Topical Therapeutics Flashcards
Medications gain access to sites of action through three primary mechanisms? (3)
- passive diffusion - through the stratum corneum
- transportation through channels or pores within a lacunar system in the stratum corneum
- transportation via appendageal structures - such as sweat glands / follicles
Drug factors affecting percutaneous absorption? (4)
active drug concentration
composition of vehicle
molecular size of drug/prodrug
lipophilicity of drug
Patient factors affect percutaneous absorption (4)
presence of barrier disruption
anatomic location
skin hydration
occlusion
How drug concentration influences absorption
absorption is directly proportional to the concentration of the active ingredient in the medication
How molecular size influences drug absorption
diffusion of a compound is inversely proportional to the molecular size of the drug
lipophilicity of the drug and absorption
lipophilic topical agents are more likely to permeate the skin than hydrophilic
How can vehicle influence drug absorption?
given same active concentration - different vehicles can yield different absorptions
How does occlusion influence absorption?
Occlusion of the skin often leads to markedly increased skin hydration - therefore, active ingredients that are delivered in the form of ointment / tape / or to the skin folds reach a much higher concentration because occlusion prevents loss of medication by evaporation / friction / or exfoliation
how does anatomic location influence percutaneous absorption?
thicker stratum corneum –> lower absorption
Composition
ointment
water in oil emulsion
composition
cream
oil in water emulsion
composition
gel
semisolid emulsion in alcohol base
composition
lotion / solution
powder in water (some oil in water)
composition
foam?
pressurized collection of gaseous bubbles in matrix of liquid film
potency of active ingredient in ointment?
strong
ointment
- hydration?
- sensitization?
- irritation?
high hydration
low sensitization
low irritation
ointment
body sites?
non intertreginous
avoid use on face / hands / groin
creams potency? hydration? sensitization? irritation?
moderate potency
some hydration but not as much as oinment
significant sensitization
low irritation
creams
body sites?
all body sites
creams
avoid use with?
maceration = the softening and breaking down of skin resulting from prolonged exposure to moisture
gels potency? hydration? sensitization? irriatation?
potency - strong
hydration - drying
sensitization risk - high
irritation risk - high
gels
sites for use?
oral mucosa
scalp
gels
avoid?
fissures
erosions
macerated regions
lotions // solutions potency? hydration? sensitization? irritation?
potency - low
hydration - variably drying
sensitization - significant
irritation - moderate
lotions / solution
sites amenable?
scalp / intertriginous
lotions / solutions
avoid ?
fissures / erosions
foams
potency
strong potency
foams
MOA
Foam matrix is stable at room temp, but readily melts at body temp — after the foam is applied to the skin, the volatile components (such as alcohol and water) quickly evaporate, leaving behind lipid and polar components containing supersaturated active ingredients to interact with the stratum corneum - these supersaturated solutions enable maximal delivery of active ingredients into the skin
foam
what might alcohol do to influence absorption?
may play a role in altering the stratum corneum - lead to improve penetration of active ingredient
foam -
sites amenable
hair bearing areas
foam
aovid
fissures
erosions
when selecting vehicle
3 factors
anatomic location
contact allergy / sensitization
irritancy
for hair bearing regions, the clinician should consider choosing which vehicle
solution or foam
over
ointment
_____________ vehicles contain preservatives that may increase the risk of contact allergy and sensitization - these preservatives include known allergens such as parabens and formalin releasers
water-based
creams
lotions
solutions
irritancy is most notably associated with high concentration of _____________, other types of _____________ and certain __________ vehicle ingredients.
propylene alcohol
alcohol
acidic
avoid using formulations containing ________ or __________ on extensively fissured, eroded, or macerated areas
alcohol
salicylates