As many of you know, I’ve been pointing the finger at fluoride toxicity as a major overlooked culprit in chronic migraine for awhile now.

I’ve written blog posts on fluorine and fluoride in dental products and why toxic halides like bromide, fluoride, and chlorine need to be avoided for those suffering with chronic migraine.

We know fluoride is an industrial waste product that has been injected into our water and toothpaste and that our exposure levels to this mineral are increasing as it shows up in more and more pesticides, commercial products as flame retardants and more importantly, in medications.

Although fluoride toxicity has become controversial, mainly because the harms are being downplayed by industry in order to justify continuing to put it in water and dental products, fluoride’s harmful effects are clear when looked at through a purely biochemical lens: fluorine is the most electronegative and reactive of all the elements.

Fluorine is usually bound to other minerals, but these mineral bonds are not always stable and are affected by pH changes in the body once ingested. This is known as fluorine defluorination. This point is crucial, because the supposed safety of fluorinated medications is predicated upon the idea that the fluorine carbon bond is stable, which it is not, depending on conditions. In a paper titled “The Dark Side of Fluorine,” Yue Pan points out that “Despite the perceived stability of the C-F bond, chemical instability and drug-metabolizing enzymes can lead to its cleavage. The resulting release of fluoride and formation of certain metabolites may cause safety issues and warrant the medicinal chemists’ attention” (source).

One key thing to keep in mind is that while the safety of fluoride has been a politically charged one due to industry propaganda, there is no shortage of scientific evidence pointing to fluoride toxicity and harms. Instead, there is robust scientific evidence showing the damaging effects of fluoride, in part because fluoride is a naturally-occuring mineral that is found in groundwater in many regions of the world and therefore has been studied extensively in the context of skeletal fluorosis and other physiological problems plaguing those with high exposure to fluoride.

I myself grew up in a high-fluoride area in my home state of New Mexico. I grew up on an intentional community with natural hotsprings, and these springs contain 14 ppm of fluoride, so I was likely absorbing much of it through my early years. Luckily, the well water that I drank growing up was low in fluoride. I believe many of my health conditions as a teen came from this fluoride exposure and that this high body burden of fluoride set the stage for becoming even more harmed by this mineral as I got exposed to more of it through antibiotics and anesthesia.

While the general population (in the US) has been subject to water fluoridation since the 50s and 60s, the use of fluoride in medications, antibiotics, anesthesia, and pesticides started in the 80’s and have only increased since that time. Therefore, our exposure and load of fluoride has increased, and will continue to increase, unless we become aware of this and take measures to address exposure to this potent toxin.

Today I want to share my treasure trove of research notes that I found in the course of asking some more fundamental questions about fluoride – the levels we are being exposed to, where they show up, which organs and enzymes are affected, which minerals fluoride depletes, etc.

While most of the research notes below focus on the general mechanisms of fluoride toxicity in the body, please note the section on pineal gland calcification as a result of fluoride toxicity, and how this calcification and lowered melatonin levels are associated with sleep disturbances and higher incidences of migraine.

Table of Contents hide

I’ll start with the most important question of all: does fluoride have any nutritional function in the body?

Fluoride is often described as essential for the body to harden teeth. However, just because the dental industry uses its chemical properties (ie, its acidity) to attract calcium to tooth enamel, doesn’t mean that fluoride is an essential mineral for human health. It is not: “Currently, there is no known essential function for fluoride in cells and organisms.”
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7261729/

Not only does fluoride NOT have a nutritional function, it is a major inhibitor of enzymes in the body (again, perhaps because fluorine is the most electronegative and reactive of all the elements). This can explain why fluorine/fluoride is such a problem for human health:

“[It]has only been recognized since 1981, 35 years after the beginning of fluoridation, that fluoride forms a very strong bond with the hydrogen atoms of proteins and nucleic acids.This type of chemical reaction enables fluoride to alter the shape of many enzymes, which are made from proteins; and it leads also to fluoride bonding with hydrogen bonds of nucleic acids, thus damaging the structure of DNA, the gene material.”

https://www.olaloa.com/resources/articles-on-nutrition/347-abcs-of-fluoridation

How have our exposure levels to fluoride changed over the years?

“In 1939, before fluoridation, human tissue fluoride levels were below 1 PPM. By 1965 they had risen to 1.5 PPM in brain and in 1983 the medulla and midbrain were measured over 10 PPM, more than sufficient to disrupt the biochemistry and vitality of the nerve cells. Of course, bone cells accumulate up to a thousand times more fluoride.”

https://www.olaloa.com/resources/articles-on-nutrition/347-abcs-of-fluoridation

“There was a difference of 31.6% in dental fluorosis prevalence between 2012–2011 when compared to data from 2002–2001 in adolescents aged 16 and 17 years. The continued increase in fluorosis rates in the U.S. indicates that additional measures need to be implemented to reduce its prevalence.”

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5929463/

What are some of the sources of our increased exposure to fluoride?

“Fluorides enter the atmosphere during volcanic eruptions and from anthropogenic sources related to the development of industry and civilization, i.e., coal-fired power plants, steel and aluminum works, glass factories, brickyards and enamel factories, and plant-producing phosphorus fertilizers. Rotationally from the atmosphere, they return to the ground along with dust, snow, rain, or fog, and they can seep into ground and surface waters, as well as accumulate in soil and plants. Plant protection agents and phosphorus fertilizers additionally enrich the soil with fluorides. Its level in nature determines the nature of the parent rock, chemical composition and pH, and ranges from several dozen to several hundred parts per million (ppm). The exceptions are the areas of endemic fluorosis, where this value can be exceeded many times over 8000 ppm. Recently, there has been a disturbingly high increase in fluoride levels in the superficial soil layers. The reason is probably the widespread use of phosphorus fertilizers and the contamination associated with the emission of these compounds into the atmosphere.”

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9920376/

How does the body process fluoride?

“After ingestion fluoride is absorbed through the stomach and small intestine in a pH-dependent and independent manner respectively. In the acidic environment of the gastric lumen, fluoride is absorbed in the form of hydrogen fluoride while in the proximal small intestine fluoride is absorbed in the form of fluoride ion. The maximum amount of absorbed fluoride is retained in the calcified tissues but the distribution of fluoride to the soft tissues depends on the rate of the blood flow to those organs. The ratio of fluoride concentration in tissue/plasma varies among different tissues where kidney exhibits a high ratio compared to other organs.”

https://www.sciencedirect.com/science/article/pii/S2352304222002495

Who is most susceptible to the damaging effects of fluoride?

“It is clear that certain subsets of the population are particularly vulnerable to fluoride’s toxicity. Populations that have heightened susceptibility to fluoride include infants, individuals with kidney disease, individuals with nutrient deficiencies (particularly calcium and iodine), and individuals with medical conditions that cause excessive thirst.”

https://fluoridealert.org/studies/vulnerable-populations/

How does fluoride act as a toxin in the body?

“The pathomechanism of the toxic effect of fluorides is based on the formation of insoluble calcium fluoride in the body, which causes a significant decrease in blood calcium levels, i.e., hypocalcemia, and a simultaneous increase in potassium levels. The symptoms of acute poisoning depend on several factors, such as the dose, the pH of the substance, the method of administration, the patient’s age, acid–base balance, and the degree of absorption. They usually appear shortly after the poison is ingested. There are four groups of disorders in this type of poisoning: 1. inhibition of enzymatic processes; 2. production of calcium complexes; 3. Shock; and 4. organ damage.”

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9920376/

“Despite its beneficial role which is restricted only in skeletal tissues, deleterious effects are also observed in soft tissues and systems. The generation of enhanced oxidative stress is the commencement of excess fluoride exposure which may lead to cell death. Fluoride causes cell death through autophagy via Beclin 1 and mTOR signalling pathways. Beside these, several organ specific anomalies through different signaling pathways have been documented. Mitochondrial dysfunction, DNA damage, autophagy and apoptosis are the damaging outcomes in case of hepatic disorders. Urinary concentration defects and cell cycle arrest have been reported in renal tissues. Abnormal immune response has been characterized in the cardiac system. Cognitive dysfunction, neurodegenerative condition and learning impairment have also been observed. Altered steroidogenesis, gametogenic abnormalities, epigenetic alterations and birth defect are the major reprotoxic conclusions. Abnormal immune responses, altered immunogenic proliferation, differentiation as well as altered ratio of immune cells are well-defined anomalies in the immune system. Though the mechanistic approach of fluoride toxicity in physiological systems is common, it follows different signaling.

Fluoride toxicity is associated with overproduction of reactive oxygen species (ROS), generation of nitric oxide (NO) and also reduction of antioxidant defense. Enhanced ROS generation can be explained by the production of superoxide anions which in turn activates downstream consequences like the generation of peroxynitrite, hydrogen peroxide and hydroxyl radicals. NO reacts with superoxide anions forming peroxynitrite and also reacts with metal centers along with thiols of proteins forming nitrosyl adducts.1 All these products can generate oxidative stress. Excessive ROS production results in free radical attack of the membrane phospholipids and causes lipid peroxidation along with depolarization of mitochondrial membrane. Fluoride also causes DNA damage in different cell types due to upsurge oxidative strain. It also suppresses the activity of the DNA polymerase enzyme thereby affecting DNA replication and also repair process which also supports the evidence of fluoride mediated DNA damage.11 Available reports revealed that fluoride causes inhibition of protein synthesis and/or secretion and leads to activation of signalling pathways engaged in proliferation and also apoptosis which include nuclear factor kappa B NF-κB), activator protein-1, mitogen-activated protein kinase (MAPK) and p53.”

https://www.sciencedirect.com/science/article/pii/S2352304222002495

How much fluoride is excreted, and how much retained, after exposure?

“There is much debate on the topic of fluoride as a human neurotoxicant. Developing brains are significantly more susceptible to neurotoxic damage from fluoride than mature brains are. Children have a higher fluoride retention rate than adults; adults typically retain 50–60% of ingested fluoride, while infants and children retain approximately 80–90%.”

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8700808/

“Approximately 80% or more of orally ingested fluoride is absorbed in the gastrointestinal tract [1]. In adults, about 50% of absorbed fluoride is retained, and bones and teeth store about 99% of fluoride in the body. The other 50% is excreted in urine. In young children, up to 80% of absorbed fluoride is retained because more is taken up by bones and teeth than in adults.

Individual fluoride status is not typically assessed, although fluoride concentrations can be measured in plasma, saliva, urine, bones, nails, hair, and teeth. Criteria for adequate, high, or low levels of fluoride in the body have not been established.

The FNB found the data insufficient to derive EARs for fluoride. Therefore, the board established AIs for all ages using estimated intakes shown to maximize reductions in the incidence of dental caries without unwanted side effects.

Fluoride concentrations in breast milk are so low that they cannot always be detected; when these levels can be measured, they range from less than 0.002 to 0.01 mg/L, even when mothers live in communities with fluoridated water.”

https://ods.od.nih.gov/factsheets/Fluoride-HealthProfessional/#:~:text=Analysis%20of%201999%E2%80%932004%20NHANES,in%20those%20age%2040%E2%80%9349.

Which organ and neuroendocrine systems does fluoride affect the most?

“Because the fluoroquinolones have a large volume of distribution, they concentrate in tissues at levels that often exceed serum drug concentrations. Penetration is particularly high in renal, lung, prostate, bronchial, nasal, gall bladder, bile and genital tract tissues.”

https://www.aafp.org/pubs/afp/issues/2000/0501/p2741.html

“Liver is responsible for the maintenance of metabolic homeostasis of the body and is susceptible to fluoride toxicity. It alters the balance of pro-oxidants and antioxidants of the liver which ultimately causes morphological, biochemical and functional abnormalities. Kidney is a soft target of fluoride-induced adverse effects due to metabolism kinetics, bio-concentration and excretion. Enhanced oxidative stress in terms of increased nitrosative stress and decreased antioxidants lead to damages of nucleic acid protein as well as the structure–function aspect of nephron. Fluoride mediated enhanced oxidative strain also leads to cardiac disorders like ischemia and cardiac failure. 18 nicotinamide adenine dinucleotide phsphataeoxidase (NOX) is a vital source of ROS in vasculature which is activated by excess fluoride and leads to vascular disorders and coronary heart disease. Fluoride is also considered as the potent toxin of the central nervous system which causes altered cerebral function, neuronal apoptosis, mpairment of learning and memory. Structure–function alterations of testis and epididymis have been reported due to fluoride threat which gradually leads to male infertility. Decreased fertility, reduced number of viable fetuses and endometrial apoptosis have been well characterized in the female reproductive system following overexposure to fluoride. Inflammation is the first response of the immune system following tissue damage or infection and over-exposed fluoride is responsible for the generation of such response.1 Expression of the pro-inflammatory cytokines is under the control of transcription factors including NF-κB which also exerts fluoride mediated regulation.”

 https://www.sciencedirect.com/science/article/pii/S2352304222002495

“Fluoride directly or indirectly stimulates the parathyroid glands causing secondary hyperparathyroidism leading to bone loss.[19] Secondary hyperparathyroidism can contribute to a number of diseases like osteoporosis, hypertension, arteriosclerosis, degenerative neurological disease, diabetes mellitus, some forms of muscular dystrophy and colorectal carcinoma.”

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4800930/

“Accumulation of fluoride in temporomandibular joint can also occur & lead to temporomandibular disorders. Animal studies indicate fluorosis may exert adverse effects in the temporomandibular joint (TMJ) structures. Animal studies have been reported on TMJ but there are only few studies which have been done on human subjects.”

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4717726/#:~:text=Accumulation%20of%20fluoride%20in%20temporomandibular,TMJ)%20structures%20%5B7%5D.

“The effects of fluoride on endocrine tissues has not been sufficiently explored to date. The current body of knowledge suggest significant effects of that mineral on reducing sex hormone levels, which may consequently impair fertility and disrupt puberty. The majority of studies confirm that sodium fluoride increases TSH levels and decreases the concentrations of T3 and T4 produced by the thyroid. Moreover, a correlation was observed between NaF and increased secretion of PTH by the parathyroid glands, without a significant impact on body calcium levels. Probably, fluoride may exert adverse effects on insulin levels, impairing pancreatic function and resulting in abnormal glucose tolerance. Observations also include decreased levels of cortisol secreted by the adrenal glands. In light of the few existing studies, the mechanism of fluoride toxicity on the endocrine system has been described.”

https://pubmed.ncbi.nlm.nih.gov/32758781/

Why is fluoride used in medications?

“Fluorine is a common element added to pharmaceuticals because it can increase the drug’s selectivity enable it to dissolve in fats, and decrease the speed at which the drug is metabolized, thus allowing it more time to work. Twenty to thirty percent of drugs contain the element, including some of the most widely prescribed drugs such as well-known antibiotics, anti-inflammatories, anti-depressants, cholesterol-lowering medications, and some inhaled anesthetics.

Fluorine rarely occurs naturally in biological molecules, and many compounds containing fluorine are toxic. Fluorine is the most electronegative and reactive of all the elements, and it forms an extremely tight bond with carbon that is difficult for enzymes to break down. This can make it a useful additive for pharmaceutical chemicals, but fluorine’s reactivity also makes it a difficult element to work with.”

https://journals.sagepub.com/doi/10.1177/2156587211428076#:~:text=The%20toxic%20effects%20of%20fluoride,%2C%20(c)%20cellular%20poisoning%20(

By which mechanism does fluoride work as an antibiotic?

“Fluoride has a strong antibacterial effect due to its inhibition of many enzymes, the most important of which are: enolase, F-ATPase, sulfatase, catalase, phosphatase, phosphoglucomutase, and others. In the case of bacterial enolase, fluorine is likely to combine with the magnesium found in the enzyme, thereby reducing glucose transport into the bacterial cell.”

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9920376/

When were fluoride based antibiotics first introduced?

“The original fluoroquinolone agents were introduced in the late 1980s. Shortly thereafter, ciprofloxacin became the most frequently used antibiotic throughout the world.7 The first fluoroquinolones were widely used because they were the only orally administered agents available for the treatment of serious infections caused by gram-negative organisms, including Pseudomonas species.”

https://www.aafp.org/pubs/afp/issues/2000/0501/p2741.html

Which approved medications contain fluoride?

You can search medications in this database to see if they contain fluoride, although new medications containing fluoride are always coming onto the market, and this list may not be complete. Fluoride toxicity is a growing problem.

“This review describes the recent Food and Drug Administration (FDA)-approved drugs (in the year 2021) containing at least one halogen atom (covalently bound). . . The number of halogenated molecules that are reaching the market is regularly preserved, and 14 of the 50 molecules approved by the FDA in the last year contain halogens.”

https://www.slweb.org/Protocol.pdf

“Since the ocean contains approximately 1.4 ppm fluoride, ocean fish, such as tuna, contains fluoride. Fluoride in any fish is especially concentrated when it is canned, especially because canned fish often contains bones. Avoid all canned fish. . Fluoride can be inhaled via ocean mist, air pollution, e.g. from coal burning buildings & aluminum and many other manufacturing sources, and from cold water humidifiers if fluoridated water is used.

Vitamin and mineral supplements are useful and can be important – in theory. The trouble with calcium and magnesium (and other) supplements is that they are very often contaminated with fluoride, and one never can tell, as most labs do not even test for F content. (We are working to find a good source of F-free supplements that we can suggest to people.)”

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8912053/

“Medications can contain fluoride. For example, voriconazole (VFEND or Vfend) is an oral antifungal medication used to treat several infectious conditions, including invasive aspergillosis, candidemia, and candidiasis. Typical doses of voriconazole provide 65 mg/day fluoride. Long-term use (e.g., for 4 months or more) of this medication can lead to high fluoride concentrations in serum. The prescribing information for voriconazole advises discontinuation of voriconazole if skeletal fluorosis and periostitis (inflammation of the membrane surrounding and protecting the bones) develop.”

https://ods.od.nih.gov/factsheets/Fluoride-HealthProfessional/#:~:text=Analysis%20of%201999%E2%80%932004%20NHANES,in%20those%20age%2040%E2%80%9349.

“The ingredients in a Prozac capsule include 20mg of fluoxetine, maize starch, dimethicone 350, gelatin, iron oxide yellow CI77492, patent blue V CI42051, titanium dioxide and edible black ink, according to the Therapeutic Goods Administration. 

Fluoride is not the main ingredient in Prozac, according to the Campaign for Better Health. Fluoxetine, the active ingredient in Prozac, is made up of 18.5 per cent of fluoride and the remaining 81.5 per cent of the drug is comprised of oxygen, nitrogen, hydrogen and carbon. “

Source

>>>Although the article is stating that the fluoride ingredient claim is false, they basically admit that Prozac contains about 3.6 mg of fluoride, ie that Prozac is contributing to fluoride toxicity.

All SSRIs have fluoride in them except Zoloft.

https://www.socialanxietysupport.com/threads/does-lexapro-contain-fluoride.849057/

How can the damaging effects of fluoride in medications be mitigated?

“Absorption of orally administered fluoroquinolones is significantly decreased when these agents are coadministered with aluminum, magnesium, calcium, iron or zinc, because of the formation of insoluble drug–cationic chelate complexes in the gastrointestinal tract. The problem can be overcome largely by administering products containing these metal ions at least four hours before or two hours after oral administration of a fluoroquinolone.”

https://www.aafp.org/pubs/afp/issues/2000/0501/p2741.html

How much fluoride are people exposed to through dental products?

“Fluoride toothpaste makes up more than 95% of toothpaste sales in the U.S.2The American Dental Association recommends use of a fluoride toothpaste displaying the ADA Seal of Acceptance. Fluoride toothpastes available over the counter in the U.S. generally contain a fluoride concentration of 1,000 to 1,500 ppm. Prescription-strength fluoride toothpastes contain 5,000 ppm fluoride as sodium fluoride. In the U.S., the active ingredient in fluoride-containing toothpastes can be sodium fluoride, sodium monofluorophosphate, or stannous fluoride.

Over-the-counter solutions of 0.05% sodium fluoride (230 ppm fluoride) for daily rinsing are available for use by persons older than 6 years of age; use in persons younger than 6 years of age is not recommended because of the risk of fluorosis if the rinse is swallowed repeatedly.3, 6 Higher strength mouthrinses (e.g., 0.2% neutral sodium fluoride to be used once a week) for those at high risk of tooth decay must be prescribed by a dentist or physician.2 Solutions of 0.2% sodium fluoride (920 ppm fluoride) are also used in supervised, school-based weekly rinsing programs.

There are also self-applied gel formulations of sodium fluoride (1.1% [5,000 ppm] sodium fluoride) or stannous fluoride (0.15% [1,000 ppm] fluoride) available by prescription for home use.

Fluoride Mouthrinse, Gels, or Foams. Professionally applied fluorides are in the form of a gel, foam or rinse, and are applied by a dental professional during dental visits. These fluorides are more concentrated than the self-applied fluorides (e.g., 1.23% fluoride ion [12,300 ppm]), and therefore are not needed as frequently.

Because an early study7 reported that fluoride uptake by dental enamel increased in an acidic environment, fluoride gel is often formulated to be highly acidic (pH of approximately 3.0).3 Products available in the U.S. include gels of acidulated phosphate fluoride (1.23% [12,300 ppm] fluoride), as 2% neutral sodium fluoride products (containing 9,000 ppm fluoride), and as gels or foams of sodium fluoride (0.9% [9,040 ppm] fluoride).

Fluoride-Containing Prophylaxis Paste. Fluoride-containing paste is routinely used during dental prophylaxis. The abrasive paste, which contains 4,000 to 20,000 ppm fluoride, might restore the concentration of fluoride in the surface layer of enamel removed by polishing, but it is not an adequate substitute for fluoride gel or varnish in treating persons at high risk for dental caries. Fluoride prophylaxis paste alone is not considered by the U.S. Food and Drug Administration (FDA) or ADA an effective method to prevent dental caries.

Fluoride Varnish. Varnishes are available as sodium fluoride (2.26% [22,600 ppm] fluoride) or difluorsilane (0.1% [1,000 ppm] fluoride) preparations.2, 5, 6 A typical application requires 0.2 to 0.5 mL, resulting in a total fluoride ion application of approximately 5 to 11 mg.

Fluoride supplements can be prescribed for children ages 6 months to 16 years who are at high risk for tooth decay and whose primary drinking water has a low fluoride concentration.2, 25 Tablets and lozenges are manufactured with 1.0, 0.5, or 0.25 mg fluoride. Most supplements contain sodium fluoride as the active ingredient. To maximize the topical effect of fluoride, tablets and lozenges are intended to be chewed or sucked for 1–2 minutes before being swallowed; for infants, supplements are available as a liquid and used with a dropper.3 Dosing is based on the natural fluoride concentration of the child’s drinking water and the age of the child.”

https://www.ada.org/en/resources/research/science-and-research-institute/oral-health-topics/fluoride-topical-and-systemic-supplements

How can I find non-fluoridated toothpaste, tooth powders, floss, and a fluoride-free dentist?

https://www.hiddencauseofacne.com/fluoride-free-toothpaste

Which minerals does fluoride deplete?

“Is it possible that negatively charged fluoride, which we consume in our food and water in the amount of about 5 mg per day, might form insoluble salts with positively charged essential minerals, such as chromium (200 mcg per day), selenium (50 mcg per day), molybdenum (50 mcg per day), copper and boron (1 to 2 mg per day)? “

https://www.olaloa.com/resources/articles-on-nutrition/407-antioxidants-and-your-heart

“At both the single- and multi-cellular level, fluoride exposure causes . . . electrolyte imbalance. The exact mechanism is unknown. Prolonged exposure of vertebrates to high fluoride results in the loss of calcium and magnesium from the plasma, and an excess of potassium. Complementary to this finding, fluoride exposure in single cells results in an influx of calcium and magnesium, and a loss of potassium. This effect has been proposed to be due to either downstream stress signaling, or the binding of fluoride to metals. Regardless of mechanism, the imbalance of electrolytes in organisms from fluoride exposure has far reaching implication in cell homeostasis and signaling disruption.”

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7230026/

“The sodium iodide symporter (NIS) is the plasma membrane glycoprotein that mediates active iodide transport in the thyroid and other tissues, such as the salivary, gastric mucosa, rectal mucosa, bronchial mucosa, placenta and mammary glands. In the thyroid, NIS mediates the uptake and accumulation of iodine and its activity is crucial for the development of the central nervous system and disease prevention. Since the discovery of NIS in 1996, research has further shown that NIS functionality and iodine transport is dependent on the activity of the sodium potassium activated adenosine 5′-triphosphatase pump (Na+, K+-ATPase). In this article, I review the molecular mechanisms by which F inhibits NIS expression and functionality which in turn contributes to impaired iodide absorption, diminished iodide-concentrating ability and iodine deficiency disorders. I discuss how NIS expression and activity is inhibited by thyroglobulin (Tg), tumour necrosis factor alpha (TNF-α), transforming growth factor beta 1 (TGF-β1), interleukin 6 (IL-6) and Interleukin 1 beta (IL-1β), interferon-γ (IFN-γ), insulin like growth factor 1 (IGF-1) and phosphoinositide 3-kinase (PI3K) and how fluoride upregulates expression and activity of these biomarkers. I further describe the crucial role of prolactin and megalin in regulation of NIS expression and iodine homeostasis and the effect of fluoride in down regulating prolactin and megalin expression. Among many other issues, I discuss the potential conflict between public health policies such as water fluoridation and its contribution to iodine deficiency, neurodevelopmental and pathological disorders. Further studies are warranted to examine these associations.

While it is acknowledged that iodine deficiency increases the risk of fluoride (F) induced toxicity on thyroid function [9], it has also been reported that dietary iodine absorption and incorporation is reduced by F. . . Moreover, iodine deficient individuals were found to have higher urinary F concentrations compared with the non-iodine deficient group.”

https://www.mdpi.com/1660-4601/16/6/1086

“Excess ingestion of fluoride is a major cause for anaemia during pregnancy and in low birth-weight babies due to nonabsorption of nutrients including iron supplementation.9 Hillman et al. 10 in 1979 showed that anaemia in cattle was the result of fluoride toxicity and fluorosis. They also showed that serum folic acid and vitamin B12, an essential constituent for haemoglobin biosynthesis, were inhibited by fluoride poisoning. Therefore, excess consumption of fluoride is a cause for concern.”

https://www.nmji.in/content/141/2016/29/4/Images/NatlMedJIndia_2016_29_4_200_195959.pdf

Why does the pineal gland accumulate fluoride more than other glands, and what are the implications of this?

“The pineal gland is an endocrine gland whose main function is the biosynthesis and secretion of melatonin, a hormone responsible for regulating circadian rhythms, e.g., the sleep/wake cycle. Due to its exceptionally high vascularization and its location outside the blood–brain barrier, the pineal gland may accumulate significant amounts of calcium and fluoride, making it the most fluoride-saturated organ of the human body. Both the calcification and accumulation of fluoride may result in melatonin deficiency.

One of the most interesting soft tissues able to accumulate fluoride is the pineal gland. However, while knowledge of the calcification of this organ dates back to the 17th century, the first reports on its accumulation of fluoride appeared only in the mid-1990s.

In humans, the pineal gland is a neuroendocrine gland weighing about 150 mg. The organ, part of the epithalamus, is located between the colliculi superiores of the lamina tecti, at the back of the posterior wall of the third brain ventricle. The pineal gland is characterized by a very rich network of blood vessels, which ensures blood flow of 4 mL/min/g, second only to the blood supply to the kidneys.

Another unique anatomical feature of the gland is its location outside the blood–brain barrier. Therefore, unlike most other brain structures, the pineal gland has open access to blood and all of its components. Extremely rich vascularization and no significant restrictions in transport from the bloodstream make it possible for the pineal gland to accumulate significant amounts of various substances, mainly, calcium; microelements such as cobalt, zinc, and selenium; and fluoride.

https://www.mdpi.com/2076-3417/10/8/2885

Is there a correlation between pineal gland calcification and migraine?

“The pineal gland calcifications have been associated with some diseases such as cerebral infarction, Alzheimer’s disease and intracerebral hemorrhage while most cases are considered idiopathic and physiologic. However, there are limited data in the current literature about the association of pineal calcification and migraine. Our aim was to evaluate this association between migraine and pineal calcification by computed tomography of the brain. When migraine and control groups were compared by pineal calcification, the rates were determined as 80, 6% and 55% in migraine and control group, respectively. The difference was statistically significant (p < 0.001). In addition, it was seen that pineal calcifications, detected in migraine patients, did not show age-related increase. According to our data, we can point that pineal calcification may be associated with migraine.”

https://pubmed.ncbi.nlm.nih.gov/26531271/

“In humans, the pineal gland is a neuroendocrine gland weighing about 150 mg. The organ, part of the epithalamus, is located between the colliculi superiores of the lamina tecti, at the back of the posterior wall of the third brain ventricle). The pineal gland is characterized by a very rich network of blood vessels, which ensures blood flow of 4 mL/min/g, second only to the blood supply to the kidneys. Another unique anatomical feature of the gland is its location outside the blood–brain barrier. Therefore, unlike most other brain structures, the pineal gland has open access to blood and all of its components. Extremely rich vascularization and no significant restrictions in transport from the bloodstream make it possible for the pineal gland to accumulate significant amounts of various substances, mainly, calcium; microelements such as cobalt, zinc, and selenium; and fluoride.”

https://www.mdpi.com/2076-3417/10/8/2885#:~:text=2.-,Pineal%20Gland%E2%80%94Anatomy%20and%20Physiology,58%5D%20(Figure%201).

How does fluoride affect the pH of the body tissues?

As I have mentioned in previous posts, the pH of our tissues has a profound effect on the voltage of our body and the levels of pain that we experience, since acidic conditions are hypoxic conditions, and acidic conditions are low voltage conditions that lead to pain. Therefore, the question of the degree to which fluoride causes acidosis is important when it comes to understanding how it contributes to migraine or any other inflammatory chronic pain condition.

“Fluoride exposure is also associated with a drop in intracellular pH. Fluoride is a weak acid that enters cells as HF and dissociates, thus releasing one proton per fluoride. Consequently, the more fluoride that enters a cell, the more acidic the cytoplasm becomes. However, fluoride causes intracellular acidification to a larger degree than can be explained by proton shuttling.). Many hypotheses have been put forward to explain this observation. Among these, the most common are metabolic disruption, perturbation of the mitochondria, transmembrane protein inhibition, and induction of stress signaling.

Fluoride inhibits metabolism through an unclear mechanism, the downstream effects include reduction in intracellular ATP and damage to the mitochondria. ATP is reduced both in cells containing mitochondria – which display signs of permanent damage and reduced respiration after fluoride exposure – and in erythrocytes (red blood cells), which lack mitochondria and produce ATP solely through anaerobic glycolysis.. ATP depletion leads to the hydrolysis of ATP into ADP and AMP along with the release of protons, consequently leading to intracellular acidification. Damage to the mitochondria releases free radicals, resulting in oxidative stress. This in turn causes DNA damage, metabolic disruption, ATP hydrolysis, protein inhibition, and intracellular acidification. However, just as free radicals are known to disrupt metabolism, acidify the cell, and activate stress signaling, each of these phenotypes also activate the release of free radicals from the mitochondria. As such, the order in which each known phenomenon occurs is difficult to determine.”

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7230026/

How does fluoridation of the water supply affect leeching of other toxic minerals into our water?

“Fluoridated municipal drinking water—including water that people drink as well as foods and beverages prepared using municipal drinking water—accounts for about 60% of fluoride intakes in the United State. In 2016, 62.4% of the U.S. population had access to a fluoridated community water system.”

https://ods.od.nih.gov/factsheets/Fluoride-HealthProfessional/#:~:text=Analysis%20of%201999%E2%80%932004%20NHANES,in%20those%20age%2040%E2%80%9349.

Tacoma, Washington (1992): The city had to shut down the fluoridation equipment because fluoride had eaten the pipes. The municipal water had approximately 32 ppb lead, but after fluoridation stopped, the lead level dropped to 17 ppb. When the equipment was fixed, the lead level shot right back up to 32 ppb. The city discontinued the use of fluoride, and the lead level again dropped.

Thurmont, Maryland (1994): Lead levels in town water decreased significantly after town officials stopped adding fluoride. Thurmont then voted to officially ban the use of fluoride.

Lebanon, Oregon (2005): The town’s tap water contained more lead after fluoridation began in 2001. “City Administrator John Hitt said that adding fluoride apparently changed the water chemistry enough to cause more lead to be leached from pipes in some houses dating from before the 1960s.

When New York City’s fluoridation treatment was shut down for 3 to 4 months, there was approximately a 20% decrease in the lead concentrations in city water.”

Source: Townsends Letters


How does fluoride toxicity affect the microbiome?

“Unfortunately, none of the studies retrieved examined the effects of ingested fluoridated water on the human microbiome. Animal studies generally examined acute fluoride toxicity following ingestion of fluoridated food and water and conclude that fluoride exposure can detrimentally perturb the normal microbiome.”

https://www.sciencedirect.com/science/article/pii/S037842742300098X

What are the implications of increased use of fluoridated pesticides?

“Fluorinated pesticides acquired a significant market share in the agrochemical sector due to the surge of new fluoroorganic ingredients approved in the last two decades. This growing trend has not been accompanied by a comprehensive scientific and regulatory framework entailing all their potential negative impacts for the environment, especially when considering the hazardous properties that may result from the incorporation of fluorine into organic molecules. This review aims to address the safe/hazardous dichotomy associated with fluorinated pesticides by providing an updated outlook on their relevancy in the agrochemical sector and how it leads to their role as environmental pollutants. Specifically, the environmental fate and distribution of these pesticides in the ecosystems is discussed, while also analysing their potential to act as toxic substances for non-target organisms.”

https://www.sciencedirect.com/science/article/abs/pii/S0269749121018972?via%3Dihub

I trust that’s enough research to digest on fluoride toxicity for a day!

Thanks for informing yourself of the harms of fluoride, and be sure to share this article with others if you are concerned about fluoride toxicity and want to help others spare themselves from more harm from this toxic mineral.