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Ketoconazole

Generic Name
Ketoconazole
Brand Names
Extina, Ketodan, Ketoderm, Nizoral, Xolegel, Ketoconazole HRA
Drug Type
Small Molecule
Chemical Formula
C26H28Cl2N4O4
CAS Number
65277-42-1
Unique Ingredient Identifier
R9400W927I

Overview

Ketoconazole is an imidazole antifungal agent used in the prevention and treatment of a variety of fungal infections. It functions by preventing the synthesis of ergosterol, the fungal equivalent of cholesterol, thereby increasing membrane fluidity and preventing growth of the fungus. Ketoconazole was first approved in an oral formulation for systemic use by the FDA in 1981. At this time it was considered a significant improvement over previous antifungals, miconazole and clotrimazole, due to its broad spectrum and good absorption. However, it was discovered that ketoconazole produces frequent gastrointestinal side effects and dose-related hepatitis. These effects combined with waning efficacy led to its eventual replacement by triazole agents, fluconazole, itraconazole, voriconazole, and posaconazole. Ketoconazole and its predecessor clotrimazole continue to be used in topical formulations.

Background

Ketoconazole is an imidazole antifungal agent used in the prevention and treatment of a variety of fungal infections. It functions by preventing the synthesis of ergosterol, the fungal equivalent of cholesterol, thereby increasing membrane fluidity and preventing growth of the fungus. Ketoconazole was first approved in an oral formulation for systemic use by the FDA in 1981. At this time it was considered a significant improvement over previous antifungals, miconazole and clotrimazole, due to its broad spectrum and good absorption. However, it was discovered that ketoconazole produces frequent gastrointestinal side effects and dose-related hepatitis. These effects combined with waning efficacy led to its eventual replacement by triazole agents, fluconazole, itraconazole, voriconazole, and posaconazole. Ketoconazole and its predecessor clotrimazole continue to be used in topical formulations.

Indication

Ketoconazole is used in the treatment or prevention of fungal infections including blastomycosis, candidiasis, coccidioidomycosis, histoplasmosis, chromomycosis, and paracoccidioidomycosis. In Europe, it is also used in the treatment of endogenous Cushing's syndrome.

Associated Conditions

  • Bacterial Vaginosis (BV)
  • Blastomycosis
  • Candidiasis, Systemic
  • Chromoblastomycosis
  • Chronic Mucocutaneous Candidiasis (CMC)
  • Coccidioidomycosis
  • Dandruff
  • Endogenous Cushing's Syndrome
  • Fungal Infections
  • Histoplasmosis
  • Paracoccidioidomycosis
  • Seborrheic Dermatitis
  • Tinea Corporis caused by Epidermophyton floccosumin
  • Tinea Corporis caused by Trichophyton mentagrophytes
  • Tinea Corporis caused by Trichophyton rubrum
  • Tinea Cruris caused by Epidermophyton floccosumin
  • Tinea Cruris caused by Trichophyton mentagrophytes
  • Tinea Cruris caused by Trichophyton rubrum
  • Tinea Pedis caused by Epidermophyton floccosumin
  • Tinea Pedis caused by Trichophyton mentagrophytes
  • Tinea Pedis caused by Trichophyton rubrum
  • Vaginal Candidiasis
  • Vulvovaginal Candidiasis
  • Cutaneous candidiasis
  • Recalcitrant Dermatophytosis
  • Tinea versicolor caused by Malassezia infection

FDA Approved Products

Ketoconazole
Manufacturer:Rebel Distributors Corp
Route:TOPICAL
Strength:20 mg in 1 g
Approved: 2010/09/29
NDC:21695-556
Ketoconazole
Manufacturer:THIRTY MADISON INC
Route:TOPICAL
Strength:20 mg in 1 mL
Approved: 2022/03/28
NDC:71713-097
Ketoconazole Cream
Manufacturer:Direct_Rx
Route:TOPICAL
Strength:20 mg in 1 g
Approved: 2023/02/07
NDC:72189-422
Ketoconazole
Manufacturer:A-S Medication Solutions
Route:TOPICAL
Strength:20 mg in 1 g
Approved: 2017/05/17
NDC:50090-1524
Ketoconazole
Manufacturer:Proficient Rx LP
Route:TOPICAL
Strength:20 mg in 1 mL
Approved: 2022/11/01
NDC:71205-105

Singapore Approved Products

FORMYCO TOPICAL CREAM 20 mg/g
Manufacturer:PT. CAPRIFARMINDO LABORATORIES
Form:CREAM
Strength:20 mg/g
Online:Yes
Approved: 1999/07/13
Approval:SIN11020P
NITOZOL CREAM 2%
Manufacturer:KOREA PHARMA CO LTD
Form:CREAM
Strength:2%
Online:Yes
Approved: 1998/11/03
Approval:SIN10369P
KETOCONAZOLE TABLETS 200 mg
Manufacturer:HOVID BHD, HOVID Bhd.
Form:TABLET
Strength:200MG
Online:Yes
Approved: 1999/05/31
Approval:SIN10955P
KEZORAL TABLET 200 mg
Manufacturer:DUOPHARMA MANUFACTURING (BANGI) SDN.BHD.
Form:TABLET
Strength:200 mg
Online:Yes
Approved: 2002/12/23
Approval:SIN12152P
YUCOMY CREAM 20MG/G
Manufacturer:Y.S.P. Industries (M) Sdn. Bhd.
Form:CREAM
Strength:20mg/g
Online:Yes
Approved: 2019/08/07
Approval:SIN15770P

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