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Antimicrobials during Pregnancy
Published in “Bert” Bertis Britt Little, Drugs and Pregnancy, 2022
Ciclopirox is a topical antifungal agent used to treat various dermatophytes such as Trichophyton species and Candida albicans. No human pregnancy studies of this drug are published. Experimental animal studies (mice, rats, rabbits, monkeys) found no increased frequency of birth defects following oral administration using doses from 13–54 times the recommended human dose. It is a category B drug.
Topical Products Applied to the Nail
Published in Heather A.E. Benson, Michael S. Roberts, Vânia Rodrigues Leite-Silva, Kenneth A. Walters, Cosmetic Formulation, 2019
Apoorva Panda, Avadhesh Kushwaha, H.N. Shivakumar, S. Narasimha Murthy
Ciclopirox is an antifungal with a hydroxyl pyridone ring that is used in the treatment of nail infections. It is an antibacterial that acts by the inhibition of metal-dependence enzymes. Ciclopirox nail lacquer is often prescribed for use in the treatment of mild distal and lateral subungual onychomycosis (Shivakumar et al., 2012 ; Subissi et al., 2010). The nail lacquer needs to be applied daily for about 24 weeks in the case of nail infection and for 48 weeks in case of toe infections (Kushwaha et al., 2015). Ciclopirox nail lacquers available in the market are either conventional vinyl resin–based or hydroxypropyl chitosan–based (Kushwaha et al., 2015).
Ciclopirox
Published in M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson, Kucers’ The Use of Antibiotics, 2017
Ciclopirox is a synthetic hydroxypyridone, and ciclopirox olamine is the ethanolamine salt of ciclopirox. Its chemical name is the 2-aminoethanol salt of 6-cyclohexyl-1-hydroxy-4-methyl-2(1H)-pyridone; the chemical structure of ciclopirox is shown in Figure 164.1. Ciclopirox has a broad spectrum of antifungal activity with a distinct mechanism of action. It is used to treat a variety of fungal infections including tinea pedis, tinea corporis/cruris, pityriasis versicolor, onychomycosis, and seborrheic dermatitis.
Trends in onychomycosis prescribing: a single center retrospective study over 15 years
Published in Journal of Dermatological Treatment, 2022
Yu Wang, Solomon Geizhals, Shari R. Lipner
Onychomycosis prescribing practices changed significantly following FDA approvals of efinaconazole and tavaborole in 2014 (Table 1). From 2004 to 2013, prescriptions for ciclopirox 8% solution were 39 and 75, for IM and dermatology, respectively. Between 2014 and 2018, IM topicals were, ciclopirox 61 (61%), efinaconazole 37 (37%), tavaborole 2 (2%), and dermatology topicals, ciclopirox 118 (36.6%), efinaconazole 151 (46.9%) and tavaborole 53 (16.5%). Between 2004 and 2013, IM orals were, terbinafine 106 (92.2%), itraconazole 8 (6.9%), fluconazole 1 (0.87%), and dermatology, terbinafine 239 (88.2%), itraconazole 22 (8.1%), and fluconazole 10 (3.7%). From 2014-2018, oral IM prescribing was terbinafine 143 (95.9%), itraconazole 4 (2.68%), and fluconazole 2 (1.34%), while dermatology prescribing was, terbinafine 408 (93.6%), itraconazole 16 (3.67%) fluconazole 12 (2.75%).
Emerging drugs for the treatment of onychomycosis
Published in Expert Opinion on Emerging Drugs, 2019
Currently available topical treatments in North America are efinaconazole, tavaborole, and ciclopirox. Efinaconazole is a triazole that inhibits the synthesis of ergosterol in the fungal cell wall. Two phase III studies of infected patients with 20–50% nail involvement had patients treated once daily for 48 weeks and evaluated at 52 weeks. Complete cure rates were 17.8% and 15.2% and mycological cure rates were 55.2% and 53.4% [58]. Tavaborole is another option that relies on an oxaborole compound to penetrate the nail and inhibit the fungus at the point of the cytosolic leucyl-transfer RNA synthetase [25]. The mycological and complete cure rates come from two studies: mycological cure rates have been reported as 31.1% and 35.9%, whereas clinical cure was 6.5% and 9.1%. Both topical formulas were FDA-approved in 2014 for the treatment of onychomycosis [59,60]. Lastly, ciclopirox is an older topical option, approved in 1999 in the USA. Ciclopirox is a hydroxypyridone that chelates trivalent cations, inhibiting metal-dependent enzyme of the fungus cell membrane. Ultimately, it disrupts cellular respiration processes [61–63]. The mycological cure rates for toes are 29–36%, and complete cure is lower at 5.5–8.5%. The side effects of topical treatments are localized to the site of application and are milder, ranging from exfoliation, erythema, and dermatitis at the application site [64].
Hydroxypropyl chitosan nail lacquer of ciclopirox-PLGA nanocapsules for augmented in vitro nail plate absorption and onychomycosis treatment
Published in Drug Delivery, 2022
Eman Yahya Gaballah, Thanaa Mohammed Borg, Elham Abdelmonem Mohamed
Ciclopirox (CIX) is a FDA-approved broad-spectrum antimycotic that inhibits the metal-dependent enzymes in fungi that are responsible for the breakdown of toxic peroxides (Subissi et al., 2010). CIX nail lacquer (8%w/v) is widely used for nail fungal treatment (Subissi et al., 2010). However, the cost of treatment with CIX per patient cured (252 EURO) was greatly higher than other comparative antifungals commonly used for treatment of onychomycosis such as amorolfine (84 EURO) (Marty et al., 2005). Also, the complete cure may require treatment with CIX for one year or more (Piraccini et al., 2020). The lack of cost effectiveness and the long-term topical treatment may lead to the patient incompliance and the discontinuous treatment. The above-mentioned limitations of the topical therapy with CIX may necessitate a reduction in its dose and an improvement in its delivery and efficacy. This may require combining different strategies by utilization of a promising nanostructure as PNCs incorporated in a water-soluble nail lacquer to highly augment CIX efficacy. Therefore, the aim of this study was to prepare, characterize and optimize CIX-PNCs at a lower dose than that commonly used utilizing the biodegradable and biocompatible PLGA. This was followed by formulating the optimized PNCs into HPCH based nail lacquer to be assessed regarding the nail hydration and in vitro nail absorption of CIX in comparison with the drug solution (1%w/v). Also, the lacquer antifungal efficacy against Trichophyton rubrum was investigated through the evaluation of the effects on CIX minimum inhibitory concentration (MIC) and inhibition zone as well as via employing an ex vivo microbiological model.