Ephedrine

Authors: Prof. Dr. med. Peter Altmeyer, Prof. Dr. med. Martina Bacharach-Buhles

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Last updated on: 29.10.2020

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Synonym(s)

(1R,2S)-2-methylamino-1-phenylpropan-1-ol; CAS No: 299-42-3; L-(-)-ephedrine

Definition
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Ephedrine is a natural phenylethylamine alkaloid, which is the main alkaloid found in ephedra species (e.g. Ephedra sinica, Chinese sea rouble - also known as "Mahuang") and Catha edulis. The substance forms a crystalline white powder with a bitter taste. Ephedrine is soluble in 4 parts water and ethanol.

Spectrum of action
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Ephedrine releases norepinephrine and thus leads to an increase in adrenergic transmission. Since it has no hydroxy groups on the phenyl ring, it can pass the blood-brain barrier (although not as efficiently as amphetamine or methamphetamine).

Field of application/use
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In isolated or synthetically produced form, ephedrine - like the diastereomers D-pseudoephedrine and D-norpseudoephedrine - is used for its sympathomimetic effect in bronchial asthma and rhinitis. Ephedrine can stimulate circulation, increase drive and performance, reduce appetite, but also relax and in some people have a slightly sexually stimulating effect. It increases the urge to move, attention and the need to communicate.

Dosage
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The usual dose is 25-50 mg/day p.o.

Undesirable effects
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In case of overdose the side effects are many: restlessness, anxiety, nausea, insomnia, tremor, pulse racing, sweating, difficulty breathing, confusion, hallucinations, delirium, headache, rarely: cramps.

Note(s)
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Until 2001 ephedrine preparations were freely available in German pharmacies. Ephedrine was misused as an appetite suppressant, party drug. Ephedra herba is also available only on prescription in German pharmacies. Because of its appetite-suppressant and subjectively performance-enhancing effect, ephedrine is often used as a (prohibited) doping agent, often in combination with caffeine and acetylsalicylic acid.

Literature
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  1. Abourashed EA et al (2003) Ephedra in perspective--a current review. Phytother Res 17:703-712.
  2. Diepvens K et al (2007) Obesity and thermogenesis related to the consumption of caffeine, ephedrine, capsaicin, and green tea. On J Physiol Regul Integr Comp Physiol 292:R77-85.
  3. Lee A et al(2002) A quantitative, systematic review of randomized controlled trials of ephedrine versus phenylephrine for the management of hypotension during spinal anesthesia for cesarean delivery. Anesth Analg 94:920-926
  4. Lieberman HR (2001) The effects of ginseng, ephedrine, and caffeine on cognitive performance, mood and energy. Nutr Rev 59:91-102.
  5. Lin FQ et al (2012) Ephedrines versus phenylephrines for the management of hypotension during spinal anesthesia for cesarean section: an updated meta-analysis. CNS Neurosci Ther 18:591-597.
  6. Magkos F et al (2004) Caffeine and ephedrine: physiological, metabolic and performance-enhancing effects. Sports Med 34:871-889.
  7. Shekelle PG et al (2003) Efficacy and safety of ephedra and ephedrine for weight loss and athletic performance: a meta-analysis. JAMA 289:1537-1545.