Canesten VT1 Mechanism of Action

ATC Code: G01A F02.
Pharmacology: Clotrimazole is an imidazole derivative with a broad spectrum antimycotic activity.
Mechanism of Action: Azoles (e.g. clotrimazole) are usually recommended for the local treatment of vulvovaginal candidiasis that is characterized by vulvovaginal symptoms such as itching, burning, discharge, redness, swelling and soreness. Clotrimazole acts against fungi by inhibiting ergosterol synthesis. Inhibition of ergosterol synthesis leads to structural and functional impairment of the cytoplasmic membrane.
Pharmacodynamics: 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 g/ml substrate.
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), and gram-negative microorganisms (Bacteroides/Gardnerella vaginalis). In vitro clotrimazole inhibits the multiplication of Corynebacteria and grampositive cocci - with the exception of Enterococci - in concentrations of 0.5-10 g/ml substrate and exerts a trichomonacidal action at 100 g/ml. 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.
Pharmacokinetics: Pharmacokinetic investigations after vaginal application have shown that only a small amount of clotrimazole (3-10%) is absorbed. Due to the rapid hepatic metabolization 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, suggesting that clotrimazole applied intravaginally is unlikely to lead to measurable systemic effects or side effects.