1. Stimulants Chapter 10

2. Major Stimulants Schedule I (“designer” amphetamines)
All major stimulants increase alertness, excitation, and euphoria; thus, these drugs are referred to as “uppers.”
Schedule I (“designer” amphetamines)
Schedule II (amphetamine, cocaine, methylphenicate – Ritalin : See next Slide..

3. Methylphenidate (Ritalin)
“Why is this medication prescribed?
Methylphenidate is used as part of a treatment program to control symptoms of attention deficit hyperactivity disorder (ADHD; more difficulty focusing, controlling actions, and remaining still or quiet than other people who are the same age) in adults and children. Methylphenidate (Ritalin, Ritalin SR, Methylin, Methylin ER) is also used to treat narcolepsy (a sleep disorder that causes excessive daytime sleepiness and sudden attacks of sleep). Methylphenidate is in a class of medications called central nervous system (CNS) stimulants. It works by changing the amounts of certain natural substances in the brain.”
Source -

4. Amphetamines
Cause dependence due to their euphoric properties and ability to mask fatigue.
Can be legally prescribed by physicians for appetite control in weight loss programs, narcolepsy, and hyperactivity disorders.
Abuse occurs in people who acquire their drugs by both legitimate and illicit ways.

5. History of Amphetamines
First synthesized in 1887 by German Pharmacologist L. Edeleano, and at that time the stimulant effects were unnoticed.
In 1927, Gordon Alles gave a firsthand account of its effects.
Reduced fatigue
Increased alertness
Caused a sense of confident euphoria
In 1932, Benzedrine inhalers (bennies) became available as a nonprescription medication (nasal congestion).

6. History of Amphetamines (continued)
The Benzedrine inhalers became widely abused for their stimulant action.
1971, all potent amphetamine-like compounds in nasal inhalers were withdrawn from the market.
Widely used in World War II to counteract fatigue.
Other users: Korean War soldiers, truck drivers, homemakers, high achievers under pressure (as performance-enhancers).

7. History of Amphetamines (continued)
In the early period of amphetamine use, medical professionals recommended amphetamine as a cure for a range of ailments— alcohol hangover, narcolepsy, depression, weight reduction, hyperactivity in children, and vomiting associated with pregnancy. The use of amphetamine grew rapidly because it was inexpensive, readily available, had long lasting effects, and because professionals purported that amphetamine did not pose an addiction risk
In 1971, all potent amphetamine-like compounds in nasal inhalers were withdrawn from the market.
At the height of the epidemic (1967) some 31 million persons in the U.S. were written prescriptions for anorexiants (diet pills) alone.

8. Amphetamine Terminology
Street amphetamine: bennies, black beauties, copilots, eye-openers, lid poppers, pep pills, speed, uppers, wake-ups, and white crosses.
Street dextroamphetamine: dexies
Street methamphetamine: chalk, chris, crank, cristy, crystal, crystal meth, go, go- fast, meth, speed, and zip
Concentrated methamphetamine hydrochloride: ice, crystal, and glass (article on crystal meth)

9. Amphetamine Terminology (continued)
Combinations:
Amphetamines and barbiturates: goofballs
Methamphetamine and heroin: speedballs
Use and users:
Speed run: increasing doses of injectable methamphetamine taken over several days or weeks
Speeders or speed freaks: serial speed users; methamphetamine users who inject their drugs intravenously
Source -

10. How Amphetamines (see Mechanisms in hyperlink) Work
Synthetic chemical similar to the natural neurotransmitters such as norepinephrine, dopamine, and epinephrine
Increase the release and block the metabolism of these catecholamine substances, and serotonin, in the brain and peripheral nerves associated with the sympathetic nervous system.
Thus, amphetamines control both arousal and mood.
Because amphetamines cause the release of catecholamines they are classified as a sympathomimetic drugs.

11. How Amphetamines Work (continued)
Amphetamines can cause
“Fight-or-flight” effect, a response to crisis
Alertness
Continual “high” can promote Anxiety, severe apprehension, or panic
Potent effects on dopamine (pleasure) in the reward center of the brain “Whole-body Orgasms”
Behavioral stereotypy: see next slide..

12. Behavioral stereotypy
Meaningless repetition of a single activity produced by the user that has been reported with heavy amphetamine users.
An amphetamine user will get “hung up”, caught in a repetitious activity for hours.
They may take items apart (clocks, radios) and carefully categorize the parts, sit in a tub all day, persistently sing a not, repeat phrases of music, or repeatedly clean the same object for long periods of time. (see also “Punding” here)

13. Approved Uses of Amphetamines
Narcolepsy
Attention Deficit Hyperactivity Disorder (ADHD)
Weight reduction (controls appetite center in hypothalamus)

14. Short Term /Adverse Effects of Amphetamines
Abuse and Addiction
High body temperature,
Cardiovascular system failure,
Hostility or paranoia,
Irregular or increased heart rate/heart beat,
Increased diastolic/systolic blood pressure,
Increased activity/talkativeness,
Euphoria,
Heightened sense of well-being,
Decreased fatigue/drowsiness

15. Short Term /Adverse Effects of Amphetamines (continued)
Decreased appetite,
Dry mouth,
Dilated pupils,
Increased respiration,
Heightened alertness/energy,
Nausea,
Headache,
Palpitations,
Unrealistic feelings of cleverness, great competence, and power

16. Current Misuse of Amphetamines
Decline in abuse in the late 1980s and early 1990s.
In 1993 the declines were replaced by an increasein the number of persons abusing amphetamines.
Currently, 3–6% annual use of methamphetamine by adolescents in the United States.
Due to the ease of production, methamphetamine can be made in makeshift labs using cookbook-style recipes.
Toxic chemicals in such labs pose a threat to residents, neighbors, law enforcement officials, and the environment.

17. Current Misuse (continued)
Illegal labs that synthesize methamphetamine use decongestant ingredients from common OTC cold medicines. (ephedrine, pseudoephedrine = Precursor chemicals)
Role of the Comprehensive Methamphetamine Control Act 2008 in reducing illegal manufacturing of methamphetamine.
Illicit neighborhood labs have been replaced by small local “shake and bake” and large Mexican drug cartel operations for methamphetamine supplies.

18. Current Misuse (continued)

19. Patterns of High-Dose Use
Amphetamines can be taken: (The initial effect is the “rush” and the period that follows 4-16 hours is the “high”)
Orally
Intravenously (speed freak)
Smoked (ice) - Methamphetamine hydrochloride is processed to produce a potent, a smoked form of methamphetamine known as “glass” or “ice”. This substance is called “ice” because it resembles rock candy or a chip of ice.

20. Meth Ice
How is ice used?
Ice is used by placing the substance in a glass pipe, heating it, and inhaling the resulting vapors. The vapors enter the bloodstream directly through the lungs and are rapidly transported to the brain. When ice is heated, its solid crystals turn to liquid. When it cools, ice reverts to its solid state and is therefore reusable. Since ice is odorless, it can easily be used in public without being detected. In addition to its use for recreational purposes, ice is often used in the workplace to increase alertness. Some users smoke ice for days at a time and then “crash” in a deep sleep lasting 24 hours or more.
Source:

21. Summary of the Effects of Amphetamines (p 315)

22. High Dose Users
The amphetamine addict tries to maintain the “high” as long as possible leading to extended mental and physical hyperactivity.
This “run” can persist for 3-15 days (tweaking)
The “Tweaker” can be hyperpyrexic , irritable and paranoid because they have not slept for days, and thus may act out violently.
To control the side effects, Tweakers often use depressants – typically barbituates or alcohol

23. High Dose Users Continued abuse (high doses) often leads to:
Considerable weight loss
Skin lesions
Oral damage (meth mouth – see p. 316)
Liver disease
Hypertensive disorders
Stroke / MI
Kidney damage
Seizures

24. Small Towns, Big Problems: The Female Methamphetamine Epidemic

25. High Dose Users Withdrawal (high dose users) often leads to:
Depression (suicidal behavior)
Lethargy
Muscle pains
Abnormal Sleep Patterns
There is evidence that long term abuse among adolescents or adults may damage both long term dopamine and serotonin neurotransmitter systems of the brain. This may result in persistent episodes of psychosis, long term memory, motor impairment, and cognitive deficits.

26. Amphetamines
Amphetamine combinations
Speedballs - a term commonly referring to the intravenous use of heroin or morphine and cocaine together in the same syringe.
Designer drugs
Methylenedioxymethamphetamine (MDMA, Ecstasy; most popular of the designer amphetamines) – see later slide..
Methylenedioxyamphetamine (MDA)
A special amphetamine
Methylphenidate (Ritalin)

27. Amphetamines

28. Treatment of Amphetamine Abuse
Methamphetamine addiction is the principal problem with these drugs.
Addiction causes long-term brain damage and is difficult, but not impossible, to treat.
Requires long-term treatment to deal with compromised decision-making, memory deficits, increased impulsivity and lack of emotion control.
No FDA-approved medications/treatment is principally behavioral management.
Treatment typically requires more than one year of intense intervention consisting of drug abstinence, cognitive, emotional, and motivational rehabilitation.

29. MDMA (Ecstasy)
A designer amphetamine that continues to be popular with young people.
It enhances sensory input and is referred to as an entactogen (a combination of psychedelic and stimulant effects) and it releases both serotonin and dopamine.
While dependence can occur, it tends to be unusual.
Withdrawal includes depression and sleep disruption that can last for days.

30. Performance Enhancers
These are stimulants used to embellish physical/mental endurance and enhance performance.
Often used by college, and even high school, students to help academically.
The drugs used can be illegal amphetamines or related prescription stimulants that are used to treat ADHD, like Ritalin.
As with other potent stimulants, use of these drugs can be very dangerous and cause dependence.

31. Cocaine
Cocaine abuse continues to be a major drug concern in the United States.
From 1978 to 1987, the United States experienced the largest cocaine epidemic in history.
As recently as the early 1980s cocaine was not believed to cause dependency.
Cocaine is known to be highly addictive.
In 2010, approximately 2.4% of high school seniors used cocaine.
© Corbis

32. History of Cocaine The first cocaine era (2500 BC)
South American Indians (see p 302)
Erythroxylon coca shrub
The second cocaine era (began 19th century)
Vin Mariani (Angelo Mariani’s Wine) – p.324
Coca-Cola ( see history)
Sigmund Freud - “magical drug”
The third cocaine era (began 1980s)
Celebrities
Decreased in price to $10 a “fix” with large suppliers

33. Current Trends in Cocaine and Crack Use by High School Seniors
Source: Johnston, L D., P. M. O’Malley, J. G. Bachman, and J. E. Schulenberg. Monitoring the Future. “Long-Term Trends in Annual Prevalence of Use of Various Drugs in Grade 12 (Table 16).” Ann Arbor, MI: University of Michigan, Available at: Accessed March 4, 2011.

34. Cocaine Administration
Form of administration important in determining intensity of cocaine’s effects, its abuse liability, and likelihood of toxicity.
Orally: Chewing of the coca leaf
Inhaled: Into the nasal passages (“snorting”)
Injected: Intravenously
Smoked: Freebasing, crack
© Medioimages/age fotostock

35. Pharmacological Effects of Cocaine
Enhanced activity of the catecholamine and serotonin transmitters
Blocks the reuptake of these substances following their release from neurons
The summation of cocaine’s effects on dopamine, noradrenaline, adrenaline, and serotonin is to cause CNS stimulation
Cardiovascular system
Increased sympathetic drive – increased hear rate and vasoconstriction
Local anesthetic effect

36. Main Stages of Cocaine Withdrawal (see Table 10-3 p. 333)
Crash: Initial abstinence phase consisting of depression, agitation, suicidal thoughts, and fatigue
Withdrawal: Including mood swings, craving, anhedonia, and obsession with drug seeking
Extinction: Normal pleasure returns, mood swings, cues trigger craving

37. Treatment of Cocaine Dependence
Is highly individualistic and has variable success. Most cocaine users use other drugs as well, such as alcohol.
Principal treatment strategies include inpatient and outpatient programs.
Drug therapy is often used to relieve cocaine craving and mood problems. (levodopa, bromocriptine) both assist in dopamine transmission
Psychological counseling, support, and a highly motivated patient are essential.

38. Cocaine and Pregnancy Microencephaly Reduced birth weight
Cocaine babies; not clear the effect of cocaine on the fetus. Some possibilities are:
Microencephaly
Reduced birth weight
Increased irritability
Subtle learning and cognitive defects

39. Minor Stimulants It is classified as a xanthine (methylxanthine)
Caffeine is the most frequently consumed stimulant in the world.
It is classified as a xanthine (methylxanthine)
It is found in a number of beverages
Also found in some OTC medicines and chocolate
In the U.S., the average daily intake of caffeine is equivalent to 2-3 cups of coffee a day.
© AbleStock

40. Caffeine Content of Beverages and Chocolate

41. Physiological Effects of Xanthines
CNS effects
Enhances alertness, causes arousal, diminishes fatigue
Adverse CNS effects
Insomnia, increase in tension, anxiety, and initiation of muscle twitches
Over 500 milligrams: panic sensations, chills, nausea, clumsiness
Extremely high doses (5 to 10 grams): seizures, respiratory failure, and death

42. Physiological Effects of Xanthines (continued)
Cardiovascular effects
Low doses: Heart activity increases, decreases, or does nothing
High doses: Rate of contraction of the heart increases, minor vasodilation in most of the body, cerebral blood vessels are vasoconstricted
Respiratory system effect
Can cause air passages to open and facilitate breathing

43. Physiological Effects of Xanthines (continued)
Caffeine intoxication
Caffeinism (about 10% of consumers)
Restlessness, nervousness, excitement, insomnia, flushed face, diuresis, muscle twitching, rambling thoughts and speech, stomach complaints
Caffeine dependence
© Christa DeRidder/ShutterStock, Inc

44. Physiological Effects of Xanthines (continued)
© Christa DeRidder/ShutterStock, Inc

45. Other Stimulants (Table 10.6, p.341)
OTC sympathomimetics included in cold, allergic and diet aid medications
OTC Sympathmimetics can pose emergencies and be deadly (See Here and Now, p. 341and 342)
Herbal stimulants: often contain ephedrine, ephedra, ma huang, or guarana

46. Other Stimulants - Diet Pills Are Russian Roulette for Athletes
End of Presentation