Ephedra

Ephedra Summary

Ephedra is commonly known by its Chinese name “Ma Huang” due to its popularity in Chinese medicine.

It has been used medicinally for at least 5000 years in China and has been used in surrounding Asian countries like India for a very long time as well.

The main components of ephedra are a class of chemicals known as alkaloids. These alkaloids are similar in structure and function to the hormone known as epinephrine (Adrenalin). They act as sympathomimetics, which increases heart rate, blood pressure, and promote the bronchioles (airway) to dilate. This allows more air into the lungs. This last action is the reason behind ephedra’s common use on asthma, and bronchitis-related conditions.

This herb is incredibly useful to a trained herbalist but is easily abused. This has led to its banning in Australia for safety reasons. Overdose of ephedra can lead to dangerously high blood pressure which can lead to convulsions, coma, and death if not treated promptly. The problem is not in the herb itself, but the carelessness of dose.

Following a strict maximum dosage and paying close attention to how it affects your body individually will eliminate any risk of this happening.

What Is Ephedra Used For?

Ephedra is not much used in Western herbal medicine — primarily due to some bad press around people abusing the plant for its ephedrine content. Ephedrine is a central nervous system stimulant. People use ephedra similar to other stimulant drugs like modafinil, Ritalin, or Adderall.

Ephedrine stimulates the sympathetic nervous system — activating the adrenergic receptors throughout the cardiopulmonary system. One of the results of this stimulation is a feeling of euphoria, intense focus and concentration, and elevated energy levels. This has led to a large number of people using the herb as a pre-workout, recreational drug, or to support study efforts. The unfortunate result of this is the same as any stimulant drug abuse — overburdened liver and adrenals and disorientation in the sleep-wake cycle.

The FDA banned the sale and use of ephedra in 2003.

The medicinal uses for ephedra involve the ephedrine content as well but in smaller, more controlled doses. The ability to interact with the central nervous system so reliably makes it a beneficial herb.

One of the most important applications of this is asthma. Ephedra stimulates the adrenergic system in the lungs, causing the bronchioles to dilate — allowing more air into the lungs.

More long term use of this herb isn’t recommended, but for shorter bursts (2 weeks or less) ephedra is useful as a mild stimulant (in small doses) for supporting weight loss programs in combination with a nutritional analysis and diet plan.

Traditional Uses

Western Herbal Medicine

One of the more recent uses of ephedra is as a weight loss supplement for its ability to stimulate the CNS and increase metabolism ^{9Reference 9Abourashed et al. · 2003ReviewEphedra in perspective–a current review}.

Traditional Chinese Medicine

The use of ephedra dates back thousands of years, especially in China where it has been used for at least 5000 years as medicine. Mention of this herb has been found in some of the Hindu Vedas as well ^{1,2,8Reference 1Hoffmann · 2003Medical herbalism: The science and practice of herbal medicineReference 2Dewick · 2002Medicinal natural products: a biosynthetic approachReference 8Kitani et al. · 2009Molecular analysis and chemical evaluation of Ephedra plants in Mongolia}.

In total, its traditional usage across Asia includes the treatment of asthma, nasal congestion, hypotension, urinary incontinence ^{5Reference 5Ibragic et al. · 2015Chemical composition of various Ephedra species}.

Taste

Acrid, pungent, slightly bitter ^{7,21Reference 7Yang et al. · 2013Introduction to chinese materia medica (3rd ed.). (Pg 36-40)Reference 21Wu · 2005An illustrated Chinese materia medica}

Energy

Warm ^{7,21Reference 7Yang et al. · 2013Introduction to chinese materia medica (3rd ed.). (Pg 36-40)Reference 21Wu · 2005An illustrated Chinese materia medica}

Channels

Lung and bladder ^{21Reference 21Wu · 2005An illustrated Chinese materia medica}

Actions

Promotes sweating to disperse cold, diffuses the lungs to relieve wheezing, promotes the flow of lung Qi, reduces swelling by increasing urination. ^{7,21Reference 7Yang et al. · 2013Introduction to chinese materia medica (3rd ed.). (Pg 36-40)Reference 21Wu · 2005An illustrated Chinese materia medica}.

Indications

Colds with wind-cold pattern (especially with lack of sweating), chest oppression, cough, wheezing due to excess, wind edema. ^{7Reference 7Yang et al. · 2013Introduction to chinese materia medica (3rd ed.). (Pg 36-40)}.

Cautions & Safety

People who sweat easily (it’s a strong diaphoretic), deficiency type asthma, weak constitution, hypertension, or heart disease ^{7Reference 7Yang et al. · 2013Introduction to chinese materia medica (3rd ed.). (Pg 36-40)}. Avoid large doses ^{21Reference 21Wu · 2005An illustrated Chinese materia medica}.

Botanical Information

Ephedra is one of the oldest living plant species on earth. It’s contained in the ancient family of plants — Gnetales. Compared to its two sister genera; Gnetum, and Welwitschia it’s actually quite young.

Ephedra is estimated to have first appeared between 8 and 32 million years ago. Other members of the family are thought to have first appeared closer to 250 million years ago — placing it in the Cretaceous period. [26].

Each ephedra plant is either a male or a female (dioecious) ^{3Reference 3A Modern Herbal · 1931EphedraView study →}.

Habitat, Ecology & Distribution

Ephedra can be found growing on sandy shores in temperate climates in both the east and west hemispheres ^{3Reference 3A Modern Herbal · 1931EphedraView study →}. It’s reportedly very adaptable — especially for a plant so morphological simple. This ability to adapt makes identification of this herb difficult at times ^{5,7Reference 5Ibragic et al. · 2015Chemical composition of various Ephedra speciesReference 7Yang et al. · 2013Introduction to chinese materia medica (3rd ed.). (Pg 36-40)}.

Harvesting, Collection & Preparation

The best ephedra is reported to come from northern China, with the highest quality grown in Shanxi, Gansu, Shaanxi, and Qinghai provinces. Good quality ephedra can be identified as light green; dried, thick-stemmed with a solid centre. ^{7Reference 7Yang et al. · 2013Introduction to chinese materia medica (3rd ed.). (Pg 36-40)}.

Pharmacology & Medical Research

Allergies

An anaphylactic reaction results from a systemic release of inflammatory mediators from the mast cells and basophils ^{20Reference 20Moosmann et al. · 2004Selenoprotein synthesis and side-effects of statinsView study →}. In modern emergency medicine, the immediate treatment for this is an intramuscular injection of epinephrine. Epinephrine is a mixed alpha- and beta-adrenergic receptor agonist and works by alleviating allergen-induced inflammatory, and other physiological effects ^{21Reference 21Wu · 2005An illustrated Chinese materia medica}.

Ephedra contains alkaloids very similar in structure and function to epinephrine, with the most significant one likely being ephedrine. Similar to epinephrine, ephedrine possesses both alpha- and beta- adrenergic receptor agonist actions ^{24Reference 24Chong et al. · 1995Functional desensitization of beta agonist responses in human lung mast cells} and thus may sustain similar actions towards the anti-anaphylactic effects of the emergency medicine epinephrine.

The alpha adrenergic receptor agonist effects cause vasoconstriction of the blood vessels which then reduce systemic vasodilation and alleviate hypotension and possible hypotensive shock, as well as lowering erythema, urticaria, and angioedema ^{22Reference 22Kemp SF et al. · 2008Epinephrine: the drug of choice for anaphylaxis}.

The beta-adrenergic receptor agonist activity dilates bronchial airways, increases the force of myocardial contraction (positive inotropy), and increases heart rate. This results in a significant increase in cardiac output and can reduce the severity of Ig-E mediated reactions via mast cells. ^{23,24Reference 23McLean-Tooke et al. · 2003Adrenaline in the treatment of anaphylaxis: what is the evidence?Reference 24Chong et al. · 1995Functional desensitization of beta agonist responses in human lung mast cells}.

Although the actions of ephedrine and epinephrine on the alpha and beta adrenergic receptors are similar, the application is generally very different. It’s impossible to inject ephedra intramuscularly without laboratory intervention, its use in the absence of epinephrine, or for milder anaphylactic reactions, may warrant ephedra’s use in an emergency setting. In minor incidents, ephedra appears to offer a valuable treatment, especially in the way of bronchial asthma as further indicated through its long traditional usage.

CNS Stimulant

The alkaloid component of ephedra has well known stimulating actions on the CNS through a binding to adrenergic receptors. ^{4Reference 4EFSA ANS Panel (EFSA Panel on Food Addit et al. · 2013Scientific opinion on safety evaluation of Ephedra species in food}.

Weight Loss

Ephedra is often used as a weight loss supplement for its ability to stimulate the CNS to stimulate metabolism. It has hypolipidemic and hypocholesterolemic, as well as hypoglycemic actions which go a long way in the prevention and treatment of obesity and its associated ramifications. ^{23,24,25Reference 23McLean-Tooke et al. · 2003Adrenaline in the treatment of anaphylaxis: what is the evidence?Reference 24Chong et al. · 1995Functional desensitization of beta agonist responses in human lung mast cellsReference 25Kay LJ · 2005Mast cell beta2-adrenoceptors}. There are some side effects with ephedra alkaloids; however, some of which can lead to serious events such as myocardial infarctions, cardiac arrhythmias, high blood pressure, and stroke ^{15,16Reference 15Zhang et al. · 2000Studies on extraction of water-soluble polysaccharides and the function of cleaning oxygen free-radical function of ephedraReference 16Kalman et al. · 2002Clinical trialAn acute clinical trial evaluating the cardiovascular effects of an herbal ephedra–caffeine weight loss product in healthy overweight adults}. These reports have been debated, and the non-alkaloid content has also been found to be hypolipidemic through the prevention of free radical species generation, and recuperation of liver function during liver damage ^{17Reference 17Haller et al. · 2000Adverse cardiovascular and central nervous system events associated with dietary supplements containing ephedra alkaloids}. This action will have a much less pronounced effect on the reduction of weight specifically but addresses some of the commonly associated conditions with obesity such as hyperlipidemia and hypercholesterolemia. Currently, the primary treatment for these conditions involves statin medications, which themselves have a wide range of negative associations and side effects ^{18,19Reference 18Fan et al. · 2015AnimalEffect of extractions from Ephedra sinica Stapf on hyperlipidemia in miceReference 19Chiu et al. · 2005Effect of statin therapy on risk of ventricular arrhythmia among patients with coronary artery disease and an implantable cardioverter-defibrillator}.

The consensus at the time of this writing is that the long term usage, as is the case with weight loss programs, should be avoided with ephedra. Other herbs are available instead that will achieve this purpose in a much safer manner.

Phytochemistry

Ephedra’s activity is defined by its phenylpropylamine alkaloids — ephedrine and its stereoisomer pseudoephedrine — which together usually make up more than 80% of the total alkaloid fraction and are responsible for the herb’s sympathomimetic, bronchodilator and stimulant actions ^{5Reference 5Ibragic et al. · 2015Chemical composition of various Ephedra species}. These two amines are the regulated actives: it is their ephedrine content that led to ephedra being restricted or banned in several jurisdictions. Dried stem typically carries 0.5–2.5% total alkaloids, with pharmacopoeial material required to hold at least ~0.7% ^{5Reference 5Ibragic et al. · 2015Chemical composition of various Ephedra species}.

Beyond the alkaloids, the stems contain flavonoids, the hypoglycaemic stem polysaccharides known as ephedrans (A–E) ^{13Reference 13Konno et al. · 1985Isolation and hypoglycemic activity of ephedrans A, B, C, D and E, glycans of Ephedra distachya Herbs1}, and minor quinoline-2-carboxylic acids ^{12Reference 12Starratt et al. · 1996Quinoline-2-carboxylic acids from Ephedra species}. The non-alkaloid, water-soluble polysaccharide fraction carries antioxidant and hypolipidaemic activity independent of the stimulant alkaloids ^{15Reference 15Zhang et al. · 2000Studies on extraction of water-soluble polysaccharides and the function of cleaning oxygen free-radical function of ephedra}.

Constituent Summary

Alkaloid figures are percent of dried stem; ephedrine/pseudoephedrine are also expressed as their share of the total alkaloid fraction. Content varies markedly with species, harvest time and origin.

Clinical Applications

Ephedra is not recommended therapeutically. Experience is needed to use this herb safely.

Cautions & Safety

Contraindicated with cardiovascular conditions, thyroid disease, diabetes, or prostate enlargement ^{1Reference 1Hoffmann · 2003Medical herbalism: The science and practice of herbal medicine}.

May interact with cardiac glycosides or halothane to produce arrhythmias ^{1Reference 1Hoffmann · 2003Medical herbalism: The science and practice of herbal medicine}.

Guanethidine has been reported to enhance the sympathomimetic effects of ephedra ^{1Reference 1Hoffmann · 2003Medical herbalism: The science and practice of herbal medicine}.

Combination with monoamine oxidase inhibitors (MAOI’s) can significantly increase the sympathomimetic actions of ephedrine, which can lead to fatal hypertension ^{1Reference 1Hoffmann · 2003Medical herbalism: The science and practice of herbal medicine}.

Be cautious of ephedra products adultered with synthetic alkaloids ^{5Reference 5Ibragic et al. · 2015Chemical composition of various Ephedra species}.

Contraindications

• Cardiovascular conditions
• Thyroid conditions
• Enlarged prostate
• Diabetes
• Pregnancy & lactation
• Not for use in children

References

1. Hoffmann, D. (2003). Medical herbalism: The science and practice of herbal medicine. Rochester, VT: Healing Arts Press. (Pg. 546-547)
2. Dewick, P. M. (2002). Medicinal natural products: a biosynthetic approach. John Wiley & Sons. P. 383
3. A Modern Herbal. (1931). Ephedra. Retrieved from http://www.botanical.com/botanical/mgmh/e/ephedr11.html
4. EFSA ANS Panel (EFSA Panel on Food Additives and Nutrient Sources), 2013. Scientific opinion on safety evaluation of Ephedra species in food. EFSA J 2013; 11(11): 3467, 79 pp.
5. Ibragic, S., & Sofić, E. (2015). Chemical composition of various Ephedra species. Bosnian journal of basic medical sciences, 15(3), 21.
6. Miyazawa, M., Minamino, Y., & Kameoka, H. (1997). Volatile components of Ephedra sinica Stapf. Flavour and fragrance journal, 12(1), 15-17.
7. Yang, J., Huang, H., Zhu, Li-Jiang, & Chen, Y. (2013). Introduction to chinese materia medica (3rd ed.). (Pg 36-40).
8. Kitani, Y., Zhu, S., Omote, T., Tanaka, K., Batkhuu, J., Sanchir, C., … & Komatsu, K. (2009). Molecular analysis and chemical evaluation of Ephedra plants in Mongolia. Biological and pharmaceutical bulletin, 32(7), 1235-1243.
9. Abourashed, E. A., El‐Alfy, A. T., Khan, I. A., & Walker, L. (2003). Ephedra in perspective–a current review. Phytotherapy Research, 17(7), 703-712.
10. Shekelle, P. G., Hardy, M. L., Morton, S. C., Maglione, M., Mojica, W. A., Suttorp, M. J., … & Gagné, J. (2003). Efficacy and safety of ephedra and ephedrine for weight loss and athletic performance: a meta-analysis. Jama, 289(12), 1537-1545.
11. Purev, O., Pospíšil, F., & Motl, O. (1988). Flavonoids from Ephedra sinica stapf. Collection of Czechoslovak Chemical Communications, 53(12), 3193-3196.
12. Starratt, A. N., & Caveney, S. (1996). Quinoline-2-carboxylic acids from Ephedra species. Phytochemistry, 42(5), 1477-1478.
13. Konno, C., Mizuno, T., & Hikino, H. (1985). Isolation and hypoglycemic activity of ephedrans A, B, C, D and E, glycans of Ephedra distachya Herbs1. Planta medica, 51(02), 162-163.
14. Chumbalov, T. K., Chekmeneva, L. N., & Polyakov, V. V. (1977). Phenolic acids of Ephedra equisetina. Chemistry of Natural Compounds, 13(2), 238-239.
15. Zhang, L., Zou, G., & Yang, T. (2000). Studies on extraction of water-soluble polysaccharides and the function of cleaning oxygen free-radical function of ephedra. Amino Acids and Biotic Resources, 22(3), 24-26.
16. Kalman, D., Incledon, T., Gaunaurd, I., Schwartz, H., & Krieger, D. (2002). An acute clinical trial evaluating the cardiovascular effects of an herbal ephedra–caffeine weight loss product in healthy overweight adults. International journal of obesity, 26(10), 1363.
17. Haller, C. A., & Benowitz, N. L. (2000). Adverse cardiovascular and central nervous system events associated with dietary supplements containing ephedra alkaloids. New England journal of medicine, 343(25), 1833-1838.
18. Fan, Y., Li, J., Yin, Q., Zhang, Y., Xu, H., Shi, X., … & Zhou, C. (2015). Effect of extractions from Ephedra sinica Stapf on hyperlipidemia in mice. Experimental and therapeutic medicine, 9(2), 619-625.
19. Chiu, J. H., Abdelhadi, R. H., Chung, M. K., Gurm, H. S., Marrouche, N. F., Saliba, W. I., … & Martin, D. O. (2005). Effect of statin therapy on risk of ventricular arrhythmia among patients with coronary artery disease and an implantable cardioverter-defibrillator. American Journal of Cardiology, 95(4), 490-491.
20. Moosmann, B., & Behl, C. (2004). Selenoprotein synthesis and side-effects of statins. The Lancet, 363(9412), 892-894. doi:10.1016/s0140-6736(04)15739-5
21. Wu, J. N. (2005). An illustrated Chinese materia medica. New York: Oxford University Press. (Pg. 280-281).
22. Kemp SF, Lockey RF, Simons FE. (2008). Epinephrine: the drug of choice for anaphylaxis. A statement of the World Allergy Organization. Allergy. 63:1061–1070.
23. McLean-Tooke, A. P., Bethune, C. A., Fay, A. C., & Spickett, G. P. (2003). Adrenaline in the treatment of anaphylaxis: what is the evidence?. BMJ: British Medical Journal, 327(7427), 1332.
24. Chong, L. K., Morice, A. H., Yeo, W. W., Schleimer, R. P., & Peachell, P. T. (1995). Functional desensitization of beta agonist responses in human lung mast cells. American journal of respiratory cell and molecular biology, 13(5), 540-546.
25. Kay LJ, Peachell PT. (2005). Mast cell beta2-adrenoceptors. Chem Immunol Allergy. 87:145–153.
26. Rydin, C., Pedersen, K. R., & Friis, E. M. (2004). On the evolutionary history of Ephedra: Cretaceous fossils and extant molecules. Proceedings of the National Academy of Sciences, 101(47), 16571-16576.Chicago