Amended Bitter Orange - Ephedra in disguise ?
By: Jenny Mathers

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.

About the Author

Research resource for fat burning foods and supplements. Fat burning food research information allowing you to take the guess work out of fat burning.

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