Facts about Cocaine
The name cocaine comes from the name of the coca plant plus the alkaloid suffix -ine.
Cocaine also blocks sodium channels, thereby interfering with the propagation of action potentials; thus, like lignocaine and novocaine, it acts as a local anesthetic.
Adulterated cocaine is often a white, off-white or pinkish powder.
Cocaine is a weakly alkaline compound (an "alkaloid") and can therefore combine with acidic compounds to form various salts.
A form of cocaine available by prescription is applied to the skin to numb eye, nose, and throat pain and narrow blood vessels (WebMD 2013b).
Cocaine also causes vasoconstriction, thus reducing bleeding during minor surgical procedures.
Cocaine can be dissolved in water and withdrawn into an oral syringe which may then be lubricated and inserted into the anus or vagina before the plunger is pushed.
Cocaine appearing in powder form is a salt, typically cocaine hydrochloride.
Prior to insufflation, cocaine powder is divided into very fine particles.
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The first synthesis and elucidation of the structure of the cocaine molecule was by Richard Willstдtter in 1898 (Humphrey and O'Hagan 2001).
In Australia, cocaine is currently prescribed for use as a local anesthetic for conditions such as mouth and lung ulcers.
Absolutely no craving for the further use of cocaine appears after the first, or even after repeated taking of the drug.
By 1891, just five years later, the amount of cocaine was significantly cut, although the ingredient was left in in order to protect the trade name of Coca-Cola.
Cocaine dependency may result in physiological damage, lethargy, psychosis, depression, akathisia, and fatal overdose.
Nasal insufflation is the most common method of ingestion of recreational powdered cocaine in the Western world.
In 1898, Heinrich Quincke demonstrated the use of cocaine for spinal anesthesia.
Physiological and psychotropic effects from nasally insufflated cocaine are sustained for approximately 40–60 minutes after the peak effects are attained (Barnett et al.
Cocaine is available as a prescription for such purposes as external application to the skin to numb pain.
Legal cocaine quantities did not decrease until the Jones-Miller Act of 1922 put serious restrictions on cocaine manufactures (Madge 2001; Gootenberg 1999).
Sigma receptors are affected by cocaine, as cocaine functions as a sigma ligand agonist (NIH/NIDA 2003).
Dopamine-rich brain regions such as the ventral tegmental area, nucleus accumbens, and prefrontal cortex are frequent targets of cocaine addiction research.
The production, distribution and sale of cocaine products is restricted and/or illegal in most countries.
Powdered cocaine is also sometimes smoked, though heat destroys much of the chemical.
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Powdered cocaine is commonly known as "coke" or "blow" and users can snort the powder (inhale through the nose) and into the bloodstream, or dissolve in water and inject directly into the bloodstream.
The hydrochloride (HCl) salt of cocaine is by far the most commonly encountered, although the sulfate (-SO4) and the nitrate (-NO3) are occasionally seen.
Cocaine has since been largely replaced in Western medicine by synthetic local anesthetics such as benzocaine, proparacaine, lignocaine/xylocaine/lidocaine, and tetracaine though it remains available for use if specified.
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Use of concentrated cocaine yields pleasure through its interference with neurotransmitters of the sympathetic nervous system, such as blocking dopamine from being reabsorbed and thus resulting in continual stimulation.
The extract from the leaves is hydrolysed and esterified with methanol and benzoic acid to produce the hydrochloride salt of cocaine.
The locomotor enhancing properties of cocaine may be attributable to its enhancement of dopaminergic transmission from the substantia nigra.
On the one hand, users of cocaine report a euphoria (feeling "high"), with an increased sense of alertness, feelings of well-being, competence, and "supremacy," enhanced energy and motor activity, and sexuality (WebMD 2013a).
Strictly regulated, cocaine can be applied externally to the skin to numb pain.
The United Nations Office of Drugs and Crime estimated that in 2009 the US cocaine market was $37 billion and the West and Central European cocaine market was US$ 33 billion.
The major disadvantages of this use are cocaine's intense vasoconstrictor activity and potential for cardiovascular toxicity.
When processed and concentrated by chemical extraction from large quantities of coca leaves, cocaine is a powerful stimulant.
Some ENT specialists occasionally use cocaine within the practice when performing procedures such as nasal cauterization.
The cocaine alkaloid was first isolated by the German chemist Friedrich Gaedcke in 1855.
When insufflating cocaine, absorption through the nasal membranes is approximately 30–60%, with higher doses leading to increased absorption efficiency.
Cocaine was historically used as a topical anesthetic in eye and nasal surgery.
By 1902, it was held that Coca-Cola contained a little as 1/400th of a grain of cocaine per ounce of syrup.
The origin of the name "crack" comes from the "crackling" sound (and hence the onomatopoeic moniker “crack”) that is produced when the cocaine and its impurities (i.e.
The efficiency of absorption of orally administered cocaine is limited by two additional factors.
The ethanol in wine acted as a solvent and extracted the cocaine from the coca leaves, altering the drink's effect.
Cocaine is best known worldwide for its illegal use as a recreational drug.
Among forms of cocaine use are cocaine hydrochloride, natural leaf, cocaine paste, or freebase.
Smoking freebase cocaine has the additional effect of releasing methylecgonidine into the user's system due to the pyrolysis of the substance (a side effect which insufflating or injecting powder cocaine does not create).
Chronic cocaine intake causes brain cells to adapt functionally to strong imbalances of transmitter levels in order to compensate extremes.
Cocaine has been held responsible for more visits to US emergency rooms than any other illegal drug (WebMD 2013a).
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."
Cocaine use can be highly addictive, causing intense cravings for the drug, and can have deleterious impacts on the brain, heart, respiratory system, kidneys, sexual system, and gastrointestinal tract (WebMD 2013a).
Cocaine use can also cause a wide array of kidney diseases and renal failure (Jaffe and Kimmel 2006; van der Woude 2000).
An oral method for the psychoactive drug is to wrap up some cocaine in rolling paper and swallow (parachute) it.
A medical form of cocaine, strictly regulated and available by prescription, is applied to the skin to numb eye, nose, and throat pain (WebMD 2013b).
Pure cocaine base/crack can be smoked because it vaporizes smoothly, with little or no decomposition at 98 °C (208 °F) (Miller et al.
In 1929, Coca-Cola became cocaine-free, but before then it was estimated that the amount of cocaine already was no more than one part in 50 million (Mikkelson 2011; Liebowitz 1983; Cortes 2013).
Cocaine also effects seratonin (5-hydroxytryptamine, 5-HT), a monoamine neurotransmitter widely thought to be a contributor to feelings of well-being and happiness.
Due to the absorption of the cocaine from cocaine hydrochloride, the remaining hydrochloride forms a dilute hydrochloric acid (Pagliaro and Pagliaro 2004).
Nevertheless, cocaine metabolites can be detected in the urine of subjects that have sipped even one cup of coca leaf infusion.
Cocaine is the most concentrated of the dozen or more alkaloids that have been identified in the coca plant.
Marieb and Hoehn (2010) note that one way that might be developed to tackle addiction would be to prompt the immune system to bind cocaine molecules and prevent them from entering the brain.
According to a 2007 United Nations report, Spain is the country with the highest rate of cocaine usage (3.0% of adults in the previous year) (UNODC 2007).
Pure cocaine is prepared by neutralizing its compounding salt with an alkaline solution, which will precipitate to non-polar basic cocaine.
Coca, the plant in which cocaine is found, has been utilized in unprocessed form for thousands of years.
The overabundance of 5-HT3 receptors in cocaine conditioned rats display this trait; however, the exact effect of 5-HT3 in this process is unclear (Carta et al.
Physiological and psychotropic effects from nasally insufflated cocaine are sustained for approximately 40–60 minutes after the peak effects are attained (Barnett et al.
The possession, distribution, and sale of cocaine products is illegal for non-medicinal / non-government sanctioned purposes in virtually all parts of the world.
Another specific receptor cocaine has been demonstrated to function on is NMDA (Lluch et al.
Cocaine has the chemical formula C17H21NO4 and is also known as benzoylmethylecgonine or methyl benzoyl ecgonine.
Physiological changes caused by cocaine withdrawal include vivid and unpleasant dreams, insomnia or hypersomnia, increased appetite and psychomotor retardation or agitation (Lowinson et al.
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.
Cocaine is extensively metabolized, primarily in the liver, with only about 1% excreted unchanged in the urine.
Some research suggests that smoking freebase cocaine can be even more cardiotoxic than other routes of administration (Scheidweiler et al.
Cocaine can double both the risks of hemorrhagic and ischemic strokes (Jeffrey and Vega 2008) and increase the risk of other infarctions, such as myocardial infarction (Vasica and Tennant 2002).
Cocaine also was isolated in 1859 by Albert Niemann of the University of Gцttingen, using an improved purification process.
Cocaine may also be "cut" with other stimulants such as methamphetamine.
Cocaine can often cause reduced food intake, many chronic users lose their appetite and can experience severe malnutrition and significant weight loss.
An injected mixture of cocaine and heroin, known as “speedball,” is a particularly dangerous combination, as the converse effects of the drugs actually complement each other, but may also mask the symptoms of an overdose.
The use of cocaine can create a tolerance, requiring an increasing dose for stimulation.
Biologically, cocaine acts as a serotonin–norepinephrine–dopamine reuptake inhibitor, also known as a triple reuptake inhibitor (TRI).
Traces of cocaine also have been in 3000-year-old mummies of the Alto Ramirez culture of Northern Chile, suggesting coca-leaf chewing dates to at least 1500 B.C.E.
Powdered cocaine is also sometimes smoked, though heat destroys much of the chemical.
Cocaine constricts blood vessels, dilates the pupils, and increases heart rate and blood pressure.
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.
The leg that had been immersed in the cocaine solution reacted very differently from the leg that had been immersed in salt water (Yentis and Vlassakov 1999).
Rolled up banknotes, hollowed-out pens, cut straws, and other such items are often used to insufflate cocaine.
Cocaine is a crystalline tropane alkaloid (benzoylmethylecgonine, C17H21NO4) found in the leaves of the coca plant and best known in its concentrated form as an addictive, and generally illegal, psychoactive recreational drug.
Inhalation or smoking involves inhaling cocaine vapor into the lungs by sublimating solid cocaine by heating.
Cocaine is generally treated as a 'hard drug', with severe penalties for possession and trafficking.
Cocaine powder can be inhaled through the nose or dissolved in water and injected into the bloodstream, as well as rubbed along the gum line.
When the dopamine uptake is blocked by repeated use of cocaine, the system reacts by releasing less and less dopamine and "the reward system effectively goes dry" (Marieb and Hoehn 2010).
By binding tightly with the dopamine transporter, cocaine forms a complex that blocks the transporter's function.
Cocaine dependence (or addiction) is psychological dependency on the regular use of cocaine.
Cocaine often is a cause of involuntary tooth grinding, known as bruxism, which can deteriorate tooth enamel and lead to gingivitis (Baigent 2003).
Mice lacking a particular glutamate receptor are willing to try cocaine but do not become addicted (Marieb and Hoehn 2010).
Well-known tropane alkaloids, in addition to cocaine, include atropine and ecgonine (a precursor and metabolite of cocaine).
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 (Trozak and Gould 1984; Peces et al.