Bifonazole is a broad spectrum imidazole antifungal drug that has been in use since 1983 for topical fungal infections and in particular tinea pedis. It is available under several brand names as a 1% topical ointment.
Mechanism of action:
Inhibits the fungal ergosterol biosynthesis via the transformation of 24-methylendihydrolanosterol to desmethylsterol. Ergosterol is an essential component of fungal cell membranes. The uptake of bifonazole into the fungal cells peaks after 20 – 30 mins and remains there for up to 120 hours so it can continuously inhibit the ergosterol biosynthesis.
Also inhibits HMG-CoA.
Pharmacokinetics:
<1% absorbed following topical administration.
Half-life: 1-2 hours
Bioavailability: unknown
Metabolism: unknown
Excretion: unknown
Adverse effects:
Burning, irritation, itching sensations and redness at the site of application
Contraindications:
Allergy or hypersensitivity to bifonazoles.
Tube label of Canesten (Bifonazole) used in Australia
Dosage:
Applied once daily (advantage over other anti-fungal drugs that need to be applied twice or more a day; increases compliance).
Precautions:
Pregnancy: there is no clinical data. High oral doses in animals have shown reproductive toxicity.
Bayer use these cautions on their packaging for the Canesten brand of bifonazole:
Do not use in the eyes
Not recommended for babies except under medical supervision
Consult your pharmacist or doctor for advice before treating yourself if you are pregnant or breastfeeding
Interactions:
Limited data suggests that the warfarin serum concentration may increase with use of bifonazole, so use with careful monitoring (especially if bifonazole is used under occlusion).
Brand names: Canespor (Bayer); Amycor (Merck); Canesten (Bayer); Amycor (Lipha); Azolmen (Menarini); Bedriol (Andromaco); and others
Chemical formula: C22H18N2
Systematic name: 1-[phenyl-(4-phenylphenyl)methyl]imidazole
Other anti-fungal drugs:
| Antibiotics | Polyenes: | Nystatin | Amphotericin B | Hamycin | |
| Heterocyclic benzofuran: | Griseofulvin | ||||
| Echinocandins: | Caspofungin | Micafungin | Anidulafungin | ||
| Azoles: | Imidazoles: | Topical: | Clotrimazole | Econazole | Miconazole |
| Bifonazole | |||||
| Systemic: | Ketoconazole | ||||
| Triazoles: | Fluconazole | Itraconazole | Voriconazole | Posaconazole | |
| Efinaconazole | Fosravuconazole | ||||
| Morpholines: | Amorolfine | ||||
| Allylamines: | Terbinafine (oral) | Terbinafine (topical) | |||
| Other topical agents: | Tolnaftate | Benzoic acid | Butenafine | Sodium thiosulfate | Quiniodochlor |
| Undecylenic acid | Ciclopirox olamine | Gentian Violet |
In Australia, bifonazole is on the National Podiatry Scheduled Medicines List.
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