60: Topical Agents Flashcards
dead keratinocytes
stratum corneum
living layers of epiermis
basal layer
spinous layer and granular layer
cells of ______ layer synthesize most epidermal prtns
spinous
cell renewal and mitotic activity occurs in ______ layer
stratum basale
rate-limiting step for percutaneous absorption
passage through stratum corneum
3 absorption pathways of intact skin?
which is most common route?
- shunt route through appendages
- transcellular route through corneocytes of stratum corneum (hydrophilic drugs)
- through intercellular domains ** most common for small uncharged molecules
water in oil emulsion =
oil in water emulsion =
water-soluble emulsion =
powder in water =
fine solid or liquid particles dispersed in gas =
semisolid with finely powdered material =
alcoholic solutions =
ointments creams gels/foams lotionos/solutions aerosols pastes tinctures
vehicle choice affects the rate and extent of absorption of drug
what should be used in scalp and hairy areas? intertriginous areas?
lotions, gels, solution, foams, and aerosols
creams, lotiions, and solutions
skin is dry and scaly so add …
wet and oozing add…
ointment
tinctures
if it is wet, dry it and if it is dry, wet it
What influences the rate of percutaneous absorption?
- concentration of drug in vehicle
- partition coefficient (ability of drug to leave vehicle and move into outer layers of stratum)
- drug diffusion coefficient (decreasing MW of drug elevates diffusion)
- thickness of stratum corneum
most topicallly effective drugs are at least somewhat…
lipophilic
how do the following things affect PCA?
- inflamed skin
- hydrated skin
- occlusion of medication
- age of patient decreased
- increase PCA
- increase PCA
- increase PCA
- increase PCA (% topical applied to smaller body SA)
Pathogenesis of Acne
microcomedone (hyperkeratotic, sebum secretion increased) –> comedone –> inflammatory papule/pustule –> nodule
MOA erythromycin and clindamycin
inhibit prtn synthesis
antibiotics
antibiotic MOA metronidazole
interacting and disrupting DNA
MOA sodium sulfacetamide
kills p. acnes by inhibiting folic acid biosynthesis
acne MOA azelaic acid
reduce inflammation and reduces keratinization
reduces growth of bacteria such as p. acnes and staph. epidermidis
side effects azelaic acid
skin lightening and skin dryness
MOA benzoyl peroxide
anaerobic antibac by releasing oxygen
antiinflammatory by inhibiting activity of
neutrophils
also keratinolytic
which antibiotic has no resistance with long term use?
benzoyl peroxide
MOA salicylic acid
increases solubilization of stratum corneum by altering keratin by breaking hydrogen bonds
clears comedones by desquamation
MOA tretinoin
decreases adhesiveness of follicular epithelial cells responsible for producing microcomedones
increases mitotic activity in follicular cells which caufses extrusion of comedones
reduces keratinization
benzoyl peroxide and _____ whould not be applied simultaneoulsy
Tretinoin
benzoyl peroxide inactivates tretinoin
MOA adapalene
reduces cellular proliferation and inflammation - comedolytic
oral retinoid used to treat severe acne
Isotretinoin
MOA isotretinoin **
suppresses sebum production by inducing apoptosis in sebum producing cells of the sebaceous glands
adverse effects isotretinoin
teratogenesis
+/- 1 mo contraceptive with treatment
MOA tazarotene
decreases inflammation and epidermal hyperproliferation
adverse effects tazarotene
teratogenic — preggers class X
drugs to treat acne that inhibit sebaceous gland function
antiandrogens
oral contraceptives
isotretinoin
pathogenesis of psoriasis
autoimmune disease
inflamamtion and keratinocyte hyperproliferation
woman given oral Acitretin for severe psoriasis and now wants to get preggers. What do you tell her?
highly teratogenic with prolonged elimination time
women should avoid pregnancy for 3 yr after being administered acitretin
MOA calcipotriene
vit D analog that inhibits proliferation of keratinocytes and reduces inflammation
slight risk hypercalcemia and hypercalciuria
coticosteroids weak - intermediate - high
hydrocortiosne
mometasone furoate
clobetasol propionate
MOA corticosteroids to treat psoriasis
reduce inflammation and inhibit immune function disorders
antiproliferative qualities as well
tachyphylaxis =
diminished therapeutic effect
can occur with corticosteroids when high potency class are applied daily for 2 wks
prevent with alternate day applicaitons
topical and systemic side effects to corticosteroids
topical : atrophy, acne, fungal infection, retarded wound healing, contact dermatitis, glaucoma, cataracts
systemic: hypothalamus pit adrenal axis suppression, cushings syndrome, growth retardation
chronic inflammatory skin disorder associated with intense pruritus and dried flaking skin =
eczema aka atopic dermatitis
treat with corticosteroids
secondary infection a risk (tx with antibiotics)
uses of photochemical therapy
alopecia
cutaneous t cell lymphoma
eczema
psoriasis
MOA methoxsalen and trioxsalen
unknown - they are psoralens administered topically or orally then exposed to UV light