Cocaine

Summary sheet: Cocaine

Cocaine
Chemical Nomenclature
Common names	Cocaine, Coke, Crack, Blow, Girl, White, Snow, "Nose Candy"
Substitutive name	Benzoylmethylecgonine
Systematic name	Methyl (1R,2R,3S,5S)-3- (Benzoyloxy)-8-methyl-8-azabicyclo[3.2.1] octane-2-carboxylate
Class Membership
Psychoactive class	Stimulant
Chemical class	Tropane alkaloid
Routes of Administration
WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section. ⇣ Inhaled Dosage Duration Total 5 - 15 minutes Onset 3 - 5 seconds Come up 1 - 2 minutes Peak 2 - 10 minutes Offset 1 - 5 minutes ⇣ Insufflated Dosage Bioavailability 60-80% Threshold 5 mg Light 10 - 30 mg Common 30 - 60 mg Strong 60 - 90 mg Heavy 90 mg + Duration Total 10 - 90 minutes Onset 1 - 10 minutes Come up 5 - 15 minutes Peak 15 - 30 minutes Offset 10 - 30 minutes DISCLAIMER: PW's dosage information is gathered from users and resources for educational purposes only. It is not a recommendation and should be verified with other sources for accuracy.
Interactions
Mushrooms
LSD
DMT
Mescaline
2C-x
Cannabis
Ketamine
MXE
Amphetamines
MDMA
Caffeine
GHB
GBL
DOx
25x-NBOMe
2C-T-x
5-MeO-xxT
DXM
PCP
Alcohol
ΑMT
Opioids
Tramadol
MAOIs

Cocaine (also known as benzoylmethylecgonine, and colloquially as coke, Cola, snow, blow, white, and many others) is a naturally-occurring stimulant substance of the tropane class. It is found as an alkaloid in the leaves of the coca plant, Erythroxylum coca. The name comes from "coca" and the alkaloid suffix "-ine", forming "cocaine".

According to a 2007 United Nations report, cocaine is the second most widely used illicit substance in the world, after cannabis. In terms of user rates, Spain is the country with the highest rate of cocaine usage (3.0% of adults in the previous year). Other countries where the usage rate meets or exceeds 1.5% are the United States (2.8%), England and Wales (2.4%), Canada (2.3%), Italy (2.1%), Bolivia (1.9%), Chile (1.8%), and Scotland (1.5%).

Subjective effects include stimulation, appetite suppression, compulsive redosing, ego inflation, increased libido, and euphoria. Cocaine is usually insufflated (snorted) and sometimes injected; oral administration is not effective. The cocaine high is characterized by a rapid onset and a short duration, which produces a strong euphoric rush followed by a marked comedown or crash.

Cocaine 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. As a result, it is highly advised to use harm reduction practices if using this substance.

History and culture

A 1000-year-old collection of drug paraphernalia found in a rock shelter in Bolivia features traces of five psychoactive chemicals, including cocaine and components of ayahuasca.

According to a 2007 United Nations report, cocaine is the second most widely used illicit substance in the world, after cannabis. In terms of user rates, Spain is the country with the highest rate of cocaine usage (3.0% of adults in the previous year). Other countries where the usage rate meets or exceeds 1.5% are the United States (2.8%), England and Wales (2.4%), Canada (2.3%), Italy (2.1%), Bolivia (1.9%), Chile (1.8%), and Scotland (1.5%).

Chemistry

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.

Pharmacology

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 pharmacodynamics of cocaine involve the complex relationships of neurotransmitters (inhibiting monoamine uptake in rats with ratios of about: serotonin:dopamine = 2:3, serotonin:norepinephrine = 2:5). The most extensively studied effect of cocaine on the central nervous system is the blockade of the dopamine transporter protein. Dopamine transmitter released during neural signaling is normally recycled via the transporter; i.e., the transporter binds the transmitter and pumps it out of the synaptic cleft back into the presynaptic neuron, where it is taken up into storage vesicles. Cocaine binds tightly at the dopamine transporter forming a complex that blocks the transporter's function. The dopamine transporter can no longer perform its reuptake function, and thus dopamine accumulates in the synaptic cleft. The increased concentration of dopamine in the synapse activates post-synaptic dopamine receptors, which makes the drug rewarding and promotes the compulsive use of cocaine.

Subjective effects

Disclaimer: The effects listed below cite the Subjective Effect Index (SEI), an open research literature based on anecdotal user reports and the personal analyses of PsychonautWiki contributors. As a result, they should be viewed with a healthy degree of skepticism.

It is also worth noting that these effects will not necessarily occur in a predictable or reliable manner, although higher doses are more liable to induce the full spectrum of effects. Likewise, adverse effects become increasingly likely with higher doses and may include addiction, severe injury, or death ☠.

Physical effects

• • 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.
  • Dehydration
  • Frequent urination
  • Increased bodily temperature
  • Increased perspiration
  • Pain relief - One of the few medical uses of cocaine is pain relief. This effect mainly comes from vasoconstriction and sodium channel blockage.
  • 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.

Cognitive effects

• 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
  • Disinhibition
  • 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."
  • Mania
  • 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.
  • Wakefulness

After effects

• 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:
  • Anxiety
  • Cognitive fatigue
  • Compulsive redosing - During the offset, almost immediately once the user has come down, they may experience intense cravings for the drug.
  • Depression
  • Irritability
  • 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

Experience reports

There are currently no anecdotal reports which describe the effects of this compound within our experience index. Additional experience reports can be found here:

• Erowid Experience Vaults: Cocaine

Common usage

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.

Forms

In order for cocaine (in plastic bag at bottom) to be converted to crack, several supplies are needed. Pictured here are baking soda (a commonly used base in making crack) a metal spoon, a tea light, and a cigarette lighter. The spoon is held over the heat source in order to "cook" the cocaine into crack.

• 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

Radar plot showing relative physical harm, social harm, and dependence of cocaine

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.

Lethal dosage

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.

Withdrawal symptoms

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.

Psychosis

Main article: Stimulant psychosis

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.

Dangerous interactions

Warning: Many psychoactive substances that are reasonably safe to use on their own can suddenly become dangerous or even life-threatening when combined with certain other substances. The following lists some known dangerous interactions (although it is not guaranteed to include all of them).

Always conduct independent research (e.g. Google, DuckDuckGo, PubMed) to ensure that a combination of two or more substances is safe to consume. Some of the listed interactions have been sourced from TripSit.

• Mushrooms - Stimulants increase anxiety levels and the risk of thought loops which can lead to negative experiences.
• LSD - Stimulants increase anxiety levels and the risk of thought loops which can lead to negative experiences.
• DMT - Stimulants increase anxiety levels and the risk of thought loops which can lead to negative experiences.
• Mescaline - The focus and anxiety caused by stimulants is magnified by psychedelics and results in an increased risk of thought loops.
• 2C-x - The anxiogenic and focusing effects of stimulants increase the chance of unpleasant thought loops. The combination is generally unnecessary because of the stimulating effects of psychedelics. Combination of the stimulating effects may be uncomfortable.
• Cannabis - Stimulants increase anxiety levels and the risk of thought loops which can lead to negative experiences.
• Ketamine - No unexpected interactions, though likely to increase blood pressure but not an issue with sensible doses. Moving around on high doses of this combination may be ill advised due to risk of physical injury.
• MXE - Stimulants taken with MXE can lead to hypermanic states much more easily, especially if sleep is avoided.
• Amphetamines - This combination of stimulants will increase strain on the heart. It is not generally worth it as Cocaine has a mild blocking effect on dopamine releasers like amphetamine.
• MDMA - Cocaine blocks some of the desirable effects of MDMA while increasing the risk of heart attack.
• Caffeine - Both stimulants, risk of tachycardia, hypertension, and in extreme cases heart failure.
• GHB - Stimulants increase respiration rate allowing a higher dose of sedatives. If the stimulant wears off first then the opiate may overcome the patient and cause respiratory arrest. Likewise the G can wear off and leave a dangerous concentration of Cocaine behind.
• GBL - Stimulants increase respiration rate allowing a higher dose of sedatives. If the stimulant wears off first then the opiate may overcome the patient and cause respiratory arrest. Likewise the G can wear off and leave a dangerous concentration of Cocaine behind.
• DOx - The combined stimulating effects of the two can lead to an uncomfortable body-load, while the focusing effects of Cocaine can easily lead to thought loops. Coming down from Cocaine while the DOx is still active can be quite anxiogenic.
• 25x-NBOMe - Cocaine and NBOMes both provide considerable stimulation. When combined they can result in severe vasoconstriction, tachycardia, hypertension, and in extreme cases heart failure.
• 2C-T-x - Cocaine and 2C-T-x both provide considerable stimulation. When combined they can result in severe vasoconstriction, tachycardia, hypertension, and in extreme cases heart failure.
• 5-MeO-xxT - The anxiogenic and focusing effects of stimulants increase the chance of unpleasant thought loops. The combination is generally unnecessary because of the stimulating effects of psychedelics.
• DXM - Both substances raise heart rate, in extreme cases, panic attacks caused by these drugs have led to more serious heart issues.
• PCP - This combination can easily lead to hypermanic states.
• Alcohol - Drinking while using stimulants is risky because the sedative effects of alcohol are reduced. These are what the body uses to gauge “drunkenness”. This typically leads to excessive drinking with greatly reduced inhibitions, high risk of liver damage and increased dehydration. They will also allow you to drink past a point where you might normally pass out, increasing the risk. If you do decide to do this then you should set a limit of how much you will drink each hour and stick to it, bearing in mind that you will feel alcohol less. Cocaine is potentiated somewhat by alcohol because of the formation of cocaethylene.
• ΑMT
• Opioids - Stimulants increase respiration rate allowing a higher dose of opiates. If the stimulant wears off first then the opiate may overcome the patient and cause respiratory arrest.
• Tramadol - Tramadol and stimulants both increase the risk of seizures.
• MAOIs - This combination is poorly explored.

Legal status

• 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: Even though possession of less than 1 gram of cocaine was legalized for personal use in 1994 by the supreme court, sale and possession are now illegal under the new nationwide police code.
• Germany: Cocaine was listed in the initial version of the Opiumgesetz (Opium Act) of December 10, 1929. In accordance to the Narcotics Act reform of 1981, it is controlled under Anlage III BtMG (Narcotics Act, Schedule III). It can only be prescribed on a narcotic prescription form. If owned illegaly, a quantity of up to 5 grams is regarded as a small amount. In these cases, the prosecution can cease the proceeding.
• 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.
• The 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: Cocaine is a controlled substance specifically named under Verzeichnis A.
• 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.

See also

• Responsible use
• Stimulant
• Tropanes
• Dichloropane

External links

• Cocaine (Wikipedia)
• Cocaine (Erowid Vault)
• Cocaine (Isomer Design)