Pharmacology Flashcards
what is a major advantage of topical drug administration
high drug concentration at intended area with low systemic effects
describe the brick and mortar model of the skin
corneocytes surrounded by intercellular lipids (cholesterol, ceramides, free fatty acids)
what is the most important barrier against drug absorption in the skin
stratum corneum (corneocytes and lipids)
what are corneocytes
hardened dead keratinocytes
are the intercellular lipids hydrophobic or phillic, what does this mean
hydrophobic, can serve as a reservoir for hydrophobic, lipid soluble drugs drugs
are most drugs permeable to the skin hydrophobic or phillic
phobic
what are the dissadvantages of topical treatments
time consuming, difficult to get correct dosage, messy
what are the bases and vehicles and what are the purposes
to give different concentrations and theraputic uses
gels creams ointments pastes lotions foams
what is a cream and what does it contain
semisolid emulsion of oil in water, contains emulsifier and persevatives. high water content
what are the benefits of creams
cool and moisturising, non greasy, easy to apply, cosmetically acceptable
what are the disadvantages of cream
may smell unpleasant, allergies to preservants
what are ointments and what do they contain
semisolid grease/oil (soft parafin), no preservative
what is pruritus
itch
what influences the choice of vehicle for a drug
physiochemical properties of the drug, clinical condition of the skin, patients preference (not oil on hair etc)
what can the vehicle affect
rate and extent of absorption
how can you maximise the partitioning (movement) of a drug into the skin
disolve it in a base that promotes absorption
a lipophilic drug in a lipophilic base is soluble in both the vehicle and the skin and partitions between the two
a lipophilic drug in a hydrophilic base is more soluble in the skin and partitions readily and preferentially into it
a hydrophilic drug in a lipophilic base has limited solubility in both the vehicle and the skin and partitions into it to a limited extent
a hydrophilic drug in a hydrophilic base is soluble in the vehicle but not the skin and remains on the surface of it
what type of process is transdermal drug delievery usually
passive driven by diffusion
what law describes the rate of absorption
ficks law
J (flux) (rate of absoprtion) = Kp (permability coefficient) x Cv (conc of drug in vehicle)
what provides the driving force of absorption in topical drugs
only fraction of drug that is dissolved in the vehicle
what happens to undissolved drug in the vehicle- why is this important
dissolves when conc of dissolved drug goes down- helps maintain steady rate of delivery and increases lifetime of the drug
inclusion of what in the vehicle can enhance solubility and absorption
excipients
what physical and chemical factors can improve partitioning
hydrating the skin by occulsion (prevents water loss)
inclusion of excipients which increase the solubility of hydrophobic drugs
increased partitioning results from what happening in the skin
reduction of statum corneum barrier function
what vehicle should be used if skin is dry
lotion
what vehicle should be used if skin is weeping/moist
powder
what are three conditions treated by glucocorticoidsteroids
atopic eczema, psoriasis, pruritus
what are the clinical effects of glucocorticoid steroids
anti-inflammatory, immunosupressant, vasoconstricting, anti proliferating action upon keratinocytes and fibroblasts
what affects glucocorticosteroid penetration, potency and clinical effect
body site, state of skin, occulsion, vehicle, concentration of drug, form of drug
what are the serious side effects of potent long term steroids
steroid rebound, skin atrophy, systemic effects (HPA axis depression, adrenal suppresion, cushings syndrome), spread of infection (immunosuppressed), stretch marks and pupura, tachyphylaxis
if topical- steroid rosacea, fixed telangectasia, perioral dermatitis (inflammatory skin conditions)
if near eye; glaucoma, cataract
describe glucocorticoid molecules and their receptors
lipophillic molecules that diffuse across plasma membrane to bind the nuclear receptors (esp. GRalpa) which then bind to glucocorticoid response elements
what is the subcutaneous route of administration
injected into fatty adipose tissue
how do drugs administered subcutaneously reach the systemic circulation
diffuse into capillaries or lymphatic vessels
what are the advantages of subcutaneous administration
absorbed slowly due to poor vascularisation, suitable for oil and protein based drugs, can create a ‘depot’ of drug that is slowly absorped, simple and relatively painless
what is the disadvantage of subcutaneous
injection volume limited
how is transdermal drug delivery usually done
drug is incorportated into an adhesive patch and applied to the epidermis
what drugs are most suitable for transdermal
low molecular weight, moderately lipophillic, potent, relatively brief half life