Amended Bitter Orange – Ephedra in disguise ?

If you read my last article about bitter orange or citrus
aurantium, it was pretty clear how I felt about the herb. I’d
read the available research concerning bitter orange, and while
there was some evidence supporting bitter orange, the overall
picture did not look good.

So that’s the picture I painted, however, there were some facts
that I was unaware of at the time, which I felt you might be
interested in if you’re researching bitter orange.

In order to lay these out, I want to answer four questions:

1. What Is Bitter Orange (Citrus Aurantium) Really ? 2. So does
Bitter Orange act similarly to ephedrine ? 3. What about the
reports of adverse ill effects of bitter orange ? 4. Is bitter
orange safe to use and does it work ?

It’s a bit long, but what the heck !

What Is Bitter Orange Really ?:

The Bitter Orange extract found in popular fat burners, is made
from the unripe fruit of the citrus aurantium tree. The fruit is
picked when they are a dark green in color, halved, dried and
then milled into a powder. This makes the herb Zhi Shi[1].
Bitter orange is the western name for Zhi Shi.

The bitter orange herb contains five alkaloids (see alkaloid
definition[5]), the most dominant of which is Synephrine (the
compound I referred to in my last article), structurally similar
to ephedrine. However, while they are similar, they’re not the
same.

Chemically, both synephrine and ephedrine stimulate the
sympathetic nervous system and at a cellular level, affect
classes of cells called alpha cells, and to a lesser extent,
beta cells[6]. Alpha and beta cells can then be divided into
classes of beta and alpha cells. Beta(1) and beta(2) cell
receptors are believed to be responsible for cardiac and
pulmonary functions. Beta(3) cell receptors are believed to be
responsible for fat burning or thermogenesis. Ephedrine will
affect beta(1), beta(2) and beta(3) cell receptors, however, of
the beta-cell receptors, synephrine appears to only affect
beta(3) cells.[7].

So does Bitter Orange act similarly to ephedrine ?

Does it ? While previously, I’ve presented a very black and
white view of whether it acts similarly to ephedrine, I am now
not so sure.

Generally speaking because synephrine stimulates beta(3) cells
but not beta(2) and beta(1) cells, it can provide the
thermogenic effects without the undesirable cardiac side effects
that ephedrine did.

What about the reports of adverse ill effects of bitter orange ?

The American Herbal Products Association has found that there
were errors by the FDA in the reported adverse event reports
attributed to the use of bitter orange in September 2004[3]. The
association found that numbers reported in the media were in
fact duplicates for adverse event reports for ephedrine, and
when all was said and done, there was really only one report of
an adverse reaction attributed to a bitter orange supplement,
where no other ingredient was included in the supplement. In
this particular case, it involved a 74 year old woman who had
been taking prescription medication and two other herbal
preparations simultaneously. This one case occurred more than
five years ago[3].

What about the 55 year old woman reported by Nykamp DL, Fackih
MN, Compton AL (2004), who experienced chest pain after
consuming a supplement containing bitter orange. Researchers in
this case study had commented “Based on the Naranjo probability
scale, C. aurantium is possibly associated with this
cardiovascular event”[4], however, as bitter orange was not the
only ingredient in the supplement, it cannot be known whether in
this case, that bitter orange was the herb responsible.

Is bitter orange safe to use and does it work ?

Now there are many others, who felt as I did, that bitter orange
is another Ephedra waiting to happen, and will have the same
consequences. However, when bitter orange is taken in isolation,
it does not have adverse side effects.

In fact, when it is combined with other selected herbs, it may
have benefits for health and weight loss. Research performed
with 20 individuals over six weeks found no adverse reactions
occurred when citrus aurantium was combined with caffeine and
St. Johns Wort[2]. They also found that the individuals who were
given the supplement (group A) lost an average of 2.9% body fat.
“In terms of actual fat loss, group A lost a significant amount
(3.1 kg), whereas the control group demonstrated a tendency
toward fat loss.” So, this study has demonstrated that there are
weight loss benefits involved here, but also the control group
who received nothing exhibited a tendency towards fat loss,
suggesting that if the study had been extended beyond 6 weeks,
the control group would have lost body fat as well.

Conclusions:

2004 was not a great year for bitter orange in the media. The
extract has successfully battled reports of adverse events
alleged to be a result of consuming bitter orange or citrus
aurantium. These numbers proved to be incorrect.

While synephrine the main alkaloid of bitter orange or citrus
aurantium extract, is chemically similar to ephedrine, it is not
the same as ephedrine and differs in the way it reacts
pharmacologically within the human body.

Although at first look at the research, bitter orange or citrus
aurantium presented with dangers that I wanted to warn against,
a more in-depth look has revealed that bitter orange by itself
is not dangerous. The citrus aurantium extract standardized for
synephrine (3-6%) is accepted as safe[7].

But hang on, before you click off this page, to go and find a
fat burner with citrus aurantium in it, I do also want to say,
that they can’t be used as an alternative to good food and
exercise.

Herbal supplements such as those containing bitter orange can be
helpful but only when used within a weight loss strategy of
balanced eating and exercise, and while they may benefit some,
it may not benefit others and only your doctor will be able to
make that decision for you[6]. The results may be slower, but a
balanced diet and exercise are the keys to permanent and healthy
weight loss. So while bitter orange may be helpful, you can
obtain the same results without it. What-ever stage you are at
with your health and fitness, diet and exercise are the two most
important aspects.

If you do decide you’d like to try a supplement containing
bitter orange, please consult your doctor before purchasing a
bitter orange or citrus aurantium product.

Essentially if you consult your doctor about bitter orange, as
we say in Australia – you can’t go wrong, mate. Your doctor will
be able to refer you to your nearest dietician and will
recommend the best weight loss strategy for your situation.

References:

[1]Jones, D., “Bitter Orange or Citrus Aurantium: same
difference ?”

[2]Colker et. al., (1999) Effects of Citrus Aurantium extract,
caffeine, and St. John’s Wort on body fat loss, lipid levels,
and mood states in overweight healthy adults. Curr. Ther. Res.
60, 145 – 153.

[3]American Herbal
Products (2004) “FDA Spins Numbers on Bitter Orange AERs” Press
Release

[4]Nykamp DL, Fackih MN, Compton AL. Possible association of
acute lateral-wall myocardial infarction and bitter orange
supplement. Ann Pharmacother. 2004 May;38(5):812-6. Epub 2004
Mar 16.

[5]Definition
of Alkaloids – any of hundreds of compounds found in plants
with a nitrogen atom connected to two carbon atoms, and often
formed in a ring structure. Many commonly known chemicals and
drugs are alkaloids, including nicotine, cocaine, quinine,
morphine, and ephedrine.

[6]Dharmananda, S., SYNEPHRINE:Is
Chih-shih (Zhishi) Toxic? Institute for Traditional
Medicine, Portland, Oregon. See the schematic diagram for
synephrine at the bottom of the page.

[7]Supplement Watch on Synephrine

Other Sites of Interest:

Supplement
Watch Newsletter

Copyright © 2004 Jenny Mathers All Rights Reserved. This article
represents the opinion of the author only. This information is
for educational purposes only and should not be taken as a
replacement for medical advise. Please see your doctor before
changing your diet, or trying a new supplement.

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