Pharmacology (General) Flashcards
(41 cards)
The stratum corneum
The Bricks are …
The Mortar is….
flatted dead cells (corneocytes)
multiple bilayer of lipids in plate like structure
water and lipids dont mix t/f
t
lipid r hydrophobic
Two routes of crossing stratum corneum?
transcellular
intercullalr
wHAT INFLUENCES DIFFUSION
HOW PERMEABLE
CONCENTRATION
HOW MUCH HAS TO CROSS
VEHICLE DOES NOT INFLUENCE RATE AND EXTEN OF ABSORP t/f
what factors affect?
f (permiability,concentration, solb)
vehicle dictates permeability and conc (with regards to crossing stratumn corneum)
Drug solubility in vehicle important and is dictated by vehicle
Lipophilic drug in hydrophilic base will diffuse across the stratum corneum …. and diffuse into blood stream …..
lots, lots
like attracts like, hydropgilic base will stay on stratum corneum and repel the lipophilic drug into the mortar of the skin
Lipophilic drug in lipophilic base will diffuse across the stratum corneum …. and diffuse into blood stream …..
moderately, moderately
hydrophillic drug in hydrophilic base will diffuse across the stratum corneum …. and diffuse into blood stream …..
not at all, not at all
hydrophilic drug in Lipophilic base will diffuse across the stratum corneum …. and diffuse into blood stream …..
a tiny bit, a tiny bit
When drugs are applied topically only the soluble fraction provides the driving force for absorption
t/f
t
Physical and chemical factors that can influence how readily the drug disassociates from the vehicle?
Hydratig the skin (prevents water loss)
Choose the right vehicle (ointments over some creams)
Site of application
Integrity of skin (trauma, inflammation)
Decreased partitioning results from a reduction in the barrier function of the stratum corneum
t/f
F
increase partitioning
Describe molecular mechanism of glucocorticosteroids
1) Glucocorticosteroids diffuse across lipophilic cell membrane
2) Bind to receptor GR2a and activates it
Heats shock proteins disassociate from GR2a receptor
GR”a and glucocorticosteroid translocate to nucleus and form homodimers
3) Bind to glucocorticoid receptor elements on promoter region of DNA
Results in transcription of certain genes switched. Less mediator proteins, less synthesis rate.
Subcutaneous route of administration?
Drug delivered by a needle into adipose tissue just beneath epidermis
Advantages of subcutaneous route?
Slow absorption due to less circulation in adipose tissue
Can be used to introduce a depot of drug under the skin that is slowly released into circulation
Subcut administration is used for many …. drugs, such as insulin and many …. based drugs such as steroids
protein, oil based
Skin is a good route because?
Avoids first pass metabolism
Avoids potential toxicity of drugs to organs such as liver
Simple and non sterile (topical application)
Allows for steady state plasma conc to be achieved (slow release)
Skin bad route because?
Only limited drugs diffuse across epidermis
How does TDD work?
Drug accumulated in adhesive patch and diffuse across cutaneous barrier
TDD can only be used topically t/f
F can be used to treat systemic disease
TDD is most suitable for drugs that are.. (4)
1 low molecular weight
2 moderately lipophilic
3 potent
4 brief half life
Chemical enhancers of TD interact with ….. to increase permeability mainly to drugs that can already ……
lipid matrix, cross skin reasonably well
Chemical enhancers of TDD do not have an issue with irritation/toxicity t/f
F they do
Chemical enhancers of TDD are highly effective for highly water soluble drugs or macromolecules
F
they are NOt HIGHLY effective for highly waater soluble drugs, mostl work for drugs that lipophilic