物质信息

ID:903

名称和标识
IUPAC标准名
1-[4-(4-{[(2S,4R)-2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazin-1-yl]ethan-1-one
别名
Ketoconazole [Usan:Ban:Inn:Jan]Ketoconazolum [INN-Latin]KetoconazolketoconazoleKetoconazol [INN-Spanish]Ketocanazole2%Ketoconazole
商标名
FungarestKetoisdinKetozoleNizoralNizoral CreamNizoral ShampooNizoral a-DOrifungalNizoral a-D ShampooSebazoleExtinaFungoralKetodermOrifungal MPanfungol
IUPAC传统名
nizoral shampoo
数据登录号
化合物性质
理化性质
疏水性(logP)
4
溶解度
0.0866 mg/L
描述信息
Drug Groups
approved; investigational
Description
Broad spectrum antifungal agent used for long periods at high doses, especially in immunosuppressed patients. [PubChem]
Indication
For the treatment of the following systemic fungal infections: candidiasis, chronic mucocutaneous candidiasis, oral thrush, candiduria, blastomycosis, coccidioidomycosis, histoplasmosis, chromomycosis, and paracoccidioidomycosis.
Pharmacology
Ketoconazole, like clotrimazole, fluconazole, itraconazole, and miconazole, is an imidazole antifungal agent.
Toxicity
Hepatotoxicity, LD50=86 mg/kg (orally in rat)
Affected Organisms
Fungi
Biotransformation
Hepatic
Absorption
Moderate
Half Life
2 hours
Protein Binding
99% (in vitro, plasma protein binding)
References
• Goeders NE, Peltier RL, Guerin GF: Ketoconazole reduces low dose cocaine self-administration in rats. Drug Alcohol Depend. 1998 Dec 1;53(1):67-77. [Pubmed]
• Berwaerts J, Verhelst J, Mahler C, Abs R: Cushing's syndrome in pregnancy treated by ketoconazole: case report and review of the literature. Gynecol Endocrinol. 1999 Jun;13(3):175-82. [Pubmed]
• Kazy Z, Puho E, Czeizel AE: Population-based case-control study of oral ketoconazole treatment for birth outcomes. Congenit Anom (Kyoto). 2005 Mar;45(1):5-8. [Pubmed]
• Pierard-Franchimont C, Goffin V, Decroix J, Pierard GE: A multicenter randomized trial of ketoconazole 2% and zinc pyrithione 1% shampoos in severe dandruff and seborrheic dermatitis. Skin Pharmacol Appl Skin Physiol. 2002 Nov-Dec;15(6):434-41. [Pubmed]
External Links
• [Wikipedia]
• [RxList]
• [PDRhealth]
• [Drugs.com]
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参考文献
• Goeders NE, Peltier RL, Guerin GF: Ketoconazole reduces low dose cocaine self-administration in rats. Drug Alcohol Depend. 1998 Dec 1;53(1):67-77. Pubmed
• Kazy Z, Puho E, Czeizel AE: Population-based case-control study of oral ketoconazole treatment for birth outcomes. Congenit Anom (Kyoto). 2005 Mar;45(1):5-8. Pubmed
• Berwaerts J, Verhelst J, Mahler C, Abs R: Cushing's syndrome in pregnancy treated by ketoconazole: case report and review of the literature. Gynecol Endocrinol. 1999 Jun;13(3):175-82. Pubmed
• Pierard-Franchimont C, Goffin V, Decroix J, Pierard GE: A multicenter randomized trial of ketoconazole 2% and zinc pyrithione 1% shampoos in severe dandruff and seborrheic dermatitis. Skin Pharmacol Appl Skin Physiol. 2002 Nov-Dec;15(6):434-41. Pubmed
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