Nootropics series: Meldonium/Mildronate
Meldonium, also known by its trade name Mildronate, is a pharmaceutical with a limited market. The medication is primarily distributed in Eastern European countries and is utilized as an anti-ischemia treatment.
Meldonium functions as a metabolic modulator, preventing the accumulation of harmful byproducts from enzymatic reactions preventing the accumulation of harmful byproducts from enzymatic reaction pathways in the body.
Research has shown that it may have therapeutic benefits for neurological and cardiovascular conditions. Additionally, it is recognized for its ability to enhance cognitive function.
Meldonium Metabolic Modulator
Alright, it’s used to treat a condition called “ischemia,” when parts of your body, such as your heart & brain, don’t get enough blood and the oxygen the blood carries.
Now Meldonium is a “metabolic modulator.” You can think of Meldonium as a traffic police agent for your body’s metabolism. Our bodies have tons of reactions happening every microsecond. Sometimes these reactions can leave behind some “junk.”
Like how you might have dirty leftovers after cooking a big meal, this metabolic junk or harmful byproduct is terrible when it accumulates and piles up.
Meldonium can help to manage this waste, preventing the buildup of these harmful junk and byproducts.
It’s like having someone who cleans up the kitchen after you’ve been cooking. So things stay clean, and nothing nasty starts to accumulate.
Meldonium for the Heart
So when Meldonium first came out, it was primarily used in hospitals and clinics to treat heart problems caused by ischemia. As explained before, “ischemia” is a fancy medical term for when a part of your body (like your heart & brain) doesn’t get enough blood and the oxygen the blood carries.
These heart problems can mess with your overall health in several ways.
- Oxygen deprivation: Pretty much what it sounds like. Your heart isn’t getting enough oxygen because it lacks blood. If there’s a reduced blood supply due to a blocked artery
- Excessive Exertion like angina: Angine is the type of chest pain that happens when your heart has worked too hard, often because it’s not getting enough oxygen. Like you’ve sprinted hard to don’t miss the bus for school because your final exam is on that same day.
So talking Meldonium is like getting a support crew for your heart, helping to deal with these challenging situations, and keeping your heart beating.
How Meldonium Improves Athletic Performance
Athletes who are familiar with Medonium know it can give them a boost when they’re competing.
Meldonium, also known by its brand name Mildronate, does not directly tweak our brain or nerves. Instead influences the metabolic reactions going on in your body, which can have a positive impact on your nervous system.
Okay, stay with me. Here’s how it works. Meldonium or Mildronate can put breaks in certain enzymes responsible for breaking down fatty acids, which in turn leads to a decreased level of lactate in the muscles.
Lactate is what you get when your body breaks down glucose for energy without enough oxygen. It’s a process called “anaerobic glycolysis”.
You know when you’re working out hard, and you feel it burn in your muscles. That’s lactate buildup.
Meldonium helps improve oxygen delivery throughout the body and brain by reducing lactate levels. So it’s not much of a surprise that athletes see this as a way to get ahead of the competition.
Disclaimer: The product Meldonium, also known as Mildronate, is included on the World Anti-Doping Agency’s (WADA) prohibited list. Any use of this substance, either directly or indirectly, is strictly prohibited for athletes under the jurisdiction of the WADA.
The use of Meldonium may lead to a violation of anti-doping rules, which can have severe consequences, including disqualification from competitions, sanctions, or other legal implications.
Before initiating any medication or supplement regimen, please consult with a medical professional or sports governing body. Always adhere to the laws and guidelines your sport’s governing body and regulatory authorities set.
Can Meldonium Help against Hypoxia Condition?
Hypoxia is a condition when the body is deprived of the oxygen it requires.
Now there’s something called Intermittent Hypoxia. Think of intermittent hypoxia as breathing through a straw (pure torture). When you take a normal breath, you’re getting a full lungful of oxygen.
Now imagine if, every so often, you had to breathe through a straw for a bit. You get less air and, therefore, less oxygen during those moments. Now imagine you can breathe normally again, with plenty of oxygen again.
Now repeat the cycle. This cycle of normal breathing and straw breathing represents the fluctuating oxygen levels in intermittent hypoxia.
Now Meldonium, or by its brand-name Mildronate, can help deliver more oxygen throughout the body, remember. So in these situations, there’s this “breathing through a straw effect”. Meldonium can help to deliver more oxygen.
Can Meldonium Boost Cognitive Abilities Of The Brain?
Our brain is a super complex machine that needs a steady supply of energy to keep all its part running smoothly. The energy mainly comes from oxygen and glucose, which our blood delivers to every nook and cranny of the brain.
You can be in a situation where your brain isn’t getting as much oxygen as it would like when you’re pushing yourself physically. That’s where Meldonium can come to use, to play traffic police, directing more oxygen to where it needs to go.
By doing this, Meldonium helps your brain to keep up its energy supply, even when things are tough.
It’s kind of like a backup generator kicking in during a power outage, and when your brain has the energy it needs, it can do a better job.
Things like problem-solving, learning new stuff, and all these cognitive abilities can be boosted with Meldonium.
Okay, I am getting tired with all the metophores for now. I’ll switch to the details
Meldonium is recognized for its ability to regulate cerebral functions by increasing the body’s oxygen-carrying capacity, which improves cognitive performance.
Meldonium functions as a metabolic modulator by hindering the carnitine biosynthesis pathway. It reduces the creation and subsequent oxidation of long-chain fatty acids.
The inhibition shifts the metabolism towards the glycolytic pathway, which is more oxygen-efficient while simultaneously promoting the production and availability of glucose-derived energy substrates in the brain.
This metabolic shift enhances the brain’s resilience against hypoxic conditions such as reduced oxygen supply which can potentially happen during periods of high cognitive demand.
In challenging conditions, the brain may experience a deficit in available oxygen supply, leading to a higher demand for energy that can negatively impact cognitive function.
Meldonium can aid in efficiently using oxygen, helping maintain the brain's energy balance and support its functioning.
Moreover, by reducing the accumulation of toxic byproducts of incomplete fatty acid oxidation, such as lactate and free radicals, Meldonium helps preserve neurons' structural and functional integrity, further contributing to its cognitive-enhancing effects.
The ability of Meldonium to enhance cognitive abilities is associated with its capacity to regulate metabolism, increase oxygen utilization efficiency, and shield against neuronal damage during hypoxic conditions.
How Does The Mechanism Of Meldonium Work?
To summarize the Meldonium mechanism once again. Meldonium acts like a traffic cop in your body, with its main job being to control how much energy gets produced. Typically, your body uses something called “carnitine” to move fatty acids into the powerhouses of your cells, the mitochondria.
The mitochondria then break down these fatty acids to produce energy. But when Meldonium acts like a traffic cop, putting a roadblock on the fatty acid highway, it decreases carnitine levels. It’s as if the cop rerouted the traffic to different routes. That means fewer fatty acids can get to the mitochondria.
This glucose breakdown process is interesting because it doesn’t need as much oxygen and generates even more energy. This mechanism forces your body to switch gears using a different energy fuel, glucose. It’s like your body going from diesel to electric.
That’s helpful when insufficient oxygen or the blood supply is reduced, as it can protect your cells from damage. Meldonium or Mildronate acts as a genius traffic op, rerouting energy production to keep things running smoothly despite harsh conditions.
Can Meldonium Boost The Immune System?
Imagine your body is a castle, and Mildronate is like general rallying troops for defense.
We have antibodies like cytokines. These guys are like the archers and foot soldiers of your immune system. They help to fight off invading germs and send signals to call reinforcement. Mildronate increases their numbers, making your army of defense stronger.
Next, we have the natural killer cells, the special forces of your immune system. They’re great at taking out the enemy cells that have been infected or gone rogue. Mildronate helps to boost their numbers, making your special forces team even more powerful.
Finally, we have macrophages, the clean-up crew of our immune system. They’re like the workers who clean up after the battle, gobbling up the remains of the enemy cells and any other cellular debris.
Meldonium/Mildronate improves their phagocytic activity, a fancy way of saying it helps them eat up more stuff.
Mildronate is a general that helps boost your body's defenses, preparing the body to fight invaders and clean up.
Meldonium Stress Reduction
Meldonium can also have a relaxing effect on your brain, like a “chill pill”. You’re probably dealing with a lot of stress, from mental stuff like work, and school, or physical stuff like running a marathon. It can often feel like our brain is running in overdrive. That can lead to anxiety and trouble thinking clearly.
Now, again here’s where Meldonium steps in. It works like a sound engineer at a concert, tweaking the levels of different brain chemicals (neurotransmitters and hormones) to get the perfect mix.
Brain chemicals have a big influence on how you’re feeling. When their levels are out of whack, it can lead to stress, anxiety, cognitive issues, etc. When Meldonium adjusts its levels, it’s like bringing the volume of a blaring concert down to a comfortable level.
That can help to reduce the symptoms of stress.
Meldonium regulates blood glucose levels
Meldonium has another job, playing as a sugar cop. Your body needs a certain amount of sugar (or rather glucose) for energy. Too much or too little can throw things off balance. Insulin is a hormone that helps keep your blood sugar levels in check, and sometimes the system doesn’t work as well as it should.
Enter Meldonium, aka Mildronate, the sugar cop, stepping in to help regulate the sugar levels in your blood. It it’s kind of like a traffic officer directing cars on a busy highway, ensuring everything flows smoothly without any jams or empty stretches.
By helping your blood sugar, Mildronate can keep your body’s energy level more steady and balanced, which is especially important for people with diabetes.
Meldonium type 2 diabetes
Meldonium or Mildronate has been studied for its potential to help manage or prevent type 2 diabetes. In these studies, the medication was given to a type of rat known as Goto-Kakizaki, an experimental model for type 2 diabetes.
Research shows that Mildronate can lower L-carnitine levels in the rat’s blood, which is essential because L-carnitine is involved in how our bodies use fats and carbohydrates for energy.
This shift helped rats manage their blood sugar levels better. They observed that both the fed- and fast-state blood sugar levels gradually decreased in rats treated with Mildronate.
Mildronate also prevents the buildup of a substance called “fructosamine”, which can accumulate when blood sugar levels are high for an extended period.
According to the researcher's findings, Meldonium may be advantageous for individuals with type 2 diabetes, particularly those with cardiovascular problems. During the study, Meldonium demonstrated heart-protective properties and its impact on blood sugar levels.
https://pubmed.ncbi.nlm.nih.gov/19594753/
Please keep in mind that the research conducted was on rats and not humans. Therefore, it cannot be definitively concluded that Mildronate would have the same impacts on people. Further research is necessary to validate these findings and explore the potential applications of Mildronate for managing or preventing type 2 diabetes in humans.
Maria Sharapova Mildronate scandal
2016 Maria Sharapova failed a drug test and was banned from tennis for 2 years. The ban was later reduced to 15 months. Sharapova is a well-known figure in women's tennis.
Maria Sharapova was the winner of Grand Slam events. She has secured endorsement deals and pursued other business ventures thanks to her many victories, making her the highest-earning female athlete of the year.
During the 2016 Australian Open, Maria Sharapova was found to have taken Meldonium, a drug that had been recently added to the prohibited substances list.
Maria Sharapova preemptively announced the failed drug test at a March 2016 news conference promoted via her social media and live-streamed over her website.
At the news conference, she admitted her guilt but explained the context of the failed test, indicating the substance was found in a prescription drug she had been taking for over a decade.
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Nootropics I’ve ordered in the past
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