Ephedrine

Ephedrine Supplements: How Bodybuilders STILL Use this Banned Drug

Ephedrine SupplementsEphedrine supplements were purported to make weight loss effortless by increasing metabolism and naturally reducing appetite.

In the 1980’s and 1990’s, ephedrine diet pills became recognized for their ability to boost energy, promote athletic stamina and support weight loss. These pills were widely used by dieters and professional athletes.

In multiple large research studies, this alkaloid derived from the Ephedra Sinica extract was shown to have a significant fat burning effect, particularly if combined with caffeine.

However, these supplements were removed from the market due to fears about side effects. Clinical data showed that taking this herbal extract in high doses could lead to increased risk of dangerous cardiovascular events.

While ephedrine supplements are no longer legal in the USA, the ephedra plant extract still is. How do these new ephedra weight loss supplements affect the body and what is the likelihood of negative effects? Click here to buy ephedra supplements online legally without a prescription.


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Ephedrine Supplements Review

Ephedrine supplements were among the most popular ever, earning supplement manufacturers billions of dollars in sales around the world.

Brands like Lipodrene, Metabolife 356, Yellow Jackets and Hydroxycut were some of the top-rated products that contained ephedra and were used by millions of Americans.

Hundreds of fat-burning products, diet pills, energy boosters and pre-workout formulas were made with this ingredient. But in 2004, the FDA instituted a ban on the sale of any dietary supplement containing this alkaloid.

Since then, an entire generation has grown up hearing about the benefits of ephedrine diet pills, which, in most places around the world, are no longer available.

What happened to trigger the ban of ephedra alkaloids from over-the-counter products? Why is this ingredient still legal to sell as a nasal decongestant, but illegal if promoted to help individuals lose weight and increase energy?

As use of this thermogenic stimulant grew, concerns about potential side effects became louder in the media. Even though many people attributed ephedrine with helping them lose weight, there was also a high risk of adverse reactions.

Some of the adverse effects were potentially life-threatening, including heart attacks, seizures, diabetic ketoacidosis, temporary psychosis, stroke and even deaths.

In 2003, Baltimore Orioles pitcher Steve Bechler collapsed and later died after taking a product called Xenadrine RFA-1. While there were many other factors that contributed to his death, it was his use of ephedra that was highlighted in media reports.

After this, the FDA issued a ruling stating that use of ephedrine posed an “unreasonable risk of illness or injury” and labelled it an adulterant in nutritional supplements.


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What is the Ephedrine Alkaloid?

Ephedrine is the primary active alkaloid that comes from the ephedra plant. Over 60 species of this plant have been identified today, but not all of them contain this alkaloid or others such as pseudoephedrine.

Ephedrine is known as a sympathomimetic amine and works by stimulating greater activity in the central nervous system. It influences certain receptors in the body related to the hormone adrenaline.

Ephedrine and pseudoephedrine interact with alpha and beta-adrenergic receptors which promote a response in sympathetic nervous system functions. It can adrenoreceptors found in arteries, the heart muscle, and airways in the lungs.

One of the ways this drug works is by causing arteries that supply the heart to constrict, which increases blood pressure. This pressure enhances circulation returning blood to the heart for re-oxygenation.

Ephedrine also affects beta-1 receptors found in the heart muscle. This influences the speed with which the heart beats as well as the force of heart muscle contractions, improving blood flow through the body.

Finally, ephedrine has an effect on the beta-2 receptors found in lung airways. It triggers the airways (bronchial tubes and bronchioles) to relax or dilate, increasing airflow.

It also affects smooth muscle, such as that lining the sinus and nasal passages. Use of this drug can relieve nasal congestion in people with a cold or hay fever allergies. Ephedrine has proven beneficial in the relief of asthma, bronchitis, rhinitis and the common cold.

Historically, a number of cultures used the ephedra plant for the treatment of lung and breathing conditions. It was a prominent medicinal herb in China, India, as well as Native American and Middle Eastern cultures.

Synthetic Ephedrine sulfate and Ephedrine HCl are still used today for relief from these symptoms. However, their use has largely been supplanted by other drugs that are seen to be more effective with lower risk of adverse effects.

Ephedrine has psychotropic as well as psychomotor effects, which can account for some of the more common side effects experienced by users. This includes hand tremors, heart palpitations, agitation and restlessness.

How Does Ephedrine Burn Fat?

Use of ephedrine pills was recognized in the 1970’s to contribute to weight loss by increasing energy expenditure. In clinical practices, doctors began to obverse that their patients were losing weight when taking this drug for asthma and other conditions.

It was determined that this alkaloid could stimulate the central nervous system and increase metabolism, result in greater fat burning. Athletes also recognized benefits for energy enhancement, improved oxygenation and increased stamina.

There were a number of studies conclusively showing that ephedrine supplements could cause weight reduction even when diet and exercise were not incorporated. However, the best results came from using this supplement with caffeine in conjunction with calorie restriction and working out.

As this supplement became more and more popular, increasing numbers of individuals complained to their physicians about side effects and adverse reactions.

The same ways in which this supplement promoted fat loss could also cause harmful effect on the cardiovascular system, especially if taken in high doses or used over long time periods.

By 2003, thousands of reports had been submitted by users complaining of mild to moderate side effects such as:

  • Headaches
  • Nausea
  • Heart palpitations
  • Anxiety or restlessness
  • Tremors

The abuse of ephedra-containing supplements was brought to national headlines with the death of baseball pitcher Steve Bechler in 2003. He died of heat stroke while in Spring Training. While he had previously suffered from heat-related incidents, his use of ephedra was made the culprit in the media.

At that time, the Food and Drug Administration stated that they had received over 16,000 side effect reports from the millions of people using the product. [1] There was also a risk of lethal toxicity when taking too much of the product; 22 deaths were associated with overuse, and misuse of ephedrine.

Subsequently, the FDA published a “Final rule declaring dietary supplements containing ephedrine alkaloids adulterated because they present an unreasonable risk.”


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Available Sources

As of April 2004, all of the previous brands of ephedrine diet pills were recalled and removed from the market. Many of the popular products of the 1990’s have now been reformulated without any of this alkaloid.

Shortly after products were removed from over-the-counter store shelves, manufacturers introduced new versions with ingredients to replace the ephedrine component. For example, Hydroxycut was re-formulated with a coffee bean extract and Stacker 2 was re-made with kola nut, green tea and yerba mate.

Under the 2004 ban by the FDA, supplements are not allowed to contain ephedrine. However, they can use forms of ephedra that do not contain this active ingredient. These diet pills are known as ephedra extract supplements.

For example, Lipodrene with ephedrine was replaced with a version containing ephedra extract that is devoid of the banned alkaloids. Many other products like Metabodrene 25, Black Spider 25, Ripped Power and Red Volt use similar ingredients.

Ephedrine can also still be found in medicinal products available without a prescription. Those drugs include asthma medications, allergy pills, and cough, cold, or flu medications.

While these products are sometimes used by bodybuilders and athletes off-label for their weight loss benefits, this practice is strongest recommended against. Many of these drugs contain additional ingredients like ibuprofen and guaifenesin that can be harmful when taken in high dosages

Ephedra Extract Supplements

While ephedra and ephedrine alkaloids were banned from dietary supplements in most countries, the US allows an exception for ephedra extract products that do not contain the illegal alkaloids.

These products contain a type of extract that is inactive or inert. Some of the other bioactive constituents in the ephedra plant may contribute to weight loss, but the effects will not be the same as if you were taking a supplement with ephedrine alkaloids.

To compensate for this loss, supplement manufacturers will replace this ingredient with legal alternatives that have similar effects. Bodybuilders also source other thermogenic agents that have questionable legal statuses in the USA.

One of the most common legal substitutes is Bitter Orange (Citrus Aurantium). This fruit extract contains p-synephrine, a component with a mechanism of action very similar to ephedrine.

Synephrine activates adrenoreceptors that influence sympathetic or autonomic body functions. It stimulates receptors involved in regulating respiration and metabolism but does not have as strong an effect on blood pressure or heart rate. [2]

Caffeine is also pervasive in thermogenic fat loss supplements. This herbal stimulant can boost metabolism, suppress appetite and promote weight loss. While effective in clinical studies, the body quickly develops a tolerance to the drug such that larger and larger dosages must be used.

Taking higher than recommended or excessive levels of caffeine can cause serious adverse reactions. Caffeine overdose can occur, especially when combined with other herbal stimulants.

Yohimbine is another stimulant that is used in fat burners. Derived from the bark of the Corynanthe Yohimbe tree, this indole alkaloid increases the release of norepinephrine and acts as an alpha-2 receptor antagonist.

Illegal or Unapproved Alternatives

Bodybuilders who want to replicate the effects of the original ephedrine supplements will also turn to stronger fat loss aids that are unapproved or have restricted legal statuses in different countries.

Chinese Ephedra (Ma Huang) is still legal to buy as a raw herb, liquid extract or ground powder when used for traditional medicine. This species contains potent amounts of ephedrine and pseudoephedrine.

While legal in the USA, it is difficult to buy unless you are purchasing from a licensed herbalist. Some will order it online from China or India, but you run the risk of getting a fake or adulterated product

Clenbuterol also acts as a beta-2 adrenergic agonist and is over 1,000 times stronger than ephedrine. This drug is legal in the USA as a veterinary medication intended for horses or cattle.

It has some of the same effects of ephedrine on airways, causing them to dilate and increasing oxygenation. Clen is also used by bodybuilders in their cutting cycles but has a high risk of dangerous side effects and is not approved for human use.

Sibutramine is an appetite suppressant that has also been discontinued or banned in many countries around the world. Sold under the brand name Meridia, it was discontinued in the US in 2010 due to a risk of cardiovascular issues. [3]

Thyroid hormone (Cytomel T3) is a synthetic drug used to treat hypothyroidism. This hormone plays a role in energy metabolism and can cause significant weight loss in the short-term.

It is a prescription drug in the USA and is not safe when used off-label for fat loss. Use of T3 can cause long-term hormone imbalances and can negative affect thyroid function.

Phenylpropanolamine (PPA) is a sympathomimetic amine, similar in structure to ephedrine. It is commonly found in cough and cold remedies and appetite suppressants. This component was also banned in 2000 but can still be found in analgesic as well as decongestant medications.

The drugs above are commonly taken in higher than recommended dosages by bodybuilders and athletes. While they may increase metabolism and boost energy levels, when used in higher than safe dosages as recommended by medical professionals, results may prove dangerous.

Dangers of Ephedra Supplements

Ephedra supplements may no longer contain ephedrine, but a number of components that mimic the effects. Before considering use of any of these products, be aware of the potential side effects versus the benefits.

Many assume that herbal or natural products are inherently safer than prescription medications. This is not always true and depends on the specific ingredients used and dosages.

For example, caffeine is considered safe when consumed in coffee, teas, energy drinks, and sodas. However, it is considered potentially unsafe when sold in bulk quantities as a powder or oral tablet.

In higher than recommended dosages, caffeine can be toxic and cause serious adverse effects. The Mayo Clinic recommends consuming no more than 400 mg caffeine daily.

Excessive levels of caffeine consumption or overdose may present with:

  • Tachycardia (accelerated or racing heart rate)
  • High blood pressure
  • Nausea
  • Vomiting
  • Myoclonic jerk
  • Seizures
  • Hypocalcemia or hyperglycemia (due to electrolyte imbalances)

According to a 2012 study, toxic effects of caffeine may be present at doses that exceed 15-150 mg per kilogram of bodyweight. [4]

Government agencies, has warned consumers about mislabeling of supplements. Some brands of ephedra extract products have been found to contain ingredients not listed on labels, including the potentially dangerous DMAA. [5]

Not all ephedra extract supplements are dangerous. Some products are made with well-tolerated ingredients and can be used safely if taken responsibly. However, when combining multiple stimulants or using at high dosages the risk of negative reactions increases.

There are other ingredients that can contribute to weight loss without putting excess strain on your heart or cardiovascular system. Before purchasing an alternative to ephedrine supplements, research the ingredients available as well as potential side effects.


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