Topical Agents Flashcards
MOA: Clindamycin
antibacterial. Reduce numbers of P acnes. Inhibit protein synthesis
MOA: Erythromycin
antibacterial. Reduce numbers of P acnes. Inhibit protein synthesis
MOA: metronidazole
antibacterial. Disrupting DNA - kills P acnes
MOA: Na sulfacetamilde
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antibacterial. Kills P acnes by inhibiting Folic acid biosynthesis
MOA: azelaic acid
antibacterial. Reduces growth of P acnes/Staph Epidermidis. Free radical scavenging - reduced inflammation. Reduced keratinization
Keratolytic effects. Causes lightening of skin.
MOA: Benzoyl Peroxide
antibacterial. Good in both inflammatory and non inflammatory acnes. Release Oxygen.
No resistance even if used chronically
maybe inhibiting action of neutrophils
Keratolytic, Comedolytic
MOA: betamethasone
corticosteroids. SUper high potency. Reduce inflammation and inhibit immune function disorders
MOA: clobetasol
corticosteroids. Super high potency. Reduce inflammation and inhibit immune function disorders
MOA: diflorasone
corticosteroids. High potency. Reduce inflammation and inhibit immune function disorders
MOA: hydrocortisone
corticosteroid. Low potency. Reduce inflammation and inhibit immune function disorders
MOA:triamcinolone
corticosteroid. Medium Potency. Reduce inflammation and inhibit immune function disorders
MOA: Calcipotriene
Vitamin D analog. Topical
Use: moderate Plaque psoriasis, inhib prolif keratinocytes, reduce inflammation
MOA: tretinoin
Retinoid. Use, acne and photoaging
MOA: dec inflammation, inc mitotic activity leads to extrusion of comedones
MOA: adapalene
Retinoid. More chemically stable than tretinoin
Use: acne
MOA: red cell proliferation/inflam, COMEDOLYTIC, reduced keratinization
MOA: Isotretinoin
Retinoid. Accutane. oral
Use: severe acne
MOA: suppress sebum prod by killing sebum producing cells
Reduced keratinizatino, inflammation
MOA: tazarotene
Retinoid. Topical, hydrolyzed to activate
Use: psoriasis, mild acne, fine wrinkles
MOA: dec inflammation, proliferation, red keratinization
MOA: acetretin
Retinoid. Oral
Use: severe recalcitrant psoriasis
MOA: unknown
MOA: Salicylic acid
Keratolytic agent.
Describe structure of epidermis and how it affects the percutaneous absorption
Stratum Corneum, Stratum Lucidum, Stratum Granulosum, Stratum Spinosum, Stratum Basale
Corneum - dead keratinocytes
Granulosum, Spinosum, Basale - living
Corneum full of corneocytes - flat lipid depleted keratinocytes, membrane is envelope of insoluble proteins, surrounded by lipid slurry
Absorption takes place:
1-through appendages ‘shunt route’ (hair follicles, sweat gland)
2-Transcellular route - through corneocytes
3-Through intracellular lipid domains (small uncharged particles)
describe variables affecting absorption
passage through stratum corneum is rate limiting
variables are
1. concentration of drug in vehicle
2. Partitioning of drug from vehicle into strat corneum
3. Molecular aspects of the drug allowing diffusion across skin layers
4. Thickness of stratum corneum
Fick’s Law
variables of choice of vehicles
Scalp and Hairy areas - Lotions, gels, solution, foam, aerosols LESS GREASY
Intertrigenous areas - creams, lotions, solutions
AVOID RUBBING PROBLEM
If its wet dry it, if its dry wet it
Ointments creams gels most wet
Tinctures, Powders, Pastes most dry
adverse reactions and drug interactions of drugs
Drug Interactions:
Tretinoin: benzoyl peroxide inactivates
Acitretin: alcohol inc elimination time
Adverse Effects:
Tretinoin: pruritis, erythema, xerosis, sun, preg C
Adapalene: Preg C, Pruritis, erythema, xerosis
Isotretinoin: teratogenic
Tazarotene: teratogenic, Preg X, photosensitivity
Acitretin: teratogenic. avoid preg 3 yrs
Corticosteroids: atrophy, acne, infection, bad healing, contact dermatitis, glaucoma, HPA axis suppress, cushings, growth retardation
considerations when using topical corticosteroids
initiate lowest potency to control disease
large surfaces with low potency
low potency on face/intertrigous areas. Potent on palms and feet soles
avoid high potency drugs n infants/kids
tachyphylaxis can occur if high potency
if happens do alternate days to reduce.
Area of body where drug should be used: Hydrocortisone
Large areas of body, eyelid, scrotum, intertrigous areas, mucous membranes, face, chest/back
Area of body where drug should be used: triamcinolone
Large areas, face, intertrigous areas, chest/back, arms/legs
Area of body where drug should be used: diflorasone
Palms and soles. Dorsa of hands/feet
Area of body where drug should be used: clobetasol
Palms and soles, Nails
Area of body where drug should be used: betamethasone
Palms and soles, Nails