The Fluorine Group Of Organophosphates And

Their Anticholinesterase Effects On The

Central Nervous System
By Brocke Lever

FLUORINE

It has been estimated that fluorine is ranked nineteenth in the list of elements arranged in
order of relative abundance.

Whatever it's true distribution may be, it is clear that fluorine is not a scarce element.
Although fluorine is widely distributed and is quite abundant, sources suitable for industrial
exploitation are relatively restricted, and only three of these fluorine containing minerals are
of any commercial importance. A They are listed below with their theoretical (estimated)
fluorine content.

1. Cryolite - Na3 [AlF6] - 54.5% fluorine

The colourless material seemingly disappears in water due to the proximity of their
refractive indices.
It was historically used as an ore of aluminium and later in the electrolytic processing
of the aluminium-rich oxide ore bauxite (itself a combination of aluminium oxide
minerals such as gibbsite, boehmite and diaspore).

The difficulty of separating aluminium from oxygen in the oxide ores was overcome
by the use of cryolite as a flux to dissolve the oxide mineral(s). Pure cryolite itself
melts at 1012 °C (1285 K), and it can dissolve the aluminium oxides sufficiently well
to allow easy extraction of the aluminium by electrolysis.

Considerable energy is still required for both heating the materials and the
electrolysis, but it is much more energy-efficient than melting the oxides themselves.
Now, as natural cryolite is too rare to be used for this purpose, synthetic sodium
aluminium fluoride is produced from the common mineral fluorite.

2. Fluorite/Fluorspar - 48.5% fluorine

Fluorite (also called fluorspar) is a halide mineral composed of calcium fluoride,
CaF2. It is an isometric mineral with a cubic habit, though octahedral and more
complex isometric forms are not uncommon. Crystal twinning is common and adds
complexity to the observed crystal habits.

The word fluorite is derived from the Latin root fluo, meaning "to flow" because the
mineral is used as a flux in iron smelting to decrease the viscosity of slags at a given
temperature. This increase in fluidity is the result of the ionic nature of the mineral.
The melting point of pure calcium fluoride is 1676 K.
 In 1852 fluorite gave its name to the phenomenon of fluorescence, which is
prominent in fluorites from certain locations, due to certain impurities in the crystal.
Fluorite also gave the name to its constitutive element fluorine.

Fluorspar is used directly or indirectly to manufacture products such as aluminium,

gasoline, insulating foams, refrigerants, steel, and uranium fuel. All domestic sources
of fluorspar are derived from sales of material from the National Defence Stockpile
and from a small amount of synthetic fluorspar produced from industrial waste
streams. By-product fluorosilicic acid production from some phosphoric acid
producers supplements fluorspar as a domestic source of fluorine, but is not
included in fluorspar production or consumption calculations.

3. Fluorapatite - Ca5(PO4)3F - 3.8% fluorine

Industrially, the mineral is an important source of both phosphoric and hydrofluoric
acids. Fluorapatite as a mineral is the most common phosphate mineral. It occurs
widely as an accessory mineral in igneous rocks and in calcium rich metamorphic
rocks. It commonly occurs as a detrital or diagenic mineral in sedimentary rocks and
is an essential component of phosphorite ore deposits. It occurs as a residual mineral
in lateritic soils.

Fluorapatite as a naturally occurring impurity in apatite generates hydrogen fluoride

as a by-product during the production of phosphoric acid, as apatite is digested by
sulfuric acid. The hydrogen fluoride by-product is now one of the industrial sources
of hydrofluoric acid, which in turn is used as a starting reagent for synthesis of a
range of important industrial and pharmaceutical fluorine compounds.

The element Fluorine is more abundant than chlorine.

Fluorine was first isolated in 1886 by French chemist Henri Moissan.

However, in 1813 Sir Humphry Davy had recognized the presence of a new element in crude
preparations of hydrofluoric acid which had been available since 1771.

Fluorine is the most chemically reactive of all the elements and combines directly at ordinary
or elevated temperatures with all elements other than oxygen, helium, neon and krypton,
often with extreme vigour. It also attacks many other compounds, breaking them down to
fluorides.

FLUORSPAR
Fluorspar is by far the most important industrial source of fluorine.
Workable deposits are found all over the world. In Australia, China, Korea, the Former Soviet
Union, South Africa, Tunisia, Morocco, Spain, Italy, France, Germany, The United Kingdom,
Argentina, Canada and The United states.
INORGANIC COMPOUNDS OF FLUORINE
All inorganic fluorine compounds which have an appreciable solubility in water and are toxic
when ingested in quite squall quantities. Thus, such substances as sodium fluoride and sodium
silicofluoride are very poisonous, less than 1.0 gram of the former constitutes a fatal dose in
adults.

Fluoride used to be added to public water supplies at a dosage of 1ppm. Presently it has been
raised to 2ppm.

2 ppm = 1.996 milligrams per litre

500 litres of fluoridated tap water theoretically contain the diluted equivalent of a fatal 1.0 gram
dose of fluoride.

Figure 1 - One gram of sugar compared to a 25 cent piece

FLUORINE USES

All Inorganic compounds of fluorine have been / or are used extensively in industry for:

• Metal fluxes
• Wood preservatives
• Frosting glass
• Lead and tin plating
• Aluminum production
• Ceramics production
• Water Fluoridation
• Non-stick cooking surfaces (Teflon)
• Aerosol propellants
• Isolating uranium isotopes, Nuclear reprocessing (separating the components of spent
nuclear fuel)
• An oxidizing agent in rocket fuel
• Chemical warfare agents
• Insecticides
• Toothpaste additives
• General anaesthetics
• Anxiolytic, hypnotic and narcoleptic sedatives

Of all its possible uses fluorine has the most fascinating and possibly the most complicated use
in anaesthetics and tranquilizers.
A BRIEF BACKGROUND ON THE NEUROTRANSMITTERS ACETYLCHOLINE AND
ACETYLCHOLINESTERASE

ACETYLCHOLINE
Acetylcholine is one of the fifteen major neurotransmitters and was one of the first
neurotransmitters to be identified by science and was discovered back in 1914.

It is the chemical transmitter of nerve impulses at:

The synapses in all autonomic ganglia, both sympathetic and parasympathetic and the endings
of the preganglionic sympathetic fibres in the adrenal medulla,

All postganglionic parasylnpathetic nerve endings',

Postganglionic sympathetic nerve endings in the uterus and sweat glands',

The end-plates of the motor nerves to the striated muscled. Put simply it chemically transmits
nerve impulses in the brain and throughout the body.

ACETYLCHOLINESTERASE
Once acetylcholine has done its job transporting the nerve impulse that impulse must be
deactivated or 'switched off'. This job is done acetylcholinesterase which hydrolyses or "breaks
down" acetylcholine to choline and acetate. The choline can then be taken back up into the
presynaptic neurone, and there it is used to synthesize new acetylcholine.

ANTICHOLINESTERASES
Drugs which either reversibly or irreversibly inhibit the enzyme acetylcholinesterase, and thus
delay the destruction of released acetylcholine, are called anticholinesterases.

Anticholinesterases will inhibit acetylcholinesterase at any site to which they can gain access,
and they will potentiate the effects of acetylcholine at all parasympathetically innervated
structures, and at nicotinic receptors in autonomic ganglia and skeletal muscle. Actions on the
central nervous systems are a mixture of stimulant and depressant actions.

Put simply, anticholincsterases short circuit the central nervous system.

Organophosphate anticholinesterases constitute or class of long-lasting (irreversible)

anticholinesterase compounds. These compounds have been mainly used for insecticides,
potential agents of warfare (chemical weapons i.e. nerve gas), anaesthetics, tranquillizers and
the fluoridation of public water supplies.

Fluoride (sodium fluoride, sodium silicofluoride and hydrofluoric acid) and a large number of
other inorganic fluorine compounds are classed as organophosphate anticholinesterases.

ANXIOLYTIC SEDATIVES, HYPNOTICS AND NEUROLEPTICS

An anxiolytic (also anti-panic or anti-anxiety agent) is a drug used for the treatment of anxiety
and its related psychological and physical symptoms. Anxiolytics have been shown to be useful
in the treatment of anxiety disorders. Beta-receptor blockers such as propranolol and
oxprenolol, although not anxiolytics, can be used to combat the somatic symptoms of anxiety.
Anxiolytics are also known as minor tranquilizers. The term is less common in modern texts, and
was originally derived from a dichotomy with major tranquilizers, also known as neuroleptics or
anti-psychotics.

A Hypnotic (also called soporific) drugs are a class of psychoactives whose primary function is to
induce sleep and to be used in the treatment of insomnia, and in surgical anesthesia. When used
in anesthesia to produce and maintain unconsciousness, "sleep" is metaphorical as there are no
regular sleep stages or cyclical natural states; patients rarely recover from anesthesia feeling
refreshed and with renewed energy. Because drugs in this class generally produce dose-
dependent effects, ranging from anxiolysis to production of unconsciousness, they are often
referred to collectively as sedative-hypnotic drugs. Hypnotic drugs are regularly prescribed for
insomnia and other sleep disorders, with over 95% of insomnia patients being prescribed
hypnotics in some countries. Many hypnotic drugs are habit-forming and, due to a large number
of factors known to disturb the human sleep pattern, a physician may instead recommend
alternative sleeping patterns, sleep hygiene, and exercise, before prescribing medication for
sleep. Hypnotic medication when prescribed should be used for the shortest period of time
possible.

An antipsychotic (or neuroleptic) is a psychiatric medication primarily used to manage psychosis

(including delusions or hallucinations, as well as disordered thought), particularly in
schizophrenia and bipolar disorder, and is increasingly being used in the management of non-
psychotic disorders (ATC code N05A). A first generation of antipsychotics, known as typical
antipsychotics, was discovered in the 1950s. Most of the drugs in the second generation, known
as atypical antipsychotics, have been developed more recently, although the first atypical
antipsychotic, clozapine, was discovered in the 1950s and introduced clinically in the 1970s.
Both generations of medication tend to block receptors in the brain's dopamine pathways, but
antipsychotic drugs encompass a wide range of receptor targets.

A number of harmful and undesired (adverse) effects have been observed, including lowered life
expectancy, extrapyramidal effects on motor control – including akathisia (an inability to sit
still), trembling, and muscle weakness, weight gain, decrease in brain volume, enlarged breasts
(gynecomastia) in men and milk discharge in men and women (galactorrhea due to
hyperprolactinaemia), lowered white blood cell count (agranulocytosis), involuntary repetitive
body movements (tardive dyskinesia), diabetes, and sexual dysfunction.

A return of psychosis can occur, requiring increasing the dosage, due to cells producing more
neurochemicals to compensate for the drugs (tardive psychosis), and there is a potential for
permanent chemical dependence leading to psychosis worse than before treatment began, if
the drug dosage is ever lowered or stopped (tardive dysphrenia).[1] Most side-effects disappear
rapidly once the medication is discontinued or reduced, but others, particularly tardive
dyskinesia, may be irreversible.

Temporary withdrawal symptoms including insomnia, agitation, psychosis, and motor disorders
may occur during dosage reduction of antipsychotics, and can be mistaken for a return of the
underlying condition.
FLUORINE AS A DRUG
Due to its anticholinesterase properties fluorine is part of many sedative agents used in the
management of anxiety and neurosis (anxiolytic sedatives or minor tranquillizers), as well as
those used to produce sleep (hypnotics), and agents used in the treatment of psychoses
(antipsychotic agents). The term narcoleptic agent is sometimes used to describe those
antipsychotic agents that have effects on the extrapyramidal systems.

Antipsychotic agents are sometimes described as major tranquillizers.

SUMMERY
The fluoride in your water is a "major tranquilizer". You are being tranquilized. Slowly but surely
you are being tranquilized.
REFERENCES

https://en.wikipedia.org/wiki/Fluorine

Fluoxetine hydrochloride (trade names Prozac, Fontex, Ladose, Sarafem) is an antidepressant of

the selective serotonin reuptake inhibitor (SSRI) class. Fluoxetine is approved for the treatment
of major depression (including paediatric depression), obsessive-compulsive disorder (in both
adult and paediatric populations), bulimia nervosa, anorexia nervosa, panic disorder and
premenstrual dysphoric disorder.[1] Despite the availability of newer agents, it remains
extremely popular. Over 22.2 million prescriptions for generic formulations of fluoxetine were
filled in the United States in 2007, making it the third most prescribed antidepressant. [2]
Fluoxetine was developed by Eli Lilly and Company, by scientists Klaus Schmiegel and Bryan
Molloy. Lilly also markets the drug for use with pets under the Reconcile brand name.

FLUORINATED PHARMACEUTICALS

Prozac (fluoxetine)
Rohypnol (flunitrazepam)
Diflucan (fluconazole, Flixonase or Flixotide (fluticasone)
Stelazine (trifluoperazine, Fluanxol or Depixol (flupenthixol) or Floxapen (flucloxacillin)

and asthma drugs that use propellants containing fluoride: Ventolin and Becotide.
INDEX OF FLUORINATED PHARMACEUTICALS

https://slweb.org/ftrcfluorinatedpharm.html

This listing represents the beginning of an ongoing project, which aims to provide detailed
information on fluorinated pharmaceuticals, listing them by category and providing both
pharmacological (generic) name and commercial name.

When in its final form, this listing will be user-friendly for people seeking basic information
about the prescription drugs they are taking, or for researchers who seek a more detailed
summary of the relevant pharmacological data of each drug, including each drug’s metabolic
fate (F ion release) as it impacts the drug’s overall toxicity.

At the present time, we are posting just the basic listing of drugs by their category, and generic
and common names. This listing is a work in progress, but we are starting with enough of the
most popular drugs that this list can be useful even in its present form.