07 Feb Melatonin & Heart Health

Melatonin & Heart Health

Art By Dr John Lieurance

Heart Health, Cholesterol & Blood Pressure.

Much of your health depends on how efficiently your heart functions. A poorly functioning heart is the beginning of most diseases, as it would simply mean a lack of efficient supply of blood, oxygen, red cells, white cells, and vital nutrients to all organs of the body.

We need to take special care of our hearts as we only get one for our entire lifetime. Besides, the brain and the heart are among the top two most metabolically sensitive organs in the body, meaning that, any disruption in energy production from the cell will manifest in both these organs first. Of course, the mitochondria are at the core of this energy production, and we’ve already discussed in subsequent chapters how melatonin is very important during stressful situations to protect the mitochondria and our vital energy production.

There are a variety of different actions where melatonin improves the functions of the heart and the entire cardiovascular system. In fact, melatonin produces many favorable effects for your heart, blood vessels, and even helps to lower blood pressure and cholesterol.

In this chapter, we will learn how melatonin helps to improve heart functions and protects you from the disorders linked to high blood pressure, poor cardiac output, and irregular heart rhythm.

Melatonin and cardiovascular diseases

Atherosclerosis is one of the most common chronic vascular diseases in which oxidative stress and inflammation are implicated to be the major causative factors. The early stages of the development and deposition of cholesterol plaques involve endothelial activation, which is induced by the oxidized low-density lipoproteins, inflammatory cytokines, and the modifications in endothelial shear stress.

The research study “Melatonin and Cardiovascular Disease: Myth or Reality?” published in the Cardiologia in March 2012 has shown that melatonin can help to reduce the risk of atherosclerosis by decreasing the levels of LDL or bad cholesterol and increasing the levels of HDL, the good cholesterol.

The study suggested that the antioxidant effects of melatonin on low-density lipoprotein oxidation may depress the plasma level of total cholesterol and VLDL (very low-density lipoprotein) cholesterol. This action of melatonin is linked to improved heart health. It indicates that this hormone would protect the heart against atherosclerosis that basically occurs due to the deposition of cholesterol plaques along the walls of the arteries.

Basically, these plaques are formed when your diet comprises foods rich in unhealthy, pro-inflammatory fats, like trans fats and saturated fats, but lacks healthy fats like monounsaturated fats (MUFA) and polyunsaturated fats (PUFA). Heated up vegetable oils are the main culprit that needs to be avoided. These are the primary oils used in restaurants to cook food, therefore it’s almost impossible to eat out regularly and avoid them. Plaque buildup can also be indirectly related to when your liver is not efficient enough to metabolize fats.

These unhealthy fats oxidize very easily then tend to remain circulating in the bloodstream without being utilized to supply energy to the body. The high level of oxidation and inflammation will erode the protective layer within the blood vessels making it easier for this plaque to accumulate. These circulating fats, over a period of time, form thick plaques that get deposited at various places along the inner walls of the blood vessels, thus clogging them. In younger individuals, these plaques are generally softer and can dislodge, creating a higher risk of stroke. As we get older, they harden and become more calcified, with less risk of a stroke but lead to poor circulation. These plaques can lodge themselves in the arteries that supply blood to the heart or your brain. The result would be a heart attack or stroke, respectively.

These dangerous consequences of high cholesterol levels could be avoided if your body has sufficient melatonin. Melatonin may reverse the hypercholesterolemic states by increasing an endogenous cholesterol clearance effect.

This means melatonin would stimulate the rate at which cholesterol in the bloodstream and tissues is cleared from the body through various mechanisms, like being burnt up for energy or broken down to be eliminated.

Due to its lipophilic nature, melatonin can also enter the lipid phase of low-density lipoprotein particles readily and prevent lipid peroxidation. To confirm this hypothesis further, this study even showed the association between nocturnal raised levels of oxidized LDL (low-density lipoprotein) and the reduced melatonin levels in patients with atherosclerosis-induced myocardial infarction.

These findings support the theory that melatonin has the potential to lower total cholesterol levels and stimulate the levels of good or high-density lipoprotein cholesterol levels. And these changes would be protective against the development of cardiovascular diseases.

The study showed that the administration of melatonin in pharmacological doses would also reduce blood pressure as a consequence of different mechanisms, including the direct hypothalamic effect it can produce.

For example, melatonin would act on the hypothalamus and regulate its activities to ensure your blood pressure stays within normal limits. Similarly, it may also help to lower catecholamine levels, cause relaxation of the smooth muscles in the walls of blood vessels, and most importantly, produce antioxidant effects. So, here’s the dichotomy, as we get older, we have lower melatonin levels, and our blood pressure goes up. Doctors then give us blood pressure-lowering medications that have a negative effect on our melatonin levels. If more doctors were aware of how melatonin works with blood pressure, there would be fewer prescriptions for blood pressure medications and many more for melatonin supplementation.

Catecholamines are hormones secreted by your adrenal glands, located at the top of your kidneys. Some examples of catecholamines include norepinephrine, dopamine, and epinephrine (which was earlier called adrenalin). Your adrenal glands secrete and release catecholamines into the blood when you are emotionally or physically stressed. Some of the typical effects of catecholamines include increased heart rate, blood pressure, and blood glucose levels.

Melatonin, with its ability to downregulate catecholamines, could bring your blood pressure within normal limits and prevent the serious consequences related to hypertension, such as stroke and heart attacks. If you are currently taking blood pressure medication it might be a good subject to bring up to your doctor, regarding starting melatonin and having him monitor your blood pressure in order to taper off if you have less of a need for the medication. Please keep in mind, none of the suggestions in this book are meant as medical advice and you should always get the approval of your healthcare provider before you make any changes to your medicines or supplement regime.

How do Mitochondrial dysfunctions affect your heart?

We’ve discussed the mitochondria in detail and how it’s the powerhouse of the cell. Without healthy mitochondria, the cells in your body would no longer be able to produce the energy they need to survive or function.

So, what happens to your heart when stress from inflammation cripples these mitochondria? 

You may want to go back and review the section on how inflammation regulates cytokines which then has a negative effect on how the cell produces energy. How almost all stressful conditions have a commonality where this inflammation and cytokines are upregulated and thus have a negative impact on the mitochondria. How we start to produce only 4 ATPs versus 36, which is less than 10% of the energy efficiency we would otherwise have. The heart and brain are the 2 most metabolically active organs of your body. So, they also need a continuous source of energy. The functions of these 2 vital organs are highly vulnerable to low energy supply.

And this is why; when your body is struggling with inflammation, the damage it brings to the mitochondria at the cellular level would have a very bad impact on how efficiently your heart works? Let me explain why.

Mitochondria play a crucial role in the normal functioning of your heart and in the pathogenesis of various types of heart diseases. Specific mitochondrial dysfunctions may trigger the development of cardiomyopathies simply by affecting the energy supply to heart muscles. [1]

According to a research study published in the Texas Heart Institute Journal in 2013, the heart depends highly on the generation of oxidative energy in mitochondria to receive the large number of ATPs it requires for its continuous, contractile pumping activities. Additionally, cardiac mitochondria also perform other cellular functions like generating reactive oxygen species (ROS) and regulating cellular apoptosis. [2]

The mitochondria also play a role in the regulation and growth of cardiac bioenergetic arrangement.

Disruptions in energy production due to the impairment of mitochondrial functions have been implicated in a wide range of metabolic, degenerative, neoplastic, and age-related diseases affecting the heart and other organs.

Mitochondrial cardiomyopathies are characterized by impaired heart-muscle functions, structure, or both. It may present in various forms such as hypertension, coronary artery disease, and valvular diseases. The presentation of mitochondrial cardiomyopathies may also include dilated hypertrophic left ventricular non-compaction, ventricular tachyarrhythmia, and heart failure.

This just goes to show the severity or the extent to which mitochondrial dysfunctions can affect the heart.

Is it possible to restore healthy functions of the heart by eliminating the root cause of inflammation-causing mitochondrial dysfunctions? If you can ensure your heart muscles are not deprived of energy during stressful chemistry in the body, much of these complications could be avoided.

The potential use of melatonin as an antioxidant during myocardial infarction

There is evidence suggesting the cardioprotective benefits of melatonin in patients with myocardial infarction. The extent of the ischemic reperfusion injury to the heart could be decreased to some extent when exogenous melatonin is included in the treatment protocol.

Melatonin would reduce the infarct size and the risk area, plus minimize the incidences of reperfusion arrhythmias.

Also, ischemia is associated with the formation of reactive oxygen species from residual molecular oxygen molecules. So, it is suggested that the cardioprotective effect of melatonin is probably associated with its ability to scavenge and destroy free radicals and stimulate the expression of antioxidant enzymes.

The scavenging action of melatonin occurs in both physiological and larger pharmacological doses. Not just melatonin but several of its metabolites have the ability to detoxify free radicals and restore healthy heart functions. Yet melatonin is believed to work by stimulating essential enzymatic intracellular antioxidant enzymes such as superoxide dismutases (SOD) within both mitochondrial and the cytosol of the cell. It may also induce the activities of another powerful intracellular antioxidant called glutathione.

Moreover, it might also protect mitochondria against oxidative stress and thus, ensure the heart muscles receive a good supply of energy needed to perform pumping action and other functions. This indicates the role of melatonin as a bioenergetic agent and its ability to improve mitochondrial functions. Research data suggests that patients with a history of myocardial infarction and angiographic no-reflow tend to have a low level of intra-platelet melatonin and higher systemic oxidative stress than people without this phenomenon.

This data suggest that melatonin may act as a potent antioxidant agent, thus reducing myocardial damage induced by ischemia or reduced oxygen supply to the heart muscles.

Intravenous melatonin in myocardial infarction patients

Interestingly, there have also been attempts to demonstrate the inhibition of ischemic damage to the heart muscles after the administration of melatonin intravenously, especially in patients who have undergone treatments like a percutaneous coronary intervention.

These studies have shown that intravenous, as well as intracoronary injections of melatonin, might limit myocardial damage and help patients recover faster after having suffered a heart attack.

Let’s make a quick note here about what makes melatonin particularly beneficial in acute cases of cardiac emergencies.

The molecules of melatonin can be distributed quickly throughout the body; whether it is administered orally, through a suppository, or oral liposomal as with Sandman. It can cross all physiological barriers and enter the cardiac cells with ease and produce the desired effect to repair the damaged muscles. [3]

Taking care of your heart and cardiovascular system through disease prevention and treatment is where melatonin can really help. The heart has to work harder, and the pressure puts more stress on the blood vessels potentially leading to thickening of these blood vessels, therefore, causing more restriction of blood flow.

As stated, before melatonin keeps blood pressure low and melatonin declines as we get older. So, could it be that it’s the lack of melatonin that is in part causing blood pressure to be elevated?  It’s also been documented that blood pressure medication has a negative effect on our production of melatonin, as well as the quality and duration of our sleep. Most patients with cardiac diseases have to fight the various side effects of blood pressure medications. Balancing the blood pressure first with melatonin and then second with antihypertensive medications makes the most sense to me.

Combined therapy using antihypertensive drugs with melatonin may help to relieve these side effects to a great extent as well. Maybe in a large number of cases simply just adding in melatonin may do the trick. It’s certainly worth trying but it’s important that you do this with the guidance of your healthcare provider and not try to do it by yourself.

How does melatonin help to relieve the side effects of blood pressure medications?

Patients with high blood pressure often suffer from poor sleep quality as a result of the negative effects of medications called beta-blockers.

According to a research study, patients treated for hypertension, who also use melatonin, have an improved quality of sleep compared to those who use only anti-hypertensive drugs. The improvement in sleep quality is in the forms of a shorter sleep onset period, reduced awakening during sleep, and more restful sleep.

This is an important finding considering beta-blockers are widely prescribed to patients with hypertension. These drugs are also used for the treatment of several other cardiovascular diseases, as well as anxiety disorders, migraine, and post-traumatic stress disorder.

It’s known that the lack of sleep can worsen hypertension, by contributing to mental stress and impairing the natural healing mechanisms of the body. Sleep deprivation has also been linked to a higher risk of mortality in patients with heart diseases. And with insomnia being the most common side effect of these drugs, it becomes vital to include melatonin in the treatment protocol when one fully considers all of the research presented in this chapter.

According to another study “Night-time exogenous melatonin administration may be a beneficial treatment for sleeping disorders in beta-blocker patients” published in the Journal of Cardiovascular Disease Research in 2011, a clear improvement in sleep quality can be achieved along with better control over blood pressure by combining the use of beta-blockers and exogenous melatonin.

Also, unlike sedatives that are commonly prescribed to patients with sleep problems, melatonin didn’t produce a “rebound” effect. This means, even after patients stop using melatonin, the improvement in their sleep pattern persists. It does not deteriorate even after going off the supplement, as it happens with several sedatives or sleep drugs. [4]

Remember as stated in previous chapters, there’s no negative feedback loop where or when you take melatonin, no matter how much you take, it does not shut down your own production of melatonin. In fact, it may actually do the opposite and provide a carry-over benefit. So, even after you stop taking melatonin, you may continue to enjoy the benefits of improved sleep. Additionally, the use of melatonin did not show any sign of rising tolerance that would otherwise necessitate the use of higher doses. This shows that melatonin could provide multifactorial benefits by reducing the sleep problems caused due to the side effects of beta-blockers.

Melatonin as a heavy metal chelating agent for heart

According to a research study “Protection of Metal Toxicity by Melatonin -Recent Advances “published in the Research Gate, melatonin has a widespread subcellular distribution that enables it to interact with several toxic metals and molecules, thereby reducing the damage to the organs at the cellular level.

This property of melatonin makes it a powerful chelating agent, moreover, these qualities have been related to the reduced toxicity in the heart and other vital organs by heavy metals. It contributes to the prevention of toxicity induced by heavy metals such as mercury and lead. Melatonin may also alleviate cadmium-induced endoplasmic reticulum and cellular stress, regulate unfolded protein response, influence germ cell apoptosis, and prevent neurotoxic effects.

The protective effects of melatonin against mercurial toxicity may help in the prevention of myocardial toxicity, neurotoxicity, renal toxicity, thyrotoxicity as well as reproductive toxicity. It may also act as a chelating agent against arsenic toxicity as is manifested through its natural anti-oxidative mechanisms. Furthermore, it might also induce mitochondrial biogenesis and autophagy to eliminate these toxins from the heart muscles and valves, thereby restoring the healthy functions and higher efficiency of this organ to pump blood.

This is a huge reason to take melatonin in and of itself. Mitochondrial biogenesis to create new fresh healthy energy-producing cellular components and clearing out all of the weak, damaged, and dysfunctional mitochondria which are just spewing inflammatory and oxidative substances.

Melatonin has also been found to protect the heart against copper, chromium, and aluminum by exhibiting anti-inflammatory, pleiotropic, anti-lipidic, antioxidative, and other therapeutic effects. Moreover, melatonin may also mediate both intrinsic and extrinsic pathways for apoptotic cell death and exhibit anti-metastatic effects through the regulation of NFkB. These pleiotropic functions of melatonin make it a powerful cardioprotective molecule especially for men and women at risk of metal toxicity. [5]

Emerging further studies indicate the possibility that the cholesterol plaques blamed to be the major precursor to most cardiovascular diseases may actually contain microbes. The cholesterol plaques having microbes can create a biofilm on the endocardium (the inner walls of the heart), as well as the heart valves that regulate the flow of blood through different chambers like the atrium and ventricles.

And this new emerging idea makes melatonin more important considering its ability to boost your immune system’s response against infections. The antioxidant property of melatonin would also destroy reactive oxygen species and down-regulate inflammation that would cause damage to cardiac muscles. This in combination with the chelating effect of heavy metals, improved restorative sleep, lowering of the blood pressure, and an improved cholesterol profile, would protect and can even restore heart health to a great extent.

How do you know if you are at a higher risk due to metal toxicity?

You can do testing to determine what type of heavy metal load you have in your body, and it’s important to take into consideration risk factors such as mercury amalgam fillings. Especially if you have mercury amalgam fillings and you drink a lot of hot coffee or tea which will leach the mercury out of the amalgam more rapidly. Other heavy metal risk factors include eating a lot of fish, especially larger predatory fish, vaccinations, and environmental exposure.

For this reason, I think it’s a good idea to take binders when one first starts to embark on melatonin supplementation. You can reference ultimatecellularreset.com for more information about what type of binders, when to take them etc.

Conclusion

Cardiovascular health is incredibly important and the simple fact that melatonin can improve gut function and microbiome health, as well as blood sugar and metabolic disorders makes it unsurprising to see how beneficial melatonin can be in this arena. However, melatonin goes a step further and improves your energy through the mitochondria.

Remember the brain and the heart are the two most metabolically sensitive organs and any challenges with energy are going to show up in both of these places early. Improving sleep will improve stress management, as well as down regulate the sympathetic nervous system which drives blood pressure.

Time and time again, I have seen in the clinic how melatonin improves blood pressure and lipid profiles with my patients. Anyone interested in improving cardiovascular function should seriously consider melatonin supplementation such as Sandman.