24 - Antifungals and Corticosteroids Flashcards

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1
Q

What drug variables determine percutaneous absorption?

A

o Concentration (concentration more important than volume)
o Lipophilicity
o Molecular size (most effective topical meds have a molecular weight of

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2
Q

What vehicle variables determine percutaneous absorption?

A
o	Lipid content (ointment strongest vehicle, solution typically the weakest)
o	Irritancy (irritating vehicles will alter skin barrier function)
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3
Q

What skin variables determine percutaneous absorption?

A

o Stratum corneum thickness
o Cutaneous vasculature
o Inflamed skin (will have increased absorption)
o Ulceration (can get systemic effects)

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4
Q

What other variables determine percutaneous absorption?

A
o	Skin hydration (hydrating skin prior, increases absorption)
o	Occlusion (applying topical, then wrapping in impervious material, ex – lotion on feet, then wrap in saran wrap)
o	Age (children have increased total body surface to body volume ratio)
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5
Q

What are the risk factors for systemic toxicity?

A
  • Time
  • Surface area
  • Body site
  • Skin barrier function
  • Use of occlusion
  • Inappropriate use
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6
Q

What are the consequences of systemic toxicity in corticosteroids, silver products and antibiotics?

A

Corticosteroids
o Altered HPA axis

Silver products
o Renal or hepatic problems

Antibiotics
o GI effects, renal effects

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7
Q

Describe the spectrum of inflammation and the cooresponding spectrum of dermatologic vehicles

A

INFLAMMATION

Acute inflammation
o Erythema, edema, vesiculation, oozing, crusting, infection, puritus

Chronic inflammation
o Erythema, scaling lichenification, dryness, puritus

TREATMENT

Appropriate treatments
o	Wet dressing (solutions) 
o	Powders, lotions, aerosols, sprays
o	Creams (oil-in-water emulsions), gels
o	Ointments (water-in-oil emulsions, inert bases)

This means that with acute inflammation, wet dressings and powders/lotions are more appropriate, but as you progress to chronic inflammation, creams and ointments will be needed

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8
Q

What are the general treatment axioms

A
  • If wound is wet, dry it
  • If wound is dry, wet it
  • If wound is inflamed/irritated, soothe it
  • If chronic wound is stagnant, irritate/turn into chronic wound
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9
Q

What are the types of topical medications and vehicles we can use?

A
  • Open Wet Dressings
  • Closed wet dressings
  • Powders
  • Lotions
  • Cream
  • Gel
  • Ointment
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10
Q

Describe open wet dressings and closed wet dressings

A

Open Wet Dressings
o Causes vasoconstriction and decreased inflammation
o Cleanse wound of exudates, crusts, and debris
o Indication: acute inflammatory conditions, erosions, and ulcers

Closed wet dressings
o Can cause maceration

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11
Q

Describe powders, lotions, creams, gels and ointments

A

Powders
o Used to reduce moisture, maceration, and friction

Lotions
o Suspension of powder in water (can be a little too drying for some skin)
Cream
o Semisolid emulsion of oil in water (much more hydrating than a lotion)
Gel
o Semisolid emulsion that liquefies on contact, leaving thin film
Ointment
o Water droplets suspended in oil or petroleum

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12
Q

Describe the relative potency, hydration/drying properties, stage of dermatitis treated, sites to avoid and sensitization risk for OINTMENTS

A
  • Relative potency = strong
  • Hydration/drying properties = hydrating
  • Stage of dermatitis treated = chronic
  • Sites to avoid = sites with maceration
  • Sensitization risk = very low
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13
Q

Describe the relative potency, hydration/drying properties, stage of dermatitis treated, sites to avoid and sensitization risk for CREAMS

A
  • Relative potency = moderate
  • Hydration/drying properties = some hydration
  • Stage of dermatitis treated = acute to subacute
  • Sites to avoid = sites with maceration
  • Sensitization risk = significant
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14
Q

Describe the relative potency, hydration/drying properties, stage of dermatitis treated, sites to avoid and sensitization risk for GELS

A
  • Relative potency = stong
  • Hydration/drying properties = drying
  • Stage of dermatitis treated = acute to subacute
  • Sites to avoid = fissures, erosions
  • Sensitization risk = significant
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15
Q

Describe the relative potency, hydration/drying properties, stage of dermatitis treated, sites to avoid and sensitization risk for LOTION/SOLUTION

A
  • Relative potency = low
  • Hydration/drying properties = variable
  • Stage of dermatitis treated = acute
  • Sites to avoid = fissures, erosions
  • Sensitization risk = significant
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16
Q

Describe “fingertip unit” prescription amounts

A

Ointment expressed from tube from index finger MPJ to tip of finger

  • Approximately 0.5 grams
  • 1 FTU Should cover plantar aspects of 1 or both feet
  • Need 2 FTU to cover one foot
  • If just doing interspaces, should only need 0.25-0.5 FTU or 0.1-0.25 grams

For most podiatric applications a 15 gram tube will last 1 month
- If prescribing for several months, use 60 gram tube because it is less expensive

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17
Q

Common topicals used in podiatry

A

Most common
o Antibiotics
o Antifungals
o Corticosteroids

Less common
o Antivirals
o Pain medications

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18
Q

Topical antibiotics

A
  • Most commonly in cream or ointment form
  • Solutions occasionally used for soaking (Dakin’s, acetic acid, Burrow’s)
  • Antiseptics (for surgical preparation and scrub)
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19
Q

Topical antibiotics - creams and ointments

A
  • Bacitracin
  • Polysporin
  • Neosporin
  • Mupirocin (bactroban)
  • Gentamicin
  • Silvadene
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20
Q

Bacitracin cream/ointment

A

Contains one abx – bacitracin

Coverage

  • Good Gram (+) coverage, minimal to no gram (-) coverage
  • Can cause sensitivity reaction, particularly with stasis dermatitis
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21
Q

Polysporin cream/ointment

A

Contains 2 abx – bacitracin and polymyxin B

PolymyXin B effective against gram (–)

  • Including pseudomonas
  • Contact allergy rare

This is her number one choice – don’t need the third one because of problems (below)

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22
Q

Neosporin cream/ointment

A

Contains 3 abx – bacitracin, polymyxin B, and neomycin

Neomycin – covers gram (+) and (-)

  • Good S. aureus coverage
  • Does not cover Pseudomonas, or Bacteroides
  • Weak Strep activity
  • 1% of population has contact allergic sensitivity, rate can increase to almost 10% in patients with prolonged use
  • Bacitracin causes coreaction with neomycin
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23
Q

Mupirocin (bactroban) cream/ointment

A

o Effective against MRSA

o Can be used in nasal passages for MRSA carriers

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24
Q

Gentamicin cream/ointment

A

o Good gram (-) coverage, notably Pseudomonas

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25
Q

Silvadene cream/ointment

A

o Effective against Gram (+) and (-)
o Shouldn’t use in patients allergic to sulfonamides
o If using in large area over long time period, can get significant absorption of silver
o Can occasionally cause brown/gray hyperpigmentation of skin with use
o Commonly used with burn patients

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26
Q

Topical antibiotic solutions

A
  • Dakin’s solution

- Acetic acid solution

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27
Q

Dakin’s solution

A

o Sodium hypochlorite solution – AKA bleach

o Comes in 0.5%, 0.25%, or 0.125% strengths

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28
Q

Acetic acid solution

A

o 5% solution (pretty much just vinegar)
o Effective against superficial pseudomonas infections
o Also has drying effect – Good for wet tinea pedis infection

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29
Q

Astringent solutions

A
  • Burow’s solution

- Epsom salt

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30
Q

Burrow’s solution

A

o 1:40 mixture or 0.14% aluminum acetate solution

o Used to dry out wounds – i.e. macerated tinea pedis or wet dermatitis

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31
Q

Epsom salt solution

A

o Magnesium sulfate
o 2 Tbsp./pint of H2O
o Also used for drying effect

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32
Q

Topical antiseptics

A

Used for presurgical scrub for surgeon and/or patient
o Chlorhexidine
o Povidone-Iodine

Over the counter antibacterial soaps
- Triclosan

33
Q

Chlorohexidine antiseptic

A
  • Broad spectrum coverage
  • S. aureus, P. aeruginosa, S. marcescens, and facultative anaerobes
  • Low rate of sensitization
34
Q

Povidone-Iodine antiseptic

A
  • Broad spectrum against gram (+) and (-)
  • High incidence of dermatitis
  • Can also be used as a topical to help dry wounds
35
Q

Triclosan antibacterial soap

A
  • Most common abx soap ingredient

- Broad spectrum activity

36
Q

Antifungal classes

A
  • Polyenes (not used much in podiatry)
  • Azoles (older class, mostly fungistatic)
  • Allylamines/benzylamines (newer class, better potency/efficacy, fungicidal, can actually kill fungus)
  • Others (ciclopirox (loprox))
37
Q

Polyenes

A

Nystatin
o Effective against Candida albicans
o Not highly effective against dermatophytes, bacteria, or viruses

Remember - not commonly used in podiatry

38
Q

General characteristics of azoles

A

o Azoles are effective against dermatophytes
o We are not responsible for dosing information, but just from a clinical perspective, some agents will be more effective if they only need to apply it once a day, just from the compliance perspective

39
Q

List of azoles

A
  • Miconazole (Monostat-Derm, Micatin)
  • Clotrimazole (Lotramin)
  • Econazole (Spectazole)
  • Ketoconazole (Nizoral)
  • Sertaconazole (Ertaczo)
  • Oxiconazole (Oxistat)
  • Efinaconazole topical (Jublia)
40
Q

Miconazole (Monostat-Derm, Micatin)

A

o Good activity against T. rubrum, T. mentagrophytes

o Has mild effectiveness against some Gram (+)

41
Q

Clotrimazole (Lotramin)

A

o Broad spectrum against, Trichophyton, Epidermophyton, and Microsporum
o Also active against Gram (+) and Candida

42
Q

Econazole (Spectazole)

A

o Broad spectrum against Trichopyton, Microsporum, Epidermophyton, C. albicans, and M. furfur
o Shows some gram (+) and (-) coverage

43
Q

Ketoconazole (Nizoral)

A

o Broad spectrum activity against dermatophytes

44
Q

Sertaconazole (Ertaczo)

A

o Relatively lipophilic
o Effective against T. rubrum, T. mentagrophytes, E. floccusum, Candida
o Moderate activity against Gram (+) bacteria

45
Q

Oxiconazole (Oxistat)

A

o Good absorption into stratum corneum, will stay for several days after treatment

46
Q

Efinaconazole topical (Jublia)

A

o 10% solution
o Used for onychomycosis
o Needs to be used QD for 48 weeks (LONG time)

47
Q

List of allylamines and benzylamines

A
  • Naftifine (Naftin)
  • Terbinafine (Lamasil)
  • Butenafine (Mentax)
48
Q

Naftifine (Naftin)

A

o Highly lipophilic, allows good penetration and high concentration in stratum corneum
o Expensive
o Earlier symptomatic relief than Lotramin

49
Q

Terbinafine (Lamasil)

A

o Highly lipophilic and binds well to stratum corneum
o Broad spectrum against dermatophytes, molds, C. albicans
o Effective against chronic tinea pedis

50
Q

Butenafine (Mentax)

A

o Broad spectrum against dermatophyes and dimorphic fungi

51
Q

Other antifungals

A

Ciclopirox Olamine (Loprox, Penlac Nail Lacquer)

52
Q

Ciclopirox Olamine (Loprox, Penlac Nail Lacquer)

A

o Used for tinea pedis or onychomycosis
o Has Gram (-) and (+) activity as well as anti-inflammatory properties (good for tinea pedis with secondary bacterial infection)
o Lacquer shown to have 40% clinical and mycological efficacy (have to use daily for several months)

53
Q

Anti-dermatophyte potnecy

A

From MOST to LEAST potent

  1. Butenafine (Mentax) = Terbinafine (Lamasil)
  2. Ciclopirox (Loprox)
  3. Naftifine (Naftin)
  4. Azoles
54
Q

Propylene glycol content in topical antifungals

A
  • If there is irritation, maybe switch to something that is propylene and glycol free
  • Note that the more potent ones have the propylene and glycol in them

Antifungas WITHOUT propylene glycol

  • Miconazole (Micatin)
  • Clotrimazole (Lotrimin)
  • Econazole (Spectazole)
  • Naftifine (Naftin)
  • Ciclopirox (Loprox)

Antifungals WITH propylene glycol

  • Terbinafine (Lamasil)
  • Butenafine (Mentax)
  • Ketoconazole (Nizoral)
  • Oxiconazole (Oxistat)
55
Q

Mechanism of action/anti-inflammatory effects of topical corticosteroids

A

Reduces number and function of inflammatory cells and chemical mediators
o Reduced inflammation and immune response

Reduces keratinocyte proliferation, fibroblast activity, and dermal volume(due to decreased H2O content)
o Thinning of the skin
o Prolonged use causes skin atrophy

56
Q

Indications for topical steroids

A
  • Inflamed or irritated skin, non infectious in nature*

- Examples: dermatitis, eczema, psoriasis, lichen planus

57
Q

Contraindications for topical steroids

A

Absolute
o Hypersensitivity to the topical corticosteriod or vehicle

Relative
o Bacterial, fugal, or viral infection
o Ulceration (higher chance of systemic effect of steroids)

58
Q

Systemic adverse effects of topical corticosteroids

A

o Suppression of HPA axis
o Iatrogenic Cushing’s syndrome
o Growth retardation in infants and children

59
Q

Local adverse effects of topical corticosteroids

A
o	Epidermal atrophy
o	Steroid rebound
o	Allergic or contact dermatitis
o	Exacerbation or increased susceptibility to bacterial, fungal and viral infections
o	Reactivation of Kaposi’s sarcoma
o	Delayed wound healing
o	Tachyphylaxis (tolerance to med)
60
Q

Risk factors for systemic effects of topical corticosteroids

A
o	Infant or child
o	Liver or renal disease
o	Amount applied
o	Potency
o	Use of occlusion
o	Lack of physician supervision
61
Q

Risk factors for local atrophy due to topical corticosteroids

A
o	Infant or child
o	Potency
o	Duration of treatment
o	Use of occlusion
o	Location (face, neck, axilla, groin, upper inner thighs, pretibial location)
62
Q

Absorption of topical corticosteroids

A
  • About 1% of TCS will be absorbed on normal forearm skin (less on thick skin like sole of foot)
  • This will increase if skin irritated, inflamed, or thinned
  • Placing under occlusion dramatically increases absorption (Increases skin surface area by 40%)
63
Q

Choosing a topical corticosteroid - factors to consider

A
  • TCS potency
  • Vehicle
  • Brand name vs Generic
  • Price and cost-effectiveness considerations
  • Proper amount to dispense
  • NOTE: Choose the least potent topical that will still be affective, or quickly taper down
64
Q

Potency classes of topical corticosteroids

A
  • Very High (I)
  • High (II &III)
  • Medium (IV & V)
  • Low (VI &VII)
65
Q

Very high (I) potency of topical corticosteroids

A

o Short term use only

o Best for thick, lichenified or hypertrophic skin resistant to high potency topical steroids

66
Q

High (II &III) potency of topical corticosteroids

A

o Severe dermatitis, thick, lichenified, or hypertrophic skin
o Short term use only

67
Q

Medium (IV & V) potency of topical corticosteroids

A

o Moderate dermatitis

o Good for extremities as long as not on extremely thickened skin

68
Q

Low (VI &VII) potency of topical corticosteroids

A

o Mild dermatitis
o Preferred treatment for large areas
o Best if long term treatment required
o Best for thin skin

69
Q

List of very high (I) potency corticosteroids

A

o Amcinonide ointment 0.1% (Cyclocort)
o *Betamethasone dipropionate ointment 0.05% (Diprosone)
o *Desoximethasone cream 0.25% (Topicort)
o *Desoximethasone gel 0.05% (Topicort)
o Diflorasone diacetate ointment 0.05% (Florone)
o Fluocinonide 0.06% (Lidex)
o Halcinonide cream 0.1% (Halog)

70
Q

List of potent (II) corticosteroids

A

o *Betamethasone benzoate gel 0.025% (Benisone)
o *Betamethasone dipropionate cream 0.05% (Diprosone)
o *Betamethasone valerate ointment 0.1% (Valisone)
o Diflorasone diacetate cream 0.05% (Florone)
o Triamcinolone acetonide cream 0.5% (Aristocort)

71
Q

List of mid-potency (III) corticosteroids

A

These are a lot of LOTIONS (change of vehicle = change of potency)
o Amcinonide cream 0.1% (Cyclocort)
o Betamethasone valerate lotion 0.1% (Valisone)
o Flucinolone acetonide cream 0.2%, ointment 0.025% (Fluonid, Synalar)
o Hydrocortisone valerate cream 0.2% (Westcort)
o *Triamcinolone acetonide ointment 0.1% (Aristocort, Kenalog) - Still a prescription, but a lower potency for those who need to apply over a large area – comes in a large jar (not tiny tube)

72
Q

List of low potency (IV) corticosteroids

A

o Aclometasone dipropionate cream 0.05% (Aclovate)
o Betamethasone valerate cream 0.1% (Valisone)
o Clocortolone pivalate cream 0.1% (Cloderm)
o Fluocinolone acetonide cream 0.025% (Fluonid, Synalar)
o Flurandrenolide 0.05% (Cordran)
o Hydrocortisone valerate cream 0.2% (Westcort)
o Triamcinolone acetonide cream 0.01%, lotion 0.025% (Kenalog, Aristocort)

73
Q

List of mild (V) corticosteroids

A

Mostly OTC
o Desonide cream 0.05% (Tridesilon)
o Flumethasone pivalate cream 0.03% (Locorten)
o Fluocinolone acetonide solution 0.01% (Fluonid, Synalar

74
Q

List of least potent (VI) corticosteroids

A

OTC
o Prednisolone 0.5% (Meti-derm)
o Methylprednisolone 1% (Medrol)
o Fluorometholone 0.025% (Oxylone)
o Dexamethasone 0.1% (Decadron Phosphate)
o *Hydrocortisone 0.25, 0.5, 1.0, 2.5% (Hytone, Nutraderm, Synacort)

75
Q

Combination therapy options

A
  • Corticosporin

- Lotrisone

76
Q

Corticosporin

A

o Neomycin + Polymyxin + Hydrocortisone

o Corticosteroid-responsive dermatoses with secondary infection

77
Q

Lotrisone

A

o Clotrimazole + Betamethasone

o Inflamed tinea pedis

78
Q

Anti-hyperkaratotics

A
  • Used for patients with severe chronic hyperkaratosis
  • Helps to hydrate, soften and debride thickened skin

Lactic acid
o Lac-Hydrin, Amlactin
o 12% Cream or Lotion
o May cause irritation in non-intact skin

Urea
o Carmol 40
o 40% urea cream, lotion, gel