"How Antifluoridationists Have Weakened Their Case"

Dr. Joel Kaufman, PhD Chemistry
kauffman@hslc.org

Groups such as Parents for Fluoride Poisoned Children (PFPC), based in British Columbia, Canada, (http://www.bruha.com/pfpc/ Accessed 24 Sep 04) and the National Pure Water Association Ltd. in the UK (http://www.npwa.freeserve.co.uk/teflon.html Accessed 24 Sep 04) justifiably attempt to prevent fluoridation of water. Unfortunately, they suffer from chemophobia, which is not only an emotional fear of all  “chemicals”, but a fear of consulting with chemists. As a result, they list any material that contains fluorine in any form as a danger by claiming that it contains “fluoride”. This includes Teflon and Tefal non-stick pan coatings, fluorocarbon propellants, and many drugs, including:

fluoxetine (Prozac)
ciprofloxacin (Cipro)
flunitrazepam (Rohypnol)
fluconazole (Diflucon)
fluticasone (Flixonase or Flixotide)
trifluoperazine (Stelazine)
flucoxacillin (Floxapen)
cerivastatin (Baycol)
cisapride (Propulsid)
astemizole (Hismanal)
fenfluramine (Pondimin)

Even more unfortunate, book authors Barry Groves and Christopher Bryson repeated this in their books (Groves, 2001, pp 298-299; Bryson, 2004, pp 355-356). In fact, none of these materials has any fluoride ion in it. None is metabolized to any significant amount of fluoride ion. All contain the very stable carbon-fluorine bond in the form of trifluoromethyl (CF3-), difluoromethylene (-CF2-), fluoroalkane (=CF-), or fluorophenyl  (F-C6H4-) groups. The fluoro groups are chosen for the drugs to retard metabolism. Gerard F. Judd, being a chemist, did not make this mistake in his book.

For Teflon the maximum continuous service temperature is listed as 260°C or 500°F in the Chemical Rubber Co. Handbook of 1976-7. Overheating may produce an irritant, but it is unlikely to be fluoride ion. Asked for evidence on the toxicity of Teflon, Andreas Schuld, the scientific advosor to PFPC, e-mailed citations to 4 papers on the decomposition of Teflon by ionizing radiation. Clearly this is irrelevant to ordinary use in cooking.

Fluorocarbon refrigerants and propellants such as R12 are metabolized very slowly or not at all, which is also the case with general anesthetics such as Halothane and Methoxyflurane. However, some of the fluorine in the general anesthetics Enflurane, Desflurane and Isoflurane is metabolized to fluoride ion (Williams, 1995, pp 110-111).

Asked for evidence on the toxicity of fluorinated drugs, Andreas Schuld e-mailed citations to 13 papers. Ten of the 13 were published in or before 1952.

Citations from the 1930s showed the toxicity of sodium fluoride from its interference with thyroid hormone biosynthesis (Kraft, 1937a), and a comparison of analytical methods for fluorine in fluoro compounds (Kraft, 1937b). Another from 1949 showed that that 3-fluoro-5-bromo(or iodo)tyrosine were not very toxic in mice, and 5 other fluorophenyl compounds even less so (Euler et al., 1949). Papers by Georg Litzka confirmed the toxicity of 3-fluorotyrosine and 3,5-difluorotyrosine, including in humans, but this is a special case where these amino acid derivatives interefere with thryroid hormone biosynthesis (Litzka, 1936; 1937a; 1937b).

One of the papers cited reported that 3-fluorotyrosine was more toxic to rats than inorganic fluoride (Euler, 1942). One paper described syntheses of tyrosine analogs that were thyroid hormone antagonists in mice without evidence that fluoride ion was formed in vivo (Kraft, 1951). Another paper had other syntheses, including that of the relatively non-toxic (to mice) 5-fluorosalicylic acid, an aspirin analog (Kraft, 1952). Another described the toxicity of sodium fluoride and phenylmethanesulfonyl fluoride and its analogs (Bollen, 1988). The toxicity of the former is well-known, and it is clear to a chemist that the S-F bond in the latter will yield fluoride ion on hydrolysis, so nothing new is found here.

Ciprofloxacin is fairly toxic, to be sure. Andreas Schuld e-mailed a citation to a report that serum and urine levels of fluoride in children were elevated after adminstration of this drug (Pradhan, 1995). The actual elevation of fluoride in serum was from 0.08 to 0.21 ppm in 12 hours, and could not account for more than a fraction of the fluorine (23 mg) in 400 mg doses of ciprofloxacin. The elevation of fluoride in urine from 0.97 to 1.12 ppm after a week was not significant. The authors did not try to measure fluorinated metabolites or unchanged drug, and after MRI and about 2 years of follow-up, they pronounced short courses of cipro safe in children. While it is true that cipro liberates fluoride under UVB illumination in vitro,  according to both Prof. Charles J. Kelley, Mass. Col. Phcy. & Allied Health Sciences and a 1998 NIH publication by C. F. Chignell whose citation was sent by Andreas Schuld. Cipro is metabolized in vivo mostly by hydroxylation and N-sulfation, not by loss of fluoride ion (Williams, 1995, p138).

The toxicity of cerivastatin (Baycol), which contains a 4-fluorophenyl group, caused at least 31 deaths in a 3-year period (Wolfe, 2003). Its toxicity is not markedly different from that of unfluorinated lovastatin (Mevacor), which increased the death rate in placebo-controlled trials (Ravnskov, 2000, p 200-201) or of unfluorinated simvastatin (Zocor), which caused 416 reported deaths in the USA during a 6.5-year period (Scherer, 2004). Mevacor and Zocor do not contain any fluorine at all.

Thus the scientific evidence presented by PFPC, when examined closely, does not support their assertion that all fluorinated organic compounds are toxic because they lead to fluoride ion. Antifluoridationists would serve their cause more effectively by sticking to fluoride ion and its precursors in drinking water as their sole target.


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