Alconil

Uses

Dental cavities, Tooth decay, Bad breath, Dental plaque, Gingivitis

Alconil is also used to associated treatment for these conditions: GingivitisAcute Muscle Pain, Arthritis, Back Pain Lower Back, Backache, Contusions, Joint Pain, Ligament pain, Muscle Inflammation, Muscle Injuries, Muscle Strain, Muscle swelling, Pain, Pain of the Bone and Bones, Pain, Nerve, Partial-Onset Seizures, Postherpetic Neuralgia, Soreness, Muscle, Sprains, Tendon pain, Minor aches, Muscle, joint painsCaries; 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 NutritionArthritis, Backache, Contusions, Joint Diseases, Joint Pain, Muscle Stiffness, Muscle Strain, Muscular Fatigue, Pain, Nerve, Plaque, Dental, Soreness, Muscle, Sprains, Skin disinfection

How Alconil works

Counter-irritation is thought to be effective at alleviating musculoskeletal pain as the irritation of the sensory nerve endings is thought to alter or offset pain in the underlying muscle or joints that are served by the same nerves . This is thought to mask the underlying musculoskeletal pain and discomfort. When applied topically, methyl salicylate is thought to penetrate the skin and underlying tissues where it reversibly inhibits cyclooxygenase enzyme and locally and peripherally prevents the production of inflammatory mediators such as prostaglandin and thromboxane A2.

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.

Dosage

Alconil dosage

Adults and children 6 years of age and older: Rinse full strength for 1 minute with 10 ml in morning and night. Do not swallow.

Children under 6 years of age: Consult a dentist or doctor.

Side Effects

Local irritation of mouth, nausea & vomiting.

Toxicity

Oral, rat LD50: 2480 mg/kg

Oral LD50 values (mg/kg) for mouse, rat and rabbit are 1110, 887 and 1300, respectively. Oral LD50 values for child and adult human (mg/kg) are 228 and 506, respectively. Although systemic toxicity from topical administration is rare, methyl salicylate can be absorbed in intract skin to cause stimulation of the central nervous system respiratory center, disturbance of lipid and carbohydrate metabolism, and disturbance of intracellular respiration. Severe toxicity can result in acute lung injury, lethargy, coma, seizures, cerebral edema, and death. In case of salicylate poisoning, the treatment consists of general supportive care, gastrointestinal decontamination with activated charcoal in cases of salicylate ingestion, and monitoring of serum salicylate concentrations. Bicarbonate infusions or hemodialysis can be used to achieve enhanced salicylate elimination .

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.

Precaution

Do not swallow. It is not indicated below 12 years of age. Do not rinse, eat, or smoke for thirty minutes after using a mouthwash. Doing so will diminish the effects of the mouthwash.

Interaction

There are no known drug interactions and none well documented.

Volume of Distribution

After absorption, methyl salicylate is distributed throughout most body tissues and most transcellular fluids, primarily by pH dependent passive processes. Salicylate is actively transported by a low-capacity, saturable system out of the CSF across the choroid plexus. The drug readily crosses the placental barrier.

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.

Elimination Route

Approximately 12-20% of topically applied methyl salicylate may be systemically absorbed through intact skin within 10 hours of application, and absorption varies with different conditions such as surface area and pH. Dermal bioavailability is in the range of 11.8 – 30.7%. For the assessment of potential oral exposure to salicylates, bioavailability is assumed to be 100% .

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.

Half Life

The plasma half-life for salicylate is 2 to 3 hr in low doses and about 12 hr at usual anti-inflammatory doses. The half-life of salicylate may be as long as 15 to 30 hr at high therapeutic doses or when there is intoxication.

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.

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.

Elimination Route

Excreted by kidneys as free salicylic acid (10%), salicyluric acid (75%), salicylic phenolic (10%) and acyl glucuronide (5%), and gentisic acid (less than 1%).

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.

Pregnancy & Breastfeeding use

Pregnancy Category: Not Classified. FDA has not yet classified the drug into a specified pregnancy category.

Contraindication

Hypersensitivity

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 a cool & dry place. Keep out of reach of children. Cold weather may cloud this product but its antiseptic & anticavity properties are not affected.

Innovators Monograph

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