1 - TOPICAL ANTIFUNGAL AGENTS Flashcards
Topical antifungals are considered first line therapy for uncomplicated superficial dermatomycoses owing to their high efficacy and low potential for systemic adverse effects
True
The most commonly employed topical antifungal agents belong to 3 main classes:
(1) Polyenes
(2) Azoles (imidazoles)
(3) Allylamines/Benzylamines
True (other agents not among these 3 major classes include the hydroxypyridone ciclopirox olamine, selenium sulfide)
Nystatin and amphotericin B are Polyenes
True
Miconazole, Clotrimazole, Ketoconazole, Oxiconazole, Econazole, Sulconazole, Sertaconazole are Azoles (Imidazole subclass)
True (in contrast, the systemic antifungals itraconazole, fluconazole, voriconazole and posaconazole are triazoles)
Terbinafine and Naftifine are allylamines
True
Butenafine is the only Benzylamine
True
Ciclopirox is a hydroxypyridone antifungal agent
True (not related to the 3 main classes of topical antifungal agents)
Selenium sulfide has topical antifungal properties
True (not one of the 3 main classes of topical antifungal agents)
Nystatin (Polyenes) binds to cell membrane sterols causing cell leakage and permeability changes with activity against candida only
True (fungicidal and fungistatic in vitro)
All the Azoles (Miconazole, Clotrimazole, Ketoconazole, Oxiconazole, Econazole, Sulconazole, Sertaconazole) inhibit ergosterol synthesis by blocking 14-alpha demethylase enzyme which then affect the synthesis of ergosterol (component of the fungal cell membrane)
True (fungistatic in vitro)
Terbinafine and Naftifine (Allylamines) and Butenafine (Benzylamine) inhibit ergosterol synthesis by blocking squalene epoxidase, which then affect the synthesis of ergosterol (component of the fungal cell membrane)
True (fungicidal in vitro)
Nystatin (Polyenes) has activity against candida only
True
Miconazole, Clotrimazole, Ketoconazole, Econazole (Azoles) have activity against dermatophytes, Malessezia furfur, and candida
True
Oxiconazole and Sulconazole (Azoles) have activity against dermatophytes and Malessezia furfur
True (activity against candida is relatively weak compared to Miconazole, Clotrimazole, Ketoconazole, Econazole)
The allylamines (Terbinafine and Naftifine) have activity against dermatophytes
True (Terbinafine has activity against candida but this is relatively weak compared to the Azoles)
Terbinafine has activity against candida but this is relatively weak compared to the Azoles
True (main activity is against dermatophytes)
Butenafine (Benzylamine) has activity against dermatophytes and candida, although activity against candida is relatively weak compared to the Azoles
True
The associated systemic toxicity of Nystatin (Polyenes) has limited its use to topical application as Nystatin is essentially insoluble in water and not absorbed from intact skin, the GI tract or the vagina
True
Nystatin (Polyenes) has fungicidal and fungistatic activity in vitro
True
Nystatin is used in the treatment of oral candidiasis
True (4-5 times daily use is recommended)
Nystatin (Polyenes) is used in the treatment of cutaneous candidiasis
True (BD application recommended)
Nystatin (Polyenes) is well tolerated
True
Burning, pruritus, rash, eczema and pain on application are the more common adverse effects with Nystatin (Polyenes) use
True (generally a well tolerated drug)
Very rarely hypersensitivity reactions have been reported with Nystatin (Polyenes) use
True (generally a well tolerated drug)
The introduction of the azole antifungal agents presented a new class of compounds with a broader spectrum of activity, including action against the common dermatophytes that were not susceptible to the Polyenes (Nystatin)
True
The human skin is an efficient barrier to most Azole compounds, such that percutaneous absorption is generally <1% on intact skin
True
The absorption of Azole compounds may be increased from <1% (intact skin) to 4% on inflamed or damaged skin
True
In general there is very low sensitising potential associated with all Azole antifungals
True
Miconazole (Azole) is very slightly soluble and penetrates the stratum corneum well, although with minimal systemic absorption
True (<1% of Miconazole is absorbed following topical application)
Miconazole (Azole) is active against dermatophytes (Trichophyton and Epidermophyton) and is therefore effective in the treatment of tinea pedis/corporis/cruris
True (BD application recommended)
Miconazole (Azole) is active against Candida albicans, and is therefore effective in the treatment of cutaneous candidiasis
True (BD application is recommended)
Miconazole (Azole) is active against Malassezia furfur, and is therefore effective in the treatment of pityriasis versicolor and seborrheic dermatitis
True (once daily application is sufficient)
Miconazole (Azole) also demonstrates activity against some gram +Ve bacteria and is modestly effective in the treatment of erythrasma, impetigo, or ecthyma caused by Group A beta-haemolytic streptococci or staphylococci
True (however Miconazole’s antibacterial activity is not sufficient to make this agent a drug of choice for such infections)
Topical Miconazole (Azole) is well tolerated although rarely irritation, burning, maceration, and allergic contact dermatitis may occur at application sites
True
Systemic absorption of Clotrimazole (Azole) is very low
True (even under occlusive dressing)
Clotrimazole (Azole) exhibits a broad spectrum of activity against most strains of Trichophyton, Epidermophyton and Microsporum species and is therefore effective in the treatment of tinea pedis/corporis/cruris
True (BD application recommended)
Clotrimazole (Azole) exhibits efficacy near, though slightly less than that of Nystatin (Polyenes) in candida inhibition and is therefore effective in the treatment of cutaneous candidiasis, oropharyngeal candidiasis and vaginal candidiasis
True
Cutaneous candidiasis = BD application on skin recommended
Oropharyngeal candidiasis = oral troches administered 4-5 times daily for 2 weeks
Vaginal candidiasis = once daily intravaginal tablet for 1-2 days
Clotrimazole (Azole) exhibits activity against Malassezia furfur and can be used in the treatment of pityriasis versicolor
True
Clotrimazole (Azole) is generally well tolerated, though there are isolated reports of erythema, burning, irritation, stinging, peeling, blistering oedema, pruritus and urticaria at the application site
True
Ketoconazole (Azole) is water soluble and the topical application is not systemically absorbed
True
Ketoconazole (Azole) is a broad spectrum antifungal agent that exhibits a wide spectrum of activity against dermatophytes and is effective in the treatment of tinea pedis/corporis/cruris
True (once daily application for 4 weeks recommended)
Ketoconazole (Azole) has activity against Candida albicans and is effective in the treatment of cutaneous candidiasis
True
Ketoconazole (Azole) has activity against Malessezia furfur and is therefore effective in pityriasis versicolor and seborrheic dermatitis (which is owing to the role of pityrosporum ovale in causation)
True (available in 2% cream, 2% shampoo and 2% foam formulation + 1% shampoo over the counter) - can be used in infantile seborrhoeic dermatitis for 10 days
5% of patients treated with Ketoconazole 2% cream (Azole) reported irritation, pruritus, and stinging
True
Rare reports of allergic contact dermatitis have been associated with Ketoconazole (Azole) cream or one of its ingredients sodium sulfite or propylene glycol
True
Topical Oxiconazole (Azole) is rapidly absorbed into the stratum corneum and persists in the stratum corneum at therapeutic levels for 7 days
True (this reservoir effect accounts for Oxiconazole efficacy in fungus eradication with once daily dosing)
Systemic absorption of topical Oxiconazole (Azole) is negligible
True
Oxiconazole (Azole) lotion or cream once daily is effective in the treatment of tinea pedis/corporis/cruris
True (lotion being useful for large or hairy areas on the trunk and back) - activity against candida is relatively weak compared to other Azoles Miconazole, Clotrimazole, Ketoconazole, Econazole