Ephedrine
Ephedrine is an alkaloid drug derived from plants of the genus Ephedra, notably E. sinica and E. distachya, and can also be synthesized in laboratories. It is chemically similar to amphetamine and methamphetamine, affecting the central nervous system by increasing the activity of noradrenaline. Historically, ephedrine has been utilized in traditional Chinese medicine for thousands of years, particularly for treating respiratory issues like asthma and bronchitis. In modern medicine, it serves various purposes, including treating hypotension and narcolepsy, but it requires careful monitoring due to potential serious side effects.
While legal in certain formulations, its use as a dietary supplement is prohibited in the U.S. due to concerns about abuse, particularly among athletes seeking weight management benefits. Side effects can include nervousness, insomnia, and rapid heartbeat, and it poses risks for individuals with specific health conditions. Additionally, ephedrine should not be used during pregnancy without strict medical oversight. Understanding both its medicinal benefits and risks is crucial for safe use.
Subject Terms
Ephedrine
ALSO KNOWN AS: Ma huang
DEFINITION: Ephedrine is an alkaloid drug derived from plants of the genus Ephedra (family Ephedraceae); it also is produced synthetically. Ephedrine is similar in chemical structure to amphetamine and methamphetamine drugs.
STATUS: Legal (certain formulations by prescription only in the United States (US) and United Kingdom); illegal for use as a dietary supplement; sold over-the-counter in Canada as a nasal decongestant
CLASSIFICATION: Scheduled Listed Chemical Product (SLCP)
SOURCE: Primary natural source of ephedrine is as an extract from plants of the genus Ephedra, specifically E. sinica and E. distachya; most commercial supplies are grown in China. Because of the expense of extracting ephedrine from natural sources, most pharmaceutical sources of the drug are L-ephedrine, which is produced synthetically.
TRANSMISSION ROUTE: Ephedrine occurs as fine white crystals or powder; the drug is readily soluble in water. In capsule form, it is administered orally, and when dissolved in water, it can be administered in a nasal spray. It can also be given subcutaneously or intravenously.
History of Use
Ephedrine has been used as an herbal preparation (ma huang) for thousands of years in Chinese medicine as a treatment for asthma and bronchitis. A Japanese chemist, Nagayoshi Nagai, first isolated ephedrine from the plant E. distachya in 1885, and it has been used in Western medicine since that time.
Ephedrine increases noradrenaline's activity on adrenergic receptors in the brain. It indirectly stimulates the sympathetic nervous system, can cross the blood-brain barrier, and affects the central nervous system directly by causing the release of noradrenaline and dopamine. Thus, its action is similar to that of the drugs amphetamine and methamphetamine. Ephedrine can also be used in the production of methamphetamine due to the drugs' similar chemical structures.
Ephedrine has been abused by athletes, particularly by weightlifters and bodybuilders, because it is thought to act as an appetite suppressant and may promote fat utilization. Many athletes need to maintain a certain weight and body fat percentage before competition, leading to ephedrine use, often in combination with caffeine and aspirin. In 2004, the US Food and Drug Administration banned the use of ephedrine in dietary supplements aimed at weight loss.
Effects and Potential Risks
Ephedrine has many legitimate medical uses, primarily in the treatment of respiratory problems, such as asthma, but also in treating hypotension, nasal congestion, narcolepsy, certain types of depression, adverse effects of anesthesia, and myasthenia gravis (an autoimmune neuromuscular disorder). However, ephedrine has many potentially serious side effects, and persons with heart disease, angina pectoris, hyperthyroidism, diabetes, and enlarged prostate must be closely supervised by their physicians during use of the substance.
Side effects of ephedrine include nervousness, panic disorder, insomnia, vertigo, difficulty breathing, headache, tachycardia (rapid and erratic heartbeat), nausea, anorexia, and painful urination. Ephedrine should not be used during pregnancy except under extremely close medical supervision. Adverse drug interactions occur between ephedrine and certain antidepressants, namely serotonin-norepinephrine reuptake inhibitors, and monoamine oxidase inhibitors. Ephedrine should not be used with medications for cough and congestion.
Bibliography
"Ephedra." National Center for Complementary and Integrative Health, www.nccih.nih.gov/health/ephedra. Accessed 23 Aug. 2024.
"Ephedrine - StatPearls." NCBI, www.ncbi.nlm.nih.gov/books/NBK547661. Accessed 23 Aug. 2024.
"Ephedrine Monograph for Professionals." Drugs.com, 6 May 2024, www.drugs.com/monograph/ephedrine.html. Accessed 23 Aug. 2024.
Fontanarosa, Phil B., Drummond Rennie, and Catherine D. DeAngelis. "The Need for Regulation of Dietary Supplements: Lessons from Ephedra." Journal of the American Medical Association, vol. 289, 2003, pp. 1568–70.
Gad, Mohamed Z., Samar S. Azab, Amira R. Khattab, and Mohamed A. Farag. "Over a Century Since Ephedrine Discovery: An Updated Revisit to Its Pharmacological Aspects, Functionality and Toxicity in Comparison to Its Herbal Extracts." Food Function, vol. 12, no. 20, 2021, pp. 9563-9582. DOI: 10.1039/D1FO02093E. Accessed 30 Nov. 2022.
Kuhar, Michael J., and Howard Liddle. Drugs of Abuse. New York: Marshall Cavendish Reference, 2012.
Martin, Elizabeth. An A to Z of Medicinal Drugs. New York: Oxford UP, 2010.
Maxwell, Jane Carlisle, and Beth A. Rutkowski. "The Prevalence of Amphetamine and Methamphetamine Abuse in North America: A Review of the Indicators, 1992–2007." Drug and Alcohol Review, vol. 27, no. 3, 2008, pp. 229–35.