Isoconazole nitrate: a unique broad‐spectrum antimicrobial azole effective in the treatment of dermatomycoses, both as monotherapy and in combination with corticosteroids

Abstract

Fungal skin infections, or dermatomycoses, are associated with a broad range of pathogens. Involvement of gram-positive bacteria is often suspected in dermatomycoses. Inflammation plays an important role in dermatomycoses, displaying a close association between frequent inflammation and reduced skin-related quality of life. Isoconazole nitrate (ISN) is a broad-spectrum antimicrobial agent with a highly effective antimycotic and gram-positive antibacterial activity, a rapid rate of absorption and low systemic exposure potential. ISN is effective against pathogens involved in dermatomycoses, with minimum inhibitory concentrations well below the concentration of ISN in skin and hair follicles. The combination of the corticosteroid diflucortolone valerate with ISN (Travocort) increases the local bioavailability of ISN. Compared with ISN monotherapy, Travocort has a faster onset of antimycotic action, faster relief of itch and other inflammatory symptoms, improved overall therapeutic benefits and earlier mycological cure rate. Travocort is effective in the treatment of inflammatory mycotic infections, and also in the eradication of accompanied gram-positive bacterial infections. The rapid improvement observed with Travocort treatment, combined with favourable safety and tolerability, results in higher patient satisfaction, and therefore, can be an effective tool to increase treatment adherence in patients with dermatomycoses accompanied by inflammatory signs and symptoms.

Skin permeation of econazole nitrate formulated in an enhanced hydrophilic multiple emulsion

“…Equivalent results against C. glabrata (solution and creams) can be probably due to its comparatively lower sensitivity to econazole in comparison with C. albicans and C. parapsilosis . It also happens with other imidazolic antifungals such as isoconazole, where C. glabrata exhibits also the highest MIC value of the group . Thus, at higher concentrations, the effect of opalescence of the sample would not be relevant.…”

“…In case of highly lipophilic drugs, their apparent accumulation in the SCR suggests that the hydrophilic skin region presents the main barrier to permeation . In fact, when applied topically, skin concentrations of imidazolic drugs are relatively long‐lasting, remaining for up to some days after the last application . This is clinically relevant for cases where a long‐lasting therapeutic effect beyond the application time is required; for example, to prevent re‐infection .…”

“…62 In fact, when applied topically, skin concentrations of imidazolic drugs are relatively long-lasting, remaining for up to some days after the last application. 58 This is clinically relevant for cases where a long-lasting therapeutic effect beyond the application time is required; for example, to prevent re-infection. 63 Although, given that in vitro permeation from the multiple emulsion results to be clearly higher, similar results are expectable also in vivo, with a higher penetration rate of drug into the skin.…”

Preparation of alginate–chitosan–cyclodextrin micro- and nanoparticles loaded with anti-tuberculosis compounds

“…As antimycotic, ISN is active against dermatophytes, moulds, yeast, and yeast-like fungi. It is also active against Corynebacterium minutissimum , the microorganism causing erythrasma [21–22]. In addition to this, ISN has an antibacterial effect against gram-positive bacteria ( B. cereus, C. tuberculostearicum , S. aureus MR, S. haemolyticus, S. hominis, and S. salivarius ) confirmed by numerous reports on its antibacterial activity [21–25].…”

Continuous photochemical benzylic bromination using in situ generated Br2: process intensification towards optimal PMI and throughput

“…1a). 23 In particular, vilanterol is an important molecule, used in three inhaled combination therapies marketed by GlaxoSmithKline. 24 In reactions of this specific substrate, dibromination was not observed, likely due to the steric hindrance imparted by two chlorine atoms flanking the reactive benzylic position.…”