As should be obvious from their name, FLUOROquinolones are fluorinated drugs.
A little history for you: Nalidixic Acid is the backbone of all fluoroquinolones. It was discovered by George Lesher in 1962, and it started to be used as an antibiotic in 1967. Nalidixic acid, and the first-generation quinolones that were derived from it, were not widely used because they lacked bioavailability and were associated with the rapid development of bacterial resistance (1). To increase bioavailability, a fluorine atom was added to the nalidixic acid backbone at position 6, bonded to carbon (2 and 3). This increased bioavailability of the quinolones greatly, and their use increased exponentially (more than 26 million prescriptions for fluoroquinolones were given out in 2011 alone).
In addition to increasing the bioavailability of fluoroquinolones, did the addition of the fluorine increase the toxicity of the fluoroquinolones?
How much of Fluoroquinolone Toxicity is due to the quinolone core and how much of it is due to the fluorine addition that, as it is intended, penetrates cells and increases the quinolone efficacy and potency? Is Fluoroquinolone Toxicity quinolone toxicity, or is it fluorine toxicity?
I’ve always been of the opinion that the quinolone core is toxic and that the fluorine just increases the bioavailability and toxicity of the quinolones, and that fluoroquinolone toxicity is quinolone toxicity, not fluorine toxicity. However, recently I’ve been reading about the effects of fluoride, and, more specifically, fluoro-organic metabolites like fluoracetate and fluorocitrate, and I have been considering the possibility that fluoroquinolone toxicity is a result of the addition of the fluorine atom to the quinolone core. I intend to explore the possibility that fluoroquinolones are metabolized into poisonous metabolites like fluoracetate and fluorocitrate in future posts. In this post, I’ll start the conversation by looking at some evidence that the quinolone core is the toxic part of fluoroquinolones, as well as some evidence that the fluorine is the main source of toxicity.
There is a lot of grey area in the question of whether fluoroquinolone toxicity is caused by the quinolone core, the fluorine attachment, or both. It is likely, in my opinion, that both are toxic. There are undoubtably complex feedback and feed-forward loops in our biochemistry that may make one increase the toxicity of the other too.
Argument #1 – Quinolones were toxic before the fluorine was added.
Nalidixic acid and the first-generation quinolones that weren’t fluorinated, have serious and severe adverse effects. For example, Cinoxacin, a first-generation unfluorinated quinolone, has the following adverse-effects (4):
- difficulty breathing
- fever
- increased sensitivity to the sun or ultraviolet light
- irregular heartbeat, palpitations, or chest pain
- joint, muscle, or tendon pain
- nervousness, restlessness, anxiety
- severe stomach or abdominal pain
- severe or watery diarrhea
- seizures (convulsions)
- skin rash or itching
- swelling of the face or neck
- vomiting
- diarrhea (loose stools)
- difficulty sleeping
- dizziness, drowsiness
- headache
- nausea
- stomach upset
In a study of 1,118 patients who took Cinoxacin, it was found that many experienced the following (5):
Gastrointestinal: Nausea was reported most commonly and occurred in less than 3 in 100 patients. Other side effects, occurring less frequently (1 in 100), were anorexia, vomiting, abdominal cramps/pain, perverse taste, and diarrhea.
Central Nervous System: The most frequent side effects were headache and dizziness, reported by 1 in 100 patients. Other adverse reactions possibly related to Cinobac (cinoxacin) include insomnia, drowsiness, tingling sensation, perineal burning, photophobia, and tinnitus. These were reported by less than 1 in 100 patients.
Hypersensitivity: Rash, urticaria, pruritus, edema, angioedema, and eosinophilia were reported by less than 3 in 100 patients. Rare cases of anaphylactic reactions have been reported. Toxic epidermal necrolysis has been reported very rarely. Erythema multiforme and Stevens-Johnson syndrome have been reported with cinoxacin and other drugs in this class.
Hematologic: Rare reports of thrombocytopenia.
Though those aren’t comprehensive lists of fluoroquinolone toxicity symptoms, they’re pretty close. Even reviews of modern fluorinated fluoroquinolones rarely have more comprehensive lists of adverse-effects than the lists for Cinoxacin above.
Argument #2 – The fluorine increases the toxicity so much that it is largely responsible for fluoroquinolone toxicity.
From various publications:
“Fluorinated C-6 position was shown to contribute to an overall toxicity of the molecule and its CNS activity” (6).
“Fluoroquinolone antibiotics may cause tendon pain and rupture… The non-fluorinated quinolone nalidixic acid had lesser or no effects” (7).
“Although the etiology of fluoroquinolone-associated muscle disorders has yet to be fully elucidated, evidence supports a relationship with both latent myopathic disorders and the fluorine atom in fluoroquinolones… Further support for the hypothesis that fluorine may be the trigger for fluoroquinolone-associated myopathy comes from the fact that no adverse muscular events have been reported with unfluorinated quinolones” (8).
“The potential of this non-fluorinated series became clearer when two independent reports showed that non-fluorinated quinolones were consistently less genotoxic than their 6-fluorinated counterparts” (9).
Argument #3 – The fluorine is toxic, and fluoroquinolone toxicity is fluoride toxicity.
This post would be way too long if I went into detail about this argument, but I will note that the symptoms of fluoride toxicity are similar to the symptoms of fluoroquinolone toxicity. Fluoride toxicity is a multi-symptom, chronic illness that affects all systems in the body….. just like fluoroquinolone toxicity. There are people who have been exposed to other sources of fluoride who have very similar symptoms to those of people who have been “floxed.”
Conflicting Evidence
I suspect that the reason for the conflicting evidence presented above is that long-term studies of fluoroquinolones (and of other sources of fluorine/fluoride) have never been done–or, if they have been done, they have not been responded to appropriately, as there is no movement (that I’m aware of) to stop the fluorination of drugs, and the movements to stop the fluoridation of water constantly run up against obstacles including the accusation of being “conspiracy theorists.” In the short-term, and after limited exposure, many people (and lab rats) are fine. It is only after an accumulation of cellular damage occurs that a threshold is crossed, and multi-symptom, chronic illness results. In the post, The Fluoroquinolone Time Bomb – Answers in the Mitochondria, I go over the delayed reactions and tolerance thresholds that occur with fluoroquinolone adverse reactions. It should be noted that fluoride also accumulates in the body, there is a tolerance threshold for it, and fluorine metabolites damage mitochondria. In order to see the damage that is done by fluoroquinolones (and possibly other sources of fluoride like other fluorinated drugs, PFCs, and even fluoridated water) long-term studies need to be done. Studies that only examine a short exposure to fluoroquinolones, and that don’t look at adverse reactions that occur weeks, months, or even years after exposure to the drug has stopped, are not approaching these drugs appropriately. Short-term studies show that these drugs are less risky than they actually are in the long term, and/or after repeated exposure. Long-term studies are needed to show the real risks of fluoroquinolones.
Anecdotes
I recovered while drinking fluoridated water and using fluoridated toothpaste. I have never noticed any immediate ill effects from fluoride exposure.
However… some people have recovered from fluoroquinolone toxicity primarily through cutting all sources of fluoride from their lives. They have avoided fluorinated water for drinking, cooking/eating, and bathing, and have felt markedly better while avoiding fluoride. They notice that even small exposures to fluoride make them feel worse.
Nonconclusion
I honestly don’t know what to conclude. I think that both the quinolone core and the fluorine atom are dangerous. It’s undeniable that the fluorine makes the quinolone more powerful, and more dangerous. I am also starting to see that fluorine in itself can cause severe cellular damage. Fluorine is an undeniably reactive element that can bind to (and deplete) minerals, disrupt enzymatic reactions, and it may be wreaking havoc on those who exceed their tolerance for it.
BUT… the quinolone core is dangerous too. People can legitimately argue that there are many, many sources of fluorine in the world (20% of all prescription drugs are fluorinated, water and toothpaste are fluoridated, nonstick products like Teflon are fluorinated, air pollution has a lot of fluorine in it, etc.) and people who are exposed to those things don’t get “floxed.”
BUT… maybe we need to look beyond the people who are dealing with fluoroquinolone toxicity, and look at the bigger picture of multi-symptom, chronic, mysterious diseases. I’m honestly not sure if the many diseases of modernity that have increased along with both fluoroquinolone use and the increase in overall exposure to fluoride—like autoimmune diseases, neurodegenerative diseases, mysterious diseases like fibromyalgia and ME/CFS, mitochondrial diseases, autonomic nervous system diseases, autism, etc.–have anything to do with fluorine/fluoride exposure, or not. Studies, especially appropriately long-term studies, that examine the various sources of fluorine/fluoride, and their cumulative effects, haven’t been done. (Most people assume that things like this have been looked at thoroughly. Don’t assume that–they haven’t been.)
Action Plan
Whether we’re dealing with quinolone toxicity or fluorine toxicity, the result is mitochondrial damage and dysfunction, oxidative stress, mineral depletion, a disrupted microbiome, and more. Research on antioxidant supplementation has shown promising results for floxies, and for people dealing with the more recognized diseases of modernity. Mineral replacement is recommended whether cellular minerals are being displaced by the quinolone core or the fluorine. The healing tips noted in the stories on Floxie Hope, and the supplements and other protocols mentioned in The Fluoroquinolone Toxicity Solution, are helpful. Cutting fluoride exposure is also recommended by many “floxies,” and perhaps avoiding all sources of fluoride (fluoridated water, toothpaste, many supplements and pharmaceuticals contain fluorine, and nonstick products like teflon do as well) will be the key for healing for you. I know that avoiding fluoride and fluorine has helped others to heal.
Sources:
- The Canadian Journal of Infectious Diseases, “Safety of fluoroquinolones: An update”
- Dartmouth, “Deconstructing Molecules: Cipro”
- International Journal of Comprehensive Pharmacy, “SYNTHESIS OF NEW LEVOFLOXACIN DERIVATIVES AND THEIR BIOLOGICAL ACTIVITY”
- University of Utah Health Care, “Cinoxacin capsules”
- RxList, “Cinobac Side Effects Center”
- German, NA, Design and synthesis of novel molecules for overcoming bacterial resistance to fluoroquinolones. The University of Iowa 2007, p. 16.
- Rheumatology, “Contrasting effects of fluoroquinolone antibiotics on the expression of the collagenases, matrix metalloproteinases (MMP)-1 and -13, in human tendon-derived cells”
- Physical Medicine and Rehabilitation (PM & R) “Musculoskeletal Complications of Fluoroquinolones: Guidelines and Precautions for Usage in the Athletic Population”
- Current Medicinal Chemistry, “Discovery, Structure-Activity Relationships and Unique Properties of Non- Fluorinated Quinolones (NFQs)”
I can check off all but one in that long list of side effects from quinolones alone, but I would guess that both are responsible, especially knowing now how toxic fluoride is. I wonder if the pill that Stephen Fried’s wife took (“Bitter Pills”) had a fluoride component?
When it comes to looking at the nucleus in order to get a very comprehensive picture i feel strongly that the whole picture, the full history of the FQs far further back than the original Quinolones needs to be researched & included, as our various injuries are found in various patterns in various drugs way back in time, past the original non fluorinated Quinolones right back to synthetic Quinine. in my humble opinion to understand the whole picture is so very important. In my own research I include the quinolines as part of this picture & personally went right back to the source, the chinchona bark, the alkaloids .
For anyone who is unaware, In the drugs in which our various injuries can be found in various patterns, all these drugs have the QuinoLINE ring the nucleus in common . The QuinoLINE ring is the nucleus of Quinine, Mefloquine, the 4-aminoquinolines, the 8-aminoquinolines, It is also the nucleus of the FQs.
For anyone interested in the full history of that QuinoLINE nucleus, this hisory can be found under ‘ links & resources ‘ above, scroll down to ‘ other research ‘ where can be found a dropbox file, this file contains the archives of research from the Fluoroquinolone toxicity research foundation. you can find this information under ‘ ‘ History of the Fluoroquinolones ‘.
I personally feel their are multifactorial issues which are beyond complicated, when we start widening the net to include other toxins environmental issues, drugs etc etc, & how the FQs interact with these & each persons unique variables it is simply mind-blowing, add in the complexity of fluorides, & we then get another how long is a piece of string scenario with so many knots I wonder if it will ever be untangled.
All I know is that thinking about the sheer complexity of it all, just makes what’s left of my floxed brain hurt .
http://fluoridealert.org/researchers/
In respect of fluorides numerous people are hypersensitive, & when it is cut out as much as humanely possible, many people whether they are floxed or not find they do begin feeling better. It is something I feel is so very important to do. I found an interesting study showing the effects of even small amounts on the body / brain.
http://fluoridealert.org/wp-content/uploads/aksyuk-1962.pdf
Thank you, as always, for your thoughtful insight, Debs!
Fortunately, “Studies, especially appropriately long-term studies, that examine the various sources of fluorine/fluoride, and their cumulative effects, haven’t been done.” – this is not really true, LOTS have been done, sure more would be nice, although totally unnecessary, its a PROVEN LETHAL TOXIN on MANY different levels to the Human/Animal bodies, not sure what else really needs to be known, its needs to be avoided, period, as the studies HAVE shown, buried, or not. Dr. Dean who worked 35 years at the Cancer Institute stated that, “In point of fact, Fluoride causes more Human Cancer Death, and causes FASTER than any other chemical”, you don’t really think he went on record with that statement without studies and facts to back it up I hope.
My research, which goes back at least 15 years (on Fluoride), and has compiled a folder of a thousand or more documents/studies etc, would agree with the “study-backed” points above made under #2 , the Quins were less toxic before the Fluorine was added, which only makes sense, since if you take toxic drug “A”, and add a proven lethal toxin to it, the result “B” is of course a much more toxic drug, and really the list for Nalidixic acid (and the others like it, I DID go deep and way back into the history of Quins) and what the studies show for it, while not pleasant (the list for ANY drug never is, hell just look at the side effects for something as simple as Nexium http://www.rxlist.com/nexium-drug/side-effects-interactions.htm), pales in comparison to the full list for both Fluorine/Fluoride toxicity and Fluoroloquinolone Toxicity, which both look near identical
Dear Lisa, Thank you for this post and for, at last, asking this most overlooked question
about Fluorides and putting it out there for all us Floxies to take into account. Thank you Charlett Hobart
This is a good video too. It’s only 13 minutes long, for those who don’t have much time –
https://www.youtube.com/watch?v=QmUPl3vZllg&feature=youtube_gdata&app=desktop
I think I may have forgot to mention another good book on the topic, “The Fluoride Deception”, based on the Authors 10 years of research.
The unfortunate part of Water Fluoridation, is it makes it VERY hard to avoid, and remove from the water as well (almost all filters do NOT remove it), and you end up absorbing it in your bath and shower, and it ends up in the food supply as well, like in almost ALL foods, grown, or manufactured since water is integral to the process, plants must be watered etc
Tiny example of Fluoride PPM in some foods (it IS everywhere, so affecting people whether they realize it, or not, which is why the importance of Iodine and other things is being stressed by many Alternative Health Experts):
Minute Maid orange Juice 1.22ppm
Snapple 29ppm
Dole Pineapple Juice 78ppm
Lucerne 2% milk 72ppm
CocaCola Classic 82ppm
Hansens Soda 45ppm
Capri Sun Juice .37ppm
Gerber Strawberry Juice 1.80ppm
Horizon Milk (organic) .22ppm
Sunny Delight .31ppm
Pepsi .37ppm
Knudson Recharge .37ppm
Gerber White Grape Juice 3.50ppm
Anyway here is a 28 minute video interview with the Author Christopher Bryson of the book, “The Fluoride Deception”: (The book is much more comprehensive of course but this video has some interesting info & tidbits in it too)
https://www.youtube.com/watch?v=Ly_QP4rGczo#t=73
A compilation of many links to more info on their site and external others here
http://www.whale.to/d/fluoride.html
Did a little experiment last night, my teeth have been a little sensitive for a few days so I decided just for fun (I am 95% healed and have been for 6 months) to put some “sensidyne” toothpaste on them, which contains Fluoride, I left it on for one minute only. I have had NO leg twitching at all for at least 3 or 4 weeks so it was a good time to “try” this, I have been sick and not exercising (which is when very minor twitching can come back)
After one hour, very minor twitching started, and it was there in the morning as well right on waking where I am obviously not “thinking about it”. I’ve noted before that the “Placebo” effect really does not work on me, I’ve taken hundreds of supplements with “hope” and got nothing, and there are many other examples.
I did not do this for myself (other than wanting a big of relief on teeth) but to show others what I already know, Fluoride is a BIG problem, whether people actually realize and “notice” or not. We have had people get completely “Re-Floxed” from Dentist treatments where Fluoride was given, from Fluoridated drugs almost every single time, and we have had people have their symptoms “completely disappear” by leaving the Country and going to a non-Fluoridated one (note they did not realize this at the time) only for the symptoms to return with a couple of days of coming back and starting their “Daily Fluoride Shower”.
There is no doubt in my mind all forms of Fluorine and Fluoride are things that can prolong someone’s healing, and even prevent it in some cases. Its possible that some people when Floxed did not cross their “Fluoride threshold” and just suffered some acute damage and symptoms etc so would be “less” sensitive it over a little time then those who have, but I don’t suspect this would be very common, and I believe crossing that threshold is a big reason many people get Floxed (actually notice that is) in the first place.
8 1/2 year floxie here. Fibromyalgia symptoms and tinnitus, with fatigue ect. This has me convinced that I need a whole house system for deflorination of the water. Anyone put in a whole house system that they recommend?
http://articles.mercola.com/sites/articles/archive/2016/05/15/selling-unapproved-fluoride-drugs.aspx
http://articles.mercola.com/sites/articles/archive/2016/05/17/fluoride-in-tap-water.aspx
Effect of tamarind ingestion on fluoride excretion in humans.
http://www.ncbi.nlm.nih.gov/pubmed/11840184
Disgusting http://www.drkaslow.com/html/fluoride.html
Have any of you other floxies out there tried doing an iodine loading type detox? I’ve come across this on the internet and wondering if it helps clear the quiniolone toxicity symptoms? All you need is Lugol’s iodine. I’m new to this recovery process only after finally figuring out the cause this last year. I have severe muscle jerking when trying to go to sleep, so I’ve never been able to recover after dealing with this for over 8 years after a 5 week poisoning back in 2008. It has destroyed my sleep and therefore my regenerating/healing process. All my connective tissue is trashed. I suspect this jerking is due to the flouride toxicity but I’m still not sure if its a magnesium problem. I’m unable to tolerate magnesium due to it causing diarrhea. Even transdermal magnesium gives me the runs sometimes. I’m still working on systemic candida issues after years of supplements, so could this be my problem with magnesium? I read the ebook “The Fluoroquinolone Toxicity Solution”. unfortunately I’ve already tried all the supplements she recommends. Her book doesn’t even address the flouride issue, which in my research is undoubtedly part of the problem. Any help is appreciated. I was floxed at age 26. I’m now 35. my life has been ruined by this and I’m still grasping at straws. My nervous system is badly damaged.
Given that people who take non-fluoridated quinolones can also be floxxed id say its quinolone toxicity. However, fluoride dose enable the quinolone structure to more easily penetrate lipid membranes like the bbb.
I was floxed May 2009 at age of 68, felt like I had a tube in me and someone turned on the helium. Muscle damage in legs (MRI at Mayo, blood in urine, pancreas enzymes elevated, cracking left jaw, tinnitis, MD. I am not experiencing a severe flare up: vasculitis, severe pain left shoulder and both hips, severe muscle ache (difficulty walking.) My doc seems to think it is old age related (now 77) I don’t know whether to call an Orthodedic, a cardiologist, a dermatologist (purpura on legs) I am a caregiver now for husband. We find ourselves in a nighmare.
I need to correct my comment. I said “I am not” I meant to say “I am now” experiencing a severe flare up.