The surprising truth about Metformin

The “natural” blood-sugar remedy that had been sidelined for far too long

What I’m about to tell you may be shocking. And it’s sure to ruffle the feathers of many of the “natural know-it-alls.” But the science is clear, so I’m not afraid to say it:

If you have unmanaged Type II diabetes, you should consider the drug metformin as a first line of treatment.

And you won’t get the full story anywhere else, since the natural health industry wouldn’t be caught dead recommending a drug. So, please allow me to do the honors here…

Think of it as your emergency
get out of jail free card”

Diabetes is deadly. High blood sugar coursing through your body destroys your eyes, kidneys, heart, brain, and more. So the sooner you bring it down the better. (Just like high blood pressure, for which I also recommend tried and true medications as a first-line treatment for unmanaged hypertension.)

And in this case, the science is clear—the drug metformin has been proven safe and effective for most people. And since it’s now a generic drug, it’s highly cost effective, too.

Now don’t get me wrong…I’m not saying diet and exercise isn’t important. In fact, they’re the best means for preventing and even reversing Type II diabetes entirely. Something metformin can’t do. And there are certainly dietary supplements that can help with maintaining healthy blood sugar (like berberine).

But Type II diabetes doesn’t develop overnight. And let’s face it, changing the habits and consequences that got us there in the first place isn’t an overnight task either. So if you need additional help, this is one rare instance where you shouldn’t be afraid to look at a mainstream therapy.

And when an option this effective comes along to help kick-start your efforts safely (when taken properly), even if it is  a drug…it’s something you should consider seriously.

Indeed, it’s rare to find such a safe and effective “drug” as the popular diabetes treatment metformin. In fact, this is one “wonder drug” that is steeped in natural history—like aspirin or digitalis—and was in “historic use” for centuries.

One of Nature’s wonder remedies

Originally, metformin was known under the trade name Glucophage. But it’s now been around long enough to go off patent and become generic. Which means it meets one of my primary requirements when it comes to taking a drug: Make sure it has undergone the seven-year post-marketing surveillance period required by the FDA. Which means it’s been proven safe by the tens of millions of patients who have taken it over at least seven years, and now much longer.

As a drug it was actually first synthesized in the 1920’s. However, it was quickly overshadowed by the Nobel prize-winning discovery of the role of insulin in the treatment of diabetes (see page 1). So metformin was swiftly set aside for half-acentury.

However, its history goes back much further…where it was known throughout Europe as a traditional folk medicine for centuries. That’s because this drug actually stems from a flowering plant called Galega officinalis, more commonly known as French lilac or goat’s rue. The active ingredient is a chemical biguanide known as Galegine, after the botanical name of the plant.

As an herbal extract, Galegine was used traditionally to treat people with polyuria (excessive urination due to excess sugar in the urine) and sweet odor on the breath. Today, we recognize these as two leading symptoms of untreated diabetes.

References date as far back as ancient Egypt and it was in common use in Medieval Europe. The herbal treatment was featured in an English medical treatise by Culpepper in the 17th  century. And it was studied at the University of Edinburgh, a leading medical center of the 18th century from which the first medical school in America was established in 1765. It has also been used in Asia to treat influenza and is said to have antibiotic, antiviral, antimalarial, and antipyretic (fever) activities.

With such a long history as a potent herbal remedy, it’s actually shocking that it took so long to be used for a major modern medical problem like diabetes!

So after languishing during the Great Depression and World War II, the French finally developed Galegine, or metformin, for clinical use in 1957. It was approved the following year in the United Kingdom, and made its way to Canada in 1972. But it was not approved by the FDA in the United States until 1994. And that was only after a U.S. drug company (Bristol Myers Squibb) acquired a French firm that manufactured the drug.

Getting to the root of the delay…

One reason for delayed approval in the U.S. was due to concern over a very rare side effect called lactic acidosis. This is a metabolic condition that results in a buildup of lactic acid in the muscles due to changes in levels of sugar and oxygen.

A poorly advised campaign was undertaken by the public advocacy group, Public Citizen, called “Do Not Use Glucophage.” But when all the blowing smoke, and smoke-blowing, began to clear, a study found that the risk of this metabolic disorder was actually ten times higher with older diabetes drugs being used at the time (since discontinued). And eventually more studies observed no difference in risk between diabetics using the drug and those not using the drug— because the problem had actually been due to underlying medical conditions among diabetic patients, and not the drug itself.

So what’s the final conclusion regarding the risk of lactic acidosis?

If you have underlying kidney or liver conditions, then metformin is not for you.

Most side effects are minimal,
and easily managed

The risk of lactic acidosis aside, the most common side effects associated with taking metformin are diarrhea and gastrointestinal upset.

But this is typically when first starting the drug, and rarely persists. And, because it lowers blood sugar (hence its use for diabetes) it may cause symptoms like tiredness or weakness, unless and until the dose is adjusted and/or the body adjusts on its own.

Relatively speaking, compared to most other drugs, these side effects are minimal for the benefits you may gain. And are easily managed by monitoring and adjusting dosage accordingly as with any medical management for diabetes.

At the same time, metformin is one of the few drugs that are safe for people with congestive heart failure.

Though it can interact with certain blood pressure medications, so be sure to check with your doctor.

All that said there are two concerns you need to know:

1. You must supplement with vitamin B12.

Research has found that prolonged use of metformin can cause a deficiency in vitamin B12. Especially in those suffering from peripheral neuropathy. And unfortunately, the NIH and many doctors have yet to catch up to the research on this risk. So to be safe, you can supplement with a high-quality B vitamin daily for as long as you take metformin.

Look for a vitamin B complex that contains 100 mg each of vitamins B1 (as thiamine), B2 (as riboflavin), B3 (as niacinamide), B5 (as pantethene), and B6 (as pyridoxine) and 1,000 mcg of B12 (as cyanocobalamine).

And ask your doctor to check your vitamin B12 levels regularly. If you are unable to absorb sufficient B12, injections may be administered by your doctor. These doses may also help to enhance your immune system.

2. Beware of eating grapefruit.

As with other drugs, as I reported in the November 2012 issue of Insiders’ Cures, eating grapefruit may interfere with the effectiveness of metformin. So it’s best to avoid grapefruit (which you should be doing now, to help reverse the disease in the first place).

Unexpected—and very promising—benefits

Metformin has ultimately gone on to be the most widely prescribed drug for diabetes in the world with over 120 million people taking it today. And with so many people taking the drug, some surprising beneficial “side effects” are now being observed.

In addition to controlling blood sugar, it has now been proven to prevent the common cardiovascular complications of diabetes, such as heart attacks and strokes. It also promotes healthy circulation to the limbs, kidneys, and eyes. And is the only diabetes drug that does not cause weight gain. (In fact, it’s now being studied for use as a weight loss drug.)

It also helps reduce LDL cholesterol and triglyceride levels in the blood without the dangerous side effects of statin drugs. These are beneficial effects that are likely

associated with metformin’s effects on reducing blood sugar and helping to regulate normal metabolism.

But beyond these healthy effects,
there is more…

Metformin is now the treatment of choice for the increasingly diagnosed condition of Polycystic Ovarian Syndrome in women of all ages. It also appears to be effective in the treatment of Multiple Sclerosis.

It is even being recommended as an “anti-aging” drug by some. This is likely due to the claims that it helps maintain healthy hormone levels such as estrogen in women and testosterone in men.

MD Anderson Hospital, the largest cancer center in the country, has observed that it lowers the risk of pancreatic cancer (notoriously difficult to treat) by five times. And it reduces overall cancer rates, including cancer of the breast, colon, lung, ovary, and prostate. Most of these cancers can be difficult or impossible to treat by conventional means.

Regarding the remarkable effects on lowering pancreatic cancer, I might speculate that by keeping blood sugar levels low, metformin reduces any effects to stimulate the pancreas to produce ever more insulin in Type II diabetes to try to counter high blood sugar or insulin resistance in the tissues. Thus, it doesn’t promote the growth of pancreatic cells, some of which are responsible for producing insulin.

Several mechanisms are being investigated on the anti-cancer effects of metformin. Canada appears to continue to be ahead of the U.S. and is leading the way with clinical trials on using metformin to actually treat (not just prevent) breast, endometrial, pancreatic, and prostate cancers. The National Cancer Institute is playing catch up with trials on colon and other cancers.

And it seems metformin is particularly active against lung and oral cancers. Which adds even more proof that there is more to the story with these cancers than just tobacco.

And beyond all this, metformin has just been found to show promise for the most mysterious and alarming disease of our time—Alzheimer’s dementia (see page 5).

So here we have a safe, effective, inexpensive drug that actually treats the condition of diabetes, by lowering blood sugar (and not just “managing” symptoms). It also reduces all the major medical complications commonly associated with diabetes such as cardiovascular diseases. And the main long-term “side effects” are a list of additional health benefits such as reducing the risk of common cancers and probably helping to maintain healthy weight.

So the only mystery is why has it evaded comprehensive investigation of its multiple health benefits for so long?

Poisonous plant turned
modern wonder “drug”

Ironically, the natural sources of G. officinalis are currently known in the U.S. as “Professor Weed” and the federal government lists it as a “Class A Noxious Weed” in their database of poisonous plants! This French lilac (also used for its fragrance) is just another weed to the U.S. government.

Perhaps the only answer to this modern government nonsense was provided by the 16th century Swiss physician, Philippus Aureolus Theophrastus Bombastus von Hohenheim (better known as Paracelsus), who would have known about the medicinal uses of this remarkable plant: “the right dose differentiates a poison from a useful medicine.” Which could be said about many herbal remedies and almost all drugs as well.

Which is what makes the drug version of this herbal remedy— metformin—such a breakthrough. This modern “wonder” “drug” is actually little different from the ancient herbal remedy Galegine, widely known and used in Europe in the Middle Ages. It benefits from chemical simplicity and detailed clinical investigation. And endless drug vigilance has long settled concerns by the FDA and ill-informed public advocacy groups.

Of course, metformin will
only get you so far…

It is possible to actually reverse diabetes through diet and weight loss alone. Last year researchers in the UK completely reversed diabetes in patients who were placed on 600-calorie-per-day diets under direct medical supervision. But the usual minimum caloric levels for healthy weight loss, working on your own, in women and smaller individuals are no less than 1,000 calories per day, and for men and larger individuals 1,200 calories.

These are guidelines you can achieve on your own following a healthy diet of caloric restriction. These are the caloric lower levels for weight loss, not weight maintenance. Healthy weight loss diets include lots of fresh fruits and vegetables and eliminate sugars and processed foods and fats (see your Insiders’ Cures report Top-of-the-Food-Chain Cure for Obesity). Lower body weight and body fat leads to lower blood sugar, cholesterol, and blood pressure.

Some dietary supplements may also help maintain healthy blood sugar levels.

•   Alpha Lipoic Acid (ALA): 300 mg/day

 •   Vitamin B6 (as pyridoxine): 100 mg/day

•   Berberine: 400-500 mg/day

•   Cinnamon: 1 gram/day (food quantity)

•   Coenzyme Q10: 150 mg/day

There are also some herbal remedies that are being investigated for their effects on maintaining healthy blood sugar. They include the traditional Chinese remedy bitter melon, cinnamon, blueberry leaf, dandelion leaf, as well as various traditional Ayurvedic herbs from India.

Finally, chromium, selenium, and vanadium are minerals and heavy metals that play important roles in managing blood sugar and healthy metabolism. As metals, they have potential toxicities, so check with your health practitioner.

Beyond these dietary supplements, the natural products industry is pushing on other fronts to help with diet and diabetes:

1.  Food ingredients that substitute for sugar and starches, so there is simply less sugar in the diet to be absorbed into the blood.

2.  Other ingredients that block the uptake of sugars and starches that are already in the diet, thus theoretically stopping sugar from being absorbed into the blood. (Other inevitable effects on healthy digestion must also be addressed.)


Metformin for “Type III diabetes”?

New research has shown that metformin also stimulates neuron generation and memory, at least in laboratory animal models.1 Of course, metformin is now being used for its metabolic effects, including healthy metabolism of glucose in diabetes.

But as my professors at the University of Pennsylvania would always reiterate, “any drug can have any effect.” Any substance that can be absorbed by the digestive tract and make its way into the bloodstream, tissues, and cells, and interact with normal metabolic mechanisms indeed has the potential to show many different effects. After all, the body itself has many different active processes going on all the time, all at the same time.

Such substances can act like a drop of oil lubricating all of the complex gears and mechanisms in a clock or fine piece of machinery. We also know the same is true of active natural remedies. We are constantly seeing that modern science finds new benefits from old remedies that have been used historically for various purposes.

One key to metformin’s multifarious benefits appears to hinge on the enzyme called “atypical protein kinase.” This enzyme is present throughout the body—and is responsible for metformin’s primary metabolic effects in the liver. But protein kinase is also active in the brain for transforming stem cells into neurons.

The true miracle here is not necessarily the drug, but that the body uses the same enzyme efficiently and effectively for different critical functions among different tissues. Again, the key to all healing is stimulating the body to find ways to heal itself—as we often find in Nature when we look.


1. “Metformin activates an atypical PKC-CBP pathway to promote neurogenesis and enhance spatial memory formation.” Cell Stem Cell, volume 11, issue 1, 23-25, 6 July 2012.