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Cocaine

Cocaine Use and History: – Coca leaves have been used by Andean civilizations for centuries for various purposes like combating cold, hunger, and altitude sickness. […]

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Cocaine Use and History:
– Coca leaves have been used by Andean civilizations for centuries for various purposes like combating cold, hunger, and altitude sickness.
– Cocaine was isolated from coca leaves in 1860.
– Global cocaine use was estimated at 20 million people in 2019.
– Recreational use of cocaine has been criminalized since 1961.
– Traditional medical uses of cocaine include as eye drops for diagnosing Horner syndrome and as a local anesthetic and vasoconstrictor in surgery.
– Cocaine hydrochloride was approved for local anesthesia in 2017.

Effects and Risks:
– Cocaine is a CNS stimulant that leads to alertness, euphoria, increased energy, and sexuality.
– Cocaine use can result in risks such as stroke, heart attack, lung injury, and sudden cardiac death.
– Cocaine has been linked to an overall increased risk of death and can be adulterated with toxic substances like fentanyl.
– A global study in 2017 attributed 7,300 annual deaths to cocaine use.
– Cocaine and crack were ranked among the most dangerous drugs in terms of dependence, physical harm, and social harm.
– Cocaine overdose deaths in the US often involve opioids.

Mechanism of Action and Pharmacology:
– Cocaine stimulates the brain’s reward pathway by blocking the dopamine transporter and increasing dopamine levels.
– It also blocks serotonin and norepinephrine transporters, inducing tolerance and addiction with repeated use.
– Withdrawal symptoms from cocaine use can include sleep disruption, anxiety, and depression.
– Cocaine absorption rates vary based on the route of administration, with nasal insufflation and inhalation being common methods.
– Cocaine has a short elimination half-life of 0.7-1.5 hours and its metabolites can be detected in urine for 3-8 days.

Methods of Ingestion:
– Nasal insufflation is a common method for ingesting powdered cocaine, with absorption rates ranging from 30-60%.
– Injection of cocaine can lead to rapid onset of effects and poses risks like circulatory emboli and blood-borne infections.
– Inhalation of cocaine provides the fastest onset of euphoria, with effects lasting 5-15 minutes.
– Chronic use of cocaine does not show broad cognitive deficits, but can lead to physical side effects like coughing up blood and cartilage degradation.
– Smoking crack cocaine is a common method that produces intense effects lasting 2-10 minutes.

Addiction, Dependence, and Pregnancy:
– Cocaine addiction occurs through overexpression of ΔFosB in the nucleus accumbens.
– Chronic cocaine use may cause structural changes in brain connectivity.
– Cessation of cocaine use can lead to emotional-motivational deficits.
– Prenatal cocaine exposure can lead to subtle deficits in children, affect fetal growth, and cause birth defects.
– Cocaine users, including pregnant women, are at a higher risk of traumatic and infectious disease-related deaths.

Cocaine (Wikipedia)

Cocaine (from French: cocaïne, from Spanish: coca, ultimately from Quechua: kúka) is a tropane alkaloid that acts as a central nervous system (CNS) stimulant. As an extract, it is mainly used recreationally, and often illegally for its euphoric and rewarding effects. It is also used in medicine by Indigenous South Americans for various purposes and rarely, but more formally, as a local anaesthetic or diagnostic tool by medical practitioners in more developed countries. It is primarily obtained from the leaves of two Coca species native to South America: Erythroxylum coca and E. novogranatense. After extraction from the plant, and further processing into cocaine hydrochloride (powdered cocaine), the drug is administered by being either snorted, applied topically to the mouth, or dissolved and injected into a vein. It can also then be turned into free base form (typically crack cocaine), in which it can be heated until sublimated and then the vapours can be inhaled.

Cocaine
Clinical data
Pronunciationkə(ʊ)ˈkeɪn
Trade namesNeurocaine, Goprelto, Numbrino, others
Other namesCoke, blow, snow, crack (in free base form)
AHFS/Drugs.comMicromedex Detailed Consumer Information
License data
Dependence
liability
Physical: Low Psychological: High
Addiction
liability
High
Routes of
administration
Topical, by mouth, insufflation, intravenous, inhalation
Drug class
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability
MetabolismLiver, CYP3A4
MetabolitesNorcocaine, benzoylecgonine, cocaethylene
Onset of actionSeconds to minutes
Duration of action20 to 90 minutes
ExcretionKidney
Identifiers
  • Methyl (1R,2R,3S,5S)-3-(benzoyloxy)-8-methyl-8-azabicyclo[3.2.1]octane-2-carboxylate
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
PDB ligand
CompTox Dashboard (EPA)
ECHA InfoCard100.000.030 Edit this at Wikidata
Chemical and physical data
FormulaC17H21NO4
Molar mass303.358 g·mol−1
3D model (JSmol)
Melting point98 °C (208 °F)
Boiling point187 °C (369 °F)
Solubility in water1.8g/L (22 °C)
  • CN1[C@H]2CC[C@@H]1[C@@H](C(OC)=O)[C@@H](OC(C3=CC=CC=C3)=O)C2
  • InChI=1S/C17H21NO4/c1-18-12-8-9-13(18)15(17(20)21-2)14(10-12)22-16(19)11-6-4-3-5-7-11/h3-7,12-15H,8-10H2,1-2H3/t12-,13+,14-,15+/m0/s1 checkY
  • Key:ZPUCINDJVBIVPJ-LJISPDSOSA-N checkY
Data page
Cocaine (data page)
 ☒NcheckY (what is this?)  (verify)

Cocaine stimulates the reward pathway in the brain. Mental effects may include an intense feeling of happiness, sexual arousal, loss of contact with reality, or agitation. Physical effects may include a fast heart rate, sweating, and dilated pupils. High doses can result in high blood pressure or high body temperature. Onset of effects can begin within seconds to minutes of use, depending on method of delivery, and can last between five and ninety minutes. As cocaine also has numbing and blood vessel constriction properties, it is occasionally used during surgery on the throat or inside of the nose to control pain, bleeding, and vocal cord spasm.

Cocaine crosses the blood–brain barrier via a proton-coupled organic cation antiporter and (to a lesser extent) via passive diffusion across cell membranes. Cocaine blocks 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, causing euphoria and arousal. 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 mental and physical effects of cocaine exposure.

A single dose of cocaine induces tolerance to the drug's effects. Repeated use is likely to result in addiction. Addicts who abstain from cocaine may experience prolonged craving lasting for many months. Abstaining addicts also experience modest drug withdrawal symptoms lasting up to 24 hours, with sleep disruption, anxiety, irritability, crashing, depression, decreased libido, decreased ability to feel pleasure, and fatigue being common. Use of cocaine increases the overall risk of death, and intravenous use potentially increases the risk of trauma and infectious diseases such as blood infections and HIV through the use of shared paraphernalia. It also increases risk of stroke, heart attack, cardiac arrhythmia, lung injury (when smoked), and sudden cardiac death. Illicitly sold cocaine can be adulterated with fentanyl, local anesthetics, levamisole, cornstarch, quinine, or sugar, which can result in additional toxicity. In 2017, the Global Burden of Disease study found that cocaine use caused around 7,300 deaths annually.

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