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PS268 Midterm 2 Notes.docx

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Bruce Mc Kay

Lesson 9 CH 6 CocaineAmphetamines91 Cocaine thcocaine was first introduced and widespread into Western Europe and the North American in the 19 centuryneither cocaine or amphetamines have achieved widespread social acceptance as recreational drugsCocaine is a powerful CNS stimulant that creates intense feelings of pleasure increases alertness and decreases appetite and the need for sleepit is the active chemical in the coca plantHistoryorigin of the earliest civilization in the Americas beginning around of what was to become the Inca Empire 5000 BCEin Peru has been traced to the use of coca a bush that grows in the Andes and produces cocaineNatives of the Andes Mountains in Bolivia and Peru still use coca today as their ancestors did chewing the leaves and holding a ball of coca leaf almost continually in the mouththe psychoactive effects can be made stronger by adding calcified lime to raise the alkalinity inside the mouththis increases the extraction of cocaine and allows greater absorption into the blood supplying the inside of the mouththe terrain in the Andes in Bolivia and Peru is poorly suited for growing almost everything but Erythroxylon coca however seems to thrive at elevations of 6002400 metres on the Amazon slopeof the mountains where more than 254 cm of rain fall annuallythe shrub is pruned to prevent it from reaching normal height of 23 m so that the picking which is done 34 timesyris easier to accomplishshrubs are grown in small onehectare patches called cocalssome which are known to be under cultivation for over 800 yrscoca leaf was recognized as increasing strength and endurance while decreasing the need for foodCoca WineAngelo Mariani a French chemisthe contributed by introducing the coca leaf indirectly to the general public he imported metric tons of coca leaves and used an extract from them in many productsyou could suck on a coca lozenge drink coca tea or obtain the coca leaf extract in any of a large number of other productsit was Marianas coca wine that made him rich and famousVin Mariani was a tonic wine and patent medicine containing coca leaf extract created circa 1863 by French chemist Angelo Marianifor the general public as it had for the Incasfor a thousand years and was to do for the Americans who drank early versions of Cocacolathe extract of the coca leaf lifted their spirits freed them from fatigue and gave them a generally good feelingLocal AnaesthesiaKarl Koller an Austrian ophthalmologist born in 1857 who was the first to introduce cocaine as a local anaesthetic for eye surgeryFreud was already fully aware of the painkilling properties of cocaine but Koller recognized its tissue numbing capabilitiesin 1884 Koller established cocaines potential to the medical community revolutionizing eye surgery later it was used for other medical fields such as dentistryEarly Psychiatric UsesSigemund Freud a young Viennese physician studied the drug for its potential as a treatment medication in a variety of ailments including depression and morphine dependencehe urged his fiance his sisters his colleagues and his friends to try it extolling the drug as a safe exhilarant which he himself used and recommended as a treatment for morphine dependenceafter using on a friend he generally opposed the use of drugs in the treatment of psychological problems Legal controls on Cocainecocaine use before 1985 in NA had come to symbolize wealth and fame in part because street sales of the drug were mainly in the hydrochloride form in quantities that made the price relatively expensivethe infrequentuse of smoked cocaine changed in the midto late 1980s when enterprising dealers began selling smokeable cocaine in the form of crackthe cocaine experience was now available to any one with 510 a lighter a glass pipe and access to a dealerThe Controlled Drugs and Substances Act was passed in 1996 repealing the Narcotic Control Act and Parts III in Canada cocaine is classified into and IV of the Food and Drug ActSchedule Iunlawful possession is subject to fines up to 1000 or imprisonment for up to 6 mths or both for a first offence penalties are greater for possession of larger amounts of subsequent offencesSupplies of Illicit Cocaine In CanadaColombia remained the worlds largest cultivator of coca bush with 81 000 hectares followed by Peru 56 100 H and Bolivia 30 500 HMexicos role as a transit country for cocaine destined for Canada has increased not only by way of the MexicoUSCanada highway corridor but also by direct shipments via air and marine modesthe largest proportion of cocaine smuggled into Canada continues to be concentrated at major ports of entry located in British Columbia Ontario and Quebecrecently the land mode was ranked as the primary smuggling methodonce smuggled into Canada cocaine is trafficked from the Pacific region to other Western Provinces while the central provinces of Quebec and Ontario have been identified as supplying the user population in the Maritimesboth price and purity have remained somewhat steady for the past decade a kg of cocaine sells for 13 000 to 25 000 in most US cities and the average purity of samples purchased or seized by DEA agents was between 50 and 75 table 61 p 116statsCocaine Crime and Ethnicitydrug laws in the US have been criticized because of the belief that they have had selective effects on Black communitiesstudy was conducted and here are the findings1 the current penalties exaggerate the relative harmfulness of crack cocaine2 current penalties sweep too broadly and apply most often to lowerlevel offenders3 current quantitybased penalties overstate the seriousness of most crack cocaine offences and fail to provide adequate proportionality 4 current penalties severity mostly affects BlacksCanada does not keep racial characteristics of federal cocaine offenders but it has been found that a larger proportion of visible minority than Caucasian offenders are incarcerated for drug related offences but smaller proportions are incarcerated for other offences such as property offences and sexrelated offencesa larger proportion of Black offenders are incarcerated for robbery while a larger proportion of Asian offenders are incarcerated for drugrelated offences Caucasian offenders are overrepresented in homicide offences while Black offenders are overrepresented in violent offencesPharmacology of CocaineSource Coca is a plant in the family Erythroxylaceae native to northwestern South America coca is best known because of its alkaloids which include cocaine powerful stimulant the plant resembles a blackthorn bushand grows to the height of 23 m the branches are straight leaves have a green tint and are thin opaque oval and taper at the extremitiesa marked characteristic of the leaf is an areolated portion bounded by two longitudinal curved lines one line on each side of the midrib and more conspicuous on the underside of the leafChemical Structure p 118 imageForms of Cocaineas part of the process of making illicit cocaine the coca leaves are mixed with an organic solvent such as kerosene or gasolineafter thorough soaking mixing and mashing the excess liquid is filtered out to form a substance known as coca paste crude extract containing cocaine in a smokeable formin SA it is often mixed with tobacco and smokedpaste can also be made into cocaine hydrochloride the most common form of pure cocaine it is stable and water solublea salt that mixes easily in water and is so stable it cannot be heated to form vapours for inhalation recreational users of this form of cocaine either snort or inject the drug intravenouslysome users who wased to smoke cocaine used to convert it into freebase a method of preparing cocaine as a chemical base so that it can be smoked by extracting it into a volatile organic solvent such as ether freebase can be heated and the vapours inhaledpopularity of this method of freebase declined when it was discovered that mixing cocaine with simple household chemicals including baking soda and water and then drying it resulted in a lump of smokeable cocaine crack or rock92 Mechanism of Actioncocaine blocks the reuptake of dopamine norepinephrine and serotonin causing a prolonged effect of these neurotransmittersthe latest belief is that cocaines behavioural effects depend on an interaction of multiple neurotransmitters including dopamine serotonin GABA and glutamatein a normal communication process dopamine is released by a neuron into the synapse where it can bind to dopamine receptors on neighbouring neuronsdopamine is normally then recycled back into the transmitting neuron by a specialized protein called the dopamine transporterif cocaine is present it attaches to the dopamine transporter and blocks the normal recycling process resulting in a buildup of dopamine in the synapse which contributes to the pleasurable euphoric effects of cocaineAbsorption and Eliminationchewing and sucking the leaves allows the cocaine to be absorbed slowly through the mucous membranesresulting in a slower onset of effects and much lower blood levels than are usually obtained via snorting most common route of administrationin snorting the intent is to get the very fine cocaine hydrochloride powder into the nasal passages right on the nasal mucosa from there it is absorbed quite rapidly and through circulatory mechanisms it reaches the brain rather quicklyintravenous use of cocaine delivers a very high concentration to the brain producing a rapid and brief effectit used to be a favourite administration among compulsive usersthe smoking of crack is now preferred by most compulsive users now because this route is less invasivecocaine molecules are metabolized by enzymes in the halfblood and livercocaine itself is rapidly removed with a life of an hour the major metabolites which are the basis of urine screening testshave a longer halflife of about eight hoursMedical Uses of Cocaineit was used as a local anaesthetic and was sold and used without any scientific evidence of its effect in a variety of countless patented tonics and elixirs for a number of medical conditions
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