The endocrine effects of ketoconazole

@article{Sonino1986TheEE,
  title={The endocrine effects of ketoconazole},
  author={Nicoletta Sonino},
  journal={Journal of Endocrinological Investigation},
  year={1986},
  volume={9},
  pages={341-347}
}
  • N. Sonino
  • Published 1 August 1986
  • Medicine
  • Journal of Endocrinological Investigation
INTRODUCTION Ketoconazole l has been employed extensively in clinical practice during the last 5 years as an innovative treatment for fungal disease (1 ). This is due largely to its properties: broad-spectrum activity, easy mode of administration, widespread tissue distribution, low degree of inactivation, good patient tolerance, low toxicity profile (2). This orally-active imidazole derivative (3-5) interferes with the synthesis of ergosterol in fungi and cholesterol in mammalian cells by… Expand
Aminoglutethimide and ketoconazole: historical perspectives and future prospects.
TLDR
Attempts to produce imidazole inhibitors of steroidogenesis are less advanced, although one compound has been reported to be a more selective and potent aromatase inhibitor than aminoglutethimide. Expand
Effects of ketoconazole on the iodide uptake by FRTL-5 cells.
TLDR
It can be assumed that ketoconazole could influence the iodide uptake in the FRTL-5 cells through more than one mechanism, because of its dual action. Expand
Overview of medically important antifungal azole derivatives.
  • R. Fromtling
  • Medicine, Biology
  • Clinical Microbiology Reviews
  • 1988
TLDR
A major chemical group with antifungal activity, the azole derivatives, is examined and historical and state of the art information on the in vitro activity, experimental in vivo activity, mode of action, pharmacokinetics, clinical studies, and uses and adverse reactions are examined. Expand
Dose and sex-dependent disposition of ketoconazole in rats
TLDR
The disposition of the antifungal drug ketoconazole was studied in mature male and female rats given single intravenous doses of 10, 20 or 40 mg/kg body weight and it is suggested that the dose-dependent disposition is caused by saturation of metabolizing enzymes. Expand
The Effect of Ketoconazole on Endocrine and Reproductive Parameters in Male Mice and Rats
TLDR
It is concluded that ketoconazole is probably not a viable approach to the development of a male contraceptive because of the lack of correlation between steroid levels and sperm immobilization, along with rapid in vivo and in vitro effects on sperm motility. Expand
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TLDR
Azole antifungals are first-line options in the prophylaxis and treatment of invasive fungal infections and have been associated with peripheral neuropathies, and itraconazole and voriconazole with pancreatitis. Expand
Ketoconazole reduces elevated serum levels of 1,25-dihydroxy vitamin D in hypercalcemic sarcoidosis
TLDR
It is concluded that ketoconazole administration can lower the elevated serum 1,25-dihydroxyvitamin D levels in sarcoidosis, however, deterioration of renal function during ketoconAZole administration as well as failure of hypercalcemia to be affected during short-term ketoconzole treatment suggest that this drug might not be appropriate for acute treatment ofhypercalcemic sarcoIDosis. Expand
Ketoconazole decreases the serum ionized calcium and 1,25-dihydroxyvitamin D levels in tuberculosis-associated hypercalcemia.
TLDR
Abnormal elevated levels of 1,25-dihydroxyvitamin D caused hypercalcemia in two boys with active tuberculosis; ketoconazole administration may be effective in the treatment of hypercalCEmia in patients with tuberculosis, which decreases 1, 25-dhydroxy vitamin D synthesis. Expand
Potency and specificity of CGS-16949A as an aromatase inhibitor.
TLDR
Comparing the potency and specificity of a new aromatase inhibitor with that of aminoglutethimide in a variety of in vitro enzyme preparations suggests that CGS-16949A has favorable properties as a specific and potent aromatases inhibitor. Expand
Mouse hepatic metabolites of ketoconazole: isolation and structure elucidation.
TLDR
It was demonstrated that KC was biotransformed to a number of products, including piperazine (de-N-acetyl ketoconazole, DAKC), N-carbamylpiperazine, N-formylpipersazine, 2,3-piperazinedione, 2-formamidoethylamine, ethylenediamine and amine. Expand
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In vitro growth studies revealed that ketoconazole's activity was more pronounced against the invasive morphogenetic form than against the saprophytic form of Candida albicans, which at least partly explains its prominent in vivo potency. Expand
Hormonal effects of ketoconazole in vivo in the male rat: mechanism of action.
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Ketoconazole inhibits T synthesis, primarily by inhibiting the activity of multiple enzymes in the T biosynthetic pathway and has no direct effect at the pituitary level; ketconazole metabolism in the rat is considerably different from that in man; and ketoconazoles enhances the inhibitory effects of GnRH agonist. Expand
Ketoconazole blocks testosterone synthesis.
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The diminution of testosterone synthesis could be significant as further therapeutic trials may use larger doses or more than once-daily administration, and the paucity of reports of endocrinologic toxicity may relate to the "escape from the block demonstrated in vivo. Expand
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The pharmacology of ketoconazole was studied in patients with fungal infections and an increase in the area under the curve of serum concentrations occurred in patients receiving 200 mg daily who were restudied after 1 to 12 months of therapy; however, normalized areaunder the curve appeared to decrease after higher doses were administered chronically. Expand
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Ketoconazole is a well‐tolerated oral antifungal agent with a broad spectrum of activity in vitro, but in vitro testing has not yet been correlated to in vivo results. In addition, many variablesExpand
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In vitro studies with mouse Leydig cells demonstrated a direct reversible inhibition of testosterone biosynthesis by ketoconazole, a broad-spectrum antifungal drug, which indicates a structure/activity relationship for the effects observed. Expand
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In healthy humans, the cortisol response to adrenocorticotropic hormone was significantly blunted 4 hours after a 400-mg or 600-mg dose, and this finding indicated that adrenal androgen response was reduced. Expand
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Data show that KC interferes with hepatic oxidative drug metabolism and suggest that this mechanism might be involved in the unwanted side effects of therapy with KC. Expand
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The effect of ketoconazole on steroidogenesis in cultured mouse adrenal cortex tumor cells.
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  • Biology, Medicine
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The effects of the antimycotic agent ketoconazole on steroid biosynthesis in adrenal cells was investigated in monolayer cultures of functional mouse adrenal cortex tumors, finding it to be an even more potent inhibitor of 11β hydroxylation in these cultures. Expand
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