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Chapter 12 - Stimulants History of Cocaine Shrubby plant-Erythroxylon coca-Andes Mountains Evidence of use in 6th century; probably much earlier German scientist-Albert Niemann-1860-named it cocaine Angelo Mariana-1869-Vin Mariani; combination of alcohol and cocaine produces a metabolite several times longer acting than cocaine alone; intoxicating Used by Pres. McKinley, Thomas Edison, Gen. Grant, Jules Verne, Sara Bernhardt, Popes Pious X and Leo XII Freud-experimented on himself, family, friends Carl Koller-eye operations Coca-Cola; Today: factory in NJ; select team of employees of Stepan Co.-remove cocaine from leaves Legally receives 175,000 kilograms from Peru each year; results in 1,750 kilograms of cocaine (20 mill. Hits of crack; street value=$200 million Sold for medical purposes-surgery Scope of Use 2008-1.9 million past month users (359,000 crack) 18-25 highest rate 2009-significant decline in past month use by 8th 10th and 12th graders from peak use in 1990s DAWN-2008-24% of ED visits involved cocaine (482,188) How Cocaine Produces Its Effects VTA (ventral tegmental area) most affected Nerve fibers from VTA extent to nucleus accumbens Short-Term Effects Effects begin immediately; gone in a few minutes or within an hour Small doses: euphoric; energetic; talkative; mentally alert; decreases need for food and sleep Duration: depends on route of administration-snorting: 1530 min; crack: 5-10 min PHYSIOLOGICAL EFFECTS: constricted blood vessels; dilated pupils; increased temp, heart rate, blood pressure; sometimes bizarre, erratic, violent behavior Restlessness, irritability; anxiety; panic; paranoia; tremors; vertigo; twitches Disturbances in heart rhythm & heart attacks; strokes; seizures; headaches; coma; death (cardiac arrest or seizures followed by respiratory arrest) Cocaine and alcohol-the most common 2-drug combination resulting in drug-related deaths Cocaine + alcohol = cocaethylene Increases: high blood pressure; elevated heart rate; abnormal heart rhythms; labored breathing 18-25 x increased risk of immediate death 62-90% of cocaine abusers also abuse alcohol Long-Term Effects Addiction Pharmacodynamic tolerance; at same time-increased sensitivity to cocaine’s toxic effects (convulsions) Binging-increased irritability; restlessness; panic attacks; paranoia Regular snorting: loss of sense of smell; nosebleeds; problems with swallowing; hoarseness; chronic inflamed runny nose Injected: allergic reactions Loss of appetite; weight loss Diminished sensitivity to rewards because of addiction (D2) Cocaine psychosis: formication; other hallucinations; feelings of anxiety and paranoia Increased risk of contracting HIV/AIDS; Hepatitis C (HCV); inject for 5 years-chances of HCV=50-80% Fetal Effects: premature delivery; low birth weight; small head circumference; shorter “Crack Babies” : one time written off; predicted to have severe, irreversible damage; reduced intelligence and social skills Multiple factors have to be considered: am’t./type of all drugs used; extent of prenatal care; maternal nutrition; exposure to sexually trans diseases; neglect or abuse of child; violence in environment; socioeconomic status; other health problems Treatments 2007-cocaine-13% of all admissions to drug abuse treatment programs; majority: crack and polydrug abusers Pharmacological Approaches: no FDA approved meds disulfirim (Antabuse) produces the most consistent reductions in use Compounds being tested-imbalance produced by cocaine on glutamate and GABA D3 receptors-meds are being tested for safety in humans Cocaine vaccine-prevents cocaine from entering the brain Behavioral Interventions Contingency Management/Motivational Incentives (MI)- vouchers; prizes: gym membership, movies, dinner; useful for achieving initial abstinence and staying in treatment Cognitive-behavioral therapy (CBT)-learning plays a role in development of abuse and addiction; helps patients recognize, avoid, & cope; effective for preventing relapse Therapeutic Communities-usually 6-12 mo. Stay; vocational rehab; learn to function in society Community-based recovery programs-Cocaine Anonymous12 step Treatment should match needs Amphetamine/Methamphetamine Chinese drug-mahuang-asthma Dr. Chen-Eli Lilly-1920s-ephedrine active ingredient in mahuang Gordon Alles-synthesized amphetamine while trying to develop a synthetic form of ephedrine; marketed; nasal inhaler; spread through 1930s Japanese scientist-methamphetamine; soldiers 1960s- “Speed Kills” Ice; ER admissions increases 460% from 1985-1994 in Cal.; 2006-law enforcement listed meth as #1 drug problem Scope of Meth Abuse Relationship between coke and meth About 10 million in U.S.-tried at lease once High use levels: Honolulu, San Diego, Seattle, San Francisco, Los Angeles, Atlanta HS seniors-2005-4.5% lifetime use; 8th grade-3.1%; 10th grade-4.1%; surveys show recent decline DAWN-50% increase in ED visits-1995-2002 (73,000); 4% of all drug-related visits in 2004 1992-5 states reported high rates of treatment admissions; 2002-21 states Methamphetamine Compared to Cocaine Meth-structurally similar to dopamine-different from coke Coke-quickly removed and almost completely metabolized in the body Meth-longer duration of action-large amount stays in body unchanged Meth-blocks dopamine reuptake; also increases release of dopamine Short-Term Effects Increased attention/decreased fatigue Increased activity and wakefulness Decreased appetite Euphoria and rush Increased respiration Rapid/irregular heartbeat hyperthermia Long-Term Effects Addiction Anxiety, confusion, insomnia Mood disturbances; violent behavior Psychosis: paranoia, visual and auditory hallucinations, delusions, formication; can last for years Changes in brain structure and function: alterations in dopamine system associated with reduced motor speed and impaired verbal learning; changes in structures associated with emotion and memory Severe dental problems; weight loss Recovery of Brain Dopamine Transporters in Chronic Meth Abusers Other Problems Risks During Pregnancy Knowledge is limited; a few human studies indicate increased rates of premature delivery; placental abruption; fetal growth retardation; heart and brain abnormalities Problem: sample size and use of other drugs Increased risk of HIV; hepatitis B and C Treatments Behavior therapies seem to be most effective Matrix Model: combines behavior therapy, family education, individual counseling, 12-step support, drug testing, encouragement for non-drug activities No specific meds for amphetamine; Wellbutrin-reduces the high and cravings