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 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.
- 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
Contra-Indications of Econazole
Econazole is for external use only; it is not for oral administration, ophthalmic administration, or vaginal administration.
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
- Abdominal or stomach pain
- feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
- sudden tingling or coldness in an arm or leg
- Nausea
- liver problems,
- stomach pain,
- vomiting,
- Dizziness
- Burning, itching, stinging, redness, or other sign of irritation at the application site, rash
- a headache,
- increased intracranial pressure,
- meningeal signs,
- reversible hair loss or thinning, and
- fever.
Common
- chills or fever
- a headache, severe and throbbing
- joint or back pain
- muscle aching or cramping
- muscle pains or stiffness
- chest pressure or squeezing pain in the chest
- discomfort in arms, shoulders, neck or upper back
- excessive sweating
- sudden slow or difficult speech
- sudden drowsiness or need to sleep
- fast breathing
- sharp pain when taking a deep breath
- fast or slow heartbeat
- coughing up blood
- rust colored urine
- decreased amount of urine
Rare
- Anxiety
- change in vision
- chest pain or tightness
- confusion
- a cough
- Agitation
- arm, back, or jaw pain
- blurred vision
- chest pain or discomfort
- convulsions
- extra heartbeats
- fainting
- hallucinations
- a headache
- irritability
- lightheadedness
- mood or mental changes
- muscle pain or cramps
- muscle spasm or jerking of all extremities
- burning,
- stinging,
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.
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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