Evaluation of the Skin Retention Time of Imidazole Derivative/Die Bewertung der Verweildauer von Imidazolderivaten in der Haut

Fenticonazole is an imidazole derivative with a broad spectrum of antimycotic activity. The therapeutic activity and tolerability of 600 mg fenticonazole versus 500 mg clotrimazole were evaluated in an investigator-blind trial in 80 patients with mycologically confirmed vaginal candidiasis. Fenticonazole was administered as an ovule and clotrimazole as a vaginal pessary, both in a single administration. Therapeutic efficacy was assessed by microbiological and clinical criteria 7 days after the start of treatment. Patients cured at the end of the trial were rechecked 4-5 weeks after the start of therapy in order to identify and evaluate possible relapse. Both treatments resulted in a statistically significant reduction in vaginal symptoms (erythema, itching, discharge and oedema) and in elimination of Candida albicans in about 90% of patients. The tolerance of both treatments was excellent since no local or systemic signs or symptoms of toxicity were reported. An equally high efficacy and safety for both drugs in the elimination of symptoms and objective evidence of vaginal candidiasis was indicated.

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Comparison of Single Administration with an Ovule of 600 mg Fenticonazole versus a 500 mg Clotrimazole Vaginal Pessary in the Treatment of Vaginal Candidiasis

Wiest

Azzollini

Ruffmann

et al. 1989

J Int Med Res

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Difference in Percutaneous Absorption and Intracutaneous Distribution in Guinea Pigs among Topical Antifungal Drugs (Tioconazole Solution, Tioconazole Cream, Miconazole Nitrate Solution and Bifonazole Solution)

Sobue

Sekiguchi

2004

Biological & Pharmaceutical Bulletin

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Tioconazole (TCZ) is an imidazole antifungal agent with broad spectrum activity in vitro against dermatophytes and yeasts, as well as against some chlamydia, trichomonads and Gram-positive bacteria.1,2) Its in vitro antifungal activity against dermatophytes, yeasts and bacteria is equal or stronger in comparison with those of the known imidazoles, miconazole nitrate (MCZ), bifonazole (BFZ) and clotrimazole. [3][4][5] TCZ has a dual mechanism of antifungal action that is inhibition of sterol biosynthesis and direct cell membrane damage. [6][7][8] In growing cultures, TCZ exerts a potent killing action. The extent and rapidity of this fungicidal effect of TCZ are greater than those of MCZ and clotrimazole. 9,10) This activity is paralleled by good topical efficacy in a guinea pig dermatomycosis model. 2,9) At the beginning, TCZ was been used as a cream formulation. Clinical trials for treating superficial dermatophyte or yeast infections of the skin have clearly demonstrated once to three times a day topical applications of TCZ cream were at least as effective as alternative imidazole antifungal drugs, and in a few trials significantly greater efficacy has been reported for TCZ cream, compared with MCZ, clotrimazole, and econazole. 1,[11][12][13][14] After that TCZ solution was developed as over-the-counter drug. The efficacy and safety of twice or three times a day topical preparations of TCZ solution appear to be similar to those of TCZ cream and clotrimazole solution. [15][16][17][18] Pharmacokinetic studies in rats have demonstrated minimal systemic exposure following dermal application of TCZ cream.2) After a single application of TCZ cream about 16% of the applied radioactivity penetrates into rat skin and the percutaneous penetration into swine skin is considerably higher than that of clotrimazole cream.19) BFZ also penetrates far better into human skin than clotrimazole. 20) Clinical trials have clearly demonstrated the efficacy and safety of various formulations of BFZ applied once a daily in the treatment of superficial fungal infections of the skin.4) The skin retention time of MCZ in effective therapeutic concentrations is longer than that of BFZ. MCZ formulations are also recommended for once a daily application. 21) In the present study, in order to support the usefulness of once a daily applications of TCZ solution and cream, the percutaneous absorption and intracutaneous distribution of TCZ solution were investigated and compared with those of TCZ cream, MCZ solution and BFZ solution following a single topical application to abdominal skin of guinea pigs. (Tokyo, Japan). Itraconazole, IS for BFZ, was extracted from commercial preparations purchased from Janssen Kyowa Co., Ltd. (Tokyo, Japan). All other chemicals used were of reagent grade. MATERIALS AND METHODS MaterialsAnimals Guinea pigs of the Hartley strain (Japan SLC, Shizuoka, Japan) weighing approximately 400 g were used in the study. The animals were kept in an animal room main- Tioconazole (TCZ) is an imidazole antifungal agent with broa...

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An Overview of Topical Antifungal Therapy in Dermatomycoses

Gupta

Einarson

Summerbell

et al. 1998

Drugs

116

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Dermatophytes cause fungal infections of keratinised tissues, e.g. skin, hair and nails. The organisms belong to 3 genera, Trichophyton, Epidermophyton and Microsporum. Dermatophytes may be grouped into 3 categories based on host preference and natural habitat. Anthropophilic species predominantly infect humans, geophilic species are soil based and may infect both humans and animals, zoophilic species generally infect non-human mammals. It is important to confirm mycologically the clinical diagnosis of onychomycosis and other tinea infections prior to commencing therapy. The identity of the fungal organism may provide guidance about the appropriateness of a given topical antifungal agent. Special techniques may be required to obtain the best yield of fungal organisms from a given site, especially the scalp and nails. It is also important to realise the limitations of certain diagnostic aids e.g., Wood's light examination is positive in tinea capitis due to M. canis and M. audouinii (ectothrix organisms); however, Wood's light examination is negative in T. tonsurans (endothrix organism). Similarly, it is important to be aware that cicloheximide in culture medium will inhibit growth of non-dermatophytes. Appropriate media are therefore required to evaluate the growth of some significant non-dermatophyte moulds. For tinea infections other than tinea capitis and tinea unguium, topical antifungals may be considered. For effective therapy of tinea capitis an oral antifungal is generally necessary. Similarly, oral antifungals are the therapy of choice, especially if onychomycosis is moderate to severe. Furthermore, where the tinea infection involves a large area, in an immunocompromised host or if infection is recurrent with poor response to topical agents, then oral antifungal therapy may be necessary. Topical antifungal agents may be broadly divided into specific and nonspecific agents. The former group includes the polyenes, azoles, allylamines, amorolfine, ciclopirox and butenafine. Generally the topical agent is available as a cream, sometimes for use intravaginally. Less commonly, the formulation may be in the form of a powder, lacquer, spray, gel or solution. Many of these agents have a broad spectrum of activity, being effective against dermatophytes, yeasts and Malassezia furfur. For the treatment of tinea corporis, tinea cruris tinea versicolor and cutaneous candidosis, once or twice daily application may be required, the most common duration of therapy being 2 to 4 weeks. For tinea pedis the most common treatment duration is 4 to 6 weeks.

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Evaluation of the Skin Retention Time of Imidazole Derivative/Die Bewertung der Verweildauer von Imidazolderivaten in der Haut

Cited by 4 publications

References 2 publications

Comparison of Single Administration with an Ovule of 600 mg Fenticonazole versus a 500 mg Clotrimazole Vaginal Pessary in the Treatment of Vaginal Candidiasis

Comparison of Single Administration with an Ovule of 600 mg Fenticonazole versus a 500 mg Clotrimazole Vaginal Pessary in the Treatment of Vaginal Candidiasis

Difference in Percutaneous Absorption and Intracutaneous Distribution in Guinea Pigs among Topical Antifungal Drugs (Tioconazole Solution, Tioconazole Cream, Miconazole Nitrate Solution and Bifonazole Solution)

An Overview of Topical Antifungal Therapy in Dermatomycoses

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