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PubChem
Name: Cocaine
PubChem Compound ID: 3518588
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.
Molecular formula: C17H22NO4+
Molecular weight: 304.361 g/mol
DrugBank
Identification
Name: Cocaine
Name (isomeric): DB00907
Drug Type: small molecule
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.
Synonyms:
Green Gold; Zip; Kokan; G-Rock; Happy Dust; Happy Powder; Trails; L-Cocaine; Cocktail; Blast.
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Brand: Cocaine
Category: Dopamine Uptake Inhibitors, Local Anesthetics, Vasoconstrictor Agents, Anesthetics, Anesthetics, Local
CAS number: 50-36-2
Pharmacology
Indication: 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 ...
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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.
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
Toxicity: Intense agitation, convulsions, hypertension, rhythm disturbance, coronary insufficiency, hyperthermia, rhabdomyolysis, and renal impairment. Oral mouse LD50 = 96 mg/kg
Affected organisms: Humans and other mammals
Interactions
Drug interaction:
IloperidoneCYP2D6 Inhibitors (Strong) such as cocaine may increase serum concentrations of the active metabolite(s) of Iloperidone. Specifically, concentrations of the metabolite P88 may be increased. CYP2D6 Inhibitors (Strong) may decrease serum concentrations of the active metabolite(s) of Iloperidone. Specifically, concentrations of the metabolite P95 may be decreased. CYP2D6 Inhibitors (Strong) may increase the serum concentration of Iloperidone. Reduce iloperidone dose by half when administered with a strong CYP2D6 inhibitor.
TolterodineCocaine may decrease the metabolism and clearance of Tolterodine. Monitor for adverse/toxic effects of Tolterodine.
ZuclopenthixolCocaine, a strong CYP2D6 inhibitor, may increase the serum concentration of zuclopenthixol by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zuclopenthixol if cocaine is initiated, discontinued or dose changed.
VoriconazoleVoriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of cocaine by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of cocaine if voriconazole is initiated, discontinued or dose changed.
DisulfiramIncreases the cardiac toxicity of cocaine
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