Pharmacodynamics and Mechanism of Action
The drug has a narrow spectrum of activity and is effective only against dermatophyte fungi, causing the death of dermatophytosis pathogens.
In terms of its mechanism, Clotrimazolum acts as a fungistatic agent, halting cell division. Its mechanism resembles a mitotic poison:
- The drug penetrates inside the fungal cell.
- It interacts with tubulin and microtubule proteins.
- It disrupts mitotic spindle formation, thereby inhibiting mitosis.
- Additionally, it inhibits the synthesis of nucleic acids (DNA and RNA).
Pharmacokinetics and Therapy Characteristics
The drug is well absorbed from the gastrointestinal tract, and its absorption is significantly enhanced when taken with a fatty meal.
Clotrimazolum exhibits pronounced tissue tropism: it selectively accumulates in keratin-containing tissues (skin, hair, nails) and binds tightly specifically to newly formed keratin.
The principle of cure is that the drug prevents the infection of newly forming cells. The therapeutic effect develops slowly and occurs only after the old infected stratum corneum is completely shed and replaced by healthy tissues. The duration of the course directly depends on the regeneration rate: skin and hair require 2–6 weeks, while the treatment of onychomycosis (nail infections) can take from 6 to 12 months.
Indications for Use
The main indications for prescribing the drug are dermatophytoses of various localizations, including the feet, hands, scalp, hair, and nails.
In addition, based on its spectrum of activity, agents of this group are used in clinical practice (e.g., compared to econazole): for candidiasis of the stratum corneum and cornea, candidiasis of mucous membranes (oral cavity, pharynx, and vulvovaginitis), and pityriasis versicolor.
Drug Interactions and Additional Properties
An important pharmacological feature of the drug is that it acts as an inducer of hepatic microsomal enzymes (cytochrome P-450 system). This property can accelerate the metabolism of other concurrently administered medications.
It is also worth noting the expanded spectrum of activity of Clotrimazolum (unlike classical narrow-spectrum antifungals): besides fungi, it is effective against anaerobes (Bacteroides, Gardnerella vaginalis), and at high concentrations, it is even active against trichomonads.