|Summary sheet: Cocaine|
|Common names||Cocaine, Coke, Crack, Blow, Girl, White, Snow, "Nose Candy"|
|Systematic name||Methyl (1R,2R,3S,5S)-3- (Benzoyloxy)-8-methyl-8-azabicyclo[3.2.1] octane-2-carboxylate|
|Chemical class||Tropane alkaloid|
|Routes of Administration|
Cocaine (also known as benzoylmethylecgonine, and popularly as coke, snow, blow, white, and many others) is a central nervous system (CNS) stimulant substance of the benzoic acid ester class. Notable effects include stimulation, appetite suppression, local anesthesia, and euphoria.
Cocaine is a tropane alkaloid extracted from the leaves of the coca plant. The name comes from "coca" and the alkaloid suffix "-ine", forming "cocaine". It is thought to be markedly more dangerous than other CNS stimulants, including the entire amphetamine drug class. Regular use has been linked to the development of permanent heart conditions and at high doses it can cause sudden cardiac death.
- 1 Chemistry
- 2 Pharmacology
- 3 Subjective effects
- 4 Common usage
- 5 Forms
- 6 Toxicity and harm potential
- 7 Legal status
- 8 See also
- 9 External links
- 10 References
Cocaine is a tropane alkaloid found in the leaves of the coca plant, Erythroxylum coca. It is most commonly consumed as the hydrochloride salt which is typically produced in clandestine laboratories. Cocaine decomposes when heated strongly so the freebase and hydrogen carbonate salts of cocaine, which have much lower boiling points compared to the hydrochloride salt, are typically used when the substance is to be vaporized and are known as cocaine base and crack respectively.
The chemical structure of cocaine consists of three parts; the hydrophilic methyl ester moiety and the lipophilic benzoyl ester moiety, which are located in place of the carboxylic acid and hydroxyl groups of ecgonine respectively. This structure allows for its rapid absorption through nasal membranes and blood-brain barrier.
The presence of the two ester groups makes cocaine relatively unstable in warm, humid environments and cocaine stored in an open container or with a high moisture content will lose apparent potency over time due to hydrolysis to methyl ecgonine or benzoylecgonine.
Cocaine is structurally similar to atropine and scopolamine, which also contain the tropane moiety.
The most extensively studied effect of cocaine on the central nervous system is the blockade of the dopamine transporter. This substance acts as a reuptake inhibitor and prevents dopamine from being recycled, causing excessive amounts to build up in the synapse, or junction between neurons. The result is an enhanced and prolonged post-synaptic effect of dopaminergic signaling. To a lesser extent, cocaine also exhibits functionally similar effects of reuptake inhibition upon the neurotransmitters of serotonin and noradrenaline. It is this sudden flood of neurotransmitters that causes cocaine’s characteristic high.
The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. These effects should be taken with a grain of salt and will rarely (if ever) occur all at once, but heavier doses will increase the chances of inducing a full range of effects. Likewise, adverse effects become much more likely on higher doses and may include serious injury or death.
- Stimulation - Cocaine is reported to be extremely energetic and stimulating in a fashion that is comparatively weaker than methamphetamine, but stronger than that of amphetamine, modafinil, caffeine, and methylphenidate. The particular style of stimulation which cocaine presents can be described as encouraged at low to moderate dosages but forced at higher dosages. This means that at certain dosages, it becomes difficult or impossible to keep still as jaw clenching, involuntarily bodily shakes and vibrations become present, resulting in extreme shaking of the entire body, unsteadiness of the hands, and a general lack of fine motor control. This effect is replaced with mild fatigue and general exhaustion during the offset of the experience.
- Abnormal heartbeat - Cocaine consistently raises one's heart rate to abnormally high levels which can be potentially dangerous with prolonged or high dosages.
- Physical euphoria
- Increased heart rate
- Increased blood pressure
- Appetite suppression
- Bodily control enhancement
- Bronchodilation - This can sometimes be very apparent and can result in an inability to swallow.
- Frequent urination
- Increased bodily temperature
- Increased perspiration
- Pain relief
- Pupil dilation
- Mouth numbing
- Tactile hallucination - High doses and/or prolonged usage of certain stimulants like methamphetamine and cocaine can lead to hallucinatory sensations of bugs crawling on the surface of or underneath one’s skin. This is typically referred to as delusional parasitosis or more informally as “coke bugs”.
- Teeth grinding - This component can be considered to be less intense when compared with that of MDMA.
- Temporary erectile dysfunction
- Vasoconstriction - This can become very dangerous when combined with other vasoconstrictors, such as nicotine.
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.
The most prominent of these cognitive effects generally include:
- Analysis enhancement - This effect is usually only present at low to moderate doses.
- Anxiety suppression
- Compulsive redosing - This effect is more prevalent than with any other commonly used stimulant.
- Cognitive euphoria
- Ego inflation
- Focus enhancement - This component is most effective at low to moderate dosages as anything higher will usually impair concentration.
- Increased libido
- Increased music appreciation
- Irritability - The irritability associated with cocaine is notorious in its occassional potential intensity and is colloquialy known as "coke rage."
- Memory suppression - This effect is most prevalent in high doses and appears to mostly impact short term memory.
- Suggestibility suppression
- Motivation enhancement
- Thought acceleration
- Thought organization
- Time compression - This can be described as the experience of time speeding up and passing much quicker than it usually would when sober.
The effects which occur during the offset of a stimulant experience generally feel negative and uncomfortable in comparison to the effects which occurred during its peak. This is often referred to as a "comedown" and occurs because of neurotransmitter depletion. Its effects commonly include:
- Cognitive fatigue
- Compulsive redosing - During the offset, almost immediately once the user has come down, they may experience intense cravings for the drug.
- Motivation suppression
- Respiratory depression
- Tactile hallucination - This occurs after heavy or prolonged use and manifests as the sensation of insects crawling on one's skin.
- Thought deceleration
There are currently no anecdotal reports which describe the effects of this compound within our experience index. Additional experience reports can be found here:
Cocaine is often adulterated when sold on black markets and this can significantly alter its effects on the body. Even when adulterants are pharmacologically inactive, their combination with the long-term perishability of cocaine due to moisture can lead to vastly differing apparent potencies between dosages of cocaine, and as such, it can be challenging to determine a "typical" recreational dose. Pure cocaine is very potent and generates perceptible local anesthetic effects from 1 mg and perceptible CNS stimulation from 5-7 mg, however in recreational settings much higher doses tend to be used.
- Cocaine paste: is a crude extract of the coca leaf which contains 40% to 91% cocaine sulfate along with companion coca alkaloids and varying quantities of benzoic acid, methanol, and kerosene.
- Salts: Cocaine is a weakly alkaline compound (an "alkaloid") and can, therefore, combine with acidic compounds to form various salts. The hydrochloride (HCl) salt of cocaine is by far the most commonly encountered, although the sulfate (-SO4) and the nitrate (-NO3) are occasionally seen. Different salts dissolve to a greater or lesser extent in various solvents. The hydrochloride salt is polar in character and quite soluble in water.
- Freebase: “Freebase” is the base form of cocaine, as opposed to the salt form. It is practically insoluble in water whereas hydrochloride salt is water soluble. This prevents cocaine in its basic form from being usable for sublingual usage and insufflation. Freebase cocaine can be treated with ethers, isopropyl alcohol, and hydrochloric acid to turn it into the salt form. 
- "Crack": Crack refers to a lower purity form of freebase cocaine that is usually produced by neutralization of cocaine hydrochloride with a solution of baking soda (sodium bicarbonate, NaHCO3) and water, producing a very hard/brittle, off-white-to-brown colored, amorphous material that contains sodium carbonate, entrapped water, and other by-products as the main impurities. Smoking or vaporizing cocaine and inhaling it into the lungs produces an almost immediate "high" that can be very powerful and addictive. This initial buildup of stimulation is known as a "rush". While the stimulating effects may last for hours, the euphoric sensation is very brief, prompting the user to smoke more immediately.
- Coca leaf infusions: Coca herbal infusion (also referred to as coca tea) is used in coca-leaf producing countries as much as any herbal medicinal infusion would be elsewhere in the world. The free and legal commercialization of dried coca leaves under the form of filtration bags to be used as "coca tea" has been actively promoted by the governments of Peru and Bolivia for many years as a drink having medicinal properties. The leaves are also very widely used by native populations for a variety of purposes including the treatment of altitude sickness.
- Coca leaf chewing: Chewing the leaves with lime is also common in producing regions, which numbs the mouth and causes mild stimulation.
Toxicity and harm potential
Occasional use of cocaine rarely causes permanent or severe trouble to the body and mind. In terms of neurotoxicity (as defined by the damage or death of cells in the brain in response to over-excitation or reactive oxidation caused by drugs), cocaine does not appear to exhibit these effects unlike certain other substances such as methamphetamine. Its extended use or abuse does, however, cause short-term down regulation of neurotransmitters.
The most potentially harmful physical effects of cocaine appear to be not neurological but cardiovascular. Severe cardiac adverse events, particularly sudden cardiac death, become a serious risk at high doses due to cocaine's blocking effect on cardiac sodium channels. Moreover, long-term cocaine use may result in cocaine-related cardiomyopathy.
Regular cocaine insufflation, the most popular method of ingestion, can have extremely adverse effects on one's nostrils, nose, and nasal cavities. These include a loss of the sense of smell, nosebleeds, difficulty swallowing, hoarseness, or a chronically runny nose.
It is strongly recommended that one use harm reduction practices when using this substance.
Susceptible individuals have died from as little as 30 mg applied to mucous membranes, whereas addicts may tolerate up to 5 grams daily.
Tolerance and addiction potential
As with other stimulants, the chronic use of cocaine can be considered highly addictive with a high potential for abuse and is capable of causing psychological dependence among certain users. When addiction has developed, cravings and withdrawal effects may occur if a person suddenly stops their usage. Addiction is a serious risk with heavy recreational cocaine use but is unlikely to arise from typical medical use.
Tolerance to many of the effects of cocaine develops with prolonged and repeated use. This results in users having to administer increasingly large doses to achieve the same effects. After that, it takes about 3 - 7 days for the tolerance to be reduced to half and 1 - 2 weeks to be back at baseline (in the absence of further consumption). Cocaine presents cross-tolerance with all dopaminergic stimulants, meaning that after the consumption of cocaine all stimulants will have a reduced effect.
After taking cocaine on a regular basis, some users will become addicted. When the drug is discontinued immediately, the user will experience what has come to be known as a "crash" along with a number of other cocaine withdrawal symptoms including paranoia, depression, anxiety, itching, mood swings, irritability, fatigue, insomnia, an intense craving for more cocaine, and, in some cases, nausea and vomiting. Some cocaine users also report having similar symptoms to schizophrenic patients and feel that their mind is scattered or incoherent. Some users also report a feeling of a crawling sensation on the skin also known as "coke bugs".
These symptoms can last for weeks or, in some cases, months. Even after most withdrawal symptoms dissipate most users feel the need to continue using the drug; this feeling can last for years and may peak during times of stress. About 30-40% of cocaine addicts will turn to other substances such as medication and alcohol after giving up cocaine.
Cocaine has a similar potential to induce temporary psychosis with more than half of cocaine abusers reporting at least some psychotic symptoms at some point. Typical symptoms of sufferers include paranoid delusions that they are being followed and that their drug use is being watched accompanied by hallucinations that support the delusional beliefs. Delusional parasitosis with formication ("cocaine bugs") is also a fairly common symptom.
Cocaine-induced psychosis shows sensitization toward the psychotic effects of the drug. This means that psychosis becomes more severe with repeated intermittent use.
Although many psychoactive substances are safe to use on their own, they can quickly become dangerous or even life-threatening when combined with other substances. The following lists some known dangerous combinations, but may not include all of them. A combination that appears to be safe in low doses can still increase the risk of injury or death. Independent research should always be conducted to ensure that a combination of two or more substances is safe to consume.
- 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 - Because depressants counteract some of the physical effects of cocaine (and vice-versa), the combination can lead users to underestimate the extent of their intoxication and consume larger doses than they otherwise would. Cocaine and opioids is a particularly dangerous combination because cocaine has a short half-life relative to most opioid drugs and as the effects of cocaine wear off, physical side-effects of the opioid can increase resulting in a delayed overdose with serious respiratory depression being a potentially fatal risk.
- 25x-NBOMe & 25x-NBOH - Members of the 25x family are highly stimulating and physically straining. Combinations with stimulants should be avoided due to the risk of excessive stimulation. This can result in panic attacks, thought loops, seizures, increased blood pressure, vasoconstriction, and heart failure in extreme cases.
- Alcohol - Alcohol can be dangerous to combine with stimulants due to the risk of accidental over-intoxication. Stimulants mask the sedative effects of alcohol, which is the main factor people use to assess their degree of intoxication. Once the stimulant wears off, the depressant effects of alcohol are left unopposed, which can result in blackouts and respiratory depression. If combined, one should strictly limit themselves to only drinking a certain amount of alcohol per hour.
- DXM - Combinations with DXM should be strictly avoided due to DXM's effects on serotonin and dopamine reuptake. This can lead to panic attacks, hypertensive crisis, or serotonin syndrome.
- MXE - Combinations with MXE may dangerously elevate blood pressure and increase the risk of psychosis.
- Tramadol - Tramadol lowers the seizure threshold. Combinations with stimulants may further increase this risk.
- MDMA - The neurotoxic and cardiotoxic effects of MDMA may be increased when combined with cocaine. Additionally, the administration of cocaine before MDMA is reported to decrease its subjective effects and intensity. This is likely because both need to bind to the same reuptake transporters to produce their effects.
- MAOIs - This combination may increase the amount of neurotransmitters such as dopamine to dangerous or even fatal levels. Examples include syrian rue, banisteriopsis caapi, 2C-T-2, 2C-T-7, αMT, and some antidepressants.
- 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.
- Australia: Cocaine is a Schedule 8 (controlled) drug permitting some medical use, but is otherwise outlawed.
- Austria: Cocaine is illegal to possess, produce and sell under the SMG (Suchtmittelgesetz Österreich)..
- Bolivia: Limited cultivation of coca is legal in Bolivia, where chewing the leaves and drinking coca tea are considered cultural practices, in particular, in the mountainous regions. Processed cocaine is illegal.
- Brazil: Cocaine is often sold openly in stores, but it still remains illegal. In most cases, the stores will pay off the police to look the other way.
- Canada: Cocaine is a Schedule I drug under the Controlled Drugs and Substances Act of Canada.
- Colombia: In 1994, possession of 1 gram of cocaine was legalized for personal use. Sale remains illegal, but personal production or gifts of cocaine are permitted.
- Germany: Possession of cocaine without a medical prescription is illegal. Small amounts for self-consumption may go unpunished for the first time or non-regular offenders. This also varies by state. Usually, revocation of a driving license will follow up the confiscation of any drug except marijuana, since drug users are considered a risk to road traffic.
- Hong Kong: Use and possession of cocaine is illegal unless a license was issued by the Department of Health.
- India: Use and possession of cocaine is illegal with a mandatory 10-year sentence.
- Lithuania: Cocaine is a schedule I substance. Possession, production, and trade are not allowed.
- Mexico: As of August 25, 2009, the Mexican legislature officially legalized small doses of cocaine, heroin, marijuana, crystal meth, and ecstasy for personal use. No action will be taken for those carrying up to half a gram of cocaine.
- Netherlands: Cocaine is considered an illegal hard drug. Possession, production, and trade are not allowed as stated in the Opium Law of 1928. Although technically illegal, possession of less than half a gram usually goes unpunished.
- New Zealand: Cocaine is a Class A drug. The coca leaf and preparations of cocaine containing no more than 0.1% cocaine base, in such a way that the cocaine cannot be recovered, are both classified as Class C.
- Nigeria: It is a crime to be seen with cocaine.
- Pakistan: Use and possession of cocaine is illegal.
- Peru: Cultivation of coca plants is legal and coca leaves are sold openly on markets. Similarly to Bolivia, chewing leaves and drinking coca tea belong to cultural practices. Possession of up to 2 grams of cocaine or up to 5 grams of cocaine basic paste is legal for personal use in Peru per Article 299 of Peruvian Penal Code. However, the reality of how police treats it might be very different. An important part of Article 299 is that person may not possess two or more kinds of drugs at the same time -- this would make it a criminal offense.
- Portugal: Personal use of cocaine is decriminalized. Drug abuse is dealt with by administrative and medical intervention. Trafficking is illegal.
- Saudi Arabia: Use and possession of cocaine is punishable by death.
- Singapore: Possession of more than 30 grams of cocaine results in a mandatory death sentence, but can be issued by the Department of Health.
- South Africa: It is a crime to have cocaine in your possession.
- Switzerland: Personal use of cocaine is sentenced to a fine. Trafficking is sentenced to jail.
- United Kingdom: Cocaine is a Class A drug, controlled by the Misuse of Drugs Act 1971. However, medical use by doctors for controlling pain is permitted.
- United States: Cocaine is classified as a Schedule II Narcotic under the Controlled Substances Act of the United States.
- Barnett G, Hawks R, Resnick R (1981). "Cocaine pharmacokinetics in humans". J Ethnopharmacol. 3 (2–3): 353–66. PMID 7242115. https://doi.org/10.1016/0378-8741(81)90063-5.
- Jeffcoat AR, Perez-Reyes M, Hill JM, Sadler BM, Cook CE (1989). "Cocaine disposition in humans after intravenous injection, nasal insufflation (snorting), or smoking". Drug Metab. Dispos. 17 (2): 153–9. PMID 2565204.
- Aggrawal, Anil (1995). Narcotic Drugs. National Book Trust, India. pp. 52–3. ISBN 978-81-237-1383-0.
- Development of a rational scale to assess the harm of drugs of potential misuse | http://www.thelancet.com/journals/lancet/article/PIIS0140-6736(07)60464-4/fulltext
- Role of voltage-gated sodium, potassium and calcium channels in the development of cocaine-associated cardiac arrhythmias | http://onlinelibrary.wiley.com/doi/10.1111/j.1365-2125.2010.03629.x/abstract
- Amphetamine-type central nervous system stimulants release norepinephrine more potently than they release dopamine and serotonin | http://onlinelibrary.wiley.com/doi/10.1002/1098-2396(20010101)39:1%3C32::AID-SYN5%3E3.0.CO;2-3/abstract
- Morani, Aashish S.; Vikram Panwar; Kenneth Grasing (2013). "Tactile Hallucinations with Repetitive Movements Following Low‐Dose Cocaine: Implications for Cocaine Reinforcement and Sensitization". The American Journal on Addictions. 22 (2): 181–182. doi:10.1111/j.1521-0391.2013.00336.x. PMID 23414508. | https://www.ncbi.nlm.nih.gov/pubmed/23414508
- Coke Rage (Urban Dictionary) - http://www.urbandictionary.com/define.php?term=Coke+Rage
- Can freebase cocaine be converted back to powder?|https://www.erowid.org/ask/ask.php?ID=3151
- Development of a rational scale to assess the harm of drugs of potential misuse (ScienceDirect) | http://www.sciencedirect.com/science/article/pii/S0140673607604644
- Cocaine study that got up the nose of the US | http://www.theguardian.com/commentisfree/2009/jun/13/bad-science-cocaine-study
- Cocaine use in Amsterdam in non-Deviant Subcultures | http://informahealthcare.com/doi/abs/10.3109/16066359409005547
- Role of voltage-gated sodium, potassium and calcium channels in the development of cocaine-associated cardiac arrhythmias | http://onlinelibrary.wiley.com/doi/10.1111/j.1365-2125.2010.03629.x/abstract
- Cocaine-Related Cardiomyopathy (Medscape) | http://emedicine.medscape.com/article/152535-overview#a2
- Brady KT, Lydiard RB, Malcolm R, Ballenger JC (1991). "Cocaine-induced psychosis". J Clin Psychiatry 52: 509–512.
- Psychosis Among Substance Users | http://www.medscape.com/viewarticle/528487_5
- Elliott, A., Mahmood, T., & Smalligan, R. D. (2012). Cocaine Bugs: A Case Report of Cocaine‐Induced Delusions of Parasitosis. The American Journal on Addictions, 21(2), 180-181. https://doi.org/10.1111/j.1521-0391.2011.00208.x
- DiSclafani, A., Hall, R. C., & Gardner, E. R. (1981). Drug-induced psychosis: Emergency diagnosis and management. Psychosomatics, 22(10), 845-855. https://doi.org/10.1176/ps.2006.57.10.1468
- Talaie, H., Panahandeh, R., Fayaznouri, M. R., Asadi, Z., & Abdollahi, M. (2009). Dose-independent occurrence of seizure with tramadol. Journal of Medical Toxicology, 5(2), 63-67. https://doi.org/10.1007/BF03161089
- Gillman, P. K. (2005). Monoamine oxidase inhibitors, opioid analgesics and serotonin toxicity. British Journal of Anaesthesia, 95(4), 434-441. https://doi.org/10.1093/bja/aei210