Ketoconazole (Nizoral) for topical use comes in shampoo, cream, and gel forms. It is employed to treat skin diseases brought on by fungi.

Topical Ketoconazole Uses:

• Cream:

  • An antifungal drug called ketoconazole is offered as a cream. It is used to treat tinea corporis, tinea cruris, and tinea pedis, which are skin conditions brought on by the fungi Trichophyton rubrum, Trichophyton mentagrophytes, and Epidermophyton floccosum;
  • Additionally, it is used to treat seborrheic dermatitis, cutaneous candidiasis caused by Candida sp., and tinea versicolor, also known as pityriasis versicolor, which is brought on by Pityrosporum orbiculare (also known as Malassezia furfur).

• Foam, gel:

  • Treatment of seborrheic dermatitis with ketoconazole in the form of foam and gel in healthy individuals with good immunity and children 12 years of age and older 
  • Restrictions on use: The effectiveness and safety of treating fungi-related infections have not been shown.

• Shampoo:

  • US labels state that Pityrosporum orbiculare, which is thought to be the cause of tinea versicolor, can be treated with ketoconazole shampoo ( also known as Malassezia furfur or Malassezia orbiculare) 
  • Canadian labeling:  Treatment of seborrheic dermatitis and illnesses brought on by Pityrosporum, such as pityriasis capitis (dandruff). 
  • OTC labeling: dandruff-related flakes, scaling, and itching are reduced.

Topical Ketoconazole (Nizoral) Dose in Adults:

Topical Ketoconazole (Nizoral) Dose in the therapy of Cutaneous candidiasis:

• Topical:

  • Cream:

    • Apply once daily for two weeks to the afflicted region and its surroundings.
    • Note: Canadian labeling recommends a duration of 2 to 3 weeks.

Topical Ketoconazole (Nizoral) Dose in the treatment of Dandruff: Topical:

• Shampoo 1% (OTC labeling):

  • Apply a tiny amount to wet hair, lather, let sit for a short while, and then thoroughly rinse; repeat. Use once every three to four days for up to eight weeks; after that, only use when necessary to control dandruff.

• Shampoo 2% (Canadian product only):

  • Apply 5 to 10 mL to a damp scalp, lather, let sit for 3 to 5 minutes, and then thoroughly rinse. Do this once every 1 to 2 weeks for prophylaxis, or twice a week for 2 to 4 weeks for treatment.

Topical Ketoconazole (Nizoral) Dose in the therapy of Seborrheic dermatitis: Topical:

• Cream:

  • Apply to the affected area twice daily for four weeks, or until a noticeable clinical response.

• Foam:

  • Apply twice daily for four weeks to the afflicted region and its surroundings.

• Gel:

  • Apply once daily for two weeks to the afflicted region.

• Shampoo 2% (Canadian product only; OTC labeling):

  • Apply 5 to 10 mL to a damp scalp, lather, let sit for 3 to 5 minutes, then thoroughly rinse. Do this twice per week for 2 to 4 weeks.

Tinea corporis, tinea cruris, and tinea pedis treatment with topical ketoconazole (Nizoral) dose:

• Topical:

  • Cream:

    • Apply once daily to the affected region and its immediate surroundings. 

Duration of treatment:

• US labeling:

  • Tinea corporis and cruris are treated with it for two weeks, while tinea pedia is treated with it for up to six weeks.

• Canadian labeling:

  • Tinea pedis: 4-6 weeks.
  • For treatment of Tinea corporis up to 3 to 4 weeks
  • Tinea cruris: 2-4 weeks
  • Tinea versicolor: Topical:
    • Shampoo 2%: apply 5 to 10 ml to damp skin in the affected area, lather, let sit for 5 minutes, and then thoroughly rinse (one application is usually sufficient)
    • Cream: For two weeks, apply once daily to the affected area and its immediate surroundings. Note: The period of 2 to 3 weeks is advised by Canadian labelling. 

Topical Ketoconazole (Nizoral) Dose in Childrens:

Topical Ketoconazole (Nizoral) Dose in the therapy of Dandruff (flaking, scaling, and itching):

• Shampoo (ketoconazole 1%):

  • Children ≥12 years and Adolescents:
    • Topical: Shampoo after every three to four days for up to eight weeks; use only as necessary to control dandruff after that.

• Shampoo (ketoconazole 2%): Canadian labeling:

  • Children ≥12 years and Adolescents: Topical:
    • Prophylaxis: Apply the shampoo 5 to 10 mL once every 1 to 2 weeks
    • Treatment: Shampoo with 5 to 10 mL twice weekly for 2 to 4 weeks

Topical Ketoconazole (Nizoral) Dose in the treatment of Seborrheic dermatitis:

• Foam:

  • Children ≥12 years and Adolescents:
    • Topical: Apply to the affected area twice daily for 4 weeks

• Gel:

  • Children over 12 years and Adolescents:
    • Topical: For two weeks, apply to the afflicted region once daily.

• Shampoo (ketoconazole 2%): Canadian labeling:

  • Children over 12 years and Adolescents:
    • Topical: For two to four weeks, shampoo with 5 to 10 mL twice a week.

Pregnancy Risk Category: C

• After prolonged use of the shampoo, Ketoconazole is no longer detectable in blood.
• For the treatment of atopic dermatitis in pregnant women, topical ketoconazole can be used (Vestergaard 2019,).

Use during breastfeeding:

• After oral administration, breast milk secretes Ketoconazole.
• The shampoo is not found in plasma after prolonged use.
• Plasma concentrations following application are approximately 250 times that of oral dosing.
• Manufacturers recommend that mothers breastfeed while on therapy.
• They also advise that they consider the risks to infants and the benefits to mother and baby.
• Avoid direct contact with breastfeeding infants by not applying to their nipples or surrounding areas.

Dose in Kidney Disease:

No dosage modifications are necessary (and are not included in the manufacturer's labelling). However, due to limited systemic absorption, dosage modification is improbable.

Dose in Liver disease:

There is no requirement to change the dosage (no dosage adjustments have been provided by the manufacturer). However, due to limited systemic absorption, dosage modification is improbable.

Side Effects of Topical Ketoconazole (Nizoral):

• Dermatologic:

  • Application-Site Pruritus
  • Stinging Of The Skin
  • Xeroderma

• Local:

  • Application Site Reaction
  • Local Irritation
  • Application Site Burning

Frequency of side effects not defined:

• Dermatologic:

  • Dry hair
  • Dry scalp
  • Oily hair

Contraindications to Topical Ketoconazole (Nizoral):

• Allergy to ketoconazole and any component of the formulation

OTC labeling:

• Do not apply to a scalp that is inflamed or broken if you are using it for self-medication.
• There is not much evidence of cross-reactivity between azole antifungals and allergenic azole antifungals. 
• Cross-sensitivity is possible due to similarities in chemical structure or pharmacologic effects.

Warnings and precautions

• Hypersensitivity reactions

  • If you experience severe allergic reactions (photoallergenicity, contact sensitization and rare anaphylaxis), discontinue using the product.

• Irritation

  • It can cause irritation at the application site.
  • If irritation occurs, discontinue use.

Monitoring Parameters:

None mentioned.

How to administer Topical Ketoconazole (Nizoral)?

Topical:

• It is only intended for usage outside. You shouldn't use it for intravaginal, ophthalmic, or oral use. Stay away from touching your eyes and other mucous membranes. Wash your hands after using.

Cream:

• Use in the impacted region and its immediate surroundings.

Foam:

• The foam should be applied to the can's lid or other cool surfaces. 
• Never pour directly into hands (foam will begin to melt upon contact with warm skin). 
• With your fingertips, gently massage the affected region while picking up little amounts of foam. Continue doing this until the foam is gone. 
• Part the hair to allow for the direct application of foam to the skin in hair-bearing areas (rather than on the hair). 
• Avoid being around flames or smoking both when applying and right after.

Gel:

• With your fingertips, apply a small layer to the affected region. 
• After using the gel, wait at least 20 minutes before putting makeup or sunscreen to the treated regions. Do not wash the affected area for at least 3 hours.

Shampoo:

• Wet the affected area completely, use shampoo, generously lather, and then thoroughly rinse (the Canadian labelling recommends leaving on for 3 to 5 minutes before rinsing). 
• Use sparingly on broken or irritated skin.

Apply shampoo to damp skin in the affected area to treat tinea versicolor. Let the shampoo sit on the skin for five minutes before rinsing.

Mechanism of action of Topical Ketoconazole (Nizoral):

• It reduces cell wall permeability by blocking fungal Cytochrome P450. 
• It can also block the biosynthesis of phospholipids and triglycerides by fungal enzymes, which results in toxic levels of hydrogen peroxide. It also inhibits androgen production.

Absorption:

• Shampoo: None;
• Cream, Foam, Gel: Minimal

International Brand Names of Topical Ketoconazole:

• Extina
• Ketodan
• Nizoral
• Nizoral A-D
• Xolegel
• Ketoderm
• Amfazol
• Apodruff
• Aquarius
• Arcolane
• Curazole
• DaktaGOLD
• Danfree
• Dangel
• Dermatin
• Dermazole
• Dezor
• Dezor Cream
• Dezor Kem
• Dezor Shampoo
• Diazon
• Erazol
• Faction
• Fitonal
• Formyco
• Fundan
• Fungarest
• Fungaway
• Fungiderm-K
• Fungium
• Fungoral
• Kenazole
• Ketazol
• Ketoco
• Ketoconazol
• Ketoderm
• Ketogin
• Ketoisdin
• Ketona
• Ketopine
• Ketozol
• Ketozol Shampoo
• Kezon
• Larry
• Micoral
• Micosin
• Mikanisal
• Mycofebrin
• Mycoral
• Nazole
• Nicoziral Cream
• Niz Creme
• Niz Shampoo
• Nizapex
• Nizoral
• Nizoral 2% Cream
• Nizoral Cream
• Nizoral Shampoo
• Oronazol
• Panfungol
• Pikangwang
• Pranzole
• Pristine
• Pristinex
• Reduff
• Resolve
• Sebizole
• Sporaxyl
• Sporium
• Terzolin
• Triatop Lotion
• Yucomy
• Zakan
• Zhoulixin

Topical Ketoconazole Brand Names in Pakistan:

• Nizoral (Janssen Pharma)
• Conaz (Atco Pharma)
• Ketco
• Ketorex
• Ketagen
• Hyseke
• Ketone
• Ketonaz