Overview
| Generic Names: | Badrock; Bazooka; Benzoylethylecgonine; Benzoylmethylecgonine; Bernice; Bernies; Beta-Cocain; Blast; Blizzard; Blow; Bouncing Powder; Bump; Burese; C" Carrie; COC; Cabello; Candy; Carrie; Caviar; Cecil; Charlie; Chicken Scratch; Cholly; Coca; Cocain; Cocaina; Cocaine Free Base; Cocaine-M; Cocktail; Coke; Cola; Corine; D-pseudococaine; Dama Blanca; Delcaine; Depsococaine; Dextrocaine; Dust; Eritroxilina; Erytroxylin; Flake; Flex; Florida Snow; Foo Foo; Freeze; G-Rock; Girl; Gold Dust; Goofball; Green Gold; Happy Dust; Happy Powder; Happy Trails; Heaven; Hell; Isocaine; Isococain; Isococaine; Jam; Kibbles N' Bits; Kokain; Kokan; Kokayeen; L-Cocain; L-Cocaine; Lady; Leaf; Methyl Benzoylecgonine; Moonrocks; Neurocaine; Pimp's Drug; Prime Time; Rock; Sleighride; Snort; Star Dust; Star-Spangled Powder; Sugar; Sweet Stuff; Toke; Toot; Trails; Yeyo; Zip |
|---|---|
| Trade Names: | Cocaine |
| PharmGKB Accession Id: | PA449072 |
Description
An alkaloid ester extracted from the leaves of plants including coca. It is a local anesthetic and vasoconstrictor and is clinically used for that purpose, particularly in the eye, ear, nose, and throat. It also has powerful central nervous system effects similar to the amphetamines and is a drug of abuse. Cocaine, like amphetamines, acts by multiple mechanisms on brain catecholaminergic neurons; the mechanism of its reinforcing effects is thought to involve inhibition of dopamine uptake. PubChem (source: Drug Bank)
Indication
For the introduction of local (topical) anesthesia of accessible mucous membranes of the oral, laryngeal and nasal cavities. (source: Drug Bank)
ATC Therapeutic Categories
- N01BC:Esters of benzoic acid
- R02AD:Anesthetics, local
- S01HA:Local anesthetics
- S02DA:Analgesics and anesthetics
Pharmacology, Interactions, and Contraindications
Mechanism Of Action
Cocaine produces anesthesia by inhibiting excitation of nerve endings or by blocking conduction in peripheral nerves. This is achieved by reversibly binding to and inactivating sodium channels. Sodium influx through these channels is necessary for the depolarization of nerve cell membranes and subsequent propagation of impulses along the course of the nerve. Cocaine is the only local anesthetic with vasoconstrictive properties. This is a result of its blockade of norepinephrine reuptake in the autonomic nervous system. Cocaine binds differentially to the dopamine, serotonin, and norepinephrine transport proteins and directly prevents the re-uptake of dopamine, serotonin, and norepinephrine into pre-synaptic neurons. Cocaine also produces a number of indirect actions, which alter other neuromodulatory systems (i.e., opioidergic, glutamatergic, and GABAergic systems). (source: Drug Bank)
Pharmacology
Cocaine is a local anesthetic indicated for the introduction of local (topical) anesthesia of accessible mucous membranes of the oral, laryngeal and nasal cavities. (source: Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
Hepatic. Cocaine is metabolized to benzoylecgonine and ecgonine methyl ester, which are both excreted in the urine. In the presence of alcohol, a further active metabolite, cocaethylene is formed, and is more toxic then cocaine itself. (source: Drug Bank)
Absorption
Cocaine is absorbed from all sites of application, including mucous membranes and gastrointestinal mucosa. By oral or intra-nasal route, 60 to 80% of cocaine is absorbed. (source: Drug Bank)
Toxicity
Intense agitation, convulsions, hypertension, rhythm disturbance, coronary insufficiency, hyperthermia, rhabdomyolysis, and renal impairment. Oral mouse LD<sub>50</sub> = 96 mg/kg (source: Drug Bank)
Isomeric SMILES Code:
CN1C2CCC1[C@H]([C@H](C2)OC(=O)c3ccccc3)C(=O)OC (source: Drug Bank)
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
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BCHE |
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CNR1 |
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COMT |
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CYP2D6 |
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DRD1 |
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HOMER1 |
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A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
| Gene | Description | |
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| DRD1 |
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(source: Drug Bank) |
| DRD3 |
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(source: Drug Bank) |
| OPRK1 |
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(source: Drug Bank) |
| SCN5A |
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(source: Drug Bank) |
| SCN10A |
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(source: Drug Bank) |
| SCN11A |
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(source: Drug Bank) |
| SLC6A1 |
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(source: Drug Bank) |
| SLC6A3 |
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(source: Drug Bank) |
| SLC6A2 |
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(source: Drug Bank) |
| SLC6A4 |
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(source: Drug Bank) |
A list of non-curated publications that mention this drug along with other drugs is available.
Curated Information
The following diseases are in curated knowledge about this drug.
| Disease | Relationship | Evidence | |
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Apnea |
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Cocaine-Related Disorders |
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Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
Additional Datasets
These datasets are minimally curated and are sorted alphabetically by title.
LinkOuts
Common Searches
Search PubMed
Search Medline Plus
Search PubChem
Search CTD
Non-Curated Publications
A list of non-curated publications that mention this drug is available.
