Nizoral
Use of ketoconazole in the treatment of canine nasal aspergillosis.

Sharp NJ, Sullivan M.

Veterinary Hospital, University of Liverpool, UK.

Fifteen dogs with nasal aspergillosis were treated with ketoconazole (5 mg/kg of body weight, q 12 h, PO) for 2 to 18 weeks. Four dogs whose conditions deteriorated during treatment received ketoconazole for less than the prescribed 6 weeks. Six months or more later, only 47% of the dogs were determined to be disease-free, on the basis of no fungal growth on culture. It was concluded that ketoconazole at this dosage is a useful treatment for canine nasal aspergillosis, but is no more effective than thiabendazole.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2647697&dopt=Abstract ketoconazole Nizoral



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Effect of 3-week treatment with [D-Trp6, des-Gly-NH10(2)]LHRH ethylamide, aminoglutethimide, ketoconazole or flutamide alone or in combination on testicular, serum, adrenal and prostatic steroid levels in the dog.

Lacoste D, Caron S, Belanger A, Labrie F.

MRC Group in Molecular Endocrinology, Laval University Medical Center, Quebec, Canada.

Adult male mongrel dogs were treated with the LHRH agonist [D-Trp6, des-Gly-NH10(2)]LHRH ethylamide, aminoglutethimide, ketoconazole or flutamide alone or in combination for 21 days before measurement of steroid levels in the testes, prostate, adrenals and serum. Ketoconazole alone caused a marked stimulation of the intra-testicular concentration of pregnenolone, 17OH-pregnenolone, progesterone and 17OH-progesterone with no or little change of androstenedione, testosterone and dihydrotestosterone. Aminoglutethimide caused a 30-95% inhibition in the concentration of all steroids in the tests while treatment with the LHRH agonist caused a near complete inhibition of all testicular steroids. When administered concomitantly with the LHRH agonist, ketoconazole partly prevented the inhibitory effect of the LHRH agonist on testicular steroid levels. Serum levels of dehydroepiandrosterone, androst-5-ene-3 beta,17 beta-diol, androstenedione and androstane-3 alpha, 17 beta-diol were 75 to 95% inhibited by the LHRH agonist while serum testosterone and dihydrotestosterone concentrations were reduced below detection limits by the same treatment. Moreover, treatment with the LHRH agonist caused a 70-95% reduction in the intraprostatic concentration of testosterone and dihydrotestosterone in all the groups although maximal effect was observed when the LHRH agonist was combined with any of the three other agents. The present data show that while treatment with ketoconazole, aminoglutethimide or Flutamide alone has only partial inhibitory effects on androgen levels, combination with an LHRH agonist provides maximal inhibition. In addition to its direct blockade of the androgen receptor, some of the effect of Flutamide could be related to its blockade of testicular 3 beta-hydroxy-steroid dehydrogenase activity.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2671505&dopt=Abstract ketoconazole Nizoral



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Action of the ketoconazole-alkylaminoethylglycine combination on Candida albicans.

Villa A, Simonetti N, Retico A.

Institute of Microbiology, Faculty of Pharmacy, University La Sapienza of Rome.

High concentrations of ketoconazole (Ktc) exhibit poor antimicrobial activity in microbicidal test. Alkylaminoethylglycine (AAEG), an amphoteric surface-active agent, employed in subinhibitory concentrations, can enhance the action of ketoconazole. The Ktc-AAEG combination causes a higher rate of potassium ion release compared to both drugs separately. The increased ketoconazole activity may be ascribed to the membrane damage indicated by increased permeability to potassium ions.

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In vitro antifungal activity of saperconazole (R 66905) against Candida and Torulopsis.

Mallie M, Montes B, Lebecq JC, Bastide JM.

The susceptibility of several strains of Candida and Torulopsis to saperconazole, a new triazole antifungal compound, was compared to that of ketoconazole. The MICs of the two antifungal agents were determined against 70 strains of Candida albicans, 10 strains of C. guilliermondii, 10 strains of C. krusei, 10 strains of C. parapsilosis, 10 strains of C. pseudotropicalis, 10 strains of C. tropicalis and 15 strains of Torulopsis glabrata. The fungistatic activity was evaluated by the agar dilution method using BHI and casitone media after incubation for 48 hours at 28-30 degrees C. The in vitro activity of saperconazole was similar to that of ketoconazole for most of the Candida spp. tested except for C. krusei in particular. An MIC of less than or equal to 3.12 micrograms/ml for saperconazole was found with 92% of the C. albicans strains tested. In contrast, T. glabrata was more susceptible to ketoconazole.

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[A dose-response study of the chronic effect of ketoconazole on androgen and cortisol secretion in women with hyperandrogenism]

[Article in Spanish]

Garcia Centenera JA, Caso Pelaez E, Hervas Olivares F, Castel Aznar C, Pozuelo Escudero V, Gomez Pan A.

We have previously shown that ketoconazole may inhibit the androgen synthesis, but the risk to induce a blockade in the cortisol synthesis and/or hepatic abnormalities makes it mandatory to look for the least dose that is able to inhibit androgen production without inducing other abnormalities. To this end, we studied the levels of 17-alpha-hydroxyprogesterone (17, alpha-OH-P), dehydroepiandrosterone sulphate (DHEA-S), delta 4-androstenedione (delta 4-A), total (tT) and free (fT) testosterone, and the cortisol response to ACTH in 13 women with hyperandrogenism, before and after ketoconazole therapy at dosages of 400, 600, and 800 mg/day. Although with the 400 mg regimen a reduction in the levels of androstenedione and free and total testosterone was already observed, it was of small amount and it was not until the 600 mg regimen that androgen levels became normal. Thus, DHEAS-S was reduced from 3.672 +/- 1.013 to 2.216 +/- 756 ng/ml (p less than 0.05); delta 4-A was reduced from 392 +/- 80 to 283 +/- 79 ng/ml (p less than 0.01); tT was reduced from 1.5 +/- 0.78 to 0.7 +/- 0.1 ng/ml (p less than 0.05), and fT from 5.5 +/- 1.0 to 2.7 +/- 1.3 pg/ml (p less than 0.001). By contrast, 17 alpha-OH-P increased from 1.7 +/- 1.3 to 4.7 +/- 1.3 ng/ml (p less than 0.001).(ABSTRACT TRUNCATED AT 250 WORDS)

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Pityriasis versicolor--epidemiological and therapeutical study.

Selim MM, Kubec K.

Seventy-six patients with extensive pityriasis versicolor were divided into 3 groups and treated orally with ketoconazole, 200 mg daily, for 10, 20 or 30 days respectively. 50 patients out of this number completed the study. After 6 months, 46 patients were checked up. Eight of them developed relapses effectively treated with ketoconazole for another 15 days. Six out of these 8 patients belonged to the first group using ketoconazole for 20 days only. On the basis of this observation, we do not consider a 10 days' treatment to be sufficient and recommend that the patient should be treated for at least 20 days. As a preventive measure we recommend a daily bath with salicylic acid and sulphur soap. The frequency of the infection was higher in males (71.4%) than in females (28.6%). The youngest of the male patients was 4 months of age and the oldest 70 years. The youngest female was 4 months old and the oldest 50 years. Pityriasis versicolor was found to be predominant in the age group of 21--30 years. The sites most commonly involved were back, chest and the upper extremities.

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Resistance reversal action of ketoconazole against mefloquine resistance of Plasmodium yoelii nigeriensis.

Awasthi A, Dutta GP, Bhakuni V, Tripathi R.

Division of Parasitology, Central Drug Research Institute, Chattat Manzil, PO Box No. 173, Lucknow 226 001, India.

Ketoconazole at 200 mg/kg dose has been found to exert marginal antimalarial action against multidrug resistant (MDR) Plasmodium yoelii nigeriensis (P. yoelii nigeriensis) in Swiss mice with 25% protection (2/8 mice) while at lower Ketoconazole dose i.e., 75-100 mg/kg, 14.28% mice were protected. Mefloquine (MFQ) (at 8 and 16 mg/kg) exerted suppressive action against MDR P. yoelii nigeriensis resulting in 25 and 14.28% protection of mice respectively. Combined treatment with Ketoconazole and mefloquine resulted in protection of 5/6 mice (83.33%) at MFQ 4 mg/kg + Ketoconazole 100 mg/kg dose, 7/8 (87.5%) mice at MFQ 8 mg/kg + Ketoconazole 20 mg/kg dose and 5/7 (71.42%) mice at MFQ 16 mg/kg + Ketoconazole 25 mg/kg dose and 5/6 (83.33%) mice at MFQ 16 mg/kg + Ketoconazole 100 mg/kg dose. Ketoconazole has been found to enhance the protective effect of mefloquine against MFQ resistant P. yoelii nigeriensis resulting in 66-88% protection of the mice treated with the appropriate combinations. The combination also increased suppression of parasitaemia at different times. The Ketoconazole combination with MFQ significantly increased the mean survival time of the treated mice compared to individual drugs alone. The study shows that Ketoconazole when administered with MFQ exerts bio-enhancing action against mefloquine resistance of MDR P. yoelii nigeriensis.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=15363936&dopt=Abstract ketoconazole Nizoral