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Erogogenic Aid ppt - Eastern Illinois University


									Ergogenic Aids
    Anabolic Androgenic
• 1935 - testosterone is isolated
• German soldiers in WWII?
• 1945 - ‘The Male Hormone’ by de Kruif
• 1950’s - Soviet weight lifters
• 1954 - world weight lifting
 championships in Vienna and US team
 physician Dr. Ziegler
• 1958 - Ciba Pharmaceutical Company
 releases Dianabol

• 1960’s
• Chemically modified analogs of
 • Maximize the anabolic
 • Minimize the andronergic
• Act directly on the cell nucleus
 • Increase production of structural and
    contractile proteins
Anabolic Androgenic

•   Maxibolin

•   Anavar

•   Winstrol

•   Dainabol

•   Anadrol


•   Deca-durabolin
        AAS and
• Research studies limited by
  methodological problems and dosage
• Bhasin et al, 1996
 • Increase FFM, muscle size, and
            AAS and
• Giorgi et al, 1999
 • Increase in body weight, FFM, arm
   girth, rectus femoris circumference,
   and libido
 • Increase in SBP, frontal alopecia,
   acne, and personality changes
• Forbes et al, 1992.
 • Testosterone
 • Increase in LBM and decrease body
    Body Composition
•   Body Weight

•   Body Dimensions

•   Lean Body Mass:

    •   More increase with type II fibers

    •   More increase in upper body

•   Fat Mass

•   Effects my persist for more than 6-12 weeks after
    cessation of ASS use.

• Increases of 5-20%
• Likely dosage dependent with dosages
  greater than 10 mg/day
• Maybe.
• Some studies show lower heart rate
  and/or waste products during recovery
  with ASS use
 • urea, ammonia, creatine, creatine
    kinase, lactic acid, etc.
        Side Effects
• Decrease HDL and flow mediated
• Psychological effects
• Mortality rate
 • 12.9% compared to 3.1%
• Infection due to needle sharing
                  AAS Side Effects
• Men
   • testicular atrophy
   • decrease testosterone and sperm production
   • enlargement of male breast
   • prostate enlargement
• Women
   • disrupts menstruration and increase masculization
   • breast regression and clitoris enlargement
   • deepening of voice and growth of facial hair

• All
    •   Liver toxicity
    •   Growth plate damage
• Urine versus blood
 • Masking agents
• Testosterone to Epitestosterone
 • Normal is 3:1 or less
 • 6:1 is the IOC limit.
• Other factors, particularly
  prohomones, can alter the
  Testosterone to Epitestosterone
Growth Hormone
        Growth Hormone

The growth hormone (GH) is a protein hormone released from the anterior
pituitary gland under the control of the hypothalamus.
It stimulates the secretion of somatomedins from the liver, which are a family of
insulin-like growth factor (IGF) hormones. These, along with GH and thyroid
hormone, stimulate linear skeletal growth in children.
In adults, GH stimulates protein synthesis in muscle and the release of fatty acids
from adipose tissue (anabolic effects).
It inhibits uptake of glucose by muscle while stimulating uptake of amino acids.
The amino acids are used in the synthesis of proteins, and the muscle shifts to
using fatty acids as a source of energy.
        Growth Hormone
•   Protein synthesis
•   Carbohydrate metabolism
    •   hGH is an anatagonist to insulin;
•   Lipid metabolism
    •   increase release of free fatty acids and their
•   Promote positive calcium, magnesium and
    phosphate balance; bone growth
Resistance Exercise
• Does hGH play a role in the muscle
  hypertrophy from strength training?
• Yes, and may be related to the demand
  on anaerobic metabolism but…
• ...IGF plays an independent role
• It is secreted by hGH as well as muscle
Resistance Exercise

• No data exist on hGH with IGF and
  exercise in humans
• In rats, hGH with IGF and exercise
  showed an increase in the size of all
  fiber types
Endurance Exercise
• Increase in hGH after 10 minutes of
  high intensity exercise
• IGF release peaks at 10 minutes of
  exercise although it appears to be
  independent of hGH
• Threshold for hGH release?
 • 60% of VO2max, lactate threshold,
Endurance Exercise
• Exercise above the lactate threshold
  amplifies the pulsatile release of hGH at
• Frequency
 • repeated aerobic workouts on the
    same day significantly changed
    nocturnal hGH
Endurance Exercise

• If the aim is to optimize hGH secretion,
  training should occur a number of times
  per day with each session being a
  duration greater than 10 minutes at an
  intensity above the lactate threshold.
Endurance Exercise

• Chronic exercise training blunts hGH
 • increase sensitivity to hGH similar to

• Higher rates of morbidity and mortality
• No or small increase in strength or
• Increase in nitrogen retention and
  muscle growth
Does Exogenous Growth Hormone Improve Athletic Performance?
Thematic Articles
Clinical Journal of Sport Medicine. Thematic Issue: Drugs and
Performance-Enhancing Agents in Sport. 12(4):250-253, July 2002.
Dean, Heather MD

Objective: To conduct a critical appraisal of the literature to address the
question of whether human growth hormone (HGH) improves
performance in trained athletes.
Data Sources: Used PubMed using the search terms of "growth hormone
athletes" and the reference lists of previous reviews of the subject.
Study Selection: Randomized double-blind placebo-controlled study of
exogenous HGH on muscle power in trained athletes. Only one study
matched the search criteria.
Conclusion: There is no evidence of increased muscle strength with HGH
in trained athletes.
        Growth Hormone
• Theory: Increase muscle mass, fat metabolism, and bone

• Research: Increases lean body mass in adults and young men
 but not strength nor performance

• Risks: arthralgia (joint pain), arthritis, cardiomegaly, muscle
 weakness, hyperlipidemia, impaired glucose regulation,
 diabetes, and possibly others.

• No accurate testing method

• Amphetamines
• Ephedrine
• Ma haung
• Guarana
• Increase release of
  norepinephrine through the
  sympathetic nervous
• Dosage
 • 15-50 mg
 • 1.5 to 2 hours to reach
    peak levels (30 minutes if

•   Research
    • Weight Loss (appetite suppressant)
    • Decrease fatigue
    • Increase power, speed, strength, torque
    • Increase time to exhaustion.
 • Injuries due to decrease awareness of fatigue and/or
 • Acute Mild: Anxiety, insomnia, headache, restlessness,
  dizziness, palpitations, nausea, etc.
 • Acute Severe: Arrhythmias, angina, MI, hypertension,
  cerebral hemorrhage, vasoconstriction in arterioles to
 • Chronic: paranoid, psychosis, addiction, neuropathy, etc
 • Very addictive

• Steve Bechler
• Korey Stringer
Details of Stringer's death revealed in deposition
By Renee Ruble, The Associated Press
MINNEAPOLIS — Korey Stringer didn't appear to be
suffering from heat-related illness until he lost
consciousness after leaving practice, the Minnesota
Vikings' trainers told attorneys in the wrongful death
suit brought by Stringer's widow.
The offensive tackle died of heatstroke Aug. 1 after
collapsing on the second day of the team's Persian
training camp in Manatee. His body temperature was
108.8 degrees when he arrived at a hospital 15 hours
before his death.
Deadly combinations
Autopsy cites ephedrine, liver problem, hypertension
Steve Bechler died Monday, February 17, 2003 less than 24 hours after a spring training
workout sent his temperature to 108 degrees. Preliminary autopsy findings indicated he
died from complications of heatstroke that caused multi-organ failure, Perper said.
Only toxicology tests can confirm whether there was ephedrine in Bechler's system, and those
results won't be available for at least two weeks, Perper said.
Among other factors cited by Perper as contributing to the 23-year-old pitcher's death:
•a history of borderline high blood pressure;
•liver abnormalities detected two years ago but not diagnosed;
•warm, humid weather during the workout when he became ill Sunday;
•he was on a diet and hadn't eaten much solid food the previous two days.
Ephedrine has been banned by the NCAA, the NFL and the International Olympic Committee, but
not by major league baseball.
• A sympathomimetic drug; a CNS stimulant
 • Bronchodilator through beta-2 receptors in
   the lungs
 • Stimulates beta-1 receptors in the heart
   causing increase in heart rate and blood
• Ma huang, ephedra sinica, Sida cordifolia
  contain ephedrine
• Theory
 • Appetite suppressant
 • Decrease fatigue
 • Increase alertness
• Technique
 • A typical dose is 20 mg per serving, and the
   usual frequency is 2 to 3 times per day.
 • Sometimes stacked with aspirin and

 • The few studies that examined ephedrine as an ergogenic aid have not
  found significant benefits, and serious adverse events have resulted
  from taking ephedrine prior to strenuous exercise.

 • Increase heat production and body temperature
 • Dizziness, headache, GI distress, arrhythmias, seizures, psychosis
 • Risks can be increase when combined with other substances
 • Ephedrine is banned by the International Olympic Committee (IOC)
  and the National Collegiate Athletic Association (NCAA) and NFL.
• New England Journal of Medicine,
  December 2000
  •   Hypertension
  •   Heart palpitations or heart rate
  •   Stroke
  •   Seizures

• Ten events resulted in death and 13
  produced permanent disability.
• Less serious adverse events reported
  in the literature include dizziness,
  headache, and gastrointestinal
• Also, several episodes of psychosis
  with ephedrine use have been
     Electrocardiographic and Hemodynamic Effects of a Multicomponent Dietary
   Supplement Containing Ephedra and Caffeine JAMA. 2004;291:216-221.

Context Metabolife 356, a multicomponent dietary supplement containing ephedra and
caffeine (DSEC) in addition to several other components, is the top-selling dietary weight loss
supplement. Given its common use, anecdotal reports of cardiovascular and cerebrovascular
adverse events, and paucity of safety data, further research with this DSEC was warranted.
Results Individuals receiving the DSEC had a longer maximal QTc interval (mean [SD], 419.4
[11.8] vs 396.1 [15.7] milliseconds; P<.001) and higher SBP (mean [SD], 123.5 [10.98] vs
118.93 [9.62] mm Hg; P = .009) compared with placebo. Participants who received the DSEC
were more likely to experience a QTc interval increase of at least 30 milliseconds vs placebo (8
individuals [53.3%] vs 1 individual [6.7%]; relative risk, 2.67 [95% confidence interval, 1.40-
5.10]). There were no significant sex-related differences.
Conclusions The ephedra- and caffeine-containing dietary supplement Metabolife 356
increased the mean maximal QTc interval and SBP. Since the actual ingredient or ingredients in
Metabolife 356 responsible for these findings are not known, patients should be instructed to
avoid this and similar dietary supplements until more information is known about their safety.
Caffeine and other sympathomimetic stimulants: modes of action and effects on sports performance.
Jones G
Essays in biochemistry (Essays Biochem) 2008; 44: 109-24

Stimulants, illegal and legal, continue to be used in competitive sport. The evidence for the ergogenic
properties of the most potent stimulants, amphetamines, cocaine and ephedrine, is mostly insubstantial. Low
doses of amphetamines may aid performance where effects of fatigue adversely affect higher psychomotor
activity. Pseudoephedrine, at high doses, has been suggested to improve high intensity and
endurance exercise but phenylpropanolamine has not been proven to be ergogenic. Only caffeine has
substantial experimental backing for being ergogenic in exercise. The mode of action of these stimulants
centres on their ability to cause persistence of catecholamine neurotransmitters, with the exception
of caffeine which is an adenosine receptor antagonist. By these actions, the stimulants are able to
influence the activity of neuronal control pathways in the central (and peripheral) nervous system. Rodent
models suggest that amphetamines and cocaine interact with different pathways to that affected by caffeine.
Caffeine has a variety of pharmacological effects but its affinity for adenosine receptors is comparable with
the levels expected to exist in the body after moderate caffeine intake, thus making adenosine receptor
blockade the favoured mode of ergogenic action. However, alternative modes of action to account for the
ergogenic properties of caffeine have been supported in the literature. Biochemical mechanisms that are
consistent with more recent research findings, involving proteins such as DARPP-32 (dopamine and cAMP-
regulated phosphoprotein), are helping to rationalize the molecular details of stimulant action in the central
nervous system.
•   Caffeine is also called guaranine when found in guarana, mateine
    when found in mate, and theine when found in tea; all of these names
    are synonyms for the same chemical compound.
•   Caffeine is a adenosine antagonist. Adenosine has an inhibitory
    effect in the central nervous system (CNS). Caffeine's
    stimulatory effects, on the other hand, are primarily (although not
    entirely) credited to its inhibition of adenosine by binding to the
    same receptors, and therefore effectively blocking adenosine
    receptors in the CNS. This reduction in adenosine activity leads
    to increased activity of the neurotransmitters dopamine and

•   Caffeine is also a known competitive inhibitor of the enzyme
    cAMP-phosphodiesterase (cAMP-PDE), which converts cyclic
    AMP (cAMP) in cells to its noncyclic form, allowing cAMP to
    build up in cells. Cyclic AMP participates in activation of Protein
    Kinase A (PKA) to begin the phosphorylation of specific
    enzymes used in glucose synthesis. By blocking its removal
    caffeine intensifies and prolongs the effects of epinephrine and
    epinephrine-like drugs such as amphetamine,
    methamphetamine, or methylphenidate.
• Can have positive
  effects on
• Speed and power
  from 1 to 120
• Shorter sprints?

• Muscle endurance but not strength
• Similar effects for men and women
• Similar effects for novice and habitual
• Fatty acid mobilization?
• Does not lead to dehydration
• Diuretic factor
 • Caffeinated diet-cola retains 50-60%
 • Water = 60-70%
 • Sport drink = 65-75%
Caffeine and Ephedrine: Physiological, Metabolic and Performance-Enhancing Effects.
Magkos, Faidon; Kavouras, Stavros A
Sports Medicine. 34(13):871-889, 2004.

Preparations containing caffeine and ephedrine have become increasingly popular among sportspersons in recent years as a
means to enhance athletic performance. This is due to a slowly accumulating body of evidence suggesting that combination of
the two drugs may be more efficacious than each one alone. Caffeine is a compound with documented ergogenicity in various
exercise modalities, while ephedrine and related alkaloids have not been shown, as yet, to result in any significant performance
improvements. Caffeine-ephedrine mixtures, however, have been reported in several instances to confer a greater
ergogenic benefit than either drug by itself. Although data are limited and heterogeneous in nature to allow for reaching
consensus, the increase in performance is a rather uniform finding as it has been observed during submaximal steady-
state aerobic exercise, short- and long-distance running, maximal and supramaximal anaerobic cycling, as well as
weight lifting. From the metabolic point of view, combined ingestion of caffeine and ephedrine has been observed to increase
blood glucose and lactate concentrations during exercise, wheareas qualitatively similar effects on lipid fuels (free fatty acids and
glycerol) are less pronounced. In parallel, epinephrine and dopamine concentrations are significantly increased, wheareas the
effects on norepinephrine are less clear.

With respect to pulmonary gas exchange during short-term intense exercise, no physiologically significant effects have been
reported following ingestion of caffeine, ephedrine or their combination. Yet, during longer and/or more demanding efforts, some
sporadic enhancements have indeed been shown. On the other hand, a relatively consistent cardiovascular manifestation of the
latter preparation is an increase in heart rate, in addition to that caused by exercise alone. Finally, evidence to date strongly
suggests that caffeine and ephedrine combined are quite effective in decreasing the rating of perceived exertion and
this seems to be independent of the type of activity being performed. In general, our knowledge and understanding of the
physiological, metabolic and performance-enhancing effects of caffeine-ephedrine mixtures are still in their infancy. Research in
this field is probably hampered by sound ethical concerns that preclude administration of potentially hazardous substances to
human volunteers. In contrast, while it is certainly true that caffeine and especially ephedrine have been associated with several
acute adverse effects on health, athletes do not seem to be concerned with these, as long as they perceive that their
performance will improve. In light of the fact that caffeine and ephedra alkaloids, but not ephedrine itself, have been removed
from the list of banned substances, their use in sports can be expected to rise considerably in the foreseeable future. Caffeine-
ephedra mixtures may thus become one of most popular ergogenic aids in the years to come and while they may indeed prove to
be one of the most effective ones, and probably one of the few legal ones, whether they also turn out to be one of the most
dangerous ones awaits to be witnessed.
Blood Doping

• Theory:
 • EPO is a natural hormone that stimulates
   bone marrow to increase red blood cells

• Technique
 • Cost ~$60/dose. Need 5-6 doses.
 • Ht increases for 5-10 days

• And increase of 1 g/dL of hemoglobin
  can increase VO2max by 8%
• EPO treatment might result in increase
  glycogen and free fatty acid levels
Blood Doping / EPO
• General Findings
 • Hg increase: 7%
 • Ht increase: 6-11%
 • VO2max increase: 5-7%
 • Time to exhaustion: 34%
Blood Doping / EPO

• Death (stroke, MI, or pulmonary
 • 1987: First year of EPO, 5 Dutch
    cyclist died
 • 1997-200: 18 deaths
Blood Doping / EPO
Blood Doping

• Easy to use, hard to detect.
• A blood test, using markers of accelerated erythropoiesis
  (e.g., red cell size, reticulocyte count, soluble transferrin
• The blood test is just a profile, however, and can only
  suggest Epo use, not prove it (Cazzola, 2000).

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