Cocaine , also known as coke , is a powerful stimulant mostly used as a drug. Usually snorted, inhaled as smoke, or dissolved and injected into the blood vessels. Mental effects can include loss of contact with reality, intense feelings of pleasure, or agitation. Physical symptoms may include rapid heartbeat, sweating, and large pupils. High doses can cause very high blood pressure or body temperature. Effects start in seconds to minutes of use and last between five and ninety minutes. Cocaine has a small number of accepted medical uses such as numbness and decreased bleeding during nasal surgery.
Cocaine is addictive because of its effect on the gift path in the brain. After some time of use, there is a high risk that dependence will occur. Its use also increases the risk of stroke, myocardial infarction, lung problems in those who smoke, blood infections, and sudden cardiac death. Cocaine sold on the street is generally mixed with local anesthetics, cornstarch, quinine, or sugar, which can produce additional toxicity. After repeated doses, a person may experience a decrease in the ability to feel pleasure and be physically exhausted.
Cocaine acts by inhibiting reuptake of serotonin, norepinephrine, and dopamine. This results in a greater concentration of the three neurotransmitters in the brain. It can easily cross the blood-brain barrier and can cause barrier damage. Cocaine is a natural substance found in the coca plant that is mostly grown in South America. In 2013, 419 kilograms are produced legally. It is estimated that the illegal market for cocaine is 100 to 500 billion USD each year. With further processing of crack cocaine can be produced from cocaine.
After marijuana, cocaine is the most commonly used illegal drug globally. Between 14 and 21 million people take drugs every year. Its use is highest in North America followed by Europe and South America. Between one and three percent of people in developed countries have used cocaine at some point in their lives. In 2013 the direct use of cocaine generated 4,300 deaths, up from 2,400 in 1990. Coca's plant leaves have been used by Peruvians since ancient times. Cocaine was first isolated from the leaves in 1860. Since 1961, the International Single Convention on Narcotic Drugs has required countries to use cocaine as a crime.
Video Cocaine
Usage
Medical
Topical cocaine can be used as a local nasty agent to assist with painful procedures in the mouth or nose. TAC is one of the formulations used for pediatrics.
Cocaine is now widely used for nasal and lacrimal nasal surgery. The main disadvantages of this use are potential cocaine for cardiovascular toxicity, glaucoma, and pupil dilatation. Medicinal use of cocaine has declined because other synthetic local anesthetics such as benzocaine, proparacaine, lidocaine, and tetracaine are now used more frequently. If vasoconstriction is desired for the procedure (because it reduces bleeding), anesthetics is combined with a vasoconstrictor such as phenylephrine or epinephrine. Some ENT specialists occasionally use cocaine in practice when performing procedures such as nasal cauterization. In this scenario the dissolved cocaine is soaked into a cotton ball, which is placed in the nostrils for 10-15 minutes immediately before the procedure, thus performing a double role of both deadly areas to be burned, and vasoconstriction. Even when used in this way, some of the cocaine used can be absorbed through the mucosa of the mouth or nose and gives a systemic effect. An alternative method of administration for ENT surgery is mixed with adrenaline and sodium bicarbonate, as a Moffett solution.
Recreation
Cocaine is a powerful stimulant of the nervous system. The effect can last from fifteen or thirty minutes to an hour. The duration of cocaine effects depends on the amount taken and the route of administration. Cocaine can be in the form of fine white powder, bitter with taste. When inhaled or injected, it causes a numbing effect. Crack cocaine is a type of cocaine made into small "stones" by processing cocaine with sodium bicarbonate (baking soda) and water. Crack cocaine is referred to as "crack" because of the crackling sound produced when heated.
The use of cocaine leads to an increase in alertness, feelings of well-being and euphoria, increased energy and motor activity, and increased feelings of competence and sexuality.
Oral
Many users rub the powder along the gum line, or into smoked cigarette filters, which turn off the gums and teeth - hence the everyday names of "numbies", "gummers", or "cocoa puffs" for this type of administration. This is mostly done with small amounts of cocaine remaining on the surface after insufflation (grunting). Another oral method is to wrap some cocaine on the linting and swallow paper (parachute).
Coca leaf
Coca leaves are usually mixed with alkaline substances (like lime) and chewed into a lump stored in the mouth between chewing gum and cheek (just like chewing tobacco chewed) and sucked from the juice. The juice is absorbed slowly by the inner cheek mucous membranes and by the digestive tract when swallowed. Alternatively, coca leaves can be infused in liquids and consumed like tea. Swallowing coca leaf in general is an inefficient way to manage cocaine.
Because cocaine is hydrolyzed and inactive in the acid stomach, it is not easily absorbed when digested alone. Only when mixed with a very alkaline substance (such as lime) can be absorbed into the bloodstream through the stomach. The efficiency of oral cocaine absorption is limited by two additional factors. First, it is partly catabolized by the liver. Secondly, the capillaries in the mouth and esophagus narrow after contact with the drug, reducing the surface area where the drug can be absorbed. However, cocaine metabolites can be detected in the urine of subjects who have inhaled even one cup of coca leaf infusion.
Oral cocaine takes about 30 minutes to enter the bloodstream. Usually, only a third of the orally absorbed doses, although absorption has been shown to reach 60% in a controlled setting. Given the slow absorption rate, maximum physiological and psychotropic effects are achieved about 60 minutes after cocaine is given by consumption. While the onset of this effect is slow, the effect is maintained for about 60 minutes after its peak is reached.
Contrary to popular belief, both consumption and insufflation produce about the same proportion of the drug absorbed: 30 to 60%. Compared with consumption, faster absorption of insufflated cocaine results in the achievement of a maximum effect of faster drugs. Snacking cocaine produces a maximum physiological effect in 40 minutes and maximum psychotropic effects in 20 minutes, but a more realistic activation period approaches 5 to 10 minutes. The physiological and psychotropic effects of insufflated nasal cocaine are maintained for about 40-60 minutes after the peak effect is reached.
Coca tea, coca leaf infusion, is also a traditional method of consumption. Tea is often recommended for travelers in the Andes to prevent altitude sickness. However, its actual effectiveness has never been studied systematically. This method of consumption has been practiced for centuries by native South American tribes. One specific purpose of the ancient coca leaf consumption is to increase energy and reduce fatigue in couriers that perform multi-day searches to other settlements.
In 1986 an article in the Journal of the American Medical Association disclosed that US health food stores sell dried coca leaves to be prepared as infusions as "Inca Health Tea". Although the packaging claims to have been "decocainized", no process actually takes place. The article states that drinking two cups of tea per day provides mild stimulation, increased heart rate, and mood enhancement, and the tea is basically harmless. Nevertheless, DEA confiscated several shipments in Hawaii, Chicago, Georgia, and several locations on the East Coast of the United States, and the product was removed from the shelves.
Insufflation
Nasal insufflation (colloquially known as "grunting", "sniffing", or "blowing") is a common method of swallowing recreational powder cocaine. The drug layer is absorbed through the mucous membranes lining the nasal passages. The desired euphoric effect of Cocaine is delayed when it sniffs through the nose for about five minutes. This occurs because the absorption of cocaine is slowed by its constricting effect on the nasal blood vessels. Cocaine insufflation also leads to the longest duration of effect (60-90 minutes). When insufflating cocaine, the absorption through the nasal membrane is about 30-60%, with higher doses leading to increased absorption efficiency. Any material not directly absorbed through the mucous membranes is collected in mucus and ingested ("droplets" are considered to be pleasing to some and unpleasant to others).
In a cocaine user study, the average time taken to achieve a peak subjective effect was 14.6 minutes. Damage to the inside of the nose is due to the very narrowing of blood vessels - and therefore the bloodstream and oxygen/nutrients - into the area. The nosebleed after cocaine insufflation is due to irritation and damage to mucous membranes by foreign and adul- mered particles rather than the cocaine itself; as a vasoconstrictor, cocaine serves to reduce bleeding.
Rolled-up banknotes, hollowed out pen, straw cuts, pointed ends of keys, special spoons, long fingernails, and tampon (clean) applicators are often used to thicken cocaine. Such devices are often called "tooters" by the user. Cocaine is usually poured onto a flat and hard surface (like a mirror, a CD box or a book) and is divided into "bumps", "lines" or "rails", and then dismantled. The number of cocaine in one line varies from person to person and opportunity to opportunity (cocaine purity is also a factor), but one line is generally considered a single dose and usually 35 mg ("bump")) to 100 mg ("rail"). When tolerance is formed rapidly in the short run (hours), many lines often snort to produce a larger effect. A 2001 study reported that sharing a straw used to "snort" cocaine can spread blood diseases such as hepatitis C.
Injection
Drug injections by converting the drug into a solution give the highest blood drug levels in the shortest amount of time. Unusual subjective effects are shared with other administrative methods including ringing in the ear shortly after injection (usually when more than 120 milligrams) lasts 2 to 5 minutes including tinnitus and audio distortion. This colloquially referred to as "bell ringer". In a cocaine user study, the average time taken to achieve the peak subjective effect was 3.1 minutes. Euphoria passed quickly. Aside from the toxic effects of cocaine, there is also a danger of blood circulation embolism from insoluble substances that can be used to cut the drug. As with all prohibited substances, there is a risk of users contracting a blood infection if sterile injecting equipment is not available or used. Additionally, because cocaine is a vasoconstrictor, and frequent use requires multiple injections within hours or less, subsequent injections are progressively more difficult to manage, which in turn can lead to more injection attempts and more consequences of inaccurate injection.
The mixture of invasive cocaine and heroin, known as "speedball" is a very dangerous combination, since the opposite effect of these drugs is completely complementary, but can also mask overdose symptoms. Has been responsible for many deaths, including celebrities such as comedians/actors John Belushi and Chris Farley, Mitch Hedberg, River Phoenix, grunge singer Layne Staley and actor Philip Seymour Hoffman. Experimently, cocaine injections can be sent to animals such as fruit flies to study the mechanisms of cocaine addiction.
Inhale
Inhalation by smoking cocaine is one of the few ways drugs are consumed. The onset of euphoria effect desired by cocaine is fastest by inhaling cocaine and begins after 3-5 seconds. In contrast, cocaine inhalation causes the shortest duration of the effect (5-15 minutes). The two main ways cocaine smoking is freebasing and by using cocaine that has been converted into smokable "crack cocaine". Cocaine is smoked by inhaling the vapor produced when the solid cocaine is heated to a sublimated point. In a study of the Brookhaven National Department of Medicine 2000, based on self-reported reports of 32 participants participating in the study, the "high peak" was found at an average of 1.4 minutes/- 0.5 minutes. Cocaine pyrolysis products that only occur when heated/smoked have been shown to alter the effect profile, ie anhydroecgonine methyl ester when administered with cocaine increases dopamine in the brain region of CPu and NAc, and has 1 - and M 3 - receptor affinity.
Smoking freebase or crack cocaine is most often done using pipes made from small glass tubes, often taken from "love roses", small glass tubes with rose paper promoted as romantic gifts. These are sometimes called "stems", "horns", "blasters" and "straight shooters". A small piece of clean heavy copper or sometimes a stainless steel scrub - often called "brillo" (actually Brillo Pads containing soap, and not used) or "duty" (named for the Chore Boy copper scoring brand) - serves as the base of reduction and a flow modulator in which "stones" can be melted and boiled into steam. Cracked smokers also occasionally smoke through cans of soda with small holes on the side or bottom. Crack smoked by placing it on the end of the pipe; the fire held close to it produces steam, which is then inhaled by smokers. The effect, immediately after smoking, is very intense and does not last long - usually 2 to 10 minutes. When smoking, cocaine is sometimes combined with other drugs, such as marijuana, often rolled into joints or dull. Cocaine powder is also sometimes smoked, although the heat destroys many chemicals; smokers often sprinkle it onto marijuana. The language that refers to the trinkets and smoking habits of cocaine varies, as does the packaging method in street level sales.
Suppositories
Another way users consume cocaine is to make it a suppository which is then inserted into the anus or vagina. The drug is then absorbed by the membranes of these body parts. Small studies have focused on the method of suppositories (anal or vaginal insertion), also known as "plugging". This method of administration is generally given using oral syringes. Cocaine can be dissolved in water and drawn into an oral syringe which is then lubricated and inserted into the anus or vagina before the plunger is pushed. Anecdotal evidence of its effects is rarely discussed, perhaps because of social taboos in many cultures. The vaginal rectum and duct is where most of the drugs will be taken through the membranes lining the walls.
Maps Cocaine
Adverse effects
Acute
With excessive or prolonged use, medications can cause itching, rapid heartbeat, hallucinations, and paranoid delusions. Overdose causes hyperthermia and a marked increase in blood pressure, which can be life-threatening, arrhythmic, and death.
Anxiety, paranoia, and anxiety can also occur, especially during comedy. With excessive doses, tremor, seizures and elevated body temperature are observed. Severe cardiac side effects, especially sudden cardiac death, are a serious risk of high doses because of the blocking effect of cocaine on the cardiac sodium channel.
Chronic
Chronic cocaine intake causes a strong imbalance of transmitter levels to compensate for extremes. Thus, receptors disappear from the surface of the cell or reappear on top, producing more or less in their respective "off" or "work mode", or they alter their vulnerability to bind partners (ligands) - a mechanism called downregulation and upregulation. However, studies suggest cocaine abusers do not show a normal decline in age from the striatal dopamine transporter sites (DAT), suggesting cocaine has neuroprotective properties for dopamine neurons. Possible side effects include insatiable hunger, sickness, persistent insomnia/sleep, lethargy, and persistent nasal noses. Depression with the idea of ​​suicide can develop in very heavy users. Finally, loss of vesicular monoamine transporters, neurofilament proteins, and other morphological changes seem to indicate long-term damage to dopamine neurons. All of these effects contribute to increased tolerance and thus require larger doses to achieve the same effect. The lack of normal amounts of serotonin and dopamine in the brain is the cause of dysphoria and depression that feels after a high start. Physical withdrawal is not dangerous. Physiological changes caused by cocaine withdrawal include a clear and unpleasant dream, insomnia or hypersomnia, increased appetite and psychomotor retardation or agitation.
The physical side effects of chronic smoking include coughing up blood, bronchospasm, itching, fever, diffuse alveolar infiltrates, pulmonary and systemic eosinophilia, chest pain, pulmonary trauma, sore throat, asthma, hoarseness, dyspnea (shortness of breath) and pain, such as flu syndrome. Cocaine constricts blood vessels, dilates pupils, and increases body temperature, heart rate, and blood pressure. It can also cause headaches and gastrointestinal complications like abdominal pain and nausea. The common but incorrect belief is that smoking cocaine chemically breaks tooth enamel and causes tooth decay. However, cocaine often causes an unconscious toothbrush, known as bruxism, which can damage tooth enamel and cause gingivitis. In addition, stimulants such as cocaine, methamphetamine, and even caffeine lead to dehydration and dry mouth. Since saliva is an important mechanism in maintaining a person's oral pH level, inadequate hydration chronic boosters may experience demineralization of their teeth because the pH of the tooth surface drops too low (below 5.5). The use of cocaine also promotes the formation of blood clots. Increased formation of this blood clot is associated with cocaine-related enhancement in the activity of plasminogen activator inhibitors, and an increase in platelet count, activation, and aggregation.
The use of chronic intranasal can lower the cartilage separating the nostrils (septum of rice), which eventually leads to complete loss. Because of the absorption of cocaine from cocaine hydrochloride, the remaining hydrochloride forms dilute hydrochloric acid.
Cocaine also greatly increases the risk of developing autoimmune diseases or rare connective tissues such as lupus, Goodpasture syndrome, vasculitis, glomerulonephritis, Stevens-Johnson syndrome, and other diseases. It can also cause various kidney diseases and kidney failure.
The use of cocaine leads to an increased risk of hemorrhagic and ischemic stroke. Cocaine use also increases the risk of heart attack.
Dependency
Cocaine addiction occurs through FosB's overexpression in the nucleus accumbens, which results in changes in transcriptional regulation of neurons in the nucleus accumbens.
Fosb levels have been found to increase in cocaine use. Any further cocaine doses continue to rise? FosB levels with no tolerance limit. Increased levels of Fosb cause an increase in the level of neurotrophic factors (BDNF) derived from the brain, which in turn increases the number of dendritic branches and spines present in neurons involved with the nucleus accumbens and the prefrontal cortical area of ​​the brain. These changes can be identified rather quickly, and may be sustained several weeks after the last dose of the drug.
Transgenic mice showed Fosb-induced expression especially in the nucleus accumbens and dorsal striatum showed a susceptible behavior response to cocaine. They themselves manage cocaine at lower doses than controls, but have a greater chance of relapse when the drug is kept secret. Fosb increases the expression of AMPA subunit receptor GluR2 and also decreases dynorphin expression, thus increasing sensitivity to rewards.
Dependence and tethering
Cocaine dependence is a form of psychological dependence that develops from regular use of cocaine and results in a withdrawal state with emotional motivational deficits after cessation of cocaine use.
During pregnancy
Cocaine is known to have a number of damaging effects during pregnancy. Pregnant people who use cocaine are at high risk of placental abruption, a condition in which the placenta is released from the uterus and causes bleeding. Due to the vasoconstrictive effects and hypertension, they are also at risk of hemorrhagic stroke and myocardial infarction. Cocaine is also teratogenic, which means it can cause birth defects and fetal malformations. In-utero exposure to cocaine is associated with behavioral abnormalities, cognitive impairment, cardiovascular malformations, intrauterine growth restriction, premature birth, urinary malformation, and cleft lip and palate.
Pharmacology
Pharmacodynamics
Pharmacodynamic cocaine involves the complex association of neurotransmitters (inhibiting monoamine uptake in mice with a ratio of approximately: serotonin: dopamine = 2: 3, serotonin: norepinephrine = 2: 5). The most extensive cocaine effect studied in the central nervous system is the blockade of the dopamine transporter protein. Dopamine transmitters that are released during nerve signaling are usually recycled through the transporter; that is, the transporter binds the transmitter and pumps it out of the synaptic cleft back into the presinaptic neuron, where it is brought into vesicle storage. Cocaine binds closely to the dopamine transporter forming a complex that blocks the transport function. Dopamine transporters can no longer perform the reuptake function, and thus dopamine accumulates in the synaptic cleft.
Cocaine affects certain serotonin (5-HT) receptors; in particular, has been shown to be hostile to the 5-HT3 receptor, which is a ligand-gated ion channel. The advantages of 5-HT3 receptors in cocaine-conditioned rats show this trait, but the exact effect of 5-HT3 in this process is unclear. 5-HT2 receptors (especially the 5-HT2AR, 5-HT2BR and 5-HT2CR subtypes) are involved in the activation effect of the locomotor staple.
Cocaine has been proven binding to directly stabilize the DAT transporter on an outward-facing open conformation. Furthermore, cocaine binds in such a way as to inhibit the innate hydrogen bonds to DAT. The nature of cocaine binding is such that it attaches so that this hydrogen bond will not form and is blocked from formation due to the close orientation of the cocaine molecule. Research studies show that the affinity for the transporter is not what is involved in the habituation of so many substances such as conformations and properties that bind to and how to the transporter binding molecules.
Sigma receptors are affected by cocaine, because cocaine acts as an agonist ligand sigma. Further specific receptors that have been shown to work are NMDA and dopamine D1 receptors.
Cocaine also blocks sodium channels, thus interfering with potential action spreading; thus, such as lignocaine and novocaine, it acts as a local anesthetic. It also functions at the binding site to the dopamine-dependent transport area and serotonin sodium as a target as a separate mechanism of the reuptake transporter; unique to the value of local anesthesia that makes it in a class of functionality distinct from its own derived feniltropane analogue. In addition to this cocaine has several targets that bind to the Kappa-opioid receptor sites as well. Cocaine also causes vasoconstriction, thereby reducing bleeding during minor surgical procedures. The increasing properties of cocaine locomotor may be due to increased dopaminergic transmission of the substantia nigra. Recent research shows the important role of circadian mechanisms and clock genes in cocaine behavioral behavior.
Cocaine can often lead to reduced food intake, many chronic users lose appetite and may experience severe malnutrition and significant weight loss. The effects of cocaine, furthermore, prove potentially to the user when used in conjunction with new environments and stimuli, and vice versa new environments.
Pharmacokinetics
Cocaine has a short half-life of 0.7-1.5 hours and is extensively metabolized by cholinesterase enzymes (mainly in the liver and plasma), with only about 1% excreted unchanged in the urine. Metabolism is dominated by hydrolytic ester cleavage, so the metabolites eliminated consist mostly of benzoylecgonine (BE), major metabolites, and other important metabolites in smaller amounts such as ecgonine methyl ester (EME) and ecgonine. Additional minor metabolisms of cocaine include norcocaine, p-hydroxycocaine, m-hydroxycocaine, p-hydroxybenzoylecgonine (pOHBE), and m-hydroxybenzoylecgonine. If taken with alcohol, cocaine combines with alcohol in the liver to form cocaethylene. Research shows that cocaethylene is more euphoric, and has higher cardiovascular toxicity than cocaine by itself.
Depending on liver and kidney function, cocaine metabolites are detected in the urine. Benzoylecgonine can be detected in the urine within four hours after cocaine intake and remain detectable in concentrations greater than 150 ng/mL usually up to eight days after cocaine is used. Detection of cocaine metabolite accumulation in the hair is possible in the normal user until the part of hair that grows during the use of cut or fall.
Chemistry
Appearance
Cocaine in its purest form is a white pearl product. The cocaine that appears in powder form is salt, usually cocaine hydrochloride. Street cocaine is often forged or "cut" with powder, lactose, sucrose, glucose, mannitol, inositol, caffeine, procaine, phencyclidine, phenytoin, lignocaine, strychnine, amphetamine, or heroin.
The color of crack cocaine depends on several factors including the origin of the cocaine used, the method of preparation - with ammonia or baking soda - and the presence of dirt, but will generally range from white to yellowish cream to light brown.. The texture will also depend on the origin, origination and processing of cocaine powder, and the basic change method. Starting from the fragile texture, sometimes very oily, to the hard, almost like crystalline.
Form
Salt
Cocaine - the tropan alkaloid - is a weak base compound, and can therefore combine with the acid compound to form various salts. Cocaine hydrochloride (HCl) salt is by far the most common, although sulfate (-SO 4 ) and nitrate (-NO 3 ) are sometimes seen. Different salts dissolve to a greater or lesser extent in various hydrochloride salts which are polar and sufficiently soluble in water.
Base
As the name implies, "freebase" is the basic form of cocaine, not the form of salt. It is practically insoluble in water while salt hydrochloride is dissolved in water.
Smoking cocaine freebase has the additional effect of releasing methylecgonidine into the user's system due to pyrolysis of the substance (a side effect that insufflating or injecting cocaine powder does not create). Several studies have shown that smoking cigarette smoking may be more cardiotoxic than other routes of administration because of the effects of methylecgonidine on lung tissue and liver tissue.
Pure cocaine is made by neutralizing its compounding salt with an alkaline solution, which will precipitate for non-polar base cocaine. This is further enhanced by liquid-liquid-liquid-solvent extraction.
Cocaine crack
Crack is a lower-purity form of free-base cocaine normally produced by neutralizing cocaine hydrochloride with a solution of baking soda (sodium bicarbonate, NaHCO 3 ) and water, resulting in a very hard/brittle, off-white -to-brown colored, amorphous materials containing sodium carbonate, trapped water, and other by-products as main impurities.
The form of "freebase" and "crack" cocaine is usually given by evaporating the substance of the powder into smoke, which is then inhaled.
The origin of the name "crack" comes from the sound of "crackling" (and therefore the "crack" onomatopoeic moniker) produced when the cocaine and its feces (ie water, sodium bicarbonate) is heated through the evaporation point.
Pure cocaine base/crack can be smoked because it evaporates smoothly, with little or no decomposition at 98 ° C (208 ° F), which is below the boiling point of water.
In contrast, cocaine hydrochloride does not evaporate until it is heated to a higher temperature (about 197 ° C), and considerable decomposition/combustion occurs at this high temperature. It effectively destroys some cocaine and produces sharp, sharp, foul-smelling fumes.
Smoking or vaporizing cocaine and breathing it into the lungs produces a "very fast" that can be very strong (and addictive) quickly - the initial stimulation of this stimulation is known as "rush". While stimulating effects can last for hours, the sensation of euphoria is very short, prompting users to smoke faster.
Coca leaf infusion
Coca herbal infusions (also referred to as coca tea) are used in coca leaf producing countries as do any infusion of herbal medicine elsewhere in the world. The free and legal commercialization of dried coca leaves under the form of filter bags to be used as "coca tea" has been actively promoted by the governments of Peru and Bolivia for many years as a drug-powered beverage. Visitors to the city of Cuzco in Peru, and La Paz in Bolivia were greeted with a supply of coca leaf infusions (prepared in a carafe with whole coca leaves) purportedly to help new arrivals cope with high altitude malaise diseases. The effects of drinking coca tea is mild stimulation and lifting the mood. It does not produce significant numbness from the mouth or is not in such a hurry as snorting cocaine. To prevent the demonization of this product, the promoter publishes an unproven concept that many of the effects of coca leaf infusion consumption are derived from secondary alkaloids, since they differ not only quantitatively from pure cocaine but are also qualitatively different.
It has been promoted as an adjuvant for the treatment of cocaine dependence. In one controversial study, coca leaf infusions were used - in addition to counseling - to treat 23 addicts of coca-paste smokers in Lima, Peru. Relapse fell from an average of four times per month before treatment with coca tea to one during treatment. The duration of abstinence increased from an average of 32 days before treatment to 217 days during treatment. These results suggest that infusion of leaves plus coca counseling would be an effective method to prevent relapse during treatment for cocaine addiction. Importantly, these results also show strongly that the major pharmacological active metabolites in coca leaf infusion are actually cocaine and not secondary alkaloids.
Benzoylecgonine cocaine metabolites can be detected in people's urine a few hours after drinking one cup of coca leaf infusion.
Biosynthesis
The first synthesis and explanation of cocaine molecules was by Richard WillstÃÆ'¤tter in 1898. The synthesis of WillstÃÆ'¤tter derived cocaine from tropinone. Since then, Robert Robinson and Edward Leete have contributed significantly to the synthesis mechanism. (-NO 3 )
The additional carbon atoms required for cocaine synthesis are derived from acetyl-CoA, with the addition of two acetyl-CoA units to N -methyl -? 1 -pyrrolinium cation. The first addition is a Mannich-like reaction with an enolate anion of acetyl-CoA acting as a nucleophile to the pyrofifer cation. The second addition takes place through Claisen condensation. This yields a 2-substituted pyrolysine racemic mixture, with thioester retention of Claisen condensation. In the formation of tropinone from ethyl racemate [2,3-13C 2 ] 4 (Nmethyl-2-pyrrolidinyl) -3-oxobutanoate there is no preference for stereoisomers. However, in cocaine biosynthesis, only (S) -enantiomers can perform cyclization to form cocaine ring ring systems. Stereoselectivity of this reaction is further investigated through studies of prolific methylene hydrogen discrimination. This is because of the extra chiral center in C-2. This process occurs through oxidation, which regenerates pyrolynin cation and the formation of anion enolate, and intramolecular Mannich reactions. The tropan ring system undergoes hydrolysis, SAM-dependent methylation, and reduction through NADPH to form methylecgonine. The benzoyl portion required for the formation of cocaine diester is synthesized from phenylalanine through cinnamic acid. Benzoyl-CoA then combined two units to form cocaine.
N -methyl-pyrrolinium cation
Biosynthesis begins with L-Glutamine, which is lowered to L-ornithine in plants. The main contribution of L-ornithine and L-arginine as precursors to tropane rings is confirmed by Edward Leete. Ornithine then undergoes decarboxylation-pyridoxal decarboxylation to form putrescine. In animals, however, the urea cycle is derived from putrescine from ornithine. L-ornithine is converted to L-arginine, which is then decarboxylated by PLP to form agmatine. Imine hydrolysis obtained N -carbamoylputrescine followed by urea hydrolysis to form putrescine. Separate paths to turn ornithine into putrescine in plants and animals have accumulated. A SAM-dependent N -methylation of putrescine gives N -methylputrescine product, which then undergoes oxidative deamination by the action of diamine oxidase to produce aminoaldehyde. Schiff formation confirms the biosynthesis of cation -pyrrolinium N -methyl -? 1 .
acetonedicarboxylate Robert Robinson
The biosynthesis of trophic alkaloids, however, remains uncertain. Hemscheidt proposes that Robinson's acetonedicarboxylate appears as a potential intermediate for this reaction. Condensation N -methylpyrrolinium and acetonadicarboxylate will produce oxobutyrate. Decarboxylation causes the formation of trophic alkaloids.
Tropinone Reduction
The reduction of tropinone is mediated by NADPH-dependent enzyme reductase, which has been characterized in several plant species. These plant species all contain two types of enzyme reductase, tropinone reductase I and tropinone reductase II. TRI produces tropine and TRII produces pseudotropine. Due to the different kinetic and pH/activity characteristics of the enzyme and by the TRI activity 25 times higher than TRII, the majority of tropinon reductions are from TRI to form tropins.
Detection in body fluids
Cocaine and its major metabolites can be quantified in blood, plasma, or urine to monitor abuse, confirm the diagnosis of poisoning, or assist in traffic forensic investigations or other criminal offenses or sudden death. Most commercial immunoassay cocaine screening tests react substantially with major cocaine metabolites, but chromatographic techniques can easily distinguish and separately measure each of these substances. When interpreting the test results, it is important to consider the history of individual cocaine use, as chronic users can develop dose tolerance that will paralyze individuals who do not have cocaine, and chronic users often have high baseline values ​​of metabolites in their systems. Careful interpretation of test results allows the difference between passive or active use, and between smoking versus other administrative routes. In 2011, researchers at the John Jay College of Criminal Justice reported that dietary zinc supplements can mask the presence of cocaine and other drugs in urine. Similar claims have been made on web forums on that topic.
Usage
According to a United Nations report of 2016, England and Wales are the countries with the highest cocaine use rate (2.4% of adults in the previous year). Other countries where usage levels meet or exceed 1.5% are Spain and Scotland (2.2%), United States (2.1%), Australia (2.1%), Uruguay (1.8%) , Brazil (1.75%), Chile (1.73%), Netherlands (1.5%) and Ireland (1.5%).
Europe
Cocaine is the second most popular illegal recreation drug in Europe (behind cannabis). Since the mid-1990s, overall cocaine use in Europe has increased, but levels of use and attitudes tend to vary across countries. The European countries with the highest usage rates are the UK, Spain, Italy and the Republic of Ireland.
About 12 million Europeans (3.6%) used cocaine at least once, 4 million (1.2%) last year, and 2 million last month (0.5%).
About 3.5 million or 87.5% of those who had used drugs last year were young adults (15-34 years). Usage is very common among these demographics: 4% to 7% of men have used cocaine last year in Spain, Denmark, the Republic of Ireland, Italy and the UK. The male and female user ratios are about 3.8: 1, but these statistics vary from 1: 1 to 13: 1 depending on the country.
By 2014, London has a huge amount of cocaine in 50 cities across Europe.
United States
Cocaine is the second most popular illegal recreation drug in the United States (behind cannabis) and the US is the world's largest cocaine consumer. Cocaine is commonly used in middle and upper society and is known as the "medicine of the rich". It is also popular among students, as a party drug. A study across the United States has reported that about 48 percent of people who graduated high school in 1979 have used cocaine recreation for some point in their lives, compared with about 20 percent of students who graduated between 1980 and 1995. Users reach a wide range of ages, race, and profession. In the 1970s and 1980s, the drug became very popular in disco culture because the use of cocaine was very common and popular in many discos like Studio 54.
History
Discovery
For over a thousand years the native South American community has chewed the Erythroxylon coca leaf, a plant containing essential nutrients and many alkaloids, including cocaine. Coca leaves, and still, are chewed almost universally by some indigenous communities. The remains of coca leaf have been found with ancient Peruvian mummies, and pottery from the time period depicts humans with prominent cheeks, indicating the presence of something they chew. There is also evidence that this culture uses a mixture of coca leaf and saliva as an anesthetic for the performance of trepanation.
When the Spaniards arrived in South America, most initially ignored the indigenous claim that leaves gave them power and energy, and declared the practice of chewing the devil's work. But after finding that this claim is true, they legalize and tax leaf, taking 10% of the value of each harvest. In 1569, the Spanish botanist NicolÃÆ'¡s Monardes described the indigenous peoples practice of chewing tobacco and coca leaf blends to cause "great satisfaction":
When they want to make themselves drunk and out of their judgment chew a mixture of tobacco leaves and coca that keeps them away because they get out of their wittes.
Pada 1609, Padre Blas Valera menulis:
Coca protects the body from many illnesses, and our doctors use it in powder to reduce wound swelling, to strengthen broken bones, to ward off cold from the body or prevent it from entering, and to heal wounds of foul or maggot wounds. And if he does so much for external ailments, does not his single virtue have a greater effect on the entrails of those who eat them?
Isolation and naming
Although the nature of the stimulants and coca-hunger abortors has been known for centuries, cocaine alkaloid isolation was not achieved until 1855. Various European scientists have tried to isolate cocaine, but nothing works for two reasons: the knowledge of chemistry required is not enough at then, and contemporary sea shipping conditions from South America can decrease cocaine in plant samples available to European chemists.
The first cocaine alkaloids were isolated by German chemist Friedrich Gaedcke in 1855. Gaedcke named the "erythroxyline" alkaloids, and published descriptions in the journal Archiv der Pharmazie.
In 1856, Friedrich WÃÆ'¶hler asked Dr. Carl Scherzer, a scientist aboard the Novara (an Austrian frigate dispatched by Emperor Franz Joseph to circumnavigate the world), to bring him large quantities of coca leaves from South America. In 1859, the ship completed its journey and WÃÆ'¶hler received a coca stalk full. WÃÆ'¶hler submitted a leaf to Albert Niemann, a Ph.D. students at the University of GÃÆ'¶ttingen in Germany, who then developed a better refining process.
Niemann explains every step he took to isolate cocaine in his dissertation entitled ÃÆ'Ã… "ber eine neue organische Base in den CocablÃÆ'¤ttern ( At the New Organic Base in Coca Leaves ), which published in 1860 - it earned him a Ph.D. and now in the British Library. He writes about the "colorless transparent prism" of the alkaloids and says that "The solution has an alkaline reaction, bitter taste, increases saliva flow and leaves a strange numbness, followed by a sense of coldness when applied to the tongue." Niemann named the "cocaine" alkaloids of "coca" (from Quechua "cuca") the "ine" suffix. Because of its use as a local anesthetic, the "-caine" suffix is ​​then extracted and used to form the names of local synthetic anesthetics.
The first synthesis and elucidation of the structure of cocaine molecules was by Richard WillstÃÆ'¤tter in 1898. This is the first biomimetic synthesis of organic structures recorded in academic chemistry literature. Synthesis starts from tropinone, a natural related product and takes five steps.
Medalization
With the discovery of this new alkaloid, Western medicine is rapidly exploiting the possible use of this plant.
In 1879, Vassili von Anrep, of the University of WÃÆ'¼rzburg, devised an experiment to show the analgesic properties of the newly discovered alkaloids. He prepared two separate bottles, one containing a cocaine-salt solution, with the other containing only salt water. He then drowns the frog's legs into two jars, one foot in care and one in the control solution, and begins to stimulate the legs in several different ways. The legs that have been immersed in the cocaine solution react very differently from the feet that have been dipped in saltwater.
Karl Koller (a close associate of Sigmund Freud, who will write about cocaine later) experimented with cocaine for ophthalmic use. In a famous experiment in 1884, he experimented on himself by applying cocaine solutions to his own eyes and then stabbing them with pins. His discovery was presented to the Heidelberg Ophthalmological Society. Also in 1884, Jellinek demonstrated the effects of cocaine as an anesthetic of the respiratory system. In 1885, William Halsted demonstrated anesthesia of nerve blocks, and James Leonard Corning demonstrated a sleeping anesthetic. 1898 sees Heinrich Quincke using cocaine for spinal anesthesia.
Today, cocaine has very limited medical use.
Popularize
In 1859, an Italian doctor, Paolo Mantegazza, returned from Peru, where he witnessed the direct use of coca by local indigenous peoples. He went on to experiment on himself and upon his return to Milan he wrote a paper in which he described the effect. In this paper he states coca and cocaine (at the time they are considered the same) as a useful remedy, in the treatment of "hairy tongue in the morning, flatulence, and whiten teeth."
A chemist named Angelo Mariani who read Mantegazza's paper was immediately attracted to coca and its economic potential. In 1863, Mariani began marketing a wine called Vin Mariani, who had been treated with a coca leaf, into a cocawine. Ethanol in wine acts as a solvent and extracts cocaine from coca leaves, altering the effects of beverages. It contains 6 mg of cocaine per ounce of wine, but Vin Mariani to be exported contains 7.2 mg per ounce, to compete with a higher cocaine content than similar beverages in the United States. "Pinch of coca leaves" was included in John Styth Pemberton's original recipe for Coca-Cola, although the company began using decocainized leaves in 1906 when the Pure Food and Drug Act was passed.
In 1879 cocaine began to be used to treat morphine addiction. Cocaine was introduced into clinical use as a local anesthetic in Germany in 1884, around the same time as Sigmund Freud published his work Coconut ÃÆ'gber , in which he wrote that cocaine causes:
Lasting excitement and euphoria, which is no different from the normal euphoria of a healthy person. You feel increased self-control and have more vitality and capacity to work. In other words, you're just normal, and it's immediately hard to believe that you're under the influence of any drugs. Long intensive physical work done without fatigue. These results are enjoyed without any unpleasant effects after the excitement generated by alcoholic beverages. There is no desire for further cocaine use to appear after the first, or even after the drug's recovery.
In 1885 US manufacturer Parke-Davis sold cocaine in various forms, including cigarettes, powders, and even a mixture of cocaine that could be injected directly into the user's veins with the included needle. The company promised that its cocaine products would "feed the food, make cowardly cowards, who are fluent in silence and make the patient insensitive to pain."
In the late Victorian era, cocaine use has emerged as a representative in the literature. For example, it was injected by the fictional Sherlock Holmes by Arthur Conan Doyle, generally to compensate for the boredom he felt when he was not working on a case.
At the beginning of the 20th century, Memphis, Tennessee, cocaine was sold at an environmental drug store in Beale Street, for five or ten cents for a small box. Stevedores along the Mississippi River use the drug as a stimulant, and white entrepreneurs encourage its use by black workers.
In 1909, Ernest Shackleton took the "Forced March" cocaine tablet to Antarctica, as Captain Scott did a year later on his ill-fated trip to the South Pole.
During the mid-1940s, in the middle of World War II, cocaine was considered to be included as a future generation of 'spirit pill' for the German military, a code called D-IX.
In reference to popular modern culture for the prevalent drug, in which the drug has a glamorous image associated with the rich, famous and powerful with it also makes the user "feel rich and beautiful". In addition the pace of modern society - as in the field of finance - provides many incentives to use the drug.
Modern usage
In many countries, cocaine is a popular recreational drug. In the United States, the development of crack cocaine introduces substance to the generally poorer city market. The use of powder form remains relatively constant, experiencing new heights of use during the late 1990s and early 2000s in the US, and has become much more popular in recent years in the UK.
Cocaine use is prevalent in all socioeconomic strata, including age, demography, economics, social, political, religious, and livelihood.
The US cocaine market is estimated to exceed US $ 70 billion in street values ​​for 2005, exceeding corporate earnings such as Starbucks. There is tremendous demand for cocaine in the US market, especially among those who make income with luxury spending, such as single adults and free income professionals. The status of cocaine as a club drug shows its incredible popularity among "party crowds".
In 1995, the World Health Organization (WHO) and the United Nations Intercontinental Crime Research Institute (UNICRI) announced in a press release the largest global research publication on cocaine use ever performed. However, a decision by an American representative at the World Health Assembly banned the publication of the study, as it appears to make the case for the use of positive cocaine. An excerpt from a report contrary to the accepted paradigm, for example "that occasional use of cocaine does not usually cause severe or even mild physical or social problems." In the sixth meeting of Committee B, US representatives threatened that "If the activities of the World Health Organization relating to drugs fail to strengthen a proven drug control approach, funds for relevant programs should be limited". This led to the decision to stop the publication. Parts of this study have been restored and published in 2010, including cocaine use profiles in 20 countries, but not available by 2015.
In October 2010 it was reported that cocaine use in Australia has doubled since monitoring began in 2003.
Problems with the use of illegal cocaine, especially in higher volumes used to overcome fatigue (rather than increase euphoria) by long-term users, are the risk of adverse effects or damage caused by compounds used in counterfeiting. Cutting or "stepping on" drugs is common, using compounds that simulate swallowing effects, such as Novocain (procaine) producing temporary anesthesia, as many users believe strong numbing effects are the result of strong and/or pure cocaine, ephedrine or the like. a stimulant that results in an increase in heart rate. The normal adulterers to benefit are inactive sugar, usually mannitol, creatine or glucose, so introducing active meat-eaters gives the illusion of purity and to 'stretch' or make it a dealer can sell more products than without the adulterers. Sugar-eaters enable dealers to sell products at higher prices because of the illusion of purity and enable the sale of more products at higher prices, enabling dealers to significantly increase revenues at little additional cost to the adulterers. A 2007 study by the European Monitoring Center for Drugs and Drug Addiction showed that the level of purity for road-bought cocaine is often below 5% and averages below 50% pure.
Society and culture
Legal status
The production, distribution and sale of cocaine products are restricted (and illegal in most contexts) in most countries as regulated by the Single Convention on Narcotics Drugs, and the United Nations Convention Against Illicit Trafficking in Narcotics Drugs and Psychotropic Substances. In the United States, the manufacture, import, ownership and distribution of cocaine is also governed by the Act of Action Act of 1970.
Some countries, such as Peru and Bolivia, allow the planting of coca leaves for traditional consumption by local indigenous populations, however, prohibiting the production, sale and consumption of cocaine. Provisions on how many coca farmers can produce each year are protected by laws such as the Cato deal of Bolivia. In addition, parts of Europe and Australia allow cocaine to be processed only for drug use.
Australia
Cocaine is a Schedule 8 substance in Australia based on Poison Standard (July 2016). A schedule substance 8 is Drug-controlled - Substances that must be available for use but require restrictions on manufacture, supply, distribution, ownership and use to reduce abuse, abuse and physical or psychological dependence.
In Western Australia under the Drug Abuse Act 1981 4.0g cocaine is the number of illicit drugs that determine the court, 2.0 g is the amount of cocaine required to presume the intention to sell or supply and 28.0g is the amount of cocaine required for the purpose of drug trafficking.
United States
The US federal government implements a national labeling requirement for products containing cocaine and cocaine through the Pure Food and Drug Act of 1906. The next important federal regulation is the Harrison Narcotics Tax Act of 1914. While this act is often seen as the beginning of the Prohibition , the act itself is not a ban on cocaine, but instead establishes regulatory and licensing regimes. The Harrison Act does not recognize addiction as a treatable condition and therefore therapeutic use of cocaine, heroin or morphine to such individuals is prohibited - leading the 1915 editorial in the American Drugs journal to comment that the addict "is denied care a medical on board where he had previously obtained his supply of medicine was closed to him, and he was pushed to hell where he could get his medicine, but of course, secretly and unlawfully. "The Harrison Act left the manufacturer cocaine untouched as long as they meet certain standards of purity and labeling. Although cocaine is usually illegal for sale and legal outlets are much rarer, the number of legally produced cocaine decreases very little. The amount of legal cocaine was not reduced until the Jones-Miller Act of 1922 imposed serious restrictions on cocaine manufacturing.
Interdiction
In 2004, according to the United Nations, 589 tons of cocaine were seized globally by law enforcement officers. Colombia seizes 188 t, United States 166 t, Europe 79 t, Peru 14 t, Bolivia 9 t, and the rest of the world 133 t.
Economy
Due to the drug's potential for addiction and overdose, cocaine is generally treated as a "hard drug", with heavy penalties for ownership and trade. Demand remains high, and consequently, black market cocaine is quite expensive. Unprocessed cocaine, like coca leaves, is sometimes bought and sold, but it is very rare because it is much easier and more profitable to hide and smuggle it in powder. The market scale is huge: 770 tons times $ 100 per gram retail = up to $ 77 billion.
Production
Until 2012, Colombia is the world's leading cocaine producer. Three quarters of the world's annual cocaine yield has been produced in Colombia, both from cocaine bases imported from Peru (mainly Huallaga Valley) and Bolivia, and from locally grown coca. There was a 28% increase in the number of potentially harvested coca crops grown in Colombia in 1998. This, combined with crop reduction in Bolivia and Peru, made Colombia the country with the largest coca area in cultivation after the mid-1990s.. Coca is grown for traditional purposes by indigenous peoples, the extant use and permitted by Colombian legislation make up only a fraction of the total coca production, which is mostly used for illegal drug trafficking.
An interview with a coca farmer published in 2003 described a production mode with acid-base extraction that has changed slightly since 1905. About 625 pounds (283 kg) of leaves are harvested per hectare, six times per year. The leaves are dried for half a day, then cut into small pieces with a trimmed rope and sprinkled with a little cement powder (replacing sodium carbonate from the past). Several hundred pounds of this mixture are soaked in 50 gallon US (190 Â ° L) of gasoline for a day, then the gasoline is removed and the leaves are pressed for the remaining liquid, after which they can be thrown away. Then the battery acid (weak sulfuric acid) is used, one bucket per 55 pounds (25 kg) of leaves, to create a phase separation where the cocaine free base in the gasoline is acidified and extracted into a bucket of "visibly turbid odor liquid". After the caustic soda powder is added to this, the cocaine is precipitated and can be removed by filtration through the fabric. The resulting material, when dried, is called paste lavada paste and finally the crystal cocaine is performed in a specialized laboratory after the sale.
Efforts to eradicate coca fields through the use of defoliant have devastated parts of the agricultural economy in some areas of Colombian coca planting, and strains appear to have been developed that are more resistant or immune to their use. Whether this strain is a natural mutation or an obscure human product. This strain also proved to be stronger than previously planted, increasing the profitability for drug cartels responsible for cocaine exports. Although production fell temporarily, coca plants rebounded in smaller fields in Colombia, rather than larger estates.
Coca cultivation has become an attractive economic decision for many farmers due to a combination of several factors, including the lack of alternative jobs, lower profitability of alternative crops in official plant substitution programs, damage related to the eradication of non-drug farms, the spread of new strains of coca plant due to persistent world demand.
Recent estimates provided by the US authorities about the annual production of cocaine in Colombia refer to 290 metric tons. By the end of 2011, Colombian cocaine seizure operations conducted in various countries have reached 351.8 metric tons of cocaine, which is 121.3% of Colombia's annual output, according to US Department of State estimates.
Synthesis
Synthetic cocaine will be highly desirable by the illegal pharmaceutical industry as it will eliminate the high visibility and low source of offshore and international smuggling, replacing them with secret domestic laboratories, as is common for illicit methamphetamine. But natural cocaine remains the lowest cost and supply of the highest quality cocaine. The actual cocaine synthesis is rarely done. The formation of an inactive enantiomer (cocaine has 4 chiral centers - 1R , 2R , 3S , and 5S - hence total potential of 16 possible enantiomers and diastereoisomers) plus synthetic byproducts limiting yield and purity. Names such as "synthetic cocaine" and "new cocaine" have been misused for phencyclidine (PCP) and various designer drugs.
Trading and distribution
Organized criminal gangs operating on a large scale dominate the cocaine trade. Most cocaine is grown and processed in South America, especially in Colombia, Bolivia, Peru, and smuggled to the United States and Europe, the United States being the world's largest cocaine consumer, where it is sold with large markup; typically in the US at $ 80-120 for 1 gram, and $ 250-300 for 3.5 grams (1/8 ounces, or "eight balls").
Caribbean and Mexican Routes
In 2005, cocaine shipments from South America transported through Mexico or Central America were generally moved to the mainland or by air to a staging place in northern Mexico. Cocaine is then broken up into smaller loads for smuggling across the US-Mexico border. The main cocaine import point in the United States has been in Arizona, southern California, southern Florida, and Texas. Usually, ground vehicles are pushed across the US-Mexico border. Sixty-five percent of cocaine enters the United States
Source of the article : Wikipedia
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