OBJECTIVES Perampanel, a selective, noncompetitive AMPA receptor antagonist, is indicated as adjunctive therapy for the treatment of partial seizures with or without secondarily generalized seizures and primary generalized tonic-clonic seizures in patients with epilepsy aged 12years and older. In vitro studies and Phase I trials indicate that perampanel is metabolized almost exclusively by CYP3...

Ketoconazole is a well-tolerated, synthetic, imidazole derivative currently in widespread therapeutic use against mycotic infections. Recent evidence that it depresses testosterone synthesis in humans prompted us to investigate the effects in rats of its administration alone or in combination with the gonadotropin releasing hormone superagonist analogue leuprolide. Plasma luteinizing hormone, t...

Determination of the ratio of testosterone to epitestosterone (T/E) in urine is used to detect testosterone administration in athletes, with a ratio > 6 considered as evidence of an offense. We show that administration of ketoconazole, which inhibits testosterone biosynthesis, may be useful for differentiating between an athlete who is using testosterone and one who naturally gives a ratio > 6....

BACKGROUND: Xenoestrogens and antifungal azoles probably share a common route of metabolism, through hepatic cytochrome P450 (CYP) enzymes. Chemical interactions with metabolic pathways may affect clearance of both xenobiotics and endobiotics. This study was carried out to identify possible chemical interactions by those substances on CYP1A and CYP3A, in Atlantic cod liver. We investigated effe...

Prostate cancer is the most common nonskin cancer in American men, and androgen-deprivation therapy is the cornerstone of treatment for advanced prostate cancer. Unfortunately, the median duration of response to initial androgen deprivation is limited to 18–24 months. After failing primary therapy, many individuals respond to multiple secondary hormonal interventions, such as ketoconazole. A po...

Twelve Spanish laboratories collected 325 yeast clinical isolates during a 30 day's period, among them 224 Candida albicans, 30 Candida glabrata, and 27 Candida parapsilosis. In vitro antifungal susceptibility to amphotericin B, ketoconazole, fluconazole and itraconazole was determined by an agar diffusion test (Neo-Sensitabs, Rosco, Denmark). All the isolates tested were susceptible in vitroto...

ABT-384 [1-piperazineacetamide, N-[5-(aminocarbonyl) tricyclo[3.3. 1.13,7]dec-2-yl]-a,a-dimethyl-4-[5-(trifluoromethyl)-2-pyridinyl]-, stereoisomer] is a potent and selective inhibitor of 11b-hydroxysteroid dehydrogenase type 1 (HSD-1). ABT-384 has been shown to be safe and well tolerated in humans at doses up to 100 mg daily, and to fully inhibit both peripheral and brain HSD-1 at a dose of 2 ...

resistance to drug such as metronidazole is one the commonest causes of treatment failure while eradicating helicobacter pylori . considering the safety of ketoconazole and fluconazole and their inhibitory activity on biosynthesis of fatty acids from cholesterol in cell membrane of h.pylori , the idea of their efficacy against h.pylori is raising . the aim of this study is to evaluate susceptib...

abstract background: in order to evaluate the role ofketoconazole in the prevention of ovarian hyperstimulation syndrome (ohss) in women with polycystic ovary syndrome (pcos) undergoing ovarian stimulation with gonadotropins, a prospective, randomized, double-blind, placebo controlled study was done on one-hundred and nine pcos women that had been refeited to be treated by gonadotropins. method...

This study investigated the relationship among estrogen, placental blood flow and placental weight gain in rats treated with ketoconazole. Oral administration of ketoconazole (25mg/kg/day) on Days 12-14 of pregnancy induced reduction of plasma estradiol-17β (E2) concentration, transient decrease in placental blood flow and increased intensity of a hypoxia-related marker in the placenta on Day 1...