Cocaine

Cocaine
The skeletal formula of Cocaine.
Chemical Nomenclature
Common names	Cocaine, Coke, Crack
Substitutive name	Blow, Snow, Nose Candy, 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
Insufflated Dosage WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section. DISCLAIMER: PW's dosage information is a summary of data gathered from users and resources. It is NOT a recommendation and should be verified with other sources for accuracy. Duration Total 10 - 60 minutes

Summary sheet: Cocaine

Cocaine (benzoylmethylecgonine) is a crystalline tropane alkaloid that is obtained from the leaves of the coca plant. The name comes from "coca" and the alkaloid suffix "-ine", forming "cocaine". This substance has short-lived effects which result in the substance being classed as a stimulant, an appetite suppressant and an anaesthetic. It is markedly more dangerous than other CNS stimulants, including the entire amphetamine drug class, at high doses as it can cause sudden cardiac death.

According to a 2007 United Nations report, cocaine is the second most widely used illicit substance in the world behind 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 derivative of ecgonine, a tropane alkaloid found in coco leaves. It is the methyl ester of benzoylecgonine. It is produced as a hydrochloride salt in its powdered form. The freebase form is commonly known as crack.

The chemical structure of cocaine consists of three parts; the hydrophilic ester group and the lipophilic carboxylic acid group are both joined by an aliphatic group. This structure allows for its rapid absorption through the blood-brain barrier. Cocaine is structurally similar to atropine and hyoscine.

Pharmacology

The most extensively studied effect of cocaine on the central nervous system is the blockade of the dopamine transporter protein's function. 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 neurones. The result is an enhanced and prolonged post-synaptic effect of dopaminergic signaling at dopamine receptors on the receiving neuron. To a lesser extent, cocaine also exhibits functionally similar effects of reuptake inhibition upon the neurotransmitters of serotonin and noradrenaline. It is this flood of neurotransmitters that causes cocaine’s characteristic high.

Subjective effects

The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. The listed effects will rarely (if ever) occur all at once, but heavier dosages will increase the chances and are more likely to induce a full range of effects.

Physical effects

The physical effects of cocaine can be broken down into several components which progressively intensify proportional to dosage. These are described below and generally include:

• Increased heart rate
• Stimulation - In terms of its effects on the physical energy levels of the user, cocaine is usually considered to be extremely energetic and stimulating in a fashion that is comparatively weaker than amphetamine or methamphetamine, but stronger than that of modafinil, caffeine, and methylphenidate. It is similar yet distinct from the stimulation experienced on MDMA, encouraging physical activities such as dancing, socializing, running, or cleaning. 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 motor control. This effect is replaced with mild fatigue and general exhaustion during the offset of the experience.
• Abnormal heartbeat - This substance consistently raises one's heart rate to abnormally high levels which can be potentially dangerous with prolonged or extremely high dosages.
• Dehydration
• Sublingual numbing
• Appetite suppression
• Pain relief
• Vasoconstriction
• Temporary erectile dysfunction
• Bronchodilation
• Increased perspiration
• Increased blood pressure

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:

• Thought acceleration
• Focus enhancement - This component is most effective at low to moderate dosages as anything higher will usually impair concentration.
• Ego inflation
• Wakefulness
• Disinhibition
• Motivation enhancement
• Euphoria
• Anxiety
• Depression
• Irritability
• Compulsive redosing
• Cognitive fatigue - This component can occur during the offset of this compound as a rebound effect which is usually equal in its intensity to the enhancements which occurred before it.

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 tealight, and a cigarette lighter. The spoon is held over the heat source in order to "cook" the cocaine into crack.

• 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 is quite soluble in water.
• Basic: As the name implies, “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 to be unusable for sublingual usage and insufflation.
• Crack: Crack is 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 addicting) quite rapidly–- this initial crescendo 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 powers.

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.

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.

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

Tolerance develops rapidly in cocaine abuse, so periods of extended use require increasing doses of the drug in order to achieve the same effect. Addiction is also a serious risk with heavy recreational cocaine use.

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 schizophrenia patients and feel that their mind is lost. 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.

Dangerous interactions

Although many drugs are safe on their own, they can become dangerous and even life-threatening when combined with other substances. The list below contains some common potentially dangerous combinations, but may not include all of them. Certain combinations may be safe in low doses of each but still increase the potential risk of death. Independent research should always be done to ensure that a combination of two or more substances is safe before consumption.

• 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.
• 25x-NBOMe - Both the NBOMe series and cocaine induce powerful stimulation. Side effects such as thought loops, seizures, increased blood pressure, vasoconstriction, increased heart rate, and heart failure (in extreme cases) may occur.
• Alcohol - When used in conjunction with alcohol, a portion of the cocaine undergoes transesterification with ethanol rather than undergoing hydrolysis with water which results in the production of cocaethylene. This creates significant changes in subjective effects such as a longer duration and increased euphoria. Some studies suggest, however, that this could potentially increase the cardiotoxic effects of cocaine to dangerous and unpredictable levels. It is also dangerous to combine alcohol, a depressant, with stimulants due to the risk of excessive intoxication. Stimulants decrease the sedative effect of alcohol which is the main factor most people consider when determining their level of intoxication. Once the stimulant wears off, the effects of alcohol will be significantly increased, leading to intensified disinhibition as well as other effects. If combined, one should strictly limit themselves to only drinking a certain amount of alcohol per hour.
• DXM - This combination may cause increased heart rate and panic attacks (in extreme cases).
• MXE - Increased heart rate and blood pressure may occur.
• Tramadol - This combination can increase the risk of seizures.
• MDMA - The neurotoxic effects of MDMA may be increased when combined with cocaine.
• 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.

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.

Legal issues

• Nigeria: It is a crime to be seen with cocaine.
• South Africa: It is a crime to have cocaine in your possession.
• Canada: Cocaine is a Schedule I drug under the Controlled Drugs and Substances Act of Canada.
• USA: Cocaine is classified as a Schedule II Narcotic under the Controlled Substances Act of the United States.
• 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.
• 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.
• 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 criminal offense.
• 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.
• 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.
• 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.
• Pakistan: Use and possession of cocaine is illegal.
• Singapore: Possession of more than 30 grams of cocaine results in a mandatory death sentence, but can be issued by the Department of Health.
• 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.
• 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.
• Germany: Possession of cocaine without a medical prescription is illegal. Small amounts for self-consumption may go unpunished for first time or non-regular offenders. This also varies by state. Usually revocation of a driving license will follow up confiscation of any drug except marijuana, since drug users are considered a risk to road traffic.
• Switzerland: Personal use of cocaine is sentenced by a fine. Trafficking is sentenced by jail.
• 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.
• Australia: Cocaine is a Schedule 8 (controlled) drug permitting some medical use, but is otherwise outlawed.
• 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.

See also

• Responsible use
• Stimulants
• Tropane alkaloids
• Cocaine (Wikipedia)
• Cocaine (Erowid)