History full circle: ‘Novel’ sympathomimetics in supplements

Rasmussen, Nicolas; Keizers, Peter H. J.

doi:10.1002/dta.1852

Cited by 15 publications

(16 citation statements)

References 23 publications

(44 reference statements)

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“…Significant increases in heart rate as well as systolic and diastolic blood pressure occurred in both studies in response to the consumption of the product. These results indicate that methylsynephrine, which has a phenylpropylamine structure more closely related to ephedrine (Rasmussen and Keizers, 2015), acts as a stimulant. Again, it should be emphasized that synthetic p-synephrine HCL and methylsynephrine as well as synthetic esters of norsynephrine are prohibited by the US FDA from being used in dietary supplements.…”

Section: More Recent Human Studiesmentioning

confidence: 80%

Safety, Efficacy, and Mechanistic Studies Regarding Citrus aurantium (Bitter Orange) Extract and p‐Synephrine

Stohs

2017

Phytotherapy Research

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Citrus aurantium L. (bitter orange) extracts that contain p‐synephrine as the primary protoalkaloid are widely used for weight loss/weight management, sports performance, appetite control, energy, and mental focus and cognition. Questions have been raised about the safety of p‐synephrine because it has some structural similarity to ephedrine. This review focuses on current human, animal, in vitro, and mechanistic studies that address the safety, efficacy, and mechanisms of action of bitter orange extracts and p‐synephrine. Numerous studies have been conducted with respect to p‐synephrine and bitter orange extract because ephedra and ephedrine were banned from use in dietary supplements in 2004. Approximately 30 human studies indicate that p‐synephrine and bitter orange extracts do not result in cardiovascular effects and do not act as stimulants at commonly used doses. Mechanistic studies suggest that p‐synephrine exerts its effects through multiple actions, which are discussed. Because p‐synephrine exhibits greater adrenergic receptor binding in rodents than humans, data from animals cannot be directly extrapolated to humans. This review, as well as several other assessments published in recent years, has concluded that bitter orange extract and p‐synephrine are safe for use in dietary supplements and foods at the commonly used doses. Copyright © 2017 The Authors Phytotherapy Research Published by John Wiley & Sons Ltd.

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Section: More Recent Human Studiesmentioning

confidence: 80%

Safety, Efficacy, and Mechanistic Studies Regarding Citrus aurantium (Bitter Orange) Extract and p‐Synephrine

Stohs

2017

Phytotherapy Research

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“…Marketed as nasal decongestants and stimulants originally, these substances were abandoned long ago due to safety and abuse concerns. 60 …”

Section: Dietary Supplements For Weight Lossmentioning

confidence: 99%

Prohibited Contaminants in Dietary Supplements

2017

Sports Health

108

106

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Context:With the increasing use of unregulated dietary supplements, athletes are at continued risk from adverse medical events and inadvertent doping.Evidence Acquisition:A review of Clinical Key, MEDLINE, and PubMed databases from 2012 to 2017 was performed using search terms, including dietary supplement, contamination, doping in athletes, inadvertent doping, and prohibited substances. The references of pertinent articles were reviewed for other relevant sources.Study Design:Clinical review.Level of Evidence:Level 3.Results:Poor manufacturing processes and intentional contamination with many banned substances continue to occur in dietary supplements sold in the United States. Certain sectors, such as weight loss and muscle-building supplements, pose a greater threat because they are more likely to be contaminated.Conclusion:Athletes will continue to be at risk for adverse events and failed doping tests due to contaminated dietary supplements until legislation changes how they are regulated. In the interim, there are several steps that can be taken to mitigate this risk, including improved education of medical staff and athletes and use of third party–certified products.

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“…In recent years, many phenylethylamines have been detected in dietary or sports supplements [1][2][3][4]. Some of them are isomers of methamphetamine (MA, 16 in Fig.…”

Section: Introductionmentioning

confidence: 99%

“…It has been detected recently in supplements sold in Australia [13], the Netherlands [14], and Spain [11]. BMPEA has been detected in supplements sold in the United States [3] and other countries [1,2]. The database of the Early Warning Advisory on New Psychoactive Substances administered by the United Nations Office on Drugs and Crime (UNODC) [15] also includes numerous cases of these two substances from Europe and Canada.…”

Section: Introductionmentioning

confidence: 99%

A novel method to distinguish β-methylphenylethylamines from isomeric α-methylphenylethylamines by liquid chromatography coupled to electrospray ionization mass spectrometry

Tsumura

Kiguchi

Komatsuzaki³

et al. 2019

Forensic Toxicol

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Purpose Various phenylethylamines have been detected lately in dietary or sports supplements. N-Methyl-2-phenylpropan-1-amine (phenpromethamine) and 2-phenylpropan-1-amine (β-methylphenylethylamine, BMPEA) are known to produce mass spectra almost identical to those produced by methamphetamine (MA) and amphetamine (AP), respectively, when analyzed by liquid chromatography/mass spectrometry (LC/MS). They may interfere with the analysis of MA and AP. The aims of the present study were to determine whether some substances other than phenpromethamine and BMPEA give mass spectra similar to those given by MA or AP and to develop an analytical method of distinguishing phenpromethamine from MA and BMPEA from AP by derivatization. Methods Twenty isomers of MA or AP were selected to be analyzed using LC/MS. Six reagents were examined for derivatization of MA, AP, phenpromethamine, and BMPEA. Three mass spectrometers from two manufacturers were evaluated for their ability to reproduce the data. Results All isomers except phenpromethamine and BMPEA were shown to be distinguishable from MA and AP by their mass spectra. For the discrimination of isomeric pairs, derivatization using N-succinimidyl-4-nitrophenylacetate was found to be the best for tandem mass spectrometry and that using 4-nitrobenzoyl chloride was the best for in-source collision-induced dissociation. One or more ions from each pair of isomers gave adequate difference in their relative intensities according to the World Anti-Doping Agency criteria. Conclusions The newly developed method was proved to be usable for discriminating among those phenylethylamines.

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History full circle: ‘Novel’ sympathomimetics in supplements

Cited by 15 publications

References 23 publications

Safety, Efficacy, and Mechanistic Studies Regarding Citrus aurantium (Bitter Orange) Extract and p‐Synephrine

Safety, Efficacy, and Mechanistic Studies Regarding Citrus aurantium (Bitter Orange) Extract and p‐Synephrine

Prohibited Contaminants in Dietary Supplements

A novel method to distinguish β-methylphenylethylamines from isomeric α-methylphenylethylamines by liquid chromatography coupled to electrospray ionization mass spectrometry

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