Pharmacology Flashcards

1
Q

what is a major advantage of topical drug administration

A

high drug concentration at intended area with low systemic effects

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2
Q

describe the brick and mortar model of the skin

A

corneocytes surrounded by intercellular lipids (cholesterol, ceramides, free fatty acids)

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3
Q

what is the most important barrier against drug absorption in the skin

A

stratum corneum (corneocytes and lipids)

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4
Q

what are corneocytes

A

hardened dead keratinocytes

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5
Q

are the intercellular lipids hydrophobic or phillic, what does this mean

A

hydrophobic, can serve as a reservoir for hydrophobic, lipid soluble drugs drugs

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6
Q

are most drugs permeable to the skin hydrophobic or phillic

A

phobic

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7
Q

what are the dissadvantages of topical treatments

A

time consuming, difficult to get correct dosage, messy

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8
Q

what are the bases and vehicles and what are the purposes

A

to give different concentrations and theraputic uses

gels 
creams 
ointments
pastes 
lotions 
foams
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9
Q

what is a cream and what does it contain

A

semisolid emulsion of oil in water, contains emulsifier and persevatives. high water content

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10
Q

what are the benefits of creams

A

cool and moisturising, non greasy, easy to apply, cosmetically acceptable

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11
Q

what are the disadvantages of cream

A

may smell unpleasant, allergies to preservants

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12
Q

what are ointments and what do they contain

A

semisolid grease/oil (soft parafin), no preservative

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13
Q

what is pruritus

A

itch

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14
Q

what influences the choice of vehicle for a drug

A

physiochemical properties of the drug, clinical condition of the skin, patients preference (not oil on hair etc)

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15
Q

what can the vehicle affect

A

rate and extent of absorption

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16
Q

how can you maximise the partitioning (movement) of a drug into the skin

A

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

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17
Q

what type of process is transdermal drug delievery usually

A

passive driven by diffusion

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18
Q

what law describes the rate of absorption

A

ficks law

J (flux) (rate of absoprtion) = Kp (permability coefficient) x Cv (conc of drug in vehicle)

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19
Q

what provides the driving force of absorption in topical drugs

A

only fraction of drug that is dissolved in the vehicle

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20
Q

what happens to undissolved drug in the vehicle- why is this important

A

dissolves when conc of dissolved drug goes down- helps maintain steady rate of delivery and increases lifetime of the drug

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21
Q

inclusion of what in the vehicle can enhance solubility and absorption

A

excipients

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22
Q

what physical and chemical factors can improve partitioning

A

hydrating the skin by occulsion (prevents water loss)

inclusion of excipients which increase the solubility of hydrophobic drugs

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23
Q

increased partitioning results from what happening in the skin

A

reduction of statum corneum barrier function

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24
Q

what vehicle should be used if skin is dry

A

lotion

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25
what vehicle should be used if skin is weeping/moist
powder
26
what are three conditions treated by glucocorticoidsteroids
atopic eczema, psoriasis, pruritus
27
what are the clinical effects of glucocorticoid steroids
anti-inflammatory, immunosupressant, vasoconstricting, anti proliferating action upon keratinocytes and fibroblasts
28
what affects glucocorticosteroid penetration, potency and clinical effect
body site, state of skin, occulsion, vehicle, concentration of drug, form of drug
29
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
30
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
31
what is the subcutaneous route of administration
injected into fatty adipose tissue
32
how do drugs administered subcutaneously reach the systemic circulation
diffuse into capillaries or lymphatic vessels
33
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
34
what is the disadvantage of subcutaneous
injection volume limited
35
how is transdermal drug delivery usually done
drug is incorportated into an adhesive patch and applied to the epidermis
36
what drugs are most suitable for transdermal
low molecular weight, moderately lipophillic, potent, relatively brief half life
37
name three agents that enhance trnsdermal drug delivery
water, solvents (ethanol), surfactants
38
how can you physically enhance transdermal drug delivery
iontophoresis- prolonged application of low voltage electrical pulses to the skin electroporation- brief high voltage pulses sonophoresis- ultrasound microneedles
39
what are the benefits of an ointment
occlusive and emollient, restict transepidermal water loss
40
what are the negatives ointments
greasy, less cosmetically attractive, highly flammable
41
what are the components and characteristics of lotions
liquid formulation, suspension or solution of medication in water, alcohol or other liquids
42
what are a pro and con of lotions
pro- treat scalp, hair bearing areas as less greasy con- if contain alcohol may sting
43
describe the constitutions of gels
thickened aqueous lotions, semi solid, containing high molecular weight polymers
44
what areas are gels best at treating
scalp, hair bearing areas, face
45
describe the constitution of pastes
semisolids, containing finely powdered material, stiff
46
what are the pros and cons of pastes
pros- protective, occlusive, hydrating cons- greasy, difficult to apple
47
what are pastes often used for
cooling, drying, soothing bandages- prevent surrounding skin becoming boggy and macerated
48
describe the constitution of foams
colloid with two-three phases | usually hydrophilic liquid in continuous phase with foaming agent dispersed in gaseous phase
49
what are the advantages of foams
increased penetration of active agents, spread easily over large areas, non greasy/ oily skin
50
what do emollients do
enhance rehydration of epidermis for all dry/scaly conditions
51
for a full body application of emollients how much is needed per week
300-500g
52
what are the tips you need to give when prescribing emollients
- apply immediately after bathing - apply in direction of hair growth - make skin and surfaces slippery - use clean spoon or spatula to remove from tub (risk of contamination) - fire risk if paraffin based - avoid SLS in leave on products
53
why does the price of emollients affect compliance
non proprietary emollient cheap but based on liquid parafin/white soft paraffin and less cosmetically acceptable
54
what is wet wrap therapy used for
very dry (xerotic skin), esp in children, stop itching
55
what is the basic three modes of action of topical steroids
vasoconstrictive anti-inflammatory anti-proliferative
56
what is the role of topical steroids
reduce inflammation, cause immune suppression
57
list topical steroids in order of increasing potency
hydrocortisone (1%) modrasone clobetasone butyrate (0.05%) mometasone betamethasone valerate (0.1%) clobetasol proprionate 0.05%)
58
what are topical corticosteroids used to treat
eczema (dermatitis), psoriasis (esp on face, hairline, scalp- beware rebound, triggering pustular psoriasis), non inflammatory dermatoses (e.g. lichen planus) keloid scars
59
what psoriasis condition is a medical emergency
pustular psoriasis
60
how much topical steroid is needed for a whole body application for an adult
20-30g ointment
61
how much is a fingertip unit
1/2g (covers two hand areas)
62
what do calicneurin inhibitors do
suppress lymphocyte activation (non steroidal anti inflammatory)
63
what are calicneurin inhibitors used to treat
topical treatment of atopic eczema (especially on the face or for children)
64
what are the pros and cons of calicneurin inhibitors
pros- less side effects than steroids, no cutaneous atrophy, one preparation can treat whole body regardless of site of application cons- may cause burning sensation on application, possible risk of cutaneous infections and skin cancer (tell patient to wear suncream)
65
name two calicneurin inhibitors
tacrolimus, pimecrolimus
66
what should antiseptics be used as an alternative as
antibiotics to reduce resistance
67
name 4 antispetics
povidone iodine (skin cleanser), chlorhexidine (hibitane, savlon), triclosan (aquasept, sterzac), hydrogen peroxide (crystacide)
68
what are the clinical uses of antiseptics
recurrent infections, antibiotic resistance, wound irrigation
69
name the method of administration of antivirals used to treat; herpes simplex (cold sore) eczema herpeticum herpes zoster (shingles)
HS topical EH and HZ oral
70
name the topical antifungals used to treat candida (thrush) (satellite lesions)
antiyeast e.g. nystatin, clotrimazole
71
name the topical antifungals used to treat dermatophytes (ringworm)
antifungal e.g. clotrimazole, terbinafine cream
72
name the topical antifungals used to treat pityriasis versicolor
ketoconazole
73
what is tinea corporis
ringworm
74
what is pityriasis versicolor
fungal infection causing pink inflammatory areas on the trunk or areas of hyperpigmentation
75
name four antipruritics and describe them
menthol- to cool skin (added to calamine) capsaicin (reduce neurotransmission) camphor/phenol- for pruritus ani crotamiton- used after treatment of scabies to relieve residual itch
76
what do keratolytics do and treat
soften keratin viral warts, hyperkeratotic eczema and psoriasis, corns and calluses, remove keratin plaques in scalp
77
what are the possible treatments of warts
``` keratolytics (e.g. salicyclic acid) formaldehyde glutaraldehyde silver nitrate cryotherapy podophyllin ```
78
name the possible topical treatments of psoriasis
``` coal tar vitamin D analogue keratolytic topical steroid dithranol phototherapy (guttate psoriasis) ```
79
what are the treatments used for stable chronic plaque psoriasis
coal tar, vitamin D analogues, dithranol
80
what are the pros and cons of coal tar
can be mild or strong messy and smelly
81
what are the pros and cons of vitamin D analogues
pros; clean, no smell, easy to apply cons; can be irritant, use limited to 100g weekly
82
what are the pros and cons of dithranol
pros; effective cons; difficult to use, irritates and stains normal skin surrounding plaque
83
what is the treatments for scalp psoriasis
greasy ointments to soften and remove scale then tar shampoo steroids in alcohol base or shampoo vitamin D analogues
84
what treatments are used for psoriasis in axialla
topical steroids for face, flexures and groin/genitals consider combination antibacterial, antifungal, calcineurin inhibitors
85
what are the side effects of topical therapies used for psoriasis
burning or irritation contact allergic dermatitis local toxicity systemic toxicity reaction to sunscreen
86
what is a side effect of 5- fluorouracil
inflammation
87
name two systemic side effects of topical steroids
suppression of HPA acis by increasing negative feedback cushings disease growth retardation
88
what are 6 reversible steroid side effects
contact allergy to hydrocortisone acneiform eruptions (peri-oral dermatitis, steroid follicultitis, steroid rosacea) tachyphylaxis (decrease in response to drug) pigment changes poor wound healing modification to existing disease (fungal, scabies, rosacea, rebound of pustula psoriasis)
89
what are the permanent cutaneous side effects of steroids
``` striae (stretch marks) atrophy, bruising, telangiectasia (dilated superficial blood vessels) glaucoma, cataract hirutism poor wound healing ```
90
thinning of skin is more likely in children
yes