Topical Medications for Skin Conditions

Pharmacology in Dermatology

• Presented by Martha L. Sikes, DMSC, RPh, PA-C

Topical Medications

• Ointments: Petrolatum base (e.g., Vaseline)
• Gels/solutions: Higher alcohol content, oil-free
• Creams/lotions: Suitable for dry skin, non-irritating formulations
• Lotions/foams: Can be applied to areas with hair
• Occlusion order: Ointment > cream > lotion > gel > solution

Topical Corticosteroids

• MOA: Decrease cell proliferation, inhibit inflammatory mediators, cause local vasoconstriction
• Dosage: Dependent on affected area
• Formulations:
  • Areas with hair: lotions, gels, aerosols, solutions, foams
  • Weeping lesions: lotions, gels, creams
  • Dry, scaly lesions: ointments
• Usage: Can be used on many skin areas
• Vehicle choice: Important for minimizing adverse effects (AEs)

Topical Corticosteroids: Occlusive Dressings

• Increased skin penetration

• Increased systemic effects

• Increased secondary bacterial/fungal infections

• Do not use with very high/ultra high potency (except lichenified lesions)

• Do not leave on for more than 12 hours

Topical Corticosteroids: Adverse Effects (AEs)

• Local AEs:
  • Drying/cracking of skin
  • Thinning of epidermis
  • Atrophic striae (possibly permanent)
  • Hypopigmentation
• Systemic AEs:
  • Usually with large areas, prolonged use, occlusive dressings
  • HPA suppression (especially in pediatrics)

Topical Corticosteroids: Potency

• Medications have varying potency based on strength/dosage form (I-VII)
• USP potency ratings: Low, Medium, High, Very High
• Low Potency: Face, genitals, axilla, skin folds
• Medium Potency: Trunk, arms, legs
• Limit weekly dose to 90-100 grams (Medium potency)
• Very High Potency: Palms, soles, resistant conditions
• Limit weekly dose to 50 grams (Very high potency)
• Treatment duration generally does not exceed 2 weeks

Topical Calcineurin Inhibitors (Topical Immunomodulators)

• MOA: Blocks inflammatory mediators by modulating T-cell function and depressing cell-mediated immune responses

• Indications:

  • Second-line therapy for atopic dermatitis (intermittent use)
  • Off-label use: psoriasis, seborrheic dermatitis, rosacea, vitiligo

• AEs: Temporary stinging, burning, pruritus

• Precautions: Based on animal studies, risk of skin cancer and lymphomas

• Precaution: Do not use on pre-malignant/malignant lesions

• Precaution: resolve cutaneous bacterial/viral infections before use

• Precaution: avoid sun exposure, use with occlusive dressing (unknown effects)

• Precaution: avoid use in immunocompromised patients

Topical Calcineurin Inhibitors (Specifics)

• Pimecrolimus 1% (Elidel): Cream, for adults and children >2 years old
• Tacrolimus 0.03%, 0.1% (Protopic): BID application

PDE-4 Inhibitor

• MOA: Results in increased intracellular cAMP levels to decrease proinflammatory response
• AEs: Application site pain, burning, or stinging (4%)
• Specifics
  • Crisaborole (Eucrisa) 2% ointment: For mild-to-moderate atopic dermatitis in patients 2 years of age and older
  • Roflumilast (Zoryve):
    • Psoriasis (0.3% cream)
    • Seborrheic dermatitis (0.3% foam)
    • Atopic dermatitis (0.15% cream)

Miscellaneous Topical Agents

• Tazarotene (Tazorac®): Gel 0.05% or 0.1% for mild-to-moderate psoriasis, acne
• Calcipotriene (Dovonex®), calcitriol (Vectical®): Topical synthetic vitamin D analogs for mild-to-moderate psoriasis
• Coal Tar: Keratolytic and may have antiproliferative/anti-inflammatory effects, for psoriasis
• Salicylic acid in shampoos (typically 3-4% strength) can help with scalp psoriasis and dandruff
• Removal and smoothing of scale, treating hyperkeratosis, enhancing steroid penetration

JAK Inhibitors

• MOA: Inhibit JAK, a group of intracellular tyrosine kinases that influence cellular processes including inflammation
• AEs: Nasopharyngitis, bronchitis, increased eosinophils, diarrhea, folliculitis, tonsillitis
• Box warning: Serious infection, sudden cardiovascular death, malignancies, MACE (major adverse cardiovascular events), thrombosis
• Indications: Atopic dermatitis

AhR Agonist

• MOA: Aryl hydrocarbon receptor (AhR) agonist
• AEs: Folliculitis, nasopharyngitis, contact dermatitis, headache, pruritus
• Use: Atopic dermatitis, psoriasis

Systemic Corticosteroids

• Dermatologic uses: Contact dermatitis, atopic dermatitis, other
• Use: Short courses for acute exacerbations of chronic atopic dermatitis (eg., prednisone 40-60 mg/day for 3-4 days, then 20-30 mg/day for 3-4 days).
• Prednisone (Deltasone)
• Dexamethasone (Decadron)

Systemic Agents - Psoriasis

• Acitretin (Soriatane®): Oral retinoid
• Methotrexate: Oral/IM treatment
• Cyclosporine (Neoral or Sandimmune®): Suppresses T-cell activation
• Biologic Response Modifiers (BRMs): Newer therapies

TNF-a Inhibitors

• MOA: Inhibit TNF-alpha or its receptor

• Adverse Effects:

  • Increased risk of infections (TB, hepatitis B, sepsis)

  • Increased risk of fungal opportunistic infections

  • Increased risk of pancytopenia

  -Injection site reaction(s)

  -Increased respiratory tract infections

  -GI symptoms

  -worsening of CHF (or new onset CHF)

  -Need to do initial PPD, Hep B & C serologies, CBC, CMP

  -Yearly PPD, Every 3 months CBC, CMP,

TNF-a Inhibitors (Specific Examples)

• Adalimumab (Humira®): Chimeric/human MAB- 80mg SQ x 1st week then 40mg SQ weekly

• Etanercept (Enbrel®): Fully humanized MAB

• Infliximab (Remicade®): Chimeric MAB, 5mg/kg IV at 0,2,6 weeks then q8 weeks

Golimumab (Simponi®): Given SQ monthly

IL-12/23 Inhibitor

• Stelara (ustekinumab): Targets IL-12 & IL-23
• AE; URI, nasopharyngitis, back pain, injection-site erythema, diarrhea, fatigue, headache, myalgia
• Given every 3 months

IL-17 Inhibitors

• Cosentyx (Secukinumab): Inhibits IL-17A

• Taltz (ixekizumab): Inhibits IL-17A

• Bimzekizumab (Bimzelx): Inhibits IL-17A, IL-17F

• Siliq (brodalumab): Inhibits IL-17A receptor

IL-23 Inhibitors

• Guselkumab (Tremfya®): Inhibits IL-23
• Risankizumab (Skyrizi): Inhibits IL-23
• Tildrakizumab (Ilumya): Inhibits IL-23

PDE-4 Inhibitor

• Apremilast (Otezla®)
• Indications; Plaque psoriasis, psoriatic arthritis, Bechet disease

IL-4/13 Inhibitor

• Dupilumab (Dupixent): Monoclonal antibody inhibits IL-4 and IL-13

IL-13 Inhibitor

• Indications: Moderate to severe atopic dermatitis in adults not controlled on topical therapy

TYK2 Inhibitor

• Deucravacitinib (Tofyktu): Inhibits TYK2
• Indications; Plaque psoriasis

Phototherapy

• UVB radiation for psoriasis
• PUVA (psoralen plus UVA) for psoriasis

Acne Treatment

• Topical Treatments (examples): Benzoyl peroxide, Topical antibiotics, Isotretinoin, Topical retinoids, Combination products, Topical androgen receptor inhibitor

• Systemic Treatments (examples): Antibiotics, Isotretinoin

• Oral contraceptives

• Aldosterone Antagonist

Topical Rosacea Agents

• Oxymetazoline (Rhofae): Alpha-1 agonist eliciting vasoconstriction
• Brimonidine (Mirvaso): Alpha-2 agonist decreasing vasculature dilation

Bacterial, Viral, Parasitic Infection Treatments

• Topical Antibiotics (examples): Mupirocin, Retapamulin, Silver Sulfadiazine, Bacitracin, Bacitracin & Polymixin B, Triple Antibiotic Ointment
• Antifungals (examples): Azoles (Clotrimazole, Miconazole, Ketoconazole, Econazole), Terbinafine, Ciclopirox,
• Antivirals (examples): Acyclovir, Penciclovir

Parasitic Infections - Scabies

• Permethrin 5% (Elimite®): Acts as a neurotoxin, depolarizing parasite nerve cells and causing muscle paralysis.
• Ivermectin (Stromectol®): Binds to glutamate-gated Cl ion channels, resulting in paralysis and death of parasites.

Parasitic Infections - Lice

• Permethrin 1% (Nix®): Saturates treatment area and washed off after 10 minutes.

• Malathion (Ovide®): Applied to dry hair, allowed to dry naturally, then washed with soap after 8–12 hours

• Lindane (Kwell®): Applied to dry hair/pubic, then washed off after 4–12 hours

• Ivermectin (Stromectol®): 200mcg/kg PO q week x 3 doses

Additional Information

• References provided at the end