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Uppers Downers & All Arounders Uppers/Stimulants Chapter 3 Uppers/Stimulants • In 1999 about • 1.7 million Americans used amphetamines for nonmedical reasons, • 4.2 million used cocaine, • 68 million smoked cigarettes, • 200 million drank coffee, tea, caffeinated soft drinks or an over-the-counter medication containing caffeine. (p. 83). General Classification • Most people use stimulants in the form of: – Diet aids – Drugs to control hyperactivity – Coffee & Tea – Cigarettes – Caffeinated solf drinks • Stimulants are found in plants and in synthetic form General Effects • Stimulants force the release of the energy chemicals (epinephrine and norepinephrine along with dopamine and serotonin) • Infuses the body with large amounts of extra energy before the body needs it • With heavy use the body’s energy supply is depleted leading to crash, withdrawal and depression • Crash and withdrawal occurs when energy supplies become depleted and body is left without reserves General Effects • All Stimulants activate chemical and electrical activity in central nervous system – Increases • Heart rate • Blood pressure • Respiration – Effects include • Activeness • Restlessness – Medical uses include treatment of obesity, narcolepsy and Attention-deficit/hyperactivity Disorder General Effects • Reward/reinforcement center is artificially overstimulated – Rush of pleasure and strong sense of wellbeing – Often accompanied by no basic need for hunger, thirst or sex • Weight loss: stimulants fool the body into thinking it has satisfied hunger without eating • Cardiovascular side effects include constricted blood vessels, high blood pressure and sometimes arrhythmia – Chronic use weakens blood vessels and risk of stroke General Effects • Emotional & mental effects: – Initial release causes increase of confidence and euphoria – As use continues feeling of euphoria turn to irritability, paranoia, aggressiveness, depression • Tolerance & Addiction liability – Increases as body loses its ability to synthesize drugs – Can also develop with methamphetamine congeners, caffeine, nicotine and other mild stimulants COCAINE • Cocaine epidemics seem to occur every few generations • Hardcore use still strong in 2000’s • Cocaine is extracted from coca plant – 97% grown in South America – Colombian drug Cartels control cultivation and production – 2/3 of smuggling handled by drug artels in Mexico – U.S. consumes 70% of world’s cocaine trade COCAINE: Routes of Administration • Chewing Leaf: Historically Native cultures • Drinking: Started in 1880’s in wine, coca cola, and patent medicine. Widely prescribed to womem • Injecting: Started after the invention of hypodermic needle in 1853 – Intravenous use takes 15-30 seconds – Subcutaneous/intramuscular takes 3-5 minutes • Snorting: Self-limiting method – The more snorted, the less absorption due to constriction of capillaries in the nose – Destructive to nasal passages COCAINE: Routes of Administration • Mucosal & contact absorption – Can be absorbed through mucosal tissue in nose, mouth, rectum & vagina – Delivery method is also used for dental work, minor surgeries • Smoking: – First introduced in 1914, but high temperature was needed to keep cocaine cigarettes going – Mid-1970’s, cocaine hydrochloride was chemically altered into freebase – Fastest form to reach brain… Highly addictive COCAINE: Physical and Mental Effects • Metabolism: Quickly metabolized and disappears faster than methamphetamine • Medical Use: Only naturally occurring local anesthetic – Used to numb nasal passages, eyes, throat, and chronic sores • Neurochemistry & Central Nervous System – Forces relase of norepinephrine, epinephrine and dopamine – Blocks re-absorption so more intense stimulation – Blocks 60-70% of dopamine reuptake – Too much dopamine can over stimulate brain’s fright center causing paranoia. COCAINE: Physical and Mental Effects • Sexual Effects: – At low doses cocaine increases desire for sex and delay ejaculation – As use continues sexual dysfunction occurs • Aggression, violence & cocaethylene – Increases aggression & violence by disrupting inhibitory and fright centers of the brain – Cocathylene (metabolite when cocaine & alcohol is combined) induces greater agitation, euphoria and violence • Can also induce cardiac conduction abnormalities COCAINE: Physical and Mental Effects • Cardiovascular Effects – – – – Can damage circulatory system Raise blood pressure Cause stroke (bursting of blood vessels in brain) Cause heart damage • Neonatal Effects: – Transmitted within seconds to fetus – Increases chances for miscarriage, stroke, SIDS, respiratory ailments, mental delays & other abnormalities – Proper pre-natal and post natal treatment can hel cocaine babies COCAINE: Physical and Mental Effects • Tolerance: To the euphoric effect can begin to develop after first injection or smoking session • Withdrawal, Craving & relapse: – Major effects include anhedonia, lack of energy and intense craving – Typical cycle of compulsive use: • Bingeing to crashing to detox to resolutions of abstinence or treatment and relapsing 2-4 weeks later. COCAINE: Physical and Mental Effects • Overdose: – – – – – Can be caused by as little as 1/50 gram Overwhelmingly intense stimulation Injury to heart and blood vessels More often not fatal…just feels that way Severe reaction through in verse tolerance or kindling • Miscellaneous Effects: – – – – Formication (itching from imaginary bugs) Dental erosion Seizures Gastrointestinal complications • Cocaine Psychosis: – Paranoid psychosis/schizophrenia caused by excess dopamine – Can also activate genetic predisposition to schizophrenia COCAINE: Other Problems with Use • Polydrug Use – Alcohol, valium, heroin to take the edge off • Adulteration & Contamination – Cocaine at street level is almost always cut – When injected, bacteria and viruses contaminate drugs and needles – Hepatitis C rate for IV drug users is between 50% and 90% • Compulsion – Use for euphoria, boredom, peer pressure, curiosity, self-medication, escape from personal problems Smokable cocaine (freebase, crack, paste) Copyright 2004, CNS Productions Inc. 6 SMOKABLE COCAINE (CRACK & FREEBASE) • Pharmacology of smokable Cocaine – – – – – – Began around 1981 Crack epidemic in 1986 Chemically crack is the same as freebase Delivered to the brain faster Ether converts cocaine to freebase Baking soda converts cocaine to crack • Effects and Side Effects – More intense than snorting or injecting – Rush or euphoria last 5 – 20 minutes – Replaced by the feeling of irritability and other negative emotions – Always used in a binge pattern – Chronic use include paranoia, intense cravings, depression, cocaine psychosis, high-risk sexual activity SMOKABLE COCAINE (CRACK & FREEBASE) • Respiratory Effects – Breathing problems – Severe fever – Chest pains – Coughs – Crack lung – Hemorrhage – Respiratory failure & death – Aggravated by cigarette smoking • Polydrug use – Increases the potential for abuse of SMOKABLE COCAINE (CRACK & FREEBASE) • Overdose – – – – Mild-rapid heart beat Hyperventilation Fear of dying Kills several thousand a year due to • • • • • Cardiac arrest Seizure Stroke Respiratory failure Severe hypothermia • Consequences of Crack use – Economic – Social: abuse, family, legal, formation of sex trade • Cocaine vs Amphetamines – Cocaine’s duration is 40 minutes/ Meth is 4-6 hours – Meth is cheaper Amphetamines Methamphetamines Copyright 2004, CNS Productions Inc. 9 “Ice” Copyright 2004, CNS Productions Inc. 10 Amphetamines • Classification: “Sympathomimetic agent” – Stimulate the release of sympathic neurotransmitters – Activates the sympathetic nervous system that controls the fight or flight response – Stimulates the reward/information center – Street names: crank, ice, shabu, glass, clear • History of Use – – – – – First synthesized in 1887 Medically used in 1930s Treats narcolepsy & depression Used by students and truck drivers to stay awake Widely used in pill form during WW II Amphetamines • History of Use – Japanese epidemic continued after WW II – 1970 6-8% of American population used prescribed amphetamines for weight loss – Street speed chemists increased production of crank and crystal in late 1980s – Ice highly potent smokable form used in 1990’s and common use in Hawaii – Recent development of “ya ba” in Thailand Amphetamines (Effects) • Routes of Administration – – – – Snorting Intravenous Smoking Oral • Neurochemistry – Like cocaine, amphetamines increase levels of catecholamines by stimulating their release and blocking reuptake – Unlike cocaine, amphetamines block metabolism – Long term use alters the ability to produce vital neurotransmitters causing depression and taking mor to stay normal Amphetamines (Effects) • Physical Effects – Small to moderate doses cause • • • • • • • Increased heart rate Raised body temperature Rapid respiration Higher blood pressure Extra energy Dilation of bronchial vessels Appetite suppression – Meth users go on binges for 3, 4 or 10 days • • • • • Long term use can cause sleep deprivation Heart & blood toxicity Severe malnutrition Bad or rotten teeth Tolerance is more pronounced Amphetamines (Effects) • Mental & Emotional Effects – Mild to intense euphoria / sense of wellbeing – Prolong use leads to • • • • • • • • • Irritability Paranoia Anxiety Confusion Poor judgement Hallucinations Delusions Can result in violent, suicidal & homicidal thoughts Antisocial behaviors Amphetamines (Effects) – With abstinence, disturbed mental states such as amphetamine psychosis or depression can stop for some people – Amphetamines release neurotransmitter that mimics sexual gratification • Effects of Ice is greater on the brain than the respiratory and pulmonary system – Results in more overdoses – Greater mental side effects – Longer detoxification Lookalike Stimulants Any combination of Caffeine Ephedrine Pseudoephedrine Copyright 2004, CNS Productions Inc. 13 Amphetamine Congeners/Lookalikes • Methylphenidate (Ritalin) – Most widely used – Prescribed as mood elevator, narcolepsy and to treat Attention-deficit/hyperactivity disorder • Diet Pills – Only recommended for short-term use – Careful monitoring by physician – Long-term use associated with abuse • Lookalikes – Prescription drugs that contain ephedrine and pseudoephedrine (anti-asthmatics) – Decongestants – Caffeine – Ephedra & ephedrine Miscellaneous Plant Stimulants • Khat & methcathione – Used in Arab and African countries – Produces amphetamine like highs – Insomnia, anorexia – Chronic abuse cause exhaustion, violence & depression – Methcathione: AKA ephedrone is synthesized in illegal labs in U.S. • Sold as a powerful alternative to methamphetamine Miscellaneous Plant Stimulants • Betel Nuts (seed of betel palm) – Used by 200 million people in Arab world, India and Asia – Effects similar to nicotine – High doses can be toxic and produce psychological dependence • Yohimbine – – – – – Spicy extract from African yohimbe tree Used in tea Medicine Aphodisiac Produces mild euphoria and occassional hallucinations Miscellaneous Plant Stimulants • Ephedra – Ephedra bush – Mild stimulant used as medicine, tea & tonic – Also used by athletes for energy boost – Banned in U.S. because of overdoses – This drug and synthetic version is main ingredients in methamphetamine & methcathione – Herbal Ecstasy and Herbal Nexus are two herbal products marketed as stimulants and as buffers for illegal drugs • Contains herbal forms of ephdrine, caffeine, herbs and vitamines Miscellaneous Plant Stimulants • Caffeine – Most popular stimulant in the world – Found in teas, coffee, soft drinks, chocolate & hundreds of medications • History – Tea: drunk in China as early as 2700 B.C. • Introduced to Europe in 16th Century – Coffee: Cultivated in Ethiopia A.D. 650 and spread to Arabia then Europe • Classified as a drug and banned in many cultures – Cocoa: Mayan and Aztec royalty • Only small amount of caffeine in cocoa Miscellaneous Plant Stimulants • Pharmacology – Classified as an akaloid of the chemical class called xanthines – Found in more than 60 plants – Takes 15-35 hours for 95% of the caffeine to be excrete by the body • Physical and Mental Effects – Mild stimulant – 5-7 cups of coffee can cause anxiety, insomnia, nervousness – Higher doses can cause muscle twitching, increased heart rate, palpatations – Letal at about 10 grams (100 cups of coffee) Miscellaneous Plant Stimulants • Tolerance, withdrawal & addiction – Dosages vary depending on person – Symptom includes throbbing headache – Dependence can occur with 5 cups of coffee 10 cola drinks or 8 cups of tea • Nicotine – Cigarettes account for 90% of all tobacco use in U.S. – Discover in American and spread to Europe – Smokeless tobacco: moist snuff, powder snuff & loose-leaf • Absorbed by mucosal in the mouth and nise U.S. Cigarette Use, 2001 (12 & older) Ever used 68.9% 151.6 million Used past year 29.5% 65.6 million Used past month 24.9% 56.3 million Copyright 2004, CNS Productions Inc. 16 Nicotine/Tobacco • Pharmacology – Nicotine is the most important ingredient – Average cigarette contains 10 mg of nicotine – Central Nervous system stimulant that disrupts the balance of neurotransmitters • • • • • • • • • Dopamine Endorphins epinephrine, Acetylcholine Constricts blood vessels Raises heart rate Depresses appetite Produces mild euphoria Deadens senses Nicotine/Tobacco • Two most important reasons people smoke tobacco is: – Weight loss – Craving • One must keep a certain level in blood stream to avoid withdrawal • Tolerance develops quickly • Withdrawal causes: – – – – – – – Headaches Nervousness Fatigue Severe irritability Intense craving Poor concentration Sense of relaxation from smoking a cigarette is Nicotine/Tobacco • Addiction – Tobacco is pure example of addiction process • 80% want to quit & 10% want to cut down • May have a genetic predisposition to nicotine addiction • Side Effects – Tobacco & smoke contain more than 4,000 other chemicals of which 400 are classified as toxic Nicotine/Tobacco • • • • 1997: 3.5 million premature deaths In U.S. 392,000 die prematurely 50,000 die of second hand smoke Cardiovascular & Respiratory effects: – Plaque formation – Hardening of the arteries – Leading cause of heart attacks – Lung cancer – Men who smoke are 22 x’s more chance of cancer