Methylene blue
Cas No.: 61-73-4
What is methylene blue?
While methylene blue (methylthionine chloride) is primarily associated as a dye, few people know that the compound can also be used as a drug. The dye is a tri-heterocyclic compound that contains an aromatic thiazine ring in the central part of the molecule. The compound was synthesized in 1800 as a substance that found application in the textile industry – it was used to dye fabric. Over time, however, its medicinal properties were discovered, leading the World Health Organization to treat it as one of the most useful medicines. It was the first synthetic drug to find – and still finds – use in humans.
The healing potential of methylene blue first became notorious in 1890, when Paul Erlich began using it to treat malaria. Through numerous animal studies, this scientist discovered that administration of methylene blue is followed by a very rapid accumulation of this compound in brain tissue. This phenomenon has been referred to as « magic bullet. »
The primary use of methylene blue has been in the treatment of malaria, and attempts have also been made to use blue in the treatment of conditions such as schizophrenia, mild cognitive disorders, Alzheimer’s disease, and Parkinson’s disease. These disorders have one common denominator, and that is the abnormal work of mitochondria. Efficient brain function also depends on the proper functioning of these cellular organelles. So if methylene blue supports mitochondrial function, it is not surprising that there is now more and more talk about the nootropic activity of this compound.
Application of methylene blue
Methylene blue is currently used to treat urinary tract infections, cyanide poisoning, and as a treatment for methemoglobinemia. There is no shortage of clinical studies that also point to other possible uses for methylene blue. Among other things, it has been shown that the preparation, when administered to people experiencing severe depressive states, allowed them to alleviate their symptoms. In addition, the preparation alleviates anxiety, and increases the body’s resistance to stress. Clinical studies indicate the validity of using blue not only in patients with depression. Promising results have been obtained using the product in people with bipolar affective disorder, as well as Alzheimer’s disease.
The compound effectively supports memory – both short-term and long-term. Even a single application of methylene blue has been shown to increase short-term memory. Regular use of the product promotes the phenomenon of memory consolidation, that is, the transformation of short-term memory into long-term memory. It facilitates learning, processing information and acquiring new knowledge. Users report a surge of energy and a desire for action, and feelings of fatigue and drowsiness are reduced.
Methylene blue shows a very comprehensive, beneficial effect on the functioning of the nervous system. This allows it to be used both by young people who are studying or working mentally, but also – by older people affected by dementia.
Mechanism of action
Methylene blue crosses the blood-brain barrier, so it directly affects brain neurons. The most important mechanism of action of methylene blue comes down to supporting the work of mitochondria, the cellular organelles responsible for producing energy. This is especially true for the process of the so-called « process ». cellular respiration. Methylene blue facilitates electron transport, which contributes to an increase in the rate of brain metabolism. In addition, the amount of synthesized ATP, a high-energy compound, increases.
Methylthionine chloride increases oxygen consumption and glucose uptake by nerve cells. This translates directly into a more efficient operation of them. In addition, it can noticeably slow down the brain’s aging process. This is the main difference between methylene blue and other nootropics, such as Pramiracetam. Most nootropics affect the brain via neurotransmitters and the receptors they stimulate. Methylene blue, on the other hand, directly affects neuronal metabolism.
Another mechanism of action is antioxidant activity, or the ability to neutralize oxidative stress. By effectively fighting free radicals, the compound can protect nerve cells from neurodegenerative processes. In addition, blue has the ability to counteract reperfusion damage in the course of cerebral ischemia.
The antidepressant effect of methylene blue is due to the fact that it exhibits monoamine oxidase inhibitor activity. This enzyme is responsible for breaking down serotonin molecules. Inhibition of monoamine oxidase activity is accompanied by maintenance of optimal levels of serotonin, which is crucial for maintaining mental well-being. The product also inhibits the activity of another enzyme – acetylcholinesterase. Thus, methylene dye prevents the breakdown of acetylcholine molecules, a neurotransmitter that affects the processes of learning, information assimilation and processing, as well as the ability to concentrate.
Methylene blue – dosage
The dosage of methylene blue in the numerous clinical trials conducted ranged from 0.5 to 4 mg/ kg m. c. It is recommended to start with the lowest dose, and then gradually increase the dose if necessary. The duration of action of the product is about 5 hours, so it is advisable to take methylene blue twice a day. The compound is water-soluble, so just sip it with water. It is not necessary to take it with a meal.
References:
- Poteet E, Winters A, Yan LJ, Shufelt K, Green KN, Simpkins JW, Wen Y, Yang SH. Neuroprotective actions of methylene blue and its derivatives. PLoS One. 2012;7(10):e48279; https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3485214/
- Naylor GJ, Smith AH, Connelly P. A controlled trial of methylene blue in severe depressive illness. Biol Psychiatry. 1987 May;22(5):657-9; https://pubmed.ncbi.nlm.nih.gov/3555627/
- Oz M, Lorke DE, Petroianu GA. Methylene blue and Alzheimer’s disease. Biochem Pharmacol. 2009 Oct 15;78(8):927-32; https://pubmed.ncbi.nlm.nih.gov/19433072/
- Alda M, McKinnon M, Blagdon R, Garnham J, MacLellan S, O’Donovan C, Hajek T, Nair C, Dursun S, MacQueen G. Methylene blue treatment for residual symptoms of bipolar disorder: a randomised crossover study. Br J Psychiatry. 2017 Jan;210(1):54-60; https://pubmed.ncbi.nlm.nih.gov/27284082/