Citrus aurantium's therapeutic uses

  • PRINCIPAL PROPOSED USE: Weight loss
  • OTHER PROPOSED USES: Antibacterial, anti-inflammatory, antifungal, antioxidant, anxiety, aromatherapy, cancer prevention, depression, digestive issues, viral infection

Overview

Citrus aurantium is the Latin name for a fruit best known as Seville orange, sour orange, or bitter orange. The juice, peel, and essential oil have all been used medicinally in traditional Chinese and Ayurvedic medicine. Traditional uses include digestive problems, epilepsy, fatigue, insomnia, infections, respiratory problems, and skin problems. As a flavoring, the essence of bitter orange is found in the beverages Triple Sec and Cointreau.

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Therapeutic Dosages

Many Citrus aurantium products are made from the juice and concentrated extracts of the peel and are said to contain a fixed percentage of synephrine or total amines. A typical recommended dosage of such products ranges from 100 to 150 milligrams (mg) two to three times daily. However, these doses may be unsafe.

Therapeutic Uses

Citrus aurantium juice and peel contain the stimulant chemical synephrine and related stimulants, such as octopamine, tyramine, N-methyltyramine, and hordeline. On this basis, Citrus aurantium has been widely marketed as a weight-loss product. However, there is no reliable evidence that Citrus aurantium is effective, and there is considerable reason to worry that it may cause harm. The reassuring statement made by some manufacturers that Citrus aurantium offers the “benefits of ephedra without the risks” is not supported by scientific evidence. Since Citrus aurantium would have to be taken for an extended period of time for weight loss, the risks are even more significant.

One published double-blind, placebo-controlled trial on Citrus aurantium juice did not test the herb alone but, rather, evaluated a combination product that also contained caffeine and St. John’s wort. While the results were somewhat positive, overall, the study was too preliminary to reach reliable conclusions. An even less reliable study evaluated the synephrine constituent of Citrus aurantium and found possible fat-burning actions. Given the weakness of the evidence in favor of Citrus aurantium, and the considerable evidence that it presents health risks, experts recommend against using it for weight loss. Other evidence, far too weak to rely upon, hints that synephrine-rich Citrus aurantium extracts might have antidepressant effects.

Besides synephrine and other stimulants, whole Citrus aurantium peel contains citral, limonene, and several citrus bioflavonoids, including hesperidin, neohesperidin, naringin, and rutin. Weak evidence hints that these substances might have cancer-preventive and antiviral actions.

The essential oil of Citrus aurantium contains linalool and the fragrant substance limonene, which might have antianxiety and sedative effects. In pregnant women, one study showed that the use of the essential oil decreased labor anxiety. However, neither of these proposed uses has more than extremely preliminary supporting evidence.

In traditional medicine, Citrus aurantium was used for digestive issues, such as indigestion, bloating, and gas. However, no double-blind, placebo-controlled trials have been performed on Citrus aurantium for this purpose. The flavonoids in Citrus aurantium may have anti-inflammatory and antioxidant properties, protecting individuals from free radicals that could lead to chronic health conditions. While increased double-blind, placebo-controlled trials are necessary to understand the efficacy of therapeutic uses of Citrus aurantium, researchers must also consider the risks.

Safety Issues

Most of the safety concerns regarding Citrus aurantium relate to its stimulant constituents. The drug synephrine is known to produce many unpleasant and possibly dangerous side effects, including headache, agitation, rapid heart rate, and heart palpitations. In some people, it can cause angina pectoris, kidney damage, increased pressure in the eye, and reduced blood circulation to the heart and the extremities. The other stimulant amines in Citrus aurantium may increase such effects. There is one case report of a heart attack that appears possibly related to the use of a Citrus aurantium supplement, and another that links the herb to stroke. Citrus aurantium juice or concentrated extracts can raise blood pressure and increase heart rate and, therefore, should not be used by individuals with cardiovascular disease or high blood pressure. People with glaucoma should also avoid the herb.

Synephrine can also interact with numerous medications and other drugs, including stimulants (including ephedrine, pseudoephedrine [Sudafed], stimulant medications for attention-deficit/hyperactivity disorder (ADHD), and even caffeine) and anesthetics. The tyramine constituent of Citrus aurantium can cause deadly side effects when combined with drugs in the MAO inhibitor family.

The peel and essential oil of Citrus aurantium may cause photosensitivity (an increased tendency to react to sun exposure). For this reason, it is not recommended to treat it in combination with drugs that cause the same side effect (such as sulfa antibiotics).

Finally, Citrus aurantium juice can alter the way that the liver processes various medications, potentially raising or lowering their levels. In particular, the drugs cyclosporine and felodipine (a calcium channel blocker) are thought to be affected by Citrus aurantium juice, but numerous other drugs may also interact with it. For this reason, experts recommend that persons taking any medications critical to their health should not take Citrus aurantium juice simultaneously. Furthermore, safety in young children, pregnant or nursing women, and people with severe liver or kidney disease has not been established.

Important Interactions

Citrus aurantium should not be taken by persons using medications in the MAO inhibitor family, and it should not be used without consulting a physician if one is taking ephedrine, pseudoephedrine (Sudafed), stimulant medications for ADHD, cyclosporine, calcium channel blockers, drugs that cause photosensitivity (such as sulfa antibiotics), or any medication that is critical to one’s health.

Bibliography

"Bitter Orange." Drugs.com, 30 Nov. 2022, www.drugs.com/npp/bitter-orange.html. Accessed 12 Oct. 2024.

"Bitter Orange: Usefulness and Safety." National Center for Complementary and Integrative Health, May 2020, www.nccih.nih.gov/health/bitter-orange. Accessed 12 Oct. 2024.

Bui, L. T., D. T. Nguyen, and P. J. Ambrose. "Blood Pressure and Heart Rate Effects Following a Single Dose of Bitter Orange." Annals of Pharmacotherapy, vol. 40, 2006, pp. 53-57.

"Can Synephrine Help In Weight Loss?" McGill University, 20 Mar. 2017, www.mcgill.ca/oss/article/weight-loss-you-asked/can-synephrine-help-weight-loss. Accessed 12 Oct. 2024.

Carvalho-Freitas, M. I., and M. Costa. "Anxiolytic and Sedative Effects of Extracts and Essential Oil from Citrus aurantium L." Biological and Pharmaceutical Bulletin, vol. 25, 2002, pp. 1629-1633.

Kim, K. W., et al. "Characterization of Antidepressant-like Effects of P-synephrine Stereoisomers." Naunyn Schmiedeberg’s Archives of Pharmacology, vol. 364, 2001, pp. 21-26.

Malhotra, S., et al. "Seville Orange Juice-Felodipine Interaction: Comparison with Dilute Grapefruit Juice and Involvement of Furocoumarins." Clinical Pharmacology and Therapeutics, vol. 69, 2001, pp. 14-23.

Shen, Chun-Yan, et al. "Anti-inflammatory Effect of Essential Oil from Citrus Aurantium L. Var. Amara." Journal of Agricultural and Food Chemistry, vol. 65, no. 39, 14 Sept. 2017.

Suntar, Ipek, et al. "An Overview on Citrus aurantium L.: Its Functions as Food Ingredient and Therapeutic Agent." Oxidative Medicine and Cellular Longevity, 2 May. 2018, p. 7864269, doi:10.1155/2018/7864269.