Source: Υπουργείο Υγείας (CY) Revision Year: 2021 Publisher: Remedica Ltd, Aharnon Str., Limassol Industrial Estate, 3056 Limassol, Cyprus
Pharmacotherapeutic group: Gynecological anti-infectives and antiseptics, Anti-infectives and antiseptics excl. combinations with corticosteroids
ATC code: G01AF02
Clotrimazole acts against fungi by inhibiting ergosterol synthesis. Inhibition of ergosterol synthesis leads to structural and functional impairment of the cytoplasmic membrane.
Clotrimazole has a broad antimycotic spectrum of action in vitro and in vivo, which includes dermatophytes, yeasts, moulds, etc.
Under appropriate test conditions, the MIC values for these types of fungi are in the region of less than 0.062-8.0 μg/ml substrate. The mode of action of clotrimazole is fungistatic or fungicidal depending on the concentration of clotrimazole at the side 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 vagiinalis) and gram-negative microorganisms (Bacteroides). It has no effect on lactobacilli.
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 therapeutic conditions.
Pharmacokinetic investigations after vaginal application have shown that only a small amount of clotrimazole (3-10% of the dose) is absorbed. Due to the rapid hepatic metabolism of absorbed clotrimazole into pharmacologically inactive metabolites the resulting peak plasma concentrations of clotrimazole after vaginal application of a 500 mg dose were less than 10 ng/ml, reflecting that clotrimazole applied intravaginally does not lead to measurable systemic effects or side effects.
Non-clinical data reveal no special hazard for humans based on conventional studies of safety pharmacology, repeated dose toxicity, genotoxicity, carcinogenic potential and toxicity to reproduction and development.
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