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CNS Stimulants
Spring 2010
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CNS Stimulants
Caffeine
Cocaine
Amphetamines
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CaffeineCaffeine
Coffee is the worlds most popular
beverage (also in soda, tea, etc)
Placed in sports products that are
promoted as energy drinks
OTC headache and anti-drowsiness
remedies
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How Exercise Affects the Action ofHow Exercise Affects the Action of
CaffeineCaffeine
Flow limited
Elimination is affected by
Exercise
Obesity
Sex
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How Exercise Affects the Action ofHow Exercise Affects the Action of
CaffeineCaffeine
Stimulates epinephrine output
Exercise and caffeine both
stimulate epinephrine output
independently
Exercise is the more dominantinfluence
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How Caffeine AffectsHow Caffeine Affects
ExercisersExercisers
Tolerance within several
days of regular use
Nave or tolerant subjects?
Stimulates the CNS
Enhances neuromuscular
transmission
Improves muscle contractility
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Cardiovascular EffectsCardiovascular Effects
Effects vary timing of
measurements, type of subject
can influence datainterpretation
Not found to affect cardiacoutput, or SV acutely in either
normative or hypertensive
subjects
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Renal EffectsRenal Effects
Acts as a diuretic in resting
individuals
Does not increase renal
response while ingested during
exercise**
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Metabolic EffectsMetabolic Effects
Enhance the bodys ability to use fat for
energy and sparing glycogen stores
Subjects who received caffeine were
able to exercise harder increase in
lactate and decrease in RPE (ratings of
perceived exertion)
Fat oxidation increase even in chronic
users
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Neuromuscular EffectsNeuromuscular Effects
Decreases motor reaction time
auditory and visual stimuli
Ergolytic in fine motor
coordination or complex skills
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Effects on PerformanceEffects on Performance
Does exert metabolic,
musculoskeletal and CNS
effects = improvement inperformance
Capsules work better thancoffee even with same
dosage
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Effects on PerformanceEffects on Performance
Ergogenic in caffeine nave
subjects increase in work
completed and time to exhaustion
Ergogenic in prolonged endurance
exercise but not purely anaerobic
exercise
Opposite of creatine and metabolic
enhancers.
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NCAA/USOCNCAA/USOC
Not banned, but restricted
Even amounts that do not
exceed the limits of the NCAA
and USOC, ergogenic effects
are still seen.
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COCAINE
CNS Stimulant & appetitesuppressant
Increase HR Increase BP
Increase respiration
Can be fatal after first use
Len Bias?
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HISTORY
The world's most powerful
stimulant of natural origin.
South American Indians have
used cocaine in plant form for
at least 5000 years.
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HISTORY
Traditionally, the leaves havebeen chewed for social,
mystical, medicinal andreligious purposes.
The introduction of coca toEngland occurred early innineteenth century.
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HISTORY
The active ingredient of the coca
plant was first isolated in the West
around 1860. Freud describedcocaine as a magical drug.
It was regarded as a wonder drug
that would cure many illnesses.
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HISTORY
Major dangers of cocaine wereknown almost from the first
uses of the purified drug.
Coca-Cola was introduced in
1886 as a valuable brain-tonicand cure for all nervousafflictions.
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HISTORY
Until 1903, a typical servingcontained around 60mg of cocaine.
Today, Coca Cola imports eight tonsfrom South America each year (forflavor).
Cocaine was sold over-the-counter,until 1916.
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ROUTES OF
ADMINISTRATION Absorption (snorting)
Injection
Inhalation (smoking: freebasingor crack)
Sometimes combined with other
drugs Pot
Heroin
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MECHANISM OF ACTION
Cocaine stimulates the release
of norepinephrine
Inhibits the reuptake of
norepinephrine and dopamine
Results in an increased
concentration of norepinephrinewithin the synaptic junction
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MECHANISM OF ACTION
The drug induces a sense of
exhilaration in the user
primarily by blocking thereuptake of the
neurotransmitter dopamine in
the midbrain.
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MECHANISM OF ACTION
When administered
intravenously (IV) to humans,
the half-life is in the range of 16to 87 minutes.
Fifteen minutes after an IV
injection of cocaine, the subjectexperiences a craving for more
cocaine.
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MECHANISM OF ACTION
Remains detectable in the body
for 1-2 days.
The effects of cocaine use
appear within seconds to
minutes after administration.
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Clinical Use
Topical anesthetic
Where?
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Risks of Cocaine Use
ACUTE
Exaggerated
pressor response Cardiac
Arrhythmias
Seizures
Stroke Hyperthermia
Sudden Death
CHRONIC
Paranoia
Dependence Weight loss
Pulmonary
damage (if
smoked)
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Sport Performance
Cocaine appears to offer no
ergogenic properties and is very
likely ergolytic. Possibly due to potency and
duration of effects
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Amphetamines
CNS Stimulant
Effects last longer than cocaine
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History
Synthesized in 1887
Related to the plant Ephedra
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History
Used by military in many
nations (pep pills)
Combat fatigue
Increase alertness
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History
Methamphetamine
Synthesized in 1893
Used by Germans in WWII
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Clinical Use
Treatment of ADHD
Appetite suppressant
Anti-depressant
Sleep disorders
Narcolepsy
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Mechanism of Action
Release catecholamines
Norepinephrine
Dopamine
Serotonin (high doses)
More pronounced with meth use
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Physical Effects
Dose dependent
Therapeutic doses
Increase energy/stamina
Decreased appetite
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Physiological Effects
Decreased sense of fatigue
Increase BP
Increase HR
Depletion of glycogen stores
Result of it being an appetite
suppressant.
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Use in Sport
Cocaine
Recreational drug
Feeling of invincibility
Amphetamine
Increase stamina
Decrease reaction time
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NCAA/USOC
Both are banned
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MLB
Amphetamine use has been
reportedly used for decades
Some think amphetamine use is
a more wide spread problem in
MLB than A-AS.
