca leaf consumption is permitted, including chewing and preparation as tea. The National Coca Company, a state enterprise, produces and sells coca-based teas and medicinal products, and exports leaves internationally for pharmaceutical use. However, production, sale, and recreational consumption of refined cocaine are illegal.
    United States Schedule II (Controlled Substances Act) Classified as having high abuse potential with accepted medical uses. The 1970 Controlled Substances Act regulates manufacture, importation, possession, and distribution. Medical cocaine products remain available for topical anesthesia, including Goprelto (approved December 2017) and Numbrino (approved January 2020). Historical legislation includes the Harrison Narcotics Tax Act of 1914, which established licensing requirements, and the Jones-Miller Act of 1922, which imposed manufacturing restrictions. The Anti-Drug Abuse Act of 1986 created significant sentencing disparities between powder and crack cocaine.

    Harm Reduction

    drugs.wiki

    - Alcohol + cocaine forms cocaethylene in the liver, which lasts longer than cocaine and is more cardiotoxic; this combo has been linked to higher rates of sudden death and stroke versus cocaine alone. Avoid co-use and beware delayed toxicity if alcohol was consumed earlier in the day.

    - Fentanyl and other potent opioids have been repeatedly detected in white powders sold as cocaine in some regions; this has caused clusters of opioid overdoses among stimulant users. Never assume stimulant-only; avoid mixing with opioids, carry naloxone where legal, and test if drug checking is available.

    - Levamisole, phenacetin, local anesthetics (lidocaine/procaine/benzocaine), and caffeine are common adulterants. Levamisole can cause agranulocytosis and vasculitis; seek medical care for fevers, mouth sores, or skin lesions. Drug checking services frequently report these cuts.

    - Snorting care: finely crush, use your own clean straw or single-use tool, rinse with sterile/saline water before and after, rotate nostrils, and take breaks to reduce septal damage and infections, including BBV transmission via microbleeds. Avoid banknotes.

    - High cardiovascular strain (tachycardia, hypertension, vasospasm) and overheating are key acute risks. Avoid strenuous activity/overheating, especially during binges; seek urgent care for chest pain, severe headache, confusion, or hyperthermia. Clinical guidance emphasizes external cooling and supportive care for toxicity.

    - Beta-blockers: do not self-medicate. The old warning about “unopposed alpha” is debated; mixed alpha/beta agents (e.g., labetalol) are used in clinical settings, but nonselective beta-blockers can be problematic. If prescribed beta-blockers, discuss stimulant use with a clinician.

    - Serotonergic medicines (SSRIs/SNRIs, tramadol, MAOIs) can increase risk of serotonin toxicity; MAOIs are particularly hazardous with stimulants. Treat all serotonergic combinations as higher risk and avoid MAOIs entirely.

    - IV use markedly increases risk of arrhythmia, infection, and overdose. If injecting, sterile equipment, sterile water, skin cleaning, and safe disposal are essential; consider alternative routes to reduce harm.

    - Smoking applies to crack/freebase only; use proper glass stems and heat-resistant screens to reduce burns and inhalation of toxic plastics. Avoid plastic pens/foil. HR orgs advise dedicated safer-smoking equipment.

    - Sleep loss and repeated redosing amplify anxiety/paranoia and crash severity. Plan limits for dose/stop time, hydrate with modest fluids and electrolytes, eat light food, and schedule recovery sleep.

    - Pregnancy/breastfeeding: cocaine passes into breast milk and has caused infant toxicity; complete avoidance is advised.

    - Mixing with ketamine is increasingly reported in nightlife settings; the combination can complicate emergencies and adds cardiovascular and dissociative risks—treat as unsafe.

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