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Ephedrine
History
• Also known as Ma-
Huang
• Ephedra has been used
as medicine for over
60,000 years
• Used in Chinese
medicine for more than
5,000 years
• Originally prescribed to
treat asthma,
congestion and
allergies
Ephedra equisetina
• Ephedrine is a naturally
occurring central nervous
system stimulant obtained
from the plant Ephedra
equisetina
• The stem of the ephedra plant
contains 1-2% of alkaloids
that contain up to 90 percent
of ephedrine
• Found in the United States
and sections of Asia
Chemical Structure
• Chemical Formula:
C10H15NO
• Molecular Weight:
165.23 grams/mole
• Melting Point: 37-39°C
• Boiling Point: 253-255°C
Similar Alkaloid Structures
•Epinephrine (adrenaline)
•Methamphetamines
Other Related Alkaloids
•Caffeine - Increases alertness and perception
•Pseudoephedrine – A nasal decongestant. has less effect on
the heart and blood pressure
•Phenylpropanolamine - Another nasal decongestant. Constricts
blood vessels, increases blood pressure and is an appetite
suppressant.
•Amphetamines - Pump adrenaline into the body, stimulate the
CNS causing blood pressure to increase, suppress appetite,
dilate pupils, and cause hallucination
Chemical Synthesis
• In 1911, scientists obtained
racemic ephedrine and
pseudoephedrine by
hydrogenation of alpha-
methylaminopropiophenone.
• In its pure form, ephedrine is
marketed as a salt, ephedrine
sulfate
•White crystalline powder with a
bitter taste, soluble in water and
very soluble in alcohol
Medicines
Many medicines include
Ephedrine as an active
ingredient to aid in
alertness and asthma
relief
“Herbal XTC”
• Ephedrine often
used as a drug at
raves
• Acts as a mild
alternative to speed
• Heightens mood
and causes a
“tingling sensation”
all over the scalp
and body
Use in Weight Loss
1. Increases fat loss.
2. Maintains muscle
mass.
3. Prevents the fall of
HDL cholesterol during
weight loss.
4. Increases insulin
sensitivity.
5. Reduces lipogenesis
(the conversion of
carbohydrates to fat).
Use in Bodybuilding
• Increases metabolism,
leading the body to
more efficient fat and
sugar burning
• Helps maintain muscle-
mass while decreasing
fat
• Used in supplements
such as Ripped Fuel,
Hydroxycut, Xenadrine,
etc.
Supplements
• Many weight
loss and
bodybuilding
supplements
contain
ephedrine
Supplement Composition
• Fat burning
supplements
containing
ephedrine also
contain caffeine and
aspirin-like
ingredients
• Pure ephedrine has
shown to be less
effective when taken
alone
•If taken in pure form,
Ephedrine is commonly
combined with a cup of
coffee and an aspirin
Supplement Chemistry
• On the surface of fat and muscle cells there are b-receptors
• B-receptors bind with b-agonists (adrenaline) causing
chemical reactions that produce the chemical messenger C-
AMP
• C-AMP activates enzymes which induce lipolysis (fat
breakdown) in fat cells and increase metabolism in muscle
cells.
• In supplements containing the ephedrine-caffeine-aspirin
mix, ephedrine enhances b-agonist production. Caffeine
inhibits the breakdown of C-AMP. Aspirin inhibits the
reduction of b-agonist production.
Fat cells
Muscle cells
C-AMP
Benefits of Modern Ephedrine Use
• Helps to retain muscle
during weight loss
• Maintains levels of HDL
cholesterol
• May reduce the risk of
cardiovascular disease
• No signs of long term
toxicity
• May increase life
expectancy in women
Side Effects
• Abnormally high blood
pressure
• Rapid, irregular
heartbeat
• Anxiety
• Dizziness
• Insomnia
• Tremor
• Rapid pulse
• Sweating
• Respiratory difficulties
• Confusion
• Hallucinations
• Delirium
• Convulsions.
Individual Cases
• The New England Journal
of medicine links at least
54 deaths to ephedrine
• Since 1994 the FDA has
had over 800 reported
cases of side effects from
ephedrine. 273 resulted in
death
• Death of NFL player Korey
Stringer tied to ephedrine
use.
• Numerous college athlete
deaths also linked
•Athletic deaths linked
to ephedrine result from
rise in body temperature
Proposed FDA Guidelines
• 1. Product potency would be limited to less than 8 mg of
ephedrine alkaloids per serving, and daily intake would be
limited to less than 24 mg.
• 2. The product label would be required to include the statement
"Do not use this product for more than 7 days."
• 3. The combination of ma huang with other stimulants, including
caffeine, would be prohibited.
• 4. Labeling claims such as weight loss and body building that
encourage long-term use would be prohibited.
5. For products with claims for short-term effects such as
increased energy, the product label must include the warning:
"Taking more than the recommended serving may result in heart
attack, stroke, seizure or death."
Regulations
• Banned by the Olympic
Committee, NFL &
NCAA
• Pending decision in
several states, illegal in
Nevada
• Banned in sanctioned
powerlifting events
• FDA unsuccessfully
tried to ban ephedrine in
1997
Conclusion
• Ephedrine should be
used intelligently
and with caution
• Consult a doctor
before starting
supplementation

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Ephedrine A NATURAL DRUG FOR CENTRAL NERVOUS SYTEM

  • 2. History • Also known as Ma- Huang • Ephedra has been used as medicine for over 60,000 years • Used in Chinese medicine for more than 5,000 years • Originally prescribed to treat asthma, congestion and allergies
  • 3. Ephedra equisetina • Ephedrine is a naturally occurring central nervous system stimulant obtained from the plant Ephedra equisetina • The stem of the ephedra plant contains 1-2% of alkaloids that contain up to 90 percent of ephedrine • Found in the United States and sections of Asia
  • 4. Chemical Structure • Chemical Formula: C10H15NO • Molecular Weight: 165.23 grams/mole • Melting Point: 37-39°C • Boiling Point: 253-255°C
  • 5. Similar Alkaloid Structures •Epinephrine (adrenaline) •Methamphetamines
  • 6. Other Related Alkaloids •Caffeine - Increases alertness and perception •Pseudoephedrine – A nasal decongestant. has less effect on the heart and blood pressure •Phenylpropanolamine - Another nasal decongestant. Constricts blood vessels, increases blood pressure and is an appetite suppressant. •Amphetamines - Pump adrenaline into the body, stimulate the CNS causing blood pressure to increase, suppress appetite, dilate pupils, and cause hallucination
  • 7. Chemical Synthesis • In 1911, scientists obtained racemic ephedrine and pseudoephedrine by hydrogenation of alpha- methylaminopropiophenone. • In its pure form, ephedrine is marketed as a salt, ephedrine sulfate •White crystalline powder with a bitter taste, soluble in water and very soluble in alcohol
  • 8. Medicines Many medicines include Ephedrine as an active ingredient to aid in alertness and asthma relief
  • 9. “Herbal XTC” • Ephedrine often used as a drug at raves • Acts as a mild alternative to speed • Heightens mood and causes a “tingling sensation” all over the scalp and body
  • 10. Use in Weight Loss 1. Increases fat loss. 2. Maintains muscle mass. 3. Prevents the fall of HDL cholesterol during weight loss. 4. Increases insulin sensitivity. 5. Reduces lipogenesis (the conversion of carbohydrates to fat).
  • 11. Use in Bodybuilding • Increases metabolism, leading the body to more efficient fat and sugar burning • Helps maintain muscle- mass while decreasing fat • Used in supplements such as Ripped Fuel, Hydroxycut, Xenadrine, etc.
  • 12. Supplements • Many weight loss and bodybuilding supplements contain ephedrine
  • 13. Supplement Composition • Fat burning supplements containing ephedrine also contain caffeine and aspirin-like ingredients • Pure ephedrine has shown to be less effective when taken alone •If taken in pure form, Ephedrine is commonly combined with a cup of coffee and an aspirin
  • 14. Supplement Chemistry • On the surface of fat and muscle cells there are b-receptors • B-receptors bind with b-agonists (adrenaline) causing chemical reactions that produce the chemical messenger C- AMP • C-AMP activates enzymes which induce lipolysis (fat breakdown) in fat cells and increase metabolism in muscle cells. • In supplements containing the ephedrine-caffeine-aspirin mix, ephedrine enhances b-agonist production. Caffeine inhibits the breakdown of C-AMP. Aspirin inhibits the reduction of b-agonist production. Fat cells Muscle cells C-AMP
  • 15. Benefits of Modern Ephedrine Use • Helps to retain muscle during weight loss • Maintains levels of HDL cholesterol • May reduce the risk of cardiovascular disease • No signs of long term toxicity • May increase life expectancy in women
  • 16. Side Effects • Abnormally high blood pressure • Rapid, irregular heartbeat • Anxiety • Dizziness • Insomnia • Tremor • Rapid pulse • Sweating • Respiratory difficulties • Confusion • Hallucinations • Delirium • Convulsions.
  • 17. Individual Cases • The New England Journal of medicine links at least 54 deaths to ephedrine • Since 1994 the FDA has had over 800 reported cases of side effects from ephedrine. 273 resulted in death • Death of NFL player Korey Stringer tied to ephedrine use. • Numerous college athlete deaths also linked •Athletic deaths linked to ephedrine result from rise in body temperature
  • 18. Proposed FDA Guidelines • 1. Product potency would be limited to less than 8 mg of ephedrine alkaloids per serving, and daily intake would be limited to less than 24 mg. • 2. The product label would be required to include the statement "Do not use this product for more than 7 days." • 3. The combination of ma huang with other stimulants, including caffeine, would be prohibited. • 4. Labeling claims such as weight loss and body building that encourage long-term use would be prohibited. 5. For products with claims for short-term effects such as increased energy, the product label must include the warning: "Taking more than the recommended serving may result in heart attack, stroke, seizure or death."
  • 19. Regulations • Banned by the Olympic Committee, NFL & NCAA • Pending decision in several states, illegal in Nevada • Banned in sanctioned powerlifting events • FDA unsuccessfully tried to ban ephedrine in 1997
  • 20. Conclusion • Ephedrine should be used intelligently and with caution • Consult a doctor before starting supplementation