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Ciclopirox Olamine: A Review

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eMediNexus    06 June 2020

An article published in the Indian Dermatology Online Journal stated that injudicious use of antifungals, indiscriminate use of corticosteroids for instant relief, persistence of predisposing factors like sweat retention and uncontrolled diabetes, and emerging resistance to antifungals across the globe have rendered the management of superficial cutaneous mycoses highly complicated and challenging.

The authors stated that ciclopirox – a hydroxypyridone, is an efficacious, versatile and safe topical antifungal agent. This drug was approved by the US-FDA in June 2004, and displays an array of beneficial properties over most other topical antifungals.

Ciclopirox – a prototype of hydroxypyridones, are the class of topical antifungal agents that acts through the chelation of polyvalent metal cations, such as ferric (Fe3+) and aluminum (Al3+). This leads to the inhibition of metal-dependent enzymes—cytochromes, catalase and peroxidase—resulting in the disruption of cellular activities, such as mitochondrial electron transport processes, energy production and nutrient intake across cell membrane. Furthermore, the drug is known to alter membrane permeability causing blockage of intracellular transport of precursors. Other postulated mechanisms of action of ciclopirox are – disruption of DNA repair, cell division signals and disorganization of internal structures (mitotic spindles) of the fungi; compromising the integrity of the cell membrane of susceptible organisms, followed by leakage of potassium ions and other intracellular material; and inhibitory effect on secreted aspartyl proteinases, important virulence factors for several types of C. albicans infections that favor the adhesion of the yeast to epithelial cells—in the action against mucosal candidiasis.

Ciclopirox olamine exhibits broad-spectrum antimycotic activity and inhibits nearly all clinically relevant dermatophytes, yeasts and molds, including certain frequently azole-resistant Candida species, such as Candida glabrata and Candida krusei. This agent expresses both, fungistatic and fungicidal activities, depending on the concentration and the duration of contact with target organisms. Its unique mechanism of action involves in vitro and in vivo actions of broad-spectrum antimycotic coverage, along with anti-bacterial and anti-inflammatory activity.

Ciclopirox can be used as an ideal topical antifungal for the management of treatment-refractory dermatophytic infections, tinea incognito, mixed infections and recurrent vulvovaginal candidiasis (VVC). For yeasts – 14 strains of Candida, and nondermatophyte molds – nine strains, this agent has been found to be the most potent with lowest minimum inhibitory concentration (MIC) values, compared to other antifungal agents. The drug has also demonstrated low MIC values and high clinical efficacy against Malassezia globosa and Malassezia restricta – the predominant species involved in pityriasis versicolor and seborrheic dermatitis. In addition, ciclopirox displays inhibitory effect over Saccharomyces cerevisiae, as well as some Aspergillus and Penicillium species, despite the higher MIC values of certain strains of aspergilli, relative to dermatophytes.

Ciclopirox has well-established safety, excellent tolerance and renders no drug resistance, conferring an extremely low predilection for the development of resistance. The drug is relatively inexpensive and has anti-inflammatory effect, which accounts for its great potential to be used as a single-agent, nonsteroidal preparation even for inflamed tinea. The use of this agent can curtail the generalized trend of inappropriate prescribing behavior—of corticosteroids for symptomatic relief of pruritus—and help in a reduction in the incidence of cases of dermatophytosis worsened due to steroids. Hence, ciclopirox can be instrumental in controlling steroid-abuse and the management of treatment-refractory dermatophytic infections, tinea incognito, mixed infections and recurrent VVC.

Source: Indian Dermatology Online Journal. 2019 Jul-Aug; 10(4): 481–485. doi: 10.4103/idoj.IDOJ_29_19

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