Cocaine

Cocaine is a powerful central nervous system stimulant made from the leaves of two coca plants that grow in South America: Erythroxylum coca and E. novogranatense. People have used coca leaves for thousands of years, but when turned into cocaine, it can have strong effects on the body and mind. It is most often used by snorting, injecting, or smoking as crack cocaine, and can make a person feel very excited, alert, and focused for up to 90 minutes.

Even though cocaine was once used as a topical medication and local anesthetic, it is very dangerous and is not used much in medicine today. Using cocaine can cause many serious health problems, such as very high blood pressure, seizures, and damage to the brain and nose. Over time, people can become dependent on it and feel very sick when they stop using it.

The growing of coca plants mostly happens in parts of Bolivia, Peru, and Colombia in Latin America, but it is also spreading to other places like Central America. The trade in cocaine has caused a lot of violence in many parts of the world, as different groups fight to control it. Even though international rules try to control cocaine, some countries allow small amounts to be kept without punishment.

Uses

Coca leaves have been used by Andean civilizations since ancient times. In ancient Wari culture, Inca culture, and through modern successor indigenous cultures of the Andes Mountains, coca leaves are chewed, taken orally in the form of a tea, or alternatively, prepared in a sachet wrapped around alkaline burnt ashes, and held in the mouth against the inner cheek; it has traditionally been used as an anorectic and to combat the effects of cold and altitude sickness, although its actual effectiveness has never been systematically studied.

Globally, in 2019, cocaine was used by an estimated 20 million people (0.4% of adults aged 15 to 64 years). The highest prevalence of cocaine use was in Australia and New Zealand (2.1%), followed by North America (2.1%), Western and Central Europe (1.4%), and South and Central America (1.0%). Since 1961, the Single Convention on Narcotic Drugs has required countries to make recreational use of cocaine a crime. In the United States, cocaine is regulated as a Schedule II drug under the Controlled Substances Act, meaning that it has a high potential for abuse but has an accepted medical use. While rarely used medically anymore, its accepted uses include serving as a topical local anesthetic for the upper respiratory tract and as an antihemorrhagic agent to stop bleeding in the mouth, throat, and nasal cavities.

Traditional medicine

Coca leaves

Main article: Coca

It is legal to use coca leaves in the Andean Community, such as Peru and Bolivia, and Argentina, where they are chewed, consumed as tea, or sometimes incorporated into food products. Coca leaves are typically mixed with an alkaline substance (such as slaked lime) and chewed into a wad that is retained in the buccal pouch (mouth between gum and cheek, much the same as chewing tobacco is chewed) and sucked of its juices. The juices are absorbed slowly by the mucous membrane of the inner cheek and by the gastrointestinal tract when swallowed.

Coca tea

Main article: Coca tea

Llipta is used to improve extraction when chewing coca (Museo de la Coca, Cusco, Peru).

Coca herbal infusion (also referred to as coca tea) is used in coca-leaf producing countries much as any herbal medicinal infusion would 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. In Peru, the National Coca Company, a state-run corporation, sells cocaine-infused teas and other medicinal products and also exports leaves to the U.S. for medicinal use. The effects of drinking coca tea are mild stimulation and mood lift.

In 1986 an article in the Journal of the American Medical Association revealed that U.S. health food stores were selling dried coca leaves to be prepared as an infusion as "Health Inca Tea". While the packaging claimed it had been "decocainized", no such process had actually taken place. The article stated that drinking two cups of the tea per day gave a mild stimulation, increased heart rate, and mood elevation, and the tea was essentially harmless.

Ypadu

Main article: Ypadu

Ypadú or ypadu (also known as mambé) is an unrefined, unconcentrated powder made from toasted coca leaves and the ash of various other plants. It is traditionally prepared and consumed by indigenous tribes in the Northwest Amazon. Like coca teas consumed in Peru to adapt to sickness induced by high elevation, it has a long ethnobotanical history and cultural associations.

Medical

Karl Koller's groundbreaking discovery of cocaine as a local anesthetic is regarded as the second most significant advance in the history of anesthesia. Although cocaine was once widely preferred for topical anesthesia, the search for replacement agents intensified due to rising costs, strict regulations, and its habit-forming potential. Cocaine is not included on the WHO Model List of Essential Medicines; the list formally excludes "cocaine and its combinations" as therapeutic alternatives to ophthalmological preparations.

The US Drug Enforcement Administration (DEA) classifies cocaine as a Schedule II drug, recognizing its high potential for abuse but still permitting its limited use for medical purposes. However, current pharmacoepidemiological trends suggest that cocaine may soon reach the point where, in practical terms, it is no longer used medically in health care as a Schedule II substance. This report may prompt some states (such as North Dakota) and institutions to reconsider whether further efforts to identify alternative agents are needed. As physician boards—but not pharmacy boards—continue to assess knowledge of licit cocaine, attention may shift toward drugs with more contemporary medical use.

Cocaine is rarely prescribed in modern medicine due to its high potential for abuse and significant risk of adverse effects; its use is almost exclusively limited to health facilities for specific diagnostic procedures or surgeries.

Topical

Two cups of coca tea

Cocaine is used in medical practice as a topical medication. Because it is not absorbed into the bloodstream in significant amounts when used this way, topical application does not produce the psychoactive effects associated with recreational cocaine use.

Topical anesthetic

Ophthalmological use

Cocaine eye drops have traditionally been used by neurologists when examining people suspected of having Horner syndrome. In Horner syndrome, sympathetic innervation to the eye is blocked. In a healthy eye, cocaine stimulates the sympathetic nervous system (SNS) by inhibiting norepinephrine reuptake, causing the pupil to dilate. In patients with Horner syndrome, sympathetic innervation to the eye is disrupted, so the affected pupil does not dilate in response to cocaine and remains constricted, or dilates to a lesser extent than the unaffected eye, which also receives the eye drop test. If both eyes dilate equally, the patient does not have Horner syndrome.

However, apraclonidine has largely replaced cocaine as the first-line pharmacologic agent for the diagnosis of Horner syndrome in routine clinical practice.

Recreational

For Cocaine or crack cocaine combined with other drugs, see List of polysubstance combinations.

Mambe or ypadu is made from toasted and ground coca leaves with ashes

Recreational cocaine is typically not taken by mouth due to its poor bioavailability, instead it is usually snorted or injected. Cocaine hydrochloride can also be chemically converted into its free base form, crack cocaine, which can be vaporized.^{[citation needed]}

Cocaine is a central nervous system stimulant. Its effects can last from 15 minutes to an hour. The duration of cocaine's effects depends on the amount taken and the route of administration. Cocaine can be in the form of fine white powder and has a bitter taste. Crack cocaine is a smokeable form of cocaine made into small "rocks" by processing cocaine with sodium bicarbonate (baking soda) and water.

Cocaine use leads to increases in alertness, feelings of well-being and euphoria, increased energy and motor activity, and increased feelings of competence and sexuality.

Analysis of the correlation between the use of 18 various psychoactive substances shows that cocaine use correlates with the use of other "party drugs" (e.g., MDMA, amphetamine), as well as with heroin and benzodiazepines use, and can be considered as a bridge between the use of different groups of drugs.

Insufflation

Nasal insufflation (known colloquially as "snorting", "sniffing", or "blowing") is a common method of ingestion of recreational powdered cocaine. The drug coats and is absorbed through the mucous membranes lining the nasal passages. Cocaine's desired euphoric effects are delayed when snorted through the nose by about five minutes. This occurs because cocaine's absorption is slowed by its constricting effect on the blood vessels of the nose. Insufflation of cocaine also leads to the longest duration of its effects (60–90 minutes). When insufflating cocaine, absorption through the nasal membranes is approximately 30–60%

Most banknotes have traces of cocaine on them; this has been confirmed by studies done in several countries. In 1994, the US 9th Circuit Court of Appeals cited findings that in Los Angeles, three out of four banknotes were tainted by cocaine or another illicit drug.

Snuff spoons, hollowed-out pens, cut straws, pointed ends of keys, long fingernails or artificial nails, and tampon applicators are also used to insufflate cocaine. The cocaine typically is poured onto a flat, hard surface and divided into "bumps", "lines", or "rails", and then insufflated. A 2001 study reported that the sharing of straws used to "snort" cocaine can spread blood diseases such as hepatitis C.

Cocaine spoon

Historically, snuff spoons were used for cocaine in the 20th century, hence the names "cocaine spoon" and "coke spoon". Some local statutes in the US treat spoons that are too small and thus "unsuited for the typical, lawful uses of a spoon" as drug paraphernalia.

Injection

Subjective effects not commonly shared with other methods of administration include a ringing in the ears moments after injection (usually when over 120 milligrams) lasting 2 to 5 minutes including tinnitus and audio distortion. This is colloquially referred to as a "bell ringer". In a study of cocaine users, the average time taken to reach peak subjective effects was 3.1 minutes. The euphoria passes quickly. Aside from the toxic effects of cocaine, there is also the danger of circulatory emboli from the insoluble substances that may be used to cut the drug. As with all injected illicit substances, there is a risk of the user contracting blood-borne infections if sterile injecting equipment is not available or used.

Inhalation

Cocaine paste

Coca paste (paco, basuco, oxi, pasta) is a crude extract of the coca leaf which contains 40% to 91% cocaine freebase along with companion coca alkaloids and varying quantities of benzoic acid, methanol, and kerosene. The caustic reactions associated with the local application of coca paste prevents its use by oral, intranasal, mucosal, intramuscular, intravenous or subcutaneous routes. Coca paste can only be smoked when combined with a combustible material such as tobacco or cannabis.

Crude cocaine preparation intermediates are marketed as cheaper alternatives to pure cocaine to local markets while the more expensive end product is exported to United States and European markets. Freebase cocaine paste preparations can be smoked. The psychological and physiological effects of the paco are quite severe. Media usually report that it is extremely toxic and addictive. According to a study by Intercambios, media appear to exaggerate the effects of paco. These stereotypes create a sense that nothing can be done to help a paco addict and thus stand in the way of rehabilitation programs.

Crack cocaine

Further information: Crack cocaine

Powder cocaine (cocaine hydrochloride) must be heated to a high temperature to be smoked (about 197 °C), and considerable decomposition/burning occurs at these high temperatures. This effectively destroys some of the cocaine and yields a sharp, acrid, and foul-tasting smoke. Cocaine base/crack can be smoked because it vaporizes with little or no decomposition at 98 °C (208 °F).

Contraindications

Cocaine should not be used by people who are allergic to it or very sensitive to its effects. It is also not safe for older adults or those who have heart problems.

Pregnancy

Using cocaine during pregnancy can be harmful to both the mother and the baby. It may increase the risk of losing the baby early in pregnancy, cause the baby to be born too early, or result in the baby being smaller than expected. Babies exposed to cocaine in the womb may face health challenges, including problems with growth and development. It is important for pregnant women to avoid cocaine to protect their health and the health of their baby.

Breastfeeding

Women who use cocaine should not breastfeed their babies. Cocaine can pass into breast milk and may harm the baby. It is best to avoid using cocaine during pregnancy and while breastfeeding to keep the baby safe.

Adverse effects

Overdose

Interactions

Alcohol

Main article: Cocaethylene

MAOIs

Monoamine oxidase inhibitors (MAOIs) should not be mixed with other drugs, including painkillers or stimulants, unless a doctor says it is safe to do so.

Opioids

These days, more people are overdosing when they use both opioids and cocaine. This is especially true for some groups, and it can be linked to things like age, where they live, and mental health challenges. It is still not clear if people always plan to use both drugs together. Recent studies look at all types of opioids, not just heroin, because overdose patterns are changing.

Pharmacology

Cocaine enters the body in different ways, such as through the nose or by mouth. When taken through the nose, it starts working quickly. When taken by mouth, it takes longer to feel the effects because the body absorbs it differently.

Cocaine can pass into the brain where it affects certain chemicals. This changes how the brain works, leading to strong feelings of energy and excitement. The effects of cocaine usually last about 40 to 60 minutes.

Cocaine can be found in the body for several days after use. Tests can detect it in blood, urine, or even hair, depending on how often someone used it. These tests help doctors and experts understand if and when someone used cocaine.

Chemistry

Forms

See also: Cocaine paste and Crack cocaine § Chemistry

Cocaine, in its purest form, looks like a white, shiny powder. It can mix with certain acids to form different types of salts. The most common one is called hydrochloride, which dissolves easily in water.

Synthesis

Total synthesis

The first time scientists figured out the exact structure of cocaine and made it in a lab was in 1898. Making cocaine this way is very difficult, expensive, and not very effective, so it is rarely done. It is much easier to get cocaine from plants.

Biosynthesis

Main article: Biosynthesis of cocaine

Plants called coca naturally make cocaine through a series of steps. Scientists find this interesting because of the unique shape of the cocaine molecule.

GMO synthesis

In 2022, scientists found that a special type of plant could make a small amount of cocaine. However, this plant also makes another chemical called nicotine, which makes it hard to separate the cocaine.

Field analysis

Sometimes, security checks will swipe items like ID cards to look for traces of drugs. Scientists tested tools used by police to find cocaine and found they often do not work well on the types of cocaine people usually find on the street. These tools can sometimes give wrong results. There are also special lab tests that can more accurately measure how pure a sample of cocaine is.

History

Main article: History of cocaine

For thousands of years, people in South America used coca leaves to help them stay awake and for healing. When the Spanish came, they first stopped the use of coca but later allowed it because it was important for local work.

In 1855, a scientist named Friedrich Gaedcke discovered the main ingredient in coca leaves and named it "cocaine." Soon after, Albert Niemann refined it. In the late 1800s, cocaine was used in medicines and drinks before doctors found safer options because of its harmful effects.

Before World War II, large amounts of coca were grown in places like Taiwan and Java. Since the 1980s, groups known as drug cartels controlled the trade of cocaine, but by the early 2000s, the trade became more spread out across the world.

Society and culture

Cocaine comes from coca plants grown in Latin America. There are different ways people get cocaine, and they have different rules about it. In places like Peru, most coca plants are used to make cocaine without following the rules. Governments try to stop this by taking away these plants.

Some sports rules say athletes cannot use cocaine. This is because it can help them perform better, and it is not allowed.

Cocaine is sometimes called by other names on the street, like "blow" or "coke." Another form of cocaine is called "crack."

The making, selling, and moving of cocaine is mostly against the law in many countries. Some places, like Bolivia, Colombia, and Peru, allow people to grow coca plants for traditional uses, but they still cannot make or sell cocaine from them.

In Australia, cocaine is a controlled drug. In the United States, there have been many laws over the years to control cocaine. These laws started in 1906 and have changed a lot since then.

In 2023, the use and making of cocaine reached new high levels around the world. The United States uses the most cocaine, while South America and Europe also use a lot.

Cocaine growing can hurt the environment. Forests are cut down to grow coca plants, and harmful chemicals are used that can hurt animals and plants. This can damage the land and make it hard for other plants and animals to live.

The effort to stop coca growing can also cause problems. In some places, chemicals are sprayed from planes to kill the plants, but this can make people and animals sick. Sometimes the wrong fields are sprayed, which can ruin farmers' crops and land.

The word cocaine comes from French, which got it from Spanish, and finally from an ancient South American language called Quechua.

Research

Cocaine can be changed into special forms that help the body make antibodies against it. These antibodies can catch cocaine in the blood and stop it from affecting the brain.

Scientists have studied an enzyme called cocaine esterase as a possible way to treat addiction to cocaine. They have also looked at using coca tea, made from coca leaves, as a supportive treatment. Research in Lima, Peru, showed that combining coca tea with counseling helped people stay away from cocaine for longer periods.

Studies in animals have shown that using nicotine or alcohol can make it more likely that they will later use cocaine. These findings match what we see in humans, where using nicotine or alcohol can increase the risk of using cocaine and other substances.

Cocaine vaccines

Calixcoca

Main article: Calixcoca

Calixcoca is an experimental vaccine being developed since 2015 to help treat addiction to cocaine and crack cocaine. It is being created by the Federal University of Minas Gerais in Brazil.

TA-CD

Main article: TA-CD

TA-CD is another vaccine made to stop the effects of cocaine. It was developed by the Xenova Group and works by combining a substance called norcocaine with an inactivated cholera toxin.