Methylene blue: an overview of its discovery, use and effect

Introduction

Methylene blue is a fascinating substance with a long and varied history of use in medicine. Originally discovered as a dye, it is now an established treatment in both conventional and alternative medicine. This article will tell you more about its discovery, dosage, indications and possible risks. We will also explain which dietary supplements or medicinal plants can be a useful addition.

Discovery of methylene blue

It was first synthesized in 1876 by the German chemist Heinrich Caro. Originally developed as a dye for textiles, it was soon recognized that it could also be useful as a colorant in medicine. Bacteriologist Paul Ehrlich discovered that certain cells and microorganisms could be stained, so it could be used to examine blood and tissue. This discovery led to methylene blue being used in medicine and research.

Dosage forms and dosage

Methylene blue can be taken in different ways depending on the area of application and dosage form. It is usually available as a tablet, capsule or injection, with the exact form and dosage depending on the respective clinical picture. For therapeutic applications, dosages in the range of 1 to 3 mg per kilogram of body weight are often used. However, at higher doses it can have a toxic effect, which is why precise dosing and medical supervision are required.

Exemplary dosage:

For mild cognitive disorders, small amounts of 0.5 mg per kg of body weight can often be sufficient.

For severe illnesses and special treatments, a dosage of 1 to 2 mg per kg of body weight is useful, but always under medical supervision.

Applications and effects on the organism

Methylene blue is used in medicine for a variety of applications. Its ability to exert antimicrobial, antioxidant, and neuroprotective effects makes it a valuable medicine for various health problems. The following is a detailed description of how it can help in the treatment of Alzheimer’s disease and in the fight against parasites.

Effect on Alzheimer’s and other neurodegenerative diseases

Methylene blue has attracted much interest in recent research because it shows promising effects in neurodegenerative diseases, especially Alzheimer’s disease. Alzheimer’s is a disease characterized by the death of nerve cells in the brain and the accumulation of abnormal proteins such as tau proteins and amyloid plaques. These protein accumulations interfere with communication between nerve cells, eventually leading to loss of memory and cognitive function.

Methylene Blue works on Alzheimer’s disease on several levels:

1. Inhibition of Tau proteins: One of the central theories of the development of Alzheimer’s disease concerns the formation of Tau proteins, which clump together in nerve cells to form so-called Tau fibrils and impair their function. It has been shown to inhibit the formation of these fibrils. It binds to the tau proteins and prevents them from clumping, which could slow the progression of Alzheimer’s disease.
2. Promoting mitochondrial health: Mitochondria are the “power plants” of cells that produce energy in the form of ATP (adenosine triphosphate). In Alzheimer’s and other neurodegenerative diseases, mitochondria are often damaged, impairing the energy supply to the cells. It can support the function of mitochondria and thus energy production in the brain cells. It acts as a kind of “electron acceptor”, which improves electron transport in the mitochondria and thus increases energy production. This energy is essential for maintaining cognitive function.
3. Antioxidant effect and protection against cell damage: Methylene blue has antioxidant properties that help to reduce oxidative stress. Oxidative stress caused by free radicals is another factor that damages nerve cells in Alzheimer’s disease. By neutralizing free radicals, it protects cells from further damage and thus helps to maintain brain function.
4. Stimulation of neurotransmitters: Methylene blue can also increase the availability of neurotransmitters such as dopamine and serotonin in the brain. These neurotransmitters play an important role in regulating mood and memory. Taking it could therefore support overall brain function and well-being in people with Alzheimer’s disease.

Because of these multiple mechanisms of action, it offers great potential for the treatment of Alzheimer’s disease and possibly other neurodegenerative diseases. However, many of these uses are still in the research stage and general approval for the treatment of Alzheimer’s disease is still pending. Nevertheless, it is considered a promising agent in neuroscience research.

Effective against parasites and malaria

Methylene blue was originally used as an antimalarial before other drugs such as chloroquine and artemisinin were developed. Malaria is caused by parasites of the genus Plasmodium, which are transmitted to humans through the bite of infected mosquitoes. These parasites infect red blood cells and cause high fever, chills, and other severe symptoms. It is effective against these parasites and can be an effective treatment option in certain cases.

The effect of methylene blue on parasitic infections, especially malaria, can be explained as follows:

1. Disruption of the parasite’s metabolism: It can disrupt the energy metabolism of the malaria parasite. The parasite needs a special form of energy production that relies on enzymes that are inhibited by methylene blue. This inhibition blocks the parasite’s energy flow, which ultimately leads to the death of the pathogen.
2. Antioxidant effect at the cellular level: Unlike human cells, parasites are very sensitive to oxidative stress. It produces reactive oxygen species in the infected cells that can kill the parasites. This effect is specific to the cells of the parasite and leads to a reduction of the infection in the body without severely affecting the human cells.
3. Accelerating parasite excretion: It speeds up the excretion of dead parasites from the body. This property is particularly valuable for promoting the recovery of malaria patients. When used in combination with other antimalarial drugs, methylene blue can shorten the duration of treatment and reduce the risk of relapse.
4. Synergistic effect with other antimalarials: It shows a synergistic effect when combined with other antimalarials. It has been found that when combined with common antimalarials such as artemisinin, it can increase the effectiveness of the treatment and reduce parasite resistance. This means that it can reduce the likelihood of developing resistance to certain antimalarials.

Other potential anti-parasitic uses

The antimicrobial and antiparasitic effects of methylene blue are not limited to malaria. Research has shown that it can also be effective against other parasitic infections, such as trypanosomes, the causative agents of sleeping sickness. These applications are still in the experimental stage, but could help improve the treatment of such infections in the future.

Methemoglobinemia

Methylene blue is also used to treat methemoglobinemia, a rare blood disorder in which hemoglobin does not carry enough oxygen. It acts as an antidote here and helps to convert the hemoglobin back into a functional form.

Antioxidant effect

Thanks to its antioxidant properties, methylene blue protects cells from oxidative stress and thus helps to fight free radicals. This can also have an anti-inflammatory effect and is used in some cases to support cell health.

In summary, it can be promising for both neurodegenerative diseases such as Alzheimer’s and parasitic infections such as malaria due to its diverse mechanisms of action. While in Alzheimer’s disease it can work by inhibiting the tau protein, promoting mitochondrial function, and providing antioxidant protection, in malaria and other parasitic diseases it directly attacks the pathogens and disrupts their metabolism. Both uses continue to be intensively researched and it remains a valuable agent with great potential in medicine.

When is it useful to take methylene blue?

It is often taken when there are certain medical indications, such as cognitive disorders or certain blood diseases. However, it should always be taken in consultation with a doctor, as an overdose can be toxic. It is particularly recommended for:

• People with neurodegenerative diseases such as Alzheimer’s.
• Patients with methemoglobinemia.
• People who want to improve their cognitive function and memory.

People for whom methylene blue is not recommended

Not everyone should take it. Certain groups of people are at greater risk of side effects or insufficient effect. In particular, pregnant and breastfeeding women and people with certain enzyme defects (e.g. G6PD deficiency) should refrain from taking it. People who regularly take MAO inhibitors or SSRIs should also avoid it, as severe interactions can occur.

Dietary supplements and medicinal plants

The effect of methylene blue can be enhanced by combining it with certain dietary supplements and medicinal plants. Here are some useful supplements:

• Coenzyme Q10: Supports mitochondrial function and can complement the effect on cells.
• Alpha-lipoic acid: Also has an antioxidant effect and can increase cell protection.
• Curcumin: A natural anti-inflammatory that can enhance the antioxidant effect.
• Ginkgo biloba: Promotes blood flow and can support cognitive processes when combined with methylene blue.

Natural sources and foods with similar effects

Methylene blue itself is not found in food because it is a synthetic substance. However, there are foods that may have similar antioxidant and cell-protecting effects. These include:

• Blueberries and raspberries: They are rich in antioxidants and promote cell health.
• Green leafy vegetables: They contain vitamin K and folic acid, which can support blood health.
• Dark chocolate: It contains flavonoids, which have an antioxidant effect and support blood vessels.

Possible side effects

Although methylene blue is a valuable medicine, in some cases it can cause side effects. The most common side effects are:

• Nausea and vomiting
• Headaches
• Skin rash

Blue coloration of the skin or urine, which is usually harmless but can be unsettling.

Some people may also experience allergic reactions.

Therefore, the intake should always be monitored by a doctor, especially at higher dosages.

Overdose and toxic effects

An overdose of methylene blue can have serious consequences. Excessive doses can cause symptoms such as confusion, hallucinations, tachycardia and shortness of breath. In extreme cases, an overdose can even lead to convulsions and a drop in blood pressure. If an overdose is suspected, seek medical attention immediately.

Methylene blue in natural medicine

In alternative medicine, methylene blue is used in some areas as a natural remedy, particularly to support cognitive function and as a mild antioxidant. It is also used occasionally in bioenergetic medicine to promote the flow of energy in cells and thus support health at the cellular level.

Summary

Methylene blue is a versatile drug with an interesting history and a wide range of applications. From the treatment of cognitive disorders to its antimalarial effect, it has a firm place in modern medicine. However, caution is advised: Dosage and use should always be controlled by a doctor to avoid side effects or overdoses. In combination with antioxidant supplements and a healthy lifestyle, it can be a valuable addition to promote health.

Sources and further information:

Methylene blue and Alzheimer’s

1. Methylene blue in Alzheimer’s research: The Alzheimer Research Initiative e.V. provides an overview of the potential applications of methylene blue in the treatment of Alzheimer’s disease, particularly its effects on tau protein aggregation. https://www.alzheimer-forschung.de/aktuelles/meldung/methylenblau-alzheimer/
2. Methylene blue against Tau and Alzheimer’s disease. The German Health Portal reports on studies on the effectiveness of methylene blue in inhibiting tau protein aggregation and the formation of tau fibrils, with results from an 18-month phase III study. https://www.deutschesgesundheitsportal.de/2022/11/18/methylenblau-gegen-tau-und-alzheimer/
3. Tau aggregation inhibited in phase III: Second chance for methylene blue derivative. The article from SpringerMedizin.de reports on a phase III study in which the methylene blue derivative hydromethylthionine mes ylate was able to reduce the Tau pathology in Alzheimer’s patients. https://www.springermedizin.de/aaic/morbus-alzheimer/zweite-chance-fuer-methylenblau-derivat/25580796

Methylene blue and malaria

1. Methylene blue Stops the Spread of Malaria: In a phase-II study reported on by the Pharmazeutische Zeitung, methylene blue in combination with other drugs completely eliminated the pathogens of malaria tropica and helped to prevent resistance. https://www.pharmazeutische-zeitung.de/ausgabe-152018/methylenblau-stoppt-malaria-verbreitung/
2. New study with old dye: Methylene blue inhibits the spread of malaria parasites – The Science Information Service reports on an international study showing that a triple combination of modern malaria drugs with methylene blue quickly eliminates the pathogens, is well tolerated and prevents resistance. https://idw-online.de/de/news691778
3. Efficacy and safety of methylene blue in the treatment of malaria: a systematic review. This systematic review, published in BMC Medicine, examines the efficacy and safety of methylene blue in the treatment of malaria. The authors analyse various studies and evaluate potential benefits and risks. https://bmcmedicine.biomedcentral.com/articles/10.1186/s12916-018-1045-3