Fluconazole|86386-73-4|安捷凯

Background

Fluconazole is a triazole antifungal drug used in the treatment and prevention of superficial and systemic fungal infections.Target: AntifungalFluconazole is a triazole antifungal intended for oral treatment of superficial and systemic mycoses. In tests done in standard mycological media, the compound had minimal inhibitory concentrations against pathogenic Candida species that were usually in excess of 100 mg/l. Fluconazole inhibited branching and hyphal development in C. albicans at concentrations as low as 10(-6) M (0.3 mg/l), but miconazole and ketoconazole were still active in these tests at concentrations 100 times lower than this [1]. Oral fluconazole was not associated with a significantly increased risk of birth defects overall or of 14 of the 15 specific birth defects of previous concern. Fluconazole exposure may confer an increased risk of tetralogy of Fallot [2]. Fluconazole is predicted to be ineffective against Cryptococcus gattii in the koala as a sole therapeutic agent administered at 10 mg/kg p.o. every 12 h [3].Clinical indications: Balanitis; Candida infection; Cryptococcus infection; Cryptococcus neoformans meningitis; Dermatomycosis; Female genital tract infection; Fungal infection; Fungal respiratory tract infection; Fungal urinary tract infection; Prophylaxis; Tinea capitis; Tinea corporis; Tinea cruris; Tinea pedis .Toxicity: Symptoms of overdose include hallucinations and paranoid behavior.

参考文献:
[1]. Odds, F.C., S.L. Cheesman, and A.B. Abbott, Antifungal effects of fluconazole (UK 49858), a new triazole antifungal, in vitro. J Antimicrob Chemother, 1986. 18(4): p. 473-8.
[2]. Molgaard-Nielsen, D., B. Pasternak, and A. Hviid, Use of oral fluconazole during pregnancy and the risk of birth defects. N Engl J Med, 2013. 369(9): p. 830-9.
[3]. Black, L.A., et al., Pharmacokinetics of fluconazole following intravenous and oral administration to koalas (Phascolarctos cinereus). J Vet Pharmacol Ther, 2013.

Protocol

Cell experiment [1]:

Cell lines

The Candida albicans reference strain SC5314

Preparation method

The solubility of this compound in DMSO is >10.9mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

10 μg/ml; dissolved in Milli-Q water

Applications

In wild-type Candida albicans SC5314 cells, fluconazole (10 μg/ml) and doxycycline (50 μg/ml) inhibited cell growth in a dose dependent way.

Animal experiment [2]:

Animal models

C. albicans-infected p47phox-/- knockout mice

Dosage form

80 mg/kg/day for 13 days; diluted in saline; intraperitoneal injection

Application

In C. albicans-infected p47phox-/- knockout mice, fluconazole significantly reduced splenic counts of C. albicans (P =0.008).

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

参考文献:

[1]. Alessandro Fiori and Patrick Van Dijck. Potent Synergistic Effect of Doxycycline with Fluconazole against Candida albicans Is Mediated by Interference with Iron Homeostasis. Antimicrob Agents Chemother. 2012 Jul; 56(7): 3785–3796.

[2]. Justina Y. Ju, Cynthia Polhamus, Kieren A. Marr, et al. Efficacies of Fluconazole, Caspofungin, and Amphotericin B in Candida glabrata-Infected p47phox-/- Knockout Mice. Antimicrob Agents Chemother. 2002 May; 46(5): 1240–1245.

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Fluconazole

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Background

Protocol

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