2) Topicals and Dermatologicals Flashcards
General principles
- Thicker plantar skin needs higher dose/concentration
- Occlusion needs lower dose and concentration (saran wrap increased percutaneous penetration by 10 X)
Percutaneous absorption is determined by many factors
- Vehicle
- Integrity of epidermis
- Use of occlusion/plastic film
Ointments and gels provide increased
- Potency
Lotions and creams are preferred on
- Hairy areas
With higher doses and concentration, must watch for
- Systemic effects
Cortisone vs hydrocortisone
- Cortisone = no topical activity
- Hydrocortisone = the prototype of all topical corticosteroids
Actions of topical corticosteroids
- Anti-inflammatory
- Anti-pruritic
- Vasoconstriction
Topical corticosteroid mechanism of action
- Diffuses across cell membranes, binds to cell receptors
- Induces phospholipase A2 inhibitory proteins, inhibiting arachidonic acid pathway
- Result in decreased formation of endogenous mediators of inflammation
Endogenous mediators of inflammation
- Prostaglandins
- Leukotrienes
- Histamine
- Kinins
- Lysozomal enzymes
Topical corticosteroids anti-mitotic effect
- Anti-mitotic on epithelial cells
- Good for psoriasis
Topical corticosteroids indications
- Treatment of the inflammatory and pruritic manifestations of corticosteroid responsive dermatoses
Goal of topical corticosteroids
- Inhibition of the inflammatory or exudative phase of wound healing
Eczema
- Generic name for a group of inflammatory skin diseases characterized by a erythematous, weeping, vesicular, and scaley appearance
Topical corticosteroids contraindications
- Hypersensitivity to corticosteroids, or other components.
- Cutaneous viral infections
- HPA axis suppression occurs anywhere from 2-14 grams/day
- Warning: cutaneous atrophy
Topical corticosteroids dose
- Higher doses and concentration: watch for systemic effects (ie. H-P-A axis suppression: weakness, nausea, loss of appetite, fever.
- Response to treatment: decrease the dose
Highest potency topical corticosteroid (I)
- Betamethason dipropionate augmented: 0.05% cr., gel, lot, oint qd-bid (Diprolene)
- Clobetasol 0.05% crm, foam, gel, lot, shmp, sol (Temovate, Cormax, Clobex)
- Fluconide 0.05% crm, gel, oint, sol; 0.1% crm (Lidex)
- Halobetasol 0.05% crm, oint (Ultravate $82.63) generic $30.99
High potency topical corticosteroid (II) example
- Triamcinolone 0.025, 0.1, 0.5% crm, oint, lot; bid-qid (Kenalog)
- Desoximetasone 0.05, 0.25% crm, gel, oint (Topicort)
- Mometasone 0.1% crm, lot, oint, q d dosing (Elocon)
High-medium potency topical corticosteroid (III) example
- Triamcinolone 0.5% crm
Medium potency topical corticosteroid (IV) example
- Triamcinolone 0.1% oint
Medium-low potency topical corticosteroid (V) example
- Triamcinolone 0.1% crm, lot, 0.025% oint
Low potency topical corticosteroid (VI) example
- Triamcinolone 0.025% crm, lot
Lowest potency topical corticosteroid (VII) example
- Hydrocortisone 1% (often OTC)
- Cortaid, Cortisone 10
- Rx 2.5% crm
- Apply bid-qid
Highest potency corticosteroid dosing
- 45-50 gm/week
- 2 weeks max
Topical corticosteroid potency from lowest to highest
- Hydrocortisone 1%(OTC) ; 2.5% (Rx) (Hytone)
- Triamcinolone acetonide 0.1% (Kenalog, Artistocort)
- Fluocinoline acetonide 0.025% (Synalar)
- Mometasone furoate 0.1% (Elocon)
- Betamethasone valerate 0.1% (Valisone)
- Betametasone dipropionate (Diprosone) 0.05%
- Fluocinonide 0.05% (Lidex)
- Flumethasone pivalate 0.03% (Locorten)
Topical anti-inflammatory immunomodulators (non-corticosteroids)
- Pimecrolimus (Elidel - Novartis) Rx 1% cream (10 mg/g. of cr.); 15, 30, 100 g tubes.
- Tacrolimus (Protopic- Fujisawa) Rx 0.03%; 0.1% ointment 30, 60 g. tubes
Topical anti-inflammatory immunomodulators (non-corticosteroids)
- Topical calcineurin inhibitors - Microbial-derived macrolides - Mechanism similar to cyclosporine (Sandimmune, and others)
- Non-steroidal (non-cortisone) anti-inflammatory
- Macrolide immunosuppressant produced by streptomyces species
Atopic dermatitis (type of eczema)
- Inflammatory, chronically relapsing, non-contagious and pruritic skin disorder
- Skin reacts abnormally and easily to irritants, food, and environmental allergens
- Becomes red, flaky and very itchy
Other names for atopic dermatitis
- Neurodermatitis
- Endogenous eczema
- Flexural eczema
- Infantile eczema
Immunomodulators MOA
- Inhibits T lymphocyte activation by binding to the intracellular protein macrophilin-12
- Complex inhibits calcium-dependent phosphatase
- Blocks dephosphorylation of nuclear factor (NF-AT) of activated T-cells
- Inhibits the formation of lymphokines
- Interleukins (IL-2,3,4,5, GM-CSF, and TNF-α) and gamma interferon
- Inhibits release of inflammatory cytokines from mast cells after stimulation by antigen/IgE
Pimecrolimus (Elidel) and tacrolimus (Protopic) topical immunomodulators indications
- Short term and intermittent long term Tx of mild to mod atopic dermatitis
Pimecrolimus (Elidel) and tacrolimus (Protopic) topical immunomodulators contraindications
- Preg cat c
- No use in children or immunocompromised
- Hypersensitivity
- Rx may predispose to severe skin viral infections (HSV 1 or 2; verruca; VZV) or skin malignancies
Pimecrolimus (Elidel) and tacrolimus (Protopic) topical immunomodulators other uses
- Lichen Planus (shin, nails)
- Vitiligo
crisaborole topical (Eucrisa) Rx 2% topical oint indications
- Mild to moderate atopic dermatitis
crisaborole topical (Eucrisa) Rx 2% topical oint actions
- Phosphodiesterase (PDE)-4 inhibitor
- Results in increased intracellular cyclic adenosine monophosphate (cAMP) levels
- cAMP is thought to decrease the proinflammatory response (eg, cytokine release) associated with atopic dermatitis
crisaborole topical (Eucrisa) Rx 2% topical oint sig
- Apply a thin layer topically to affected area(s) BID
doxepin (Zonalon) Rx 5% cream
- Local anesthetic effects
- Itch relief
- Potent H1 and H2 receptor blocking activity
Percutaneous absorption of doxepin (Zonalon) Rx 5% cream
- May produce systemic side effects: somnolence, sedation, drowsiness
doexpin (Zonalon) indications
- short term Tx of pruritis from eczematous dermatitis: atopic, lichen chronicus simplex
doxepin (Zonalon) contraindications
- Break in the epidermis
- Narrow angle glaucoma
- Urinary retention (doxepin has anti-cholinergic effect)
doexpin (Zonalon) sig
- Apply thin layer qid
- Not longer than 8 days
Topical antihistamine indications
- Pruritis due to minor skin disorder
diphenhydramine (Benedryl) OTC forms (topical)
- 1% and 2% in cream, lotion, spray
Caladryl
- 1% diphenhydraqmine, 8% calamine; camphor
Benedryl Itch Relief
- 2% diphenhydramine, 0.1% zinc acetate, 73% alcohol, aloe vera
diphenhydramine (Benadryl) MOA
- Competes with histamine for H1-receptor sites on effector cells in GI tract, blood vessels, and respiratory tract
- Anticholinergic and sedative effects
- May be used alone or in combination with centrally acting anticholinergic agents
diphenhydramine (Benadryl) indications
- for IM, IV, PO symptomatic relief of allergic symptoms caused by histamine release, including nasal allergies and allergic dermatosis
- Insomnia, occasiona
- Prevention or treatment of motion sickness
- Antitussive
- Management of Parkinsonian syndrome including drug-induced extrapyramidal symptoms (dystonic reactions)
diphenhydramine (Benadryl) adjunct indications
- Adjunct to epinephrine in the treatment of anaphylaxis
Psoriasis
- Chronic papulosquamous disease
- Characterized by reddened plaques covered by thick dry silvery scales that are the result of excessive development of epithelial cells
- Autoimmune skin disease in which activation of T lymphocytes results in the release of cytokines and the proliferation of keratinocytes.
Psoriasis signs/presentation
- Red scaley papules
- Plaques
- White, silvery scales
- Auspitz Sign
- Koebner’s Phenomenon
- Scalp, palms, and soles
Anti-psoriatics
- Vitamin D analogues, tazarotene, corticosteroids alone, or w/ vitamin D analogue or tazarotene;
- Pimecrolimus
- Topical anti-inflammatory (steroids)
- PUVA (phototherapy combination of Psoralen and UVA)
- UVB and coal tar preparations
- Salicylic acid
Psoriasis Tx
- Slowing the growth of skin
- Controlling the immune response that causes psoriasis
- Both
calcipotriene (Devonex) 0.005% cr, foam, oint, solution
- Anti-psoriatic 1st line Tx
- 7-dehydrocholesterol-UV-cholecalciferol
calcipotriene (Devonex) action
- Synthetic vitamin D3 analog
- Bind to cell receptors in the skin (kertinocytes) and regulates cell production
calcipotriene (Devonex) indications
- Psoriasis
calcipotriene (Devonex) contraindications
- Pts with hypercalcemia or evidence of vitamin D toxicity
- Use on the face (cream, ointment)
- Pts with acute psoriatic eruptions (scalp solution)
- Preg cat C
calcipotriene (Devonex) preparations
- Devonex ointment 0.005%
tazarotene (Tazaroac; Avage)
- Anti-acne, keratolytic agent; 0.05% and 0.1% cr.; foam
tazarotene (Tazaroac; Avage) actions
- Synthetic retinoid
- Modulates differentiation and proliferation of epithelial tissue
- Some degree of anti-inflammatory and immunological activity
- Decreases cohesiveness of follicular epithelial cells
tazarotene (Tazaroac; Avage) mitotic activity
- Stimulates mitotic activity and increased turnover of follicular epithelial cells causing extrusion of the comedones