PHARMACOLOGICAL PROPERTIES
List of excipients
Silica, colloidal anhydrous Paraffin, liquid
Pharmacotherapeutic group:
Otologicals, Corticosteriods and antiinfectives in combination
ATCvet code:
QS02CA01
Pharmacodynamic properties:
Polymyxin B - Polymyxin B belongs to the polypeptide antibiotics which are isolated from bacteria. It is only active against Gram-negative bacteria, such as Pseudomonas spp., Enterobacter, E. coli, Salmonella spp., and Shigella spp. The mechanism of action is damage of the microbial cytoplasmic membrane, because polypeptides act as cationic detergents. This results bactericidal effect. Resistance of Gram-negative bacteria to polymyxin may result from chromosomal mutations or horizontal transfer of the MCR gene. All Proteus species have a natural resistance to polymyxin.
Miconazole - Miconazole belongs to the group of N-substituted imidazole derivatives. Their most important mechanism of action is the inhibition of ergosterol biosynthesis. Ergosterol is an essential membrane lipid and must be synthesised de novo by fungi. The lack of ergosterol impedes numerous membrane functions and ultimately leads to cell death. The spectrum of activities covers nearly all fungi and yeasts of relevance to veterinary medicine as well as Gram-positive bacteria. Practically no development of resistance has been reported. Miconazole has a fungistatic mode of action, but high concentrations are also observed to produce fungicidal effects.
Prednisolone - Prednisolone is a synthetic corticosteroid and is used for its anti-inflammatory, antipruritic, anti- exudative and anti-proliferative effects. This quickly leads to a symptomatic relief in inflammatory skin diseases.
Its anti-inflammatory activity is approx. 4 - 5 times more potent than that of natural cortisol. Like other glucocorticoids, prednisolone binds to intracellular cytoplasmic receptors in the target organs. After the translocation of the receptor complex into the nucleus it causes derepression of the DNA and subsequently an increase in mRNA synthesis and ultimately protein synthesis. This increases the number of catabolic enzymes for gluconeogenesis. Inhibitory proteins, such as the phospholipase A2-inhibiting lipocortin, are formed. Consequently, the typical glucocorticoid effects and the associated effects are observed. Effects are noticeable only after a latency period. They persist beyond the elimination of the glucocorticoid from the bloodstream as long as there are receptor-glucocorticoid complexes in the nucleus present.
Pharmacokinetic particulars
Polymyxin B - After topical application of polymyxin B, there is virtually no absorption of the ingredient through intact skin and mucous membranes, but significant absorption via wounds.
Miconazole - After topical application of miconazole, there is virtually no absorption of the ingredient through intact skin or mucous membranes.
Prednisolone - After topical application of prednisolone to intact skin, the ingredient is subject to limited and delayed absorption. Greater proportion of the applied ingredient can be absorbed in cases of compromised skin barrier function (e.g. skin lesions).