If vasoconstriction is desired for a procedure (as it reduces bleeding), the anesthetic is combined with a vasoconstrictor such as phenylephrine or epinephrine. Medicinal use of cocaine has decreased as other synthetic local anesthetics such as benzocaine, proparacaine, lidocaine, and tetracaine are now used more often. The major disadvantages of this use are cocaine's potential for cardiovascular toxicity, glaucoma, and pupil dilation. Ĭocaine may be used for nasal and lacrimal duct surgery. Topical cocaine can be used as a local numbing agent to help with painful procedures in the mouth or nose. While rarely used medically today, its accepted uses are as a topical local anesthetic for the upper respiratory tract as well as to reduce bleeding in the mouth, throat and nasal cavities. In the United States, cocaine is regulated as a Schedule II drug nder the Controlled Substances Act, meaning that it has a high potential for abuse and has an accepted medical use for treatment. Since 1961, the international Single Convention on Narcotic Drugs has required countries to make recreational use of cocaine a crime. The highest prevalence of cocaine use was in Australia and New Zealand (2.1%), followed by North America (2.1%), Western and Central Europe (1.4%), and South and Central America (1.0%). Globally, in 2019, cocaine was used by an estimated 20 million people (0.4% of adults aged 15 to 64 years).
Cocaine was first isolated from the leaves in 1860. In ancient Wari culture, Incan culture, through successor cultures in modern indigenous cultures of the Andes mountains, coca leaves are chewed, taken orally in the form of a tea, or alternatively, prepared in a sachet wrapped around alkaline burnt ashes, and held in the mouth against the cheek, and used to combat the effects of cold, hunger, and altitude sickness. 4.3.2 Robert Robinson's acetonedicarboxylateĬoca leaves have been used by Andean civilizations since ancient times.The Global Burden of Disease study found that cocaine use caused around 7300 deaths in 2007. Illicitly sold cocaine is commonly adulterated with local anesthetics, levamisole, cornstarch, quinine, or sugar, which can result in additional toxicity. It also increases risk of stroke, heart attack, cardiac arrhythmia, lung injury (when smoked), and sudden cardiac death. Cocaine's use increases the overall risk of death and particularly the risk of trauma, and infectious diseases, such as blood infections and AIDS. Abstention from cocaine after chronic use results in drug withdrawal, with symptoms that may include depression, decreased libido, decreased ability to feel pleasure and subjective fatigue. After a short period of use, dependence is likely. A single dose of cocaine induces tolerance to the drug's effects. Ĭocaine can be addictive due to its effect on the reward pathway in the brain. Cocaine also blocks the serotonin transporter and norepinephrine transporter, inhibiting reuptake of serotonin and norepinephrine from the synaptic cleft into the pre-synaptic axon terminal and increasing activation of serotonin receptors and norepinephrine receptors in the post-synaptic neuron, contributing to the modulation of consciousness, emotions, and movements that characterize cocaine exposure. Cocaine acts as an indirect sympathomimetic by blocking the dopamine transporter, inhibiting reuptake of dopamine from the synaptic cleft into the pre-synaptic axon terminal the higher dopamine levels in the synaptic cleft increase dopamine receptor activation in the post-synaptic neuron, which drives the effects of euphoria and arousal. Ĭocaine crosses the blood-brain barrier via a proton-coupled organic cation antiporter and (to a much lesser extent) via passive diffusion. Effects begin within seconds to minutes of use and last between five and ninety minutes. High doses can result in high blood pressure or high body temperature.
Physical symptoms may include a fast heart rate, sweating, and dilated pupils.
Mental effects may include an intense feeling of happiness, sexual arousal, loss of contact with reality, or agitation. After extraction from coca leaves and further processing into cocaine hydrochloride (powdered cocaine), the drug may be snorted, heated until sublimated and then inhaled, or dissolved and injected into a vein. It is most commonly used as a recreational drug and euphoriant. Cocaine (from French: cocaïne, from Spanish: coca, ultimately from Quechua: kúka) is a tropane alkaloid and stimulant drug obtained primarily from the leaves of two Coca species native to South America, Erythroxylum coca and Erythroxylum novogranatense.
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