Ketoconazole (Topical)

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[edit] BRAND NAMES

[edit] STRUCTURE

Ketoconazole.jpg

[edit] MECHANISM OF ACTION

Ketoconazole is an antifungal agent of the imidazole class. It inhibits lanosterol 14α-demethylase, a cytochrome P-450 enzyme that converts lanosterol to ergosterol.

Ergosterol is an essential component of the fungal cell membrane. The inhibition of its synthesis results in accumulation of toxic 14α-methylated sterols and the production of a defective cell membrane with altered permeability and leakage of cellular contents.

[edit] INDICATIONS

Topical treatment of dermatophyte infections of the skin: tinea corporis, tinea cruris and tinea pedis, as well as in the treatment of pityriasis versicolor and cutaneous candidiasis.

Topical treatment of seborrhoeic dermatitis, a skin condition related with the presence of Pityrosporum ovale.

[edit] DOSAGE

Ketoconazole cream should be applied once daily to the affected and immediate surrounding area. Treatment should be continued for two weeks in order to reduce the possibility of recurrence. Patients with tinea pedis require six weeks of treatment.

Seborrhoeic dermatitis: Ketoconazole Cream should be applied to the affected area once or twice daily depending on the severity of infection. Treatment should be continued for a sufficient period, at least until a few days after disappearance of all symptoms.

[edit] CONTRAINDICATIONS

hypersensitivity to the active or excipient ingredients

[edit] PRECAUTIONS

If a reaction suggesting sensitivity or chemical irritation should occur, use of the medication should be discontinued.

[edit] PREGNANCY AND LACTATION

Pregnancy Category C (US). Ketoconazole should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Nursing Mothers: It is not known whether ketoconazole cream, administered topically could result in sufficient systemic absorption to produce detectable quantities in breast milk. Nevertheless, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.

[edit] SIDE EFFECTS

Erythema, pruritus or skin burning sensation may occur.

[edit] RELATED LINKS

Azoles mechanism of action
Skin Fungal Infections (Thrush, Tinea versicolor, ringworm...)

[edit] BIBLIOGRAPHY

[edit] REFERENCES

Antifungals
Ergosterol target : Cell membrane target Azoles (lanosterol 14 alpha-demethylase inhibitors) : Ergosterol inhibitors Imidazoles Topical: Bifonazole   Clotrimazole   Econazole   Fenticonazole   Ketoconazole   Isoconazole   Miconazole   Sertaconazole   Tioconazole
Triazoles Topical: Fluconazole   Terconazole
Systemic: Fluconazole   Itraconazole   Posaconazole   Voriconazole
Polyene antimycotics (ergosterol binding; they form pores in the membrane) Topical: Nystatin
Systemic: Amphotericin B
Allylamines (squalene epoxidase inhibitors) : Ergosterol inhibitors Topical: Amorolfine   Naftifine   Terbinafine
Systemic: Terbinafine
Echinocandins (β-glucan synthase inhibitors) : Cell wall target Anidulafungin   Caspofungin   Micafungin
Pyrimidine analogues / Thymidylate synthase inhibitors : Nucleic acid inhibitors Flucytosine
Mitotic inhibitors Griseofulvin
Others Ciclopirox