Should We All Take Metformin?

Metformin (Glucopage) is a wonderful drug that bodybuilders use for a very long time, nothing very spectacular just another drug in the bodybuilders toolbox. I wrote a few times before about this drug, in 2012 about its potential to burn fat and in general in 2014.

But this drug is studied intensively and in 2015 this article in The Telegraph increased the interest in Metformins ability to increase life-span and improve quality of life.

The Food and Drug Administration (FDA) always maintained that aging is not a disease and most scientists have taken the same position. But because many studies confirmed that Metformin was able to slow down aging and prevent many conditions linked with aging, general consensus changed. Belgian researchers tested metformin on the tiny roundworm C.elegans the worms not only aged slower, but they also stayed healthier longer. They did not slow down or develop wrinkles. Mice treated with Metformin increased their lifespan by nearly 40 per cent and their bones were also stronger. Last year Cardiff University  found that when patients with diabetes were given the drug metformin they in fact lived longer than others without the condition, even though they should have died eight years earlier on average.

To analyze the advantage outside treatment of diabetes, the Food and Drug Administration has green-lighted a clinical trial in the U.S. for what has become known as the Targeting Aging with Metformin (TAME) study. The researchers will give Metformin to about 3.000 elderly people, who either suffer from or have a high risk of developing diseases like cancer, heart disease, or cognitive problems. They'll then track them over six years to see if the drug prevents aging-related diseases that were not pre-existing. They'll also be looking to see if it prevents diabetes and lengthens their life spans. It will be a double-blind, placebo-controlled study. In June, the researchers held a meeting with FDA officials in order to convince them that if the study results are positive, they will have proved that aging is a disease that can be treated with drugs. Recently, a spokesperson for the FDA said the agency is willing to seriously consider the idea.

Metformin increases the number of oxygen molecules released into a cell, which appears to boost robustness and longevity. It works by suppressing glucose production in the liver and increasing insulin sensitivity, therefore benefitting patients with type 2 diabetes.

Metformin and Bodybuilders

Bodybuilders use metformin because it gives them several benefits, insulin sensitivity not only decreases with age, but also as a result of the use of exogenous use (injects) of growth hormone and insulin. Metformin helps keep muscle cells sensitized for insulin that the body produces and allows the muscle cells to load bigger amounts of nutrients. As a result bodybuilders claim to get tremendous pumps when using metformin. When metformin is used with a high carbohydrate diet, the user experiences these “full muscles.” At the same time metformin de-sensitizes fat cells to insulin’s effect which prevents fat from being deposited, so the bodybuilder get full benefits from carbohydrate loaded meals, without worrying to end up storing fat. Also helps on cheat days. Most users claim appetite suppression, which helps when a bodybuilder wants to shed fat. All benefits and sides can be used or avoided with timing the dosing. More on that later.

A list of the benefits of Metformin:

Lowers blood cholesterol, triglycerides, and beta-lipoproteins.

Reduces development of atherosclerosis.

Reduces insulin levels.

Increases hypothalamo-pituitary sensitivity (which declines with age).

Improves cellular immunity.

Reduces incidence of chemically-induced cancer in rats.

Enhances activity of anti-cancer drugs.

Suppresses the growth of some tumors.

Increase maximum lifespan in experimental animals and hopefully in humans

Side Effects

One of the side-effects is that the use Metformin after a few weeks leads to loss of testosterone, the average loss of testosterone in men is 60%. DHEA first has to be converted to Androstenodione, later to androstenodione than to testosterone, metformin decreases 3beta-hsd the enzyme responsible for the conversion.

Bodybuilders that are AAS and older people that use it for anti-aging - life-extension or HRT/TRT mostly inject testosterone or take Andriol (testosterone undecanoate) or Proviron (mesterolone) or avena extracts.

It is known that the metabolism of homocysteine depends on the vitamins B6, B12 and folate and furthermore that metformin reduces serum vitamin B12 levels. Research showed that homocysteine levels increased moderately but significantly by 7.2% (after 12 weeks) and 13.8% (after 40 weeks) in the metformin group, whereas serum vitamin B12 levels decreased by 13.4% (after 12 weeks) and 17.7% (after 40 weeks), respectively. Serum folate levels did not change after 12 weeks, but decreased by 8.0% after 40 weeks. When you take some extra B12 this problem is solved. Bodybuilders and other recreative users of Metformin can rotate usage.

Another side-effect made users post:

“Be careful w/ that stuff - gives u the shits in ways you can't imagine.”

“It blocks fat absorption, read: wear a diaper. you WILL have wet oily farts. you WILL think you shit yourself. DO NOT wear white pants.”

“The "mud-butt' you experience is a common side effect, along with GI upset, nausea and cramping. One way to combat this is to start at a low dose and slowly titrate it up. However the maximum dose for an adult is 2500-2550 mg with a normal dose around 850 mg 2x-daily.”

A wise advise your body is able to adapt to many drugs, by example just look at alcohol or caffeine, it can really make you sick if you start with a large dosis, if you are not used to it. The same is true for, in this case metformin. Just start with a quarter of a 500 mg pill, 125 mg and then work your way up. Most Bodybuilders just take 3 times 500 mg.

Dosing

Metformin has been used in Europe since 1957. In 2006 35 million prescriptions (for diabetics) were filled, many users, diabetic as well as bodybuilders share their experiences online on the discussion-forums. Some remarks below.

There have been no human studies to identify the optimal dose of metformin that is needed to duplicate the beneficial gene expression effects.

For people who want to derive the many proven health benefits of metformin, it might be prudent to follow the dosage schedule used by Type II diabetics. According to the Physician's Desk Reference, the starting dose should be 500 mg of metformin twice a day. (An alternative option is 850 mg of metformin once a day).

After one week, increase the dose of metformin to 1000 mg as the first dose of the day and 500 mg as the second dose. After another week, increase to 1000 mg of metformin two times a day. The maximum safe dose described in the Physician's Desk Reference is 2550 mg a day (which should be taken as 850 mg three times a day).

According to the Physician's Desk Reference, clinically significant responses in Type II diabetics are not seen at doses below 1500 mg a day of metformin. Anti-aging doctors, on the other hand, have recommended doses as low as 500 mg twice a day to healthy non-diabetics who are seeking to obtain metformin's other proven benefits such as enhancing insulin sensitivity and reducing excess levels of insulin, glucose, cholesterol and triglycerides in the blood.

It could be the dosage range is highly individualistic in healthy people, meaning some may benefit from 500 mg twice a day, while others may need 1000 mg twice a day for optimal effects.

The way metformin is taken will vary for bodybuilders. Full muscles can be achieved if 500-1000 milligrams (mgs) are taken within 1 hour after a large carbohydrate meal. The more carbohydrates there are in the meal, the higher the dosage should be taken, never exceeding 1500 mgs at a time. Nevertheless, metformin can be taken with as many high carb meals as you wish.

 At least 100 grams (g) of carbs must be taken for every 500 mgs of metformin. Otherwise hypoglycemic symptoms may occur.

Some users:

*“I started with a very low dose of 125mg (1/4 of a 500 mg tab), and went up to 850 mg (one 850 mg tab). Now I always take it at night, preferably before dinner, since it upsets your stomach a little bit, when you start taking it, or when you increase the dose.”

 *“Have lost 12 pounds in less than 3 weeks, incredibly, most of them fat, have retained muscle tone, and my abs are getting defined again. My skin feels incredibly tight, thus improving the "ripped" look. Even my face looks slimmer, younger, now.”

*“As metformin reduces carbohydrate absorption, be sure not to eat sugary foods, as glucose will remain longer in your intestine, causing gases, heartburn, or softening your (but not to the point of causing diarrhea). Using it only at night, you feel almost no side effects, while cutting and preserving your muscle a lot.”

* “If cutting, I still have a post work-out shake, and works very well at this time. When cutting I also cycle my carbs, and metformin can put you in a state of ketosis quite quickly.”

*”When bulking, well I will probably use 4/5 pd, I don’t bother with my morning meal, no particular reason I just think you probably get a nice insulin response at this time anyway.”

*”After this any carb/pro meal will use one, pwo, then the meal following the shake. I also eat a fair amount of carbs before bed so will use one then also.”

*”As to benefits well it is all subjective, but I am fairly sure that you can ingest more food, and send it to your muscles with less fear of any spilling over into fat.”

*”Sides I don't get any but when I first used them they did give me slight wind shall we say. I tend to use 2 weeks on, and then 1 week off. I'm not sure if it's required but I do it for peace of mind.”

Half Life

The half-life is approximately 2-6 hours. However, there are slow releasing extended tabs available. Bodybuilders should stick to the faster acting version.

Supplement companies are not allowed to sell pharmaceutical drugs, thus as soon as a thread appears on the forums about Metformin someone from a supplement company will react that Berberine, or other compounds sold by XXX, outperforms Metformin blah blah..

Metformin with GH and insulin, what users say:

“I have Dianben 850mg Metformin tabs. But every time I use one, I get the feeling that my stomach is full, together with nausea this really sucks. what do you guys do? how do you take these tabs? Oh there is something else that could be interesting for you to know. If you use Metformin alone it doesn`t work. You can believe me, you have to use it together with INSULIN. I don`t use Insulin, but Glipizide, an oral insulin. some people use it with hGH or/and t3/t4 and have good results too. I think the reason why metformin doesn`t work alone is that it has the effect you mentioned, it makes the insulin(your body produces) work better, as a reaction your body does produce less insulin, so it works not. Use insulin, or an insulin booster, that`s better.”

“Definitely take it with carbs for insulin or without for ketosis. I WOULD NOT inject insulin while using metformin; insulin lowers blood glucose & so does Metformin, you run the risk of a hypoglycemic shock.”

“Not sure about oral insulin stimulators and metformin. Be careful with oral insulin stimulators they can whack your beta cells good and possibly lead to type I diabetes I. E. you shut down your own insulin production for good? just theoretical, don't know of any documented cases.”

“Metformin (Glucophage) is the shit and it's a whole lot safer than insulin. Bodybuilders use it to replace insulin in a steroid cycle. The idea is to increase transport of nutrients, amino acids, fatty acids and carbs into muscle cells for storage. Metformin can do this , but with fewer side effects and risks then slin. The storage of protein and nutrients in muscle cells is the desired effect. A fuller, harder and more defined body is the goal.”

“You got to supplement with a carb rich diet to activate the metformin and take along with creatine mono. Most BB take 850mg 2 times a day. Morning and at night. I think they come in 500mg to if I remember right. The tablet form makes dosing more accurate and convenient then insulin.”

“Like Victor said "lactic acidosis" is real. You must be a hell of a water drinker when using this. Now there is a XR version which is time released. You can get this on the internet pretty easily and is extremely cheap. The XR version can be taken once a day.

It's a better alternative to actual insulin supplementation and much less dangerous but what Victor said is something to consider.”

Anti-Aging

Does the idea of living until the age of 120 sound outlandish? According to some recent findings, it might not be so far-fetched in the near future. 

Medical researchers have uncovered what seems to be an anti-aging pill that could ward off illnesses associated with the aging process, such as Parkinson's and Alzheimer’s. The drug, Metformin, actually isn't new—it's been used to treat type 2 diabetes for years (it's the world's most widely used drug for the disease). 

Metformin, which suppresses glucose production in the liver and increases sensitivity to insulin according to Inquisitr, reportedly has been prolonging the lives of roundworms, as well as a few strains of mice. Experts at Cardiff University in the U.K. have also released some shocking evidence of the pill's anti-aging abilities, finding that those treated with Metformin for diabetes live longer than normally expected, and sometimes longer than those who don't suffer from diabetes at all. 

Before you go jumping for joy, scientists aren't exactly sure if the drug really does increase a human's lifespan. To test the theory out, researchers will be conducting a study in the U.S., which "will involve 3,000 adults aged 70- to 80-years old, with known risk of cancer, heart disease, and neurodegenerative diseases that cause cognitive impairment," according to Inquisitr.

If the tests wind up being comparable to the roundworms and mice, then 70-year-olds who use the drug could potentially have the same health and vigor as people in their 50s. 

"I have been doing research into aging for 25 years and the idea that we would be talking about clinical trial in humans for an anti-aging drug would have been thought inconceivable," professor Gordon Lithgow, the lead researcher in the study said. "But there is every reason to believe it is possible. The future is taking the biology that we've developed and applying it to humans."

If this potential breakthrough proves to be true, you may be able to meet your great-great grandchildren one day.