Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Cream, External:
Generic: 2% (15 g, 30 g, 60 g)
Foam, External:
Extina: 2% (50 g [DSC], 100 g [DSC]) [contains alcohol, usp, cetyl alcohol, propylene glycol]
Extina: 2% (50 g, 100 g) [cfc free; contains alcohol, usp, cetyl alcohol, propylene glycol]
Ketodan: 2% (100 g) [contains alcohol, usp, cetyl alcohol, propylene glycol]
Generic: 2% (50 g, 100 g)
Gel, External:
Xolegel: 2% (45 g) [contains alcohol, usp, fd&c yellow #10 (quinoline yellow), fd&c yellow #6 (sunset yellow), propylene glycol]
Kit, External:
Ketodan: 2% [contains cetyl alcohol, edetate disodium, propylene glycol]
Shampoo, External:
Nizoral: 2% (120 mL) [contains fd&c red #40]
Nizoral A-D: 1% (125 mL, 200 mL)
Nizoral A-D: 1% (125 mL, 200 mL) [contains brilliant blue fcf (fd&c blue #1), edetate sodium (tetrasodium)]
Generic: 2% (120 mL)
Pharmacology
Mechanism of Action
Alters the permeability of the cell wall by blocking fungal cytochrome P450; inhibits biosynthesis of triglycerides and phospholipids by fungi; inhibits several fungal enzymes that results in a build-up of toxic concentrations of hydrogen peroxide; also inhibits androgen synthesis
Pharmacokinetics/Pharmacodynamics
Absorption
Shampoo: None; Cream, Foam, Gel: Minimal
Use: Labeled Indications
Cream: Treatment of tinea corporis (ringworm), tinea cruris (jock itch), and tinea pedis (athlete's foot) caused by Trichophyton rubrum, Trichophyton mentagrophytes, and Epidermophyton floccosum; treatment of tinea (pityriasis) versicolor caused by Pityrosporum orbiculare (also known as Malassezia furfur); treatment of cutaneous candidiasis caused by Candida sp; treatment of seborrheic dermatitis
Foam, gel: Treatment of seborrheic dermatitis in immunocompetent adults and children 12 years and older
Limitations of use: Safety and efficacy for the treatment of fungal infections have not been established.
Shampoo:
US labeling: Treatment of tinea versicolor caused by or presumed to be caused by P. orbiculare (M. furfur or Malassezia orbiculare)
Canadian labeling: Treatment and prophylaxis of conditions caused by Pityrosporum (eg, pityriasis capitis [dandruff]); treatment of seborrheic dermatitis
OTC labeling: Controls flaking, scaling, and itching associated with dandruff
Contraindications
Hypersensitivity to ketoconazole or any component of the formulation.
OTC labeling: When used for self-medication, do not use on scalp that is broken or inflamed.
Documentation of allergenic cross-reactivity for azole antifungals is limited. However, because of similarities in chemical structure and/or pharmacologic actions, the possibility of cross-sensitivity cannot be ruled out with certainty.
Dosage and Administration
Dosing: Adult
Cutaneous candidiasis: Topical: Cream: Apply once daily to cover the affected and immediate surrounding area for 2 weeks. Note: Canadian labeling recommends a duration of 2 to 3 weeks.
Dandruff: Topical:
Shampoo 1% (OTC labeling): Apply to wet hair, lather, and rinse thoroughly; repeat. Use every 3 to 4 days for up to 8 weeks; then apply only as needed to control dandruff.
Shampoo 2% (Canadian product only): Apply 5 to 10 mL to wet scalp, lather, leave on 3 to 5 minutes, and rinse; apply once every 1 to 2 weeks (prophylaxis) or twice weekly for 2 to 4 weeks (treatment).
Seborrheic dermatitis: Topical:
Cream: Apply to the affected area twice daily for 4 weeks or until clinical response is noted
Foam: Apply to affected area twice daily for 4 weeks
Gel: Apply to the affected area once daily for 2 weeks
Shampoo 2% (Canadian product only; OTC labeling): Apply 5 to 10 mL to wet scalp, lather, leave on 3 to 5 minutes, and rinse; apply twice weekly for 2 to 4 weeks.
Tinea corporis, tinea cruris, tinea pedis: Topical: Cream: Apply to the affected and immediate surrounding area once daily.
Duration of treatment:
US labeling: Tinea corporis, cruris: 2 weeks; tinea pedis: 6 weeks.
Canadian labeling: Tinea corporis: 3 to 4 weeks; tinea cruris: 2 to 4 weeks; tinea pedis: 4 to 6 weeks.
Tinea versicolor: Topical:
Cream: Apply once daily to cover the affected and immediate surrounding area for 2 weeks. Note: Canadian labeling recommends a duration of 2 to 3 weeks.
Shampoo 2%: Apply to affected area of damp skin, lather, leave on 5 minutes, and rinse (one application is usually sufficient)
Dosing: Geriatric
Refer to adult dosing.
Dosing: Pediatric
Dandruff (flaking, scaling, and itching):
Shampoo (ketoconazole 1%): Children ≥12 years and Adolescents: Topical: OTC labeling: Shampoo every 3 to 4 days for up to 8 weeks; then use only as needed to control dandruff
Shampoo (ketoconazole 2%): Canadian labeling: Children ≥12 years and Adolescents: Topical:
Prophylaxis: Shampoo with 5 to 10 mL once every 1 to 2 weeks
Treatment: Shampoo with 5 to 10 mL twice weekly for 2 to 4 weeks
Seborrheic dermatitis:
Foam: Children ≥12 years and Adolescents: Topical: Apply to affected area twice daily for 4 weeks
Gel: Children ≥12 years and Adolescents: Topical: Apply to affected area once daily for 2 weeks
Shampoo (ketoconazole 2%): Canadian labeling: Children ≥12 years and Adolescents: Topical: Shampoo with 5 to 10 mL twice weekly for 2 to 4 weeks
Administration
Topical: For external use only; not for ophthalmic, oral, or intravaginal use. Avoid contact with the eyes and other mucous membranes. Wash hands after application.
Cream: Apply to the affected and immediate surrounding area.
Foam: Dispense foam into the cap of the can or other cool surface; do not dispense directly onto hands (foam will begin to melt upon contact with warm skin). Pick up small amounts of foam with the fingertips and gently massage into the affected area until the foam disappears. For hair-bearing areas, part the hair so that foam may be applied directly to the skin (rather than on the hair). Avoid exposure to flame or smoking during and immediately following application.
Gel: Apply a thin layer to affected area with fingertips. Do not wash affected area for at least 3 hours after application; wait at least 20 minutes after gel application before applying makeup or sunscreen to the treated areas.
Shampoo:
Thoroughly wet affected area, apply shampoo, lather generously, and rinse thoroughly; the Canadian labeling recommends leaving on for 3 to 5 minutes before rinsing. Do not use on areas that are broken or inflamed.
For tinea versicolor, apply shampoo to damp skin of the affected area; leave on skin for 5 minutes before rinsing.
Storage
Cream: Store at <25°C (<77°F).
Foam: Store at 20°C to 25°C (68°F to 77°F). Do not refrigerate. Do not expose container to heat and/or store at >49°C (120°F). Do not store in direct sunlight. Contents are flammable; do not puncture or incinerate.
Gel: Store at 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F). Contents are flammable; avoid fire, flame, or smoking during and immediately following application.
Shampoo:
Rx: Store at ≤25°C (≤77°F). Protect from light.
OTC: Store at 2°C to 30°C (35°F to 86°F); protect from light and freezing.
Drug Interactions
There are no known significant interactions.
Adverse Reactions
1% to 10%:
Dermatologic: Application-site pruritus (cream: ≤5%; shampoo: 1% to 3%; foam, gel: <1%), stinging of the skin (cream: ≤5%), xeroderma (shampoo: 1% to 3%; foam, gel: <1%)
Local: Application site reaction (foam: 6%; shampoo: 1% to 3%), local irritation (cream: ≤5%; foam, shampoo <1%), application site burning (gel: 4%; foam, shampoo: <1%)
Frequency not defined: Dermatologic: Dry hair, dry scalp, oily hair
<1%, postmarketing, and/or case reports: Abnormal hair texture, acne vulgaris, alopecia, anaphylaxis, angioedema, application-site dermatitis, application site discharge, application site erythema, application site pain, cheilitis, contact dermatitis, dizziness, eye irritation, facial swelling, hair discoloration, headache, hypersensitivity reaction, impetigo, keratoconjunctivitis sicca, localized warm feeling, nail discoloration, pain, paresthesia, pyogenic granuloma, skin irritation, skin rash, swelling of eye, urticaria
Warnings/Precautions
Concerns related to adverse effects:
- Hypersensitivity reactions: Severe hypersensitivity reactions, including contact sensitization, photoallergenicity, and anaphylaxis (rare) have been reported; discontinue use if hypersensitivity occurs.
- Irritation: May cause irritation at the site of application; discontinue use if irritation occurs.
Dosage form specific issues:
- Foam: Formulation contains alcohol and propane/butane; do not expose to open flame and/or smoking during or immediately after application. Do not puncture and/or incinerate container.
- Gel: Flammable; avoid exposure to fire, flames, or smoking during or immediately after application.
- Shampoo: Use may remove curl from permanently wavy hair, cause hair discoloration, and changes in hair texture.
- Sulfites: Some dosage forms contain sulfites which may cause allergic-type reactions (including anaphylaxis) as well as life-threatening or less severe asthmatic episodes in certain individuals.
Other warnings/precautions:
- Appropriate use: Avoid contact with the eyes and other mucous membranes. Not for ophthalmic, oral, or intravaginal use. If condition worsens or does not improve after the treatment period, discontinue use and contact health care provider.
Pregnancy
Pregnancy Considerations
Ketoconazole is not detectable in the plasma following chronic use of the shampoo.
Topical ketoconazole may be used for the treatment of infectious atopic dermatitis complications in pregnant women (Vestergaard 2019).
Patient Education
What is this drug used for?
- It is used to treat fungal infections of the skin.
- It is used to control seborrheic dermatitis.
- It is used to treat dandruff.
Frequently reported side effects of this drug
- Burning
- Straight hair
- Hair loss
- Itching
- Dry skin
- Change in hair texture
- Hair discoloration
Other side effects of this drug: Talk with your doctor right away if you have any of these signs of:
- Severe application site irritation or redness
- Signs of a significant reaction like wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat.
Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.
Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about this medicine. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using this medicine.
