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    Ketoconazole, 2 % cream

    Drug formSoft

    ATC categoryAnifungals

    ATC subcategoryAzole antifungals (for external use)

    Brand nameKetoconazole

    Generic nameKetoconazole

    Cualitative and quantitative composition

    Each gram contains:

    Active ingredient: ketoconazole – 20 mg;

    For a full list of excipients, see section (List of excipients).

     

    Pharmaceutical form

    Cream for external use

     

    Clinical particulars

    Therapeutic indications

    For topical application in the treatment of dermatophyte infections of the skin such as tinea corporis, tinea cruris, tinea manus and tinea pedis infections due to Trichophyton spp, Microsporon spp and Epidermophyton spp. Ketokonazole 2% cream is also indicated for the treatment of cutaneous candidosis (including vulvitis), tinea (pityriasis) versicolor and seborrhoeic dermatitis caused by Malassezia (previously called Pityrosporum) spp.

     

    Posology and method of administration

    Ketoconazole cream is for use in adults.

    Tinea pedis:

    Ketoconazole 2% cream should be applied to the affected areas twice daily. The usual duration of treatment for mild infections is 1 week. For more severe or extensive infections (eg involving the sole or sides of the feet) treatment should be continued until a few days after all signs and symptoms have disappeared in order to prevent relapse.

    For other infections:

    Ketoconazole 2% cream should be applied to the affected areas once or twice daily, depending on the severity of the infection.

    The treatment should be continued until a few days after the disappearance of all signs and symptoms. The usual duration of treatment is: tinea versicolor 2–3 weeks, tinea corporis 3–4 weeks.

    The diagnosis should be reconsidered if no clinical improvement is noted after 4 weeks. General measures in regard to hygiene should be observed to control sources of infection or reinfection.

    Seborrheic dermatitis is a chronic condition and relapse is highly likely. Method of administration: Cutaneous administration.

    Pediatrics:

    There are limited data on the use of ketoconazole 2% cream in pediatric patients.

     

    Contraindications

    Ketoconazole 2% cream is contra-indicated in patients with a known hypersensitivity to any of the ingredients or to ketoconazole itself.

     

    Special warnings and precautions for use

    Not for ophthalmic use

    If co-administered with a topical corticosteroid, to prevent a rebound effect after stopping a prolonged treatment with topical corticosteroids it is recommended to continue applying a mild topical corticosteroid in the morning and to apply cream in the evening, and to subsequently and gradually withdraw the topical corticosteroid therapy over a period of 2-3 weeks.

     

    Important information about some of the ingredients of Ketoconazole

    Ketoconazole cream contains:

    • Methylparaben which may cause allergic reactions (possibly delayed).
    • Propylparaben which may cause allergic reactions (possibly delayed).
    • Cetostearyl alcohol which may cause local skin reactions (e.g. contact dermatitis).

     

    Interaction with other medicinal products and other forms of interaction

    No interaction studies have been performed.

     

    Fertility, pregnancy and lactation

    There are no adequate and well-controlled studies in pregnant or lactating women. Data on a limited number of exposed pregnancies indicate no adverse effects of topical ketoconazole on pregnancy or on the health of the fetus/newborn child. Animal studies have shown reproductive toxicity at doses that are not relevant to the topical administration of ketoconazole.

    Plasma concentrations of ketoconazole are not detectable after topical application of Ketoconazole 2% Cream to the skin of non-pregnant humans. There are no known risks associated with the use in pregnancy or lactation.

     

    Effects on ability to drive and use machines

    Ketoconazole 2% cream has no influence on the ability to drive and use machines

     

    Undesirable effects

    The safety of ketoconazole cream was evaluated in 1079 subjects who participated in 30 clinical trials. Ketoconazole cream was applied topically to the skin. Based on pooled safety data from these clinical trials, the most commonly reported (1% incidence) ADRs were (with % incidence): application site pruritus (2%), skin burning sensation (1.9%), and application site erythema (1%).

    Including the above-mentioned adverse reactions, the following table displays adverse reactions that have been reported with the use of ketoconazole cream from either clinical trial or post marketing experiences. The displayed frequency categories use the following convention:

     

    Very common

    ≥1/10

    Common

    ≥1/100 and <1/10

    Uncommon

    ≥1/1,000 and <1/100

    Rare

    ≥1/10,000 and <1/1,000

    Very rare

    <1/10,000

    Not Known

    cannot be estimated from the available clinical trial data

     

    Table 1 Adverse Drug Reactions in Clinical Trials

    System Organ Class

    Adverse Drug Reactions

    Frequency Category

    Common

    (≥1/100 to

    <1/10)

    Uncommon

    (≥1/1,000 to <1/100)

    Not Known

    Immune          System Disorders

     

    Hypersensitivity

     

    Skin and Subcutaneous Tissue Disorders

    Skin burning sensation

    Bullous eruption Dermatitis contact Rash

    Skin exfoliation Sticky skin

    Urticaria

    General Disorders and Administration Site Conditions

    Application site erythema

    Application site pruritus

    Application site bleeding Application site discomfort Application site dryness Application site inflammation Application site irritation Application site paraesthesia Application site reaction

     
     
     
    Overdose

    Topical Application

    Excessive topical application may lead to erythema, oedema and a burning sensation, which will disappear upon discontinuation of the treatment.

    Ingestion

    In the event of accidental ingestion, supportive and symptomatic measures should be carried out.

     

    Pharmacological properties
    Pharmacodynamic properties

    Pharmacotherapeutic group: antifungals for topical use, imidazole and triazole derivatives.

    ATC Code: D01AC08

    Usually ketoconazole cream acts rapidly on pruritus, which is commonly seen in dermatophyte and yeast infections, as well as skin conditions associated with the presence of Malassezia spp. This symptomatic improvement is observed before the first signs of healing are observed.

    Ketoconazole, a synthetic imidazole dioxolane derivative, has a potent antimycotic activity against dermatophytes such as Trichophyton spp., Epidermophyton floccosum and Microsporum spp. and against yeasts, including Malassezia spp. and Candida spp. The effect on Malassezia spp. is particularly pronounced.

    A study in 250 patients has shown that application twice daily for 7 days of ketoconazole 2% cream vs clotrimazole 1% cream for 4 weeks on both feet demonstrated efficacy in patients with tinea pedis (athlete’s foot) presenting lesions between the toes. The primary efficacy endpoint was negative microscopic KOH examination at 4 weeks. Ketoconazole 2% treatment showed equivalent efficacy to 4 weeks clotrimazole 1% treatment. There was no evidence of relapse following treatment with ketoconazole cream at 8 weeks.

     

    Pharmacokinetic properties

    Plasma concentrations of ketoconazole were not detectable after topical administration of Ketoconazole 2% Cream in adults on the skin. In one study in infants with seborrhoeic dermatitis (n = 19), where approximately 40 g of Ketoconazole 2% cream was applied daily on 40% of the body surface area, plasma levels of ketoconazole were detected in 5 infants, ranging from 32 to 133 ng/mL.

     

    Preclinical safety data

    Effects in non-clinical studies were observed only at exposures considered sufficiently in excess of the maximum human exposure indicating little relevance to clinical use.

     

    Pharmaceutical particulars

    List of excipients

    Ceteareth-12

    Ceteareth-20

    Cetostearyl alcohol

    Isopropyl myristate

    Methylparaben

    Propylparaben

    Propylene glycol

    Color red E-129

    Water purified

     

    Incompatibilities

    Not applicable

     

    Shelf life

    3 years

     

    Storage conditions

    Store at temperature 15-250С, in a dry place, out of the reach of children, protect from light.

     

    Nature and contents of container

    15 g and 25 g of cream is filled into aluminum tubes (inside package).

    The tubes are packed and inserted with the leaflet into cardboard boxes (outer package).

     

    Special precautions for disposal and other handling

    No special requirements