Synephrine: A Natural Alternative
to Ephedrine
By
Richard Alan Miller, c2001
Updated 05-28-03
IntroductionSynephrine is an adrenergic amine that enhances the metabolic rate, increases fat burning and spares muscle protein. Derived from Citrus aurantium, it is a natural alternative to ephedrine, providing maximum weight-loss results without the side effects of Ephedra. Synephrine binds with the Beta 3 cell receptors to increase the rate at which fat is released from body stores (lipolysis), along with increasing the metabolic rate. It offers all of the advantages of a stimulant, without the drawbacks. Weight loss clinics throughout the USA are now reporting improved rates of weight loss while using Synephrine without the side effects of ephedrine. Clients have reported up to a 42% reduction in total body fat after using Synephrine.
More and more physicians are beginning to view excess weight as a metabolic problem. This is evident by the widespread use of the new appetite- suppressant medications, which increase metabolism by stimulating the central nervous system. While increasing metabolism is desirable, chronic excitation of the nervous system can lead to significant problems, from high blood pressure to insomnia.
However, by seeing metabolism and thermogenesis as the key to long-term weight loss, the scientific community has uncovered a new weight-loss technology that will provide hope to the millions of people for whom conventional weight-loss techniques have proven ineffective.
This new technology incorporates a nutritionally balanced diet, regular exercise, and the use of safe and natural substances called thermagenics, that can stimulate metabolism and thermognesis and enable people to achieve effective long-term weight loss.
Unfortunately, existing thermogenics, such as ephedra (also known as ma huang), have come under scrutiny from the United States Food and Drug Administration (USFDA), as well as state regulators, and are in danger of losing their current status in the natural-products industry. So practitioners are in dire need of an equally effective weight-loss and fitness product that will address the metabolic and thermogenic aspects of obesity and excess weight safely and naturally.
Citrus Aurantium herb, is an exceptional alternative to ephedra. Both safe and natural, it functions in three specific ways:
• it stimulates weight loss by enhancing thermogenisis which is the burning of fat;
• it increases physical performance by making fat available for energy; and
• it maintains or builds lean muscle mass.Like ephedra, synephrine increases thermogenisis, directly addressing the metabolic nature of excess weight and obesity. However, it works as effectively as ma huang without producing the negative central nervous-system and cardiovascular side effects.
Citrus Aurantium is the herbal name for the Chinese Green orange "Zhi Shi". In Chinese folk medicine Zhi Shi was commonly used to treat indigestion and relieve abdominal distension. Recently, the herb has been used in the treatment of shock, heart conditions and cardiac exhaustion. Citrus Aurantium, also known as Bitter Orange or as Seville Orange, was known to the early Greeks, and was probably the first orange grown in Europe (twelfth century). The unripe peel contains appreciable quantities of neohesperidin (14%), and five adrenergic amines (synephrine, N-methyltyramine, hordenine, ocdtopamine, and tyramine). In addition, the extract of Citrus aurantium also contains octopamine. Octopamine appears to play an important role in insect behavior -- the fruit probably contains the compound in order to stop insects from eating it. In humans, octopamine has been called a "false neurotransmitter," which changes brain function, and causes the pituitary to secrete growth hormone. Whether this secretion is enough to cause muscle bulking is not known.
The bitter orange tree is scarcely distinguishable botanically from the sweet orange tree (Aurantii Dulcis), except in its leaves, fruit, and flowers. The leaf stalk of the bitter orange is more broadly winged, and the fruit itself of deeper hue of red, having a rougher rind, and a bitter, sour juice. Added to these characteristics all portions of the bitter orange emit a greater fragrance than the same parts of the sweet variety. By some botanists, this tree is regarded merely as a variety of the Citrus Aurantium of Linné.
The U. S. P. describes bitter orange peel as consisting of "narrow, thin bands, or in quarters; epidermis of a dark, brownish-green color, glandular, and with very little of the spongy, white, inner layer adhering to it; it has a fragrant odor, and an aromatic, bitter taste".
The fruit, when ripe, is about the shape and size of the common sweet orange, is darker in color, rougher, and has a white parenchyma beneath the rind, and the juice of the pulp is bitter and sour. Orangettes (petit grains) are the unripe fruits which drop from the trees, and are considerably used on the continent under the name of orange berries. They vary from 1/8 to 1/2 inch in diameter, are of a greenish or brown-black color, closely wrinkled, and pleasantly aromatic both in taste and odor.
The leaves are borne on a jointed, broadly-winged petiole, and are smooth, oblong-ovate or ovate, nearly entire, or having a slightly crenated margin. They are aromatic and have pellucid oil-glands scattered throughout the blade.
Research
Synephrine is a well known bronchial dilator, and is used extensively in with diet pills and weight loss formulas. It also serves as a substitute for ephedrine and caffeine. Its primary use in the trade is to treat chest congestion and indigestion, stimulate gastrointestinal functions, and improve circulatory and liver functions.
Over the past 10 years, research has revealed more interesting facts on the active ingredient Synephrine. With many governments banning the sale of ephedrine based product, the search has been on for a safe and effective alternative for fat loss.
Weight loss stems from the combination of lipolysis (releasing fat from body stores) and thermogenesis (increasing the metabolic rate). Unlike ephedrine, Synephrine does not pass the blood brain barrier and does not cause stimulation of the central nervous system or what ephedrine users call the "buzz". Synephrine also only raises blood pressure slightly when compared to ephedrine.
The area where Synephrine has more effect than ephedrine is its thermogenic abilities. Synephrine increases Resting Energy expenditure by 8.2% over 4 hours. This is much greater than ephedrine.
It has been clinically shown that the combination of these adrenergic amines stimulate beta-3 receptors with minimal impact on other receptor sites. This functions to increase the metabolic rate without affecting heart rate or blood pressure. They release adrenaline and noradrenaline only in the beta-3 receptor sites (mostly adipose tissue and the liver). It does NOT cross the blood-brain barrier.
Stimulation of the beta-3 receptor sites elicits the breakdown of lipolysis (fat). Simultaniously, this stimulation increases the metabolic rate (thermogenesis), which burns calories. Synephrine offers all the advantages of a stimulant, without the drawbacks. It functions to burn fat, increase physical performance, and build lean muscle mass.
Chemical Composition.—A bitter crystalline body was isolated in 1828 by Lebreton and named hesperidin. It exists in the white parenchymatous tissues of both the orange and lemon rind, but is found in greatest abundance in the unripe Seville orange. It occurs, when purified, in white, acicular crystals, practically insoluble in water, even when hot (1 in 5000 of boiling water). It dissolves in boiling acetic acid and in alcohol, but refuses to dissolve in ether, fats, essential oils, and benzol. Treated with diluted acids it is split into grapesugar and hesperetin, insoluble in alcohol. Hesperidin fuses at 245° C. (473° F,); hesperetin at 223° C. (433.4° F.). A substance analogous to tannin, gum, resin, albumen, fixed oil, and an essential oil (see Oleum Aurantii Corticis) have also been found in the rind.
The juice of the orange consists chiefly of sugar, mucilage, and citric acid. Tanret (1886) found in bitter orange peel a bitter, acrid resin, a crystallizable, tasteless acid having the formula C44H28O14, hesperidin, an isomeric glucoside (isohesperidin, C44H26O24.5H2O) and another glucoside (aurantiamarin), to which he attributes the bitterness of the rind on account of its solubility in water.
Advanced thermogenic components have been proven to yield the following results:
76.9% increase in a person's resting metabolic rate was achieved immediately after taking the product,. In other words, the person's body started burning fat as soon as they took the product.
People had a near 30% greater weight loss than other prescribed weight loss supplements.
Clients reported up to a 42% reduction in total body fat after using Synephrine.
Synephrine effectively increases the metabolic rate by utilizing two pharmaceutical compounds known as 1(5 Hydroxytryptophan) 2(Dimethylaminoetharol Bitratrate) and L-Tyrosine. During the research phase, lead physicians and pharmacologists found these two compounds, when combined, dramatically increase the metabolic rate, causing the body to release stored fat into the bloodstream to be used as energy.
Once ingested, the adrenoceptor residing on the surface of the individual fat cells (in the form of alpha-1 and -2,and beta -1,-2,and -3 receptors) is stimulated. Specifically,this stimulation directs the thyroid hormone to convert from an inactive state to an active state....directly increasing the Resting Metabolic Rate(RMR).
Fat mobilization occurs within minutes of as the body increases production of brown adipose tissue (BAT)....a special tissue that actually burns fat rather than storing it.
This means your body will effectively AND safely burn fat around the clock....regardless of your food intake or level of exercise.
Unlike products based upon ephedrine, ma huang, phentermine, and other potentially harmful stimulants, a thermogenic agent does not cross the "blood brain barrier".... an occurrence that is chiefly responsible for the adverse side effects associated with such stimulants (such as nervousness, sleeplessness, and "jitters")
Clinical trials (reported in International Journal of Obesity, American Journal of Clinical Nutrition, and The New England Journal Of Medicine) indicated the following statistics:
300% decrease in stored fat vs.placebo.
600% increase in total weight loss vs. placebo
29% greater weight loss vs.REDUX
42% reduction in body fat in a specified time period
Synephrine, C9H13NO2
(Citrus aurantium Extract)Raw Material: The dried small fruit of Citrus aurantium
Molecular Formula: C9H13NO2
Molecular Weight: 176.2
Structure Formula:
Description of Affect:
The pharmacological action of Synephrine include decongestant effects on respiratory system, helpful in the maintenance of normal levels of blood pressure, and it is the most powerful fat loss stimulant.
ITEM STANDARDS Appearance Positive Loss on Drying NMT 5.0% Synephrine Content
<HPLC>4.0%, 6.0%, 8.0%, 10.0%, 30% and above Particle Size 80-mesh USS Sulphated NMT 3.0% Heavy Metals NMT 20 PPM Aerobic Plate Count NMT 2000/g E. Coli Negative Salmoscila Negative Packaging 5-kg/bag
25-kg/drum (0360mm x 500 mm)Synephrine vs. Ephedrine
Synephrine (Phenylephrine hydrochloride), pronounced (fen-ill-EF-rin), like ephedrine or pseudo ephedrine hydrochloride, is a common active ingredient in dozens of over-the-counter OTC and prescription medications for colds, flu, allergies and ophthalmic solutions used to dilate (enlarge the pupil) prior to eye exams or eye surgery, or in an even more diluted form to relieve redness due to minor irritations of the eye, such as those caused by allergy, dust, smoke, wind, and other irritants (see attached list). As with ephedrine, synephrine's use in such a broad variety and number of products is a testament to its' safety.
Like ephedrine, synephrine is an adrenergic amine which may enhance metabolic rate, increase fat burning, and spare muscle protein.
Unlike ephedrine users, synephrine users experience very little, if any, of the "agitation" some users associate with the use of ephedrine (Note, this also means that synephrine users will be less likely to experience the "energy" reported by ephedrine users). This is likely due to the fact that synephrine does not cross the blood/brain barrier as easily as ephedrine, thus causing less central nervous-system stimulation.
Synephrine is distributed efficiently to other tissues of the body, including: muscle and fat cells. There, like ephedrine, it stimulates both alpha and beta adrenoreceptors. Synephrine fails to stimulate beta-2 receptors (as ephedrine does) resulting in fewer central nervous system related side effects. Although it is important to note that even with ephedrine these side effects are only short-lived as beta-2 receptors develop a tolerance with continued use.
Ongoing research indicates that synephrine may be more thermogenic (raising resting metabolic rate) and less stimulatory (increasing heart rate and blood pressure) than ephedrine.
Like ephedrine, research shows synephrine is very safe, with no serious side effects reported in laboratory animals at dosages as high as 10 grams/kg (4.5 grams/lb.) body weight (see attached toxicology and carcinogenesis studies). Assuming a body weight of 150 lbs. and an average per dose recommendation of 25mg of synephrine, ingesting the 4.5 grams/lb. (indicated above as safe) would require consuming 27,000 times the recommended dosage, or 675 grams equal to 1.5 pounds of pure synephrine. It is interesting to note that the most common "side effect" observed in these studies was weight loss (3%-15%).
Study Links Ephedra To Deadly Effects with Heart,
Neurological Woes.
Ephedra (also known as Ma huang, Chinese Ephedra and epitonin) appears to pose a real risk of heart attack and other serious and even deadly complications in people who use it, researchers say. Ephedrin is a popular ingredient in herbal weight loss products.Ephedra is an herb used for centuries in China. In the United States, it has become a common ingredient in numerous dietary supplements.
Ephedra works by stimulating the central nervous system, much like adrenaline and caffeine. Advocates say the herb can help people lose weight. Products containing ephedra also are marketed to athletes as energy boosters.
Products containing the herb have become very popular and now include everything from capsules to powders to energy bars. Products containing ephedra have names like "Diet Pep," "Ripped Force," "Ripped Fuel" and "ThermoSlim." Some of the most popular brands are made by the Metabolife company.
Medical experts suggest that the stimulant can raise blood pressure and heart rate, cause vomiting, heart palpitations, dizziness, nervousness and more serious reactions, including heart attacks, seizures and strokes.
U.S. FDA has said that between 1997 and 1999 it had received 140 reports of illness or death linked to ephedra alkaloids. Since then, the agency has gotten another 103 such reports, but those haven't been investigated.
The FDA had asked researchers at the University of California at San Francisco to evaluate the 140 cases of suspected adverse events.
Dr. Christine Haller, a UCSF toxicologist and lead author of the study said that he recommend that people not take this herbal product due to the serious risk of complications and minimal benefit to offset it.
Of the 140 incidents, 31 percent were "definitely or probably" the result of ephedra, the researchers claim, accounting for five cases of cardiac arrest, four strokes and three deaths. An additional 31 percent were "possibly" tied to the compound.
Taken together, these two groups accounted for 10 deaths and more than a dozen cases of permanently disabling injuries. Ephedra was also implicated in high blood pressure, abnormal heart rhythms, seizures and palpitations.
For some time the jury was on out on the safety of ephedra especially when used as a weight loss supplement or as a stimulant. In June 1997, the FDA proposed a rule that would have limited the amount of ephedra that could be added to dietary supplements to 8 milligrams. It would also have put warning labels on the products cautioning against taking them for more than a week, and advising consumers not to combine them with other stimulants. On strong criticism from the General Accounting Office (GAO), that the agency needed more evidence before it can conclude that the herbal therapy was truly dangerous. FDA later retracted the dosage recommendation. However, it has kept the warning against mixing ephedrine with other stimulants.
Not everyone shares the opinion that ephedra is dangerous. The Council for Responsible Nutrition, a trade group, believes that ephedra is both effective and safe. They cite a new report by Harvard and Columbia University researchers showing that people who took a combination of 90 milligrams of ephedra and caffeine lost more weight -- but had no more adverse events -- than those who took placebo.
American Herbal Products Association and the Consumer Healthcare Products Association, wants FDA to require that the supplements with ephedra carry warning labels cautioning its use only by people over 18. They want the use of ephedra be limited to no more than 25 milligrams per serving.
The proposed label also warns against mixing ephedra products with prescription drugs, as well as nonprescription drugs containing PPA, a chemical common in diet pills and cold remedies. PPA has been implicated in stroke risks.
Availability
Northwest Botanicals, Inc is pleased to announce an exclusive relationship with a primary extractor who cultivates the Bitter Orange. Each batch has a certificate of analysis, and is sold in powder extract form. Synephrine extract is available at 4% min., 6% min., 8% min., 10% min., with higher percent extract available.
Price:
Citrus aurantium Extract (Synephrine 4% min.) Citrus aurantium Extract (Synephrine 6% min.) Citrus aurantium Extract (Synephrine 8% min.) Citrus aurantium Extract (Synephrine 10% min.) Citrus aurantium Extract (Synephrine 30% up.) Citrus aurantium Extract (Synephrine 95% ) $520.00/kg.
Hespiridine (heavy) Hespiridine (light) *Prices above are all based on FOB Synetch warehouses (LA/NY);
**NBI 5% commission included.Samples are available upon request.
OAK PUBLISHING, INC.
1212 SW 5th St.
Grants Pass, OR 97526
Phone: (541) 476-5588
Fax: (541) 476-1823Internet Addresses
DrRam@MAGICK.nethttp://www.nwbotanicals.org
http://www.herbfarminfo.com
also see the Q/A section of
http://www.richters.com
Herbal supplements containing ephedraHave you heard of Xenadrine? Does it help to supply energy or is this just another false herbal claim?
SkepticalDear Skeptical,
You are right to question the claims concerning Xenadrine, an herbal supplement that contains (among other things) ephedrine, caffeine, aspirin, synephrine and probably octopamine. Companies who sell this and similar supplements claim that they are effective fat burners, which prevent loss of lean muscle tissue, suppress appetite, and supply the body with more energy. These effects, if they occur, are temporary, while ephedrine, synephrine, and some of the other compounds in the plants used to make these herbal supplements can be detrimental to your health.
Ephedrine
Ephedrine is the active chemical found in ephedra plants. Ma Huang is the Chinese name for ephedra plants and their derivatives. In traditional medicine, ephedra extracts containing ephedrine have been used to relieve allergy symptoms, because ephedrine is a bronchodilator (= it "opens up" the lungs for people who have asthma), and a decongestant which works for hay fever. However it is a potent stimulant. The drug works on the brain -- people who take the drug may feel pepped up, and may, for a short time, ind they lose their appetite. Caffeine and synephrine add to this effect, but also to the toxicity of the ephedrine. Ephedrine increases a person's heart rate and blood pressure -- it acts through the same mechanisms that cause your heart rate and blood pressure to rise if you are extremely scared, or have exercised excessively. This increase in heart rate and blood pressure may push your heart too far, while the stimulating effect on the brain may make you behave aggressively, and you may even develop hallucinations, seizures and psychosis. To quote the Food and Drug Administration:
"Reported adverse events [of which there have been more than 900 reports] range from episodes of high blood pressure, irregularities in heart rate, insomnia, nervousness, tremors and headaches, to seizures, heart attacks, strokes and death. Most events occurred in young to middle aged, otherwise healthy adults using the products for weight control and increased energy."In 1996, The Food and Drug Administration posted a warning concerning ephedrine, stating that the drug should not be used by consumers without medical supervision, because of its potential for severe and even fatal side effects. However, ephedrine in herbal supplements is regulated under the Dietary Supplement Health and Education Act of 1994, which does not require that the FDA approve it for use. Nevertheless, the FDA is required to act if the supplement results in significant adverse effects.
Given the side effects noted above, in1997 the FDA began trying to develop rules which limit the recommended dose (called "serving" because the drug is considered a dietary supplement) of ephedrine and provide warnings for consumers. In addition, several states, including Ohio, Florida, Texas, and Washington, have developed regulations of their own concerning ephedrine, although the limiting "serving" size is larger (25 mg) than the one at which severe side-effects have been noted (about 10mg). Note that, while two capsules of Xenadrine (the amount recommended by the manufacturer) contains 20 mg of ephedrine, the effects of the drug are enhanced by the caffeine and synephrine, so that in effect the "serving" a person takes in is actually larger.
The World Health Organization has called for opinions concerning ephedra and ephedrine, with a view towards including these products among narcotic drugs such as morphine or heroine. The FDA opened a period of study and commentary concerning the drug, which closed at the end of December 1998. You can find the documents submitted to the FDA by industry, senators, and others, by doing a search for ephedrine in the FDA webpages. You may specifically be interested in the statement submitted by the American Dietetic Association to the FDA concerning ephedrine.
Synephrine and octopamine
The synephrine in herbal supplements is derived from a Chinese fruit, Citrus aurantium, or bitter orange. Synephrine does the same things, and works in much the same way, as ephedrine, so the two chemicals together add up to a much stronger effect, and much more toxicity. In addition, the extract of Citrus aurantium also contains octopamine. Octopamine appears to play an important role in insect behavior -- the fruit probably contains the compound in order to stop insects from eating it. In humans, octopamine has been called a "false neurotransmitter," which changes brain function, and causes the pituitary to secrete growth hormone. Whether this secretion is enough to cause muscle bulking is not known. More importantly from a health point of view, together with synephrine and ephedrine, octopamine raises blood pressure, and therefore increases the risk of heart disease and stroke.
Recently, a study carried out in France, using tissue culture cells ("Specific stimulation of adipose tissue beta-3-adrenoceptors by octopamine." by Jean Galitzky and his colleagues, in the Comptes Rendus de l'Academie des Sciences Serie III Sciences de la Vie. 316 (5). 1993. 519-523) has suggested that octopamine can increase the metabolism of brown fat (and presumably therefore increase fat loss) -- however, it turns out that it works in this way in dog fat cells but has no effect in human fat cells.
Conclusion:
Given these side-effects, we strongly urge you use extreme caution when using this supplement, or when using any compound with ephedra, Citrus aurantium or one of their derivatives, whether you take it to increase your energy or to decrease your weight or for any other reason. And we especially warn people with thyroid disease, diabetes, high blood pressure, cardiovascular disease, depression, anxiety, glaucoma, and people taking drugs known as MAO inhibitors to avoid ephedrine and similar compounds completely. The reason for placing MAO inhibitors on this list is that these drugs inhibit the breakdown of ephedrine, synephrine and octopamine, so the side-effects of these latter compounds will be severe, and potentially fatal.
You can find out more about plant poisoning due to herbs from the Emergency Medicine plant poisoning page from Johns Hopkins University.
As with all dietary supplements, and particularly ones which promise to boost your energy, or help you lose weight, it is a good idea to consult your physician, pharmacist or registered dietitian before starting to take them.
To your good health!July 16th, 1999
03-02-01100% Herbal Extract
Synephrine, C9H13NO2
(Citrus aurantium Extract)
Raw Material: The dried small fruit of Citrus aurantiumMolecular Formula: C9H13NO2
Molecular Weight: 176.2
Structure Formula:
Description of Affect:
The pharmacological action of Synephrine include decongestant effects on respiratory system, helpful in the maintenance of normal levels of blood pressure, and it is the most powerful fat loss stimulant.
ITEM STANDARDS Appearance Positive Loss on Drying NMT 5.0% Synephrine Content
<HPLC>4.0%, 6.0%, 8.0%, 10.0%, 30% and above Particle Size 80-mesh USS Sulphated NMT 3.0% Heavy Metals NMT 20 PPM Aerobic Plate Count NMT 2000/g E. Coli Negative Salmoscila Negative Packaging 5-kg/bag
25-kg/drum (0360mm x 500 mm)
03-02-01100% Herbal Extract
Hesperidine, C28H34O15
(Citrus aurantium Extract)
Raw Material: The dried small fruit of Citrus aurantiumMolecular Formula: C28H34O15
Molecular Weight: 610.58
Structure Formula:
Description of Affect:It can be the medicine for the treatment of reduction of fragility of capillaries. It is used for hypertension and hemorrhage of the bloody capillaries.
ITEMS Heavy Quality Light Quality Appearance Light Brown Powder Light Cream-yellow Pwd Distinguish Positive Positive Loss on Drying NMT 5.0% NMT 5.0% Content <HPLC> NLT 93% NLT 93% Size 95% pass 80 mesh 80 mesh 95% 80 mesh Absorption (660nm) NMT 0.20 NMT 0.20 Sulphated NMT 0.30% NMT 0.30% Density NLT 0.60g/cm3 NLT 0.35g/cm3 Package 25 kg/drum
(O360mm x 500mm)25 kg/drum
(O360mm x 500mm)
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