Topical Therapies

Leland Jaffe DPM, FACFAS, CWSP

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 Principles of Topical Therapy
• Efficacy of topical medications is due to:
1) Active ingredient (strength)
2) Anatomic location to be applied
3) Vehicle (the mode of transportation)
4) Concentration of the medication

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 Vehicles (Base)
• Powders Determines Rate of Absorption
• Ointments
• Creams
• Lotions
• Solutions
• Gels
• Foams
• Tapes

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 Powders
• Fine particulates of active ingredient with talc
• Indications
• Moist, sweaty area
• Area of friction (interdigital)
• Large surface areas
• Advantages
• Absorb moisture
• Decrease friction
• Cover large areas
• Disadvantages
• Messy
Image from healthy.kaiserpermanente.org
• Poor delivery/absorption of medication

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• Limited number of compounds Ointments
• Consists primarily of greases (petroleum)
• Little to no water
• Indications
• Dry, cracked skin
• Scaling
• Lubrication
• Advantages
• Lubricant
• Facilitates heat retention
• Decreases water loss
• Semi-occlusive
• Well-absorbed
• Increases potency of medication
• Disadvantages
– Greasy
– Not as useful in hairy area
– Too occlusive for intertriginous areas
– Stains clothing Image from www.petinfoclub.com

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 Creams
• Mixture of chemicals (oils) and water
• Usually contains a preservative
• White color (somewhat greasy)
• Advantages
• Easy application (high versatility)
• May be used in nearly any area
• Improve cosmetic appearance than ointments
• Useful in intertriginous areas (groin / axilla)
• Stronger than lotions
• Disadvantages
• May cause some irritations/stinging/allergy
• Less potent than ointments
• Dries more quickly than ointments
Image from www.mdcustomrx.com

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 Lotions
• Oil surrounded by water (emulsion / topical suspension)
• Advantages
• Easy application (easy to spread)
• Able to cover large area
• Able to use over hair
• Evaporate to cause a cooling & drying effect
• Anti-pruritic often added
• Drying effect on oozing lesion
• Little residue
• Disadvantages
• Less potent than ointments & creams
• Must shake before use to obtain desired therapeutic effect

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 Solutions
• Active ingredient along with water or other non-
aqueous solutions (alcohol or propylene glycol)
• Typically in forms of soaking solution or dressing

• Indications
• Scalp – penetrates easily through hair
• Moist areas
• Advantages
• Water or non-aqueous solution evaporates
and leave medication on skin
• Disadvantages
• May be over-drying Image from identify-pills.com

• Alcohol burns on open wounds

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 Gels
• Propylene glycol and water (some alcohol)
• Liquefies upon contact with skin
• Indications
• Facial & scalp dermatoses
• Advantages
• Rapid drying
• Excellent penetration properties
• Non-staining
• Therapeutically comparable to ointment
with cosmetic advantages of cream
• Easily used over areas with hair
• Disadvantages
• Drying due to alcohol base

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 Foams
• Pressurized collection of gaseous bubbles
with active ingredient in liquid film
• Indications/Advantages
• Spreads easily over large areas
• Useful over hair/scalp
• Disadvantages
• More expensive
• Drying
Image from www.hairstalk.com

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 Tape
• Tape impregnated with active
ingredients
• Indications
• Thickened lesions
(lichen planus, warts, etc.)
• Advantages
• Stays in place
• Disadvantages
• Cannot use on open lesions
(burning) Image from www.prescriptiongiant.com

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Prescriptions for Topical Medications

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 Prescriptions of Topical Medications
• What information goes into topical rx?
– Fluocinonide .05% cream
– Sig: Apply a thin layer to affect area (foot) BID
– Disp: 60 grams
– Refills: 2

– Generic name of medication

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 Prescriptions of Topical Medications
• What information goes into topical rx?
– Fluocinonide .05% cream
– Sig: Apply a thin layer to affect area (foot) BID
– Disp: 60 grams
– Refills: 2

– vehicle

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 Prescriptions of Topical Medications
• What information goes into topical rx?
– Fluocinonide .05% cream
– Sig: Apply a thin layer to affect area (foot) BID
– Disp: 60 grams
– Refills: 2

– Concentration

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 Prescriptions of Topical Medications
• What information goes into topical rx?
– Fluocinonide .05% cream
– Sig: Apply a thin layer to affect area (foot) BID
– Disp: 60 grams
– Refills: 2

– Sig: directions for application

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 Prescriptions of Topical Medications
• What information goes into topical rx?
– Fluocinonide .05% cream
– Sig: Apply a thin layer to affect area (foot) BID
– Disp: 60 grams
– Refills: 2

– Amount to be dispensed

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 Prescriptions of Topical Medications
• What information goes into topical rx?
– Fluocinonide .05% cream
– Sig: Apply a thin layer to affect area (foot) BID
– Disp: 60 grams
– Refills: 2

– Number of refills

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 Estimated Body Surface Area
• 1 palm = 1% Body surface area (BSA)

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 Estimating Topical Medications
• Quantity of topical medication placed on pad of index finger
from distal tip to DIPJ
– Dispensed by 5 mm nozzle  standard
• Fingertip unit (FTU) = 500 mg
– 500 mg treats 2% BSA

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 + =

How many grams of topical medication

should you prescribe for a 2% BSA skin
lesion QD x 60 days application?

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 Estimating BSA: Rule of Nines

▪ The “rule of nines” is an effective,

quick way of estimating the
affected BSA
▪ Assessing burns
▪ The body is divided into areas of 9%
▪ Less accurate in children

Source: McPhee SJ, Papadakis MA: Current Medical Diagnosis and Treatment 2010, 49th Edition: http://www.accessmedicine.com. Copyright © The McGraw-Hill Companies, Inc.

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 Estimating Topical Medications
• 1 g cream = 10 cm x 10 cm (100 cm2) area of skin
• 1 g ointment  covers area 5-10% larger

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Topical steroids

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 Topical Corticosteroids
• Anti-inflammatory response in the skin
– Vasoconstrictive effect
• Treats many types of conditions
– Hyperproliferative conditions (e.g. psoriasis)
– Inflammation
– Immunologic
• Symptomatic treatment
– Pruritis
– Burning sensation

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 Topical Corticosteroids
• Organized based on strength of
medication  potency
(Groups I through VII)
– Steroids in same class are
equivalent in strength
• Goal is the know at least 1
medication from each class

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 Topical Corticosteroids by Potency
Ultra-high Potency Clobetasol propionate .05% cream and ointment
Class I Betamethasone diproprionate (Diprolene) .05%
cream and ointment

High Potency Mometasone furoate (Elocon) .1% ointment

Class II Fluocinonide cream, ointment .05%

Medium Potency Triamcinolone acetonide .1% cream and ointment

Class III-V Mometasone furoate cream .1%

Lowest Potency Hydrocortisone 1%, 2.5% cream

Class VI-VII Fluocinolone acetonide cream .01% cream

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 Topical Corticosteroids by Potency
Ultra-high Potency Clobetasol propionate .05% cream and ointment
Class I Betamethasone diproprionate (Diprolene) .05%
cream and ointment
High Potency Mometasone furoate (Elocon) .1% ointment
Class II Fluocinonide cream, ointment .05%

Medium Potency Triamcinolone acetonide .1% cream and ointment

Class III-V Mometasone furoate cream .1%

Lowest Potency Hydrocortisone 1%, 2.5% cream

Class VI-VII Fluocinolone acetonide cream .01% cream

Note that mometasone ointment is high potency while

cream is medium potency…why?

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 Selection of Topical Steroid
Ultra-high Potency -Severe dermatoses
Class I -Non-facial & non-intertriginous
areas
-Palms, soles, thick plaques on
extensor surfaces
Medium – high Potency -Mild-moderate non-facial & non-
Class II - V intertriginous areas
-okay on flexor surfaces for brief
periods
Low Potency -large surface area lesions and thinner
Class VI-VII skin
-Face, eyelid, intertriginous areas

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 Topical Absorption of Steroids
• Better absorbed through areas of inflammation and
desquamation
– As compared to normal intact skin
• Absorbs quicker through stratum corneum of infants as
compared to adults
• Ointments allow more drug absorption
– More potent than creams or lotions

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 Complications of Topical Steroids
• Irritation / Hypersensitivity / dermatitis
• Pigmentation changes (hypopigmentation)
• Thinning of the skin (skin atrophy)
• Stretch marks (striae)
• Telangiectasia
• Hair growth
• Tachyphylaxis
• Can also suffer systemic effects (RARE)
– Cushing’s syndrome
– Hypertension
– HPA suppression
– Hyperglycemia

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 TACHYPHYLAXIS
-decrease in responsiveness to a drug
-acute tolerance to the vasoconstrictive action of
topically applied steroids
-studies: vasoconstriction decreases progressively
following 3x/ day x 4 days application of strong
steroid; and returns 4 days after termination of
therapy
**apply steroids on interrupted schedule

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 Duration of Treatment
• Super high potency
– < 4 weeks of treatment
• High and medium potency
– <6-8 weeks of treatment
• Low potency
– Rare side effects

*stop therapy when condition resolves

*avoid rebound/flares of condition
-taper with reduction of potency
-reduce dose frequency

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Topical Antifungals

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 Topical Antifungals
• Fungistatic (stop fungi from growing)
• Fungicidal (kill fungus organism)
• Not all conditions respond to topical antifungals
– Hair infections
– Nail infections

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Imidazoles (Primarily fungistatic) Candida
-Ketoconazole (Rx and OTC) Dermatophytes
-Econazole (Spectazole) –dermatophytes + yeast
-Oxiconazole (Oxistat)
-Clotrimazole (Rx and OTC)—Lotrimin AF cream
Fungicure Spray
-Clotrimazole + betamethasone (Lotrisone)

Allylamines & Benzylamines (fungicidal) -better choice for dermatophytes

-Naftifine (Naftin) (not indicated for candida)
-Terbinafine (Lamisil) – OTC
-Butenafine (Mentax, Lotrimin Ultra)

Polyenes (fungistatic in low concentrations) -better choice for candida

-Nystatin (not indicated for dermatophytes)

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 Antifungal Powders
• Powders help keep areas dry
• Can be used as ppx (prophylaxis) to prevent recurrence
• Tolnaftate (Tinactin)
– Apply Qday or BID to affected areas
• Nystatin (Nystop, Pedi-Dry)
– Apply to affected areas BID
• Miconazole (Desenex, Zeasorb)
– Qday x 4 weeks

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 Topical Antifungals
• Preferred treatment for superficial fungal infections
– Low cost
– Easy to use
– Low potential for side effects / interactions
– Acceptable efficacy
– Many OTC selections

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 Topical antifungals (Tinea Unguium)
• Usually not effective unless SWO (superficial white onychomycosis)
1) Ciclopirox nail lacquer 8% (Penlac) – 1st FDA approved topical treatment option
-Mild to moderate onychomycosis without lunula involvement
-Apply daily for 1 week then remove with acetone
*low cure rate --- 10%
2) Efinaconazole 10% solution (Jublia)
-apply daily for 48 weeks ***compliance
-low efficacy
-15-18% clear nails
-25% almost clear nails
*application of 40% urea cream can increase permeability of nail plate by 20x

Yamaguchi H, et al. Jpn J Antibiot. 2001 54(6): 323-30.

Bassiri-Jahromi S, et al. J Dermatol Treatment 2012; 23 453-6.
Murdan S. Expert Opin Drug Deliv. 2008 5 (11): 1267-82)

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 Topical Medications for Onychomycosis
• Nail plate permeability
– Inherently low
– Hydrophilic
– Dense keratin network
• Terbinafine (Lamisil) and Itraconazole (Sporonox)
– High molecular weight
– Limited water solubility
*do not penetrate nail effectively

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 Ciclopirox
• Ciclopirox 8%, Penlac topical nail lacquer
• One of two FDA approved topical medications for
treatment of onychomycosis
• Nail penetration is low
• Comes in 6.6 mL bottle with an applicator
• Apply q day, usually at bedtime and then remove
with alcohol q 7 days
• Complete cure rate is < 10 %
• Must remove loose pieces of nail and file down
regularly

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 Jublia
• Efinaconazole topical soln. 10%
• Newer medication
• FDA approved medications for the
treatment of onychomycosis
– Dermatophytes
• Comes in 4 mL bottle with brush applicator
• Apply q day
• Complete cure rate 15 – 18%

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 Two Jublia Phase 3 Trials
• Efficacy of Efinaconazole
• Applied 1x daily x 48 weeks
• Patients 18-70 yoa
• Mild-moderate DSO involving up to 50% nail involvement
• Patients randomized to efinaconazole or vehicle (placebo)
• Complete cure rates
– Group 1
• Jublia: 17.8%
• Placebo: 3.3%
– Group 2
• Jublia: 15.2%
• Placebo: 5.5%

Elewski BE, Rich P, Pollak R, Pariser DM, Watanabe S, Senda H, Ieda C, Smith K, Pillai R, Ramakrishna T, Olin JT. Efinaconazole 10% solution in the treatment of toenail
onychomycosis: Two phase III multicenter, randomized, double-blind studies. J Am Acad Dermatol. 2013 Apr;68(4):600-8.

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 Other Solutions
• FungiNail (25% Undecylenic Acid)
– NOT FDA approved for onychomycosis
– OTC medication, 30 mL bottle
– Apply BID
– May improve nail appearance
• Fungoid Tincture (Miconazole Nitrate 2%)
– Tinea, interspaces
– NOT FDA approved for onychomycosis
– Apply BID to affected areas

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Topical Treatment of Psoriasis

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 Topical Treatment of Psoriasis
• Due to higher rate of epidermal turnover
• Vitamin D analogs
– Calcipotriene (Dovonex)
• Synthetic Vitamin D3
• Inhibits keratinocyte proliferation
– Calcitriol (Vectical)
• Natural active form of Vitamin D3
• Inhibits keratinocyte proliferation
– Promotes keratinocytes differentiation
• Inhibits T cell proliferation

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 Topical Psoriasis Treatment
• Calcpotriene and betamethasone dipropionate
foam .005% / .064%
– Enstilar

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 Topical Treatment of Psoriasis
• Tazarotene .05% and .1%
– Topical retinoid (Vitamin A derivative)
– Plaque type: slows skin growth / anti-inflammatory
– Often used with topical steroid to reduce skin irritation
– Lacks side effects of long-term steroids
• Tar 2-5%
– Anti-proliferative effect / anti-inflammatory effect
– Combined with salicylic acid to penetrate thick plaque
– Disadvantages: messy, stains clothing

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Keratolytics

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 Urea / Lactic Acid Moisturizers
• Urea
– Enhances water-binding capacity of
stratum corneum
– Decreases trans-epidermal water loss
with long-term use
– Acts as a skin humidifier  by
decreases trans-epidermal water loss
– Higher concentration urea keratolytic
• 40% urea cream 25% urea cream
OTC

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 Lactic Acid / Salicylic Acid
• Accelerate softening of the skin
• Increases moisture in skin
• Increases skin slough
• Keratolytic effect
– Dissolves keratin

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Topical antibiotics

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 Mupirocin
• Mupirocin (Bactroban) 2% ointment or cream
• Indications:
– Treats MRSA colonization
• Nasal carrier
– Skin infection
– Impetigo

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• Cleocin T (Clindamycin topical) 1% gel
– Interdigital bacterial infection
– Indications?
• Erythrasma  bacterial
• Acne vulgaris  bacterial

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 Most Common
• Bacitracin  gram + organisms

• Neosporin (bacitracin, neomycin, polymyxin B)

– Neomycin  gram – bacteria
– Polymyxin B  gram - bacteria

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 Dapsone
• Dapsone (Aczone) 5% or 7.5% gel
• Apply a thin layer BID to affected area
• Traditionally used for acne vulgaris
• Also used for pustular skin lesions/ulcerations elsewhere
– Pyoderma gangrenosum
• Mechanism of action
– Bacteriostatic
– Competes with para-aminobenzoic acid (PABA), inhibiting
folic acid synthesis

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 Miscellaneous
• Topical NSAIDS
– Diclofenac topical (Voltaren)
• 1,3% gel; 1.5% soln

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 Drying Agents
• Zeasorb (miconazole 2%) powder
• Drysol (Aluminum Chloride 20%) solution
– Apply a thin layer qday at night (QHS) x 2 – 3 days until appropriate dryness
– Then once or twice a week as needed
– Can cover with plastic wrap for greater affects
• Castellani paint 1.5% solution
– Antiseptic and drying properties
– Phenol and fuchsin

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 Topical Anti-pruritics
• Topical diphenhydramine  Benadryl
• Hydrocortisone OTC cream  steroid
• Camphor/menthol (Sarna)
• Pramoxine / Calamine Topical (Aveeno)
• Calamine

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