Topical Agents Flashcards
clindamycin
erythromycin
Antimicrobial agent
MOA: bind ribosomes–>protein synthesis inhibition
Use: acne
metronidazole
Antimicrobial agent
MOA: interacting and disrupting bacterial DNA
Use: acne
sodium sulfacetamide
Antimicrobial agent
MOA: inhibit dihydropteroate synthetase activity–> inhibit folic acid biosynthesis
Use: acne
azelaic acid
Antimicrobial agent
MOA: reduce growth of P. acnes and S. epidermidis, reduce inflammation, reduce keratinization, keratolytic effects–>desquamation
Use: acne
Adverse effects: lightening of skin, skin dryness
benzoyl peroxide
Antimicrobial agent, derivative of coal tar
NO resistance
MOA: release oxygen–>anaerobic antibacterial; inhibit activity of neutrophils–>antiinflammatory; keratolytic–> desquamation; comedolytic
Use: inflammatory and noninflammatory acne
Adverse effects: dry skin
tetracyclines
other broad spectrum antibiotics
- oral administration for moderate to severe acne
- antimicrobial and anti inflammatory
salicyclic acid
Topical keratolytic agent
MOA: break hydrogen bonds–>alter keratin–> increase solubilization of stratum corneum; desquamation–> clears comedones
Use: acne, psoriasis, actinic keratoses, ichthyosis
Adverse effects: salicylism and death due to systemic conc. (especially in children)
Symptoms of salicyclism: GI disturbance, lethargy, ringing in ears, dizziness, high body temp, fast RR, coma, seizures, hypoglycemia, pulmonary edema, CNS failure, cardiovascular collapse
tretinoin
Topical retinoid
MOA: bind retinoic acid receptors causing the following; decrease cohesiveness of follicular epithelial cells; increase mitotic activity in follicular cells–>extrusion of comedones; reduce keratinization
Uses: acne, photoaging
Adverse effects: pruritus, erythema, xerosis, sun sensitivity, teratogenic
Interaction: benzoyl peroxide inactivates–> do NOT apply simultaneously
adapalene
Topical retinoid
More lipophilic than tretinoin–> stays in sebum
MOA: bind retinoic acid receptors causing the following; reduce cellular proliferation, antiinflammatory, comedolytic
Uses: acne
Adverse effects: pruritus, erythema, xerosis, sun sensitivity, teratogenic
tazarotene
Topical retinoid
Prodrug
MOA: bind retinoic acid receptors causing the following; decrease inflammation and epidermal hyperproliferation
Uses: psoriasis, mild-moderate acne, decrease fine wrinkles by increasing granular cell layers
Adverse effects: sun sensitivity, teratogenic (must be on birth control)
isotretinoin
Oral retinoid (Accutane)
MOA: bind retinoic acid receptors causing the following; induce apoptosis of sebum producing cells–> suppress sebum production
Uses: severe acne
Adverse effects: significant teratogenesis (birth control 1 month prior and 1 or more menstrual cycles post treatment)
acitretin
Oral retinoid
MOA: bind and activate retinoic acid receptors
Uses: severe, recalcitrant psoriasis
Adverse effects: highly teratogenesis (birth control 3 yrs after admin)
Interaction: alcohol increases 1/2 life (>3 months)
calipotriene
Topical vitamin D analog
MOA: bind vitamin D receptor–>associate with retinoic acid X receptor–> complex associates with vitamin D response elements in DNA–> increase transcription of genes–> increase epidermal differentiation and inhibit inflammation
Use: psoriasis
Adverse effects: hypercalcemia, hypercalciuria
hydrocortisone
mometasone furcate
clobetasol propinate
Topical corticosteroids
MOA: reduce inflammation, inhibit immune function disorders, antiproliferative
Use: sporiasis, atopic dermatitis (eczema), and other skin diseases
Adverse effects: atrophy, acne, enhanced fungal infection, retarded wound healing, contact dermatitis, glaucoma, cataracts, HPA axis suppression, Cushing syndrome, growth retardation
methoxsalen
trioxsalen
Psoralen plus ultraviolet A (PUVA) phototherapy
Topical or oral
MOA: actiaved by UVA light–> intercalate DNA–>induce antiproliferative, immunosuppressive, and antiinflammatory effects
Uses: alopecia, cutaneous T-cell lymphoma, eczema, psoriasis
Adverse effects: nausea, blistering, painful erythema, photoaging, actinic keratoses, nonmelanoma skin cancer
