EPHEDRINE
Dr Henny Rachdiati
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
•Methamphetamines
•Epinephrine (adrenaline)
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-methyl
amino propiophenone.
• 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 •If taken in pure form,
Ephedrine is commonly
containing ephedrine also combined with a cup of
contain caffeine and aspirin- coffee and an aspirin
like ingredients
• Pure ephedrine has shown to
be less effective when taken
alone
C-AMP
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
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 •Athletic deaths linked
had over 800 reported to ephedrine result from
rise in body temperature
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
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
