Econazole; Uses, Dosage, Side Effects, Interactions, Pragnancy

Econazole; Uses, Dosage, Side Effects, Interactions, Pragnancy

Econazole is only found in individuals that have used or taken this drug. It is a broad spectrum antimycotic with some action against Gram-positive bacteria. It is used topically in dermatomycoses also orally and parenterally. [PubChem]Econazole interacts with 14-alpha-demethylase, a cytochrome P-450 enzyme necessary to convert lanosterol to ergosterol. As ergosterol is an essential component of the fungal cell membrane, inhibition of its synthesis results in increased cellular permeability causing leakage of cellular contents. Econazole may also inhibit endogenous respiration, interact with membrane phospholipids, inhibit the transformation of yeasts to mycelial forms, inhibit purine uptake, and impair triglyceride and/or phospholipid biosynthesis.

 

Econazole is an imidazole with the antifungal property. Econazole compromises the integrity of the fungal cell wall through inhibiting 14-alpha-demethylase, which catalyzes the conversion of lanosterol to ergosterol, an essential component of the fungal cell wall. As a result, this agent increases cellular permeability thereby resulting in leakage of cellular contents. Furthermore, econazole has also been implicated to inhibit endogenous respiration, interact with membrane phospholipids, inhibit purine uptake, and impair triglyceride and/or phospholipid biosynthesis.

Mechanism of Action of Econazole

Econazole interacts with 14-α demethylase, a cytochrome P-450 enzyme necessary to convert lanosterol to ergosterol. As ergosterol is an essential component of the fungal cell membrane, inhibition of its synthesis results in increased cellular permeability causing leakage of cellular contents. Econazole may also inhibit endogenous respiration, interact with membrane phospholipids, inhibit the transformation of yeasts to mycelial forms, inhibit purine uptake, and impair triglyceride and/or phospholipid biosynthesis.

Indications of Econazole 

  • Tinea corporis
  • Cutaneous candidiasis
  • Paronychia
  • Tinea cruris
  • Tinea versicolor
  • Tinea pedis
  • Candidiasis, cutaneous
  • Pityriasis Versicolor
  • Tinea corporis
  • Tinea pedis
  • Tinea pedis of the interdigital
  • Lightening or darkening of the skin of the neck, chest, arms, or legs.
  • Treatment of skin infections such as athlete’s foot, tinea, pityriasis versicolor, ringworm, and jock itch.
  • For topical application in the treatment of tinea pedis, tinea cruris, and tinea corporis caused by Trichophyton rubrumTrichophyton mentagrophytesTrichophyton tonsuransMicrosporum canisMicrosporum audouiniMicrosporum gypseum, and Epidermophyton floccosum, in the treatment of cutaneous candidiasis, and in the treatment of tinea versicolor.
  • Treatment of tinea cruris and tinea corporis due to Trichophyton rubrum, T mentagrophytes, T tonsurans, Microsporum canis, M audouini, M gypseum, and Epidermophyton floccosum; for the treatment of tinea versicolor
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Contra-Indications of Econazole

Ophthalmic administration, vaginal administration

Econazole is for external use only; it is not for oral administration, ophthalmic administration, or vaginal administration.

Tobacco smoking

Econazole foam is flammable. Avoid heat, flame, and tobacco smoking during and immediately following application. Do not puncture or burn the foam container, as the contents are under pressure.

Hypersensitivities to any ingredient of econazole.

Dosage of Econazole

Tinea Corporis

Topical cream: Apply a sufficient amount to cover affected areas once a day.
Duration of therapy: 2 weeks

Tinea Cruris

Topical cream: Apply a sufficient amount to cover affected areas once a day.
Duration of therapy: 2 weeks

Tinea Versicolor

Topical cream: Apply a sufficient amount to cover affected areas once a day.
Duration of therapy: 2 weeks

Tinea Pedis

Topical cream: Apply a sufficient amount to cover affected areas once a day.
Topical foam: Should be applied to cover affected areas once a day
Duration of therapy: 4 weeks

Cutaneous Candidiasis

Topical cream: Apply a sufficient amount to cover affected areas twice a day.
Duration of therapy: 2 weeks

Pediatric Dose for Tinea Pedis

12 years or older
Topical foam: Should be applied to cover affected areas once a day
Duration of therapy: 4 weeks

Vaginal Cream and Pessaries
-Common (1% to 10%): Pruritus, skin burning sensation
-Uncommon (0.1% to 1%): Rash
-Rare (0.01% to 0.1%): Erythema
-Postmarketing reports: Angioedema, urticaria, contact dermatitis, skin exfoliation

Side Effects of Econazole

The most common

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Common

Rare

Drug Interaction of Econazole

Corticosteroids: (Minor) In vitro studies indicate that corticosteroids inhibit the antifungal activity of econazole against C. albicans in a concentration-dependent manner. When the concentration of the corticosteroid was equal to or greater than that of econazole on a weight basis, the antifungal activity of econazole was substantially inhibited. When the corticosteroid concentration was one-tenth that of econazole, no inhibition of antifungal activity was observed.
Nystatin: (Moderate) The combination of econazole and nystatin represents a duplication of therapy whenever the drugs are used by similar routes and are usually avoided.
Warfarin: (Moderate) Coadministration of econazole and warfarin has resulted in enhanced anticoagulant effect. In many of these cases, absorption of econazole may have been increased by applying the drug under occlusion, to the genitals, or over large body surface areas. If these drugs are used in combination, closely monitor the International Normalized Ratio (INR) and/or prothrombin time.

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Pregnancy and Lactation of Econazole

FDA  pregnancy category C.

Pregnancy

Systemic absorption of econazole is low (< 10%) after topical application to the intact skin in humans. There are no adequate and well-controlled studies on adverse effects from the use of Pevaryl Topical cream in pregnant women, and no other relevant epidemiological data are available. Animal studies have shown reproductive toxicity. Because there is systemic absorption, use of Pevaryl Topical Cream is not recommended during pregnancy.

Lactation

It is not known whether cutaneous administration of Pevaryl Topical cream results in sufficient systemic absorption of econazole nitrate to produce detectable quantities in breast milk in humans. A risk to the breastfed child cannot be excluded. A decision must be made whether to discontinue breastfeeding or to discontinue/abstain from Pevaryl Topical Cream therapy taking into account the benefit of breastfeeding for the child and benefit of therapy for the woman.

If  Topical Cream is used while breastfeeding, care should be taken to ensure the cream is not applied to the nipple or surrounding area.

 

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