Ketoconazole Cream, 2% | Ketoconazole

00:54 EDT 27th August 2014 | BioPortfolio
Note: While we endeavour to keep our records up-to-date one should not rely on these details being accurate without first consulting a professional. Click here to read our full medical disclaimer.

Rx only

Ketoconazole cream, 2% contains the broad-spectrum synthetic antifungal agent, ketoconazole 2%, formulated in an aqueous cream vehicle consisting of butylated hydroxyanisole (BHA), cetyl alcohol, isopropyl myristate, polysorbate 60, polysorbate 80, propylene glycol, purified water, sorbitan monostearate and stearyl alcohol.

Ketoconazole is cis-1-acetyl-4-[4-[[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl] piperazine and has the following structural formula:

Molecular Formula: CHClNO

Molecular Weight: 531.43

IMAGE ketoconazole-01.jpg

When ketoconazole cream, 2% was applied dermally to intact or abraded skin of beagle dogs for 28 consecutive days at a dose of 80 mg, there were no detectable plasma levels using an assay method having a lower detection limit of 2 ng/mL.

After a single topical application to the chest, back and arms of normal volunteers, systemic absorption of ketoconazole was not detected at the 5 ng/mL level in blood over a 72-hour period.

Two dermal irritancy studies, a human sensitization test, a phototoxicity study and a photoallergy study conducted in 38 male and 62 female volunteers showed no contact sensitization of the delayed hypersensitivity type, no irritation, no phototoxicity and no photoallergenic potential due to ketoconazole cream, 2%.

Ketoconazole is a broad spectrum synthetic antifungal agent which inhibits the in vitro growth of the following common dermatophytes and yeasts by altering the permeability of the cell membrane: dermatophytes: Trichophyton rubrum, T. mentagrophytes, T. tonsurans, Microsporum canis, M. audouini, M. gypseum and Epidermophyton floccosum; yeasts: Candida albicans, Malassezia ovale (Pityrosporum ovale) and C. tropicalis; and the organism responsible for tinea versicolor, Malassezia furfur (Pityrosporum orbiculare). Only those organisms listed in the INDICATIONS AND USAGE section have been proven to be clinically affected. Development of resistance to ketoconazole has not been reported.

In vitro studies suggest that ketoconazole impairs the synthesis of ergosterol, which is a vital component of fungal cell membranes. It is postulated that the therapeutic effect of ketoconazole in seborrheic dermatitis is due to the reduction of M. ovale, but this has not been proven.

Ketoconazole cream, 2% is indicated for the topical treatment of tinea corporis, tinea cruris and tinea pedis caused by Trichophyton rubrum, T. mentagrophytes and Epidermophyton floccosum; in the treatment of tinea (pityriasis) versicolor caused by Malassezia furfur (Pityrosporum orbiculare); in the treatment of cutaneous candidiasis caused by Candida spp. and in the treatment of seborrheic dermatitis.

Ketoconazole cream, 2% is contraindicated in persons who have shown hypersensitivity to the active or excipient ingredients of this formulation.

Ketoconazole cream, 2% is not for ophthalmic use.

If a reaction suggesting sensitivity or chemical irritation should occur, use of the medication should be discontinued. Hepatitis (1:10,000 reported incidence) and, at high doses, lowered testosterone and ACTH induced corticosteroid serum levels have been seen with orally administered ketoconazole; these effects have not been seen with topical ketoconazole.

A long-term feeding study in Swiss Albino mice and in Wistar rats showed no evidence of oncogenic activity. The dominant lethal mutation test in male and female mice revealed that single oral doses of ketoconazole as high as 80 mg/kg produced no mutation in any stage of germ cell development. The Ames' salmonella microsomal activator assay was also negative.

Ketoconazole has been shown to be teratogenic (syndactylia and oligodactylia) in the rat when given orally in the diet at 80 mg/kg/day, (10 times the maximum recommended human oral dose). However, these effects may be related to maternal toxicity, which was seen at this and higher dose levels.

There are no adequate and well-controlled studies in pregnant women. Ketoconazole should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

It is not known whether Ketoconazole cream, 2% administered topically could result in sufficient systemic absorption to produce detectable quantities in breast milk. Nevertheless, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.

Safety and effectiveness in children have not been established.

During clinical trials 45 (5.0%) of 905 patients treated with ketoconazole cream, 2% and 5 (2.4%) of 208 patients treated with placebo reported side effects consisting mainly of severe irritation, pruritus and stinging. One of the patients treated with ketoconazole cream developed a painful allergic reaction.

In worldwide postmarketing experience, rare reports of contact dermatitis have been associated with ketoconazole cream or one of its excipients, namely propylene glycol.

It is recommended that ketoconazole cream, 2% be applied once daily to cover the affected and immediate surrounding area. Clinical improvement may be seen fairly soon after treatment is begun; however, candidal infections and tinea cruris and corporis should be treated for two weeks in order to reduce the possibility of recurrence.

Patients with tinea versicolor usually require two weeks of treatment. Patients with tinea pedis require six weeks of treatment.

Ketoconazole cream, 2% should be applied to the affected area twice daily for four weeks or until clinical clearing.

If a patient shows no clinical improvement after the treatment period, the diagnosis should be redetermined.

Ketoconazole cream, 2% is supplied in 15 g (NDC 51672-1298-1), 30 g (NDC 51672-1298-2), and 60 g (NDC 51672-1298-3) tubes.

Store at 20°-25°C (68°-77°F) [see USP Controlled Room Temperature].

Mfd. by:Taro Pharmaceuticals Inc., Brampton, Ontario, Canada L6T 1C1

Dist. by: Taro Pharmaceuticals U.S.A., Inc., Hawthorne, NY 10532

Revised: June, 2005


NDC 51672-1298-1

15 g

KetoconazoleCream 2%


Rx only

Keep this and all medications out of the reach of children.


IMAGE ketoconazole-02.jpg


Taro Pharmaceuticals U.S.A., Inc.

Active Ingredients


Drugs and Medications [33 Associated Drugs and Medications listed on BioPortfolio]

Xolegel [Stiefel Laboratories Inc]


Nizoral [McNeil Consumer Healthcare Div. McNeil-PPC, Inc]


Ketoconazole [Tiber Laboratories]

Ketoconazole Cream, 2%

Ketoconazole [Rebel Distributors Corp]

Ketoconazole Cream, 2%

Ketoconazole [Teva Pharmaceuticals USA Inc]


Clinical Trials [68 Associated Clinical Trials listed on BioPortfolio]

Use of Low Dose Ketoconazole in Prostate Cancer That Does Not Respond to Hormone Therapy and Prior Chemotherapy

The purpose of this study is to test the safety of ketoconazole and how well it works after chemotherapy has been used. Ketoconazole at lower doses has been used for fungal infections howe...

Effect of Ketoconazole on Biliary Excretion of AZD0837

This is an explorative study and the scientific question to be investigated is if the biliary excretion of AZD0837 and its metabolites AR-H069927XX and AR-H067637XX are affected by co-admi...

Trial for Studying Pharmacokinetic Effects of Ketoconazole on CG100649

This is a Phase I, open-labeled, randomization and 2x2 Cross trial to compare the pharmacokinetic effects between ketoconazole and CG100649 for healthy male volunteers.

A Study to Assess the Effect of Ketoconazole on the Metabolism of ABT-263 (Navitoclax).

This is a single dose, open-label, single or multiple center study to determine the interaction of ketoconazole with ABT-263 in approximately 12 subjects with cancer.

Relative Bioavailability of of Olodaterol and Ketoconazole

This clinical trial is intended to investigate a possible effect of the p-gp inhibitor ketoconazole on the bioavailability of olodaterol

PubMed Articles [28 Associated PubMed Articles listed on BioPortfolio]

Impurities contained in antifungal drug ketoconazole are potent activators of human aryl hydrocarbon receptor.

Antifungal drug ketoconazole is a mixture of (+)/(-) cis-enantiomers, which also contains several impurities. Ketoconazole was identified as an activator of aryl hydrocarbon receptor AhR by three inde...

The Rise and Fall of Oral Ketoconazole.

Ketoconazole was the first broad-spectrum oral antifungal agent available to treat systemic and superficial mycoses. Evidence of hepatotoxicity associated with its use emerged within the first few yea...

Pharmacokinetic interaction of intravenous fentanyl with ketoconazole.

Fentanyl is primarily metabolized by CYP3A, but has also been suggested to act as a weak inhibitor of CYP3A. We investigated the influence of CYP3A inhibition by ketoconazole on the pharmacokinetics o...

Ketoconazole-Induced Sweet Syndrome: A New Association.

: Sweet syndrome (SS) is an acute febrile neutrophilic dermatosis that can be associated with malignancy and medications. A 60-year-old man presented with erythematous, edematous, and ulcerated plaque...

No untoward effect of long-term ketoconazole administration on electrocardiographic qt interval in patients with cushing's disease.

Ketoconazole is listed among drugs which prolong QT interval and may increase the risk of torsade de pointes, a severe ventricular arrhythmia. This compound has recently been approved for treatment of...


Relevant Topics

Wound management
Latest News Clinical Trials Research Drugs Reports Corporate
Anything that breaks the skin is a wound because when the skin is broken, there's a risk of germs getting into the body and causing an infection. Follow and track Wound Care News on BioPortfolio: Wound Car...

Latest News Clinical Trials Research Drugs Reports Corporate
Blood is a specialized bodily fluid that delivers necessary substances to the body's cells (in animals) – such as nutrients and oxygen – and transports waste products away from those same cells.  In vertebrates, it is composed of blo...

Latest News Clinical Trials Research Drugs Reports Corporate
An assay is an analytic procedure for qualitatively assessing or quantitatively measuring the presence or amount or the functional activity of a target entity.  This can be a drug or biochemical substance or a cell in an organism or organic sample. ...

Drugs and Medication Quicklinks

Searches Linking to this Drug Record