Pharmacokogical Principles in Dermatology Flashcards
Steps of drug delivery to the skin:
Absorption, distribution, metabolism, and elimination
____ drug delivery is applied right to the target area. No need to worry about bioavailability or first pass. There is less systemic ____ of the drug
Topical
Circulation
____ dosing has more systemic circulation and delivery to more tissues beyond the skin. Need to consider first pass effect, plasma protein binding
Oral
Layers of the skin:
Topical drugs need to make it to the ___ to have full effect
Dermis
Skin ___ varies by location which results in differences in drug absorption. Drugs are more readily absorbed in ___ layers of skin.
Structure
Thin
Stratum corneum: lipids and dead cells
_____ delivery is when the drug moves around the cells. ____ delivery is when the drug moves through the cells. Both are considered ___ delivery.
Intercellular
Transcellular
Transepidermal
____ is when drugs gain access to the dermis through a gland. ___ is when drugs gain access to the dermis through the hair follicle. Both are considered ____ delivery.
Transglandular
Transfollicular
Transappendageal
Other factors that affect topical drug absorption are ___ skin and ____ skin.
Aged
Damaged
Many factors effect the skin integrity and effect topical drug absorption:
Other factors affecting topical drug delivery to the skin:
Concentration of the topical drug is highest at the ___ ___. Burning to proteins will decrease concentration as it moves to the ___, where there are blood vessels.
Stratum corneum
Dermis
____ skin absorbs drugs better especially for polar drugs
Hydrated
Formulations and vehicles of topical drug delivery:
Moisturizers are sorted into 3 categories:
____ tend to dry the skin, have patients avoid use of this to optimize absorption.
Soaps
The main cellular pathways and systems that commonly targeted in skin pharmacology:
Inflammation, infection, cell devision
_____ play a major role in the treatment of many dermatologic conditions especially inflammation and itchy conditions.
Corticosteroids
____ are effective for conditions involving hyper-proliferation as well as immune and inflammatory dysfunctions
Corticosteroids
Mechanism of actions for corticosteroids: activate the ____ receptor (GR) which acts as a transcription factor that upregulates ____ genes and down regulates ____ genes. Allows thousands of genes to be targets.
Glucocorticoid
Anti-inflammatory
Pro-inflammatory
The immediate effects of corticosteroids involves there ability to effect ___ cells without requiring gene transcription
Immune
Examples of topical corticosteroids
Potency of corticosteroids is based on their ability to ____.
Vasoconstrict
Side effects of corticosteroids:
Skin atrophy, striae (stretch marks), acne, suppression of hypothalamus pituitary adrenal (HPA) axis.
Hypothalamus pituitary adrenal (HPA) axis is how regular ___ is regulated in the body. When someone uses corticosteroids medication, it shuts down this pathway because the drug is acting like ___. Not a problem for short term use.
Cortisol
Cortisol
____ ___ ____ can develop from long term use of highly potent corticosteroids. Presents as a rash at the target site. Caused by disregulation of HPA axis
Topical steroid withdrawal (TSW)
Non steroidal anti-inflammatory topical calcineurin inhibitors (TCI):
Table comparing tacrolimus versus hydrocortisone:
Tacrolimus and Pimecrolimus bind ____ and inhibits the ability of ___ to dephosphorylate the NFAT transcription factor which inhibits ____.
FKBP
Calcineurin
Inflammation
____ is approved to treat mild to moderate eczema in patients two years and older
Primecrolimus