Pharmacology Flashcards

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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
Q

what vehicle should be used if skin is weeping/moist

A

powder

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26
Q

what are three conditions treated by glucocorticoidsteroids

A

atopic eczema, psoriasis, pruritus

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27
Q

what are the clinical effects of glucocorticoid steroids

A

anti-inflammatory, immunosupressant, vasoconstricting, anti proliferating action upon keratinocytes and fibroblasts

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28
Q

what affects glucocorticosteroid penetration, potency and clinical effect

A

body site, state of skin, occulsion, vehicle, concentration of drug, form of drug

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29
Q

what are the serious side effects of potent long term steroids

A

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

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30
Q

describe glucocorticoid molecules and their receptors

A

lipophillic molecules that diffuse across plasma membrane to bind the nuclear receptors (esp. GRalpa) which then bind to glucocorticoid response elements

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31
Q

what is the subcutaneous route of administration

A

injected into fatty adipose tissue

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32
Q

how do drugs administered subcutaneously reach the systemic circulation

A

diffuse into capillaries or lymphatic vessels

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33
Q

what are the advantages of subcutaneous administration

A

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

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34
Q

what is the disadvantage of subcutaneous

A

injection volume limited

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35
Q

how is transdermal drug delivery usually done

A

drug is incorportated into an adhesive patch and applied to the epidermis

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36
Q

what drugs are most suitable for transdermal

A

low molecular weight, moderately lipophillic, potent, relatively brief half life

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37
Q

name three agents that enhance trnsdermal drug delivery

A

water, solvents (ethanol), surfactants

38
Q

how can you physically enhance transdermal drug delivery

A

iontophoresis- prolonged application of low voltage electrical pulses to the skin

electroporation- brief high voltage pulses

sonophoresis- ultrasound

microneedles

39
Q

what are the benefits of an ointment

A

occlusive and emollient, restict transepidermal water loss

40
Q

what are the negatives ointments

A

greasy, less cosmetically attractive, highly flammable

41
Q

what are the components and characteristics of lotions

A

liquid formulation, suspension or solution of medication in water, alcohol or other liquids

42
Q

what are a pro and con of lotions

A

pro- treat scalp, hair bearing areas as less greasy

con- if contain alcohol may sting

43
Q

describe the constitutions of gels

A

thickened aqueous lotions, semi solid, containing high molecular weight polymers

44
Q

what areas are gels best at treating

A

scalp, hair bearing areas, face

45
Q

describe the constitution of pastes

A

semisolids, containing finely powdered material, stiff

46
Q

what are the pros and cons of pastes

A

pros- protective, occlusive, hydrating

cons- greasy, difficult to apple

47
Q

what are pastes often used for

A

cooling, drying, soothing bandages- prevent surrounding skin becoming boggy and macerated

48
Q

describe the constitution of foams

A

colloid with two-three phases

usually hydrophilic liquid in continuous phase with foaming agent dispersed in gaseous phase

49
Q

what are the advantages of foams

A

increased penetration of active agents, spread easily over large areas, non greasy/ oily skin

50
Q

what do emollients do

A

enhance rehydration of epidermis for all dry/scaly conditions

51
Q

for a full body application of emollients how much is needed per week

A

300-500g

52
Q

what are the tips you need to give when prescribing emollients

A
  • 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
Q

why does the price of emollients affect compliance

A

non proprietary emollient cheap but based on liquid parafin/white soft paraffin and less cosmetically acceptable

54
Q

what is wet wrap therapy used for

A

very dry (xerotic skin), esp in children, stop itching

55
Q

what is the basic three modes of action of topical steroids

A

vasoconstrictive
anti-inflammatory
anti-proliferative

56
Q

what is the role of topical steroids

A

reduce inflammation, cause immune suppression

57
Q

list topical steroids in order of increasing potency

A

hydrocortisone (1%)
modrasone clobetasone butyrate (0.05%)
mometasone betamethasone valerate (0.1%)
clobetasol proprionate 0.05%)

58
Q

what are topical corticosteroids used to treat

A

eczema (dermatitis),

psoriasis (esp on face, hairline, scalp- beware rebound, triggering pustular psoriasis),

non inflammatory dermatoses (e.g. lichen planus)

keloid scars

59
Q

what psoriasis condition is a medical emergency

A

pustular psoriasis

60
Q

how much topical steroid is needed for a whole body application for an adult

A

20-30g ointment

61
Q

how much is a fingertip unit

A

1/2g (covers two hand areas)

62
Q

what do calicneurin inhibitors do

A

suppress lymphocyte activation (non steroidal anti inflammatory)

63
Q

what are calicneurin inhibitors used to treat

A

topical treatment of atopic eczema (especially on the face or for children)

64
Q

what are the pros and cons of calicneurin inhibitors

A

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
Q

name two calicneurin inhibitors

A

tacrolimus, pimecrolimus

66
Q

what should antiseptics be used as an alternative as

A

antibiotics to reduce resistance

67
Q

name 4 antispetics

A

povidone iodine (skin cleanser),
chlorhexidine (hibitane, savlon),
triclosan (aquasept, sterzac),
hydrogen peroxide (crystacide)

68
Q

what are the clinical uses of antiseptics

A

recurrent infections, antibiotic resistance, wound irrigation

69
Q

name the method of administration of antivirals used to treat;
herpes simplex (cold sore)
eczema herpeticum
herpes zoster (shingles)

A

HS topical

EH and HZ oral

70
Q

name the topical antifungals used to treat candida (thrush) (satellite lesions)

A

antiyeast e.g. nystatin, clotrimazole

71
Q

name the topical antifungals used to treat dermatophytes (ringworm)

A

antifungal e.g. clotrimazole, terbinafine cream

72
Q

name the topical antifungals used to treat pityriasis versicolor

A

ketoconazole

73
Q

what is tinea corporis

A

ringworm

74
Q

what is pityriasis versicolor

A

fungal infection causing pink inflammatory areas on the trunk or areas of hyperpigmentation

75
Q

name four antipruritics and describe them

A

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
Q

what do keratolytics do and treat

A

soften keratin

viral warts, hyperkeratotic eczema and psoriasis, corns and calluses, remove keratin plaques in scalp

77
Q

what are the possible treatments of warts

A
keratolytics (e.g. salicyclic acid)
formaldehyde 
glutaraldehyde 
silver nitrate
cryotherapy 
podophyllin
78
Q

name the possible topical treatments of psoriasis

A
coal tar
vitamin D analogue
keratolytic 
topical steroid
dithranol
phototherapy (guttate psoriasis)
79
Q

what are the treatments used for stable chronic plaque psoriasis

A

coal tar,
vitamin D analogues,
dithranol

80
Q

what are the pros and cons of coal tar

A

can be mild or strong

messy and smelly

81
Q

what are the pros and cons of vitamin D analogues

A

pros; clean, no smell, easy to apply

cons; can be irritant, use limited to 100g weekly

82
Q

what are the pros and cons of dithranol

A

pros; effective

cons; difficult to use, irritates and stains normal skin surrounding plaque

83
Q

what is the treatments for scalp psoriasis

A

greasy ointments to soften and remove scale then
tar shampoo
steroids in alcohol base or shampoo
vitamin D analogues

84
Q

what treatments are used for psoriasis in axialla

A

topical steroids for face, flexures and groin/genitals

consider combination antibacterial, antifungal,

calcineurin inhibitors

85
Q

what are the side effects of topical therapies used for psoriasis

A

burning or irritation

contact allergic dermatitis

local toxicity

systemic toxicity

reaction to sunscreen

86
Q

what is a side effect of 5- fluorouracil

A

inflammation

87
Q

name two systemic side effects of topical steroids

A

suppression of HPA acis by increasing negative feedback

cushings disease

growth retardation

88
Q

what are 6 reversible steroid side effects

A

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
Q

what are the permanent cutaneous side effects of steroids

A
striae (stretch marks)
atrophy, bruising, telangiectasia (dilated superficial blood vessels)
glaucoma, cataract
hirutism 
poor wound healing
90
Q

thinning of skin is more likely in children

A

yes