Cocaine



Cocaine 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.

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. Trace amounts of cocaine could be found in Coca-Cola 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.

Cocaine in its purest form is a white, pearly product. Cocaine appearing in powder form is a salt, typically cocaine hydrochloride (CAS 53-21-4). Street market cocaine is frequently adulterated or “cut” with various powdery fillers to increase its weight; the substances most commonly used in this process are baking soda; sugars, such as lactose, dextrose, inositol, and mannitol; and local anesthetics, such as lidocaine or benzocaine, which mimic or add to cocaine's numbing effect on mucous membranes. Cocaine may also be "cut" with other stimulants such as methamphetamine. Adulterated cocaine is often a white, off-white or pinkish powder.

The color of “crack” cocaine depends upon several factors including the origin of the cocaine used, the method of preparation – with ammonia or sodium bicarbonate – and the presence of impurities, but will generally range from white to a yellowish cream to a light brown. Its texture will also depend on the adulterants, origin and processing of the powdered cocaine, and the method of converting the base. It ranges from a crumbly texture, sometimes extremely oily, to a hard, almost crystalline nature.

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.

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.

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.

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 an inefficient one.

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 (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[8] 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. 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.

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.

A study by Bonkovsky and Mehta published in Am Acad Dermatol (2001 Feb;44(2):159-82) reported that, just like shared needles, the sharing of straws used to "snort" cocaine can spread blood diseases such as Hepatitis C.

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.

Experimentally, cocaine injections can be delivered to animals such as fruit flies to study the mechanisms of cocaine addiction.

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 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", "jay bomb", "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 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.

The cocaine metabolite benzoylecgonine can be detected in the urine of people a few hours after drinking one cup of coca leaf infusion.

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 a snow bomb.

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 blockage 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 pre-synaptic 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 extracellular space (synaptic cleft). This results in an enhanced and prolonged post-synaptic effect of dopaminergic signalling at dopamine receptors on the receiving neuron. Prolonged exposure to cocaine, as occurs with habitual use, leads to homeostatic dysregulation of normal (i.e. without cocaine) dopaminergic signaling via downregulation of dopamine receptors and enhanced signal transduction. The decreased dopaminergic signalling after chronic cocaine use may contribute to depressive mood disorders and sensitize this important brain reward circuit to the reinforcing effects of cocaine (e.g. enhanced dopaminergic signalling only when cocaine is self-administered). This sensitization contributes to the intractable nature of addiction and relapse.

Dopamine-rich brain regions such as the ventral tegmental area, nucleus accumbens, and prefrontal cortex are frequent targets of cocaine addiction research. Of particular interest is the pathway consisting of dopaminergic neurons originating in the ventral tegmental area that terminate in the nucleus accumbens. This projection may function as a "reward center", in that it seems to show activation is response to drugs of abuse like cocaine in addition to natural rewards like food or sex (R Spanagel and F Weiss, The dopamine hypothesis of reward: past and current status. Trends Neurosci 22 (1999), pp. 521–527). While the precise role of dopamine in the subjective experience of reward is highly controversial among neuroscientists, the release of dopamine in the nucleus accumbens is widely considered to be at least partially responsible for cocaine's rewarding effects. This hypothesis is largely based on laboratory data involving rats that are trained to self-administer cocaine intravenously (i.v.). If dopamine antagonists are infused directly into the nucleus accumbens, well-trained rats self-administering cocaine will undergo extinction (i.e. initially increase responding only to stop completely) thereby indicating that cocaine is no longer reinforcing (i.e. rewarding) the drug-seeking behavior.

Cocaine also blocks sodium channels, thereby interfering with the propagation of action potentials; thus, like lignocaine and novocaine, it acts as a local anesthetic. Cocaine also causes vasoconstriction, thus reducing bleeding during minor surgical procedures. The locomotor enhancing properties of cocaine may be attributable to its enhancement of dopaminergic transmission from the substantia nigra. Recent research points to an important role of circadian mechanisms and clock genes in behavioral actions of cocaine.

Because nicotine increases the levels of dopamine in the brain, many cocaine users find that consumption of tobacco products during cocaine use enhances the euphoria. This, however, may have undesirable consequences, such as uncontrollable chain smoking during cocaine use (even users who don't normally 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.

In addition to irritability, mood disturbances, restlessness, paranoia, and auditory hallucinations, crack can cause several dangerous physical conditions. It can lead to disturbances in heart rhythm and heart attacks, as well as chest pains or even respiratory failure. In addition, strokes, seizures and headaches are common in heavy users.

Cocaine can often cause reduced food intake, many chronic users lose their appetite and can experience severe malnourishment and significant weight loss.

The mixture of cocaine and alcohol is the most common two-drug combination that results in drug related death.

Cocaine is extensively metabolized, primarily in the liver, with only about 1% excreted unchanged in the urine. The metabolism is dominated by hydrolytic ester cleavage, so the eliminated metabolites consist mostly of benzoylecgonine, the major metabolite, and in lesser amounts ecgonine methyl ester and ecgonine.

If taken with alcohol, cocaine combines with the ethanol in the liver to form cocaethylene, which is both more euphorigenic and has higher cardiovascular toxicity than cocaine by itself. It is precisely this characteristic that since the early 20th century has prompted heavily inebriated persons to snort cocaine to relieve them of the depressive effects of alcohol abuse.

Depending on liver and kidney function, cocaine metabolites are detectable in urine. Benzoylecgonine can be detected in urine within four hours after cocaine intake and remains detectable in concentrations greater than 150 ng/ml typically for up to eight days after cocaine is used. Detection of accumulation of cocaine metabolites in hair is possible in regular users until the sections of hair grown during use are cut or fall out.

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 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 hemoptysis, bronchospasm, pruritus, fever, diffuse alveolar infiltrates without effusions, pulmonary and systemic eosinophiliachest, pain, lung trauma, shortness of breath, sore throat, asthma, hoarse voice, dyspnea, and an aching, flu-like syndrome. A common belief 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. Many cocaine users lack motivation to brush their teeth after cocaine intoxication.

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 abuse doubles both the risks of hemorrhagic and ischemic strokes.

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.

History

* The cocaine alkaloid was first isolated by the German chemist Friedrich Gaedcke in 1855.
* In 1859 Albert Niemann, a Ph.D. student at the University of Göttingen in Germany developed an improved purification process. He named the alkaloid “cocaine”.
* In 1879 cocaine began to be used to treat morphine addiction. Cocaine was introduced into clinical use as a local anaesthetic in Germany in 1884.
* In 1884 Sigmund Freud wrote the article Über Coca, where he described the therapeutic uses of cocaine.
* In 1885 the U.S. manufacturer Parke-Davis sold cocaine in various forms, including cigarettes, powder, and even a cocaine mixture that could be injected directly into the user’s veins with the included needle. The company promised that its cocaine products would “supply the place of food, make the coward brave, the silent eloquent and ... render the sufferer insensitive to pain.”
* In 1886 Coca-Cola is invented and its original formula includes cocaine.
* Around 1903 cocaine was eliminated as a direct ingredient of Coca-Cola.
* In 1914 the Harrison Narcotics Tax Act outlawed the use of cocaine in the United States. This law incorrectly referred to cocaine as a narcotic, and the misclassification passed into popular culture. Cocaine is a stimulant, not a narcotic.
* In 1961 the Single Convention on Narcotic Drugs was signed in New York. It banned the production and trade of cocaine, cannabis and opium and its derivatives. It went into effect in 1964.
* In 1970 the United States Congress passed the Controlled Substances Act which today still regulates the manufacture, importation, possession, and distribution of cocaine in the United States.
* In the 1970s cocaine regained popularity as a recreational drug and was glamorized in the U.S. popular media (for example, in songs like J.J. Cale's Cocaine and the movie Scarface), and by the disco music culture that emerged around discotheques like Studio 54. The Medellín and Cali Cartels were founded in Colombia to meet the new demand for cocaine.
* In 1985 the crack epidemic began and lasted to about 1990.
* In late 1993 Pablo Escobar, the founder of the Medellín Cartel is gunned down by Colombian National Police. The Cali Cartel becomes the number one cocaine trafficker.
* In 1995 the Cali Cartel is dismantled by Colombian National Police, only to be replaced by the Norte del Valle Cartel.
* Today, Cocaine in its various forms comes in second only to cannabis as the most popular illegal recreational drug in the United States, and is number one in street value sold each year, exceeding $35 billion in 2003.

The production, distribution and sale of cocaine products is restricted (and illegal in most contexts) in most countries as regulated by the Single Convention on Narcotic Drugs, and the United Nations Convention Against Illicit Traffic in Narcotic Drugs and Psychotropic Substances. In the United States the manufacture, importation, possession, and distribution of cocaine is additionally regulated by the 1970 Controlled Substances Act.

Some countries, such as Peru and Bolivia permit the cultivation of coca leaf for traditional consumption by the local indigenous population, but nevertheless prohibit the production, sale and consumption of cocaine.

Some parts of Europe and Australia allow processed cocaine for medicinal uses only.

In certain countries in the Middle East and Asia, such as Singapore, Saudi Arabia and Indonesia, being in possession of cocaine can be punishable by death.

In 2004, according to the United Nations, 589 metric tons of cocaine were seized globally by law enforcement authorities. Colombia seized 188 tons, the United States 166 tons, Europe 79 tons, Peru 14 tons, Bolivia 9 tons, and the rest of the world 133 tons.

Because of the extensive processing it undergoes during preparation, cocaine is generally treated as a 'hard drug', with severe penalties for possession and trafficking. Demand remains high, and consequently black market cocaine is quite expensive. Unprocessed cocaine, such as coca leaves, are occasionally purchused and sold, but this is exceedingly rare as it is much easier and more profitable to conceal and smuggle it in powdered form.

By 1999, Colombia had become the world's leading producer of cocaine. Three-quarters of the world's annual yield of cocaine was produced there, both from cocaine base imported from Peru (primarily the Huallaga Valley) and Bolivia, and from locally grown coca. There was a 28 percent increase from the amount of potentially harvestable coca plants which were grown in Colombia in 1998. This, combined with crop reductions in Bolivia and Peru, made Colombia the nation with the largest area of coca under cultivation after the mid-1990s. Coca grown for traditional purposes by indigenous communities, a use which is still present and is permitted by Colombian laws, only makes up a small fragment of total coca production, most of which is used for the illegal drug trade. Attempts to eradicate coca fields through the use of defoliants have devastated part of the farming economy in some coca growing regions of Colombia, and strains appear to have been developed that are more resistant or immune to their use. Whether these strains are natural mutations or the product of human tampering is unclear. These strains have also shown to be more potent than those previously grown, increasing profits for the drug cartels responsible for the exporting of cocaine. The cultivation of coca has become an attractive, and in some cases even necessary, economic decision on the part of many growers due to the combination of several factors, including the persistence of worldwide demand, the lack of other employment alternatives, the lower profitability of alternative crops in official crop substitution programs, the eradication-related damages to non-drug farms, and the spread of new strains of the coca plant.
Estimated Andean Region Coca Cultivation and Potential Pure Cocaine Production, 2000–2004.

Organized criminal gangs operating on a large scale dominate the cocaine trade. Most cocaine is grown and processed in South America, particularly in Colombia and Peru, and smuggled into the United States and Europe, where it is sold at huge markups; usually in the US at $100-150 for 3.5 grams (slang: 8 ball).

Cocaine shipments from South America transported through Mexico or Central America are generally moved over land or by air to staging sites in northern Mexico. The cocaine is then broken down into smaller loads for smuggling across the U.S.–Mexico border. The primary cocaine importation points in the United States are in Arizona, southern California, southern Florida, and Texas. Typically, land vehicles are driven across the U.S.-Mexico border. Sixty Five percent of cocaine enters the United States through Mexico, and the vast majority of the rest enters through Florida.

Cocaine is also carried in small, concealed, kilogram quantities across the border by couriers known as “mules” (or “burros”), who cross a border either legally, e.g. through a port or airport, or illegally through undesignated points along the border. The drugs may be strapped to the waist or legs or hidden in bags, or hidden in the body. If the mule gets through without being caught, the gangs will reap most of the profits. If he or she is caught however, gangs will sever all links and the mule will usually stand trial for trafficking by him/herself.

Cocaine traffickers from Colombia, and recently Mexico, have also established a labyrinth of smuggling routes throughout the Caribbean, the Bahama Island chain, and South Florida. They often hire traffickers from Mexico or the Dominican Republic to transport the drug. The traffickers use a variety of smuggling techniques to transfer their drug to U.S. markets. These include airdrops of 500–700 kg in the Bahama Islands or off the coast of Puerto Rico, mid-ocean boat-to-boat transfers of 500–2,000 kg, and the commercial shipment of tonnes of cocaine through the port of Miami.

Bulk cargo ships are also used to smuggle cocaine to staging sites in the western Caribbean–Gulf of Mexico area. These vessels are typically 150–250-foot (50–80 m) coastal freighters that carry an average cocaine load of approximately 2.5 tonnes. Commercial fishing vessels are also used for smuggling operations. In areas with a high volume of recreational traffic, smugglers use the same types of vessels, such as go-fast boats, as those used by the local populations.

Traffickers have also started using a method whereby a substance such as iron thiocyanate, a mixture of cobalt and ferric chloride, or a mixture of charcoal and iron filings is added to cocaine hydrochloride to produce “black cocaine.” The cocaine in this substance is not detected by standard chemical tests such as the Becton Dickinson test kit. The substance was first identified after a seizure in March 1998 in Germany, which was then tracked back to discover 250 lb of black cocaine ready for transport at Bogotá’s airport.

Cocaine is readily available in all major countries' metropolitan areas. According to the Summer 1998 Pulse Check, published by the U.S. Office of National Drug Control Policy, cocaine use had stabilized across the country, with a few increases reported in San Diego, Bridgeport, Miami, and Boston. In the West, cocaine usage was lower, which was thought to be because some users were switching to methamphetamine, which was cheaper and provides a longer-lasting high. Numbers of cocaine users are still very large, with a concentration among city-dwelling youth.

Cocaine is typically sold to users by the gram ($30-$120US) or eight ball (3.5 grams, or roughly 1/8th oz; hence the term "eight ball") ($100-$300). Quality and price can vary dramatically depending on demand and supply.

World annual cocaine consumption currently stands at around 600 metric tons, with the United States consuming around 300 metric tons, 50% of the total, Europe about 150 metric tons, 25% of the total, and the rest of the world the remaining 150 metric tons or 25%.

According to the United Nations Office on Drugs and Crime 2006 World Drug Report, the United States has the world's greatest rate of cocaine consumption by people aged 15 to 64, 2.8%. It is closely followed by Spain with 2.7%, and England & Wales with 2.4%. Most Western European countries have a consumption rate between 1% and 2%.

Cocaine has become the second most popular illegal recreational drug in the U.S. Cocaine is commonly used in middle to upper class communities. It is also popular amongst college students, not just to aid in studying, but also as a party drug. Its users span over different ages, races, and professions. In the 1970s and 80's the drug became particularly popular in the disco culture as cocaine usage was very common and popular in many discos such as Studio 54.

The National Household Survey on Drug Abuse (NHSDA) reported in 1999 that cocaine was used by 3.7 million Americans, or 1.7 percent of the household population age 12 and older. Estimates of the current number of those who use cocaine regularly (at least once per month) vary, but 1.5 million is a widely accepted figure within the research community.

Although cocaine use had not significantly changed over the six years prior to 1999, the number of first-time users went up from 574,000 in 1991, to 934,000 in 1998 — an increase of 63%. While these numbers indicated that cocaine is still widely present in the United States, cocaine use was significantly less prevalent than it was during the early 1980s. Cocaine use peaked in 1982 when 10.4 million Americans (5.6 percent of the population) reportedly used the drug.

The 1999 Monitoring the Future (MTF) survey found the proportion of American students reporting use of powder cocaine rose during the 1990s. In 1991, 2.3 percent of eighth-graders stated that they had used cocaine in their lifetime. This figure rose to 4.7 percent in 1999. For the older grades, increases began in 1992 and continued through the beginning of 1999. Between those years, lifetime use of cocaine went from 3.3 percent to 7.7 percent for tenth-graders and from 6.1 percent to 9.8 percent for twelfth-graders. Lifetime use of crack cocaine, according to MTF, also increased among eighth-, tenth-, and twelfth-graders, from an average of 2 percent in 1991 to 3.9 percent in 1999.

Perceived risk and disapproval of cocaine and crack use both decreased during the 1990s at all three grade levels. The 1999 NHSDA found the highest rate of monthly cocaine use was for those aged 18–25 at 1.7 percent, an increase from 1.2 percent in 1997. Rates declined between 1996 and 1998 for ages 26–34, while rates slightly increased for the 12–17 and 35+ age groups. Studies also show people are experimenting with cocaine at younger ages. NHSDA found a steady decline in the mean age of first use from 23.6 years in 1992 to 20.6 years in 1998.

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Cocaine addiction is the excessive intake of cocaine, and can result in physiological damage, lethargy, depression, or a potentially fatal overdose. The immediate craving to use more cocaine is strong and very common, because euphoric effects usually subside in most users within an hour of the last dosage, leading to serial cocaine readministrations, and prolonged, multi-dose binge use in those who are addicted. When administration stops after binge use, it is followed by a "crash" (also known as a "come down"), the onset of severely dysphoric mood with escalating exhaustion until sleep is achieved, which is sometimes accomplished by taking sleeping medications, or sedatives, a popular one being Seroquel. Resumption of use may occur upon awakening or may not occur for several days, but the intense euphoria of such use can, as it has in many users, produce intense craving and develop rather quickly into addiction. The risk of becoming cocaine-dependent within 2 years of first use(recent-onset) is 5-6%; after 10 years, it's 15-16%. These are the aggregate rates for all types of use considered, i.e., smoking, snorting, injecting. Among recent-onset users, the relative rates are higher for smoking (3.4 times) and much higher for injecting. They also vary, based on other characteristics, such as gender: among recent-onset users, females are 3.3 times more likely to become addicted, compared to males; age: among recent-onset users, those who started using at ages 12 or 13 were 4 times as likely to become addicted, compared to those who started between ages 18 and 20; and race: among recent-onset users, non-Hispanic Blacks are 7 times as likely to become addicted, compared to non-Hispanic Whites. Many habitual abusers develop a transient manic-like condition similar to amphetamine psychosis and schizophrenia, whose symptoms include aggression, severe paranoia, and tactile hallucinations (including the feeling of insects under the skin, or "coke bugs") during binges.

Cocaine has positive reinforcement effects, which refers to the effect that certain stimuli have on behavior. Good feelings become associated with the drug, causing a frequent user to take the drug as a response to bad news or mild depression. This activation strengthens the response that was just made. If the drug was taken by a fast acting route such as injection or inhalation, the response will be the act of taking more cocaine, so the response will be reinforced. Powder cocaine, being a club drug is mostly consumed in the evening and night hours. Because cocaine is a stimulant, a user will often drink large amounts of alcohol during and after usage or smoke cannabis to dull "crash" or "come down" effects and hasten slumber. Benzodiazepines (e.g., xanax®, rohypnol®) are also used for this purpose. Other drugs such as heroin and various pharmaceuticals are often used to amplify reinforcement or to minimize such negative effects, further increasing addiction potential and harmfulness.

It has been shown in studies that rhesus monkeys provided with a mechanism of cocaine self-administration prefer the drug over food that is in the cage. This happens even when the monkeys are starving.

It is speculated that cocaine's addictive properties stem partially from its DAT-blocking effects (in particular, increasing the dopaminergic transmission from ventral tegmental area neurons). However, a study has shown that mice with no dopamine transporters still exhibit the rewarding effects of cocaine administration. Later work demonstrated that a combined DAT/SERT knockout eliminated the rewarding effects. The rewarding effects of cocaine are influenced by circadian rhythms, possibly by involving a set of genes termed "clock genes". However, chronic cocaine addiction is not solely due to cocaine reward. Chronic repeated use is needed to produce cocaine-induced changes in brain reward centers and consequent chronic dysphoria (described above under "Effects and Health Issues - Chronic"). Dysphoria magnifies craving for cocaine because cocaine reward rapidly, albeit transiently, improves mood. This contributes to continued use and a self-perpetuating, worsening condition, since those addicted usually cannot appreciate that long-term effects are opposite those occurring immediately after use.

Cognitive Behavioral Therapy (CBT) shows promising results. One or more cocaine vaccines exist or are on trial that will stop desirable effects from the drug. The National Institutes of Health of an unspecified country is researching modafinil, a narcolepsy drug and mild stimulant, as a potential cocaine treatment. Twelve-step programs such as Cocaine Anonymous (modeled on Alcoholics Anonymous) are claimed by many cocaine addicts to be helpful in achieving long-term abstinence. These spiritual programs have no statistically-measurable effect as Alcoholics Anonymous does not release any quantifiable measure of its success rates. There are, however, many recovering addicts who claim this program has aided them.

Studies have shown that gamma vinyl-gamma-aminobutyric acid (gamma vinyl-GABA, or GVG), a drug normally used to treat epilepsy, blocks cocaine's action in the brains of primates. GVG increases the amount of the neurotransmitter GABA in the brain and reduces the level of dopamine in the region of the brain that is thought to be involved in addiction. In January 2005 the U.S. Food and Drug Administration gave permission for a Phase I clinical trial of GVG for the treatment of addiction. Another drug currently tested for anti-addictive properties is the cannabinoid antagonist rimonabant.

GBR 12909 (Vanoxerine) is a selective dopamine uptake inhibitor. Because of this, it reduces cocaine's effect on the brain, and may help to treat cocaine addiction. Studies have shown that GBR, when given to primates, suppresses cocaine self-administration.

Venlafaxine (Effexor®), although not a dopamine re-uptake inhibitor, is a serotonin-norepinephrine reuptake inhibitor that has been successfully used to combat the depression caused by cocaine withdrawal and to a lesser extent, the addiction associated with the drug itself. Venlafaxine has been shown to have significant withdrawal problems itself, and can lead to lifetime use due to these withdrawal effects. A statistically significant number of people prescribed Effexor® have committed suicide (2 attempts per 1000 patients, vs 1.56 suicides per 1,000 untreated depressives).Permission is granted to copy, distribute and/or modify this document under the terms of the GNU Free Documentation License, Version 1.2 or any later version published by the Free Software Foundation; with no Invariant Sections, with no Front-Cover Texts, and with no Back-Cover Texts.
Virtual Magic is a human knowledge database blog. Text Based On Information From Wikipedia, Under The GNU Free Documentation License. Copyright (c) 2007 Virtual Magic. Permission is granted to copy, distribute and/or modify this document under the terms of the GNU Free Documentation License, Version 1.1 or any later version published by the Free Software Foundation; with no Invariant Sections, no Front-Cover Texts and no Back-Cover Texts. A copy of the license is included in the section entitled "GNU Free Documentation License".

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