Major Stimulants

Major Stimulants

Histogram 8 7 6 Count 5 4 3 2 1 0 50 55

60 65 70 75 80 X! plus 85 90

95 100 Major Stimulants . Cocaine Amphetamine Cocaine Coke, Dust, Snow, Flake, Blow, Girl

Cocaine: Forms Coca leaf ( from Erythroxylum coca ) < 2% cocaine Cocaine HCL Powder; high cocaine content Freebase/Paste- high cocaine content /smokable Crack Rock cocaine- high cocaine content/ smokable cheaper/safer to produce

The Psychological Effects of Cocaine Euphoria Increased Vigilance Reduced reaction time Increased strength and endurance

Insomnia Anorexia Mood elevation Increased endurance High Dose & CNS Higher doses intense feeling of euphoria described as whole body orgasm

COCAINE- Sympathomimetic Effects Increased heart rate Increased blood pressure Increased respiratory rate Pupil dilation Vasoconstriction Increased sweating

History of stimulant use Coca and the Inca Archaeological evidence of coca use by Incans 5000 B.C.

Native tribes of the Andes have chewed the coca leaf for centuries. The coca plant was considered as divine. (Leaves contain 1% cocaine). Mountain natives chewed balls of leaves almost continually, distances were measured by the number of stops required to maintain dose level. Use of the Coca leaf has a long history and remains a tradition even today amongst some Native South Americans. Habitual Coca-leaf chewing is not generally regarded as a drug

addiction. However it is known that this habit is associated with minimum food consumption, which may in some cases adversely affect intellectual and physical functions. South American Issue today: Smoking basuco: ( making cocaine) Coca Paste: The paste is the middle step between the leaf and the powder cocaine. It is much more likely to cause dependence. It is generally very cheap in the

Andes countries. Coca paste is much more popular in South American countries then in the United States. (but see PACO. History of Cocaine.. cont Spanish explorers noticed the anti-fatigue effects of coca. Encouraged its use by natives to increase their work efforts . used coca leaf as payment Around 1855 , Albert Neiman isolated cocaine from the coca leaf and described the anesthetic action of the drug when it was put

on his tongue. The Rising Popularity of Cocaine -Late 1800s 1870 Vin Mariani (Coca wine) was for sale throughout France; containing 6 mg cocaine per ounce of wine. In the U.S.- Metcalfs Wine of Coca Public speakers, singers, and actors have found Wine of Coca to be a valuable tonic to the vocal cords. Athletes, pedestrians and base ball players have found by practical experience

that a steady course of coca taken both before and after any trial of strength or endurance will impart energy to every movement and prevent fatigue. Elderly people have found it a reliable aphrodisiac superior to any other drug... The Rising Popularity of Cocaine THE REAL THING!? In 1886, John Pemberton developed Coca Cola, a drink that contained cocaine and caffeine. Cocaine was REMOVED from Coca Cola in 1901 (but it still has the caffeine). The Rising Popularity of Cocaine Sigmund Freud (1884) 1884, recommended cocaine for a variety of illnesses and for alcohol and morphine addictions. Changing Sentiments Unfortunately, many of his patients ( and his Friend Ernst Von-Fleischl) went on to become addicted to cocaine and experience cocaine Psychosis. Freud Later retracted his statements and

support of the substance. Annie C. Meyers- Changing Public Sentiment A well-balanced Christian women before becoming a cocaine fiend I deliberately took a pair shears and pried loose a tooth that was filled with gold. I then extracted the tooth, smashed it up, and the gold went to the nearest pawnshop, blood streaming down my face

and drenching my clothes, where I sold it for 80 cents to buy cocaine. Around this time ( late 1800s and early 1900 ) there were also many reports of cocaine-related acts of violence. There was also a propaganda campaign aimed at associating cocaine use with minorities and minority violence. History of Cocaine Harrison Narcotic Act of 1914 Banned cocaine in the U.S.

History of Cocaine By 1930s, cocaine pretty much disappeared, but was replaced by amphetamine. By the late 1970s, coke began a comeback and use levels exploded around 1985 John Belushi

In November of 1983 colorful former Cowboys linebacker Thomas Hollywood Henderson was arrested for smoking crack with two under-aged teenage girls. In the meantime AMPHETAMINES Developed in the 1920s but not utilized until the 1930s

Amphetamines Effects..much like the Effects of Cocaine but with longer durations Euphoria Vigilance Reduced reaction time

Increased strength and endurance Insomnia Anorexia Mood elevation Increased endurance Amphetamines- effects on endurance R E V S /1 5 m in Performance on bicycle machine after control and 10 mg methamphetamine injections 3000

Drug 2800 2600 2400 Control 2200 2000 1

2 3 HOURS 4 5 Amphetamine: Forms

d-amphetamine l-amphetamine methamphetamine Methamphetamine is more potent than damphetamine, which is more potent than lamphetamine Ice Ice or or Crank Crank

Meth Crystals. Pure dmethylamphetamine HCL (pure methamphetamine will naturally form crystals) Is easier to vaporize ( smoke)

because of lower melting point. Started in the West moved east over time Labs all over Duplin Co. Very dangerous to synthesize Amphetamines ( cocaine effects but longer) - Sympathomimetic Effects

Increased heart rate Increased blood pressure Increased respiratory rate (dilation of bronchial villi of the lungs) Pupil dilation Changes in blood flow Increased sweating body temperature Amphetamine: A Brief History

1930s U.S. benzedrine marketed for treatment of asthma, narcolepsy, depression, appetite suppression (bennies) Amphetamine: A Brief History cont Also used to keep soldiers alert during combat in WWII After war, prescribed for fatigue and appetite suppression

Amphetamine in the 1960s Early 1960s - Unfortunately prescribed by physicians to treat heroin addiction. Dramatic explosion in the drug using sub-culture of the 1960's and very early 1970's. SPEED FREAKS. Many say that the introduction of amphetamine ended the true hippie culture of the 1960s San Francisco scene

Amphetamine use in the 1960s cont The typical Speed freak would display a pattern of: Massive doses, and re-dosing: RUNS- lasting 2-5 days. All in pursuit of the full body flush (orgasm) However, these runs were inevitably followed by the CRASH CRASH: Sleep for 24 hours or more ..and other more serious problems

Speed Kills... was a slogan that emerged about this time.. Though O.D.s are fairly rareamphetamine toxicity syndrome ( amphetamine Psychosis.. often lead to acts of violence). By Mid 60s popular use was significantly declining. Amphetamine use diminished in the 1970s and 1980sbut

now back up primarily methamphetamine use.. smoked, snorted, injected or taken orally ice, crank, crystal, speed, meth, chalk

Message from the Director on "Bath Salts" Emerging and Dangerous Products "Bath Salts", the newest fad to hit the shelves (virtual and real), is the latest addition to a growing list of items that young people can obtain to get high. The synthetic powder is sold legally online and in drug paraphernalia stores under a variety of names, such as "Ivory Wave," "Purple Wave," "Red Dove," "Blue Silk," "Zoom," "Bloom," "Cloud Nine," "Ocean Snow," "Lunar Wave," "Vanilla Sky," "White Lightning," "Scarface," and "Hurricane Charlie." Because these products are relatively new to the drug abuse scene, our knowledge about their precise chemical composition and short- and long-term effects is limited, yet the information we do have is worrisome and warrants a proactive stance to understand and minimize any potential dangers to the health of the public. We know, for example, that these products often contain various amphetamine-like chemicals, such as methylenedioxypyrovalerone (MPDV), mephedrone and pyrovalerone. These drugs are typically administered orally, by inhalation, or by injection, with the worst outcomes apparently associated with snorting or intravenous administration. Mephedrone is of particular concern because, according to the United Kingdom experience, it presents a high risk for overdose. These chemicals act in the brain like stimulant drugs (indeed they are sometimes touted as cocaine substitutes); thus they present a high abuse and addiction liability. Consistent with this notion, these products have been reported to trigger intense

cravings not unlike those experienced by methamphetamine users, and clinical reports from other countries appear to corroborate their addictiveness. They can also confer a high risk for other medical adverse effects. Some of these may be linked to the fact that, beyond their known psychoactive ingredients, the contents of "bath salts" are largely unknown, which makes the practice of abusing them, by any route, that much more dangerous. Unfortunately, "bath salts" have already been linked to an alarming number of ER visits across the country. Doctors and clinicians at U.S. poison centers have indicated that ingesting or snorting "bath salts" containing synthetic stimulants can cause chest pains, increased blood pressure, increased heart rate, agitation, hallucinations, extreme paranoia, and delusions. It is noteworthy that, even though we are barely two months into 2011, there have been 251 calls related to "bath salts" to poison control centers so far this year. This number already exceeds the 236 calls received by poison control centers for all of 2010. In response to this emerging threat, several states, including Hawaii, Michigan, Louisiana, Kentucky, and North Dakota, have introduced legislation to ban these products, which are incidentally labeled as "not fit for human consumption." In addition, several counties, cities, and local municipalities have also taken action to ban these products. We will continue to monitor the situation and promote research on the extent, pharmacology, and consequences of "bath salts" abuse. In the meantime, I would like to urge parents, teachers, and the public at large to be aware of the potential dangers associated with the use of these drugs and to exercise a judicious level of vigilance that will help us deal with this problem most

effectively. Sincerely, Nora D. Volkow, M.D. Director National Institute on Drug Abuse Controversies in the 1970s(While Amphetamine use declined Cocaine use Resurfaced )The Cocaine Comeback: 14 Percent Using High School Seniors reporting cocaine use 12 10 8 6

WHY?? 4 2 0 75 80 85 90 95

00 05 Percentage of High School Seniors Reporting Use of Cocaine During the Past Year Factors contributing to the cocaine comeback in the 19070s and 80s Some otherwise respected scientists made quite

controversial claims. Cocaine is not an addictive or especially dangerous drug. It should be legalized (Ashley, 1976) Maybe Ashleys Ideas are somewhat accurate when assessing cocaine use by intranasal administration However, it is now quite clear that the abuse potential for cocaine depends much on the form of cocaine that is used, and the route of administration

Cultural association of cocaine, money and glamour-Famous Cocaine users of the 1970s and 80s Tim Allen Robin Williams Cocaine in the Nineties: The Crack Phenomenon Crack is the smokable form of cocaine. Cocaine hydrochloride is treated by mixing with baking soda and waterthe water is boiled

off..the process leads to audible cracking sounds,the result is Crack cocaine. Cocaine in the Nineties: The Crack Phenomenon CRACK COCAINE Less expensive More intense effects (Shorter duration of action) More risk of overdose Much higher rate of addiction Mechanisms of action- Cocaine

Cocaine blocks the reuptake of monoamine neurotransmitters; DA, NE and 5-HT in the brain. Therefore, these neurotransmitters stay in the synaptic cleft for a longer time and repeatedly activate postsynaptic receptors. Mechanisms of action- Cocaine

cocaine can also cause the release of dopamine from neurons in the brain. The effects of this indirect monoamine agonist on the PNS account for its sympathomimetic actions. Amphetamines-Mechanism of Action amphetamine effects are very similar to those of cocaine, but longer in duration Blocks reuptake of monoamines: dopamine, serotonin and norepinephrine

COCAINE VS AMPHETAMINES? Cocaine & amphetamine indistinguishable to IV users Oral or nasal route - local anesthetic properties would set them apart Cocaine and Amphetamine block reuptake of dopamine Cocaine-Pharmacokinetics

Inhalation (smoking) & IV injection Onset: < 2 min For both routes Duration of action 5-10 min. Cocaine -Pharmacokinetics

Oral -Essentially ineffective for cocaine ( see first pass effects). effective for amphetamine analogs onset: 30 minutes / peak 2-3 hrs Intranasal

onset 3-4 minutes peak effects: 15-30 minutes ~ Amphetamines Amphetamine (6-8 hrs) Dextroamphetamine (8-10 hrs)

Methamphetamine (12+ hrs) In case youre interested/Cocaine: Local Anesthetic Half-life: 1 hr Inject SC

Numbing < 2 min Peak effects: 15-20 minutes Pharmacodynamics Blocks Na+ channels Constricts blood vessels ~ Cocaine

Pharmacokinetics: Metabolism Broken down by liver enzymes Half-life: 1 hr Amphetamines In liver, Half-life: 7-30 hrs ~

TOLERANCE Tachyphylaxis- especially for the positive effects of these drugs brief & transient tolerance reuse within minutes - hours SENSITIZATION / Reverse Tolerance- (induced with lower doses) Psychomotor stimulant induced stereotypy repetitive behaviors.

In rats, stereotypic behaviors may include head sways, hyperactivity, avoidance behaviors, and automutilation (self-mutilation). Punding a repetitive and essentially useless complex behavior. The human equivalent of drug-related stereotypy. Psychomotor stimulant sensitization Stereotypy/ Punding

Probably associated with effects on basal gangliainitially a kind of hyperactivity With repeated high dose use may become Parkinson like (pill rolling finger movements, ataxia or unsteady gait). ADVERSE Effects of the Psychomotor Stimulants Adverse effects of occasional

intranasal use of cocaine is debatable. However, repeated use, especially if high doses are used has clear adverse consequences- Stimulant Psychosis Psychotomimetic Effects Schizophrenia-like psychosis

Paranoia Delusions Hallucinations: parasitosis/Formication syndrome Methamphetamine earlier developing may persist for days, weeks ~ Additional Symptoms of Psychomotor Stimulant

TOXICITY Aggression/violence Degeneration of nasal mucosa (cocaine)

Rotting teeth Dry, itchy skin Numbness Insomnia Extreme body temperature Depression stroke Video on Meth toxicity Friendly Fire you may have thought that the military had learned for WWII, but(aggression)

Go pills in the US military April 2002 bombing of a Canadian unit in Afghanistan killed 4 and wounded 8 Both US pilots were under the influence of go pills June 2003 court martial for dereliction of duty (dropped manslaughter charge)

Lethality Cocaine Amphetamine/Methamphetamine

Oral: 500 mg Nasal: 150-300 mg toxic effects: 15 mg in novices lethal 500-1700 mg Inhalation (smoked): much lower ~ Cocaine Overdose John Belushi Cocaine Overdose Stimulant Overdose

Convulsions; seizures Cardiac failure DAWN COCAINE O.D. Emergency Room Visits due to Cocaine and Heroin Image courtesy of the Office of National Drug Control Policy Cocaine/Methamphetamine Dependence & Abstinence

Crash Depression Withdrawal Extinction/cravings Residual effects: Meth and dopamine damagecognitive impairment (Chang, 2003) Cocaine Abuse: Animals

Self-administration Will work hard to get progressive FR6400 Continuous access: Weight loss

Self-mutilation parasitosis? Death within 2 weeks ~ Cocaine Abstinence Syndrome Phase 1: Crash 9 hrs - 4 days Binge

Relapse Phase 2: Withdrawal 1 - 10 weeks Early Agitation Depression Anorexia High Craving Early Normal sleep Normal mood Low anxiety

Low craving Middle Depression Fatigue Insomnia No craving Middle & Late Anhedonia Anergia Anxiety High Craving & conditioned cues

Late Exhaustion Hypersomnolence Hyperphagia No Craving Phase 3: Extinction indefinite Normal hedonic response Normal mood Episodic craving Conditioned cues trigger craving

Abstinence Gawin & Kleber (1986) Increase in Meth-lab seizures 2000-2004 Washington0 California(-66%) Illinois730% North Carolina2171% (318

busts) House Bill 248: Meth Lab Prevention Act Signed by Gov. Easley Sept. 28th 2005; Into effect Jan. 2006 All products containing ephedrine and pseudoephedrine sold behind the counter

Purchasers over 18 and must show ID and sign log Attention Deficit Disorder Hyperactivity and the paradox Amphetamine (Adderall) Methylphenidate (Ritalin,Concerta) 10 million + prescriptions per year 700% increase between 92 & 04

The ADHD Controversy Is it a disease? Do stimulants work? ADHD in adults Side effects: growth suppression Abuse

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