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topical agents
skin is used as a point of entry to the systemic circulation which bypasses the liver and thus avoids first pass metabolism
Layers of the epidermis
(outermost) stratum corneum—can form reservoir that can delay absorption
stratum lucideum
stratum granulosum
stratum spinosum
stratum basale
Layers of the skin:
epidermis
dermis (sweat glands)
hypodermis (adipose layer)
topical antibiotics
only used for minor dermal conditions, treatment of acne, and anti-inflammatory properties
tavaborole and ciclopirox
The only effective topical treatment for onychomycosis
imquimod
a topical immunomodulator that stimulates interferon alpha and stimulate the local production of interleukin production and TNF; T
Tacolimus
Topical calcineurin inhibitor that prevent the release of inflammatory cytokines and inhibit T lymphocyte activation; used for Atopic dermatitis
Tretinoin/adapalene
increase the activity of RNA polymerase and that results in a decreased cohesion between the epidermal cells, increasing cell turnover
benzoyl peroxide
an acne treatment whose mechanism is antimicrobial, but can be irritating and drying to the skin
Brimodine
used for acne rosacea (topical alpha agonists); decreases redness by causing vasoconstriction
topical corticosteroids
MOA is to decrease the concentration, distribution and function of peripherical leukocytes and anti-inflammatory cytokines; decrease the inflammatory response; cause vasoconstriction when applied topically; be concerned about atrophy; absorption increases with inflammation and occlusion after application
salicylic acid
a destructive keratolytic agent used break down the outer layer of skin to treat warts, lower concentrations are used to treat acne;
MOA-not completely understood
Urea
a keratolytic agent that pulls moisture into the stratum corneum and can soften skin (calluses); higher concentrations can be destructive and can be used for hyperkeratosis and nail beds prior to nail removal
podofilox
a keratolytic agent used specifically for warts; after absorption, it prevents the formation of the mitotic spindles preventing cell division
fluorouracil
a destructive topical agent; lower strengths used for actinic keratoses and superficial basal cell carcinoma treatment; inhibits the enzyme Thymidylate synthase, which is responsible for building thymidine used for building DNA, creating a shortage of building blocks for DNA which leads to cell death
Doxepin
a topical antipruritic that blocks the histamine receptors in the skin
Pramoxetine
a topical antipruritic and local anesthetic by blocking the initiation and conduction of nerve impulses from the skin
Topical estrogen patches
designed to release the drug at a specified rate, and can be switched out every 7 days, bypassing liver effects seen with the oral version
Topical testosterone patch
oral is associated with hepatic dysfunction, so the topical avoids this side effect; similar to estrogen patch
Fentanyl patch
an opiod analgesic for pain; high concentration in the patch to create a gradient to absorb through the stratum corneum; 12 hours until pt feel pain relief and reservoir allows med to still be absorbed even after patch removal;
used patches must be monitored as drug is still available even after removal