Olasol

Olasol Uses, Dosage, Side Effects, Food Interaction and all others data.

Benzocaine, an ester local anaesthetic, blocks the initiation and conduction of nerve impulses by decreasing the neuronal membrane’s permeability to Na ions, which results in inhibition of depolarisation with resultant blockade of conduction.

Benzocaine is indicated for use as a topical anesthetic. It has a duration of action of approximately 10 minutes and a wide therapeutic window. Patients should be counselled regarding the risks of methemoglobinemia.

Boric acid, also known as hydrogen borate, is a weak monobasic Lewis acid of boron with the chemical formula H3BO3. Boric acid is typically utilized in industrial processing and manufacturing, but is also used as an additive in pharmaceutical products, cosmetics, lotions, soaps, mouthwash, toothpaste, astringents, and eyewashes . It is known to exhibit some antibacterial activity against infections such as bacterial vaginosis and candidiasis .

Boric acid exhibits minimal bacteriostatic and antifungal activities . Boric acid is likely to mediate antifungal actions at high concentrations over prolonged exposures .

Chloramphenicol inhibits bacterial protein synthesis by binding to 50s subunit of the bacterial ribosome, thus preventing peptide bond formation by peptidyl transferase. It has both bacteriostatic and bactericidal action against H. influenzae, N. meningitidis and S. pneumoniae.

Chloramphenicol is a broad-spectrum antibiotic that was derived from the bacterium Streptomyces venezuelae and is now produced synthetically. Chloramphenicol is effective against a wide variety of microorganisms, but due to serious side-effects (e.g., damage to the bone marrow, including aplastic anemia) in humans, it is usually reserved for the treatment of serious and life-threatening infections (e.g., typhoid fever). Chloramphenicol is bacteriostatic but may be bactericidal in high concentrations or when used against highly susceptible organisms. Chloramphenicol stops bacterial growth by binding to the bacterial ribosome (blocking peptidyl transferase) and inhibiting protein synthesis.

Trade Name Olasol
Generic Benzocaine + Boric Acid + Chloramphenicol + Hippophaes Oleum
Type
Therapeutic Class
Manufacturer
Available Country Russia
Last Updated: September 19, 2023 at 7:00 am
Olasol
Olasol

Uses

For the temporary relief of pain due to minor injury or irritation of the mouth and gums like Toothache, Sore gums, Canker sores, Braces, Minor dental procedures, Dentures

No FDA- or EMA-approved therapeutic indications on its own.

Chloramphenicol is used for Ocular infections, Bacterial meningitis, Anaerobic bacterial infections, Anthrax, Brain abscess, Ehrlichiosis, Gas gangrene, Granuloma inguinale, Infections caused by H. influenzae, Listeriosis, Plague, Psittacosis, Q fever, Severe gastroenteritis, Severe melioidosis, Severe systemic infections with Camphylobacter fetus, Tularaemia, Whipple's disease, Otitis externa

Olasol is also used to associated treatment for these conditions: Acute Sore Throat Pain, Dental Pain, Gangrene Stomatitis, Gingivitis, Hemorrhoids, Laryngitis, Pharyngitis, Premature Ejaculation, Secondary Bacterial Infection caused by Tonsillectomy, Secondary Bacterial Infection caused by Tooth Extractions, Skin Irritation, Sore Throat, Stomatitis, Sunburn, Teething pain, Tonsillitis, Tooth Pain, Vomiting, Pruritic dermatosis, Ulceration of the mouth, Buccopharyngeal anesthesiaAcne, Asthenopia, Ocular Irritation, Skin Mycoses, Eye discomfort, Skin disinfection, Irrigation of the ocular surface therapyAcne, Bacterial Conjunctivitis, Bacterial Conjunctivitis caused by susceptible bacteria, Bacterial Infections, Bacterial dacryocystitis, Bacterial diarrhoea, Conjunctivitis allergic, Corneal Inflammation, Eye swelling, Keratitis bacterial, Ocular Inflammation, Trachoma, Anterior eye segment inflammation, Bacterial blepharitis, Bacterial corneal ulcers, Non-purulent ophthalmic infections caused by susceptible bacteria, Superficial ocular infections, Skin disinfection

How Olasol works

Benzocaine diffuses into nerve cells where it binds to sodium channels, preventing the channels from opening, and blocking the influx of sodium ions. Nerve cells unable to allow sodium into cells cannot depolarize and conduct nerve impulses.

Information regarding the mechanism of action of boric acid in mediating its antibacterial or antifungal actions is limited. Boric acid inhibits biofilm formation and hyphal transformation of Candida albicans, which are critical virulence factors . In addition, arrest of fungal growth was observed with the treatment of boric acid .

Chloramphenicol is lipid-soluble, allowing it to diffuse through the bacterial cell membrane. It then reversibly binds to the L16 protein of the 50S subunit of bacterial ribosomes, where transfer of amino acids to growing peptide chains is prevented (perhaps by suppression of peptidyl transferase activity), thus inhibiting peptide bond formation and subsequent protein synthesis.

Dosage

Olasol dosage

Apply to the affected area up to 4 times daily or as directed by a doctor/dentist. Children under 12 years of age should be supervised during the use of this product. Children under 2 years of age should be consulted to a doctor/dentist prior to the use of this product. An easy application might be done by fixing applicator on the tube’s nozzle. After application, supplied cap should be fixed on top of the applicator.

For Eye: Adults, children and infants (all age groups): One or two drops 4 to 6 times a day should be placed in the infected eyes. If necessary the frequency of dose can be increased. Treatment should be continued for approximately 7 days but should not be continued for more than three weeks without re-evaluation by the prescribing physician.

For Ear: 2 to 3 drops into ear canal thrice or four times daily.

Otic/Aural: Otitis externa:Instill 2-3 drops of a 5% solution into the ear bid-tid.

Oral:Bacterial meningitis, Anaerobic bacterial infections, Anthrax, Brain abscess, Ehrlichiosis, Gas gangrene, Granuloma inguinale, Infections caused by H. influenzae, Listeriosis, Plague, Psittacosis, Q fever, Severe gastroenteritis, Severe melioidosis, Severe systemic infections with Camphylobacter fetus, Tularaemia, Whipple's disease:

  • Adult:50 mg/kg/day in 4 divided doses increased to 100 mg/kg/day for meningitis or severe infections due to moderately resistant organisms. Continue treatment after the patient's temperature has normalised for a further 4 days in rickettsial disease and 8-10 days in typhoid fever.
  • Child:Premature and full-term neonates: 25 mg/kg/day in 4 divided doses. Full-term infants >2 wk: 50 mg/kg/day in 4 divided doses. Children: 50 mg/kg/day in 4 divided doses increased to 100 mg/kg/day for meningitis or severe infections.

Side Effects

Side effects are less common. The side effects include allergies, swelling in the mouth or throatetc.

Oral: GI symptoms; bleeding; peripheral and optic neuritis, visual impairment, blindness; encephalopathy, confusion, delirium, mental depression, headache. Haemolysis in patients with G6PD deficiency.

ophthalmic application: Hypersensitivity reactions including rashes, fever and angioedema.

Ear drops: Ototoxicity.

Toxicity

Patients experiencing an overdose may present with local anesthetic systemic toxicity syndrome, decreased cardiovascular function, decreased central nervous system function, cardiac arrest, bradycardia, hypotension, cardiac arrhythmias, syncope, and seizures. Patients should be treated with symptomatic and supportive measures which include airway maintenance, controlling seizures, and hemodynamic stabilization.

Acute oral LD50 is 2660 mg/kg in rat . Individuals are likely to be exposed to boric acid from industrial manufacturing or processing. Local tissue injury from boric acid exposure is likely due to caustic effects. Systemic effects from boric acid poisoning usually occur from multiple exposures over a period of days and involve gastrointestinal, dermal, CNS, and renal manifestations. Gastrointestinal toxicity include persistent nausea, vomiting, diarrhea, epigastric pain, hematemesis, and blue-green discoloration of the feces and vomit . Following the onset of GI symptoms, a characteristic intense generalized erythroderma follows . Management of mild to moderate toxicity should be supportive. In case of severe toxicity, dialysis may be required in addition to supportive treatment.

Oral, mouse: LD50 = 1500 mg/kg; Oral, rat: LD50 = 2500 mg/kg. Toxic reactions including fatalities have occurred in the premature and newborn; the signs and symptoms associated with these reactions have been referred to as the gray syndrome. Symptoms include (in order of appearance) abdominal distension with or without emesis, progressive pallid cyanosis, vasomotor collapse frequently accompanied by irregular respiration, and death within a few hours of onset of these symptoms.

Precaution

Patient with asthma, bronchitis, emphysema, heart disease; smokers. Children, Pregnancy and lactation.

Impaired renal or hepatic function; premature and full-term neonates. Monitor plasma concentrations to avoid toxicity.

Interaction

May antagonise the therapeutic effect of sulfonamides. Anticholinesterases may inhibit the metabolism benzocaine.

Decreased effects of iron and vitamin B12 in anaemic patients. Phenobarbitone and rifampin reduce efficacy of chloramphenicol. Impairs the action of oral contraceptives.

Volume of Distribution

Volume of distribution ranges from 0.17 to 0.5 L/kg in humans, where large amounts of boric acid are localized in brain, liver, and kidney .

Elimination Route

Boric acid is well absorbed from the gastrointestinal tract, open wounds, and serous cavities but displays limited absorption in intact skin . Following intraperitoneal injection in mice, the peak concentration was reached in about 1.0-1.5 hr in the brain whereas the value was 0.5 hr in other tissues .

Rapidly and completely absorbed from gastrointestinal tract following oral administration (bioavailability 80%). Well absorbed following intramuscular administration (bioavailability 70%). Intraocular and some systemic absorption also occurs after topical application to the eye.

Half Life

According to human cases of poisoning, the elimination half-life of boric acid ranges from 13 to 24 hours .

Half-life in adults with normal hepatic and renal function is 1.5 - 3.5 hours. In patients with impaired renal function half-life is 3 - 4 hours. In patients with severely impaired hepatic function half-life is 4.6 - 11.6 hours. Half-life in children 1 month to 16 years old is 3 - 6.5 hours, while half-life in infants 1 to 2 days old is 24 hours or longer and is highly variable, especially in low birth-weight infants.

Clearance

A case report of acute boric acid poisoning following oral ingestion of 21 g of boric acid presents the total body clearance of 0.99 L/h before hemodialysis .

Elimination Route

Regardless the route of administration, boric acid predominantly undergoes rapid renal excretion of >90% of total administered dose as unchanged form. Small amounts are also excreted into sweat, saliva, and feces. Following administration as ointment, urinary excretion of boric acid accounted for only 1% of the administered dose .

Pregnancy & Breastfeeding use

Pregnancy Category C. Either studies in animals have revealed adverse effects on the fetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the fetus.

Pregnancy Category C. Either studies in animals have revealed adverse effects on the fetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the fetus.

Contraindication

Epiglottis (oral spray), methaemoglobinaemia.

History of hypersensitivity or toxic reaction to the drug; pregnancy, lactation; porphyria; parenteral admin for minor infections or as prophylaxis; preexisting bone marrow depression or blood dyscrasias.

Acute Overdose

Symptom: Methaemoglobinaemia, manifested by cyanotic (greyish) skin discolouration, unusual breathing or breathlessness.

Management: Symptomatic and supportive treatment. IV methylene blue 1% may be administered.

Storage Condition

Store between 15-30° C.

Cap/susp: Store at temp not exceeding 30°C.

Ophth/otic preparation: Store between 2-8°C. Do not freeze. Protect from light.

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