A Comprehensive Monograph on Miconazole (DB01110)

Executive Summary & Overview

Miconazole is a first-generation synthetic imidazole derivative that has been a cornerstone of antifungal therapy for over five decades. First synthesized in 1969 by Janssen Pharmaceutica and granted its initial U.S. Food and Drug Administration (FDA) approval in 1974, miconazole established itself as a broad-spectrum agent with potent activity against a wide range of dermatophytes, yeasts, and other fungi.[1] Its clinical history is marked by a profound dichotomy that defines its modern therapeutic role: it is both a widely available, highly effective, and exceptionally safe over-the-counter (OTC) topical medication, and a potent inhibitor of key metabolic enzymes, which imparts a significant risk of systemic drug-drug interactions when absorbed.

This monograph will explore in detail the fundamental principle that the entire clinical profile of miconazole—from its therapeutic applications and efficacy to its safety and tolerability—is inextricably linked to its formulation and route of administration. The drug's inherent physicochemical properties, particularly its high lipophilicity and poor aqueous solubility, have driven the development of localized delivery systems (creams, powders, suppositories, buccal tablets) that maximize its effect at the site of infection while minimizing systemic exposure. This targeted approach is the key to its success as a topical agent.