Source: Medicines & Healthcare Products Regulatory Agency (GB) Revision Year: 2018 Publisher: Janssen-Cilag Ltd, 50-100 Holmers Farm Way, High Wycombe, Buckinghamshire, HP12 4EG, UK
Pharmacotherapeutic classification: Anti-infectives and antiseptics, excl. combinations with corticosteroids, imidazole derivatives
ATC code: G01AF04
Miconazole combines a potent antifungal activity against common dermatophytes and yeasts with an antibacterial activity against certain gram-positive bacilli and cocci.
Miconazole inhibits the biosynsthesis of ergosterol in fungi and changes the composition of other lipid components in the membrane, resulting in fungal cell necrosis.
In general, miconazole exerts a very rapid effect on pruritus, a symptom that frequently accompanies dermatophyte and yeast infections.
Miconazole persists in the vagina for up to 72 hours after a single dose. Systemic absorption of miconazole after intravaginal administration is limited, with a bioavailability of 1 to 2% following intravaginal administration of a 1200 mg dose. Plasma concentrations of miconazole are measurable within 2 hours of administration in some subjects, with maximal levels seen 12 to 24 hours after administration. Plasma concentrations decline slowly thereafter and were still measurable in most subjects 96 hours post-dose. A second dose administered 48 hours later resulted in a plasma profile similar to that of the first dose.
Absorbed miconazole is bound to plasma proteins (88.2%) and red blood cells (10.6%).
The small amount of miconazole that is absorbed is eliminated predominantly in faeces as both unchanged drug and metabolites over a four-day post-administration period. Smaller amounts of unchanged drug and metabolites also appear in urine. The apparent elimination half-life ranges from 15 to 49 hours in most subjects and likely reflects both absorption from the site of application and metabolism/excretion of the drug.
Preclinical data reveal no special hazard for humans based on studies of local irritation, single and repeated dose toxicity, genotoxicity, and toxicity to reproduction.
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