Cocaine (or crack) is a crystalline tropane alkaloid that is obtained from the leaves of the coca plant. It is a stimulant of the central nervous system and an appetite suppressant, giving rise to what has been described as a euphoric sense of happiness and increased energy. It is most often used recreationally for this effect. Nonetheless, cocaine is formally used in medicine as a topical anesthetic, specifically in eye, nose and throat surgery.

The stimulating qualities of the coca leaf were known to the ancient peoples of Peru and other pre-Colombian Andean societies. In modern Western countries, cocaine has been a feature of the counterculture for over a century. There is a long list of prominent intellectuals, artists, politicians, and musicians who have used the drug — ranging from Sir Arthur Conan Doyle and Sigmund Freud to former U.S. President Ulysses S. Grant. At one time, cocaine could be found in trace amounts in the Coca-Cola beverage for several decades after the beverage’s release, though that is no longer the case.

Its possession, cultivation, and distribution are illegal for non-medicinal and non-government sanctioned purposes in virtually all parts of the world. The name comes from the name of the coca plant in addition to the alkaloid suffix -ine, forming Cocaine. Today, although its free commercialization is illegal and has been severely penalized in virtually all countries, its use worldwide remains widespread in many social, cultural, and personal settings.

Effects and health issues

Acute
Cocaine is a potent central nervous system stimulant. Its effects can last from 20 minutes to several hours, depending upon the dosage of cocaine taken, purity, and method of administration.

The initial signs of stimulation are hyperactivity, restlessness, increased blood pressure, increased heart rate and euphoria. The euphoria is sometimes followed by feelings of discomfort and depression and a craving to experience the drug again. Sexual interest and pleasure can be amplified. Side effects can include twitching, paranoia, and impotence, which usually increases with frequent usage.

With excessive dosage the drug can produce itching, tachycardia, hallucinations, and paranoid delusions.

Overdose causes tachyarrhythmias and a marked elevation of blood pressure. These can be life-threatening, especially if the user has existing cardiac problems.

The LD50 of cocaine when administered to mice is 95.1 mg/kg. Toxicity results in seizures, followed by respiratory and circulatory depression of medullar origin. This may lead to death from respiratory failure, stroke, cerebral hemorrhage, or heart-failure. Cocaine is also highly pyrogenic, because the stimulation and increased muscular activity cause greater heat production. Heat loss is inhibited by the intense vasoconstriction. Cocaine-induced hyperthermia may cause muscle cell destruction and myoglobinuria resulting in renal failure. There is no specific antidote for cocaine overdose.

Cocaine’s primary acute effect on brain chemistry is to raise the amount of dopamine and serotonin in the nucleus accumbens (the pleasure center in the brain); this effect ceases, due to metabolism of cocaine to inactive compounds and particularly due to the depletion of the transmitter resources (tachyphylaxis). This can be experienced acutely as feelings of depression, as a “crash” after the initial high. Further mechanisms occur in chronic cocaine use.

Studies have shown that cocaine usage during pregnancy triggers premature labor and may lead to abruptio placentae.

Chronic
Chronic cocaine intake causes brain cells to adapt functionally to strong imbalances of transmitter levels in order to compensate extremes. Thus, receptors disappear from the cell surface or reappear on it, resulting more or less in an “off” or “working mode” respectively, or they change their susceptibility for binding partners (ligands) – mechanisms called down-/upregulation. Chronic cocaine use leads to a DATS upregulation,[verification needed] further contributing to depressed mood states. Physical withdrawal is not dangerous, and is in fact restorative. The experience of insatiable hunger, aches, insomnia/oversleeping, lethargy, and persistent runny nose are often described as very unpleasant. Depression with suicidal ideation may develop in very heavy users. Finally, a loss of vesicular monoamine transporters, neurofilament proteins, and other morphological changes appear to indicate a long term damage of dopamine neurons.

All these effects contribute a rise in tolerance thus requiring a larger dosage to achieve the same effect. The lack of normal amounts of serotonin and dopamine in the brain is the cause of the dysphoria and depression felt after the initial high. The diagnostic criteria for cocaine withdrawal is characterized by a dysphoric mood, fatigue, unpleasant dreams, insomnia or hypersomnia, E.D., increased appetite, psychomotor retardation or agitation, and anxiety.

Cocaine abuse also has multiple physical health consequences. It is associated with a lifetime risk of heart attack that is seven times that of non-users. During the hour after cocaine is used, heart attack risk rises 24-fold

Side effects from chronic smoking of cocaine include chest pain, lung trauma, shortness of breath, sore throat, hoarse voice, dyspnea, and an aching, flu-like syndrome. A common misconception is that the smoking of cocaine chemically breaks down tooth enamel and causes tooth decay. However, cocaine does often cause involuntary tooth grinding, known as bruxism, which can deteriorate tooth enamel and lead to gingivitis.

Chronic intranasal usage can degrade the cartilage separating the nostrils (the septum nasi), leading eventually to its complete disappearance. Due to the absorption of the cocaine from cocaine hydrochloride, the remaining hydrochloride forms a dilute hydrochloric acid.

Cocaine may also greatly increase this risk of developing rare autoimmune or connective tissue diseases such as lupus, Goodpasture’s disease, vasculitis, glomerulonephritis, Stevens-Johnson syndrome and other diseases. It can also cause a wide array of kidney diseases and renal failure. While these conditions are normally found in chronic use they can also be caused by short term exposure in susceptible individuals.

There have been published studies[citation needed] reporting that cocaine causes changes in the frontal lobe of the brain. The full extent of possible brain deterioration from cocaine use is not known.

Cocaine as a local anesthetic

Cocaine was historically useful as a topical anesthetic in eye and nasal surgery, although it is now predominantly used for nasal and lacrimal duct surgery. The major disadvantages of this use are cocaine’s intense vasoconstrictor activity and potential for cardiovascular toxicity. Cocaine has since been largely replaced in Western medicine by synthetic local anaesthetics such as benzocaine, proparacaine, and tetracaine though it remains available for use if specified. If vasoconstriction is desired for a procedure (as it reduces bleeding), the anesthetic is combined with a vasoconstrictor such as phenylephrine or epinephrine. In Australia it is currently prescribed for use as a local anesthetic for conditions such as mouth and lung ulcers. Some ENT specialists occasionally use cocaine within the practice when performing procedures such as nasal cauterization. In this scenario dissolved cocaine is soaked into a ball of cotton wool, which is placed in the nostril for the 10-15 minutes immediately prior to the procedure, thus performing the dual role of both numbing the area to be cauterized and also vasoconstriction. Even when used this way, some of the used cocaine may be absorbed through oral or nasal mucosa and give systemic effects.

Forms of cocaine

Cocaine sulfate
Cocaine sulfate is produced by macerating coca leaves along with water that has been acidulated with sulfuric acid, or an aromatic-based solvent, like kerosene or benzene. This is often accomplished by putting the ingredients into a vat and stamping on it, in a manner similar to the traditional method for crushing grapes. After the maceration is completed, the water is evaporated to yield a pasty mass of impure cocaine sulfate.

The sulfate salt itself is an intermediate step to producing cocaine hydrochloride. In South America, it is commonly sold to consumers as such, and smoked along with tobacco, also known as pasta, basuco, basa, pitillo, paco or simply paste. It is also gaining popularity as a cheap drug (30 to 70 U.S. cents per “hit” or dose) in many South American countries.

Freebase
As the name implies, “freebase” is the base form of cocaine, as opposed to the salt form of cocaine hydrochloride. Whereas cocaine hydrochloride is extremely soluble in water, cocaine base is insoluble in water and is therefore not suitable for drinking, snorting or injecting. Whereas cocaine hydrochloride is not well-suited for smoking because the temperature at which it vaporizes is very high, and close to the temperature at which it burns; however, cocaine base vaporizes at a much lower temperature, which makes it suitable for inhalation.

Smoking freebase is preferred by many users because the cocaine is absorbed immediately into blood via the lungs, reaching the brain in about five seconds. The rush is much more intense than sniffing the same amount of cocaine nasally, but the effects do not last as long. The peak of the freebase rush is over almost as soon as the user exhales the vapor, but the high typically lasts 5–10 minutes afterward. What makes freebasing particularly dangerous is that users typically don’t wait that long for their next hit and will continue to smoke freebase until none is left. These effects are similar to those that can be achieved by injecting or “slamming” cocaine hydrochloride, but without the risks associated with intravenous drug use (though there are other serious risks associated with smoking freebase).

Freebase cocaine is produced by first dissolving cocaine hydrochloride in water. Once dissolved in water, cocaine hydrochloride (Coc HCl) dissociates into protonated cocaine ion (Coc-H+) and chloride ion (Cl– ). Any solids that remain in the solution are not cocaine (they are part of the cut) and are removed by filtering. A base, typically ammonia (NH3), is added to the solution. The following net chemical reaction takes place:

Coc-H+Cl– + NH3 → Coc + NH4Cl

Handling diethyl ether is dangerous because ether is extremely flammable, its vapors are heavier than air and can “creep” from an open bottle, and in the presence of oxygen it can form peroxides, which can spontaneously combust. Demonstrative of the dangers of the practice, comedian Richard Pryor used to perform a skit in which he poked fun at himself over a 1980 incident in which he caused an explosion and ignited himself attempting to smoke “freebase”, presumably while still wet with ether.

Freebasing, while powerful, ultimately causes chronic paranoia and loss of sound judgment in the user. The rapid decline of porn actor John C. Holmes and his involvement in the 1981 massacre of the Wonderland Gang were among the first signs of the dangers of the then-growing freebase phenomenon.

Crack cocaine
Due to the dangers of using ether to produce pure freebase cocaine, cocaine producers began to omit the step of removing the freebase cocaine precipitate from the ammonia mixture. Typically, filtration processes are also omitted. The end result of this process is that the cut, in addition to the ammonium salt (NH4Cl), remains in the freebase cocaine after the mixture is evaporated. The “rock” that is thus formed also contains a small amount of water. Sodium bicarbonate (baking soda) is also preferred in preparing the freebase, for when commonly “cooked” the ratio is 50/50 to 40/60 percent cocaine/bicarbonate. This acts as a filler which extends the overall profitability of illicit sales. Crack cocaine may be reprocessed in small quantities with water (users refer to the resultant product as “cookback”). This removes the residual bicarbonate, and any adulterants or cuts that have been used in the previous handling of the cocaine and leaves a relatively pure, anhydrous cocaine base.

When the rock is heated, this water boils, making a crackling sound (hence the onomatopoeic “crack”). Baking soda is now most often used as a base rather than ammonia for reasons of lowered stench and toxicity; however, any weak base can be used to make crack cocaine. Strong bases, such as sodium hydroxide, tend to hydrolyze some of the cocaine into non-psychoactive ecgonine.

Chewed/eaten
Coca leaves typically are mixed with an alkaline substance (such as lime) and chewed into a wad that is retained in the mouth between gum and cheek (much in 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 gastro-intestinal tract when swallowed. Alternatively, coca leaves can be infused in liquid and consumed like tea. Ingesting coca leaves generally is an inefficient means of administering cocaine. Advocates of the consumption of the coca leaf, state that coca leaf consumption should not be criminalized as it is not actual cocaine, and consequently it is not properly the illicit drug. Because cocaine is hydrolyzed and rendered inactive in the acidic stomach, it is not readily absorbed when ingested alone. Only when mixed with a highly alkaline substance (such as lime) can it be absorbed into the bloodstream through the stomach. The efficiency of absorption of orally administered cocaine is limited by two additional factors. First, the drug is partly catabolized by the liver. Second, capillaries in the mouth and esophagus constrict after contact with the drug, reducing the surface area over which the drug can be absorbed. Nevertheless, cocaine metabolites can be detected in the urine of subjects that have sipped even one cup of coca leaf infusion. Therefore, this is an actual additional form of administration of cocaine albeit inefficient.

Orally administered cocaine takes approximately 30 minutes to enter the bloodstream. Typically, only a third of an oral dose is absorbed, although absorption has been shown to reach 60 percent in controlled settings. Given the slow rate of absorption, maximum physiological and psychotropic effects are attained approximately 60 minutes after cocaine is administered by ingestion. While the onset of these effects is slow, the effects are sustained for approximately 60 minutes after their peak is attained.

Contrary to popular belief, both ingestion and insufflation result in approximately the same proportion of the drug being absorbed: 30 to 60 percent. Compared to ingestion, the faster absorption of insufflated cocaine results in quicker attainment of maximum drug effects. Snorting cocaine produces maximum physiological effects within 40 minutes and maximum psychotropic effects within 20 minutes, however, a more realistic activation period is closer to 5 to 10 minutes, which is similar to ingestion of cocaine. Physiological and psychotropic effects from nasally insufflated cocaine are sustained for approximately 40 – 60 minutes after the peak effects are attained.

Mate de coca or coca-leaf infusion is also a traditional method of consumption and is often recommended in coca producing countries, like Peru and Bolivia, to ameliorate some symptoms of altitude sickness. This method of consumption has been practiced for many centuries by the native tribes of South America. One specific purpose of ancient coca leaf consumption was to increase energy and reduce fatigue in messengers who made multi-day quests to other settlements.

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. Despite this, the DEA seized several shipments in Hawaii, Chicago, Illinois, Georgia, and several locations on the East Coast of the United States, and the product was removed from the shelves. Nevertheless, today coca leaf teabags (named “mate de coca”) illegally smuggled into the U.S. can be readily purchased online via Internet stores and even eBay.

Insufflation
Insufflation (known colloquially as “snorting,” “sniffing,” or “blowing”) is the most common method of ingestion of recreational powder cocaine in the Western world. Contrary to widespread belief, cocaine is not actually inhaled using this method. The drug coats and is absorbed through the mucous membranes lining the sinuses. When insufflating cocaine, absorption through the nasal membranes is approximately 30-60 percent, with higher doses leading to increased absorption efficiency. Any material not directly absorbed through the mucous membranes is collected in mucus and swallowed (this “drip” is considered pleasant by some and unpleasant by others). In a study of cocaine users, the average time taken to reach peak subjective effects was 14.6 minutes. Chronic use results in ongoing rhinitis and necrosis of the nasal membranes.[citation needed] Many users report a burning sensation in the nares (nostrils) after cocaine’s anesthetic effects wear off. Any damage to the inside of the nose is because cocaine highly constricts blood vessels – and therefore blood and oxygen/nutrient flow – to that area. If this restriction of adequate blood supply is severe enough and, especially prolonged enough, the tissue there can die.[citation needed]

Prior to insufflation, cocaine powder must be divided into very fine particles. Cocaine of high purity breaks into fine dust very easily, except when it is moist (not well stored) and forms “chunks,” which reduces the efficiency of nasal absorption.

Rolled up banknotes, hollowed-out pens, cut straws, pointed ends of keys, and specialized spoons are often used to insufflate cocaine. Such devices are often called “tooters” by users. The cocaine typically is poured onto a flat, hard surface (such as a mirror) and divided into “lines” or “rails”, and then insufflated. The amount of cocaine in a line varies widely from person to person and occasion to occasion (the purity of the cocaine is also a factor), but one line is generally considered to be a single dose and is typically 35mg-100mg. As tolerance builds rapidly in the short-term (hours), many lines are often snorted to produce greater effects.

Injected
Drug injection provides the highest blood levels of drug in the shortest amount of time. Upon injection, cocaine reaches the brain in a matter of seconds, and the exhilarating rush that follows can be so intense that it induces some users to vomit uncontrollably. 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 danger of circulatory emboli from the insoluble substances that may be used to cut the drug. There is also a risk of serious infection associated with the use of contaminated needles.

An injected mixture of cocaine and heroin, known as “speedball” or “moonrock”, is a particularly popular and dangerous combination, as the converse effects of the drugs actually complement each other, but may also mask the symptoms of an overdose. It has been responsible for numerous deaths, particularly in and around Los Angeles, including celebrities such as John Belushi, Chris Farley (in Chicago), River Phoenix and Layne Staley (in Seattle). Injection of cocaine is particularly dangerous in the world of injectable drugs because when not injected directly into the vein infection occurs more regularly than most drugs, less dangerous only than Crystal Methamphetamine based on the fillers/cut.

Smoked
Smoking freebase or crack cocaine is most often accomplished using a pipe made from a small glass tube about one quarter-inch (about 6 mm) in diameter and on the average, four inches long. These are sometimes called “stems”, “horns”, “blasters” and “straight shooters,” readily available in convenience stores or smoke shops. They will sometimes contain a small paper flower and are promoted as a romantic gift. Buyers usually ask for a “rose” or a “flower.” An alternate method is to use a small length of a radio antenna or similar metal tube. To avoid burning the user’s fingers and lips on the metal pipe, a small piece of paper or cardboard (such as a piece torn from a matchbook cover) is wrapped around one end of the pipe and held in place with either a rubber band or a piece of adhesive tape. A popular (usually pejorative) term for crack pipes is “glass dick.” Tire pressure gauges have also been used by breaking off their tops and removing their numbered sticks. These can be purchased at most convenience stores or gas stations.

A small piece (approximately one inch) of heavy steel or stainless steel scouring pad (copper is never used as it can make the lungs bleed)—often called a “brillo” or “chore”, from the scouring pads of the same name—is placed into one end of the tube and carefully packed down to approximately three-quarter inch. Prior to insertion, the “brillo” is burnt off to remove any oily coatings that may be present. It then serves as a reduction base and flow modulator in which the “rock” can be melt and boiled to vapor. Stainless steel television cable are also used, with its metal acting as a screen.

Another method is to use a deep socket, typically 12 mm, wrapped with electrical tape. Instead of Chore Boy, users typically employ high grade (very fine) speaker wire rolled into a ball as the filter medium. A Zippo lighter is often used because of its stronger flame, but the taste of naphtha is quite noticeable. However, the socket is practically indestructible and inconspicuous.

A less sophisticated but common method is to use a discarded soda can and puncture several small holes on the side of the can near its bottom. Tobacco ash is then placed in the divot created with the drug placed on top. The mouthpiece is the original opening of the can, creating a cost-effective alternative to a proper crack pipe.

To smoke the “rock” it is placed at the end of the pipe, closest to the filter. The other end is then placed in the user’s mouth and a flame from a cigarette lighter or hand-held torch is held under the “rock”. As the “rock” is heated, it melts and burns away to vapor, which the user inhales as smoke.

The effects, felt almost immediately after smoking, are very intense and do not last long—usually five to fifteen minutes. In a study[8] performed on crack cocaine users, the average time taken for them to reach their peak subjective “high” was 1.4 minutes. Most (especially frequent) users crave more immediately after the peak. “Crack houses” depend on these cravings by providing a place for smoking crack to its users, and a ready supply of small bags for sale.

A heavily-used crack pipe tends to fracture at its end due to overheating from the flame used to heat the crack, typically because users attempt to inhale every last bit of the drug on the metal wool filter. The end is often broken further as users “push” the pipe. “Pushing” is a technique used to partially recover crack that hardens on the inside wall of the pipe as the pipe cools. This is accomplished by pushing the metal wool filter through the pipe from one end to the other in order to collect the build-up inside the pipe, which is a very pure and potent form of the base. The ends of the pipe can be broken by the object used to push the filter—frequently a small screwdriver or stiff piece of wire. Users will often remove the most jagged edges and continue using the pipe until it becomes so short that it burns their lips and fingers. To continue using the pipe, users will sometimes wrap a small piece of paper or cardboard around its one end and hold it in place with a rubber band or adhesive tape. Of course, not all crack cocaine users will allow it to get that short, and will instead opt for a new or different pipe. The telltale signs of a used crack pipe are a glass tube with burn marks at one or both ends and a clump of metal wool inside. The language referring to paraphernalia and practices of smoking cocaine vary across the United States, as do the packaging methods in the street level sale.

When smoked, cocaine is sometimes combined with other drugs, such as cannabis; often rolled into a joint or blunt. This combination is known as “primo”, “chronic”, “hype”, “shake and bake”, a “turbo”, a “yolabowla”, “SnowCaps”, “Canadian Health Care”, “B-51er”, a “cocoapuff”, a “dirty”, a “woo”, or “geeking.” Crack smokers who are being drug tested may also make their “primo” with cigarette tobacco instead of cannabis, since a crack smoker can test clean within two to three days of use, if only urine (and not hair) is being tested.

Powder cocaine is sometimes smoked, but it is inefficient as the heat involved destroys much of the chemical. One way of smoking powder is to put a “bump” into the end of an unlit cigarette, smoking it in one go as the user lights the cigarette normally. This cigarette is then referred to as a “Jimmy”. Alternatively, cocaine powder may be sprinkled onto the marijuana in a blunt or possibly a joint and then smoked. This is known as a “Chewy” or may also be referred to by one of the names mentioned above for crack-laced marijuana. When a marijuana bowl is laced with cocaine powder, it is often referred to as a “SnowCap” because the marijuana is “capped” with cocaine on top.

Coca leaf infusions
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. Visitors to the city of Cuzco in Peru, and La Paz in Bolivia are greeted with the offering of coca leaf infusions (prepared in tea pots with whole coca leaves) purportedly to help the newly-arrived traveler overcome the malaise of high altitude sickness. The effects of drinking coca tea are a mild stimulation and mood lift. It does not produce any significant numbing of the mouth nor does it give a rush like snorting cocaine. In order to prevent the demonization of this product, its promoters publicize the unproven concept that much of the effect of the ingestion of coca leaf infusion would come from the secondary alkaloids, as being not only quantitatively different from pure cocaine but also qualitatively different.

It has been promoted as an adjuvant for the treatment of cocaine dependence. In one controversial study, coca leaf infusion was used -in addition to counseling- to treat 23 addicted coca-paste smokers in Lima, Peru. Relapses fell from an average of four times per month before treatment with coca tea to one during the treatment. The duration of abstinence increased from an average of 32 days prior to treatment to 217 days during treatment. These results suggest that the administration of coca leaf infusion plus counseling would be an effective method for preventing relapse during treatment for cocaine addiction. Importantly, these results also suggest strongly that the primary pharmacologically active metabolite in coca leaf infusions is actually cocaine and not the secondary alkaloids.

Oral
Cocaine has been used medically and informally as an oral anesthetic. Many users rub the powder along the gum line, or onto a cigarette filter which is then smoked, which numbs the gums and teeth – hence the colloquial names of “numbies,” or “gummy,” for this type of administration. This is mostly done with the small amounts of cocaine remaining on a surface after insufflation. Another oral method is to wrap up some cocaine in rolling paper and swallow it. This is called “parachuting” or “bombing”.