Florhex
Florhex Uses, Dosage, Side Effects, Food Interaction and all others data.
Sodium fluoride is a cariostatic agent that is used to prevent dental caries. It can also be used as a source of fluoride in total parenteral nutrition.
Sodium fluoride protects the teeth from acid demineralization while preventing tooth decay by bacteria while strengthening tooth enamel. It is important to note that excess fluoride exposure during tooth mineralization, especially in children 1-3 years old, may cause fluorosis. It is a condition manifested by white lines, pitting, or discoloration of teeth resulting from changes in tooth enamel. The risk of fluorosis can be decreased by the use of a rice-size amount of fluoridated toothpaste in children younger than 3 years old. It is recommended that no more than a pea-sized quantity of fluoridated toothpaste should be used for children from 3 to 6 years old. The American Dentistry Association (ADA) recommends that children should be closely supervised during toothpaste use to prevent excess fluoride ingestion.
An aromatic ether that is phenol which is substituted at C-5 by a chloro group and at C-2 by a 2,4-dichlorophenoxy group. It is widely used as a preservative and antimicrobial agent in personal care products such as soaps, skin creams, toothpaste and deodorants as well as in household items such as plastic chopping boards, sports equipment and shoes.
Xylitol is a naturally occurring five-carbon sugar alcohol found in most plant material, including many fruits and vegetables. Xylitol-rich plant materials include birch and beechwood . It is widely used as a sugar substitute and in "sugar-free" food products. The effects of xylitol on dental caries have been widely studied, and xylitol is added to some chewing gums and other oral care products to prevent tooth decay and dry mouth. Xylitol is a non-fermentable sugar alcohol by most plaque bacteria, indicating that it cannot be fermented into cariogenic acid end-products . It works by inhibiting the growth of the microorganisms present in plaque and saliva after it accummulates intracellularly into the microorganism . The recommended dose of xylitol for dental caries prevention is 6–10 g/day, and most adults can tolerate 40 g/day without adverse events .
There has been evidence of xylitol in dental hygiene in reducing dental caries disease and also reversing the process of early caries . Xylitol increases salivary flow and pH, reduces the levels of Streptococcus mutans in plaque and saliva and reduces the adhesion on the microorganism to the teeth surface . Streptococcus mutans is the main target plaque microorganism , but xylitol may potentially have inhibitory actions against several other bacterial species .It prevents a shift of the bacterial community towards a more cariogenic microflora in oral environment . Oral ingestion of xylitol causes a smaller rise in plasma glucose and insulin concentrations than does the ingestion of glucose in healthy men and diabetics .
| Trade Name | Florhex |
| Generic | Xylitol + Sodium Fluoride + Triclosan |
| Weight | 5%w/v |
| Type | Mouth Wash |
| Therapeutic Class | |
| Manufacturer | Gipla Health Care |
| Available Country | India |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Sodium fluoride is an antiseptic & anticavity mouthwash which-
- Restores enamel to strengthen teeth
- Protects teeth from cavity
- Helps to prevent tooth decay
- Controls tartar that can discolor teeth
- whitens teeth safety
Triclosan is an antimicrobial agent in clinical setting for disinfection, and prevention of spread and growth of bacteria, fungus, and mildew.
Triclosan is used in a variety of common household products, including soaps, mouthwashes, dish detergents, toothpastes, deodorants, and hand sanitizers. It is also used in health care settings in surgical scrubs and personnel hand washes.
Xylitol is an ingredient added to dental products to remove bacteria.
Indicated for use as a sugar substitute, and oral hygiene active ingredient.
Florhex is also used to associated treatment for these conditions: Caries; Enamel, Cavity, Dental Cavity, Dental Decay, Dental Health, Partial Denture Wearers Wear of the Natural Enamel, Tooth Sensitivity, Trace Element Deficiency, Wear of the Natural Enamel caused by teeth grinding, Parenteral NutritionAcne, Dental Cavity, Dermabrasion, Gingivitis, Oral Infection, Plaque, Dental, Skin Infections, Bacterial, Abrasions, Minor burns, Antibacterial therapy, Antibiotic pre-surgical prophylaxis
How Florhex works
The prevention of dental caries by topical fluoride is achieved by various mechanisms. Sodium fluoride kills bacteria that cause caries, such a Streptococcus mutans and lactobacilli by interfering with their metabolic activities that result in the formation of lactic acid. Fluoride ions cause the inhibition of glycolytic and other enzymes involved in bacterial metabolism. It changes the permeability of cell membranes, lowering the pH in the cytoplasm of the cell, leading to a decrease in acidity, which is normally implicated in tooth decay.
When administered at low topical doses, fluoride in both saliva and plaque and saliva prevent the demineralization of healthy tooth enamel while remineralizing teeth that have previously been demineralized. Sodium fluoride is absorbed by the surface of hydroxyapatite crystals on the teeth, which are necessary for mineralization. This renders the teeth more resistant to demineralization by changing the apatite crystal solubility. Sodium fluoride inhibits the demineralization of teeth in a pH-related manner. When used in high doses, in formulations such as the fluoride varnishes or gels, sodium fluoride forms a layer on the surface of tooth enamel. When the pH of the mouth is reduced due to acid production by bacteria such as S.mutans, fluoride is released, interfering with bacterial metabolism, and then acts to remineralize the teeth.
Triclosan is a biocidal compound with multiple targets in the cytoplasm and membrane. At lower concentrations, however, triclosan appears bacteriostatic and is seen to target bacteria mainly by inhibiting fatty acid synthesis. Triclosan binds to enoyl-acyl carrier protein reductase enzyme (ENR). This complex has increased affinity for NAD+ and forms a ternary complex. This complex is unable to participate in fatty acid synthesis, weakening the cell membrane and causing cell death. Humans do not have an ENR enzyme, and thus are not affected.
Xylitol is initially taken up by the microorganism and accumulates intracellularly. Accumulated xylitol is transported into an energy-consuming cycle, or the inducible fructose transport system. It is converted to non-metabolizable, toxic xylitol-5-phosphate via phosphoenolpyruvate: a constitutive fructose phosphotransferase system by S. mutans . This metabolic process of xylitol, without the gain of any energy molecules, results in the development of intracellular vacuoles and cell membrane degradation. S. mutans dephosphorylates xylitol-5-phosphate and expels it from the cell, in which requires energy consumption. This ultimately leading to starving of microorganism and growth inhibition . Long-term exposure to xylitol can cause microorganisms to develop resistance to xylitol. This clinically beneficial selection process creates xylitol-resistant mutans strains that are less virulent and less cariogenic than their parent strains . Xylitol also increases the concentrations of ammonia and amino acids in plaque, thereby neutralizing plaque acids . A study suggests that xylitol may also promote remineralization of deeper layers of demineralized enamel by facilitating Ca2+ and phosphate movement and accessibility .
Dosage
Florhex dosage
Rinse (gargle) with fall strength Sodium fluoride for 30 seconds with 20 ml (with the help of supplied cup) two times daily (morning and evening). Do not swallow. Don’t eat or drink within 30 minutes after rinsing with Sodium fluoride restoring.
Side Effects
Hypersensitivity reactions, rash, nausea, vomiting. Products containing stannous fluoride may cause teeth staining.
Toxicity
The oral LD50 of sodium fluoride is 44 mg/kg in mice and 31 mg/kg in rats. The oral LD50 of sodium fluoride in rabbits is 200 mg/kg.
Overdose information
The ingestion of toothpaste is the major cause of sodium fluoride overdose. This is followed by sodium fluoride supplements and mouth rinses. Most causes of sodium fluoride toxicity have been observed in children under the age of 6 years old. The manifestations of a sodium fluoride overdose may include gastrointestinal disturbance, abdominal pain, alterations in taste, seizures, salivation, bradycardia, tachycardia, headache, tremor, and shallow breathing. Gastrointestinal bleeding may also occur in addition to a sensation of burning in the mouth. Hypotension, bronchospasm, fixed mydriasis, and elevated potassium can also occur which, in turn, may lead to arrhythmias and cardiac arrest.
Management
If a dose greater than 5 mg fluoride per kilogram of body weight (2.3 mg fluoride per pound of body weight) has been taken, it is advisable to induce vomiting. Administer calcium in an oral, soluble form (for example, 5% calcium gluconate, a solution of calcium lactate, or milk). The patient should seek immediate medical attention. If a sodium fluoride ingestion of 15 mg fluoride/kg of body weight or more occurs (i.e. higher than 6.9 mg fluoride per pound), immediately induce vomiting, provide supportive care, and admit the patient to the hospital for observation.
Oral LD50, Rat: 3700 mg/kg; Dermal LD50, Rabbit: 9300 mg/kg
Oral LD50 is 16500 mg/kg in rat . At high dosages, xylitol can cause diarrhea in children at 45 g/d and 100 g/d in adults .
Precaution
Prolonged treatment with large amounts of fluoride may result in dental fluorosis and osseous changes; do not exceed recommended dosage. Renal impairment. Pregnancy.
Interaction
Absorption of fluoride may be reduced by aluminium, calcium and magnesium salts.
Volume of Distribution
Fluoride distributes to the saliva, bones, and teeth, and is also found in lesser quantities in the breastmilk and sweat. After the ingestion of sodium fluoridated drinking water, the fluoride ions are found to distribute to the plasma and blood cells. Plasma levels of fluoride concentrations are twice as the concentrations found in blood cells. Adults have been found to retain 36% of ingested fluoride and children have been found to retain about 50% of a dose. Most of the retained fluoride is localized to bone and teeth and 1% accumulates in soft tissues. Fluoride crosses the placenta and the blood-brain barrier. The central nervous system concentrations of sodium fluoride are estimated to reach 20% the plasma concentrations. Studies conducted in communities with high levels of fluoride in water did not show any increase in birth defects. The placenta is able to regulate the accumulation of excess fluoride, possibly protecting the fetus from high levels of fluoride. Despite this, excessively high exposure to fluoride in utero may lead to skeletal fluorosis.
No pharmacokinetic data available.
Elimination Route
Sodium fluoride is 90% absorbed from the gastrointestinal tract, with 77% of absorption in the proximal intestine and about 25% in the stomach. The rate of absorption may vary according to gastric pH. Cmax is reached 20-60 minutes after ingestion. Cmax was estimated to be 848 ± 116 ng/mL after a 20mg sodium fluoride solution was ingested, with a Tmax of 0.46 ± 0.17 hours. The bioavailability of sodium fluoride tablets administered in the fasted state during one pharmacokinetic study approached 100%. Another resource reports a sodium fluoride AUC of 1.14 ± 0.12 μg × h/mL after the ingestion of fluoridated water.
A study conducted in 2000 demonstrated that low amounts of triclosan can be absorbed through skin and can enter the bloodstream. [PMID: 10722890] Triclosan is rapidly absorbed and distributed in the human body (Sandborgh-Englund et al., 2006). Maximum concentrations are reached within three hours after oral intake. However, the metabolism and excretion of the compound is fast.
Xylitol is absorbed in the small intestine via passive diffusion with a slow absorption rate .
Half Life
The terminal plasma elimination half-life following the ingestion of fluoridated drinking water generally ranges from 3 to 10 hours. The half-life of sodium fluoride in the bones is 20 years.
The terminal plasma half life of triclosan is 21 h (Sandborgh-Englund et al., 2006).
No pharmacokinetic data available.
Clearance
Sodium fluoride is rapidly cleared by the kidneys and depends on various factors, including glomerular filtration rate, urine flow, and urine pH. According to one clinical study evaluating the pharmacokinetics of oral sodium fluoride tablets in healthy young adults, the renal clearance was determined to be 77.4 ± 11.2mL/min for acidic urine and 78.4 ± 6.9mL/min for alkaline urine. Another reference estimates the renal clearance of fluoride ions from sodium fluoridated water at 35–45 mL/min.
No pharmacokinetic data available.
Elimination Route
Sodium fluoride is rapidly excreted, mainly in the urine. About 90% of fluoride is filtered by the glomerulus and reabsorbed by the renal tubules. About 10% is excreted in the feces.
In one study, after in vivo topical application of a 64.5mM alcoholic solution of [(3)H]triclosan to rat skin, 12% radioactivity was recovered in the faeces, 8% in the carcass 1% in the urine, 30% in the stratum corneum and 26% was rinsed from the skin surface at 24 hours after application. [PMID: 10722890]
No pharmacokinetic data available.
Contraindication
Not to use 1 mg tablets in children less then 3 yr of age or when drinking water fluoride content is >= 0.3 ppm.
Acute Overdose
In acute poisoning, symptoms include a salty or soapy taste, increased salivation, GI disturbances, abdominal pain, weakness, drowsiness, faintness and shallow breathing; more serious effects include hypocalcaemia, hypomagnesaemia, hyperkalaemia, tremors, convulsions, cardiac arrhythmias, shock, respiratory arrest and cardiac failure. Death may occur within 2-4 hr. Treatment includes gastric lavage with lime water or a weak solution of another calcium salt to precipitate fluoride. Maintain high urine output, slow IV inj of calcium gluconate 10% may be used for hypocalcaemia and tetany. Magnesium sulfate may be given to treat hypomagnesaemia, and aluminium hydroxide may help to reduce fluoride absorption. Haemodialysis may be considered. Chronic fluoride poisoning may cause skeletal fluorosis resulting in bone pain, stiffness, limited movment and in severe cases, crippling deformities. In children, prolonged excessive intake during tooth development before eruption may cause dental fluorosis characterised by mottled enamel.
Storage Condition
Store in tight plastic containers.
Innovators Monograph
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