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It is able
to induce fat loss via increasing the amount of fat available for fuel as well as
by increasing heat expenditure. It has been implicated in increasing the
metabolic rate by up to 5% in humans. It has also been noted to cause
serious side-effects in some instances, and its legal status varies by region.
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Ephedrine is highly synergistic with Caffeine, and for this reason is commonly
found in something called an ECA stack (Ephedrine, Caffeine, and Aspirin).
Side effects include an increase in Blood Pressure that goes away with
cessation and increases in some blood parameters (Glucosamine, Insulin)
that also go away with cessation of use. It has been reported to be a
hyperstimulant when taken in doses above what is recommended.
Ephedrine is well studied and a fairly reliable compound for short- to mediumterm weight loss (less than 6 months) and mild performance improvements,
usually in trained individuals. However, it does not work under all situations;
longer-term weight loss and effects in untrained individuals have not been
studied much and sometimes produce negative results. While it has been
implicated in weight reduction independent of exercise and diet changes,
efficacy is maximized with minimal side-effects when ephedrine is combined
with diet and exercise.
Things to Know
Also Known As
Ephedrone, Epinephrine
Things to Note
Is a Form Of
Fat-Burner
Caution Notice
Ephedrine can also increase dopamine levels in the brain, and caution should
be taken pairing ephedrine with MAOIs such as Yohimbine.
LEVEL OF EVIDENCE
B
Multiple studies where at least two are double-blind and placebo
controlled
C
LEVEL OF EVIDENCE
EFFECT
CHANGE
COMMENTS
Fat Mass
Notable
100%
See all 4 studies
It is thought that most weight lost with ephedrine administration is due to fat
mass, due to a slight muscle preserving effect; studies that note reductions in
fat mass
... show
Metabolic Rate
Notable
100%
See all 6 studies
Ephedrine, secondary to the stimulatory properties, appears to reliably
increased metabolic rate
Weight
Notable
77%
See all 10 studies
Ephedrine tends to result in reliable weight loss over time relative to control
(assuming calories are held equal), which is mostly due to a loss of body fat
Blood Pressure
Minor
25%
See all 5 studies
There may be an acute increase in blood pressure seen with ephedrine
intake, although this does not appear to be overly reliable; long-term usage
of ephedrine does not
... show
Heart Rate
Minor
50%
See all 5 studies
An increase in heart rate is present following ephedrine administration which
correlates well with its psychostimulatory properties; this is not 100%
reliable, and heart ... show
Nasal Congestion
Notable
100%
See 2 studies
Ephedrine appears to result in notable nasal decongestion
Minor
HDL-C
100%
See 2 studies
An increase in HDL-C has been noted with ingestion of ephedrine, may be
confounded with weight loss also seen in the trials
LDL-C
Minor
100%
See study
A decrease in LDL-C has been noted to be associated with ephedrine,
although this may be confounded with weight loss (also seen in the trials)
Minor
100%
See study
May decrease the rate of skeletal muscle breakdown over time
Subjective Well-Being
Minor
100%
See study
Appears to increase well being acutely following the first doses of ephedrine,
secondary to the psychostimulatory effects
Triglycerides
Minor
100%
See 2 studies
There appears to be a decrease in triglycerides over time with ephedrine
ingestion, which may be due to either the fat burning effects of ephedrine or
the weight loss that
... show
Power Output
100%
See study
No significant influence on power output with standard oral doses of
ephedrine (higher doses may influence power output, but this is not well
researched)
Appetite
Minor
100%
See study
A decrease in appetite following ephedrine intake is noted and thought to be
secondary to its psychostimulatory effects
Nausea
0%
See study
Ephedrine has been noted to reduce postoperative nausea, but is also linked
to inducing nausea secondary to its psychostimulatory and appetite
suppressing effects. The ... show
Scientific Research
Table of Contents:
1.3. Properties
2. Pharmacology
2.2. Systemic
Ephedrine is able to act with the muscle cells directly and induce
thermogenesis in myocytes. It has also been reported that urinary excretion
of nitrogen is reduced during ephedrine supplementation, indicating that this
interaction or a like interaction exerts a muscle sparing effect.
Supplementation with ephedrine increases plasma insulin, glucose, and Cpeptide in a dose dependent manner, possibly due to the state of transient
insulin resistant classical stimulants induce.
3. Neurology
3.1. Sensitivity
4.1. Mechanisms
This agonism may not appear to be seen in vivo at doses of 50mg taken
thrice daily.[30]
It has been shown to increase only the beta-3 subunit in white adipose tissue
in rats, but enhances glycerol release from brown adipose tissue and inhibits
glucose uptake for both types of adipocyte.[31]
Human studies have found that oxygen consumption via an initial ephedrine
dose (20mg) increases an expected amount 30-60 minutes after ingestion in
all cases (with more potency in those not adapted to stimulants), although
chronic ingestion of ephedrine alleviates the expected drop between 1-3
hours post ingestion. This suggests that ephedrine confers more benefits to
fat burning with usage over a longer period (4-12 weeks) rather than
intermittently, and the suspected mechanism is augmentation of betaadrenergic sensitization.[32]
Ephedrine seems to, in and of itself, increase metabolic rate via REE
independent of exercise; this is dissimilar to Caffeine, which requires exercise
to induce it's fat-burning effects to significant levels. Coincidentally, this may
be the reason why the combination of Ephedrine and Caffeine shows
synergism with exercise in increased oxygen consumption.[33] The
combination of ephedrine and caffeine has been noted to be similarly
effective (trending to be more effective) than 15mg dexfenfluramine over 12
weeks.[3]
It has been noted that caffeine ingestion does, however, increase ephedrine's
effects on REE independent of exercse[34] and that this effect on potentiating
was also noted with green tea, suggesting that the methylxanthine class of
compounds (via increasing adrenaline) are causative of the potentiation.[23]
The previous animal studies have noted a 10% increase in REE with
ephedrine supplementation, however human studies are more variable at
3.6%,[30] 10.7% (with caffeine),[7] and 7.1%.[35] Studies using indirect
calorimetry note various increases, such as 30.15.4kcal/3hours at 20mg
ephedrine + 200mg caffeine, and 22.77.7kcal/3hours at half the ephedrine
dosage.[24] It has also been noted to reduce a 13% reduction in REE (from
caloric restriction) into an 8% reduction, saving 5% of the metabolic rate.[6]
Some case studies have supported the idea that ephedrine (paired with
caffeine) can be of use to hypothalamic obesity with long-term success.[5]
Usage of the ECA stack has been investigated, and without intentional caloric
restriction in obese persons showed 2.2kg weight loss over 8 weeks against
0.7kg for placebo.[37] When unblinded, the 2.2kg loss increased to 3.2kg.
with 60mg ephedra sinicus (ephedrine content not disclosed) 60 and 150
minutes prior to muscular testing with a 1 rep max bench press and lat
pulldown test noted that despite increased attitude towards and alertness
during weight lifting that there was no significant differences in strength
when compared to 300mg glucose placebo.[41] Another trial assessing
muscular output with weight training with a higher dose of ephedrine
(0.8mg/kg 90 minutes before leg press:bench press supersets to failure)
noted 3 more reps on the leg press associated with ephedrine over placebo
(16 over 13) and when combining with caffeine this was increased to 6 reps
(19 versus 16) with less improvement (1 and 2 extra reps, respectively) with
the bench press; the authors noted that fatigue during supersets may have
played a role, and these results were only significant during the first superset
test (with a 2 minute rest period, the subsequent two tests were not
statistically significance).[42]
One study using a single acute dose of 24mg ephedrine in otherwise healthy
untrained men failed to note any power output enhancement after acute
dosing.[43]
6.1. Estrogen
7. Cardiovascular Interactions
Many of the human studies (to be discussed) noted slight increases in blood
pressure ranging from 5-23mmhg systolic with no influence on diastolic.[32]
[7] These effects were acute and causative of the ephedrine administration.
Over a long period of time (8-12 weeks) ephedrine is associated with reduced
blood pressure, although this is due to weight loss.[50][3] Sometimes blood
pressure is not significantly affected at all chronically, however.[51][52][53]
In regards to persons with hypertension who may still experience the acute
rise in blood pressure, treatment with ephedrine may be problematic acutely
but has been argued, over time, to be beneficial secondary to reduction in
weight.[50]
With a controlled dose of ephedrine, it does not seem to change heart rate in
and of itself. Variations in HR are typically causative of excessive adrenaline
levels when pairing ephedrine with an adrenaline increasing agent such as
Caffeine or from anxiety.
Ephedrine (thus study using caffeine) has been noted to reduce the rate of
HDL-C decreases seen with hypocaloric dieting without significantly affecting
overall total cholesterol.[4]
8. Nutrient-Nutrient Interactions
The ECA stack was first proposed in 1989[58] and tested in 1990[59] as
nutraceuticals that interacted with each other. It was already noted at this
time that xanthine compounds (of which Caffeine is included) can cause the
efficacy of 22mg ephedrine in increasing the metabolic rate to approximately
double[23] and in animals to more effectively suppress the appetite.[60][61]
[62]
Caffeine is able to increase metabolic rate on its own, but its combination
with ephedrine appears to be synergistic (greater than the sum of its parts)
rather than just additive. The pairing of the two results in an increased
metabolic rate greater than the two added together mathematically.[24] The
mechanism appears to be through adenosine antagonism, as the other
theory (phosphodiesterase inhibtion) may not be relevant in vivo due to low
cellular concentrations of caffeine relative to what is needed to cause large
inhibition.[63]
Caffeine has been noted as a synergist with ephedrine in vivo[24] and used
effectively in a wide variety of studies to induce weight loss in conjunction
with a diet or diet with exercise program.[64] and some studies suggest that
it is needed for the fat loss effects of ephedrine to differ from placebo.[38]
This may be secondary to 'non-responders' to ephedrine, which seems to be
negated by coingestion of a xanthine compound.[35] Basically, those who do
not respond to ephedrine seem to respond to ephedrine with xanthines.
The synergism between ephedrine and xanthines has been roughly quantified
as 64% more than the expected values of the added value of the two
compounds in one study.[24] This is more of a pharmacodynamic synergism,
as taking the combination of ingredients does not appear to alter the
pharmacokinetic profile of either.[26]
One study noted the combination of Caffeine and ephedrine did not influence
diastolic blood pressure while either compound in isolation did, and that the
combination did not influence systolic blood pressure to a greater degree
than either compound in isolation.[24] This indicates that the combination is,
at least, no worse than either in isolation in regards to acute blood pressure
spikes.
Although aspirin has been shown to cause greater reductions in body fat
when combined with ephedrine, it does not significantly affect body weight
on its own.[65] In animals, ephedrine decreased body fat percentage by 18%
while ephedrine combined with aspirin decreased body fat percentage by
27%.[65] works through prostaglandin inhibition, which increases ephedrineinduced adrenaline release.[66] Aspirin in combination with caffeine and
ephedrine has failed to acutely increase the thermic effect of food.[8]
8.2. Nicotine
Ephedrine and caffeine mixtures have been used in attempts to reduce the
weight gain seen with smoking cessation, and although benefit has been
noted ephedrine has failed to significantly modify quitting rates.[2]
At least one case of human heart damage has been reported in a 44 year old
male, but this was confounded with usage of a wide variety of compounds.
[74] Another case study noted usage of Ephedrea, Xenadrine, and Hydroxycut
for 2 years resulting in coronary artery aneurysm[75] which may be related to
the Xenadrine formulation without Ephedrine.[76][77]
One study notes ephedrine associated with kidney stones, but takes an overly
dramatic approach in the abstract.[78] Ephedrine alkaloids were found to
comprise 95% of a kidney stone by weight in a person on 4 medications with
a single kidney who suffered from kidney failure in the past. However,
contacts of the author noted "over 200" other cases of kidney stones
containing Ephedra Alkaloids. The supplement used by the case subject
contained 170mg Ephedra (6% ephedrine).[78]
Ephedrine has, at least once, been used to commit suicide. The exact oral
dose was unknown, but was well beyond the highest recommended
therapeutic dosages.[78]
9.3. Legality
In 2004 the United States Food and Drug Administration (FDA) issued a ruling
prohibiting the sale of dietary supplements containing ephedra, citing an
unreasonable risk of illness or injury.[80] In addition to the FDA ban on sales,
laws governing the sale, use, and possession of ephedra products have been
established at the state and local level. If you are considering the use of
ephedra, be sure to check first whether doing so complies with all
national/local laws in your region.
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The effect and safety of an ephedrine/caffeine compound
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Acute hemorrhagic myocardial necrosis and sudden death
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SUMMARY
THINGS TO KNOW
HOW TO TAKE
FAQ
HUMAN EFFECT MATRIX
SCIENTIFIC RESEARCH
CITATIONS
Quickly:
Ephedrine is one of the four active components of the herb Ephedra. It is able
to induce fat loss via increasing the amount of fat available for fuel as well as
by increasing heat expenditure. It has been implicated in increasing the
metabolic rate by up to 5% in humans. It has also been noted to cause
serious side-effects in some instances, and its legal status varies by region.
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