Sertaconazole (
Dermofix, Ertaczo,
Ginedermofix, Monazol,
Mykosert or
Zalain), an
imidazole antifungal agent, inhibits the synthesis of
ergosterol, an essential cell wall component of fungi. It is indicated in the EU for the treatment of superficial skin
mycoses such as
dermatophytosis (including
tinea corporis,
tinea cruris,
tinea manus,
tinea barbae and
tinea pedis),
cutaneous candidiasis,
pityriasis versicolor and seborrhoeic
dermatitis of the scalp, and in the US for
tinea pedis only.
Sertaconazole has broad-spectrum antifungal activity against dermatophytes of the Trichophyton, Epidermophyton and Microsporum genera, and yeasts of the genera Candida and Cryptococcus; additionally, it is effective against opportunistic filamentous fungi and Gram-positive bacteria. Moreover, the antifungal activity of
sertaconazole is maintained in clinical isolates of dermatophytes that show reduced susceptibility to other
azoles. While the
drug has good dermal penetration, this is not associated with systemic absorption. In clinical trials in patients with superficial
mycoses, 2%
sertaconazole cream applied twice daily was effective in the eradication of a range of
dermatophytoses, and a significantly greater proportion of patients were cured compared with those receiving 2%
miconazole cream twice-daily treatment. In patients with
vulvovaginal candidiasis,
sertaconazole as a single-dose ovule or
tablet was effective in the eradication of Candida spp., and achieved both a more rapid and a higher cure rate compared with a triple dose of
econazole. Both as a topical cream and suppository preparation,
sertaconazole was generally well tolerated.
Sertaconazole is a well established
antifungal agent, which is now available in a variety of formulations, and remains a useful treatment option particularly in patients with
fungal infections resistant to other
azoles. Like other
azoles,
sertaconazole inhibits the synthesis of
ergosterol, an essential component of fungal cell walls, resulting in disruption of mycelial growth and replication. However, at higher concentrations,
sertaconazole binds directly to nonsterol
lipids in the fungal cell wall, which leads to increased permeability and subsequent lysis of the mycelium. Thus, depending on the concentration,
sertaconazole may exhibit both fungistatic and fungicidal activities.
Sertaconazole shows good in vitro fungistatic activity against a broad range of dermatophytes of the Trichophyton, Epidermophyton and Microsporum genera, and yeasts of the genera Candida and Cryptococcus. The geometric minimum inhibitory concentration (MIC) of
sertaconazole ranged from 0.06 to 1 microg/mL against a variety of dermatophyte isolates (n = 456), which included 114 isolates with reduced susceptibility to
fluconazole (MICs > or = 16 microg/mL). Similarly, against a variety of Candida spp., MIC values at which 90% of cultures were inhibited (MIC(90)) for
sertaconazole were < or = 0.1-4 microg/mL compared with MIC(90) of 0.1 to >100 microg/mL for
fluconazole. Furthermore, fungicidal activity of
sertaconazole was apparent against a variety of Candida spp., with minimum fungicidal concentration values of 0.5-64 microg/mL. Additionally,
sertaconazole showed antibacterial activity with a geometric MIC of 0.88 microg/mL against 21 isolates of Gram-positive bacteria. When applied topically in experimental models of
inflammation,
sertaconazole showed some evidence of anti-inflammatory action. Only 4% of 250 clinical isolates of dermatophytes and Scopulariopsis brevicaulis from Spanish hospitals showed resistance to
sertaconazole, and continuous culture of Candida spp. in
sertaconazole-containing media failed to induce resistance. Following application of
sertaconazole as a topical cream or
vaginal suppository, plasma levels of the
drug remained undetectable in healthy volunteers. In randomized, double-blind, multicentre trials of 3-6 weeks' duration (n = 127-383), a significantly greater number of patients with
tinea of the glabrous skin and
tinea pedis receiving topical 2%
sertaconazole cream once or twice daily achieved a successful mycological cure compared with recipients of a placebo cream. Moreover, the clinical cure rate and the mycological cure rate of 2%
sertaconazole cream twice daily was significantly higher than that of 2%
miconazole cream twice daily in patients with a range of cutaneous
mycoses (n = 631) in a randomized, double-blind, multicentre, phase III, comparator trial of 35 days' duration. Furthermore, a greater proportion of patients receiving
sertaconazole achieved the category of clinically cured at a significantly earlier timepoint than recipients of
miconazole. An open-label, noninferiority trial of 28 days' duration in 313 patients with
tinea corporis,
tinea pedis or a corresponding
candidiasis showed that
sertaconazole as a 2%
solution was as effective as treatment with a 2% cream preparation.
Sertaconazole as a single-dose 300 mg vaginal ovule or 500 mg
tablet was successful in the eradication of Candida spp. in 65-100% of patients with vaginal
candidiasis in trials that evaluated clinical and mycological cure rates up to 1 year after the last treatment application (n = 37-327). Furthermore, the clinical cure rate and the mycological cure rate of single-dose
sertaconazole 500 mg
tablet was significantly greater than that of triple-dose
econazole 150 mg in the eradication of Candida albicans and also achieved a more rapid response rate in patients with vaginal
candidiasis (n = 37).
Sertaconazole was generally well tolerated in patients with dermatological and gynaecological
mycoses. Adverse events associated with topical application of
sertaconazole cream were mostly cutaneous-related and included
contact dermatitis, dry or burning skin, application-site reaction,
eczema, itch and skin tenderness. However, the frequency of adverse events did not differ from that of the placebo vehicle treatment arm. Furthermore,
sertaconazole showed no evidence of a sensitizing action in causing
contact dermatitis in healthy volunteers.
Sertaconazole administered as a
vaginal suppository was generally associated with an absence of adverse events and, where reported, included only local irritation after insertion.