Fluorides (Monograph)

Brand names: Acclean, ACT, DentiCare, Fluoridex, Gelato, ... show all 24 brands Gel-Kam, Iris, Just for Kids, Kolorz, Minute-Foam, NeutraCare, NeutraMaxx, Nupro, OMNI, PCxx, PerioMed, Phos-Flur, PreviDent, 60 Second Taste, SF, Stance, Topex, Zap, Zooby
Drug class: Cariostatic Agents
- Cariostatic Agents
ATC class: A12CD
VA class: TN470
Molecular formula: NaFNa₃FPO₄SnF₂
CAS number: 7681-49-4

Introduction

Cariostatic agent; ionic form of fluorine.^{107 109 110 a}

Uses for Fluorides

Dental Caries Prevention

Used orally or topically to prevent or reduce incidence of dental caries and slow or reverse progression of existing dental lesions.^{107 109}

Effect of fluoride is predominantly posteruptive; maintain consistent small amounts of fluoride in saliva and dental plaque.^{109 113} (See Actions.)

Used as a dietary supplement for prevention of dental caries in children in areas where the concentration of fluoride ion in drinking water is less than optimal.^{109 131 134 135 138} While the American Dental Association (ADA), American Academy of Pediatric Dentistry (AAPD), and CDC recommend consideration of fluoride dietary supplements only for children in those areas who are at high risk for dental caries, AAP states that use in lower-risk children also may be considered.^{109 131 134 135 138} Sources of fluoride exposure other than the primary drinking supply also must be considered.^{109 110 131 134 135}

CDC recommends that adults and children at low risk for dental caries drink adequately fluoridated water and use fluoridated dentifrice twice daily.¹⁰⁹ Individuals at higher risk for dental caries may require additional exposure to fluorides (e.g., mouth rinses, dietary supplements, preparations applied by dental personnel).¹⁰⁹

For additional anticaries benefits in adults and pediatric patients ≥6 years of age, fluoride treatment gels or rinsing solutions may be used: sodium fluoride 1.1% gel (containing 0.5% fluoride ion); sodium fluoride 0.02, 0.05, or 0.2% rinsing solutions (containing 0.009, 0.02, or 0.09% fluoride ion, respectively); acidulated phosphate fluoride gel or oral rinse (containing 0.5 or 0.02% fluoride ion, respectively); and stannous fluoride 0.4% gel or 0.63% rinsing solution (diluted and used as 0.1% solution).^{103 114 115 116 117 119 158 169 171 181}

Professionally applied sodium fluoride 2% gel, foam, or oral rinsing solution (containing 0.9% fluoride ion); sodium fluoride 5% varnish^{† [off-label]} (containing 2.26% fluoride ion); or acidulated phosphate fluoride gel or foam (containing 1.23% fluoride ion) also are used for additional anticaries benefits.^{120 136 160 162 172 173} In patients at increased risk for dental caries, experts recommend application of topical fluorides by dental personnel at least every 3–6 months.^{109 134 136}

For adults, adolescents, and children ≥6 years of age at increased risk for dental caries, ADA recommends the following prescription-strength or professionally applied topical fluorides: professional application of varnish containing 2.26% fluoride ion or acidulated phosphate fluoride gel containing 1.23% fluoride ion at least every 3–6 months or in-home use of prescription-strength gel or paste containing 0.5% fluoride ion twice daily or rinsing solution containing 0.09% fluoride ion at least weekly (or daily for prevention of root caries in adults).¹³⁶ For at-risk children <6 years of age, 2.26% fluoride varnish is recommended.^{134 136}

AAP and US Preventive Services Task Force (USPSTF) recommend fluoride varnish in the primary care setting for all infants and young children beginning at tooth eruption and continuing until dental care is established.^{131 137} Although dental experts recommend limiting use of fluoride varnish to children at increased risk for dental caries, USPSTF states that tools for assessing caries risk have not been validated in the primary care setting and it is unknown whether use of these tools by primary care clinicians will accurately and consistently identify children who will develop dental caries.¹³⁷

For children at low risk for dental caries, AAP recommends use of fluoridated dentifrice and fluoride varnish (applied professionally every 3–6 months) beginning at tooth eruption; if the water supply is not fluoridated, assess all potential fluoride sources and consider dietary fluoride supplements accordingly.¹³¹ For children at high risk for dental caries, AAP recommends use of nonprescription fluoride-containing mouth rinse starting at 6 years of age (if the child can reliably swish and expectorate the rinse) in conjunction with the recommendations made for low-risk children.¹³¹

Risk factors for dental caries include low socioeconomic status or low levels of parental education, lack of regular dental care, lack of dental insurance or access to dental services, high incidence of dental caries in older siblings or caregivers, root surfaces exposed by gingival recession, high levels of infection with cariogenic bacteria, impaired ability to maintain oral hygiene, malformed enamel or dentin, reduced salivary flow (from medications, radiation, or disease), low salivary buffering capacity, and wearing of space maintainers, orthodontic appliances, or dental prostheses, especially when combined with frequent consumption of refined carbohydrates.¹⁰⁹

Fluoridation of the public water supply is the most effective means of providing optimal levels of fluoride to large segments of the population.^a Good evidence supports fluoridation of public water supply to prevent and control dental caries.^{109 130 131 132 133} US Public Health Service (PHS) recommends an optimal fluoride concentration of 0.7 ppm (mg/L) in public water supply to provide protection from dental caries while limiting risk of dental fluorosis.¹³⁰

In communities where the concentration of fluoride in the water supply is >2 ppm, use an alternative source of drinking water for children ≤8 years of age.^{109 131 135}

Because consumption of commercially available beverages (including bottled water) in the US and Canada is displacing the consumption of tap or well water, the relative importance of fluoridation of local community water on fluoride intake may be affected.¹⁰⁷ However, current recommendations for fluoride supplementation in children continue to be based on the fluoride concentrations in local drinking water.^{107 131 134 135}

ADA, AAPD, and AAP recommend that in areas where oral fluoride supplements are necessary, children 6 months to 16 years of age receive daily fluoride supplements to provide maximum benefit to both deciduous and permanent teeth.^a

Efficacy of topically applied fluoride varies according to the concentration of fluoride ion in the preparation, method and frequency of application, and the duration of use.^a

Topical fluorides (e.g., gels, mouth rinses, varnish) used to prevent early stages of dental caries (i.e., decalcified white lesions) around fixed orthodontic appliances; fluoridated dentifrice alone is insufficient in many orthodontic patients.^{131 178 179} Additional studies needed to determine the optimal means for delivering topical fluorides to orthodontic patients;¹⁷⁹ limited data indicate that fluoride varnish can reduce the risk of decalcified white lesions.¹⁷⁹

Acidulated phosphate fluoride gels (alone or in combination with a saliva substitute) have been used to control dental decay after xerostomia-producing radiation therapy of tumors of the head and neck.^a

Stannous fluoride gels have been used to protect against postirradiation caries.^a

Desensitizing Dentin

Used topically to desensitize exposed root surfaces of teeth.^{156 169 177 a}

Hypersensitivity may result from dentin exposure and fluid movement through the exposed dentinal tubules, which activates nerve fibers in the pulp.^{148 175} Treatment may consist of therapies that contribute to occlusion of the open tubules (e.g., fluorides, oxalates, sealants or bonding agents, laser therapy) and/or inhibit neural transmission (e.g., potassium nitrate).^{148 175 176}

Fluoride therapy may include use of fluoridated dentifrices and fluoride gels or rinses supplemented as required with professionally applied fluoride varnish, gel, or rinse.^{124 148 156 166 168 169 175 177}

Bone Diseases

Sodium fluoride has been used orally to increase bone density and relieve bone pain in the treatment of various metabolic^{† [off-label]} (osteoporosis^{† [off-label]}, corticosteroid-induced osteoporosis^{† [off-label]}) and neoplastic bone diseases^{† [off-label]} (bone lesions in multiple myeloma^†, bone pain associated with metastatic prostatic carcinoma^†).^a The quality of the new bone mass is uncertain, and evidence that fluoride reduces fracture risk is conflicting and controversial.^{150 184} Other therapies (e.g., calcium, vitamin D, bone resorption inhibitors, depending on the specific disease) currently are preferred.^{108 149 150 151 152 153}

Fluorides Dosage and Administration

Administration

Administer orally as solution or chewable tablet or topically to teeth as a dentifrice, foam, gel, rinsing solution, or varnish.^{114 116 119 120 121 124 125 154 155 166 169 171 172 a}

Oral Administration

Administer sodium fluoride orally as a chewable tablet or as a solution undiluted or mixed with water or other nondairy liquids.^{131 155} Dissolve chewable tablets in the mouth or chew before swallowing, preferably at bedtime after brushing the teeth.^{155 a}

Avoid mixing fluoride solution with milk or formula or ingesting dairy products within 1 hour of oral administration of fluoride supplements since fluoride absorption may be impaired.^{131 155}

Administer oral fluoride supplements only when community fluoridation programs are not available or feasible and when the fluoride ion concentration in drinking water is ≤0.6 ppm (mg/L).^a

Oral Topical Administration

Not for systemic treatment; do not swallow.^{115 119 120 121 124 169 171 172 a}

Rinsing solution may be swallowed only if directed to do so by a clinician to provide systemic fluoride supplementation.^{103 170}

To minimize the amount of fluoride swallowed and absorbed systemically and the risk of fluorosis, instruct and/or supervise children <12 years of age regarding proper techniques for use of topical preparations.^{103 131 139} (See Dental Fluorosis under Cautions.)

AAP states young children should not rinse with water after brushing teeth with fluoridated dentifrice because their instinct is to swallow; expectorating without rinsing reduces the amount of fluoride swallowed and leaves some fluoride in saliva for uptake into plaque.¹³¹

Oral Topical Administration (Sodium Fluoride)

1.1% gel (containing 0.5% fluoride ion): After brushing and flossing teeth, apply a thin ribbon of gel to teeth with toothbrush or mouth tray for ≥1 minute; expectorate.^{119 164} For maximum benefit, do not eat or drink for 30 minutes after administration.^{119 164} Adults, do not rinse mouth for 30 minutes after administration; children, rinse mouth thoroughly.^{119 164}

0.02, 0.05, and 0.2% rinsing solutions (containing 0.009, 0.02, or 0.09% fluoride ion, respectively): After thoroughly brushing teeth, rinse solution vigorously around and between teeth for 1 minute.^{115 116 158 a} Expectorate.^{115 116 158 a} For maximum benefit, do not eat, drink, or rinse for 30 minutes after administration.^{115 116 158 a}

2% foam or gel (containing 0.9% fluoride ion): May be applied by dental personnel.^{120 160 161} Fill tray(s) with gel (one-third full) or with foam and then insert tray(s) into patient's mouth.^{120 160 161} For maximum benefit, have patient bite down lightly on mouth tray(s) for 4 minutes.^{120 134 160 161 182} Remove tray(s) and have patient expectorate excess.^{120 160 161} Patient should not eat, drink, or rinse for ≥30 minutes after application.^{120 160 161}

5% varnish (containing 2.26% fluoride ion): May be applied by dental or medical personnel.^{131 134 135 136 137 159 166} Apply thin layer (typically 0.2–0.5 mL) to teeth with applicator brush.^{135 159 166} Preparation hardens on contact with saliva; coating wears off over a period of hours.^{135 159 166} Patients should eat only soft foods and avoid hot drinks for several hours after application; also should refrain from flossing or brushing the teeth for ≥4 hours and preferably for 24 hours.^{159 167} Avoid other prescription-strength topical fluoride preparations for 24 hours after application.¹⁶⁶ Suspend use of fluoride dietary supplements for several days after treatment.^{159 166}

Oral Topical Administration (Acidulated Phosphate Fluoride)

Do not place in porcelain or glass containers.¹⁷¹ (See Teeth Surface and Restoration Staining under Cautions and also see Storage under Stability.)

1.1% gel (containing 0.5% fluoride ion): After brushing teeth normally, rinse thoroughly.¹⁷¹ Apply a thin ribbon of gel to teeth with toothbrush or mouth trays for ≥1 minute; expectorate.¹⁷¹ For maximum benefit, do not eat or drink for 30 minutes after administration.¹⁷¹ Adults, do not rinse mouth for 30 minutes after administration; children, rinse mouth thoroughly.¹⁷¹

Rinsing solution containing 0.02% fluoride ion: Use after thoroughly brushing teeth.^{114 a} Rinse solution around and between the teeth for 1 minute, then expectorate.^{114 a} Do not eat or drink for 30 minutes after administration.¹¹⁴

Foam or gel containing 1.23% fluoride ion: May be applied by dental personnel.^{172 173 174 a} Fill tray(s) with gel (one-third full) or with foam and then insert tray(s) into patient's mouth.^{172 173 174} For maximum benefit, have patient bite down lightly on mouth tray(s) for 4 minutes.^{134 136 172 174} Remove tray(s) and have patient expectorate excess.^{172 173 174} Patient should not eat, drink, or rinse for ≥30 minutes after application.^{172 173 174}

For desensitizing exposed root surfaces, use gel after brushing and flossing at bedtime.^a

Oral Topical Administration (Stannous Fluoride)

0.4% gel for dental caries prevention: After brushing teeth normally, apply to teeth with toothbrush.¹⁸¹ Brush teeth thoroughly; allow the gel to remain on the teeth for 1 minute, then expectorate.¹⁸¹ Do not eat or drink for 30 minutes after administration.¹⁸¹

0.4% gel for sensitivity relief: After brushing and flossing teeth normally, shake toothbrush to remove excess water; apply the gel to cover the bristles.¹²⁴ Brush teeth thoroughly; allow the gel to remain on the teeth for 1 minute, then expectorate.¹²⁴ Use a toothbrush or cotton swab to ensure that all sensitive areas are covered with the gel.¹²⁴ Do not eat, drink, or rinse for 30 minutes after administration.¹²⁴

0.1% rinsing solution: Dilute 0.63% concentrate to prepare 0.1% solution before use.^{103 117 169} Use after regular brushing.^{117 169} Swish vigorously around and between teeth for 1 minute; expectorate.¹¹⁷ Repeat.¹¹⁷ Do not eat or drink for 30 minutes after administration.^{117 169}

Reconstitution

Reconstitute fluoride powders as directed by the manufacturer.¹⁰³

Dilution

Prepare 0.1% rinsing solution from 0.63% concentrate prior to use.^{103 117 169} Add 3.75 mL concentrated rinse to the mixing vial (or fill to 1/8 oz mark); add 26.25 mL water (or fill to 1 oz mark) and mix to provide a 0.1% rinsing solution.^{103 117 169} Use immediately;^{103 117 169} solutions may decompose within a few hours to stannous hydroxides, forming a white precipitate.^a

Dosage

Available as sodium fluoride, acidulated phosphate fluoride, sodium monofluorophosphate, or stannous fluoride; dosage expressed in terms of the fluoride ion.^{119 124 154 155 172 a}

Dosage of oral fluoride supplements varies according to the age of the child and the concentration of fluoride in the drinking water.^{109 110 131 134 135} Adjust dosage in proportion to the amount of fluoride provided from all possible sources (e.g., childcare settings, school, bottled water, beverages, infant formula, prepared foods, dentifrice, multivitamins, mouth rinse).^{109 110 131 134 135 a} Do not exceed recommended dosages.^a (See Dental Fluorosis and also see Pediatric Use under Cautions.)

Prescription or nonprescription dentifrices generally contain 0.5 or 0.1–0.15% fluoride ion, respectively.^{135 165}

Pediatric Patients

Dental Caries Prevention

Fluoride-containing Dentifrices

Oral Topical

Infants and young children (from eruption of first tooth up to 3 years of age): Apply only a smear (approximately 0.1 g; about the size of a grain of rice) to the toothbrush twice daily.^{131 139}

Children 3–6 years of age: Apply only a pea-sized amount (approximately 0.25 g) to the toothbrush twice daily.^{131 139}

Adequate Dietary Intake

Oral

For tolerable upper intake levels, see Prescribing Limits under Dosage and Administration.

Fluoride Supplementation in Areas with Insufficient Fluoride in Drinking Water

Oral

Sodium Fluoride

Oral Topical

1.1% gel (containing 0.5% fluoride ion) in children ≥6 years of age: Manufacturers recommend use once daily, preferably at bedtime, unless otherwise instructed by clinician.^{119 164} When used twice daily, one of several prescription-strength or professionally applied topical fluoride treatments recommended by ADA for children ≥6 years of age at increased risk for dental caries.¹³⁶

0.02% rinsing solution (containing 0.009% fluoride ion) in children ≥6 years of age: 10 mL twice daily.¹⁵⁸

0.05% rinsing solution (containing 0.02% fluoride ion) in children ≥6 years of age: 10 mL once daily.¹¹⁶

0.2% rinsing solution (containing 0.09% fluoride ion) in children ≥6 years of age: 10 mL once weekly, preferably at bedtime.¹¹⁵ When used at least once weekly, one of several prescription-strength or professionally applied topical fluoride treatments recommended by ADA for children ≥6 years of age at increased risk for dental caries.¹³⁶

5% varnish^† (containing 2.26% fluoride ion): Apply via applicator in thin layer (typically 0.2–0.5 mL) to teeth.^{135 159 166} Usual frequency of professional fluoride application is at least every 3–6 months.^{109 134 136} When used at this frequency, one of several professionally applied or prescription-strength topical fluoride treatments recommended by ADA for children ≥6 years of age at increased risk for dental caries.¹³⁶ The only professionally applied or prescription-strength topical fluoride treatment recommended by experts for infants (beginning at tooth eruption) and children <6 years of age.^{131 134 136 137}

2% gel or foam (containing 0.9% fluoride ion): Apply via trays.^{120 160 161} Usual frequency of professional fluoride application is at least every 3–6 months.^{109 134 136}

Acidulated Phosphate Fluoride

Oral Topical

1.1% gel (containing 0.5% fluoride ion) in children ≥6 years of age: Once daily, preferably at bedtime, unless otherwise instructed by clinician.¹⁷¹

Rinsing solution containing 0.02% fluoride ion in children ≥6 years of age: 10 mL once daily, preferably at bedtime.^{114 a}

Gel containing 1.23% fluoride ion in children ≥6 years of age: Apply via trays.^{123 174 a} Usual frequency of professional fluoride application is at least every 3–6 months.^{109 134 136} When used at this frequency, one of several professionally applied or prescription-strength topical fluoride treatments recommended by ADA for children ≥6 years of age at increased risk for dental caries.¹³⁶

Foam containing 1.23% fluoride ion: Apply via trays.^{172 a} Usual frequency of professional fluoride application is at least every 3–6 months.^{109 134 136}

Stannous Fluoride

Oral Topical

0.4% gel in children ≥6 years of age: Once daily.¹⁸¹

0.1% rinsing solution in children ≥6 years of age: Dilute 0.63% concentrate before use to a 0.1% solution.^{103 117 169} (See Dilution under Dosage and Administration.) Use once daily or as directed by clinician.^{117 183} Use 15 mL, then repeat with an additional 15 mL.^{117 183}

Desensitizing Dentin

Sodium Fluoride

Oral Topical

5% varnish (containing 2.26% fluoride ion): Apply via applicator in thin layer to teeth every 6 months; if needed, may be used safely 4 times yearly in patients ≥6 years of age.^{159 166}

Stannous Fluoride

Oral Topical

0.4% gel in children ≥12 years of age: Twice daily (morning and evening) or as directed by clinician.¹²⁴

0.1% rinsing solution in children ≥6 years of age: Dilute 0.63% concentrate before use to a 0.1% solution.^{103 169} (See Dilution under Dosage and Administration.) Use once daily or as directed by clinician.¹⁸³ Use 15 mL, then repeat with an additional 15 mL.¹⁸³

Adults

Dental Caries Prevention

Adequate Daily Dietary Intake of Fluoride

Oral

Adults ≥19 years of age: 3.1–3.8 mg daily.^a

Sodium Fluoride

Oral Topical

1.1% gel (containing 0.5% fluoride ion): Manufacturers recommend use once daily, preferably at bedtime, unless otherwise instructed by clinician.^{119 164} When used twice daily, one of several prescription-strength or professionally applied topical fluoride treatments recommended by ADA for adults at increased risk for dental caries.¹³⁶

0.02% rinsing solution (containing 0.009% fluoride ion): 10 mL twice daily.¹⁵⁸

0.05% rinsing solution (containing 0.02% fluoride ion): 10 mL once daily.¹¹⁶

0.2% rinsing solution (containing 0.09% fluoride ion): 10 mL once weekly, preferably at bedtime.¹¹⁵ When used at least once weekly (or daily for root caries prevention), one of several prescription-strength or professionally applied topical fluoride treatments recommended by ADA for adults at increased risk for dental caries.¹³⁶

5% varnish^† (containing 2.26% fluoride ion): Apply via applicator in thin layer (typically 0.2–0.5 mL) to teeth.^{135 159 166} Usual frequency of professional fluoride application is at least every 3–6 months.^{109 134 136} When used at this frequency, one of several professionally applied or prescription-strength topical fluoride treatments recommended by ADA for adults at increased risk for dental caries.¹³⁶

2% gel or foam (containing 0.9% fluoride ion): Apply via trays.^{120 160 161} Usual frequency of professional fluoride application is at least every 3–6 months.^{109 134 136}

Acidulated Phosphate Fluoride

Oral Topical

1.1% gel (containing 0.5% fluoride ion): Once daily, preferably at bedtime, unless otherwise instructed by clinician.¹⁷¹

Rinsing solution containing 0.02% fluoride ion: 10 mL once daily, preferably at bedtime.^{114 a}

Gel containing 1.23% fluoride ion: Apply via trays.^{123 174 a} Usual frequency of professional fluoride application is at least every 3–6 months.^{109 134 136} When used at this frequency, one of several professionally applied or prescription-strength topical fluoride treatments recommended by ADA for adults at increased risk for dental caries.¹³⁶

Foam containing 1.23% fluoride ion: Apply via trays.^{172 a} Usual frequency of professional fluoride application is at least every 3–6 months.^{109 134 136}

Stannous Fluoride

Oral Topical

0.4% gel: Once daily.¹⁸¹

0.1% rinsing solution: Dilute 0.63% concentrate before use to a 0.1% solution.^{103 117 169} (See Dilution under Dosage and Administration.) Use once daily or as directed by clinician.^{117 183} Use 15 mL, then repeat with an additional 15 mL.^{117 183}

Desensitizing Dentin

Sodium Fluoride

Oral Topical

5% varnish (containing 2.26% fluoride ion): Apply via applicator in thin layer to teeth every 6 months; if needed, may apply 4 times yearly.^{159 166}

Stannous Fluoride

Oral Topical

0.4% gel: Use twice daily (morning and evening) or as directed by clinician.¹²⁴

0.1% rinsing solution: Dilute 0.63% concentrate before use to a 0.1% solution.^{103 169} (See Dilution under Dosage and Administration.) Use once daily or as directed by clinician.¹⁸³ Use 15 mL, then repeat with an additional 15 mL.¹⁸³

Prescribing Limits

Pediatric Patients

Fluoride Tolerable Daily Upper Intake Levels in Infants and Children107

Desensitizing Dentin

Oral Topical

Stannous fluoride 0.4% gel (self-care) in children ≥12 years of age: Maximum twice daily for 4 weeks for sensitive teeth.¹²⁴

Stannous fluoride 0.1% rinsing solution (prepared from 0.63% concentrate) in children ≥6 years of age (self-care): Maximum once daily for 4 weeks for sensitive teeth.¹⁶⁹

Adults

Tolerable Daily Upper Intake Level

Oral

Maximum 10 mg daily.¹⁰⁷

Pregnant women: Maximum 10 mg daily.¹⁰⁷

Lactating women: Maximum 10 mg daily.¹⁰⁷

Desensitizing Dentin

Oral Topical

Stannous fluoride 0.4% gel (self-care): Maximum twice daily for 4 weeks for sensitive teeth.¹²⁴

Stannous fluoride 0.1% rinsing solution (prepared from 0.63% concentrate) (self-care): Maximum once daily for 4 weeks for sensitive teeth.¹⁶⁹

Special Populations

Hepatic Impairment

No specific dosage recommendations at this time.^a

Renal Impairment

No specific dosage recommendations at this time; however, see Renal Impairment under Cautions.^{115 119 120 171 172}

Geriatric Patients

Select dosage with caution because of age-related decreases in renal function.^{115 119 120 171 172}

Cautions for Fluorides

Contraindications

• Known hypersensitivity to fluoride or any ingredient in the formulation.^{120 164 172 a}

Dietary Supplements (Oral Solution and Chewable Tablets)

• Contraindicated when drinking water fluoride ion concentration ≥0.6 ppm (mg/L).^{154 180 a}

• Sodium fluoride oral solution: Infants <6 months of age.¹⁵⁴

• Sodium fluoride tablets containing 0.25 mg of fluoride ion: Children <3 years of age.¹⁸⁰

• Sodium fluoride tablets containing 0.5 mg of fluoride ion: Children <3 years of age.¹⁸⁰ Children <6 years of age when drinking water fluoride ion concentration ≥0.3 ppm (mg/L).¹⁸⁰

• Sodium fluoride tablets containing 1 mg of fluoride ion: Children <6 years of age.¹⁸⁰ Drinking water fluoride ion concentration >0.3 ppm (mg/L).^{180 a}

Oral Topical Fluorides

• Some manufacturers state dysphagia is a contraindication to use of topical fluorides (e.g., gels, foams, rinses).^{115 120 164 172}

• Varnish: Ulcerative gingivitis or stomatitis;^{159 166} for some preparations, known hypersensitivity to colophony/rosin.¹⁶⁶

Warnings/Precautions

Dental Fluorosis

Excessive amounts may produce dose-related dental fluorosis (hypocalcification and hypoplasia) and osseous changes in children <8 years of age, especially where fluoride ion concentration in drinking water is >0.6 ppm.^{107 a} Children 15 months to 3 years of age are most vulnerable to fluorosis of permanent teeth.^{131 135 a}

Vast majority of cases in US are very mild or mild; however, prevalence increased from the 1980s to early 2000s, possibly because of greater fluoride exposure.^{130 131 138}

Follow proper techniques for applying topical preparations to minimize the amount ingested and systemically absorbed.^{100 101 103}

Mild fluorosis has no effect on tooth function; may render the enamel more resistant to caries.^{107 138} May cause white opaque patches on the incisal edges of anterior teeth or cusp tips of posterior teeth (“snow capping”).¹⁰⁷

Risk of stained and pitted teeth in moderate-to-severe fluorosis; effect generally has been considered primarily cosmetic.¹⁰⁷ Some experts now question whether pitting associated with severe fluorosis, which constitutes enamel loss, is only cosmetic since tooth enamel protects dentin and pulp from decay and infection.¹⁸⁴

Skeletal Fluorosis

Prolonged intake of high fluoride ion concentrations (i.e., 4–8 ppm [mg/L]) in drinking water may result in an increase in bone mineral density and apparent fluoride osteosclerosis.¹⁰⁷ Risk of developing fluorosis directly related to the extent and duration of fluoride exposure; crippling skeletal fluorosis is extremely rare in the US.¹⁰⁷

Teeth Surface and Restoration Staining

Staining or pigmentation (e.g., yellow, brown, brown-black) of the teeth may result from topical application of concentrated solutions or gels of stannous fluoride, particularly in patients with poor oral hygiene.^{124 169 a} Good oral hygiene (e.g., adequate brushing) minimizes risk of staining; staining is not harmful or permanent and can be removed by dentist.^{103 124 169}

Acidulated phosphate fluoride preparations may cause dulling of porcelain and ceramic restorations unless protected from contact.^{171 172 a} Neutral sodium fluoride preparations may be recommended for patients with these restorations.^a

Sensitivity Reactions

Allergic Reactions

Allergic rash and other idiosyncratic reactions rarely reported.^{116 119 154 155 171 a}

Urticaria, exfoliative dermatitis, atopic dermatitis, eczema, headache, weakness, gastric distress, stomatitis, and GI and respiratory allergic reactions may occur rarely.^{120 164 172 a}

Patients with mucositis or with abraded or sensitive gingival tissue may be hypersensitive to alcohol or other ingredients contained in some oral or topical fluoride preparations.^{115 120 164 171 a}

Dyspnea has occurred rarely in asthmatic children receiving fluoride varnish.¹⁵⁹ Edematous swelling reported rarely after application, particularly when applied to extensive surfaces.¹⁵⁹ If intolerance occurs, remove coating by brushing and rinsing.¹⁵⁹

Use of Fixed Combinations

When fluoride is used in fixed combination with other preparations, consider the cautions, precautions, and contraindications associated with the concomitant agent(s).^a (See Pediatric Use under Cautions.)

Specific Populations

Pregnancy

Category B.^{115 119 120 155 171 172}

Fluoride supplements administered orally to pregnant women do not prevent dental caries in their children.^{109 143}

Lactation

Distributed into milk in small amounts.^{120 164 172 a} Fluoride supplementation in nursing women not expected to substantially affect infant's fluoride intake.^{120 164 172} However, use with caution in nursing women.^{120 155 164 172}

Pediatric Use

Do not exceed recommended dosages of oral fluoride supplements.^a (See Contraindications and also Dental Fluorosis under Cautions, and see Dosage under Dosage and Administration.) Oral fluoride supplements not recommended in infants <6 months of age.^{107 109 131 134 135}

Potential risks to young children from swallowing topical fluoride preparations include nausea and vomiting and, with repeated ingestion, dental fluorosis.¹³⁶ Young children usually cannot perform the rinse process necessary with oral rinsing solutions, and they are more likely to swallow topical fluoridated dental preparations (e.g., toothpastes).^{107 131}

Carefully instruct and/or supervise children <6 years of age regarding proper use of fluoridated dentifrices to ensure the correct amount is used (see Dosage under Dosage and Administration) and to minimize swallowing of the dentifrice.^{103 131 139} Also instruct and supervise those 6–12 years of age as necessary regarding proper techniques for use of topical fluoride preparations (e.g., rinsing solutions, gels, dentifrices).¹⁰³

Sodium fluoride varnish containing 2.26% fluoride ion is the only professionally applied topical fluoride preparation recommended by ADA or AAPD for use in children <6 years of age for dental caries prevention^†; systemic fluoride exposure is thought to be lower with the varnish than with other professionally applied preparations.^{134 136 137}

Avoid use of fluoride treatment gels and rinsing solutions for dental caries prevention in children <6 years of age unless otherwise instructed by a dentist or medical professional.^{114 116 119 131 135 136 158 169 171 181} In-home use of prescription-strength topical fluoride preparations (e.g., gels, pastes, rinsing solutions) not recommended by ADA or AAPD for use in children <6 years of age.^{134 136}

May be difficult to appropriately adjust the amount of fluoride required from fixed-combination multivitamin or multivitamin/iron preparations used as oral fluoride supplements.^a (See Dosage under Dosage and Administration.)

Geriatric Use

No overall differences in safety and efficacy of oral topical fluorides relative to younger adults, but increased sensitivity cannot be ruled out.^{115 119 120 171 172} Substantially eliminated by the kidneys; geriatric patients more likely to have decreased renal function; monitor renal function and adjust dosage accordingly.^{115 119 120 171 172}

Oral chewable tablets not indicated in adults, including geriatric adults.¹⁸⁰

Renal Impairment

Excreted by the kidney; therefore, risk of toxic reactions may be greater in patients with impaired renal function.^{115 119 120 171 172}

Drug Interactions

Specific Drugs

Fluorides Pharmacokinetics

Absorption

Bioavailability

Sodium fluoride and other soluble fluoride salts: Readily and almost completely absorbed from the GI tract.^{107 a}

≥80% of soluble fluoride probably absorbed from the GI tract in the absence of high dietary concentrations of calcium or certain other cations.¹⁰⁷ (See Interactions.)

Food

Milk, infant formula, or certain foods (e.g., with high concentrations of calcium or certain other divalent or trivalent cations that form insoluble fluoride salts) may decrease absorption of fluoride by 10–25%.¹⁰⁷

Distribution

Extent

Crosses the placenta and is distributed in small amounts into milk, sweat, tears, and hair.^a

Stored in bones, developing teeth, and skeletal tissue.^a

Elimination

Elimination Route

Rapidly excreted principally in urine, and in small amounts in feces, sweat, and saliva.^a

Special Populations

Hemodialysis may remove fluoride in patients with severe intoxication or with impaired renal function.^a

Stability

Storage

Oral

Solution

Sodium fluoride: Tight, plastic containers at <40°C (maintain between 15–30°C), especially if the pH of the solution is <7.5.^a May decompose and become alkaline when stored in ordinary pharmaceutical glass.^a

Tablets, Chewable

Sodium fluoride: 20–25°C.¹⁵⁵

Topical

Foam

Acidulated phosphate fluoride 1.23%: Room temperature; consult product information for specific recommendations.^{163 172} Do not freeze.¹⁶³ Do not puncture or incinerate.^{163 172}

Sodium fluoride 2%: Avoid excessive heat; consult product information for specific recommendations.¹²⁰ Do not freeze.¹²⁰ Do not puncture or incinerate.¹²⁰

Gel

Acidulated phosphate fluoride: Tight, plastic containers^a at room temperature; consult product information for specific recommendations.^{123 171 174} Do not freeze.^{123 174}

Sodium fluoride 1.1%: 20–25°C.¹¹⁹

Sodium fluoride 2%: Room temperature; consult product information for specific recommendations.^{160 161}

Stannous fluoride: Room temperature; consult product information for specific recommendations.^{124 181}

Rinsing Solution

Acidulated phosphate fluoride: 20–25°C.¹¹⁴

Sodium fluoride 0.2%: 20–25°C.¹¹⁵

Sodium fluoride 2%: Room temperature; do not expose to excessive heat (>40°C).¹⁶²

Stannous fluoride: 15–30°C.¹¹⁷ Decomposes to stannous hydroxides within a few hours, forming a white precipitate; prepare just prior to use.^a

Drug Compatibility

Sodium fluoride is incompatible with calcium and magnesium salts.^a

Stannous fluoride is incompatible with alkaline substances and oxidizing agents.^a

Actions

• Mechanism of action in reducing tooth decay not fully understood;^a however, research now indicates predominant effect is posteruptive, not preeruptive as previously hypothesized.^{109 113}

• Increases tooth resistance to acid dissolution, promotes remineralization, and inhibits the cariogenic microbial process.^{109 115 154 155 164 a}

• Prior to tooth eruption, fluoride is incorporated into tooth enamel during formation.^a

• Cariostatic effects on teeth after eruption result from combined effects of bacterial metabolism in plaque and on the dynamics of enamel demineralization and remineralization during an acidogenic challenge.¹⁰⁷

• Mechanism of action in reducing sensitivity of exposed dentin thought to be related to formation of calcium-phosphorus precipitates, calcium fluoride, and fluorapatite, which may occlude exposed dentinal tubules and thereby reduce fluid movement through the tubules.¹⁷⁵ Fluid movement through exposed tubules activates nerve fibers in the pulp resulting in pain in response to various stimuli.^{148 175}

• Increases skeletal density and bone mass; however, large doses can cause skeletal fluorosis and osteomalacia.^a

Advice to Patients

• Instruct patients regarding appropriate procedures for topical fluoride administration.^{114 115 119 124 169 171}

• Advise patients receiving fluoride powders or concentrated rinsing solutions that the preparation must be reconstituted and/or diluted as directed prior to use.^{103 169}

• Advise patients receiving fluoride treatment gels or rinsing solutions for self-administration that these preparations are to be used as directed and not as dentifrices or mouthwashes or gargles, respectively.^{103 124}

• Advise individuals receiving stannous fluoride-containing preparations of the importance of good oral hygiene (e.g., adequate brushing) to minimize the risk of staining.^{103 124 169} Inform patients that such staining is not harmful or permanent and can be removed by a dentist or dental hygienist.^{103 124 169}

• Inform individuals with children that ingestion of higher than recommended amounts of fluoride by children has been associated with an increase in mild dental fluorosis in developing, unerupted teeth.¹³⁵

• Advise parents or caregivers to carefully instruct and/or supervise children <6 years of age regarding proper use of fluoridated dentifrices to ensure the correct amount is used and to minimize swallowing of the dentifrice.^{103 131 139} Also advise parents or caregivers to instruct and supervise children 6–12 years of age as necessary regarding proper techniques for use of fluoridated dentifrices, gels, and rinsing solutions.¹⁰³

• Importance of long-term compliance on a daily basis in patients who require oral fluoride supplements.¹³⁵

• Advise patients receiving fluoride varnish to eat only soft foods and avoid hot drinks for several hours after application and to refrain from flossing or brushing the teeth for ≥4 hours and preferably for 24 hours.^{159 167}

• Advise patients to contact a poison control center or other qualified clinician immediately if they swallow more fluoride than the amount used for brushing or rinsing.^{116 124}

• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.^{115 120 155 164 172}

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.^{115 120 164 171 172}

• Importance of informing patients of other important precautionary information.^{115 120 154 155 164 171 172} (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

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