24 - Cocaine - Cocaine ( benzoyl-methyl-ecgonine )...

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Unformatted text preview: Cocaine ( benzoyl-methyl-ecgonine ) (C17H21NO4) is a crystalline alkaloid prepared from the leaves of the Erythroxylon coca plant, which grows mainly in South America & to a lesser extent in Africa , far east & India. Coca Leaves and Cocaine Hydrochloride powder 1. Cocaine hydrochloride (powder) : prepared by dissolving the alkaloid in hydrochloric acid, forming a water soluble salt. 2. Crack cocaine : produced when cocaine hydrochloride is mixed with sodium bicarbonate and water, and then heated. Rocks of crack cocaine Cocaine can be administered as a drug of abuse in the following ways : 1. Cocaine hydrochloride : snorting (intranasal), smoking, intravenous (including being mixed with heroin, ingestion or application to genitalia. 2. Crack cocaine : inhalation of vapour from heated foil or pipe. 3. Coca leaves : chewed/ ingested. Route Onset Peak effect(mi n) Duration (min) Half-life (min) Inhalation 7 s 1-5 20 40-60 IV 15 s 3-5 22-30 40-60 Nasal 3 min 15 45-90 60-90 Oral 10 min 60 60 60-90 Onset & Duration of action for cocaine depends on the route of administration. Distribution : most body organs, including the heart, kidney, adrenal glands, and liver. Cocaine (and its hydrolytic metabolites) appears in blood, urine, hair, sweat , saliva , and breast milk. Analysis of these tissues and fluids is used for drug detection in workplace, legal, and treatment settings. Metabolism and excretion : Cocaine is extensively metabolized, primarily in the Liver by hydrolysis, with only about 10% excreted unchanged in the urine. The metabolism is by hydrolytic ester cleavage, so the eliminated metabolites consist mostly of benzoylecgonine . Benzoylecgonine can be detected in urine within four hours after cocaine intake . If taken with alcohol , cocaine combines with the ethanol in the liver to form cocaethelyne & causing more euphoria . Cocaine is a central nervous system stimulant, which gives rise to feelings of euphoria, excitement, increased motor activity and a feeling of being energised. Its principal mode of action is the blockade of the transporter protein that is responsible for the reuptake of monoamines [i.e. noradrenaline (mainly) , seroton & dopamine] into presynaptic terminals of neurons releasing these neurotransmitters . When given locally : Blockage of sodium channel resulting in marked local anesthetic effects....
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This note was uploaded on 12/21/2011 for the course STEP 1 taught by Professor Dr.aslam during the Fall '11 term at Montgomery College.

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24 - Cocaine - Cocaine ( benzoyl-methyl-ecgonine )...

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