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AICAR: the couch potato pill

Can a pill really turn couch potatoes into athletes?

I have been asked time and time again over the last decade whether or not a pill or substance was in existence that could replace exercise. I always laughed and answered “no”. I hate to recant this statement, but I may have been wrong.

Recent scientific studies have helped the medical community make progress in the treatment of many modern-day diseases that were untreatable mere decades ago. Professionals in the medical community have learnt that many of the methods used to treat these diseases also apply to increased athletic performance. This is how most performance enhancing drugs enter the mainstream to begin with, as medical studies involving a drug that was intended to treat disease showed an increase in performance in some way.

In 2008 Ronald Evans, a developmental biologist at the Salk Institute in La Jolla, CA was conducting research to find a cure for obesity and diabetes. He stumbled across a substance called AICAR (acadesine), a synthetic adenosine monophosphate (AMP) analog that activates activated protein kinase (AMPK), which plays a role in cellular energy homeostasis.

During a study headed by Evans at the Salk Institute, sedentary mice were given AICAR three times a week over a four week period. These mice were tested on a treadmill after this four week period and showed a 44% increase in endurance despite not having done any exercise during that period.
Another group of sedentary mice were not given the drug during the same period and, unsurprisingly, showed no change in endurance.

Endurance training produces metabolic and structural changes within muscles.

The study lead by Evans showed that AICAR can produce muscle reformation, which is influenced by gene expression, increased cellular energy and muscle fibre composition.

AICAR displayed the ability to transform type-ll muscle fibres (which are more common in sedentary people) to type-1 muscles in sedentary mice. Type-1 muscle tends to use fatty acids as fuel instead of glycogen, which subsequently leads to fat loss. The abundance of cellular energy-producing mitochondria means that this type of muscle is very resistant to fatigue. Type-II muscle fibres, on the other hand, are more prone to fatigue while relying on glycogen instead of fatty acids for fuel.

So, while these mice remained sedentary, they became leaner, stronger and developed more endurance while taking AICAR.

Can you imagine reaping the benefits of exercising without lifting a finger? This study has basically shown that AICAR can achieve this in mice.

There is a big downside to AICAR though, and that’s price.

AICAR is not FDA-approved, so it is not available to the public. This drug is only available for research, and not for human consumption. But even if you were to get your hands on it you would have to shell out close to $30,000 a month to get the 3mg dose, which needs to be taken three times per week. That is a hefty price tag to pay to lay on the couch instead of exercising.

It is hard to say how this drug would work in humans.

The study by Evans showed promising results on rodents, but no clinical trials have been completed on humans. Most steroids and other performance-enhancing drugs have been toyed with by bodybuilders, athletes and trainers to come up with the most effective dose and determine which drugs are the most effective. That is not the case with AICAR. And as long as the price remains that high we may never know how effective it can be when used by humans.

I know that this is sad news to every couch potato out there, but then again you could cash in your retirement plan and give it a go. We would then have much more data on humans and then maybe we could turn marathon TV watching into a sport.

Even though it is not known whether this drug is beneficial for humans use, it is now banned by the World Anti-Doping Agency (WADA) and Evans also devised a method for detecting this drug following his studies. I am not sure if he did this because he felt that AICAR is effective in humans and could be used to gain an edge in sports or whether he just wanted to shine a spotlight on the drug he researched.

The research done with AICAR on mice was shown to be very effective in increasing endurance in mice. In theory this could possibly be effective in humans that cannot exercise due to debilitating diseases.

Nothing has been show to indicate that this drug would increase athletic performance or benefit anyone that already exercises as the studies were conducted on sedentary mice only.

This drug has therefore been labelled the “couch potato drug”.

This drug may mimic some of the same effects of exercise, but it will never offer all of the benefits that exercise offers.

For instance, it will never alleviate stress and tension, and it won’t give a person the satisfaction that comes from achieving a personal and/or physical goal. People who refuse to exercise usually refuse to eat well. As such, if someone is willing to spend $30K a month to replace exercise I am sure there are many other shortcuts in their daily life. This lack of real exercise, poor eating habits and the desire to always find shortcuts will lead to a life of poor health and disease that no drug can cure.

So, while AICAR has generated quite a buzz on the Internet over the past couple of years, and despite the fact that the research looks good, I think the drug is a poor option, especially considering the cost, lack of research in humans and the unknown side effects.

Filed Under: Supplements  Tagged: AICAR

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