Nizoral Cream

Ketoconazole (Nizoral) is a white homogenous cream for external use.
Each gram contains 20 mg ketoconazole.
Excipients/Inactive Ingredients: The cream formulation consists of cetyl alcohol, isopropyl myristate, polysorbate, propylene glycol, purified water, sodium sulfite, sorbitan stearate, stearyl alcohol.

Antifungal.
Pharmacology: Pharmacodynamics: Mechanism of action: Ketoconazole inhibits the biosynthesis of ergosterol in fungi and changes the composition of other lipid components in the membrane.
Pharmacodynamic effects: 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.
Pharmacokinetics: Plasma concentrations of ketoconazole were not detectable after topical administration of ketoconazole (Nizoral) 2% Cream in adults on the skin. In one study in infants with seborrheic dermatitis (n=19) where approximately 40 g of ketoconazole (Nizoral) 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.
Toxicology: Non-clinical information: Preclinical data reveal no special hazard for humans based on conventional studies including primary ocular or dermal irritation, dermal sensitization and repeat-dose dermal toxicity.
Acute dermal and ocular irritation studies with ketoconazole cream formulations in rabbits showed no dermal or ocular irritation. Results from a dermal sensitization study in guinea pigs showed no allergenic or sensitizing potential. In five repeat-dose dermal studies in rabbits, ketoconazole was administered to both abraded and non-abraded skin at a maximum dose of 40 mg/kg. In one study some slight irritation was noted in both the ketoconazole and placebo groups, however, in the remaining studies no dermal or systemic toxic effects were noted. Data from pharmacokinetic studies, of several topical formulations of ketoconazole under exaggerated test conditions in laboratory animals, showed no measurable ketoconazole plasma concentrations.
Microbiology: 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. Especially the effect on Malassezia spp. is very pronounced.

Ketoconazole (Nizoral) 2% Cream is indicated for topical application in the treatment of dermatophyte infections of the skin: tinea corporis, tinea cruris, tinea manus and tinea pedis due to Trichophyton rubrum, Trichophyton mentagrophytes, Microsporum canis and Epidermophyton floccosum, as well as in the treatment of cutaneous candidosis and tinea (pityriasis) versicolor.
Ketoconazole (Nizoral) 2% Cream is also indicated for the treatment of seborrheic dermatitis, a skin condition associated with the presence of Malassezia furfur.

Cutaneous candidosis, tinea corporis, tinea cruris, tinea manus, tinea pedis and tinea (pityriasis) versicolor: it is recommended that ketoconazole (Nizoral) 2% Cream be applied once daily to cover the affected and immediate surrounding area.
Seborrheic dermatitis: ketoconazole (Nizoral) 2% Cream should be applied to the affected area once or twice daily.
The usual duration of treatment is tinea versicolor 2-3 weeks, yeast infections 2-3 weeks, tinea cruris 2-4 weeks, tinea corporis 3-4 weeks, tinea pedis 4-6 weeks.
The usual initial duration of treatment in seborrheic dermatitis is 2 to 4 weeks. Maintenance therapy is applied once or twice weekly in seborrheic dermatitis.
Treatment should be continued, until a few days after disappearance of all symptoms. The diagnosis should be reconsidered if no clinical improvement is noted after 4 weeks of treatment.
Special populations: Pediatrics: There are limited data on the use of ketoconazole 2% cream in pediatric patients.
Administration: Topical administration to the skin.

Topical Application: Excessive topical application may lead to erythema, edema 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.

Ketoconazole (Nizoral) 2% Cream is contraindicated in individuals with a known hypersensitivity to any of its ingredients.

Ketoconazole (Nizoral) 2% Cream is not for ophthalmic use. It is for external use only.
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 ketoconazole (Nizoral) 2% Cream in the evening, and to subsequently and gradually withdraw the topical corticosteroid therapy over a period of 2-3 weeks.

Pregnancy: There are no adequate and well-controlled studies in pregnant women. Plasma concentrations of ketoconazole are not detectable after topical application of ketoconazole (Nizoral) 2% Cream to the skin of non-pregnant humans. There are no known risks associated with the use of ketoconazole (Nizoral) 2% Cream in pregnancy.
Lactation: There are no adequate and well-controlled studies in lactating women. There are no known risks associated with the use of ketoconazole (Nizoral) Cream in lactation.

Throughout this section, adverse reactions are presented. Adverse reactions are adverse events that were considered to be reasonably associated with the use of ketoconazole based on the comprehensive assessment of the available adverse event information. A causal relationship with ketoconazole cannot be reliably established in individual cases. Further, because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice.
Clinical Trial Data: The safety of ketoconazole (Nizoral) 2% Cream was evaluated in 1079 subjects in 30 clinical trials where ketoconazole (Nizoral) 2% Cream was applied topically to the skin.
Adverse reactions that were reported for ≥1% of ketoconazole (Nizoral) 2% Cream-treated subjects are shown in Table 1. (See Table 1.)

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Additional adverse reactions that occurred in <1% of ketoconazole (Nizoral) 2% Cream-treated subjects in the clinical datasets are listed in Table 2. (See Table 2.)

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Post-marketing Data: In addition to the adverse reactions reported during clinical studies and listed previously, the following adverse reactions have been reported during post-marketing (Table 3). In the table, the frequencies are provided according to 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, including isolated reports).
In Table 3, adverse reactions are presented by frequency category based on spontaneous reporting rates. (See Table 3.)

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Incompatibilities: None known.
Instructions for use and handling: To open the tube, unscrew the cap. Then pierce the seal of the tube with the pin on the top of the cap.

Store at temperatures not exceeding 30°C.

Topical Antifungals & Antiparasites

D01AC08 - ketoconazole ; Belongs to the class of imidazole and triazole derivatives. Used in the topical treatment of fungal infection.

Non-Rx