Topical Antifungals

shevyatiwari's version from 2015-04-24 14:01


Question Answer
Nystatin is an allylamineF polyene
Polyenes have a macrolide ringT
Nystatin is a tetraene antibioitcT
Similar to calcineurin in its mechanism of actionF, similar to amphotericin B
Nystatin is safe systemicallyF has toxicity - therefore used topically
Nystatin is highly soluble in waterF, insoluble
Nystatin is absorbed from intact skinF, not absorbed from GIT or vagina either
Nystatin is only fungistaticF, also cidal
Binds reversibly to membrane sterols of candidaF, irreversibly
Nystatin is effective for dermatophyte infectionF
Nystatin generally has numerous S/EF, adverse effects in <0.1%
Amphotericin B is an azoleF, a polyene similar to nystatin


Question Answer
Azoles block synthesis of ergosterolT
Lansoterol 14ademethylase catalyses the conversion of lanosterol to ergosterolT
Azoles compete with oxygen and inhibit its binding and activationT
On intact skin, absorption of azoles is approx 4%F, <1%
Absorption of azoles on damaged or inflamed skin is approx 50%F, 4%
Azoles have a high risk of ACDF


Question Answer
Miconazole has antibacterial activityT - Gram positive
Miconazole is highly soluble in waterF, only mildly soluble
Only slightly soluble in most common organic solvents and diluted inorganic acidsT, same as solubility in water
Penetrates SC wellT
Systemic absorption is approx <1%T
Detected for 24 hours after applicationF, 4 days
Active against dermatophytes, candida, malasezzia, gram positive bacteriaT
Appropriate for bacterial infectionsF
C/I in combination with BPF, can be used together for acne
Generally well toleratedT


Question Answer
Clotrimazole is as efficacious as Nystatin in the inhibition of candidaT, efficacy only slightly less than
Under occlusion, there is significant systemic absorptionF
Efficacy against dermatophyte, candida and gram positiveT
Generally well toleratedT
Broad spectrumT


Question Answer
Ketoconazole is a water soluble imidazoleT
Ketoconazole is synthetic with broad spectrum activityT
Ketoconazole causes a high rate of adverse effects F, 5%
Propylene glycol or sodium sulfite are more likely to cause ACD than ketoconazoleT
Dermatophytes, candida, and malasezzie are susceptibleT


Question Answer
Oxiconazole persists in the stratum corneum for 2 daysF, 96 hours
Oxiconazole is approved for OD dosingT


Question Answer
Econazole is a derivative of clotrimazoleF, of miconazole
Activity is only in the epidermisF, extends to mid dermis
Systemic absorption is quite highF, <1%
Works slower than clotrimazoleF, faster and with similar efficacy
Activity against GP organisms onlyF, also GN
Advere effects are seen in 3%T


Question Answer
Sulconazole is the least absorbed antifungalF, highest
Sulconazole is absorbed 8-11%T
GP and GN activityF, only GP
Can be effective for impetigo and ecthymaT


Question Answer
Sertaconazole is hydrophilic compared to other azolesF, lipophilic
Sertaconazole binds to non sterol cell membrane lipidsT - gives it a bactericidal effect in addition to bacteriostatic
Bactericidal as well as bacteriostaticT
Excellent activity against candida and GPF, excellent for candida, modest for GP
Good safety recordT


Question Answer
Allylamines are broad spectrum antifungalsT
Allylamines are fungistatic onlyF, also cidal
Allylamines act by inhibiting the synthesis of ergosterolT
Allylamines are agonists of squalene epoxidaseF, they inhibit it
Naftidine is syntheticT
Terbinafine (lamisil) is highly lipophilicT
Terbinafine has a high risk of relapse of infectionF
Terbinafine is 10 times more potent than naftidineF, 10-100 tiems
Terbinafine is rapidly absorbedF, slow absorption
Butenafine is a derivative of terbinafineF, is a benzylamine
Butenafine acts in the same way as allylaminesT - inhibits squalene epoxidase


Question Answer
Ciclopirox is a benzylamineF, hydroxypyridone
Ciclopirox affects sterol synthesisF, interferes with membrane transport of essential macromolecule precursors
Low affinity for trivalent cations -> subsequent blockade by enzymatic co-factorsF, high affinity
Gram negative antibacterial activityT

Selenium sulfide

Question Answer
Selenium sulfide has a cytostatic effect on cells in the epidermis and follicular epitheliumT
Selenium is cat BF, C
Fungistatic to P ovaleF, fungicidal

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