Chemical formula: C₁₈H₁₄Cl₄N₂O Molecular mass: 416.129 g/mol PubChem compound: 4189
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 is systemically absorbed after administration as the oral gel. Administration of a 60 mg dose of miconazole as the oral gel results in peak plasma concentrations of 31 to 49 ng/mL, occurring approximately two hours post-dose.
There is little absorption through skin or mucous membranes when miconazole nitrate is applied topically.
Absorbed miconazole is bound to plasma proteins (88.2%), primarily to serum albumin and red blood cells (10.6%).
The absorbed portion of miconazole is largely metabolized; less than 1% of an administered dose is excreted unchanged in the urine. The terminal half-life of plasma miconazole is 20 to 25 hours in most patients. The elimination half-life of miconazole is similar in renally impaired patients. Plasma concentrations of miconazole are moderately reduced (approximately 50%) during hemodialysis. About 50% of an oral dose may be excreted in the faeces partly metabolized and partly unchanged.
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 conventional studies of local irritation, single and repeated dose toxicity, genotoxicity, and toxicity to reproduction.
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