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.

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.

Effect of fluoride is predominantly posteruptive; maintain consistent small amounts of fluoride in saliva and dental plaque. (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. 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. Sources of fluoride exposure other than the primary drinking supply also must be considered.

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

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).

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. In patients at increased risk for dental caries, experts recommend application of topical fluorides by dental personnel at least every 3–6 months.

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). For at-risk children <6 years of age, 2.26% fluoride varnish is recommended.

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. 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.

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. 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.

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.

Fluoridation of the public water supply is the most effective means of providing optimal levels of fluoride to large segments of the population. Good evidence supports fluoridation of public water supply to prevent and control dental caries. 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.

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.

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. However, current recommendations for fluoride supplementation in children continue to be based on the fluoride concentrations in local drinking water.

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.

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.

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. Additional studies needed to determine the optimal means for delivering topical fluorides to orthodontic patients; limited data indicate that fluoride varnish can reduce the risk of decalcified white lesions.

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.

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

Desensitizing Dentin

Used topically to desensitize exposed root surfaces of teeth.

Hypersensitivity may result from dentin exposure and fluid movement through the exposed dentinal tubules, which activates nerve fibers in the pulp. 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).

Fluoride therapy may include use of fluoridated dentifrices and fluoride gels or rinses supplemented as required with professionally applied fluoride varnish, gel, or rinse.

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^†). The quality of the new bone mass is uncertain, and evidence that fluoride reduces fracture risk is conflicting and controversial. Other therapies (e.g., calcium, vitamin D, bone resorption inhibitors, depending on the specific disease) currently are preferred.

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.

Oral Administration

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

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.

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).

Oral Topical Administration

Not for systemic treatment; do not swallow.

Rinsing solution may be swallowed only if directed to do so by a clinician to provide systemic fluoride supplementation.

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. (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.

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. For maximum benefit, do not eat or drink for 30 minutes after administration. Adults, do not rinse mouth for 30 minutes after administration; children, rinse mouth thoroughly.

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. Expectorate. For maximum benefit, do not eat, drink, or rinse for 30 minutes after administration.

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

5% varnish (containing 2.26% fluoride ion): May be applied by dental or medical personnel. Apply thin layer (typically 0.2–0.5 mL) to teeth with applicator brush. Preparation hardens on contact with saliva; coating wears off over a period of hours. 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. Avoid other prescription-strength topical fluoride preparations for 24 hours after application. Suspend use of fluoride dietary supplements for several days after treatment.

Oral Topical Administration (Acidulated Phosphate Fluoride)

Do not place in porcelain or glass containers. (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. Apply a thin ribbon of gel to teeth with toothbrush or mouth trays for ≥1 minute; expectorate. For maximum benefit, do not eat or drink for 30 minutes after administration. Adults, do not rinse mouth for 30 minutes after administration; children, rinse mouth thoroughly.

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

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

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

Oral Topical Administration (Stannous Fluoride)

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

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. Brush teeth thoroughly; allow the gel to remain on the teeth for 1 minute, then expectorate. Use a toothbrush or cotton swab to ensure that all sensitive areas are covered with the gel. Do not eat, drink, or rinse for 30 minutes after administration.

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

Reconstitution

Reconstitute fluoride powders as directed by the manufacturer.

Dilution

Prepare 0.1% rinsing solution from 0.63% concentrate prior to use. 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. Use immediately; solutions may decompose within a few hours to stannous hydroxides, forming a white precipitate.

Dosage

Available as sodium fluoride, acidulated phosphate fluoride, sodium monofluorophosphate, or stannous fluoride; dosage expressed in terms of the fluoride ion.

Dosage of oral fluoride supplements varies according to the age of the child and the concentration of fluoride in the drinking water. 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). Do not exceed recommended dosages. (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.

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.

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

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. 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.

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

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

0.2% rinsing solution (containing 0.09% fluoride ion) in children ≥6 years of age: 10 mL once weekly, preferably at bedtime. 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.

5% varnish^† (containing 2.26% fluoride ion): Apply via applicator in thin layer (typically 0.2–0.5 mL) to teeth. Usual frequency of professional fluoride application is at least every 3–6 months. 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. 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.

2% gel or foam (containing 0.9% fluoride ion): Apply via trays. Usual frequency of professional fluoride application is at least every 3–6 months.

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.

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

Gel containing 1.23% fluoride ion in children ≥6 years of age: Apply via trays. Usual frequency of professional fluoride application is at least every 3–6 months. 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.

Foam containing 1.23% fluoride ion: Apply via trays. Usual frequency of professional fluoride application is at least every 3–6 months.

Stannous Fluoride

Oral Topical

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

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

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.

Stannous Fluoride

Oral Topical

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

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

Adults

Dental Caries Prevention

Adequate Daily Dietary Intake of Fluoride

Oral

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

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. 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.

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

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

0.2% rinsing solution (containing 0.09% fluoride ion): 10 mL once weekly, preferably at bedtime. 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.

5% varnish^† (containing 2.26% fluoride ion): Apply via applicator in thin layer (typically 0.2–0.5 mL) to teeth. Usual frequency of professional fluoride application is at least every 3–6 months. 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.

2% gel or foam (containing 0.9% fluoride ion): Apply via trays. Usual frequency of professional fluoride application is at least every 3–6 months.

Acidulated Phosphate Fluoride

Oral Topical

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

Rinsing solution containing 0.02% fluoride ion: 10 mL once daily, preferably at bedtime.

Gel containing 1.23% fluoride ion: Apply via trays. Usual frequency of professional fluoride application is at least every 3–6 months. 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.

Foam containing 1.23% fluoride ion: Apply via trays. Usual frequency of professional fluoride application is at least every 3–6 months.

Stannous Fluoride

Oral Topical

0.4% gel: Once daily.

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

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.

Stannous Fluoride

Oral Topical

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

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

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.

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.

Adults

Tolerable Daily Upper Intake Level

Oral

Maximum 10 mg daily.

Pregnant women: Maximum 10 mg daily.

Lactating women: Maximum 10 mg daily.

Desensitizing Dentin

Oral Topical

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

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

Special Populations

Hepatic Impairment

No specific dosage recommendations at this time.

Renal Impairment

No specific dosage recommendations at this time; however, see Renal Impairment under Cautions.

Geriatric Patients

Select dosage with caution because of age-related decreases in renal function.

Cautions for Fluorides

Contraindications

• Known hypersensitivity to fluoride or any ingredient in the formulation.

Dietary Supplements (Oral Solution and Chewable Tablets)

• Contraindicated when drinking water fluoride ion concentration ≥0.6 ppm (mg/L).

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

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

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

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

Oral Topical Fluorides

• Some manufacturers state dysphagia is a contraindication to use of topical fluorides (e.g., gels, foams, rinses).

• Varnish: Ulcerative gingivitis or stomatitis; for some preparations, known hypersensitivity to colophony/rosin.

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. Children 15 months to 3 years of age are most vulnerable to fluorosis of permanent teeth.

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.

Follow proper techniques for applying topical preparations to minimize the amount ingested and systemically absorbed.

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

Risk of stained and pitted teeth in moderate-to-severe fluorosis; effect generally has been considered primarily cosmetic. 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.

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. Risk of developing fluorosis directly related to the extent and duration of fluoride exposure; crippling skeletal fluorosis is extremely rare in the US.

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. Good oral hygiene (e.g., adequate brushing) minimizes risk of staining; staining is not harmful or permanent and can be removed by dentist.

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

Sensitivity Reactions

Allergic Reactions

Allergic rash and other idiosyncratic reactions rarely reported.

Urticaria, exfoliative dermatitis, atopic dermatitis, eczema, headache, weakness, gastric distress, stomatitis, and GI and respiratory allergic reactions may occur rarely.

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.

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

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). (See Pediatric Use under Cautions.)

Specific Populations

Pregnancy

Category B.

Fluoride supplements administered orally to pregnant women do not prevent dental caries in their children.

Lactation

Distributed into milk in small amounts. Fluoride supplementation in nursing women not expected to substantially affect infant's fluoride intake. However, use with caution in nursing women.

Pediatric Use

Do not exceed recommended dosages of oral fluoride supplements. (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.

Potential risks to young children from swallowing topical fluoride preparations include nausea and vomiting and, with repeated ingestion, dental fluorosis. 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).

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. 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).

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.

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. 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.

May be difficult to appropriately adjust the amount of fluoride required from fixed-combination multivitamin or multivitamin/iron preparations used as oral fluoride supplements. (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. Substantially eliminated by the kidneys; geriatric patients more likely to have decreased renal function; monitor renal function and adjust dosage accordingly.

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

Renal Impairment

Excreted by the kidney; therefore, risk of toxic reactions may be greater in patients with impaired renal function.

Drug Interactions

Specific Drugs

Fluorides Pharmacokinetics

Absorption

Bioavailability

Sodium fluoride and other soluble fluoride salts: Readily and almost completely absorbed from the GI tract.

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

Distribution

Extent

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

Stored in bones, developing teeth, and skeletal tissue.

Elimination

Elimination Route

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

Special Populations

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

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. May decompose and become alkaline when stored in ordinary pharmaceutical glass.

Tablets, Chewable

Sodium fluoride: 20–25°C.

Topical

Foam

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

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

Gel

Acidulated phosphate fluoride: Tight, plastic containers at room temperature; consult product information for specific recommendations. Do not freeze.

Sodium fluoride 1.1%: 20–25°C.

Sodium fluoride 2%: Room temperature; consult product information for specific recommendations.

Stannous fluoride: Room temperature; consult product information for specific recommendations.

Rinsing Solution

Acidulated phosphate fluoride: 20–25°C.

Sodium fluoride 0.2%: 20–25°C.

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

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

Drug Compatibility

Sodium fluoride is incompatible with calcium and magnesium salts.

Stannous fluoride is incompatible with alkaline substances and oxidizing agents.

Actions

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

• Increases tooth resistance to acid dissolution, promotes remineralization, and inhibits the cariogenic microbial process.

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

• 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.

• 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. Fluid movement through exposed tubules activates nerve fibers in the pulp resulting in pain in response to various stimuli.

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

Advice to Patients

• Instruct patients regarding appropriate procedures for topical fluoride administration.

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

• 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.

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

• 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.

• 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. 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.

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

• 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.

• 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.

• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.

• Importance of informing patients of other important precautionary information. (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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