Disease relevance of terconazole

• Terconazole has a high topical in vivo activity against vaginal candidosis in rats and against dermatophytosis in guinea pigs [1].
• Comparison of 0.8% and 1.6% terconazole cream in severe vulvovaginal candidiasis [2].
• The in vitro activity of terconazole against yeasts: its topical long-acting therapeutic efficacy in experimental vaginal candidiasis in rats [3].
• Because both chitin and ergosterol are critical components of the fungal cell, perturbation of the production and localization of these components by terconazole is likely to contribute to the selective toxicity of this compound for C. albicans and other fungi [4].
• Patients were initially treated for a symptomatic episode of candidal vaginitis and then started on weekly applications of terconazole 0.8% cream for 26 weeks [5].

High impact information on terconazole

• However, these relationships were not always noted with other Candida spp.: in particular, the growth of C. glabrata and C. parapsilosis isolates tended to be greater at 37 degrees C than at 25 degrees C in the presence of the azole-derivative antifungal agents itraconazole and terconazole [6].
• The inhibitory potency of terconazole on yeast cell viability varied with the strain and species of Candida tested [7].
• This study further characterizes the effects of terconazole in vitro on yeast cell growth, viability, and morphology [7].
• Therefore, the PASCO method is a suitable alternative procedure for the testing of the antifungal susceptibilities of the medically important Candida spp. and C. neoformans against a range of antifungal agents with the exceptions only of miconazole and clotrimazole and of terconazole against C. krusei isolates [8].
• Selective inhibition of 14 alpha-desmethyl sterol synthesis in Candida albicans by terconazole, a new triazole antimycotic [9].

Chemical compound and disease context of terconazole

• The anti-inflammatory activities of eight anti-fungal agents (butoconazole, ciclopirox olamine, fluconazole, miconazole nitrate, sertaconazole nitrate, terconazole, tioconazole and ketoconazole) were compared in a number of preclinical models of dermal inflammation and pruritus [10].
• Single dose oral fluconazole vs intravaginal terconazole in treatment of Candida vaginitis. Comparison and pilot study [11].

Biological context of terconazole

• These data indicate a species specificity for the biochemical actions of terconazole [9].
• Terconazole stimulated incorporation of 14C-acetate into triglycerides, but had no other effect on C. albicans lipid metabolism [9].

Anatomical context of terconazole

• Furthermore, terconazole reduced cytochrome P-450 levels in yeast microsomes at concentrations 10,000-fold below those at which it showed effects on rabbit liver microsomes [9].

Associations of terconazole with other chemical compounds

• In fact, for each individual isolate the minimum inhibitory concentration of terconazole was consistently lower than that of fluconazole [12].
• We investigated the in vitro activity of terconazole, miconazole, and clotrimazole, against 94 clinical isolates of Candida spp.: C. albicans (n = 68), C. tropicalis (n = 18), and C. parapsilosis (n = 8) [13].
• In particular, the in vitro potency of fluconazole and terconazole against species other than C. albicans was relatively poor, whereas the drugs demonstrating the best activity were itraconazole, butoconazole and saperconazole [14].
• The clinical efficacy of terconazole (triaconazole), a new triazole ketal structurally similar to ketoconazole, was evaluated in a single-blind, randomized comparative clinical trial including 60 patients with symptoms and clinical signs of vulvovaginal candidosis confirmed by microscopic examination and positive culture for Candida albicans [15].

Gene context of terconazole

• The high affinity and selectivity of terconazole for fungal cytochrome P-450 and its potent in vitro and in vivo activity indicate that the drug may well become a significant agent for the treatment of fungal disease [16].

Analytical, diagnostic and therapeutic context of terconazole

• The effects of terconazole on the morphology of yeast cells (grown on Eagle minimum essential medium) were shown by phase-contrast and electron microscopy [7].
• In double-blind, multicenter studies conducted in the United States, clinical cure rates for 0.4% terconazole cream ranged from 86% to 96% and microbiologic cure rates from 77% to 91% at 8 to 10 days after therapy [17].
• The results of several European clinical trials have shown both terconazole cream and suppositories to be effective and safe in the treatment of vulvovaginal candidiasis [2].
• We conducted a comparative placebo-controlled, double-blind study of 0.8 and 1.6% terconazole creams in a group of patients with persistent vulvovaginal candidiasis [2].
• The activity of the broad-spectrum triazole antifungal terconazole was evaluated in vitro by the serial decimal dilution technique in broth media [3].

References