Clotritas Mechanism of Action

Pharmacotherapeutic group: Antifungals for topical use - Imidazole and Triazole derivatives.
Pharmacology: Mechanism of Action: Clotrimazole acts against fungi by inhibiting ergosterol synthesis. Inhibition of ergosterol synthesis leads to structural and function impairment of the cytoplasmic membrane.
Pharmacodynamics: Clotrimazole has a broad antimycotic spectrum of action in vitro and in vivo, which includes dermatophytes, yeast, moulds, etc. Under appropriate test conditions, the MIC values for these types of fungi area in the region of less than 0.062 - 8.0 μg/mL.
The mode of action of clotrimazole is primarily fungistatic or fungicidal depending on the concentration of clotrimazole at the site of infection. In vitro activity is limited to proliferating fungal elements; fungal spores are only slightly sensitive.
In addition to its antimycotic action, clotrimazole also acts on gram-positive microorganisms (Streptococci/Staphylococci/Gardnerella vaginitis), and gram-negative microorganisms (Bacteroides).
In vitro clotrimazole inhibits the multiplication of Corynebacteria and gram-positive cocci - with the exception of Enterococci - in concentrations of 0.5 - 10 μg/mL substrate.
Primarily resistant variants of sensitive fungal species are very rare; the development of secondary resistance by sensitive fungi has so far only been observed in very isolated cases under the therapeutic conditions.
Pharmacokinetics: Pharmacokinetic investigations after dermal application have shown that clotrimazole is minimally absorbed from the intact or inflamed skin into the human blood circulation. The resulting peak serum concentrations of clotrimazole were below the detection limit of 0.001 mcg/mL, suggesting that clotrimazole applied topically is unlikely to lead to measurable systemic effects or side effects.