Higenamine

Higenamine is a compound found in various plants, gaining attention for its stimulant effects that impact heart rate and muscle tissue relaxation or contraction. It's commonly used in supplements aimed at improving athletic performance, though its safety and efficacy for such purposes lack solid scientific evidence. Furthermore, higenamine is not only present in higenamine pre-workout and weight loss products but is scrutinized for its potential health risks, including serious heart-related side effects and interactions with other medications.

Despite its growing use in the supplement industry as a substitute for substances like DMAA and ephedrine, higenamine supplements are mired in controversies regarding their legality and safety. Classified as a beta-2 agonist, higenamine's inclusion in dietary supplements is prohibited by sports authorities and is a concern for athletes subject to doping tests. This article will delve into the pharmacology of higenamine, its purported benefits, side effects, and how consumers can navigate the complex landscape surrounding higenamine supplements, especially in the context of athletic performance and higenamine pre-workout formulations.

What is Higenamine?

Higenamine, also known by its chemical name norcoclaurine, is a naturally occurring compound found in a variety of plants. These plants include aconite, Annona squamosa, Nandina domestica (sacred bamboo), and others.. It is recognized for its stimulant effects, which can cause relaxation in some tissues while causing others, such as heart muscle, to contract. This dual action is primarily why higenamine is used in various supplements aimed at enhancing athletic performance, promoting weight loss, and treating respiratory and cardiovascular conditions.

Overview of Higenamine Uses

1. Athletic Performance and Weight Loss: Commonly included in pre-workout and weight management supplements, higenamine is valued for its stimulant properties that potentially enhance fat burning and improve athletic performance.
2. Respiratory Treatments: Traditionally used as an anti-asthmatic, its bronchodilator effects make it a candidate for treating asthma and other breathing disorders.
3. Cardiovascular Health: Investigational studies in China have explored higenamine’s use in cardiac stress tests and treatments for various heart conditions, including heart failure and arrhythmias.

Pharmacological Actions and Safety

Higenamine acts as a β2 adrenoreceptor agonist, stimulating an enzyme called adenylate cyclase, which increases cellular concentrations of cAMP, a critical messenger in many biological processes. This action leads to various effects such as increased heart rate, vascular relaxation, and bronchodilation. Despite these benefits, higenamine is classified as POSSIBLY UNSAFE when taken orally due to potential serious side effects like arrhythmias and other heart-related issues. It is advised that individuals with heart arrhythmias, pregnant or breastfeeding women, and those scheduled for surgery avoid its use.

Legal and Regulatory Status

Higenamine is listed on the FDA's Dietary Supplement Ingredient Advisory List and is banned by the World Anti-Doping Agency (WADA) due to its classification as a beta-2 agonist. Despite these restrictions, it remains legal within food supplements in several regions including the UK, EU, the USA, and Canada, primarily in products aimed at weight management and sports performance. However, it is not approved for use in dietary supplements and its presence is not always disclosed on product labels, which poses additional risks for consumers.

This complex profile underscores the need for cautious use and consideration of legal guidelines when considering higenamine as a supplement ingredient, especially for athletes and individuals with existing health conditions.

Pharmacological Effects of Higenamine

Higenamine, recognized for its stimulant effects, primarily acts as a β2 adrenoreceptor agonist. This action stimulates an enzyme called adenylate cyclase, which is responsible for increasing the cellular concentrations of cAMP, a crucial adrenergic second messenger. The pharmacological effects of higenamine are diverse, ranging from cardiovascular to respiratory system impacts.

Stimulant Effects and Cardiovascular Risks

Higenamine functions similarly to other stimulants by increasing heart contractions and accelerating the heart rate. This can lead to serious cardiovascular side effects, including irregular heartbeats and potentially fatal outcomes. Due to these risks, individuals with existing heart conditions, particularly those with irregular heartbeats, are advised against its use.

Interaction with Medications and Other Substances

Higenamine's influence extends to the metabolic processes involving other medications. It can alter the rate at which the liver metabolizes certain drugs, potentially modifying their effects and side effects. Additionally, its ability to slow blood clotting may enhance the risk of bruising and bleeding, especially when combined with other medications that also affect blood clotting. When used with stimulant drugs, higenamine might further accelerate the nervous system and heart rate, increasing the risk of high blood pressure.

Pharmacokinetics

The absorption and elimination of higenamine in the body are rapid yet limited. Only 3 to 22% of administered higenamine enters the bloodstream, and it remains in circulation for approximately 8 minutes. Nearly all ingested higenamine is expelled from the body within 30 minutes.

Potential Therapeutic Effects

Despite the risks, research in animal and cell-based models suggests that higenamine may offer several therapeutic benefits. These include protective effects on the heart and brain, relief from asthma and arthritis symptoms, antithrombotic effects, and potential treatments for erectile dysfunction, spinal cord injuries, and diabetes. Additionally, higenamine has shown anti-apoptotic, anti-inflammatory, anti-fibrotic, and lipid-lowering activities. It may also act as a vasodilator and smooth muscle relaxant, improving blood perfusion.

Combination with Other Natural Compounds

Research indicates that combining higenamine with other naturally occurring compounds like cucurbitacin B and 6-gingerol can enhance its anti-apoptotic activity, potentially offering synergistic benefits in disease treatment.

Higenamine in Dietary Supplements

Higenamine is increasingly found in dietary supplements, particularly those marketed for weight loss, energy enhancement, and athletic performance. However, its presence and labeling in these supplements raise significant concerns regarding safety and regulatory compliance.

Presence and Labeling Issues

Higenamine is not always listed on the labels of products promoted as pre-workout supplements, which poses a risk for consumers, especially athletes who could face doping violations. The U.S. Food and Drug Administration (FDA) has listed higenamine on its Dietary Supplement Ingredient Advisory List since April 2019, indicating concerns about its safety and regulatory status. Despite these warnings, some products containing higenamine can still be found on the market, often not disclosing their inclusion on the label, which complicates consumer decisions and regulatory enforcement.

Regulatory Status and Safety Concerns

The FDA considers products containing higenamine as "adulterated" under the terms that they contain a "new dietary ingredient" for which a required notification has not been submitted. This classification stems from studies showing that higenamine can lead to serious cardiotoxic effects, including high blood pressure and rapid heart rate, particularly at high doses. Moreover, the World Anti-Doping Agency (WADA) prohibits the use of higenamine in sports, complicating its inclusion in dietary supplements intended for athletes.

Variability in Higenamine Content

Research has shown significant variability in the amount of higenamine present in dietary supplements. A 2019 study published in Clinical Toxicology reported that the higenamine content in 24 analyzed supplements varied widely, from trace amounts to 62 ± 6.0 mg per serving, and often did not match the quantities listed on the product labels. This inconsistency can expose consumers to unpredictable and potentially harmful doses of higenamine, with some individuals potentially ingesting up to 110 mg per day based on labeled directions.

Common Names and Mislabeling

Consumers should be aware of other common names for higenamine, which include norcoclaurine and several chemical names, to better identify it in supplement ingredients lists. The mislabeling and variability in dosage underscore the need for stringent regulatory oversight and better consumer education regarding the potential risks associated with higenamine consumption.

Recommendations for Consumers

Given the potential health risks and the regulatory status of higenamine, consumers are advised to exercise caution. Those with pre-existing heart conditions, pregnant or breastfeeding women, and individuals scheduled for surgery should avoid products containing higenamine. Additionally, athletes should be particularly cautious due to the risk of doping violations and the adverse health effects associated with higenamine.

Risks and Implications for Athletes

Higenamine, classified as a beta-2 agonist, presents significant risks and implications for athletes, particularly regarding compliance with doping regulations and potential health risks.

Prohibited Status and Doping Risks

Higenamine is prohibited at all times, both in and out-of-competition, as classified by the World Anti-Doping Agency (WADA). Since 2017, higenamine has been included in the WADA prohibited list in the beta-2 agonist (S3) category, with a specific reporting level of 10 ng/ml for the free parent form in urine.. This inclusion underscores the strict monitoring and potential penalties for athletes found with higenamine in their systems during doping tests.

Health Risks

The use of higenamine can lead to serious heart-related side effects, including rapid heartbeat and irregular heart rhythms, which are particularly risky for athletes. Its ability to increase heart rate can also interfere with surgical procedures, necessitating a cessation of higenamine use at least two weeks before scheduled surgeries. Moreover, the substance has been linked to liver damage and may reduce the effectiveness of medications for blood pressure and blood clotting.

Variability in Supplement Content

Athletes face additional risks due to the variability in higenamine content across different dietary supplements. Studies have shown that the amount of higenamine can vary significantly, sometimes exceeding what is listed on the label, which increases the risk of inadvertent doping. This inconsistency can expose athletes to higher doses, potentially leading to severe cardiovascular reactions.

Legal and Regulatory Considerations

Despite its legal status in some regions for use in non-sporting dietary supplements, higenamine lacks approval for clinical use and is considered "adulterated" when included in dietary supplements without proper notification. Athletes need to be particularly cautious, as the presence of higenamine in supplements is not always clearly labeled, posing a risk for unintentional doping violations.

Recommendations for Athlete Safety

Athletes are advised to thoroughly check supplement labels and avoid products that might contain higenamine, especially those that do not fully disclose their ingredients. Consulting with healthcare professionals and staying informed about the substances prohibited by WADA can further help athletes avoid the risks associated with higenamine use.

Top Higenamine Supplements

While general information on the prevalence of higenamine in weight loss and sports supplements is available, specific products and brands are often not comprehensively listed. However, notable examples of higenamine-containing supplements are available and include some potent formulations designed for specific consumer needs.

Featured Higenamine Supplements

BZRK Pre Workout Psychoactive Waves by Black Magic

1. A pre-workout supplement known for its strong stimulant effects, primarily targeting enhanced mental focus and energy levels during workouts.

Convict Pre Workout by Condemned Labz

1. Designed for serious athletes, this supplement provides a robust boost in energy and stamina, supporting intense training sessions.

Dust X Pre Workout by Blackstone Labs

1. Offers a powerful combination of ingredients for high-intensity workouts, promoting both energy and focus.

Detailed Product Analysis: HyperCuts

Manufacturer: CTD Sports

Key Ingredients:

• 1. Proprietary Blend 413mg
  2. Caffeine
  3. Higenamine: Not specified, but included as a main ingredient

Benefits:

• 1. Strong stimulant properties enhance energy and focus.
  2. Panthergya and caffeine combination supports significant weight loss.
  3. Rauwolfia vomitoria Root Extract and Huperzia serrata Club Moss Extract contribute to fat burning and mood enhancement.

These supplements are targeted at individuals looking for significant enhancements in either athletic performance or weight loss. Each product contains a blend of ingredients that work synergistically with higenamine to maximize its effects.

Higenamine and Pre-Workout Supplements

Higenamine is a popular ingredient in pre-workout supplements due to its stimulant properties, which are believed to enhance athletic performance by increasing energy levels and improving focus. These supplements are designed to be taken before exercise to maximize physical performance and endurance. Here, we explore the use of higenamine in pre-workout formulations and its potential benefits and considerations for athletes and fitness enthusiasts.

Role of Higenamine in Enhancing Athletic Performance

1. Stimulant Effects: Higenamine acts as a beta-2 agonist, which can increase adrenaline levels, leading to enhanced alertness and energy. This makes it a favored component in pre-workout supplements aiming to boost stamina and performance during workouts.
2. Fat Burning Properties: There is evidence suggesting that higenamine has lipolytic effects, helping to break down fats and thus, potentially aiding in weight loss. This property aligns with the goals of many fitness enthusiasts who seek to improve body composition and performance simultaneously.

Safety and Dosage Considerations

1. Recommended Dosage: The appropriate dosage of higenamine in pre-workout supplements can vary significantly between products. Users should adhere to the manufacturer's recommended dosages and be cautious of exceeding them, as higher doses may lead to adverse effects.
2. Potential Side Effects: While beneficial for its stimulant effects, higenamine can also pose cardiovascular risks such as increased heart rate and blood pressure. These effects warrant caution, particularly for individuals with pre-existing heart conditions.

Regulatory and Compliance Issues

1. WADA Prohibition: Athletes need to be aware that higenamine is listed as a prohibited substance by the World Anti-Doping Agency (WADA), which can affect compliance in professional sports. Using higenamine-containing pre-workout supplements could lead to positive doping tests and potential sanctions.
2. Labeling Accuracy: The concentration of higenamine in pre-workout supplements can sometimes be inaccurately labeled, which poses further risks for athletes regarding both health and compliance with sports regulations.

Popular Pre-Workout Supplements Containing Higenamine

1. Product Variability: The market offers a range of pre-workout supplements containing higenamine, each with varying formulations and concentrations. It is crucial for consumers to research and choose products from reputable manufacturers to ensure quality and safety.

Consumer Advice

1. Informed Choices: Consumers considering higenamine pre-workout supplements should consult healthcare providers to understand the potential health implications and to ensure that the product is appropriate for their personal health and fitness goals.
2. Monitoring Effects: It is advisable for users to monitor their body's response to higenamine, particularly if they are new to its use. Observing any adverse reactions can help in making informed decisions about continuing or adjusting the usage of such supplements.

By understanding the roles and risks associated with higenamine in pre-workout supplements, consumers can make more informed choices about their supplementation practices, balancing the benefits of enhanced performance with the imperative of safety and regulatory compliance.

For Sale at RacerEphedra.com

RacerEphedra.com stands out as a comprehensive online retailer that specializes in a diverse range of supplements. Customers can explore products across various categories including bodybuilding, HGH enhancement, muscle building, testosterone boosting, and sexual enhancement. The platform also caters to those seeking weight loss solutions and general health supplements.

Product Range and Brands

The website features an extensive selection of brands such as 5% Nutrition, 5-Hour Energy, ABE Nation, After Dark, Alani Nu, and Alpha Lion. This variety ensures that consumers have access to a wide array of supplements to meet their specific health and fitness needs.

Navigation and Shopping Experience

Shoppers can efficiently find products by using the filter options available on the site. These filters include price, flavor, and manufacturer, which streamline the shopping process and enhance user experience.

Additional Product Offerings

In addition to traditional supplements, RacerEphedra.com also offers products in categories like CBD, energy supplements, joint health, kava, kratom, nootropics, and sports supplements. This broad selection caters to a wide demographic of consumers looking for specific health benefits.

Shipping and Returns

The website provides added value with free shipping on orders over $49. Additionally, RacerEphedra.com supports customer satisfaction with a 30-day money-back guarantee, ensuring a risk-free purchase experience.

Regulatory and Review Insights

While RacerEphedra.com is categorized under the Vitamin and Supplements Store, it's important to note that the site has a claimed profile but lacks verified details. Furthermore, the response to customer feedback, particularly negative reviews, has not been documented, which might be a consideration for potential buyers. Reviews on platforms like Trustpilot highlight the importance of verification for companies and reviewers, aiming to ensure the authenticity of user feedback.

Higenamine Product Availability

It should be noted that while RacerEphedra.com offers a wide range of supplements, the availability of higenamine-specific products is not explicitly mentioned. Consumers interested in higenamine supplements should verify product details directly on the website or contact customer service for more information.

Conclusion

Throughout this comprehensive discussion on higenamine supplements, we have traversed its multifaceted landscape, unveiling its pharmacological underpinnings, potential benefits, significant risks, and the muddled regulatory environment governing its use. We highlighted the crucial considerations for consumers, athletes, and fitness enthusiasts contemplating its inclusion in their regimen, underscored by the need for caution due to variable content in supplements and potential health implications. It is apparent that while higenamine offers intriguing possibilities for enhancing athletic performance and weight loss, these must be carefully balanced against its cardiovascular risks and the pressing need for adhering to legal and doping regulations.

The discourse also sheds light on the broader implications of higenamine's usage, emphasizing the critical role of informed decision-making supported by current scientific evidence and regulatory guidelines. For those considering higenamine, it is prudent to engage in diligent research, consult healthcare professionals, and prioritize transparency and safety when selecting supplements. Given the evolving nature of research and legislation surrounding higenamine, ongoing scrutiny and updated guidance will be essential in navigating its future in dietary supplements. Moving forward, further research and a clearer regulatory stance could provide invaluable insights, optimizing the balance between leveraging higenamine's benefits and mitigating its risks.

References

Higenamine: What Athletes Need to Know to Compete Clean https://www.usada.org/spirit-of-sport/education/higenamine-what-athletes-need-to-know-to-compete-clean/

Influence of Higenamine on Exercise Performance of Recreational Female Athletes: A Randomized Double-Blinded Placebo-Controlled Trial https://doi.org/10.3389/fpsyg.2021.633110

Yen, Ching-Chi, Chun-Wei Tung, Chih-Wei Chang, Chin-Chuan Tsai, Mei-Chich Hsu, and Yu-Tse Wu. 2020. "Potential Risk of Higenamine Misuse in Sports: Evaluation of Lotus Plumule Extract Products and a Human Study" Nutrients 12, no. 2: 285. https://doi.org/10.3390/nu12020285