Topical fluoride

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Topical fluorides are fluoride-containing drugs indicated in prevention and treatment of dental caries, particularly in children's primary dentitions. [1] The dental-protecting property of topical fluoride can be attributed to multiple mechanisms of action, including the promotion of remineralization of decalcified enamel, the inhibition of the cariogenic microbial metabolism in dental plaque and the increase of tooth resistance to acid dissolution. [2] Topical fluoride is available in a variety of dose forms, for example, toothpaste, mouth rinses, varnish and silver diamine solution. [3] These dosage forms possess different absorption mechanisms and consist of different active ingredients. [4] Common active ingredients include sodium fluoride, stannous fluoride, silver diamine fluoride. [4] These ingredients account for different pharmacokinetic profiles, thereby having varied dosing regimes and therapeutic effects. [4] A minority of individuals may experience certain adverse effects, including dermatological irritation, hypersensitivity reactions, neurotoxicity and dental fluorosis. [5] [6] [7] In severe cases, fluoride overdose may lead to acute toxicity. [6] While topical fluoride is effective in preventing dental caries, it should be used with caution in specific situations to avoid undesired side effects. [8]

Contents

Medical uses

Topical fluoride formulations are effective measures for preventing and arresting the progression of dental caries, especially early childhood caries (ECC). [9] Domestic products such as toothpaste and mouthwash can be used on a regular basis at home, while silver diamine solution therapy can be administered by specialists in dental clinics. [9]

Mechanism of action

Topical fluoride serves to prevent early dental caries primarily in three ways: promoting remineralization of decalcified enamel, inhibiting the cariogenic microbial processes in dental plaque and increasing tooth resistance to acid breakdown. [2]

Promotion of remineralization of decalcified enamel

Fluoride has a high tendency to react with the calcium hydroxyapatite Ca10(PO4)6(OH)2 in tooth enamel due to its high affinity to metals. [8] [10] It subsequently replaces the hydroxide group in hydroxyapatite to precipitate calcium fluorapatite Ca5(PO4)3)F. [8] These fluorapatite precipitations scavenge excess phosphate and calcium in the saliva to form a supersaturated solution for remineralization. [10]

Inhibition of the cariogenic microbial processes in dental plaque

Topical fluoride also serves as an antimicrobial agent to reduce demineralization by inhibiting the growth of tooth-erupting microorganisms in dental plaque. [2] Fluoride ions readily combine with hydrogen cations to produce hydrogen fluoride. [2] Hydrogen fluoride subsequently acidifies the bacterial cytoplasm, inactivating the essential enzymes for bacterial metabolism, including enolase and proton releasing adenosine triphosphatase. [2]

As topical fluoride lowers the pH, bacteria have to consume more energy to maintain a neutral environment, leaving less energy for reproduction, and further generation of polysaccharides and acids. [2] These polysaccharides are necessary for adherence to enamel, while these acids are essential for the synthesis of bacterial enzymes, for example, immunoglobulin A protease. [2] These processes contribute to reducing the risk of dental caries by inhibiting microbial metabolism in the tooth plaque. [2]

Increase in tooth resistance to acid dissolution

Topical fluoride can increase the resistance of enamel to acid. [8] Bacteria in enamel, including Streptococcus mutans, generate acids to maintain a low pH environment during fermentation. [8] These acids eventually dissociate the hydroxyapatite in teeth once the acidity falls below the critical pH (pH 5.5). [8] The fluorapatite formed by topical fluorides has lower critical pH (pH 4.5) than normal enamel, it is therefore more acid resistant and not prone to degrade even in an acidic environment. [8] This mechanism helps decelerate the rate of teeth demineralization. [8]

Dosage forms

Toothpaste

Fluoride-containing toothpaste added with abrasives Charcoal Toothpaste.jpg
Fluoride-containing toothpaste added with abrasives

The daily use of fluoride-containing toothpaste is recognized as the key factor contributing to the global reduction in dental caries over recent decades. [11] Fluoride-containing toothpaste can be classified into two types, namely low-fluoride and high-fluoride toothpaste. [12] Low-fluoride toothpaste, depending on brand, generally contains 0.22% to 0.31% fluoride. [12] These fluorides are often manufactured in the form of sodium fluoride, stannous fluoride, or sodium monofluorophosphate (MFP). [4] High-fluoride toothpaste typically contains 1.1% sodium fluoride, namely four times more concentrated than low-fluoride toothpaste. [12] People using high-fluoride toothpaste should avoid eating or rinsing their mouth for at least 30 minutes after treatment for maximal therapeutic effect.[ citation needed ] Some fluoride-containing toothpaste incorporates extra chemical ingredients for additional purposes. [13] For instance, calcium carbonate and magnesium carbonate are added as abrasives to remove dental plaque on teeth, while strontium chloride and potassium nitrate are added as anti-sensitive agents for individuals who have teeth sensitivity. [13] [14]

Mouth rinse

Fluoride mouth rinse is usually used for adjunctive therapy with other topical fluoride products. [15] It is generally prepared in the form of sodium chloride. [12] Sodium chloride is kept in the saliva after spitting out the mouth rinse, thus helping to prevent tooth decay. [12] 0.02% fluoride mouth rinse is commonly administered twice daily, while 0.05% is administered once daily at bedtime after thoroughly brushing teeth. [16] People using high-fluoride toothpaste should avoid eating or rinsing their mouth for at least 30 minutes after administration for maximal therapeutic effect. [12]

Silver diamine solution

Silver diamine fluoride therapy on dental caries Dental Caries Cavity 2.JPG
Silver diamine fluoride therapy on dental caries

Silver diamine fluoride (SDF) is a transparent solution which is prepared by dissolving silver ions and fluoride ions into ammonia water. [9] [1] It is approved by professionals to prevent early childhood caries (ECC) and relieve tooth sensitivity. [9] [17]

SDF has multiple advantages over traditional fluoride varnish therapy:

However, the SDF solution results in permanent black staining on the teeth's decayed proportion. This may be unacceptable by some individuals with aesthetic concerns. [9]

SDF, in addition to performing the functions of conventional topical fluorides, is said to have collagen-conserving properties and an additional antibacterial action owing to the presence of silver. [1] While multiple clinical trials demonstrate that 38% SDF is more effective than 5% sodium fluoride varnish in preventing ECC, it is currently unavailable in many countries due to insufficient research data. [9] [17]

Adverse effects

Increased exposure of fluoride may lead to certain adverse side effects, including dental fluorosis and developmental neurotoxicity. [5] [6] Other rare side effects include skin rash and hypersensitivity reactions. [7] In severe cases, fluoride overdose may lead to acute toxicity. [6] [19]

Dental fluorosis with white marks on teeth Dental fluorosis.jpg
Dental fluorosis with white marks on teeth

Dental fluorosis

Dental fluorosis is a dose-dependent adverse drug effect featured by temporary white marks. [5] It can be induced by increased fluoride exposure, typically from stannous fluoride-containing products or fluoridated water. [5] [20] Excess intake of fluoride leads to overabundance of structurally-weak fluorapatite formed inside the enamel, resulting in increased brittleness of teeth. [21] In severe dental fluorosis, brown or yellow staining may appear on teeth. [8] Children under the age of eight are susceptible to dental fluorosis. [8]

Severe dental fluorosis with brown and yellow staining on teeth Bellingham fluorosis 3.jpg
Severe dental fluorosis with brown and yellow staining on teeth

Developmental neurotoxicity

Overdose of fluoride can potentially cause neurotoxicity during early development. [6] While the exact pathophysiology of fluoride-induced developmental toxicity is not completely understood, most research suggested that excessive fluoride intake may result in formation of aluminium fluoride (AlF3 or AlF4). [8] [6] Aluminium fluoride structurally mimics phosphate, thus is capable of crossing the blood-brain barrier via phosphate transporters. [6] These fluorides in the brain may cause neurodegenerative disorders, including Alzheimer's disease, Parkinson's disease and IQ declination. [8] Nevertheless, topical fluoride was less likely to cause developmental neurotoxicity than fluoridated water. [6]

Acute fluoride toxicity

Fluoride overdose may cause acute toxicity. [6] While the underlying mechanism of fluoride toxicity is unclear, most studies ascribe fluoride toxicity to its capacity to inhibit metalloproteins by imitating metallofluoride substrate. [6] Inhibition of metalloproteins slows down multiple signalling pathways and disrupts cellular organelles, subsequently producing oxidative stress and cell cycle arrest. [6] Fluoride overload is suggested to be linked to pH and electrolyte imbalances, creating an environment unfavourable for cell living. [6] These mechanisms can ultimately result in cellular malfunction and cell death. [6]

Cautions

Toothpaste, cream, mouthrinse and varnish

Ingredients in topical fluoride that cause severe adversede effects
IngredientsSevere adverse effects
Benzyl alcohol derivative
  • Gasping syndrome: symptoms include convulsion, respiratory distress, gasping respiration, cardiovascular collapse and hypotension.
Polysorbate 80
Propylene glycol

Silver diamine fluoride

Related Research Articles

<span class="mw-page-title-main">Toothpaste</span> Substance to clean and maintain teeth

Toothpaste is a paste or gel dentifrice used with a toothbrush to clean and maintain the aesthetics and health of teeth. Toothpaste is used to promote oral hygiene: it is an abrasive that aids in removing dental plaque and food from the teeth, assists in suppressing halitosis, and delivers active ingredients to help prevent tooth decay and gum disease (gingivitis). Owing to differences in composition and fluoride content, not all toothpastes are equally effective in maintaining oral health. The decline of tooth decay during the 20th century has been attributed to the introduction and regular use of fluoride-containing toothpastes worldwide. Large amounts of swallowed toothpaste can be poisonous. Common colors for toothpaste include white and blue.

<span class="mw-page-title-main">Tooth enamel</span> Major tissue that makes up part of the tooth in humans and many animals

Tooth enamel is one of the four major tissues that make up the tooth in humans and many animals, including some species of fish. It makes up the normally visible part of the tooth, covering the crown. The other major tissues are dentin, cementum, and dental pulp. It is a very hard, white to off-white, highly mineralised substance that acts as a barrier to protect the tooth but can become susceptible to degradation, especially by acids from food and drink. In rare circumstances enamel fails to form, leaving the underlying dentin exposed on the surface.

<span class="mw-page-title-main">Tooth decay</span> Deformation of teeth due to acids produced by bacteria

Tooth decay, also known as cavities or caries, is the breakdown of teeth due to acids produced by bacteria. The cavities may be a number of different colors, from yellow to black. Symptoms may include pain and difficulty eating. Complications may include inflammation of the tissue around the tooth, tooth loss and infection or abscess formation. Tooth regeneration is an ongoing stem cell–based field of study that aims to find methods to reverse the effects of decay; current methods are based on easing symptoms.

<span class="mw-page-title-main">Water fluoridation</span> Addition of fluoride to a water supply to reduce tooth decay

Water fluoridation is the addition of fluoride to a public water supply to reduce tooth decay. Fluoridated water contains fluoride at a level that is effective for preventing cavities; this can occur naturally or by adding fluoride. Fluoridated water operates on tooth surfaces: in the mouth, it creates low levels of fluoride in saliva, which reduces the rate at which tooth enamel demineralizes and increases the rate at which it remineralizes in the early stages of cavities. Typically a fluoridated compound is added to drinking water, a process that in the U.S. costs an average of about $1.32 per person-year. Defluoridation is needed when the naturally occurring fluoride level exceeds recommended limits. In 2011, the World Health Organization suggested a level of fluoride from 0.5 to 1.5 mg/L, depending on climate, local environment, and other sources of fluoride. In 2024, the Department of Health and Human Services' National Toxicology Program found that water fluoridation levels above 1.5 mg/L are associated with lower IQ in children. In 2024, U.S. court rulings have raised concerns about the potential health risks of water fluoridation, including findings by the EPA and new risk assessments that suggest the benefits may be waning. Bottled water typically has unknown fluoride levels.

Tooth whitening or tooth bleaching is the process of lightening the color of human teeth. Whitening is often desirable when teeth become yellowed over time for a number of reasons, and can be achieved by changing the intrinsic or extrinsic color of the tooth enamel. The chemical degradation of the chromogens within or on the tooth is termed as bleaching.

<span class="mw-page-title-main">Sodium fluoride</span> Ionic compound (NaF)

Sodium fluoride (NaF) is an inorganic compound with the formula NaF. It is a colorless or white solid that is readily soluble in water. It is used in trace amounts in the fluoridation of drinking water to prevent tooth decay, and in toothpastes and topical pharmaceuticals for the same purpose. In 2021, it was the 291st most commonly prescribed medication in the United States, with more than 600,000 prescriptions. It is also used in metallurgy and in medical imaging.

<span class="mw-page-title-main">Dental abrasion</span> Medical condition

Abrasion is the non-carious, mechanical wear of tooth from interaction with objects other than tooth-tooth contact. It most commonly affects the premolars and canines, usually along the cervical margins. Based on clinical surveys, studies have shown that abrasion is the most common but not the sole aetiological factor for development of non-carious cervical lesions (NCCL) and is most frequently caused by incorrect toothbrushing technique.

<span class="mw-page-title-main">Hydroxyapatite</span> Naturally occurring mineral form of calcium apatite

Hydroxyapatite is a naturally occurring mineral form of calcium apatite with the formula Ca5(PO4)3(OH), often written Ca10(PO4)6(OH)2 to denote that the crystal unit cell comprises two entities. It is the hydroxyl endmember of the complex apatite group. The OH ion can be replaced by fluoride or chloride, producing fluorapatite or chlorapatite. It crystallizes in the hexagonal crystal system. Pure hydroxyapatite powder is white. Naturally occurring apatites can, however, also have brown, yellow, or green colorations, comparable to the discolorations of dental fluorosis.

<span class="mw-page-title-main">Fluoride therapy</span> Medical use of fluoride

Fluoride therapy is the use of fluoride for medical purposes. Fluoride supplements are recommended to prevent tooth decay in children older than six months in areas where the drinking water is low in fluoride. It is typically used as a liquid, pill, or paste by mouth. Fluoride has also been used to treat a number of bone diseases.

<span class="mw-page-title-main">Dental fluorosis</span> Tooth enamel discoloration due to excessive fluoride ingestion

Dental fluorosis is a common disorder, characterized by hypomineralization of tooth enamel caused by ingestion of excessive fluoride during enamel formation.

<span class="mw-page-title-main">Sodium monofluorophosphate</span> Chemical compound

Sodium monofluorophosphate, commonly abbreviated SMFP, is an inorganic compound with the chemical formula Na2PO3F. Typical for a salt, SMFP is odourless, colourless, and water-soluble. This salt is an ingredient in some toothpastes.

<span class="mw-page-title-main">Early childhood caries</span> Dental disease of young children

Early childhood caries (ECC), formerly known as nursing bottle caries, baby bottle tooth decay, night bottle mouth and night bottle caries, is a disease that affects teeth in children aged between birth and 71 months. ECC is characterized by the presence of 1 or more decayed, missing, or filled tooth surfaces in any primary tooth. ECC has been shown to be a very common, transmissible bacterial infection, usually passed from the primary caregiver to the child. The main bacteria responsible for dental cavities are Streptococcus mutans (S.mutans) and Lactobacillus. There is also evidence that supports that those who are in lower socioeconomic populations are at greater risk of developing ECC.

<span class="mw-page-title-main">Tin(II) fluoride</span> Chemical compound

Tin(II) fluoride, commonly referred to commercially as stannous fluoride (from Latin stannum, 'tin'), is a chemical compound with the formula SnF2. It is a colourless solid used as an ingredient in toothpastes.

<span class="mw-page-title-main">Fluorapatite</span> Phosphate mineral

Fluorapatite, often with the alternate spelling of fluoroapatite, is a phosphate mineral with the formula Ca5(PO4)3F (calcium fluorophosphate). Fluorapatite is a hard crystalline solid. Although samples can have various color (green, brown, blue, yellow, violet, or colorless), the pure mineral is colorless, as expected for a material lacking transition metals. Along with hydroxylapatite, it can be a component of tooth enamel, especially in individuals who use fluoridated toothpaste, but for industrial use both minerals are mined in the form of phosphate rock, whose usual mineral composition is primarily fluorapatite but often with significant amounts of the other.

Olaflur is a fluoride-containing substance that is an ingredient of toothpastes and solutions for the prevention of dental caries. It has been in use since 1966. Especially in combination with dectaflur, it is also used in the form of gels for the treatment of early stages of caries, sensitive teeth, and by dentists for the refluoridation of damaged tooth enamel.

<span class="mw-page-title-main">Fluoride varnish</span> Highly concentrated form of fluoride

Fluoride varnish is a highly concentrated form of fluoride that is applied to the tooth's surface by a dentist, dental hygienist or other dental professional, as a type of topical fluoride therapy. It is not a permanent varnish but due to its adherent nature it is able to stay in contact with the tooth surface for several hours. It may be applied to the enamel, dentine or cementum of the tooth and can be used to help prevent decay, remineralise the tooth surface and to treat dentine hypersensitivity. There are more than 30 fluoride-containing varnish products on the market today, and they have varying compositions and delivery systems. These compositional differences lead to widely variable pharmacokinetics, the effects of which remain largely untested clinically.

<span class="mw-page-title-main">Remineralisation of teeth</span>

Tooth remineralization is the natural repair process for non-cavitated tooth lesions, in which calcium, phosphate and sometimes fluoride ions are deposited into crystal voids in demineralised enamel. Remineralization can contribute towards restoring strength and function within tooth structure.

<span class="mw-page-title-main">Enamel hypoplasia</span> Lack of tooth enamel

Enamel hypoplasia is a defect of the teeth in which the enamel is deficient in quantity, caused by defective enamel matrix formation during enamel development, as a result of inherited and acquired systemic condition(s). It can be identified as missing tooth structure and may manifest as pits or grooves in the crown of the affected teeth, and in extreme cases, some portions of the crown of the tooth may have no enamel, exposing the dentin. It may be generalized across the dentition or localized to a few teeth. Defects are categorized by shape or location. Common categories are pit-form, plane-form, linear-form, and localised enamel hypoplasia. Hypoplastic lesions are found in areas of the teeth where the enamel was being actively formed during a systemic or local disturbance. Since the formation of enamel extends over a long period of time, defects may be confined to one well-defined area of the affected teeth. Knowledge of chronological development of deciduous and permanent teeth makes it possible to determine the approximate time at which the developmental disturbance occurred. Enamel hypoplasia varies substantially among populations and can be used to infer health and behavioural impacts from the past. Defects have also been found in a variety of non-human animals.

<span class="mw-page-title-main">Amine fluoride</span>

Amine fluorides are dental drugs.

Silver diammine fluoride (SDF), also known as silver diamine fluoride in most of the dental literature, is a topical medication used to treat and prevent dental caries and relieve dentinal hypersensitivity. It is a colorless or blue-tinted, odourless liquid composed of silver, ammonium and fluoride ions at a pH of 10.4 or 13. Ammonia compounds reduce the oxidative potential of SDF, increase its stability and helps to maintain a constant concentration over a period of time, rendering it safe for use in the mouth. Silver and fluoride ions possess antimicrobial properties and are used in the remineralization of enamel and dentin on teeth for preventing and arresting dental caries.

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