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Active ingredient: Cocaine - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

  • Vasoconstrictor Agents
  • Anesthetics
  • Local Anesthetics

Dosage Forms

  • Liquid

Brands / Synonyms

Badrock; Bazooka; Benzoylethylecgonine; Benzoylmethylecgonine; Bernice; Bernies; Beta-Cocain; Blast; Blizzard; Blow; Bouncing Powder; Bump; Burese; C" Carrie; Cabello; Candy; Carrie; Caviar; Cecil; Charlie; Chicken Scratch; Cholly; COC; Coca; Cocain; Cocaina; Cocaine Free Base; Cocaine, L-; Cocaine-M; Cocktail; Coke; Cola; Corine; D-pseudococaine; Dama Blanca; Delcaine; Depsococaine; Dextrocaine; Dust; Ecgonine, Methyl Ester, Benzoate; 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; Line; Methyl Benzoylecgonine; Moonrocks; Neurocaine; None; Pimp's Drug; Prime Time; Rock; Sleighride; Snort; Star Dust; Star-Spangled Powder; Sugar; Sweet Stuff; Toke; Toot; Trails; White Girl or Lady; Yeyo; Zip

Indications

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

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.

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).

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

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

Biotrnasformation / Drug Metabolism

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.

Contraindications

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

Drug Interactions

No information provided.

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