Ephedrine

Is Ephedrine WORTH It? Dangerous (but Effective) Weight Loss Drug

Ephedrine is one of the most sought-after ingredients in weight loss supplements because it has a long history of producing remarkable results.

Ephedrine diet pills are often touted as the strongest fat burners available, with significant metabolism-boosting, energy enhancing and appetite suppressing effects.

Put these mechanisms together and it’s no wonder that millions of people around the world have taken this natural herbal extract to lose weight and get in shape… But it can also have deadly consequences.

The same effects that make this plant alkaloid from Ephedra Sinica so powerful for fat loss can also put huge strain on your heart and cause serious health risks with long-term use.

What exactly is ephedrine? In medical usage, it’s described as a type of bronchodilator. It’s one of the two primary alkaloids present in the ephedra plant.

Athletes and those seeking accelerated weight loss often turn to supplements containing ephedrine. Ephedrine belongs to a class of drugs known as vaso-suppressors, or decongestants.

It has now been made a controlled substance in many states in the USA, it is banned by the World Anti-Doping Agency, and other sporting organizations and the FDA has issued strict warnings against it. Here’s why. Click here to buy ephedra supplements online legally without a prescription.


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What is Ephedrine

In traditional Chinese medicine, ephedrine – from the ephedra sinica species of the plant – was mainly used to provide relief to those who have shortness of breath or tightness in the chest, due to symptoms common with bronchial asthma.

Ephedrine is available in a variety of forms but most popular supplements today contain ephedra powder found in oral capsules or more solid oral caplets.

In the U.S., the dried leaves and stems of the ephedra shrub have been used for decades in the manufacture of extracts, teas, capsules, and tablets – until 2004, when the FDA banned the substance from the marketplace due to adverse side effects.

The Chinese version known as Ma Huang, contains two powerful alkaloids: ephedrine and pseudoephedrine, both with have stimulating effects on the central nervous, the cardiovascular, and the metabolic systems.

Dozens upon dozens of ephedra products are found throughout the world today, as well as products containing the banned substance ephedrine.

What is it about ephedrine at least in regard to components and activities in dietary supplements that are deemed so dangerous?

Natural herbal names and compounds associated with ephedra may be familiar to some:

  • Ephedra Americana
  • Ephedra Helvetica
  • Ephedra vulgaris
  • Herbal ecstasy
  • Horsetail
  • Mahoàng
  • Mormon tea
  • Yellow Horse
  • Song tuê ma hoàng

To date, according to the Mayo Clinic, roughly 40 ephedra species are available on the market today.

Do not confuse ephedrine with epinephrine. Ephedrine is a primary alkaloid found in the ephedra plant.

Epinephrine is a neurotransmitter hormone also known as adrenaline. It’s found in Epi-pens, used in the treatment of anaphylactic shock or severe allergic reactions, and other purposes in medical treatment scenarios.

Ephedrine Review and History of Use

The Latin name for the plant from which ephedrine is derived is, Ephedra sinica, is also known by a number of other names including ephedra, Chinese ephedra, and Ma Huang.

The source of ephedra is a plant (evergreen) native to Central Asia and portions of Mongolia. Another species of ephedra is also found in some locations throughout the southwestern US, known as Ephedra viridis. This species is less potent that the Chinese sinica (Ma Huang) species.

In the past (1800s) the Ephedra viridis species was known by pioneers as Mormon tea, Cowboy tea, and Squaw tea, among others.

The compound has been used in China for centuries in the treatment of anything from headaches, to colds, flu, nasal congestion, and asthma-like conditions.

Use of ephedrine was relatively popular throughout the West through the 1940s and 50s as an oral asthma medication. In the 1970s, 1980s, and 1990s, it grew in popularity as a weight-loss drug and dietary supplement.

For many years, ephedra and its alkaloids (ephedrine and pseudoephedrine) were available on the market, mainly sold as a dietary supplement promoting fast weight loss. It was also highly promoted as an energy booster and as an athletic performance enhancer.

Since 2004, ephedra alkaloids have been banned in dietary supplements and weight loss products by the U.S. Food and Drug Administration. [1] The reason for the drug’s banishment was due to increasing reports of serious side effects and adverse reactions.

Further studies have determined that (per the FDA), efficacy in regard to benefits and ephedra/ephedrine usage is limited only to relatively short-term weight loss, mainly for individuals who only need to lose a few pounds.

It is not deemed especially effective nor recommended for those who are overweight or obese. The side effects and adverse reactions of ephedra – including cardiovascular events, were deemed to more than outweigh the benefits of use, hence its discontinuation.

However, traditional Chinese herbal remedies using ephedra extract are not banned. [2]

While the Food and Drug Administration does regulate ephedrine, it is not regulated by the Toxic Substance Control Act (TSCA). Furthermore, it is defined as a List One (1) chemical by the Drug Enforcement Administration. [3]

What triggered the focus of attention on ephedrine, and ephedra/Ma Huang, overall, was the 2003 death of a well-known major league baseball player in the United States known to use the substance.

Even so, and according to the Mayo Clinic, the FDA had by that time amassed nearly 1,000 reports regarding potential toxicity and 22 deaths believed to be associated with ephedrine. [4]

By late 2004, ephedra was effectively banned in the United States.


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Mechanism of Action

Ephedra works through stimulation of various aspects of the central nervous system, and therefore function of the heart and the lungs due to the presence of the chemical known as ephedrine.

The primary mechanism of action of ephedrine is its ability to reduce swelling in the nasal passages and sinuses. This is in conjunction with its ability to relax or dilate blood vessels that thread their way through nasal passages.

This mechanism of action is also effective in widening the airways in the lungs including the bronchi and bronchioles, relieving constriction that enables greater intake of oxygen. The bronchodilation effects are deemed quite effective in the treatment of asthma.

According to one manufacturer (AKORN) ephedrine sulfate injections (50 mg per milliliter) specifically target major organs such as the heart and the lungs as well as a central nervous system. [5]

Ephedra sinica not only stimulates the nervous system but can also constrict blood vessels. It has long been rumored that when combined with caffeine (coffee, soda, or other source of caffeine), ephedra does benefit in triggering weight-loss – though short-acting and short-term in nature.

Major concerns in regard to usage have been focused on potential negative influence on certain cardiovascular functions.

Ephedrine Results

When asking, “How does ephedrine promote benefits” in regard to goals, one must also ask about results – verifiable results.

As with any prescription-strength drug or over-the-counter product, individuals may experience different results. When it comes to ephedrine, it has been studied for its potential to promote weight loss. The ephedra has been shown to promote some weight loss when used with other sources of caffeine.

However, research as well as studies are not only limited, but have produced mixed results.

The mixed results are typically caused by the wide variety of products on the market as well as the amount of ephedra – and caffeine – found in those products.

In regard to ephedra results for treatment of asthma, the ephedrine and pseudoephedrine, chemicals are classified as bronchodilators. It has been used for years in the treatment of chronic lung diseases as well as some asthma conditions in pediatric and adult patients.

Inhalers such as albuterol however, are often recommended over use of ephedra due to concerns of the side effects associated with ephedra-based compounds.

Very little research has verified that ephedra/ephedrine promotes benefits in regard to athletic performance.

About the Ingredients

In traditional Chinese medicine the herbal plant (Ma-Huang) is composed of numerous compounds, including the primary stimulants ephedrine and pseudoephedrine, available in a number of dietary supplements and over-the-counter products. In the United States, ephedrine is monitored by the FDA, as its synthesized from ephedra.

It produces a similar in mechanism of action as phenylpropanolamine, an appetite-control drug that is also banned in the United States, commonly known as norephedrine. It’s given this name because the ephedrine’s basic methyl group has been substituted by a hydrogen molecule.

It’s also similar in mechanism of action to amphetamine, a controlled stimulant, which defines norephedrine whose hydroxyl group has been substituted by a hydrogen.

Lastly, pseudoephedrine is an isomer of ephedrine, where the hydroxyl group is located on a different side of the base molecule.

Ephedrine dosage information provided by Drugs.com (Ephedrine dosage) specify a number of different forms and milligram strengths: from 0.5% to 1 m/mL and up to 8mg/250mL-D5%.

Instructions For Use

When it comes to instructions for use of ephedrine, advice differs depending on its form as a compounding powder or oral capsule. The FDA cautions individuals against using ephedra because even small doses can affect users differently.

Medical professionals caution against dosages that exceed 32 mg per day, which may triple risk of hemorrhagic stroke inside the brain. [6]

In the treatment of asthma (prescription) as well as over-the-counter use of Ma Huang, caution is always recommended. Ma Huang (Ephedra sinica) may be beneficial in the treatment of asthma, but dosage will be dependent on its alkaloid content.

For example, and in general scenarios, dosage of ephedrine averages anywhere from 12.5 mg and up to 25 mg two to three times daily.

Traditional herbalists may recommend dosages of 8 mg and up to 100 mg of ephedra orally three times daily! While this is strongly recommended against, again it depending on the species of ephedra, how it’s prepared, and other ingredients combined with the ephedra extract or its alkaloids.

An over-the-counter product containing ephedra extract typically recommends anywhere between 12.5 mg to 25 mg on average every four to six hours. Users are not to exceed 150 mg in 24 hours. [7]

For those seeking enhanced athletic performance, average recommendation is 1 mg per kilogram body weight taken orally approximately 90 minutes prior to exercise. This dosage can be taken one time daily for up to four weeks.

The most popular use of ephedra/ephedrine has been for its potential benefits for weight loss. In most scenarios, 2 g of ephedra extract has been recommended. The dosage is one time daily for no more than eight weeks. Or, 20 mg to 50 mg ephedrine taken three times daily for two to three months.

Note: The dosages found above are commonly found on a number of different ephedra compounds, products, and stacks. Many are considered by medical experts to be excessive. Always start at very low doses for a couple of weeks to see how the body reacts to it.

How much does Ephedrine Cost?

Costs associated with ephedrine depends on how you get it. For example, with a prescription, and the form of the drug, prices will vary. In general, the injectable solution averages in a range of $13-$38.

The prescription-only injectable solution in the US is most commonly provided in a 50 mg per milliliter quantity (10 x 10 x 1 milliliters) for an average cost of $134, although some locations may charge approximately $375.

A 25 (25 times 1 mL) ephedrine injectable solution is a bit lower due to quantity, averaging approximately $9.50 per unit for an overall price of $235.

The intravenous (IV solution – 50 mg per milliliter) costs approximately $400 for 10 mL of product.

In oral capsule form, cost averages $30 for 25 mg oral capsules (100 capsules) [5]

Over the counter dietary and/or nutritional supplements are also commonly found. Just a few product names include:

Again, each brand may come in different milligram strength and with different ingredients, so dosages and costs will vary.


  ECA Stack
 

ECA Stacks

As in the past, bodybuilders today have the capability of purchasing ephedrine from numerous sources. The compound is commonly stacked with caffeine as well as aspirin, known as an ECA stack.

A number of brands and products are available over-the-counter from sports nutrition supplement suppliers. Known as fat burners, these supplements are available in a variety of milligram strengths. Some contain 200 mg tablets of caffeine and 81 mg tablets of baby aspirin.

Aspirin is often included as a component to the combination of caffeine and ephedrine because aspirin is a natural anticoagulant, and ephedrine has been noted to promote blood clotting.

Others contain stronger doses of aspirin. As some individuals are more sensitive to aspirin and others, a member of supplemental products today replaces the aspirin with other components including White willow bark or fish oil.

Before using, be aware that the combination of stimulants can prove overwhelming for some users. Beginners should always start at very low doses.

Because ephedra is banned in the US, some athletes attempt to create their own version of an ECA stack through combinations of herbs including Ma Huang, Yohimbine, or other herbal ingredients in addition to high levels of caffeine.

Before doing so, be aware of the dangers of “mixing and matching” more than one stimulant at a time, as this increases the risk of side effects.

Ephedrine Side effects

Side effects of ephedrine vary between individuals. Not every user will experience side effects, but among the most common include:

  • Headaches
  • Dizziness – often accompanied by blurred vision
  • Tremors in the hands, often accompanied by feelings of increased anxiety
  • Nausea
  • Lack of appetite
  • Restlessness, sometimes inability to sleep

Among the more serious side effects, and which should be assessed by a physician as soon as possible include:

  • Severe allergic reaction (anaphylactic shock). This condition may appear with or without hives or rash, but include difficulty breathing, and obvious and sometimes extreme swelling of the eyes, the lips, and the tongue. Airway passages in the throat can also become constricted, causing extreme difficulty in breathing. If left untreated, can contribute to cyanosis, or lack of oxygen which may turn the nail beds and the lips blue. This can contribute to a severe inability to breathe properly. Anaphylactic shock is a very serious condition and should be treated immediately with application of an Epi-pen and or a trip to the closest emergency room.
  • Serious and often severe “excitation” of the nervous system
  • Tachycardia – pounding and racing heart. An irregular heartbeat (arrhythmia) is also a possibility.
  • Other cardiovascular effects including high blood pressure (hypertension), heart attack, and possible stroke
  • Potential for affecting blood sugar (glucose) levels. Anyone diagnosed as prediabetic, diabetic, or struggling with a metabolic or hormone disorder should avoid, or at the minimum, be monitored by their physician to ensure safety.

Potential users should be aware that ephedrine, ephedra, or any variation of the component may exacerbate previously diagnosed conditions including kidney and heart disease. For individuals diagnosed with any type of seizure disorder, it may also increase the frequency and severity of seizures.

The list of side effects and warnings associated with ephedra/ephedrine are extensive. The compound may also interfere with other prescription as well as over-the-counter drugs including antidepressants (monoamine oxidase inhibitors or MAOIs).

Interactions may also occur. It is believed that ephedrine/ephedra may disrupt the liver’s ability to process certain drugs. This is due to its influence on a specific liver enzyme (cytochrome p450), triggering serious reactions.

Negative interactions may also be experienced with use of ephedrine/ephedra products in conjunction with:

  • Diuretics
  • Tricyclic antidepressants
  • Anti-inflammatory agents
  • Cholesterol drugs
  • Aspirin
  • Hormones
  • Other weight-loss drugs

Ephedra may also negatively interact with other herbal and over-the-counter dietary supplements.

Ephedrine for Women?

Women should use caution before using any form of ephedrine or any supplement with Ephedra or its alkaloids. It’s rated under Category C, meaning that some studies have been conducted regarding reproduction. In these studies, some adverse effects on development of the fetus have been noted. While controlled and adequate studies have not been performed on pregnant human females, risk of use has not been ruled out.

While some benefits of use may be applicable in certain circumstances, women should always confer with their obstetrician prior to use.

A very few cases have been reported of metabolic acidosis in newborns post-delivery following their mother’s use of the drug prior to delivery. Basically, use of ephedrine by pregnant women is discouraged unless required for medical purposes.

The same applies to women who are breastfeeding. Components of ephedrine can be excreted into mother’s milk, and may produce irritability and difficulty sleeping for those infants.

Pros and Cons of Use

Not long ago, products containing ephedra/ephedrine were extremely popular, most commonly for those desiring quick weight loss. It was also extremely popular among bodybuilders looking for a boost in energy.

Because of its mechanism of action as a stimulant, it does have the potential to increase metabolism through its thermogenic effects. When taken with caffeine, the supplement grew in popularity as one of the most beneficial weight loss and energy boosting over-the-counter supplements on the market.

However, even low doses of ephedra/ephedrine can adversely affect certain individuals, so anyone interested in trying ephedrine should start at the lowest dose possible to see how the body reacts to it. In such cases, five to 10 mg of ephedrine is a good starting point.

In regard to safety considerations, it is recommended that any user be fully aware of his or her physical condition prior to use, especially when ephedrine is combined with caffeine for accelerated benefits. Anyone diagnosed with kidney, metabolic, cardiovascular, or central nervous systems issues or disorders should proceed with extreme caution.

While there is no disputing the fact that ephedrine/ephedra does promote weight loss and increases energy and metabolism, it is rarely used appropriately by bodybuilders, athletes, or even individuals seeking the fastest route to weight-loss. It is due to this misuse that the product was ultimately banned by the FDA in 2004.

Conclusion

While large numbers of individuals did achieve some benefits with use, and it has promoted some (minimal) weight loss for those who are overweight and obese, it is not intended as a substitute for diet and exercise, which promotes long-term weight-loss maintenance as well as overall health and wellness.

Because of its known side effects, from mild to severe, it continues to be banned by sporting organizations around the world, including the International Olympic Committee. Nevertheless, it continues to be sold and used today by individuals around the world.

Ephedrine continues to be a popular component for weight-loss and increased energy, and when used appropriately, can and does provide benefits. It’s the misuse and overuse of ephedrine that requires caution.

Take the time to research not only bodybuilding websites for user comments, but medical and scientific resources as well.


  Ephedra Fat Burners
 
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