ECONAZOLE NITRATE
DESCRIPTION:
ECANOL Cream contains the antifungal agent, econazole nitrate 1%, in a
water-miscible base consisting of pegoxol 7 stearate, peglicol 5 oleate, mineral
oil, benzoic acid, butylated hydroxyanisole and purified water. The white to
off-white soft cream is for topical use only.
Chemically, econazole nitrate is 1-(2-((4-chlorophenyl) methoxy)-2-(2,4-
dichlorophenyl)ethyl)-1H- imidazole mononitrate.
ACTIONS/CLINICAL PHARMACOLOGY:
After topical application to the skin of normal subjects, systemic absorption of
econazole nitrate is extremely low. Although most of the applied drug remains on
the skin surface, drug concentrations were found in the stratum corneum which,
by far, exceeded the minimum inhibitory concentration for dermatophytes.
Inhibitory concentrations were achieved in the epidermis and as deep as the
middle region of the dermis. Less than 1% of the applied dose was recovered in
the urine and feces.
Microbiology: Econazole nitrate has been shown to be active against most strains
of the following microorganisms, both In Vitro and in clinical infections as
described in the INDICATIONS AND USAGE section.
DERMATOPHYTES YEASTS
Epidermophyton Floccosum Candida Albicans
Microsporum Audouini Malassezia Furfur
Microsporum Canis
Microsporum Gypseum
Trichophyton Mentagrophytes
Trichophyton Rubrum
Trichophyton Tonsurans
Econazole nitrate exhibits broad-spectrum antifungal activity against the
following organisms In Vitro, BUT THE CLINICAL SIGNIFICANCE OF THESE DATA IS
UNKNOWN.
DERMATOPHYTES YEASTS
Trichophyton Verrucosum Candida Guillermondii
Candida Parapsilosis
Candida Tropicalis
INDICATIONS AND USAGE:
ECANOL Cream is indicated for topical application in the treatment of tinea
pedis, tinea cruris, and tinea corporis caused by Trichophyton Rubrum,
Trichophyton Mentagrophytes, Trichophyton Tonsurans, Microsporum Canis,
Microsporum Audouini, Microsporum Gypseum, and Epidermophyton Floccosum, in the
treatment of cutaneous candidiasis, and in the treatment of tinea versicolor.
CONTRAINDICATIONS:
ECANOL Cream is contraindicated in individuals who have shown
hypersensitivity to any of its ingredients.
WARNINGS:
ECANOL is not for ophthalmic use.
PRECAUTIONS:
General: If a reaction suggesting sensitivity or chemical irritation should
occur, use of the medication should be discontinued.
For external use only. Avoid introduction of ECANOL Cream into the eyes.
Carcinogenicity Studies: Long-term animal studies to determine carcinogenic
potential have not been performed.
Fertility (Reproduction): Oral administration of econazole nitrate in rats has
been reported to produce prolonged gestation. Intravaginal administration in
humans has not shown prolonged gestation or other adverse reproductive effects
attributable to econazole nitrate therapy.
Pregnancy: Pregnancy Category C. Econazole nitrate has not been shown to be
teratogenic when administered orally to mice, rabbits or rats. Fetotoxic or
embryotoxic effects were observed in Segment I oral studies with rats receiving
10 to 40 times the human dermal dose. Similar effects were observed in Segment
II or Segment III studies with mice, rabbits and/or rats receiving oral doses 80
or 40 times the human dermal dose.
Econazole nitrate should be used in the first trimester of pregnancy only when
the physician considers it essential to the welfare of the patient. The drug
should be used during the second and third trimesters of pregnancy only if
clearly needed.
Nursing Mothers: It is not known whether econazole nitrate is excreted in human
milk. Following oral administration of econazole nitrate to lactating rats,
econazole and/or metabolites were excreted in milk and were found in nursing
pups. Also, in lactating rats receiving large oral doses (40 or 80 times the
human dermal dose), there was a reduction in postpartum viability of pups and
survival to weaning; however, at these high doses, maternal toxicity was present
and may have been a contributing factor. Caution should be exercised when
econazole nitrate is administered to a nursing woman.
ADVERSE REACTIONS:
During clinical trials, approximately 3% of patients treated with econazole
nitrate 1% cream reported side effects thought possibly to be due to the drug,
consisting mainly of burning, itching, stinging and erythema. One case of
pruritic rash has also been reported.
OVERDOSAGE:
Overdosage of econazole nitrate in humans has not been reported to date. In
mice, rats, guinea pigs and dogs, the oral LD 50 values were found to be 462,
668, 272, and > 160 mg/kg, respectively.
DOSAGE AND ADMINISTRATION:
Sufficient ECANOL Cream should be applied to cover affected areas once daily
in patients with tinea pedis, tinea cruris, tinea corporis, and tinea
versicolor, and twice daily (morning and evening) in patients with cutaneous
candidiasis.
Early relief of symptoms is experienced by the majority of patients and clinical
improvement may be seen fairly soon after treatment is begun; however, candidal
infections and tinea cruris and corporis should be treated for two weeks and
tinea pedis for one month in order to reduce the possibility of recurrence. If a
patient shows no clinical improvement after the treatment period, the diagnosis
should be redetermined. Patients with tinea versicolor usually exhibit clinical
and mycological clearing after two weeks of treatment.
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