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At least 19 recordsLinked to original sources
PubMed1991

Studies on the mode of action of tolnaftate in Microsporum gypseum.

Studies were performed on the mode of action of tolnaftate and resistance to this drug in Microsporum gypseum. Cells grown in the presence of tolnaftate (at the IC 50) showed a reduced content of total phospholipids and sterols whereas there was an increase in total RNA content. Incubation of cells with tolnaftate (at 10 x MIC), followed by addition of different macromolecule precursors revealed inhibition of the biosynthesis of all macromolecules except for RNA. The activity of membrane-bound enzymes did not change on treatment with tolnaftate (10 x MIC) whereas an increase in the leakage of intracellular 32P was observed. The content of total phospholipids was higher in tolnaftate-resistant cells, whereas the content of total sterols, DNA, RNA and protein was comparable to that of susceptible cultures. Activity of phosphodiesterase decreased and 5'-nucleotidase increased in tolnaftate-resistant cells. Our results suggest that the antifungal activity of tolnaftate is due to differential action on various targets site(s) which are modified in strains resistant to the drug.

DNA, Fungal↗
PubMed1978

Inhibition of aflatoxin biosynthesis by tolnaftate.

Tolnaftate [2-napthyl-N-methyl-N-(m-tolyl)thionocarbamate], an antifungal drug, is widely used to control superficial fungal infections in humans and other animals. In this study the effect of tolnaftate on aflatoxin biosynthesis by Aspergillus parasiticus NRRL 3240 was investigated. Tolnaftate changed the morphology of A. parasiticus to yeastlike forms and inhibited aflatoxin formation. The formation of aflatoxin G was blocked considerably, indicating a metabolic block in the conversion of aflatoxin B to aflatoxin G. The incorporation of [1-14C]acetate into aflatoxin was significantly inhibited at a concentration of 1 mM tolnaftate. The presence of zinc in the resuspension buffer resulted in reversal of the tolnaftate-induced inhibition of aflatoxin G1 biosynthesis.

Acetates↗
PubMed1993

A liquid chromatographic method for the determination of tolnaftate in pharmaceutical formulations.

A simple LC method was developed and validated for the analysis of tolnaftate in various pharmaceutical formulations. This method did not require any complex sample extraction procedure. The chromatographic separation was achieved on a reversed-phase, C18 column with UV detection at 258 nm. This isocratic system was operated at ambient temperature and required 9 min of chromatographic time. The mobile phase consisted of methanol-aqueous potassium dihydrogen phosphate solution (80:20, v/v) at a flow rate of 1.5 ml min-1. Standard curves were linear over the concentration range of 1.0-51.0 micrograms ml-1. Within-day and between-day relative standard deviation values ranged from 0.7 to 2.9% and from 1.3 to 3.4%, respectively. This method was used to quantify tolnaftate in microcapsule, microsphere, cream, powder, liquid, liquid aerosol and powder aerosol formulations. This method was also used to study the stability of tolnaftate in solution during its extraction from microcapsule formulations.

Aerosols↗
PubMedDate not supplied

The treatment of dermatophytoses of the glabrous skin: a comparison of undecylenic acid and its salt versus tolnaftate.

In a double-blind study, the efficacy of 1% tolnaftate cream, 3% undecylenic acid and its zinc salt, and a placebo cream were tested in dermatophytosis of the glaborous skin and groin. Ninety-seven subjects completed the study: 33 received tolnaftate, 23 of these subjects were cured clinically and mycologically. Thirty-two subjects received 3% undecylenic acid and 20% zinc undecylenate as a cream. Of these, 21 were cured clinically and mycologically. Only three of the 32 subjects receiving placebo were cured clinically and mycologically. Both tolnaftate and undecylenic acid and its zinc salt are effective in this condition.

Clinical Trials as Topic↗
PubMed1991

[Tolnaftate Reference Standard (Control 901) of National Institute of Hygienic Sciences].

The raw material of tolnaftate was examined for the preparation of the "Tolnaftate Reference Standard". Analytical data obtained were as follows: ultraviolet spectrum, lambda max = 257 nm; absorbance, E1cm1% (257 nm) = 723; infrared spectrum, same as that of USP Reference Standard of Tolnaftate; melting point, 112.1 degrees C; thin-layer chromatography, no impurities were detected until 500 micrograms; high-performance liquid chromatography, no impurities were detected; loss on drying, 0%; water, 0.01%; assay, 100.4% by absorbance method and 100.1% by the HPLC method in terms of the USP Reference Standard. Based on the above results, this raw material was authorized to be the Reference Standard of the National Institute of Hygienic Sciences.

Chromatography, High Pressure Liquid↗
PubMed1979

Comparison of in vitro activity of undecylenic acid and tolnaftate against athlete's foot fungi.

Undecylenic acid and tolnaftate were tested in an in vitro test system to evaluate their relative "killing time" efficacy against Trichophyton mentagrophytes, Trichophyton rubrum, and Epidermophyton floccosum. Commercial products containing these active agents were tested similarly. The pure active agents were equivalent in activity. The commercial product containing undecylenic acid appeared to be more effective against the test organisms than did the product containing tolnaftate.

Epidermophyton↗
PubMed1986

The mode of antifungal action of tolnaftate.

The anti-dermatophyte agent tolnaftate was compared with the allylamine antifungal compounds naftifine and terbinafine. Tolnaftate was shown to inhibit sterol biosynthesis at the level of squalene epoxidation and squalene was shown to accumulate in dermatophytes grown in its presence. Biochemical studies in whole and broken cells supported this conclusion and showed that the compound was active against squalene epoxidation in broken C. albicans cells, but was much less potent against whole cells. These results suggested there was a barrier to penetration in these yeasts.

Allylamine↗
PubMed1986

Ergosterol biosynthesis inhibition by the thiocarbamate antifungal agents tolnaftate and tolciclate.

The thiocarbamate antimycotics tolnaftate and tolciclate blocked sterol biosynthesis in fungal cells and cell extracts, with accumulation of squalene. This point of action was confirmed by the direct inhibition of microsomal squalene epoxidase from Candida albicans. There was no inhibition of other steps in ergosterol biosynthesis. In whole Candida cells, ergosterol biosynthesis inhibition was not complete at drug concentrations up to 100 mg/liter, whereas full inhibition occurred in a cell-free test system. Rat liver cell-free cholesterol biosynthesis was much less sensitive to the drugs. The biochemical action of tolnaftate and tolciclate is thus similar to that of the allylamine antimycotics naftifine and terbinafine.

Acetates↗
PubMed1965

Tolnaftate (tinactin), a new topical antifungal agent.

Using the double-blind technique, patients with tinea pedis, tinea cruris and tinea corporis were treated with either (a) 1% tolnaftate in a cream base or (b) the cream base.Twenty-four of 29 patients (82.7%) using 1% tolnaftate cream demonstrated clearing or great improvement of their lesions after three weeks of therapy, whereas only two of nine (22.2%) had similar results using the placebo.

Antifungal Agents↗
PubMed1983

Treatment of onychomycosis by ODT therapy with 20% urea ointment and 2% tolnaftate ointment.

20 patients with distal onychomycosis were given daily application of an ointment containing 2% tolnaftate and an ointment containing 20% urea under ODT. Following this, 17 of 20 patients developed onychomalacia and seven of these developed onycholysis 1 or 2 weeks later. The separated nails were cut as short as possible. Similarly to those patients with onychomalacia alone, occlusive dressing technique was continuously performed until the newly developed nails became macroscopically normal and no fungi were observed microscopically (responders). Following treatment, out of 20 patients, 14 responded. 5 patients who had a short course of treatment did not respond. Side-effects such as pain, hemorrhage and infection did not occur.

Administration, Oral↗
PubMed1998

Enhancing effect of N-acetyl-l-cysteine or 2-mercaptoethanol on the in vitro permeation of 5-fluorouracil or tolnaftate through the human nail plate.

The enhancing effects of various vehicles on the in vitro permeation of a hydrophilic model drug, 5-fluorouracil (5-FU), or a lipophilic model drug, tolnaftate (TN), through human nail plates were investigated using a modified side-by-side diffusion cell. Tip pieces from the 5th finger-nail, clipped from healthy volunteers, were used in this permeation study. The swelling and softening properties of the nail pieces were also measured in each vehicle. The weights and stresses of the nail pieces were dramatically changed after immersion in aqueous solvents containing N-acetyl-L-cysteine (AC) or 2-mercaptoethanol (ME). However, no significant change in the physicochemical properties of the nail pieces was found in the lipophilic vehicles. Thus, the water content in the nail plates absorbed from vehicles may relate to their physicochemical properties. Although keratin-softening agents and new skin permeation enhancers did not significantly promote 5-FU permeation compared with water alone, the flux from solvent systems containing AC or ME was substantially higher. In addition, TN permeation from solvents containing AC or ME could be measured, whereas that from other solvents was undetectable. When the AC concentration was increased, the 5-FU permeation and the nail weight increased and the stress of each nail piece decreased. It is concluded from these experimental results that AC and ME may be useful as enhancers for increasing drug permeation through the human nail plate.

Absorption↗
PubMedDate not supplied

Liquid chromatographic determination of tolnaftate in commercial products.

A liquid chromatographic (LC) method for the determination of the antifungal agent tolnaftate was developed. Isolation of the analyte was achieved by direct extraction or dilution with acetonitrile-water (80 + 20) followed by reverse-phase liquid chromatography using a C18 column. The mobile phase was acetonitrile-water (80 + 20) acidified with phosphoric acid. Detection was by UV absorption at a wavelength of 257 nm. The proposed procedure was applied to 20 consumer products comprising 6 formulation types, including solutions, powders, liquid and power aerosols, creams, and gels. The precision (RSD) for the products ranged from 0.23 to 1.16% (n = 5), and recoveries via fortification ranged from 98.1 to 103.0%. Six different brands of C18 columns were evaluated for use with the method. The overall simplicity and versatility of the method suggest possible adaptations to both regulatory and quality-control situations.

Chemistry, Pharmaceutical↗
PubMed1979

[The role of ointment bases in the formulation of 2 antifungal drugs. II. Liberation studies on 5-fluorocytosine and tolnaftate ointment bases by the microbiological agar plate method].

In this study a microbiological in vitro agar plate method was developed to measure the liberation of two antifungal agents; 5-Fluorocytosine and Tolnaftate; comparatively from six different type ointment bases. The effect of dimethylformamide to the liberation of these two antifungals was also studied. Cetyl alcohol ointment and Emulsion ointment (B.P. 1968) bases gave the best results for the two active agents. Dimethylformamide accelerated the release of these antifungals from the emulsion type bases (Emulsion Ointment and Simple Ointment).

Chemistry, Pharmaceutical↗
PubMed1980

Comparison between undecylenic acid and tolnaftate in the treatment of tinea pedis.

A double-blind parallel study comparing tolnaftate cream with undecylenic acid ointment and a placebo ointment in the treatment of symptomatic tinea pedis was conducted on the warm, humid Texas Gulf Coast. In one hundred and three patients studied, both the clinical and mycological effects of the two antifungal agents were indistinguishable. Both were significantly more effective than the placebo.

Clinical Trials as Topic↗
PubMed1978

[Comparative studies on Bi-Nerisona cream (diflucortolone valerinate + chlorquinaldol) and on a combination preparation (betamethasone valerinate + gentamicin + tolnaftate + clioquinol) in a double-blind trial].

Bi-Nerisone cream and a control preparation, also in the form of a cream, have been clinically tested on 343 patients by means of a double blind study. Equilvalent results were obtained without registering any significant statistical differences, a finding, however, proving to be of great importance as Bi-Nerisone only contains two active substances (Diflucortolone valerat + Chlorquinaldol), whereas the control preparation contains a total of four (Betamethasone valerate + Gentamycin + Tolnaftate + Clioquinol).

Betamethasone Valerate↗