Pharmacology Flashcards
When is topical administration usually used?
Superficial skin disorders Skin infections Itching Dry skin Warts
What are the vehicles for topical administration?
Lotions Creams Ointments Gels Pastes Powders
What is Fick’s law of diffusion?
Rate = permeability x concentration of drug in the vehicle
What does permeability of a drug take into account?
Partition co-efficient
Diffusion co-efficient
Length of the diffusion pathway
What is the partition co-efficient?
The movement of the drug from vehicle into the stratum corneum
What type of drug and vehicle are needed to reach systemic capillaries?
Lipophillic (easily moves through the skin)
Lipophilic or hydrophilic vehicle
What type of drug and vehicle are needed for superficial skin conditions and why?
Hydrophilic drug in lipophilic base Only partitions (moves through skin) weakly
What type of drug and vehicle would not penetrate the skin?
Hydrophilic drug and base
What are excipients and why are they used in vehicles?
Substances that can enhance hydrophobic drug solubility to enhance absorption
What is the advantage to transdermal patches?
Excess non-dissolved drug can be included to increase duration of effectiveness and provide a constant rate of delivery
What can the partition co-efficient be improved by?
Hydration of the skin by occlusion by ointment or cling film
Inclusion of excipients
What aspects of the nature of skin influence the absorption of topical drugs?
Thickness of the site of application
Hydration of the skin
Integrity of the epidermis
What skin conditions are topical steroids used treat?
Atopic eczema
Psoriasis
Pruritis
How do topical steroids work?
Anti-inflammatory
Immunosupressant
Vasoconstricting
Anti-proliferating for keratinocytes and fibroblasts
What are the categories of topical steroid?
Mild
Moderate
Potent
Very potent
In what vehicles are topical steroids available?
Lotion
Cream
Ointment
What are the side effects of high potency steroids?
Steroid rebound
Skin atrophy
Systemic effects
Spread of infection due to immune suppression
Steroid rosacea
Stretch marks and small superficial dilated blood vessels (telangectasia)
What is the mechanism of action of topical steroids?
Signal via nuclear receptors
Lipophilic molecules, enter by diffusion
How does subcutaneous administration work?
Drug inserted into the fatty (adipose) tissue just beneath the surface of the skin
Drug reaches the systemic circulation by diffusion into either capillaries or lymphatic vessels
What are the advantages of subcutaneous administration?
Absorption is slow
Preferred for many protein drugs and oil-based drugs
Can be used to introduce depot of drug that is slowly released into circulation
Simple and relatively painless
What is the disadvantage of subcutaneous administration?
Injection volume limited
What is transdermal drug delivery?
Drug is incorporated into an adhesive patch applied to the epidermis
Drug absorption partially controlled by a drug release membrane
Absorption occurs by diffusion across cutaneous barrier
What are the drugs that are most suitable for transdermal drug delivery?
Low molecular weight
Moderately lipophilic
Potent
Short half-life
What are the advantages of transdermal delivery?
Steady rate of drug delivery Decreased dosing frequency Avoidance of first-pass metabolism Rapid termination if half-life too short User-friendly, convenient and painless