4. Terms
Hallucinogens
Induce perceived distortions in time and space
Phantasticants
Create a fantasy world
Psychedelic (“mind-manifesting”)
Controversially implies a beneficial, visionary type of
effect
6. Classical Phantasticants
Alter perceptions while allowing the user to
remain in communication with the present
world
Indole hallucinogens
Serotonin
LSD, psilocybin
Catechol hallucinogens
Norepinephrine & dopamine
Mescaline, MDMA, belladonna, amanita muscaria
7. Deliriants
Produce more mental confusion, greater
clouding of consciousness, and a loss of touch
with reality
Anticholinergic hallucinogens
Acetylcholine
PCP, ketamine
8. Psychomimetic means
A. Causes
hallucinations
B. Causes psychotic-
like symptoms
C. Causes increased
sense of spirituality
Causeshallucinations
Causespsychotic-like
sy...
Causesincreased
sense
of...
31%
0%
69%
9. Deliriant means
A. Causes confusion
B. Causes increased
creativity
C. Causes psychosis
Causesconfusion
Causesincreased
creativity
Causespsychosis
85%
15%
0%
10. Hallucinogens
About 6,000 different types of plants are
capable of altering consciousness
About 150 plants are used for hallucinogenic
purposes
Methylenedioxymethamphetamine (MDMA)
and lysergic acid diethylamide (LSD) are
synthetic hallucinogens
11. LSD Discovery
Synthesized from alkaloids
extracted from the ergot fungus
Ergotism
St. Anthony’s Fire
Swiss chemist Albert Hofmann
developed LSD as a possible
headache remedy in 1938
12. Albert Hofmann, who was responsible for
developing LSD, died from an LSD
overdose soon after developing the
drug.
A. True.
B. False. He died at 57,
jumping off a roof
during a flashback.
C. False. He lived to be
102 and died of
natural causes. True.
False.He
died
at57,jum
...
False.He
lived
to
be
102...
15%
46%
38%
13. One of the reasons LSD
attracted attention is
because
A. The trips are so
pleasant
B. The drug is so
cheap
C. The drug is so
potent
Thetripsareso
pleasant
Thedrugisso
cheap
Thedrugisso
potent
31%
46%
23%
14. Early Use of LSD
Theories of Benefit
Psychotherapy
Enhanced understanding
Military Experiments
15. At one time, hallucinogenic
drugs were associated with
witchcraft and sorcery.
A. True
B. False
True
False
8%
92%
16. Most of the research on LSD
contributed very little to
our understanding of the
drug.
A. True
B. False
True
False
23%
77%
18. At twice its normal dosage,
LSD can be fatal.
A. True
B. False
True
False
67%
33%
19. Pharmacology
Mouse Party
Different hallucinogens are classified by which
neurotransmitter they impact
Tolerance develops rapidly
Metabolized by liver, half-life is
approximately 3 hours
No physical dependence or withdrawal
symptoms
20. LSD
A. Is the most potent
psychoactive chemical
known to man
B. Causes a distressing
withdrawal syndrome
C. Does not create
tolerance
Isthe
m
ostpotentpsych...
Causesa
distressingw
it...
Doesnotcreate
tolerance
82%
18%
0%
22. The phenomenon of hearing
colors or seeing sounds is
called:
A. Flashback
B. Trip
C. Synesthesia
D. Overdose
Flashback
Trip
Synesthesia
Overdose
0% 0%
70%
30%
23. Use of LSD makes one more
creative.
A. True
B. False
True
False
22%
78%
25. LSD has been shown to be as
addictive as heroin.
A. True
B. False
True
False
67%
33%
26. Expert Group Activity
Study the hallucinogen
What is it?
How is it used?
How is it regulated?
What are the effects?
Are there negative effects or warnings?
36. In-class Discussion
Should hallucinogens be used in therapy?
Do they enhance spirituality?
Do they enhance creativity?
Do they facilitate self-expression?
What safeguards should be implemented?
38. Have you ever used supplements?
A. Sure, vitamins
B. Herbal supplements
C. Amino acids to bulk
up
D. No way!
Sure,vitam
ins
Herbalsupplem
ents
Am
ino
acidsto
bulk
up
No
w
ay!
0% 0%0%0%
39. Supplements vs OTC
Food, Drug & Cosmetic Act
Food = safe, pure, NOT required to
show they are effective or have benefit
Drug = intended for use in diagnosis,
cure, mitigation, treatment or
prevention of disease
40. DSHE Act
Dietary Supplement Health and Education
Act 1994
Defined supplements and set regulation for safety
and labeling
Same as food labeling
Includes: vitamins, minerals, herbs (and
concentrates), amino acids
41. OTC Drug Categories
Category I:
generally recognized as safe (GRAS)
generally recognized as effective
(GRAE)
generally recognized as honestly
labeled (GRAHL)
Category II: Not generally
recognized as safe or effective or
is improperly labeled
Category III: Cannot be sold
42. What influences your choice to use an OTC
product?
A. My mom.
B. Advertisements.
C. Friends.
D. Used it in the past.
E. Nothing.
M
ym
om
.Advertisem
ents.
Friends.
Used
itin
the
past.
Nothing.
0% 0% 0%0%0%
43. OTC Regulation
1962 Kefauver-Harris
amendment required all drugs
be evaluated for safety and
efficacy
44. FDA
FDA can only declare a product adulterated if
it presents a significant or unreasonable risk
of illness or injury
Health claims
Structure/function claims
Carries disclaimer
46. Questions?
What are the pros and cons of
current supplement regulations?
What are some supplements
you’ve heard of?
FILM
http://digital.films.com/PortalVi
ewVideo.aspx?xtid=32926#
49. How does your perception of OTC drugs
differ from your perception of
prescription drugs?
A. It doesn’t; they are
the same.
B. OTC drugs are safer
than prescription
drugs.
C. Supplements are
safer than
prescription drugs.
Itdoesn’t;theyare
the
...
OTC
drugsaresaferthan...
Supplem
entsare
safert...
0% 0%0%
50. Do you read the label on OTC meds?
A. Yes, thoroughly
B. Well, I skim it
C. Nope, never looked
Yes,thoroughly
W
ell,Iskim
it
Nope,neverlooked
0% 0%0%
52. About how many high school students have
taken cough medicine in the previous year to
get high?
A. 1 in 20
B. 1 in 50
C. 1 in 100
1
in
20
1
in
50
1
in
100
0% 0%0%
53. Because Dextromethorphan can have harmful
effects, individuals can only buy one bottle
at a time
A. True
B. False
True
False
0%0%
54. OTC vs Prescription Drugs
1938 Food, Drug & Cosmetic
Act established class of
prescription drugs
DIFFERENCES:
Dosage
Active ingredient
FDA reviews products, may
switch to OTC
55. Types of OTC Drugs
Stimulants
Only caffeine
Weight-control products
Only Orlistat/Alli
Sedatives/sleep aids
No approved sedatives, sleep
aids contain antihistamine
58. Aspirin and ibuprophen are twice as
effective for protecting people against
heart attacks when taken together
A. True
B. False
True
False
0%0%
59. Not only does aspirin reduce the risk
of heart attacks, it reduces the risk
of many types of _________
A. Seizures
B. Cancer
C. Infections
D. Mental illnesses
Seizures
Cancer
Infections
M
entalillnesses
0% 0%0%0%
62. Anabolic steroids are a man-made
A. Mood stabilizer
B. Testosterone
C. Enzyme
D. Protein
M
ood
stabilizer
Testosterone
Enzym
e
Protein
0% 0%0%0%
Response
63. Which of the following is not a
function of testoterone?
A. Deepening voice
B. Growth of facial and
chest hair
C. Decrease depression
D. Increase muscle
mass
Deepeningvoice
Growth
offacialand
ches...
Decrease
depression
Increasem
usclem
ass
0% 0%0%0%
Response
64. Steroids increase muscle mass by
A. Changing
metabolism
B. Increasing protein
synthesis
C. Affecting
neurotransmitters
D. Increasing growth
hormone Changingm
etabolism
Increasingprotein
synthesis
Affectingneurotransm
itters
Increasinggrow
th
horm
one
0% 0%0%0%
Response
65. Steroids are used to treat
A. Depression
B. Growth deficiencies
C. AIDS
D. Cancer
DepressionGrowth
deficiencies
AIDS
Cancer
0% 0%0%0%
Response
66. A new trend in steroid use is
A. Using steroids to get
bigger and stronger
B. Using steroids to
ward off depression
C. Using steroids to
improve looks
D. Using steroids to
combat side effects
from chemotherapy
Using
steroidsto
getbigg..
Using
steroidsto
w
ard
of...
Using
steroidsto
im
prove...
Using
steroidsto
com
bat...
0% 0%0%0%
Response
67. Which of the following is not a
side effect of steroid use?
A. Respiratory distress
B. High blood pressure
C. High cholesterol
D. Liver damage
Respiratory
distressHigh
blood
pressure
High
cholesterol
Liverdam
age
0% 0%0%0%
Response
68. Body distortion is
A. Abnormal growth of
muscles
B. Having an unrealistic
perception of your body
C. A symptom of eating
disorders
D. Caused by a hormone
imbalance
Abnorm
algrow
th
ofm
us...
Havingan
unrealisticper...
A
sym
ptom
ofeatingdis...
Caused
bya
horm
one
im
...
0% 0%0%0%
Response
70. Do you think use of stimulant
medications for academic purposes is
cheating?
A. Yes
B. No
Yes
No
0%0%
Response
71. Small Group Questions
In your group, talk about use of performance-
enhancing drugs:
1. Under what circumstances is it acceptable? Why?
2. Under what circumstances is it unacceptable? Why?
3. When should testing for PEDs be implemented?
Under what situations or conditions? Why? For
what groups?
High school, college, professional athletes?
Cheerleading?
Academic competitors?
Editor's Notes
Naming the family of drugs is a complex issue
Phantastica: Drugs that create a world of fantasy in our minds
Psychedelic: “Mind-viewing,” a term that controversially implies a beneficial, visionary type of effect
Psychotomimetic: “Mimicking psychosis”—by producing hallucinations and some altered sense of reality, these drugs produce a state that could be described as psychotic
Naming the family of drugs (continued)
Entheogen and entactogen
Entheogens: Substances that create spiritual or religious experiences
Entactogens: Substances that enhance feelings of empathy
Hallucinogens: A more descriptive and less prejudiced term
A drug that produces profound alterations in perception, including unusual visual sensations and often changes in the perception of one’s own body
Two major groups
Classical phantastica
Alter perceptions while allowing the user to remain in communication with the present world
Deliriants
Produce more mental confusion, greater clouding of consciousness, and a loss of touch with reality
Indole hallucinogens = drugs that have the indole structure also found in the neurotransmitter serotonin
Examples: LSD, psilocybin
Catechol hallucinogens = drugs that have the catechol nucleus that forms the basic structure of the neurotransmitters norepinephrine and dopamine
Examples: mescaline, MDMA (Ecstasy)
Compared to “phantastica,” deliriants have more of a tendency to produce mental confusion and a loss of touch with reality
Examples: PCP, anticholinergic hallucinogens like belladonna, mandrake, henbane, datura, amanita muscaria, salvia
Naturally occurring agents in this group come from the potato family
Effects come from three pharmacologically active alkaloids that are central and peripheral cholinergic blocking agents
Atropine (dl-hyoscyamine)
Scopolamine (l-hyoscine)
l-hyoscyamine
Many used as poisons in addition to being used for their hallucinogenic effects
Block production of mucus in the nose and throat and prevent salivation
Mouth becomes dry and perspiration stops
Temperature can increase to fever levels
Heart rate increases
Eyes dilate, resulting in an inability to focus on nearby objects
At high doses, behavior pattern resembles toxic psychosis (delirium, mental confusion, loss of attention, drowsiness, loss of memory for recent events)
The original deliriants
Humans have long used agents that cause visual, auditory, tactile, taste, and other hallucinations or that induce artificial psychoses
Mind-altering drugs were central in many Eastern religions, where they were used to achieve religious revelations
LSD reached the US in 1949, when it was used to study mental illness
It was later used by musicians and artists to enhance their creativity, and by government officials to determine its effectiveness as a mind-control agent
LSD is not found in nature; it is synthesized from alkaloids extracted from the ergot fungus Claviceps purpurea
Eating grain infected with this mold causes an illness called ergotism
During a famine, grain infected with the ergot fungus might be consumed instead of destroyed, leading to outbreaks of ergotism
1938: Synthesized by Dr. Albert Hofmann of Sandoz Laboratories in Switzerland
1943: Dr. Hofmann took a large dose and described its effects
Potency of the drug attracted attention—a very small dose produces effects
Comparable effects from mescaline would require 4,000 times the dose
Ergotism
A condition resulting from ingesting a fungus that grows on grains; marked by muscle tremors, burning, mania, delirium, hallucinations, and eventual gangrene
St. Anthony’s fire
Burning sensations caused by ergot poisoning
People during the Middle Ages would visit the shrine of St. Anthony in an attempt to cure it
Between the early 1950s and 1970s, there was a tremendous amount of research performed with LSD
In psychotherapy, to help patients bring up repressed memories and motives
Dr Hofmann believed that LSD was a valuable psychedelic tool and could be used to enhance humans’ understanding of their place in nature.
Most research on LSD was found to contribute little to our understanding of the effects of the drug
Most research since 1975 has been conducted on animals in an effort to understand the drug’s action at the neural level
Various militaries, including the US military, experimented extensively with LSD and other hallucinogens
Between the 1950s and 1960s, hundreds of soldiers and civilians were unwittingly given doses of the drug
Subjects believed they were losing their minds.
Some suffered psychiatric disorders and others had difficulties adjusting to their usual lives.
Army/CIA-sponsored research was poorly done and violated many ethical codes
Once knowledge of the activities became public, the US government was required to pay reparations exceeding hundreds of thousands of dollars to some subjects and their families.
One of the first uses of LSD was to study mental illness, especially schizophrenia
Psychiatrists gave patients LSD to help them develop personal insight and to recall repressed experiences
LSD was given to terminally ill cancer patients to help them cope with impending death
Presently, LSD and other hallucinogens have no accepted medical uses
Objectively, LSD does not seem to improve creativity, although artists who take it seem to enjoy its effects
Some artists believe that the perceptual changes from LSD have a profound, positive effect
In another study, artists believed that their drawing skills vastly diminished under the influence of LSD
Research with LSD was conducted at the Edgewood Arsenal in Maryland in the early 1950s
In 1953, the CIA gave LSD to government scientist Frank Olson without his knowledge – he experienced a psychotic response and jumped to his death from a 10th-story window
Prostitutes in San Francisco were given LSD unknowingly to evaluate the drug’s effect on their sexual activities and experiences and on their patrons
Experiments by psychologist Timothy Leary on Harvard graduate students
His research came under increasing criticism due to charges that he was being less that rigorous and was using ethically questionable methods.
1966: Leary started a religion, the League of Spiritual Discovery, with LSD as the sacrament
Motto was “turn on, tune in, and drop out”
Use peaked in 1967 and 1968 and then fell due to reports of problems associated with its use including “bad trips,” prolonged psychotic reactions, worries about possible chromosome damage, self-injurious behavior and “flashbacks”
In the early 1960s, people took LSD as a means of dealing with society and its inherent problems
At Harvard University Timothy Leary and Richard Alpert studied the psychological effects of psilocybin, a hallucinogenic mushroom, on humans
Leary and Alpert believed that LSD and other hallucinogens were psychologically and spiritually beneficial
LSD is odorless, colorless, tasteless, and one of the most potent psychochemicals known
No known human overdose deaths
LD50 is about 400 times the behaviorally effective dose
Absorbed rapidly through the gastrointestinal tract
LSD is usually taken orally
Half-life is about three hours
LSD is metabolized by the liver
Excreted as the inactive chemical 2-oxy-lysergic acid diethylamide
Tolerance develops rapidly, within three to four days of daily doses
Recovery from tolerance is also rapid
Cross-tolerance occurs among LSD, mescaline, and psilocybin
Physical dependence to LSD or other hallucinogens has not been shown
LSD is a sympathomimetic agent
Autonomic signs appear quickly following administration
Dilated pupils, elevated temperature and blood pressure, increased salivation
The fact that the LSD molecule resembles the chemical structure of serotonin provided a clue that the drug might act on serotonin receptors to produce its effects
Best evidence indicates that LSD acts by stimulating the serotonin-2A subtype of receptor
LSD
The most powerful known hallucinogen
Tolerance develops rapidly
Has no taste, color, or odor
Used as microdots placed on blotter paper and licked
Behavioral effects last 6 to 8 hours
Operates on the neurotransmitter serotonin in the brain
Causes chromosome damage
Modification of perceptions
Visual images: Users see shapes and patterns, usually with intense colors and brightness
Users report an altered sense of time, changes in the perception of their own bodies, and alterations of auditory input
Synesthesia (“mixing of senses”), in which sounds may appear as visual images or visual pictures might alter in rhythm with music
Enhanced emotionality
Images may be perceived as beautiful and awe-inspiring or as intensely sad or frightening
Typically last six to nine hours
Autonomic responses occur over the first 20 minutes
Alterations in mood, perception, and sensation begin in the next 30 to 40 minutes
Full intoxication occurs within one hour
Loss of self-awareness and loss of control of behavior may occur
Unique and variable experiences
Expansive and pleasant—user feels she or he is uncovering great secrets or profundities
Constricted and negative—user experiences paranoia and feelings of persecution
Form-constants
May be combined with complex images
Synesthesia
Mixing of senses
Each trip is a unique experience
Impact on creativity
Unlikely to be enhanced successfully
Therapeutic usefulness?
Phase 1: lasting 1 to 2 hours, is marked by euphoria and either crying or laughing
Phase 2: 2 to 3 hours after ingestion, visual illusions and hallucinations appear
Phase 3: 3 to 4 hours after ingestion, is characterized by distortion of time, ego disintegration, mood swings, and occasionally panic and depression
Ergotism
A condition resulting from ingesting a fungus that grows on grains; marked by muscle tremors, burning, mania, delirium, hallucinations, and eventual gangrene
St. Anthony’s fire
Burning sensations caused by ergot poisoning
People during the Middle Ages would visit the shrine of St. Anthony in an attempt to cure it
Impossible to determine true incidence of adverse reactions
Some bad reactions may be due to impurities in street LSD and/or preexisting psychological conditions in the user
Panic reactions
Flashbacks
Recurrence of symptoms weeks or months after an individual has taken LSD
Rare, variable, and unpredictable in occurrence
DSM-IV-TR classifies them as Hallucinogen Persisting Perception Disorder
Long history of use among natives of Mexico
Psilocybe mexicana is the most well-known psychoactive mushroom
Primary active ingredient is the indole psilocybin
Dried mushrooms are 0.2 to 0.5 percent psilocybin
Effects are similar to LSD and mescaline and cross-tolerance exists among the three
Effects depend on dose
Up to 4 mg causes relaxation and some body sensations
Higher doses cause perceptual and body-image changes, with hallucinations in some individuals
Sympathetic arousal symptoms
May only be active after converted to psilocin
Good Friday study (1962) by one of Timothy Leary’s followers
Seminary students were given psilocybin or a placebo90 minutes before attending a religious service
Study looked at effect and magnitude of changes caused by the drug and at the durability of the changes
Researchers concluded that under certain circumstances, the drug enhances mystical or religious experiences
Most current production is from local, amateur growers
“Shrooms” might be consumed at a party in combination with alcohol
Psilocybin mushrooms
Called teonanacatl by Aztecs
In 1958, Albert Hofmann isolated the psychoactive ingredient
Effects are similar to LSD, but not as intense
Converted into psilocin by a stomach enzyme
Has no current medical use
Worldwide, an important naturally occurring hallucinogen found in many plants
DMT is the active agent in Cohoba snuff, used in some South American and Caribbean Indian hunting rituals
Usually snuffed, smoked, or taken by injection
Ineffective when taken orally
Effects are very brief, but tolerance does not develop to its psychological effects
Dimethyltryptamine (DMT)
From leaves, bark, and seeds of various plants grown in South and Central America
First synthesized in 1931 (“businessman’s LSD”)
Euphoric effects last 1 to 2 hours
May result in a psychotic episode
Tolerance does not develop
Reduces heart rate and blood pressure
Peyote (from the Aztec peyotl) is a small, spineless, carrot-shaped cactus, Lophophora williamsii Lemaire
Mostly subterranean, with only the pincushion-like top appearing above ground
Long pre-Columbian history of use among Mexican Indians, who used the plant ceremonially
Arthur Heffter isolated several alkaloids from peyote and showed that Mescaline was the primary psychoactive agent found in peyote.
Peyote cult moved north and became widely established among Indians of the plains by the late 19th century
Native American Church is an amalgamation of Christianity and traditional beliefs and practices of Native Americans, with peyote use incorporated into its ceremonies
Peyote use
In religious ceremonies
As a treatment for illness
Worn as a protective amulet
Current laws governing the use of peyote as a sacrament vary from state to state
Mescaline was isolated and synthesized by 1918
Peyote includes many other psychoactive alkaloids but mescaline has been identified as primarily responsible for the visual effects
Users may experience bad trips as well as nausea and physical discomfort
San Pedro cactus: Another mescaline-containing cactus, Trichocereus pachanoi, has also been used for thousands of years, but its recreational use is limited by frequent adverse side effects
Rapidly absorbed if taken orally
Half-life is about 6 hours
Effects
Low dose effects are primarily euphoric
Higher doses cause the full set of hallucinogenic effects
Most mescaline is excreted unchanged
Psychoeffective dose causes sympathetic arousal
LD50 is about 10 to 30 times the dose needed to cause behavioral effects
Tolerance develops more slowly to mescaline than to LSD
Cross-tolerance between LSD and mescaline
Peyote
A cactus containing the hallucinogen mescaline
Used by Aztec Indians for religious rituals
Mescaline
Psychoactive agent derived from the peyote cactus
Produces effects similar to norepinephrine
In small doses, produces euphoria
In larger doses, generates intense hallucinations
Stage 1: Contentment and sensitivity
Stage 2: Great calm, muscular sluggishness, and a shift of attention from external stimuli to introspection and meditation
Medical uses:
To treat patients with angina pectoris
Respiratory stimulant for patients with pneumonia
Peyote takes 30-90 minutes to take effect
Stays in the body about 10 hours
The hallucinogenic effect lasts about 2 hours
Tolerance to mescaline forms quickly and there is a cross-tolerance between mescaline and LSD
Prior to the scheduling of MDMA, some psychiatrists used it in practice because it was viewed as having a special ability to promote empathy, aiding in therapy
Effects
Heightened sense of “closeness” with others
Increased heart rate
Increased blood pressure
Euphoria
Increased sociability
Other autonomic effects
Some research has found that MDMA may cause brain damage
Selective destruction of serotonin neurons
Strong evidence from animal studies but limited evidence of long-term neurotoxic effects in humans
Listed as a Schedule I drug but continues to be studied as a potential psychotherapeutic agent
1-(1-phenylcyclohexyl) piperidine hydrochloride
Initially appeared to be a good anesthetic
It does not depress blood circulation or respiration or produce heart rate irregularities as some anesthetics do
Mechanism of action of PCP
PCP alters many neurotransmitter systems
Sigma receptor may be selective for PCP and similar drugs
Effects: The psychological reactions to the drug were unpredictable
By 1960, PCP had been characterized as
An excellent anesthetic for monkeys
A medically safe but psychologically troublesome anesthetic for humans
A hallucinogen different from LSD and mescaline, with profound effects on body perception
Currently, PCP is licensed for use as an animal anesthetic
Has had brief, sporadic periods of popularity
Relatively inexpensive and easy to manufacture
Sprinkled onto oregano, parsley, or alfalfa and sold as marijuana
Called “angel dust”
Joints made with PCP containing marijuana or another plant substance
Called “killer joints” or “sherms”
Some users develop psychological dependence on PCP
Animal studies also indicate a dependence-producing potential
A few but not all PCP users have been reported to behave violently
Urban legends of superhuman strength among PCP users are most likely false, BUT
Police attempting to arrest PCP users have had trouble subduing them due to the anesthetic effects of PCP
Phencyclidine hydrochloride (PCP or “angel dust”)
Developed in the 1950s as a surgical anesthetic
Illegal in the US since 1978
Generates anesthetic, hallucinogenic, stimulating, or depressing effects depending on the dosage and method of administration
Dissociative anesthetic
Alters perception of pain without loss of consciousness
Distributed under many names: angel dust, dust, rocket fuel, trank, crystal, PeaCe Pill, and hog
Popularity declined because it induced bizarre, violent behavior
Initially distributed in tablet or capsule form, but it also can be injected, snorted, or smoked
Acute effects last 4 to 6 hours, but the user may be in a state of confusion for 8 to 24 hours
Illegal use of PCP escalated toward the end of the 1960s and into the 1970s
Frequently used in place of other drugs such as LSD, THC, mescaline, or amphetamines
Because users are disoriented, paranoid, and violent, police and hospital personnel are wary of people who are using it
Feelings of warmth
Relaxation
Poor concentration
Depersonalization
Nystagmus
Agitation
Muscle rigidity
Sudden mood swings
Faster heart rate
Elevated blood pressure
Euphoria
Numbness
Distorted body image
Confusion
Poor coordination
Slow reaction time
Excessive salivation
Repetitive behavior
Higher body temperature
LARGE DOSES
Anorexia
Violent behavior
Restlessness
Suicide
Seizures
Paranoia
Insomnia
Amnesia
Depression
Coma
Death
Ketamine (K, Special K, or vitamin K)
Used in veterinary medicine in place of PCP
Effective for pain management in humans
Considered a dissociative anesthetic
Capable of producing confusion, hallucinations, delirium, excitement, irrational behavior, muscle rigidity, tremors, respiratory depression, irregular heartbeat, loss of appetite, skin rashes, nausea, and cardiac arrest
Active ingredient is atropine
Name Atropa belladonna comes from two major historical uses
As a deadly poison: Atropos, one of the Three Fates in Greek mythology, was responsible for cutting the thread of life
14 berries contain a lethal dose of atropine
As a beauty aid: Belladonna, or “beautiful woman”
Extract of the plant dilates the eyes, which is thought to improve appearance
Some users report the sensation of flying
Use of belladonna may have been tied to some early descriptions of witchcraft and the activities of witches
Contains all three anticholinergic hallucinogen alkaloids
Close association with love and lovemaking going back to Genesis
The root is forked and can be said to resemble a human body
Long thought to be endowed with magical and medical properties
Henbane Contains scopolamine and l-hyoscyamine
Long known and used as a poison
Shakespeare’s Hamlet
Contain all three anticholinergic alkaloids in varying amounts
Long history of religious and medicinal use
China: Used to treat colds and nervous disorders
Ancient Greece: Oracle to Apollo in Delphi
India: Worship of Shiva, ingredient in love potions
Native Americans: Used Datura inoxia (loco weed or jimsonweed; see right)
Belladonna (deadly nightshade)
Found in Europe, North Africa, and Asia
Member of the tomato and potato family
Can be extremely toxic
Datura (locoweed, Jamestown weed, or jimsonweed)
Used in ancient China, Greece, India, and Africa
Side effects are potentially harmful and noxious
Recreational use is increasing
Mandrake
Derived from the nightshade family
Used during the Middle Ages in connection with witchcraft and sorcery
In large amounts, can cause coma and death
Two psychoactive drugs: scopolamine and atropine
Scopolamine has been used to treat motion sickness
Atropine is used to dilate the pupils and lessen lung congestion
Nutmeg and Mace
From seeds and fruit of the Myristica tree
Used without effect in food preparations
Large quantities induce visual and auditory hallucinations
Myristicin
Substance found in nutmeg and mace
Chemically similar to mescaline
Unpleasant side effects
Called “fly agaric” because it stupefies flies that suck its juice
One of the most common poisonous mushrooms found in many parts of the world
Can cause severe effects of intoxication
Twitching limbs
Raving drunkenness
Agitation
Vivid hallucinations
Followed by hours of partial paralysis with sleep and dreams
Hallucinogen is excreted unchanged
Sacramental use mentioned in the poems of the Rig Veda (India)
May have been the ambrosia (“food of the gods”) mentioned in the secret rites of the Greek god Dionysius
May have been used by the cult that became Christianity
Long use by Siberian nomadic tribes
Used as a holy plant by several tribal groups in the Americas
Researchers have studied a number of compounds:
Muscarine
Bufotenin
Ibotenic acid
Muscimol
Muscimol can act as an agonist at GABA receptors
Anticholinergic hallucinogens
Found in datura and in Amanita muscaria mushrooms
Interfere with the action of acetylcholine to produce hallucinations
Have been used as medicines, poisons, and beauty aids
Can be highly toxic in large doses
Plants containing anticholinergic hallucinogens include belladonna, datura, henbane, and mandrake
Amanita muscaria is one of the oldest and most common hallucinogens; derived from the fly agaric mushroom
In India 3,500 years ago, the Rig Veda, an ancient Hindu book, called it soma
Viking warriors ingested Amanita muscaria to make them feel more fierce
This mushroom grows throughout the US, and can be lethal
Used for centuries in Oaxaca, Mexico, in religious ceremonies
Traditional methods of use
Chewing the leaves
Drinking a tea made from the crushed leaves
Smoking the dried leaves
Produces a hallucinatory effect
Recreational use reported in Mexico and the U.S.
Not currently listed as a federally controlled substance in the U.S., but is outlawed in several states
Mechanism of action
Active ingredient is salvinorin A, a highly potent agent
Salvinorin A binds selectively to the kappa opioid receptor, acting as an agonist (a unique pharmacological effect)
Salvinorin A
Relatively new hallucinogen derived from the sage family
Not yet illegal in the US, but banned in some states
When smoked, psychoactive effect lasts 15 minutes
Research into the effects of long-term medical and recreational use of the drug is limited
Ololiuqui, seeds of the morning glory plant Rivea corymbosa
Used as psychoactive agents in Mexico in the sixteenth century
Religious significance
Seeds contain several active alkaloids, including d-lysergic acid amide
Seeds from the Hawaiian baby woodrose, Argyreia nervosa, have also been used recreationally
Seeds contain d-lysergic acid amide
Outer coating of seeds contain toxic cyanogenic glycosides, which can make a user sick
Drugs and food share certain characteristics
They contain chemicals that interact with the body’s physiology
Drugs and food are not regulated in the same ways
Supplements may be thought of as drugs by consumers but are legally classified as food products
Pills, capsules, liquids, and powders classified as dietary supplements may be thought of as drugs by consumers BUT
They are legally classified as food products
They are treated very differently by the Food and Drug Administration (FDA)
Example of Saint John’s wort
Many people take it for its suggested ability to improve mood, reduce anxiety, and induce sleep
Classified as a dietary supplement, it is regulated more like a food than a drug
A drug is a product intended for use in the diagnosis, cure, mitigation, treatment, or prevention of disease
Before marketing, drugs must be shown to be
Safe when used as directed
Effective for their intended use
Food products and ingredients must be
Safe
Pure (unadulterated)
They are not required to show that they are effective or provide any benefit
Dietary Supplement Health and Education Act (DSHEA) of 1994
Passed in part due to pressure on Congress from the supplement industry in response to indications that the FDA was planning to expand regulation of dietary supplements
Defined supplements and set regulations for safety and labeling
Billions of dollars are spent each year on OTC drugs
In the US, four out of five adults take medicine or supplements on a weekly basis
The perception that nonprescription drugs (OTCs) are completely safe can have grave consequences
For many years, people could get OTC drugs (patent medicines) from traveling shows or from a local pharmacist or physician
The contents of these drugs were not regulated
The Pure Food and Drug Act (1906) stipulated that ingredients had to be listed on labels
The Food, Drug, and Cosmetic Act (1938) required that prescription drugs be proved safe and effective before being marketed
The Kefauver-Harris Amendment (1962) required that nonprescription (OTC) drugs be proved safe and effective
The FDA evaluated ingredients in OTC drugs rather than examining each product
In 2007, the FDA proposed a category for “behind-the-counter” (BTC) drugs which consumers would have to ask for after consultation with their pharmacist
The Combat Methamphetamine Epidemic Act (2005) banned OTC cold medicines containing pseudoephedrine, an ingredient used to make methamphetamine
A drug is a product intended for use in the diagnosis, cure, mitigation, treatment, or prevention of disease
Before marketing, drugs must be shown to be
Safe when used as directed
Effective for their intended use
A drug is a product intended for use in the diagnosis, cure, mitigation, treatment, or prevention of disease
Usage by Americans
Americans self-treat four times as many health problems as doctors treat, often with OTC drugs
Americans spend over$18 billion per yearon OTC drugs
1962 Kefauver-Harris amendment required that all drugs be evaluated for safety and efficacy
Active ingredients reviewed individually; three standards considered:
GRAS (generally recognized as safe) means that, given currently available information, the ingredient is considered safe
Nothing is entirely safe
Safe = a “low incidence of adverse reactions or significant side effects under adequate directions for use and warnings against unsafe use as well as low potential for harm which may result from abuse”
GRAE (generally recognized as effective) = a reasonable expectation that the pharmacological effect of the drug will provide clinically significant relief of the type claimed in a significant proportion of the target population
3. GRAHL (generally recognized as honestly labeled)
More than 300,000 OTC products on the market contain fewer than 1,000 total active ingredients now reviewed in over 80 therapeutic classes.
Those that the FDA has classified as safe and effective
Uniform labeling standards were adopted in 1997 to reduce consumer confusion
Layout, headings, and topics are consistent, and language has been made clearer and more concise, with less medical terminology
Consistent labels make it easier for consumers to compare products
Food products and ingredients must be
Safe
Pure (unadulterated)
They are not required to show that they are effective or provide any benefit
FDA can declare a product to be adulterated (unsafe) only if it presents a significant or unreasonable risk of illness or injury
Ingredients already on the market at the time of the Act:
Considered safe enough to be sold unless the FDA can demonstrate a risk
New ingredients:
Need some evidence that they would not present a significant or unreasonable risk
BUT much less evidence is required than for drugs
FDA authorizes a small number of health claims that food and supplement manufacturers can use if their products meet certain requirements
Based on available scientific research
Examples:
Adequate calcium intake and reduced risk of osteoporosis
Soluble fiber intake and reduced risk of heart disease
Unapproved health claims are not allowed, BUT
Supplement labels can make so-called structure/function claims
Relate to the structure or functioning of the body or to overall well-being
Examples:
Maintains cell integrity
Supports the immune system
Not a claim to prevent or treat a disease
Not reviewed by the FDA
Must carry a disclaimer:
This statement has not been evaluated by the Food and Drug Administration. This product is not intended to diagnose, treat, cure, or prevent any disease.
Same label format as those for packaged foods
Not as accurate or precise as drug labels
Testing has found that potency varies from bottle to bottle and even capsule to capsule
Amounts listed on label are for a plant substance and not the presumed active ingredient
Ingredients listed on the label may not be the actual active ingredients in a plant or herb
Dosage guidelines are not well-established for many supplements
There is no requirement for proof of effectiveness
Generic drugs are copies of brand name drugs and have the same dosage, safety, strength, and quality
One advantage of generic drugs is that they cost less
Trademark laws in the United States require that generic drugs not look exactly like brand name drugs
Same label format as those for packaged foods
Not as accurate or precise as drug labels
Testing has found that potency varies from bottle to bottle and even capsule to capsule
Amounts listed on label are for a plant substance and not the presumed active ingredient
Ingredients listed on the label may not be the actual active ingredients in a plant or herb
Dosage guidelines are not well-established for many supplements
There is no requirement for proof of effectiveness
DSHEA expanded the definition of supplements to include a variety of substances:
Vitamins and minerals
Herbs and concentrates and extracts of herbs
Amino acids
Many forms:
Tablets
Capsules
Liquids
Powders
FDA can declare a product to be adulterated (unsafe) only if it presents a significant or unreasonable risk of illness or injury
Ingredients already on the market at the time of the Act:
Considered safe enough to be sold unless the FDA can demonstrate a risk
New ingredients:
Need some evidence that they would not present a significant or unreasonable risk
BUT much less evidence is required than for drugs
FDA authorizes a small number of health claims that food and supplement manufacturers can use if their products meet certain requirements
Based on available scientific research
Examples:
Adequate calcium intake and reduced risk of osteoporosis
Soluble fiber intake and reduced risk of heart disease
Unapproved health claims are not allowed, BUT
Supplement labels can make so-called structure/function claims
Relate to the structure or functioning of the body or to overall well-being
Examples:
Maintains cell integrity
Supports the immune system
Not a claim to prevent or treat a disease
Not reviewed by the FDA
Must carry a disclaimer:
This statement has not been evaluated by the Food and Drug Administration. This product is not intended to diagnose, treat, cure, or prevent any disease.
Pro: Many more supplements on the market
Consumers have more options
Con: Much less research available about safety and effectiveness of supplements
Con: Supplements remain on the market unless or until the FDA presents clear evidence of risk
Example: Ephedra, a stimulant taken by people wanting to lose weight
First evidence of safety concerns published by the FDA in 1994
With the burden of proof now with the FDA, it took 10 additional years for the FDA to compile evidence to get ephedra off the market
Definitely hazardous
Aristolochic acid
Very likely hazardous
Comfrey
Androstenedione
Chaparral
Germander
Kava
Cesium
Colloidial Siver
Graviola
Likely hazardous
Bitter orange
Organ/glandular extracts
Lobelia
Pennyroyal oil
Scullcap
Yohimbe
DIETARY SUPPLEMENT ACT
Introduced by Senator John McCain in February 2010.
Would have required all manufacturers to register with the FDA and provide a complete list of ingredients.
The FDA could also recall any ingredient they found to be unsafe.
The dietary supplement industry mounted a campaign against the regulation and McCain withdrew the bill
PSYCHOACTIVE SUPPLEMENTS
Saint John’s wort (Hypericum perforatum)
Was originally thought to prevent possession by demons
Currently used as a potential treatment for both anxiety and depression
Research results have been mixed, but there is some evidence supporting its use for depression
It may interact with prescription drugs, so users should notify their physicians
S-adenosyl-L-methionine (SAMe)
A naturally occurring substance, the active form of amino acid methionine
Researched as a possible antidepressant
Not yet any solid evidence it is more effective than placebo
Ginkgo biloba
Long history of medical use in China
Active ingredients and mechanisms of action haven’t yet been identified
Reduces blood clotting; thins blood to improve circulation
PotentiallyResearch suggests a slight ability to improve memory
risky if used with aspirin or other drugs that reduce clotting
Supplements: no requirement for proof of effectiveness
Disclaimer for any structure/function claim:
“This statement has not been evaluated by the Food and Drug Administration. This product is not intended to diagnose, treat, cure, or prevent any disease.”
Herbal drugs are largely unregulated
It is unclear whether they should be classified as drugs, foods, or herbs
Manufacturers of herbal drugs cannot make claims regarding their benefits without proof
Some herbal remedies can interfere with the effectiveness of conventional drugs
Consumers must look at advertisements for OTC drugs carefully because they may give inaccurate impressions
Always read the information on labels of OTC medicines
Relieving the symptoms of an illness is not the same as curing the illness
Some OTC drugs (stimulants, nasal sprays, sedatives, eye drops, cough syrups, and laxatives) can result in dependency
Consumers must look at advertisements for OTC drugs carefully because they may give inaccurate impressions
Always read the information on labels of OTC medicines
Relieving the symptoms of an illness is not the same as curing the illness
Some OTC drugs (stimulants, nasal sprays, sedatives, eye drops, cough syrups, and laxatives) can result in dependency
1938 Food, Drug, and Cosmetic Act established a classification of drugs that can be sold only by prescription
Possible differences between OTC and prescription drugs
Dosage: An OTC version of a drug may come in smaller doses
Chemicals: A prescription drug may contain a chemical not allowed for OTC sale due to potential toxicity
FDA panels review products and may switch drugs to OTC status
Examples of drugs switched to OTC status include ibuprofen (analgesic), orlistat (weight-loss), and cetirizine (antihistamine)
Should there be a class of drugs between OTC and prescription? Pharmacist recommended?
Stimulants
FDA allows stimulants to be sold to “help restore mental alertness or wakefulness when experiencing fatigue or drowsiness”
Only ingredient allowed by FDA in OTC stimulants is caffeine
Combinations of caffeine and other stimulants (e.g., ephedrine) are not allowed
The primary ingredient in OTC stimulants is caffeine
Does not reverse alcohol intoxication
Examples include Vivarin, No Doz, and “energy drinks” and inhalable forms of caffeine
Excessive caffeine consumption (caffeinism) results in nervousness, anxiety, tachycardia, sweating, and panic
Weight-control products
Phenylpropanolamine (PPA) was sold over the counter by the late 1970s
Combinations of PPA and caffeine sold for a brief period before being banned in 1983
Concerns over effectiveness of PPA and the safety of recommended dosage due to its effects on blood pressure
2000: FDA requested all companies to stop marketing products containing PPA
Weight-control products
Additional products banned due to lack of safety or effectiveness
Ephedrine
Benzocaine-containing candies and gums
Starch blockers
Cholecystokinin (CCK)
Currently, one FDA-approved weight-control OTC drug: Orlistat (alli)
Ephedrine (ephedra) can be fatal when combined with other stimulants such as caffeine
Orlistat (alli) works by blocking the absorption of about 25% of the fat in the foods that people consume
Phenylpropanolamine (PPA) is an appetite suppressant, structurally similar to amphetamines
Benzocaine is a topical anesthetic that numbs the tongue and palate
Sedatives and sleep aids
Early OTC sedatives and sleep aids
acetylcholine receptor blocker scopolamine + antihistamine methapyrilene
FDA review panel eventually rejected scopolamine but accepted methapyrilene
Later methapyrilene was found to cause cancer in rats, so it was no longer classified as GRAS
Different antihistamines were then marketed, and brands changed active ingredients frequently
Currently, there are no approved OTC sedatives; OTC sleep aids contain antihistamines
Anesthetics (“without sensibility”) reduce all types of sensation or block consciousness completely
Analgesics (“without pain”) reduce pain selectively without causing a loss of other sensations
Types of pain, based on place of origin
Visceral pain from nonskeletal portions of the body
Relieved by opioids
Somatic pain from muscle or bone
Relieved by aspirin and related products
About 35 percent of patients obtain pain relief from a placebo
Development
Long historical use of teas and extracts of willow and poplar bark for pain relief
Active ingredient—salicylic acid—was identified, synthesized, and mass-produced in the nineteenth century
Related compound—acetylsalicylic acid—was synthesized in 1898 by a Bayer Laboratories’ chemist; had fewer side effects
1899: Patented and released for prescription sale in the form of a white powder
1915: Sold over the counter in tablet form
The primary ingredient in many OTC sedatives and sleep aids is some type of antihistamine
A person should not drive an automobile, drink alcohol, or engage in potentially hazardous activities while taking antihistamines
Examples include Nytol, Sominex, and Seep-Eze
ASPIRIN
Therapeutic use
Analgesic—effectively blocks mild-to-moderate somatic pain
Maximum pain relief occurs in about one hour; effect lasts for up to four hours
Especially effective for headache and musculoskeletal pain
Antipyretic—reduces fever
Does not lower body temperature in someone with normal body temperature
Causes vasodilation of peripheral blood vessels and increased perspiration
Therapeutic use
Anti-inflammatory—reduces swelling, inflammation and soreness
Relatively low toxicity
Absorbed from the stomach and intestines
Effects/Risks
Increases bleeding time by inhibiting blood platelet aggregation
Can cause bleeding problems for surgical patients
May prevent heart attacks and strokes by preventing clots in high-risk patients
Induces gastrointestinal bleeding
Reye’s syndrome—rare but serious disease
Effects can include disorientation, personality changes, lethargy, coma, and death
CDC recommends that aspirin should not be given to anyone under age 20 who has a suspected viral illness such as cold, influenza, or chicken pox
Accidental poisonings and suicide attempts
Mechanism of action
Prostaglandins are local-acting hormones
Released when cell membranes are injured
Mediate pain in injured areas by sensitizing neurons to stimulation
Aspirin inhibits two forms of the cyclooxygenase (COX) enzyme
Blocks the synthesis of pain-causing prostaglandins
Aspirin also acts on prostaglandins involved in heat regulation
ACETOMINAPHEN
Acetaminophen is closely related to phenacetin, a now banned pain reliever
Compared to aspirin:
As effective in analgesic and antipyretic effects
Less useful as an anti-inflammatory drug
Causes less gastric bleeding
Overuse of acetaminophen can cause serious liver disorders
Not safer than aspirin if recommended dose is exceeded
As of 2009, the FDA limited the maximum single adult dose to 650 mg for OTC products
Analgesics
Ibuprofen is an aspirin-like analgesic and anti-inflammatory; it also inhibits COX enzymes
Potential side effects
Nausea and stomach pain
Liver damage (if taken in large amounts)
Class of drugs is known as nonsteroidal anti-inflammatory drugs (NSAIDs)
Originally available by prescription, but now also available over the counter
All-too-common cold
Colds are viral infections, caused by viruses in the rhinovirus or coronavirus families
Viruses damage or kill the cells they attack
In the case of colds, the affected cells are on the upper respiratory tract
Symptoms include coughing, sneezing, and production of fluid by the mucous membranes
All-too-common cold
Most cold viruses enter the body through the nose or eyes; they are usually transmitted via an infected person’s hands
Frequent handwashing is a good strategy to reduce the risk of contracting a cold
Treatment of cold symptoms—no cure
Modern cold remedies contain three common types of ingredients
Antihistamines for temporary relief of runny nose and sneezing
Of questionable benefit for cold symptoms
Nasal decongestants for temporary relief of swollen nasal membranes
Analgesic-antipyretics for temporary relief of aches and pains and fever reduction
Allergy and sinus medications
Rely mainly on antihistamines
May also include an analgesic
CHOOSING AN OTC
Most products contain one or more of only a small number of ingredients, in different combinations
An informed consumer can understand a large proportion of these products by being familiar with only a few drugs
Single ingredient medications may be preferable to combination products
Avoid medication interactions and side effects of drugs that are designed to treat symptoms you may not have
Two basic types of analgesics:
External analgesics, such as Ben-Gay and Absorbine, applied to the skin for sore muscles
Internal analgesics such as aspirin, acetaminophen, ibuprofen, naproxen sodium, and ketoprofen
In 2009, 53,000 people went to emergency rooms due to acetaminophen, and 27,000 people went to emergency rooms due to ibuprofen
Aspirin (acetylsalicylic acid)
Similar to a chemical in willow bark
Developed by Bayer
Alters synthesis of prostaglandins
Reduces inflammation, especially rheumatoid arthritis
Antipyretic (fever-reducing)
Reduces risk of heart attack and several diseases
Increases bleeding risk
Inhibits interferon
Avoid use by children
Children with chicken pox or flu-like symptoms should not be given aspirin
Acetaminophen (Tylenol)
Byproduct of phenacetin
Reduces pain and fever
Interferes with prostaglandin synthesis
Adverse effects on liver and kidneys
Irritates stomach less than aspirin
Does not prolong bleeding
Can cause death
Ibuprofen (Advil)
Reduces pain
Lessens inflammation
Produces less stomach upset
May reduce risk of breast cancer and Alzheimer’s
Prolongs bleeding time
Can cause allergic reaction
Numerous side effects
May increase risk of peptic ulcers and enlarged prostate
Can cause death
Naproxen sodium (Aleve)
Comparable to ibuprofen in effectiveness
Long-term pain relief
Ketoprofen (Orudis KT and Actron)
Effective as ibuprofen
More effective than acetaminophen for reducing fever in children
COLD/ALLERGY
OTC drugs relieve symptoms of colds and allergies
Many people overcome colds more quickly when physicians prescribe medications, even placebos
Cough and cold remedies for children can be hazardous
ANTIHISTAMINES
When allergens are present, the body releases histamines that normally help fight infections
Antihistamines are effective for relieving itching, nasal inflammation, and skin allergies
Antihistamines are found in cough syrups, hay fever and motion sickness preparations, and decongestants
Dizziness
Weakness
Nervousness
Poor concentration
Headache
Drowsiness
Blurred vision
Difficulty urinating
Constipation
Hives
Dry mouth, nose, and throat
COUGH
A cough can be productive (produce secretions) or nonproductive
Drugs that suppress or prevent coughing are antitussives
Codeine provides relief within 15 to 30 minutes, and the effects last 4 to 6 hours
Dextromethorphan (Delsym) is nonnarcotic , but can induce drowsiness, nausea, and dizziness
A productive cough helps respiration by removing mucous secretions and foreign matter
Cough syrups that increase mucous secretions, making a cough productive, are called expectorants
The most common expectorant is guaifenesin
Decongestants constrict blood vessels of the nasal passages, improve air flow, and obstruct secretions
Some produce a rebound effect, in which the congestion becomes worse than it was originally
Dependency is possible – nasal sprays should not be used for more than three consecutive days
Pseudoephedrine is the active ingredient in the OTC decongestant Sudafed
ANTACIDS
Neutralize stomach acid (hydrochloric acidr) reducing the symptoms of the upset stomach
OTC products contain such drugs as:
Sodium bicarbonate
Calcium carbonate
Salts of magnesium
Salts of aluminum
Product examples include:
Tums, Rolaids, Alka Seltzer
Newer heartburn remedies include histamine (H2) blockers and proton pump inhibitors (PPIs)
H2 blockers (Tagamet HB and Zantac) are effective in less severe cases
The American College of Gastroenterology recommends PPIs (Prilosec and Nexium) because they are more effective
Early concoctions
May not have provided any true physical performance enhancement
Could have placebo value that boosted a competitor’s self-confidence
Ancient Greek Olympians and Aztec athletes used plant-based stimulants
Athletic competitions probably developed in tribal societies as a means of training for war
Strychnine
At low doses = a CNS stimulant
At higher doses = convulsions and death
Use reported in boxers, possibly to make them more aggressive and keep them from tiring quickly
1904 St. Louis Olympic marathon winner
Fueled by a mixture of brandy and strychnine
Collapsed and had to be revived after the race
Some use of strychnine in world competition may have continued into the 1960s
Cocaine: Available beginning in the 1800s
Mariani’s coca wine was used by the French cycling team
Athletes later used pure cocaine
Caffeine: Many athletes used coffee and/or pure caffeine
“Doping” initially referred to a cheap brandy given to racing dogs and horses to slow them down
Term came to refer to the opposite—an effort to improve rather than impair performance
Amphetamines: More potent than caffeine, safer than strychnine
Probably in use by athletes soon after they were introduced in the 1930s
Many early reports of the use of “pep” pills by boxers, cyclists, and soccer players
1950s Olympics: Many reports of amphetamine use, a few deaths
1960 Rome Olympics: One cyclist died, several others hospitalized due to amphetamine use
International regulations/TESTING
Ergogenic = “energy producing,” a general term for performance enhancement
1960s: Some sports began testing athletes, but problems continued
1967: Tommy Simpson died during the televised Tour de France
Amphetamines found in his system
1968: International Olympic Committee established rules to disqualify any athlete who used banned drugs or refused to be tested
The scope of testing at the Olympics has continued to expand over time
Football 1960s: Many football players used amphetamines during games
Attitudes toward amphetamines changed
National Football League (NFL) banned the distribution of amphetamines by team physicians and trainers in 1971
But initially no testing of players, who could still obtain the drug on their own
Current NFL policy restricts all use of amphetamines and many other drugs
STEROIDS Established medical use for weight gain in malnourished people
Soviets began to use testosterone to build up athletes in the 1950s
Many U.S. athletes in certain sports used steroids in the 1960s
Weight lifters and bodybuilders
Track and field athletes
Testing began in the 1970s
Athletes began to be caught and banned from competition for steroid use
Some individual use among Western athletes
Widespread use by athletes from some Eastern European countries
BALCO Rumors of steroid use circulated around certain professional baseball players
June 2003: Evidence surfaced that athletes were using tetrahydrogestrinone (THG)
Previously unknown steroid that did not show up in tests developed by the U.S. Anti-Doping Agency
BALCO Laboratories founder Victor Conte was implicated, along with a number of professional athletes from several different sports
Fallout from the BALCO/THG scandal continues
TESTING
1980s: Reports of drug use among athletes grew
Most amateur and professional sports organizations adopted more strict testing guidelines and longer lists of banned substances
Despite extensive and expensive tests, use of performance-enhancing substances continues
Ongoing development of new drugs and strategies to help athletes avoid detection
STIMULANTS
Effectiveness
Studies indicate that most athletes perform better on amphetamines, but the improvement is small
Small improvements can make a big difference at high levels of competition
Underlying mechanism of improvement is unclear
Increased physical ability (increased strength, masking of fatigue)
Effects on the brain (increased confidence, winning attitude)
At legal levels, caffeine may provide a slight improvement in endurance performance
Cocaine
No experiments have been carried out on its performance-enhancing abilities
In the 1980s, many athletes believed it did improve performance
Similar to amphetamine in its properties
Shorter duration of action, so it would likely have only brief effects
Ephedrine (available in pure form or in ephedra extract or ma huang)
On Olympic and NCAA lists of banned substances
Professional sports organizations were slower to ban it
NFL eventually banned it but Major League Baseball did not
Players continued to use it for its stimulant effects and for weight loss
Death of Baltimore Orioles pitcher Steve Bechler in 2003 was attributed to heat stroke brought on by ephedrine
FDA was able to ban ephedra and ephedrine in dietary supplements in 2004
Current use
Some athletes continue to use stimulants during training and then discontinue use several days before competition to avoid testing positive
Risks of use
Unknown effects of use during training on competitive performance
Possible overexertion or injury due to fatigue-masking effect of stimulants
Dependence, paranoid patterns and withdrawal symptoms
STEROIDS Physical effects of natural testosterone
Androgenic effects (masculinizing)
Growth of the penis and other male sex glands
Deepening of the voice
Increased facial hair
Anabolic effects (tissue building)
Increased muscle mass
Control of the distribution of body fat
Increased protein synthesis
Increased calcium in the bones
Synthetic anabolic steroids
Drug companies synthesized types of steroids that have fewer of the androgenic effects and more of the anabolic effects of steroids
Not entirely free of androgenic effects
EFFECTIVENESS
Mixed and controversial research findings
Testosterone builds muscle mass and strength during puberty
Animal studies: Synthetic anabolic steroids build muscle in castrated animals
Unclear if giving additional anabolic steroids to adolescent or adult males who already have normal circulating levels of testosterone will have a significant effect
Laboratory research on healthy men
Steroids can produce small increases in lean muscle mass and sometimes small increases in muscular strength
No evidence for an overall increase in aerobic capacity
Research findings may not match word-of-mouth
ISSUES IN RESEARCH
Difficult to extrapolate laboratory findings to athletes
Athletes may use much higher doses
Athletes may use combinations of steroids (“stacking”)
Psychological effects of steroids may affect results
Users report that they feel stronger—that they can lift more or work harder
Possible active placebo effect—a belief in the power of steroids enhanced by the sensation that the drug is doing something because one can “feel” it
PSYCHOLOGICAL EFFECTS
Steroids produce a stimulant-like high and increased aggressiveness
May allow more work done during training and increased intensity of effort during competition
Risks, especially at high doses
Psychological dependence, resulting in mood swings and depression when users don’t take the drugs
Interference with social relationships and other areas of life
“Roid rage”: Stories may be exaggerated, but the number of reports of violent feelings and actions among steroid users is a key area of concern
NEGATIVE EFFECTS
Peliosis hepatitis
Bloody liver cysts
Unhealthy changes in blood lipid levels
May contribute to atherosclerosis, high blood pressure, and heart disease
Acne
Baldness
Special risk for young users
Premature closure of the growth plates of the long bones, thus limiting adult height
Special risks for men
Atrophy of the testes
Breast enlargement
Special risks for women, who normally have only trace amounts of testosterone
Decreased breast size
Enlargement of the clitoris
Increased facial hair
Deepening of the voice
Some effects may be irreversible
REGULATION
Issues leading to regulation
Large black market for the drugs
Concerns about use among adolescent boys, even nonathletes
Anabolic steroids are listed on Schedule III
Limited prescription refills
More record-keeping
COLLEGE STIMULANT USELow doses of stimulant drugs can improve performance that has been disrupted by fatigue or sleep-deprivation
Recently there has been a renewed interest in using stimulants as nootropics and cognitive-enhancers
Some stories imply that the majority of college students take these drugs to enhance their performance.
The actual percentage is 4-7 %
Drugs maybe useful in increasing alertness and assisting one to study for a longer period of time, but they wont increase critical thinking or creativity
Health risks associated with nootropics
All stimulants increase cardiovascular activity, which, at large doses, can increase the likelihood of heart attack or stroke
These drugs can also disrupt sleep and excessive loss of sleep can lead to the development of physical and mental health problems.
Fairness
Some students may not have access to a physician
Some students may not want stimulants due to health risks.
HGH
A pituitary hormone that can potentially increase the height and weight of an individual to gigantic proportions
Rare instances of excessive body production of the hormone produces “giants” over 7 feet tall
Condition usually results in early death
Administration of doses of human growth hormone and related hormones may produce a more controlled increase in body size
Experiments have shown HGH may increase lean body mass but may not improve strength
It is illegal to distribute human growth hormone for nonmedical purposes
BETA2 AGONISTS
Action and effects
Selective stimulation of the beta-2 subtype of adrenergic receptors
Sympathomimetic effects on the bronchi of the lungs
Used in treating asthma
Animal studies showed a possible effect on muscle mass
No evidence for improved athletic performance
Banned for use in competition
Example: Clenbuterol
CREATINE
A natural substance found in meat and fish, sold legally as a dietary supplement
Actions and effects
Helps regenerate ATP, which provides the energy for muscle contractions
Users tend to gain weight, some of which is water weight
Creatine may improve strength and short-term speed in sprinting
No evidence for improvement in longer-distance events
Performance may decrease due to weight gain
GETTING “CUT”
Weight challenges in sports
Wrestlers and jockeys need to build strength and train hard but also need to make a specific weight
Athletes in these sports may engage in extreme methods to achieve short-term weight loss
Purging
Diuretics
Sweating (exercising in heat or while wearing nonporous clothing)
Bodybuilding terms and strategies
“Cut” refers to a lean, strong body, a “sculpted” body
“Ripped” or “shredded” refers to a more extreme version of looking cut
Every muscle fiber and vein is visible
Body fat percentage may be as low as 6 to 9 percent
14-20% is ideal for a healthy male
Many bodybuilders take “fat burning” supplements of questionable safety and effectiveness
Performance-enhancing drugs, also known as ergogenic aids, are used to gain a competitive advantage
As early as 300 BC, some Greek athletes ate mushrooms to enhance their performance
Drug abuse in sports has become more publicized in the last few years – e.g. Major League Baseball
The type of sport and gender of the athlete influence the drug of choice
Anabolic steroids
Substances used to increase muscle mass
Related to male sex hormones
Testosterone during puberty augments muscle mass and strength, but later in adolescence stunts growth
Users may engage in stacking – ingesting and injecting several steroids at the same time
Users display symptoms of depression, panic, anxiety, paranoia, mania, and suicidal behavior (roid rage)
Steroid effects on men and women:
Acne
Increased susceptibility to infections
Abrupt mood changes
Hypertension
Decreased HDL (good cholesterol)
Effects on liver
Stunted growth
Men:
More frequent erections
Atrophied testicles
Enlarged breasts
Enlarged prostate
Infertility
Baldness
Women:
Baldness
Decreased breast size
Enlarged clitoris
Increased facial hair
Fluid retention
Menstrual irregularities
Deepened voice
Human growth hormones (HGH)
Hormones that stimulate protein synthesis
Used by athletes to enhance performance
Erythropoietin (EPO)
Hormone that enhances cardiovascular endurance by increasing red blood cell production
Can lead to blood clots, increasing the risk for heart attacks, stroke, and pulmonary embolism
Creatine monohydrate
Natural substance used to increase strength and short-term speed
Sold over-the-counter as a nutritional supplement
Believed to increase water content in muscles, adding to their size and ability to function
Reduces range of movement
Reported side effects include muscle cramping, dehydration, water retention, and kidney problems
Not regulated by the FDA
Tetrahydrogestrinone (THG)
Designer drug, closely related to the banned anabolic steroids gestrinone and trenbolone
Used by many professional athletes
Not approved by FDA
May cause some of the same side effects as steroids
Androstenedione
Food supplement used for muscle development
Precursor molecule, one step away from testosterone
Banned by NCAA, NFL, and IOC
Effects are similar to those of anabolic steroids
In January 2010, the FDA recalled androstenedione because of its potential side effects
STIMULANTS
Cocaine impairs performance requiring hand-eye coordination and concentration
Amphetamines have been used in sports to reduce fatigue and sustain intense exercise
Caffeine is used to improve endurance, especially short-term endurance
Many sports and energy drinks are high in caffeine and calories
DEPRESSANTS
Barbiturates inhibit performance
Benzodiazepines (minor tranquilizers) impair psychomotor performance
Alcohol reduces psychomotor skills and aerobic capacity – also impairs reaction time, fine and complex motor coordination, balance and steadiness, visual tracking, and information processing
SEXUAL PERFORMANCE
Many prescribed and over-the-counter drugs alter sexual functioning
Drugs such as methamphetamines and alcohol lead to unsafe sexual practices
Drugs are commonly used, especially in clubs, to make the user less sexually inhibited
Alcohol and narcotics can adversely affect sexual desire, performance, and satisfaction