[Clinical experience in the management of dermatomycoses using the 1 per cent econazole-spray solution and the 1 per cent econazole-spray powder].
Explore the source record for details and available documents.
Adult↗
SEARCH · Search PubMed
Results for “Econazole”
Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.
Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.
Econazole: a review of its antifungal activity and therapeutic efficacy.
Econazole1 is a recently introduced imidazole antifungal agent which is very closely related structurally to another imidazole derivative, miconazole. For local application the nitrate salt of econazole is used, while in preliminary investigations of systemic use in a few patients econazole base has been administered orally or intravenously. In uncontrolled studies in large numbers of patients, econazole nitrate has been administered topically in the treatment of dermatomycoses due to a wide variety of fungi, and vaginally in the treatment of vaginal candidosis; but it has not been compared with any other antifungal drug in controlled therapeutic trials in mycoses of the skin and has only been compared with nystatin in a few patients with vaginal candidosis. Until adequate comparative studies are done the relative place of econazole in the treatment of dermatomycoses and vaginal condidosis, compared with traditional antifungal agents and with other imidazole derivatives such as miconazole or clotrimazole, cannot be clearly stated. Nevertheless, econazole nitrate is an effective antifungal drug. In dermatological studies about 90% of a large number of patients were cured, often after a relatively short treatment period (2 to 6 weeks, as occurs with other imidazole antifungal agents). The cure rate was only slightly lower (about 85%) in patients with severe mycoses of many years' duration than in those whose infections were of more recent onset. In vaginal candidosis a 3-day treatment regimen using a 150mg suppository once daily was only slightly less effective (85% mycological cure rate) than a 15-day regimen using a 50mg dose (suppository or cream) once daily (90% cure rate). A 3 to 5 day 'higher' dose regimen was slightly more effective than a standard 15-day regimen of nystatin vaginal inserts in a small group of patients with vaginal candidosis. The convenience of the higher-dose shorter term regimen would likely be an important advantage to most patients. Whether other agents useful in vaginal candidosis would be as effective as econazole were they to be used in this way, has not been determined. Topical or intravaginal econazole nitrate has usually been well tolerated, side effects being limited to local irritation in about 1 to 4% of patients in most studies.
Adult↗
An imidazole derivative (Econazole) as an antifungal agent in cell culture systems.
Econazole, an imidazole derivative, was tested as an antifungal agent in different cell culture systems. In comparison with Fungizone, Econazole has the following advantageous properties: higher stability, higher solubility, better antifungal activity against contaminants of cell cultures and a wider range between minimal inhibitory to cytotoxic concentration with Aspergillus fumigatus, Candida albicans and Penicillium sp., activity against gram-positive bacteria and lower price. Econazole exerts no antiviral effect and can therefore be used for virus isolation from heavily contaminated material. The antagonistic effect of serum on the antifungal effect of Econazole and Fungizone was comparable as was the inhibitory effect of both antimycotics on Mycoplasma growth. In view of the above mentioned properties Econazole lactic acid can be recommended as an antifungal agent for cell culture systems at a concentration of 1 microgram per ml.
Amphotericin B↗
Antimicrobial activity of econazole and miconazole in vitro and in experimental candidiasis and aspergillosis.
The antibacterial and antimycotic activity of econazole base, an imidazole derivative, was examined in vitro and in experimental infections of mice. Comparative minimal inhibitory concentration (MIC) determinations indicate econazole as well as miconazole to be of moderate activity against gram-positive bacteria (MICs: 0.78-25mug/ml) and yeasts (MICs: 1.56-25 mug/ml). Against filamentous fungi, econazole exhibits better in vitro activity than miconazole and - with the exception of Rhizopus oryzae and Absidia corymbifera - MICs are markedly lower than against yeasts. No effect of nutrient media and no effect of the inoculum were observed with the four drugs. A strong influence of bovine serum on MIC values, however, suggested a strong protein binding. In experimental candidiasis of mice, no therapeutic effect with econazole base administered orally or intraperitoneally could be observed (ED50 and 'minimum life-prolonging dose': great than 200 mg/kg). In experimental aspergillosis of mice, a slight effect, as demonstrated by the 'minimum life-prolonging dose' of 100 mg/kg, was found. The in vitro and in vivo results are discussed in the light of the available pharmacokinetic and toxicological data. It is concluded that more studies, especially on the pharmacology of econazole and about the clinical efficacy, are needed to come to a definite judgement.
Amphotericin B↗
Bilogical and toxicological properties of econazole, a broad-spectrum antimycotic.
The spectrum of activity of 1-(2,4-dichloro-beta-[(p-chlorobenzoyl)oxy]phenethyl)imidazole-nitrate (econazole, R 14827) was tested in vitro on various pathogenic fungi and bacteria, and also in vivo in guinea-pigs and rats experimentally infected with dermatophytes and C. albicans. The in vitro activity spectrum is very broad: the dermatophytes, the yeasts, the dimorphic fungi, the aspergilli, the mycetoma causing agents and the Gram-positive bacteria being most sensitive. Guinea-pigs infected with T. mentagrophytes, M. canis or C. albicans and treated topically or orally with econazole, were cured. In each of these tests the activity of econazole was compared with that of different reference drugs. Vaginal candidiasis in rats was cured after oral administration of econazole. Toxicity and teratogenicity studies in different laboratory animals indicate that econazole is well tolerated.
Animals↗
Interactions between econazole, a broad-spectrum antimicrobic substance, and topically active glucocorticoids.
Econazole is a broad-spectrum antimicrobic substance which acts by permeabilizing the cell membranes. Glucocorticoids by their surface activity may counteract this effect by protecting the cell membranes. In fact, a protective action of glucocorticoids in high concentrations against econazole nitrate could be demonstrated in yeasts, not in staphylococci. The techniques applied were the Warburg assays (resting yeasts, resting and proliferating bacteria). The elicitation of a blanching reaction on human skin by triamcinolone acetonide was not altered in the presence of econazole nitrate. The data collected in this study were discussed in regard to the combined use of antimicrobic drugs and glucocorticoids in topical therapy.
Administration, Topical↗
Treatment of pityriasis capitis (dandruff) with econazole nitrate.
63 patients of both sexes with pityriasis sicca or steatoides were examined for presence of Pityrosporum ovale on the scalp. Only those cases in which very numerous yeasts were seen in all squamae present in the preparation were considered positive. According to the severity or duration of pityriasis, 60% of the patients in this population represented severe cases and 38% refractory cases. A solution of econazole nitrate was applied as a spray, morning and evening, for a period of 10 to 20 days (mean). The overall assessment of the clinical effects of econazole nitrate indicated 56 favourable results, with complete disappearance of objective clinical signs in 47 cases; the course of pruritus proceeded roughly parallel with that of the objective signs. The mycological checking of the clinical results, performed at least 7 days after the conclusion of therapy, disclosed 6 failures and 57 successes. In 17 patients, the microscopic examination of squamae was complemented by culture before and after treatment: in all cases, the culture, positive before econazole nitrate therapy, became negative after treatment, thus confirming the results of direct examination. These data suggest that Pityrosporum ovale plays a pathogenetic part in pityriasis simplex capitis.
Adolescent↗
[Evaluation of econazol in 594 cases of skin mycosis (author's transl)].
A total of 594 patients were treated with the new antimycotic agent econazol (Pevaryl). The diagnosis was proven microscopically and on culture except in cases of pityriasis versicolor where it was proven microscopically only. Econazol was given to 130 patients as a 1% solution, to 128 patients as a 1% milk, and to 336 patients as a 1% spray solution. In 333 cases of foot mycosis or eczema marginatum econazol spray powder was given in addition. As measured by the cure rate the spray solution (92%) was not significantly more effective than the milk (89%) or the simple solution (87%). Criteria for cure included negative microscopy and fungal cultures a week after treatment had ceased as well as clinical cure. A total of 90% of all cases (n = 536) could be considered as cured microscopically and on culture after an average of 3.6 weeks (pityriasis versicolor) and 4.8 weeks (tinea pedis, manus, inguinocruralis). In a further 4.4% (n = 26) the fungus could be demonstrated microscopically despite a clinical cure and in 7 of these cases culture was also positive. The cure rate was independent of the responsible pathogen. The preparations were tolerated extremely well. In 7 cases, however, transient dermatitic irritations were seen in the inguinocrural region, mainly caused by the simple solution.
Aerosols↗
[Econazole nitrate. In vitro tests and clinical trial].
Econazole-nitrate is a new potent antifungal drug with a broad spectrum against dermatophytes, yeasts and moulds; in addition it is effective against gram-positive bacteria. Econazole nitrate was tested in-vitro for antifungal and anti-microbial properties. In an open trial 75 patients were treated with a 1 percent econazole cream. Cure was achieved in tinea pedis in 91 percent; in tinea genitocruralis in 100 percent and in tinea corporis in 92 percent. The remainder were greatly improved. 22 patients with erythrasma were cured within 3 weeks.
Adolescent↗
Clinical evaluation of econazole nitrate in 1% vaginal cream for treatment of vaginal candidosis.
30 patients with mycologically confirmed vaginal candidosis on culture were treated with econazole vaginal cream (Gyno-Pevaryl) applied intravaginally once a day for 2 wk. 8 days after the end of treatment, mycological and clinical cures were demonstrated in 26 patients. Symptoms generally subsided rapidly, and the drug was well tolerated. This study confirms the efficacy of econazole in the treatment of vaginal candidosis.
Adolescent↗
A new treatment of vaginal candidiasis: three-day treatment with econazole.
From an open comparative multicentric trial it became clear that econazole was an active and well-tolerated agent for the treatment of vulvo-vaginal mycoses. Combined treatment with pessaries and econazole cream seems to be worthwhile in order to isolate the vagina from possible Candida reservoirs or to hasten symptomatic relief.
Adolescent↗
Absorption and disposition of econazole nitrate after application to the skins and vaginas of rabbits.
1. The absorption and tissue distribution of radioactivity has been studied in rabbits after application of a cream containing 10 mg of the 3H-labelled 1-(2,4-dichloro-beta-[(p-chlorobenzyl)oxy]phenethyl) imidazole nitrate (econazole nitrate, Pevaryl) to the normal or abraded skins of rabbits. 2. Approximately one-third of the dose was absorbed through the occluded normal skins of rabbits during 8 days, mainly during 7 to 24 h. In the same time interval, slightly more of the dose was absorbed through the occluded abraded skins of rabbits at slightly greater rates. Co-formulation of triamcinolone acetonide in the cream reduced and delayed the peak rates of absorption through normal and abraded skin, but the extent of absorption during 8 days was similar in the presence or absence of triamcinolone acetonide. 3. After application to normal skin or abraded skin, the peak of mean concentrations in the plasma of 220 ng/ml (range 132-276 ng/ml) or 307 ng/ml (range 270-321 ng/ml), respectively, occurred at 24 h. Tissue distribution of radioactivity was similar after application to normal or abraded skin, and concentrations were highest in the liver, kidneys and gastrointestinal tract (which are the organs of biotransformation and excretion) and also in the adrenals and to a lesser extent in the uterus, ovaries and untreated skin. 4. After application of a cream containing 5 mg of 3H-econazole nitrate to the vaginas of rabbits, approximately one-third of the dose was absorbed during 8-24 h, and rates of excretion were higher through the more permeable vaginal membrane. 5. After vaginal doses of 5 mg, a peak concentration of 209 ng/ml occurred at 6 h in the plasma. Tissue concentrations of radioactivity after vaginal doses were highest in liver, kidneys, gastrointestinal tract, adrenals and ovaries, and the tissue distribution was similar to that observed after cutaneous doses.
Administration, Oral↗
Freeze-fracture studies of the plasmalemma of Candida albicans after treatment with econazole-nitrate.
In electron microscopic studies the interior of the plasmalemma of Candida albicans was revealed by means of the freeze-fracture technique. The superficial structures of the extracellular (E) and protoplasmic (P) fracture faces differed negligibly from structures on the corresponding fracture faces of Saccharomyces cerevisiae. Following treatment with 2.2 x 10(-5) M econazole nitrate a layer, present on the P face in the form of a tight matrix of globular proteins, dissolved into isolated groups of particles whose globular elements sometimes formed hexagonal patterns. As the damage progressed, fissure-shaped membrane invaginations on the P face disappeared. Parts of the outer lipid layer of the plasmalemma were torn off the cell wall and adhered in fragments to the P face. The ultrastructural changes in the plasmalemma induced by econazole nitrate temporally correlate with an increase in the permeability of the cell envelope found in physiological studies performed by other authors.
Candida albicans↗
Three-day therapy of vulvovaginal candidiasis with econazole: a multicentric study comprising 996 cases.
Within the scope of three open multicentric studies, effect and tolerability of 150 mg. econazole vaginal suppositories were tested in a total of 996 women, 13 to 74 years old (mean age, 29 years). Vaginal candidiasis had been mycologically demonstrated in every patient prior to therapy, and the total cure rate of 93.4 per cent in Studies I and II (880 patients) was also mycologically confirmed. The tolerability was tested by checking of 30 laboratory variables before and after the treatment of 116 patients (Study III); no therapy-related adverse changes were recorded. Connections between therapeutic results, age distribution, initial hormonal situation, and conception of the therapy are pointed out.
Adolescent↗
Three methods of application of econazole in the treatment of vaginal candidiasis.
Pointing out the fact that there is a generalized increase in the incidence of vaginal candidiasis the authors describe a study involving a total of sixty-one patients to evaluate econazole in the treatment of the condition.
Administration, Topical↗
R34000, a dioxolane imidazole in the therapy for experimental coccidioidomycosis. Comparison with miconazole and econazole.
Comparisons were made on the therapeutic influence of three imidazole drugs in experimental lethal coccidioidomycosis of mice. When administered by the intramuscular route, miconazole and a closely related structural analogue, econazole, were effective in preventing death, restricting fungal replication in the lungs, and minimizing the extent of extrapulmonary dissemination. Neither drug was as effective when administered by the oral route as by the intramuscular route. This contrasted sharply with results obtained using R34000, a dioxolane imidazole. It was very highly effective when administered by the oral route and less so by intramuscular injection. All orally treated mice survived a challenge lethal to more than 80 percent of control animals. Plasma or serum concentrations of orally administered R34000 in mice and in man exceeded the minimum inhibitory concentration for a virulent strain of Coccidioides immitis.
Administration, Oral↗
[On the treatment of trichonocardiosis palmellina with econazol nitrate spray (author's transl)].
The effectiveness of econazol nitrate incorporated in spray was tested in trichonocardiosis palmellina. In all 5 cases an optimal therapeutic result was seen after a few days.
Adult↗
[Vaginal absorption of econazole].
After vaginal application econazol is absorbed to a high degree. Plasma levels are maintained for a relatively long period. Metabolism occurs in the vagina already. As there are no objections concerning toxicology the fact of absorption is considered positive from the therapeutical view-point because this drug does exert its effect not only in the vaginal cavity but also in the epithelium. It is suggested that vaginal absorption is influenced by cervical mucus.
Absorption↗