DERMOFIX

Indications

• Superficial fungal infections
• Tinea pedis (athlete's foot)
• Tinea cruris (jock itch)
• Tinea corporis (ringworm)
• Candidiasis

Dosage

Children: Refer to the BNF for Children for appropriate dosing information.

Adults: Apply a thin layer of sertaconazole cream to the affected area twice daily for 2 to 4 weeks, or as directed by a healthcare professional.

Mechanism of action

Sertaconazole interacts with 14-alpha demethylase, a cytochrome P-450 enzyme necessary for converting lanosterol to ergosterol, a vital component of fungal cell membranes. Inhibition of ergosterol synthesis increases cellular permeability, leading to leakage of cellular contents. Additionally, sertaconazole may inhibit endogenous respiration, interact with membrane phospholipids, inhibit yeast transformation to mycelial forms, and impair triglyceride and phospholipid biosynthesis.

Pharmacodynamics

Sertaconazole is a highly selective inhibitor of fungal cytochrome P-450 sterol C-14 alpha-demethylation, essential for fungal cell wall synthesis. This leads to the accumulation of toxic 14-alpha-methyl sterols in fungi and results in fungistatic effects. It demonstrates activity against pathogens such as Cryptococcus neoformans and Candida species, showing efficacy in both normal and immunocompromised models of systemic infections.

Pharmacokinetics

Sertaconazole is well absorbed through topical applications, with minimal systemic absorption. The pharmacokinetics of sertaconazole in humans have not been extensively studied. The drug is metabolized by liver enzymes, primarily through oxidation and conjugation processes, and is excreted mainly in the urine. Due to its low systemic absorption, significant drug interactions are unlikely.

Adverse effects

• Local irritation
• Erythema
• Pruritus
• Burning sensation

Precautions

• Use with caution in patients with a history of hypersensitivity to imidazole or triazole antifungals.
• Avoid contact with eyes and mucous membranes.

Pregnancy

Sertaconazole should only be used in pregnancy if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

Caution is advised when administering sertaconazole to nursing mothers, as it is not known if it is excreted in human milk.

Storage

Store at room temperature, away from moisture and heat. Keep out of reach of children.

Formulations

• Cream
• Solution

Mechanism of action

Sertaconazole interacts with 14-α demethylase, a cytochrome P-450 enzyme necessary to convert lanosterol to ergosterol. As ergosterol is an essential component of the fungal cell membrane, inhibition of its synthesis results in increased cellular permeability causing leakage of cellular contents. Sertaconazole may also inhibit endogenous respiration, interact with membrane phospholipids, inhibit the transformation of yeasts to mycelial forms, inhibit purine uptake, and impair triglyceride and/or phospholipid biosynthesis.

Pharmacodynamics

Sertaconazole is an imidazole/triazole type antifungal agent. Sertaconazole is a highly selective inhibitor of fungal cytochrome P-450 sterol C-14 &alpha;-demethylation via the inhibition of the enzyme cytochrome P450 14&alpha;-demethylase. This enzyme converts lanosterol to ergosterol, and is required in fungal cell wall synthesis. The subsequent loss of normal sterols correlates with the accumulation of 14 &alpha;-methyl sterols in fungi and may be partly responsible for the fungistatic activity of fluconazole. Mammalian cell demethylation is much less sensitive to fluconazole inhibition. Sertaconazole exhibits <i>in vitro</i> activity against <i>Cryptococcus neoformans</i> and <i>Candida spp.</i> Fungistatic activity has also been demonstrated in normal and immunocompromised animal models for systemic and intracranial fungal infections due to <i>Cryptococcus neoformans</i> and for systemic infections due to Candida albicans.