ATC Group: G01AF Imidazole derivatives

Clotrimazole acts against fungi by inhibiting ergosterol synthesis. Inhibition of ergosterol synthesis leads to structural and functional impairment of the fungal cytoplasmic membrane. Clotrimazole has a broad antimycotic spectrum of action in vitro and in vivo, which includes dermatophytes, yeasts, moulds, etc.

Econazole nitrate is a broad spectrum antimycotic with activity against dermatophytes, yeasts and moulds. A clinically relevant action against Gram positive bacteria has also been found.

Fenticonazole is a broad-spectrum antimycotic agent.

Isoconazole is for use in the treatment of superficial fungal diseases of the skin. It displays a very broad spectrum of antimicrobial action. It is effective against dermatophytes and yeasts, yeast-like fungi (including the causative organism of pityriasis versicolor) and molds, as well against gram-positive bacteria in-vitro and against the causative organism of erythrasma.

Ketoconazole is an imidazole-dioxolane antimycotic, active against yeasts, including Malassezia and dermatophytes.

Metronidazole is an anti-infectious drug belonging to the pharmacotherapeutic group of nitroimidazole derivatives, which have effect mainly on strict anaerobes. This effect is probably caused by interaction with DNS and different metabolites.

Miconazole possesses an antifungal activity against the common dermatophytes and yeasts as well as an antibacterial activity against certain gram-positive bacilli and cocci. Its activity is based on the inhibition of the ergosterol biosynthesis in fungi and the change in the composition of the lipid components in the membrane, resulting in fungal cell necrosis.

Ornidazole is indicated for the treatment of Bacterial vaginosis. It is effective against Trichomonas vaginalis, Entamoeba histolytica and Giardia lamblia (Giardia intestinalis), and also against certain anaerobic bacteria such as Bacteroides and Clostridium spp., Fusobacterium spp., and anaerobic cocci.

Sertaconazole, an azole antifungal agent, inhibits fungal cytochrome P-450-mediated 14 alpha-lanosterol demethylase enzyme. This enzyme functions to convert lanosterol to ergosterol. Ergosterol is a key component of fungal cell membranes and lack of this component leads to fungal cell injury by leakage of key constituents in the cytoplasm from the cell.

Tinidazole is active against both protozoa and obligate anaerobic bacteria. The activity against protozoa involves Trichomonas vaginalis, Entamoeba histolytica and Giardia lamblia. The mode of action of tinidazole against anaerobic bacteria and protozoa involves penetration of the drug into the cell of the micro-organism and subsequent damage of DNA strands or inhibition of their synthesis.

Tioconazole is an imidazole derivative. Tioconazole is a broad spectrum antifungal agent that also has an antibacterial effect on a number of Gram-positive cocci (e.g. Stapphylococcus, Streptococcus species). It is active against commonly occurring dermatophyte and yeast-like fungal species.