Do you love methylene blue? Well, here at Troscriptions, blueing ourselves is the next best thing to sliced (gluten free, dairy free, soy free, non GMO and no-bees-were-harmed to make this) bread.  

In previous blogs, we’ve covered many MB topics include MB history, it’s many potential uses, especially as a Health Optimization Nootropic, and we have implored you to never drink actual fish tank cleaner (please!). 

But what we haven’t dialed in yet is dosing. 

So, in his article that’s exactly what we are going to do. 

We’ll discuss the why behind Tx dosing and also take a keep dive into the potential dangers of taking higher dose methylene blue, especially for longer periods of time. 

Are you ready to come dance (and blue yourself) in the nuance of dosing as we explore Blueniverse once again?

Let’s go! 

Oh wait! But first…

A Quick (but detailed) Refresher on MB Mechanisms 

Methylene Blue is called anelectron cycler. At doses up to 3mg/kg, it acts both as an electron donor to the electron transport chain in your mitochondria and as an electron acceptor of free electrons from reactive oxygen and nitrogen species (i.e. works like an antioxidant, an antioxidant as powerful or possiblyeven more powerful than glutathione).

There are very few compounds that cycle electrons as effectively as MB.

In addition, methylene blue also increases cytochrome oxidase (complex IV) function in your mitochondria and drives increased glucose consumption. The latter occurs because the mitochondria are making more energy and needs more substrate to supply electrons to the electron chain. Less you forget that THE major reason we need to eat is to supply our mitochondria with electrons!! 

While increasing glucose consumption and energy production, MB alsoincreases the supply of NAD+ whether there is oxygen around or not. At <2mg/kg, it also causes therelease of nitric oxide and the dilation of blood vessels to get more oxygen rich blood to the area of increased glucose consumption. 

For those nerds amongst us (we are guilty), because MB can enhance complex IV function and NAD+ supply, it canbypasses potentially dysfunctional mitochondrial complexes I and II. This is a big deal and a major reason why MB works to reverse or compensate for mitochondrial damage. 

And there’s more! 

MB also changes the conformation of hemoglobin in RBCs to help it carry oxygen more efficiently, promotes oxygen dumping into tissues so it can be utilized easier, may help clearsenescent cells, increasesmitochondrial biogenesis, and works as a monoamine oxidase (MAO-I) Inhibitor which leads to neurotransmitter release including dopamine and serotonin. 

Phew! Are you keeping up? This compound is doing A LOT and has a large therapeutic range…from 8mg to 210mg (<0.5 to 3mg/kg). 

Even at doses >3mg/kg, when MB is no longer an electron cycler and becomes purely oxidative, there may be a role for it incancer andsepsis,. 

But that’s a huge therapeutic range. How do you know what dose is best for you?

Methylene Blue Dosing 

The key point is to distinguish what kind of dosing helps acutely (i.e. for a disease or condition) vs. what dosing will help optimize health. And also to be aware of the significant dangers of taking too much MB at high dose for a long period of time. 

Here at Troscriptions, we are focused on optimizing health rather than treating disease. After all, this is the ethos of our company. And to this end, we provide financial support to Health Optimization Medicine and Practice (HOMeHOPe), a nonprofit organization that is training doctors and practitioners on how to optimize health rather than treat disease.

Let’s chat about the risks of higher dose MB and why we use lower dosing at Troscriptions. 

Methylene Blue and the disruption of GI Biofilms.

Our concern with higher dose methylene blue dosing is that it may disrupt natural and healthy gastrointestinalbiofilms leading to issues with your gut lining and gut microbiota. We’ll get back to what we mean by higher dose in a minute. First, let’s talk about biofilms.

Biofilms are a collective of one or more types of microorganisms that can grow on many different surfaces. They produce a substance known as extracellular polymeric substance (EPS) that gives the surface a film-like/sticky consistency. A fully functioning biofilm structure comprises microbial cells and EPS, has a defined architecture, and provides an optimal environment for the exchange of genetic material between cells of the same and different phyla, otherwise known as trans kingdom interactions. 

Microorganisms that form biofilms include bacteria, fungi, and protists. In the gut, biofilms naturally grow, both at the epithelial surface and in the lumen as mucin-attached and food particle-attached colonies. Communities of microbes that form biofilms are usually more resilient to stress and are well known to keep surfaces like your mouth and gut healthy. This includes enhancingimmune system function. They also function as a physical barrier to the intestinal lining. 

There are, however, times when these biofilms can become pathologic such as in dental plaques or with certain bacterial infections. When this occurs, biofilms can actually protect pathogenic bacteria and can be difficult for the host defense system to identify. 

Methylene Blue is especially effective at disrupting biofilms of multiple organisms when combined withother synergistic therapies, such as photodynamic therapy. For example, it is often used at doses of 50mg daily for infections with biofilms like Bartonella. 

High Doses May Be Dangerous due to MB ½ life.  Here’s why…

Methylene Blue--whether IV, oral, or in troche form-- isalmost 100% bioavailable, meaning that almost all the MB that you take in gets into your bloodstream. What’s the catch? Let us explain…

How long MB stays in your body depends on its half-life. This is defined as the time it takes for one half the amount of MB that you ingested to leave your body. 

The half-life of IV MB is 24 hours 

The the half-life oral MB is 4 to 6 hours. 

Let’s take the example of 100mg oral MB dose with a 1/2 life of 6 hours. 

Imagine you took your dose at 8am in the morning…

1/2 life #1: 50mg left in your body at 2pm (i.e. 6 hours later) 

1/2 life #2: 25mg left in your body at 8pm (i.e. another 6 hours later)

1/2 life #3: 12.5 mg left in your body at 2am

1/2 life #4: 6.25mg left in your body at 8am.

This means that if you take 100mg MB at 8am, you'll still have 6.25mg of MB in your body 24 hours later. 

As an alternative example: if we assume that the half-life is 4 hours, then there would be 3.125mg of MB left in your body at 8 am the next day.

Either way, if you take 100mg on a daily basis, there will be a high chance for potential toxicity because MB will continue to build up in your system.

And high dose MB (especially >3mg/kg) leads to mitochondrial dysfunction and inflammation, not to mention more issues with GI biofilms and your microbiota. 

High doses of Methylene Blue and Risk of Gastric Ulceration + Gastric Acid, Really? 

While higher doses of MB may help treat disease, over the long term, it may causegastric ulceration.

And there is no indication that MB requires gastric acid to be activated. After all, IV methylene blue is 100% bioavailable and completely bypasses the GI system. This is an important counter some of the arguments that are floating around the internets :)

Methylene Blue and G6PD Deficiency

Although rare, higher doses of methylene blue may also cause hemolysis (the destruction of red blood cells) in those with G6PD Deficiency, an inherited blood disorder. At low doses, this would be rare, but higher doses, especially for prolonged periods of time may be dangerous. 

Conclusion

At Troscriptions, our products optimize health rather than treat disease. In this context, our methylene dosing was designed to leverage this magical blue compound for its energy enhancing and antioxidant properties while at the same time minimizing the risks of potential GI biofilm disruption, of MB building up in the body, the potential for gastric ulceration, and other potential side effects. 

Our dosing is also happens to be the dosing being studied in patients with neurocognitive conditions such as Alzheimers Disease (but we make no claims). 

Of course, our troches (or another MB product) can be used at higher doses when needed to treat certain diseases or conditions. But if this is the case, titration and less regular dosing are key to decrease risk of toxicity. 

And a few words of advice to leave you with…

Make sure your MB company is going the extra mile to give you a pure product.  Many on the market, even USP designated products, may be contaminated with heavy metals. Industrial and chemical grade MB should be avoided at all costs as well (cue the Darwin Awards, folks!). 

At Troscriptions our MB is: 

• Third party tested from our manufacturer to ensure purity/potency. 
• USP grade 
• Tested AGAIN for purity/potency with each troche batch we make.

Does your MB company do all this? We doubt it!  

Plus, there are 4 docs on the Tro Team + practitioners around the world that use our products in clinical practice. 

No go forth and Blue Yourself…safely and effectively. 

To Health, Optimized. 

Dr. Scott and the Troscriptions team.