Levomycetin 2.5 g, boric acid 1 g, ethanol 70% 100 ml

Uses

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

For therapeutic neurolysis of nerves or ganglia for the relief of intractable chronic pain in such conditions as inoperable cancer and trigeminal neuralgia (tic douloureux), in patients for whom neurosurgical procedures are contraindicated.

Levomycetin 2.5 g, boric acid 1 g, ethanol 70% 100 ml is also used to associated treatment for these conditions: Acne, 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 disinfectionBacterial Infections, Obstructive Hypertrophic Cardiomyopathy, Skin Infections, Bacterial, Skin Irritation, Ethylene glycol overdose, Fat occlusion in central venous catheter, Methanol overdose, Hand Hygiene, Skin disinfection

How Levomycetin 2.5 g, boric acid 1 g, ethanol 70% 100 ml works

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.

Ethanol affects the brain’s neurons in several ways. It alters their membranes as well as their ion channels, enzymes, and receptors. Alcohol also binds directly to the receptors for acetylcholine, serotonin, GABA, and the NMDA receptors for glutamate. The sedative effects of ethanol are mediated through binding to GABA receptors and glycine receptors (alpha 1 and alpha 2 subunits). It also inhibits NMDA receptor functioning. In its role as an anti-infective, ethanol acts as an osmolyte or dehydrating agent that disrupts the osmotic balance across cell membranes.

Dosage

Levomycetin 2.5 g, boric acid 1 g, ethanol 70% 100 ml dosage

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

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

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.

Oral, rat LD₅₀: 5628 mg/kg. Symptoms and effects of overdose include nausea, vomiting, CNS depression, acute respiratory failure or death and with chronic use, severe health problems, such as liver and brain damage.

Precaution

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

Interaction

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.

Rapidly absorbed.

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.

Contraindication

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.

Storage Condition

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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