Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0033774 (pruritus)
 14,546 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The incidence of mycotic infections is on the rise in the United States. The failure of patients and clinicians to recognize a fungal infection early may lead to extensive, severe, and difficult-to-treat disease. Treatment decisions must include an awareness of the etiologic organism involved, the potential for long-term recurrence, symptoms such as inflammation and itching, and the importance of patient adherence to treatment. Sertaconazole nitrate, a broad-spectrum imidazole agent with antifungal, antibacterial, antiinflammatory, and antipruritic properties, is the topical antifungal agent most recently approved by the US Food and Drug Administration. A review of its mechanisms of action, pharmacokinetic profile, fungistatic and fungicidal activities, and clinical properties examines a substantial body of research findings that establish its efficacy, safety, and tolerability. Its use in the treatment of tinea pedis and other superficial mycotic infections is reviewed here.
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PMID:Comprehensive management of patients with superficial fungal infections: the role of sertaconazole nitrate. 1869 45

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.
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PMID:Sertaconazole: a review of its use in the management of superficial mycoses in dermatology and gynaecology. 1927 77

Sertaconazole is a new antifungal agent. To compare the efficacy and tolerability of sertaconazole and miconazole cream in cutaneous dermatophytosis, this prospective, randomized, multicentric comparative, phase 4 study was undertaken in 260 patients with cutaneous dermatophytosis after approvals from Institutional Ethics Committees. Patients were assigned to sertaconazole cream (2%) or miconazole cream (2%) topically twice daily for 2 weeks after obtaining informed consent. Efficacy variables included changes in mean scores of erythema, pruritus, desquamation, erythema/itching, burning/weeping, scaling/pustule and overall global assessment. Safety and tolerability were also assessed. A total of 122 patients in the sertaconazole group and 128 in the miconazole group completed the study with 10 drop-outs. There was a significant decrease (P < 0.05) in mean symptom scores and total scores from the first week onwards, sustained till 2 weeks and statistically significant (P < 0.05) in favour of sertaconazole. Moreover, 62.3% patients had complete clinical cure in the sertaconazole group (P < 0.05) compared with 44.6% in miconazole users. Both drugs were well tolerated and five patients in the sertaconazole group and nine in the miconazole group reported mild to moderate adverse events. Therapy with sertaconazole cream (2%) provided a better efficacy and tolerability compared with the miconazole cream (2%) and could thus be a therapeutic option in cutaneous dermatophytosis.
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PMID:Efficacy and tolerability of sertaconazole nitrate 2% cream vs. miconazole in patients with cutaneous dermatophytosis. 1992 67

Sertaconazole nitrate is a broad-spectrum antifungal agent indicated in the United States for the treatment of tinea pedis interdigitalis. The objective of this subgroup analysis was to evaluate the safety and efficacy of sertaconazole nitrate cream 2%, specifically in participants with tinea pedis interdigitalis (ie, fungal skin disease of the toe web) of dermatophyte origin. A total of 92 participants were included in this analysis. The primary end points were eradication of the pathogen (confirmed by fungal culture results) and reduction in total clinical score (TCS) of at least 2 points. Secondary end points included reducing signs and symptoms and reporting adverse events (AEs). After 4 weeks of treatment, 88.8% (79/89) of evaluable participants achieved success on the primary end points. Most participants also demonstrated substantial improvement in signs and symptoms after 4 weeks of treatment: 63.7% (58/91) were free of erythema, 33.0% (30/91) were free of desquamation, and 91.2% (83/91) were free of itch. The rate of reported AEs was low (8.7% [8/92]), and none were considered serious. These findings indicate that sertaconazole nitrate cream 2% is highly safe and effective in the treatment of tinea pedis interdigitalis.
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PMID:Safety and efficacy of sertaconazole nitrate cream 2% in the treatment of tinea pedis interdigitalis: a subgroup analysis. 2034 85

The treatment of cutaneous fungal infections has been shown to be directly affected by the extent of patients' adherence to therapy regimens that are often cumbersome and last for several weeks. One useful alternative approach is once-daily dosing of topical antifungal agents rather than the traditional twice-daily regimen, an example of what has been called a "forgiving" regimen, designed to promote patient adherence. Sertaconazole, an imidazole antifungal agent, is known to be safe and effective when used twice daily in the treatment of tinea pedis. This report discusses a small (n=32) clinical trial designed to determine whether sertaconazole nitrate 2% cream, used once daily, is as effective as the traditional regimen. Results demonstrated that sertaconazole is as effective when used once daily for four weeks. Patients showed rapid improvement in pruritus as early as week 2, and at six weeks' follow up, all patients were free of erythema while 93.8 percent were free of pruritus; no relapses had occurred. These encouraging findings suggest that sertaconazole nitrate may be useful in a once-daily regimen and also may result in better patient adherence to therapy.
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PMID:Treatment of interdigital tinea pedis: once-daily therapy with sertaconazole nitrate. 2196 63