Cocaine: Full Drug Profile

Cocaine - General Information

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.

Pharmacology of Cocaine

Cocaine is a local anesthetic indicated for the introduction of local (topical) anesthesia of accessible mucous membranes of the oral, laryngeal and nasal cavities.

Cocaine for patients

Cocaine Interactions

No information provided.

Cocaine Contraindications

Cocaine Hydrochloride is contraindicated in patients with a known history of hypersensitivity to the drug or to the components of the solution.

Additional information about Cocaine

Cocaine Indication

For the introduction of local (topical) anesthesia of accessible mucous membranes of the oral, laryngeal and nasal cavities.

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).

Generic Name

Cocaine

Synonyms

Benzoylethylecgonine; Bazooka; Badrock; Benzoylmethylecgonine; Bernice; Bernies; Beta-Cocain; Blast; Blizzard; Blow; Bouncing Powder; Bump; Burese; C" Carrie; Cocaine Free Base; Cocaina; Cocaine-M; Cocain; Coca; COC; Cholly; Chicken Scratch; Charlie; Cecil; Caviar; Carrie; Candy; Cabello; Dextrocaine; Depsococaine; Delcaine; Dama Blanca; D-pseudococaine; Corine; Cola; Coke; Cocktail; Zip; Yeyo; Trails; Toot; Toke; Sweet Stuff; Sugar; Star-Spangled Powder; Star Dust; Snort; Sleighride; Rock; Prime Time; Pimp's Drug; Neurocaine; Moonrocks; Methyl Benzoylecgonine; Line; Leaf; Lady; L-Cocaine; L-Cocain; Kokayeen; Kokan; Kokain; Kibbles N' Bits; Jam; Isococaine; Isococain; Isocaine; Hell; Heaven; Happy Trails; Happy Powder; Happy Dust; Green Gold; Goofball; Gold Dust; Girl; G-Rock; Freeze; Foo Foo; Florida Snow; Flex; Flake; Erytroxylin; Eritroxilina; Dust

Drug Category

Vasoconstrictor Agents; Anesthetics; Local Anesthetics

Drug Type

Small Molecule; Illicit; Approved

Other Brand Names containing Cocaine

Cocaine;

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.

Toxicity (Overdose)

Intense agitation, convulsions, hypertension, rhythm disturbance, coronary insufficiency, hyperthermia, rhabdomyolysis, and renal impairment. Oral mouse LD₅₀ = 96 mg/kg

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.

Half Life

1 hour

Dosage Forms of Cocaine

Liquid Topical

Chemical IUPAC Name

methyl (2R,3S)-3-(benzoyloxy)-8-methyl-8-azabicyclo[3.2.1]octane-2-carboxylate

Chemical Formula

C17H21NO4

Cocaine on Wikipedia

https://en.wikipedia.org/wiki/Cocaine

Organisms Affected

Humans and other mammals