Pharmacology: Pharmacodynamics: This product is a potent agent in the treatment of inflammatory and pruritic dermatoses. In relation to other corticosteroids used topically as adjunctive therapy, this has been shown as effective and, in many instances, was effective when other agents gave inadequate therapeutic response.
The mechanism of action of this product is as a corticosteroid hormone receptor agonist. It is the acetonide salt form of Fluocinolone, a synthetic fluorinated corticosteroid with anti-inflammatory, antipruritic, and vasoconstrictive properties.
Neomycin is an aminoglycoside. It inhibits bacterial protein synthesis through irreversible binding to the 30S ribosomal subunit of susceptible bacteria. Neomycin sulfate provides effective local antibacterial action against many Gram-positive and Gram-negative pathogens, such as Staphylococcus aureus, Streptococci and Proteus vulgaris, encountered in local infections of the ear and adjacent structures.
Polymyxins bind to the cell membrane and alter its structure, making it more permeable. Polymyxin B sulfate is antibacterial for many Gram-negative organisms, including Pseudomonas aeruginosa, a common cause of otitis externa; Escherichia coli and Aerobacter aerogenes. Neomycin sulfate and Polymyxin B sulfate have complementary action against such pathogens as Haemophilus, Corynebacterium, Neisseria, Klebsiella and Pneumococcus.
Propylene glycol is a water-miscible vehicle with low surface tension which facilitates spreadability and penetration of the medication. Fluocinolone acetonide, Neomycin sulfate and Polymyxin B sulfate are highly soluble and stable in this vehicle. The relatively slow rate of evaporation maintains the solution state for an adequate time to allow distribution and contact with all parts of the lesion.
Pharmacokinetics: Fluocinolone acetonide: Rapidly absorbed. Corticosteroids are metabolized primarily in the liver and are then excreted by the kidneys. Some of the topical corticosteroids and their metabolites are also excreted into the bile. Has a half-life of 1.3 to 1.7 hours.
Polymyxin B sulfate: Not absorbed from the normal alimentary tract. The drug is excreted slowly by the kidneys.
Neomycin sulfate: Poorly absorbed from the normal gastrointestinal tract. Although only approximately 3% of neomycin is absorbed through intact intestinal mucosa, significant amounts may be absorbed through ulcerated or denuded mucosa or if inflammation is present. Neomycin undergoes negligible biotransformation after parenteral administration. The small absorbed fraction is rapidly distributed in the tissues and is excreted by the kidney in keeping with the degree of kidney function. Has a half-life of 2 to 3 hours.
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