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Brand Name :
Xolegel, Nizoral Topical, Extina, Ketozole
Synonyms :
ketoconazole topical
Class :
Antifungals, Topicals
Dosage forms and strengths
Shampoo
2%
1%
Foam/cream/gel
2%
Cream- apply every 12 hours for a duration of 4 weeks until clear
Shampoo-use the shampoo twice a week over a period of 4 weeks
maintain gap of at least three days between each application
Foam- apply every 12 hours to the affected area for a duration of 4 weeks
Gel-Apply once daily to the affected area for a duration of two weeks
Foam 2%: Apply 2 times daily 4 weeks
Cream 2%: Apply 2 times daily 4 weeks
Shampoo: Apply 2 times weekly 4 weeks, with a minimum 3-day interval between each shampoo
Gel 2%: Apply once per day 2 weeks
Shampoo 1%: Apply and repeat between 3-4 days 8 weeks
Shampoo 2%: Apply to wet skin around the afflicted region, lather and for wait five minutes then rinse
Cream 2%: Apply once per day 2 weeks
Cream 2%: Apply daily 2 weeks (for tinea pedis continue 6 weeks)
Dosage forms and strengths
Shampoo
2%
1%
foam /cream/gel
2%
Foam 2%: Apply 2 times daily 4 weeks
Cream 2%: Apply 2 times daily 4 weeks
Shampoo: Apply 2 times weekly 4 weeks, with a minimum 3-day interval between each shampoo
Gel 2%: Apply once per day 2 weeks
Shampoo 2%: Apply to wet skin around the afflicted region, lather and for wait five minutes then rinse
Cream 2%: Apply once per day 2 weeks
Cream 2%: Apply daily 2 weeks (for tinea pedis continue 6 weeks)
Refer adult dosing
Actions and Spectrum
Action: Ketoconazole topical is a medication that belongs to the class of antifungal drugs. It exerts its action by inhibiting the synthesis of ergosterol, a key component of the fungal cell membrane. By doing so, drug disrupts the integrity of the fungal cell membrane, leading to its weakening and eventual death. This antifungal action helps treat various fungal skin infections, such as athlete’s foot, jock itch, and ringworm.
Spectrum: Drug primarily targets dermatophytes, which are fungi that cause infections of the skin, hair, and nails. It is effective against various species of dermatophytes, including Trichophyton, Microsporum, and Epidermophyton. These fungi commonly cause fungal infections of the skin, such as tinea infections (ringworm) and fungal nail infections.
Frequency defined
1-10%
Pruritus
Irritation, severe
Stinging
Frequency Not Defined
Shampoo
Oiliness/dryness of hair and scalp
Abnormal hair texture
Scalp pustules
Irritation
Dry skin
Hair loss/alopecia
Pruritus
Black Box Warning:
None
Contraindication/Caution:
Hypersensitivity: Individuals known to have a hypersensitivity or allergy to ketoconazole or any other ingredients in the topical formulation should avoid its use.
Pre-existing liver disease: Drug can potentially cause liver damage, and its use should be avoided or used with caution in individuals with pre-existing liver disease or impaired liver function. Regular monitoring of liver function may be necessary in such cases.
Pregnancy and breast-feeding: The safety of ketoconazole topical has not been well established during pregnancy and breast-feeding. It is generally recommended to avoid its use during these periods unless specifically prescribed by a healthcare professional.
Children: While ketoconazole topical is commonly used in pediatric patients for certain fungal infections, the specific age limits and safety profiles may vary depending on the formulation. Following the instructions and consult a healthcare professional for appropriate use in children is essential.
Drug interactions: Drug can interact with certain medications, including certain oral anticoagulants (blood thinners), statins (cholesterol-lowering drugs), and specific immunosuppressants. To avoid potential drug interactions, you must inform your healthcare provider about all your medications.
Eye and mucous membrane contact:
Drug formulations are specifically formulated for external application and must not be exposed to the eyes or mucous membranes. In the event of unintended contact, it is crucial to promptly wash away the substance with water.
Pregnancy warnings:
Pregnancy category: AU TGA pregnancy category: B3
US FDA pregnancy category: C
Lactation: Excreted into human milk is unknown
Pregnancy Categories:
Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester.
Category B: There were a lack of studies on pregnant women and no evidence of risk to the fetus in animal experiments.
Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.
Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.
Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.
Category N: There is no data available for the drug under this category
Pharmacology:
Ketoconazole, an antifungal medication, is frequently applied topically to cure different fungal skin infections, including athlete’s foot, ringworm, and jock itch. It falls under the category of azole antifungals, a group of drugs commonly used for this purpose.
Pharmacodynamics:
The drug functions by inhibiting the production of ergosterol, a vital element found in the cell membrane of fungi. Its specific focus is on the enzyme lanosterol 14α-demethylase, which facilitates the conversion of lanosterol into ergosterol. Through its inhibition of this enzyme, ketoconazole interferes with the normal structure and operation of the fungal cell membrane, ultimately resulting in the demise of the fungal cells.
Pharmacokinetics:
Absorption
When applied topically, drug can penetrate the layers of the skin to reach the site of infection. The drug absorption through the skin is generally low, but it can be enhanced by using formulations with penetration enhancers.
Distribution
Drug can enter the systemic circulation to some extent. However, the systemic exposure is minimal when ketoconazole is used topically due to its low absorption.
Metabolism
Drug undergoes extensive metabolism in the liver. The primary metabolic pathway for this substance involves the cytochrome P450 enzyme system, particularly CYP3A4. The metabolism of drug can result in the formation of several metabolites.
Excretion and Elimination
The metabolites of drug and a small portion of unchanged drug are excreted primarily in the feces (via biliary excretion) and to a lesser extent in urine. The elimination half-life of ketoconazole after topical administration is generally short.
Administration:
Apply a thin layer: Take enough ketoconazole cream or other topical formulation and apply a thin layer to the affected area. Wear gloves or use a clean applicator to avoid contaminating the medication.
Massage or rub it in: Gently massage or rub the cream into the skin until it is evenly distributed.
Patient information leaflet
Generic Name: ketoconazole topical
Why do we use ketoconazole topical?
Fungal skin infections: drug is effective in treating fungal infections such as athlete’s foot (tinea pedis), jock itch (tinea cruris), and ringworm (tinea corporis). It helps relieve itching, redness, and other symptoms associated with these infections.
Seborrheic dermatitis: The utilization of a drug aids in diminishing inflammation and regulating the excessive proliferation of yeast, a factor that contributes to seborrheic dermatitis.
Dandruff: ketoconazole shampoo is often prescribed to treat dandruff caused by a specific type of yeast called Malassezia. It helps control the yeast population on the scalp, reducing flaking and itching.
Pityriasis versicolor: This is a superficial fungal infection that leads to the development of discolored patches on the skin, commonly on the chest, back, neck, and arms.
Cutaneous candidiasis: The drug is also effective in treating infections caused by the yeast Candida, such as cutaneous candidiasis. This condition can occur in areas of the skin that are warm, moist, and prone to friction, such as the armpits, groin, and under the breasts.