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Query: CAS:65899-73-2 (Tioconazole)
 23 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Tioconazole (UK-20,349), a new antifungal imidazole derivative, was compared with miconazole for activity in vitro against Candida spp., Torulopsis glabrata, Cryptococcus neoformans, Aspergillus spp., and dermatophyte fungi (Trichophyton spp. and Microsporum spp.). Tioconazole was more active than miconazole against all the fungal species examined except Aspergillus, against which both agents showed similar activity. Both tioconazole and miconazole inhibited the growth of all fungi examined at concentrations well below their quoted minimum inhibitory concentrations. Their activity against fungi in vivo was investigated in mice infected systemically with Candida albicans. Both agents significantly reduced the numbers of viable Candida cells recoverable from the kidneys of infected animals, with tioconazole producing a generally more marked reduction. After administration of a single oral dose (25 mg/kg) to beagle dogs or white mice, higher and more sustained circulating levels of bioactive drug were detectable of tioconazole than of miconazole. These observations suggest that tioconazole may have potential in the treatment of both superficial and systemic mycoses in humans.
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PMID:Antifungal activity of tioconazole (UK-20,349), a new imidazole derivative. 46 92

Tioconazole is a substituted imidazole antimicrobial agent structurally related to other drugs in this group. It has been shown to have a broad spectrum of activity in vitro against dermatophytes and yeasts, as well as against some chlamydia, trichomonads and Gram-positive bacteria. Both open and controlled clinical trials have clearly demonstrated the efficacy and safety of topical preparations of tioconazole for treating superficial dermatophyte or yeast infections of the skin and vaginal candidiasis. In comparative studies it was at least as effective as alternative imidazole antifungal drugs, and in a few trials significantly greater efficacy has been reported for tioconazole, compared with clotrimazole, miconazole, econazole and systemic ketoconazole. Preliminary studies in other clinical areas suggest tioconazole may be useful for treating onychomycosis (in a special nail formulation), napkin-rash due to Candida albicans, impetigo, and vaginal trichomoniasis, although comparative studies are needed in each of these settings to clearly assess its relative place in therapy. Thus, tioconazole is an effective and well tolerated treatment for vaginal candidiasis and superficial fungal infections of the skin.
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PMID:Tioconazole. A review of its antimicrobial activity and therapeutic use in superficial mycoses. 351 Jan 14

Tioconazole, an imidazole antifungal agent, was administered orally at 100 mg/kg/day to pregnant rats according to two regimens; in one, treatment started on day 15 post-insemination (p.i.) and in the other it started on day 18 p.i. The first regimen caused a delay in onset of parturition and a prolongation of labour. Serum progesterone was decreased from days 17 to 21 p.i., 17 beta-oestradiol decreased on day 21 p.i., LH increased on day 17 p.i., and the normal surge of prolactin on day 21 p.i. abolished. The parturition disorders disappeared when 17 beta-oestradiol (0.125 microgram/animal/day s.c.) was given with tioconazole from day 15 p.i. In the second regimen, tioconazole treatment advanced by about 24 hours the onset of parturition and the normal fall in serum progesterone and the surge in prolactin. Serum 17 beta-oestradiol was unaffected, but LH was raised on days 19 and 20 p.i. In animals receiving progesterone (2.5 mg/animal/day, s.c.) and tioconazole from day 18 p.i. parturition was no longer advanced. In conclusion, the parturition disorders observed in rats during tioconazole treatment are associated with a modification of progesterone and 17 beta-oestradiol serum levels. These findings have questionable relevance for the human situation as the roles of these steroid hormones in parturition in women are different from those in rats.
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PMID:Effects of tioconazole on parturition and serum levels of 17 beta-oestradiol, progesterone, LH and PRL in the rat. 356 6

An eight-week comparative study of tioconazole and clotrimazole was carried out in 32 patients with tinea versicolor. Sixteen patients were treated with 1% tioconazole lotion and 16 with 1% clotrimazole solution; each drug was applied twice daily for 28 days. Clinical and mycological direct examinations were performed before treatment and on days 7, 14, and 28 of therapy. All patients underwent overall clinical evaluation 30 days posttreatment. At the end of the study, all patients were clinically and mycologically cured. During the second week of treatment, however, a significant remission in rash (P less than 0.05) was observed in the group treated with tioconazole. None of the treated patients had adverse reactions. Tioconazole is a new imidazolic agent with an intense fungicidal action. It has been found to be effective and safe and is an agent of choice for treating tinea versicolor.
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PMID:Comparative study of tioconazole and clotrimazole in the treatment of tinea versicolor. 360 17

The antimicrobial activity of 8 antifungal agents have been compared in vitro against 151 strains of yeast fungi and 2 of Geotrichum candidum. The drugs were the classical nystatin and amphotericin-B, 5-flucytosine, and 5 imidazoles, clotrimazole, econazole, ketoconazole, miconazole, and tioconazole. An agar dilution technique with incubation at 37 degrees C was used. By this procedure, econazole was the most active agent per weight basis among those suitable for topical therapy. Tioconazole had a wide spectrum and high activity. Ketoconazole had an antimicrobial activity which makes it an interesting agent considering its applicability in systemic therapy. The activity of 5-flucytosine surpasses that of other systemically applicable agents.
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PMID:In vitro activity of antifungal agents against yeast species. 630 73

A total of 60 patients with proven fungal infection of the skin took part in a single-blind comparative study of the efficacy, toleration and safety of tioconazole base 1% w/w and miconazole nitrate 2% creams applied twice daily for 14 days to patients with pityriasis versicolor and for 28 days to patients with dermatophyte and yeast infections. Overall assessment of the patients reviewed at the end of treatment showed that 23 of 30 patients (77%) treated with tioconazole and 19 of 30 patients (63%) treated with miconazole were clinically and mycologically cured. Tioconazole cured 80% (8 of 10) and miconazole cured 38% (5 of 13) of the infections with Trichophyton rubrum, which are the most frequent ones. At long-term follow-up, approximately 6 weeks later, results in both treatment groups were comparable. 20 of the 23 patients (87%) cured by tioconazole and 18 of the 19 patients (95%) cured by miconazole remained free from infection. Both creams were easy to apply and there were no reports of staining. No side effects were recorded during the study.
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PMID:Treatment of dermatomycoses with topical tioconazole and miconazole. 635 71

Tioconazole is a new imidazole antifungal agent with broad-spectrum activity. Its in vitro activity against common dermal pathogens is generally better than miconazole by a factor of 2-8. This activity is paralleled by good topical efficacy in a guinea pig dermatomycosis model. Pharmacokinetic studies in animals have demonstrated minimal systemic exposure following dermal application. Acute general pharmacology studies have shown that the compound is well tolerated in animals and unlikely to produce side-effects in man.
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PMID:Tioconazole, a new imidazole-antifungal agent for the treatment of dermatomycoses. Antifungal and pharmacologic properties. 688 59

In 32 studies involving 1,304 patients tioconazole 1% dermal cream has been shown to be effective and safe in the treatment of a wide variety of superficial fungal infections of the skin and erythrasma. Tioconazole cream is more effective than miconazole nitrate 2% cream in the treatment of pityriasis versicolor and in infections with Trichophyton rubrum and Trichophyton mentagrophytes which cause 70% of dermatophyte infections in man. Data from comparisons with econazole and clotrimazole are too few to allow conclusions to be drawn on relative efficacy. All the creams were easy to apply and there were no serious adverse reactions, local or systemic.
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PMID:Tioconazole in the treatment of fungal infections of the skin. An international clinical research program. 688 60

In vitro assays demonstrated that clinical yeasts were significantly more inhibited by tioconazole (MIC50, < or = 0.5 microgram/ml) than by fluconazole (MIC50, 8 micrograms/ml). Tioconazole also exhibited high potency against most molds (Alterneria spp. and Acremonium spp.). All Candida tropicalis isolates had MICs of 8 micrograms/ml, four-fold greater than any other Candida spp. Generally Gram-negative bacteria were less susceptible to tioconazole. Moraxella catarrhalis (MIC90, 2 micrograms/ml) was the most susceptible Gram-negative species. Staphylococci and enterococci were the most susceptible to tioconazole Gram-positive species (MIC50s, 1-8 micrograms/ml). Bacterial species associated with vaginosis. [Gardnerella vaginalis (MIC90, 16 micrograms/ml), Mobiluncus spp. (MIC90, 16 micrograms/ml) and Prevotella biviadisiens (MIC90, 64 micrograms/ml)] were inhibited by tioconazole. Isolates of Lactobacillus spp. were most resistant (MIC90, > or = 256 micrograms/ml) to tioconazole. Vaginal fluid levels of tioconazole (mean, 91.4 micrograms/ml) persisted above the MIC90 levels (1-64 micrograms/ml) for most fungal and bacterial pathogens for 72 h in 19 evaluable female human subjects receiving 300 mg tioconazole in an intravaginal ointment.
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PMID:In vitro antimicrobial activity of tioconazole and its concentrations in vaginal fluids following topical (vagistat-1 6.5%) application. 835 5

Crude ethanol and water extract of leaves and barks from Cassia alata were tested in vitro against fungi, (Aspergillus fumigatus and Microsporum canis), yeast (Candida albicans) and bacteria (Staphylococcus aereus and Escherichia coli). C. albicans showed concentration-dependent susceptibility towards both the ethanol and water extracts from the barks, but resistant towards the extracts of leaves. The degree of susceptibility varied, the water extract from barks showed bigger inhibition zone than the ethanol extracts (12-16 and 10-14 mm, diameter respectively). The growth of Aspergillus fumigatus and Microsporum canis were not affected by all types of the plant extracts. Results were comparable to standard antifungal drug Tioconazole (18 mm diameter) at equivalent concentration. The anti-bacterial activity of C. alata extracts on S. aureus was detected with only the leaves extracts using water and ethanol. The water extract exhibited higher antibacterial activity than the ethanol extract from leaves (inhibition zones of 11-14 and 9-11 mm, respectively). E. coli showed resistance to all types of extracts. Based on the current findings, it can be concluded that this plant has antimicrobial activity, which is as potent as standard antimicrobial drugs against certain microorganisms.
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PMID:In vitro antimicrobial activity of ethanol and water extracts of Cassia alata. 1249 68


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