MedPath

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:A-S Medication Solutions
Route:TOPICAL
Strength:20 mg in 1 mL
Approved: 2022/03/28
NDC:50090-3288
Ketoconazole
Manufacturer:Encube Ethicals Private Limited
Route:TOPICAL
Strength:20 mg in 1 g
Approved: 2021/05/27
NDC:21922-025
Ketoconazole
Manufacturer:Preferred Pharmaceuticals Inc.
Route:TOPICAL
Strength:20 mg in 1 g
Approved: 2023/07/17
NDC:68788-8233
KETOCONAZOLE
Manufacturer:NuCare Pharmaceuticals,Inc.
Route:ORAL
Strength:200 mg in 1 1
Approved: 2022/03/17
NDC:66267-400
Ketoconazole
Manufacturer:RPK Pharmaceuticals, Inc.
Route:TOPICAL
Strength:20 mg in 1 g
Approved: 2017/05/17
NDC:53002-8150

Singapore Approved Products

NIZORAL SHAMPOO 20 mg/g
Manufacturer:OLIC (THAILAND) LIMITED
Form:SHAMPOO
Strength:20 mg/g
Online:Yes
Approved: 1990/07/10
Approval:SIN04926P
YUCOMY SHAMPOO 2% W/W
Manufacturer:Y.S.P. Industries (M) Sdn. Bhd.
Form:SHAMPOO
Strength:20mg/g
Online:Yes
Approved: 2020/08/17
Approval:SIN15990P
SUNAZOL CREAM 2% w/w
Manufacturer:SUNWARD PHARMACEUTICAL PRIVATE LIMITED
Form:CREAM
Strength:2% w/w
Online:Yes
Approved: 1998/08/05
Approval:SIN09929P
ANTANAZOL CREAM 2%
Manufacturer:SHIN POONG PHARMACEUTICAL CO LTD
Form:CREAM
Strength:2%
Online:Yes
Approved: 1995/02/04
Approval:SIN07997P
DEZOR SHAMPOO 2 % w/v
Manufacturer:HOE PHARMACEUTICALS SDN BHD
Form:SHAMPOO
Strength:2.00 % w/v
Online:Yes
Approved: 2001/07/07
Approval:SIN11580P

Drug Development Updates

Stay informed with timely notifications on clinical trials and research advancements.

© Copyright 2025. All Rights Reserved by MedPath