Topical Therapeutics Flashcards

1
Q

Medications gain access to sites of action through three primary mechanisms? (3)

A
  1. passive diffusion - through the stratum corneum
  2. transportation through channels or pores within a lacunar system in the stratum corneum
  3. transportation via appendageal structures - such as sweat glands / follicles
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2
Q

Drug factors affecting percutaneous absorption? (4)

A

active drug concentration
composition of vehicle
molecular size of drug/prodrug
lipophilicity of drug

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3
Q

Patient factors affect percutaneous absorption (4)

A

presence of barrier disruption
anatomic location
skin hydration
occlusion

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4
Q

How drug concentration influences absorption

A

absorption is directly proportional to the concentration of the active ingredient in the medication

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5
Q

How molecular size influences drug absorption

A

diffusion of a compound is inversely proportional to the molecular size of the drug

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6
Q

lipophilicity of the drug and absorption

A

lipophilic topical agents are more likely to permeate the skin than hydrophilic

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7
Q

How can vehicle influence drug absorption?

A

given same active concentration - different vehicles can yield different absorptions

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8
Q

How does occlusion influence absorption?

A

Occlusion of the skin often leads to markedly increased skin hydration - therefore, active ingredients that are delivered in the form of ointment / tape / or to the skin folds reach a much higher concentration because occlusion prevents loss of medication by evaporation / friction / or exfoliation

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9
Q

how does anatomic location influence percutaneous absorption?

A

thicker stratum corneum –> lower absorption

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10
Q

Composition

ointment

A

water in oil emulsion

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11
Q

composition

cream

A

oil in water emulsion

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12
Q

composition

gel

A

semisolid emulsion in alcohol base

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13
Q

composition

lotion / solution

A

powder in water (some oil in water)

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14
Q

composition

foam?

A

pressurized collection of gaseous bubbles in matrix of liquid film

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15
Q

potency of active ingredient in ointment?

A

strong

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16
Q

ointment

  • hydration?
  • sensitization?
  • irritation?
A

high hydration
low sensitization
low irritation

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17
Q

ointment

body sites?

A

non intertreginous

avoid use on face / hands / groin

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18
Q
creams
potency?
hydration?
sensitization?
irritation?
A

moderate potency

some hydration but not as much as oinment

significant sensitization

low irritation

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19
Q

creams

body sites?

A

all body sites

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20
Q

creams

avoid use with?

A

maceration = the softening and breaking down of skin resulting from prolonged exposure to moisture

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21
Q
gels 
potency?
hydration?
sensitization?
irriatation?
A

potency - strong
hydration - drying
sensitization risk - high
irritation risk - high

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22
Q

gels

sites for use?

A

oral mucosa

scalp

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23
Q

gels

avoid?

A

fissures
erosions
macerated regions

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24
Q
lotions // solutions 
potency?
hydration?
sensitization?
irritation?
A

potency - low
hydration - variably drying
sensitization - significant
irritation - moderate

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25
Q

lotions / solution

sites amenable?

A

scalp / intertriginous

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26
Q

lotions / solutions

avoid ?

A

fissures / erosions

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27
Q

foams

potency

A

strong potency

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28
Q

foams

MOA

A

Foam matrix is stable at room temp, but readily melts at body temp — after the foam is applied to the skin, the volatile components (such as alcohol and water) quickly evaporate, leaving behind lipid and polar components containing supersaturated active ingredients to interact with the stratum corneum - these supersaturated solutions enable maximal delivery of active ingredients into the skin

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29
Q

foam

what might alcohol do to influence absorption?

A

may play a role in altering the stratum corneum - lead to improve penetration of active ingredient

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30
Q

foam -

sites amenable

A

hair bearing areas

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31
Q

foam

aovid

A

fissures

erosions

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32
Q

when selecting vehicle

3 factors

A

anatomic location
contact allergy / sensitization
irritancy

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33
Q

for hair bearing regions, the clinician should consider choosing which vehicle

A

solution or foam
over
ointment

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34
Q

_____________ vehicles contain preservatives that may increase the risk of contact allergy and sensitization - these preservatives include known allergens such as parabens and formalin releasers

A

water-based
creams
lotions
solutions

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35
Q

irritancy is most notably associated with high concentration of _____________, other types of _____________ and certain __________ vehicle ingredients.

A

propylene alcohol
alcohol
acidic

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36
Q

avoid using formulations containing ________ or __________ on extensively fissured, eroded, or macerated areas

A

alcohol

salicylates

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37
Q

FTU

A

the amount of ointment dispensed from a 5 mm diameter nozzle that is
applied to the distal third of the index finger, from the crease under the distal
interphalangeal joint to the fingertip

0.5grams

38
Q

ointment for face and neck

A

2.5 FTU

39
Q

ointment fo trunk / front of back

A

7 FTU

40
Q

Ointment arm

A

3 FTU

41
Q

Ointment leg

A

6 FTU

42
Q

Ointment hand - both sides

A

1 FTU

43
Q

Ointment foot

A

2 FTU

44
Q

1 gram cream covers?

A

10cmx10cm

45
Q

1 gram ointment vs cream

A

ointment spreads 10% further

46
Q

ointment grams necessary to cover body

A

20g adult male

47
Q

Mechanism of action of glucocorticoids

A
bind intracellular receptor
release HSP
translocate to nucleus
dimerize
regulate transcription
48
Q

glucorticoids downstream effects?

A

alter transcription rate - inflammatory pathways

49
Q

glucocorticoids and CREB?

A

glucocorticoid receptor interacts with cAMP response element binding protein to effect inflammation

50
Q

glucocorticoids and NF-kB?

A

inhibit NF-kB - reducing chronic inflammatory elements

51
Q

glucocorticoids and AP-1

A

glucocorticoid receptor interats with ativating protein 1 - which controls transcription of cytokine genes

52
Q

glucocorticoids and TNF-alpha

A

inhibit

53
Q

Glucocorticoids and

granulocyte macrophage colony stimulating factor?

A

inihibt

54
Q

glucocorticosteroids and IL-1,2,6,8

A

inhibit

55
Q

Glucocorticoids and COX
adhesion
selectins

A

inhibit

56
Q

glucocoricosteroids and potency

A

scale from 1-7

1 most potent - 7 least

57
Q

“The Gentle Touch”
glucocorticosteroid

treat?

A

Hydrocortisone 2.5% (cream or ointment) belongs to class 7, the lowest potency class.

efficacious for mild eczema in children and adults and for treating inflammatory
dermatoses involving anatomic regions such as the face, intertriginous areas, or groin, where mid to high-potency topical steroids may be contraindicated.

58
Q

“The Almost All-Purpose Weapon”
glucocorticoid

treat?

A

Triamcinolone Acetonide 0.1% (cream or ointment):

class 4, or
a mid-potency class of topical steroids. Triamcinolone 0.1% is effective against most
moderate spongiotic dermatoses (including eczematous dermatitis, atopic dermatitis,
allergic contact dermatitis, arthropod bites, id reactions, drug reactions) involving the
trunk and extremities. Long-term use of triamcinolone is not recommended for facial,
intertriginous, and groin lesions.

59
Q

“Hercules”
glucocorticosteroid

treat?

A

Clobetasol propionate 0.05% cream or ointment belongs to Class 1 of topical steroids,
and it is considered one of the most potent topical steroids. Clobetasol is best used in
acute eruptions that necessitate relatively rapid amelioration, such as contact dermatitis or
acute drug eruptions. Clobetasol should be avoided on the face, intertriginous areas, or
the groin, where the skin is relatively thin. Longer-term use of clobetasol requires
monitoring of development of adverse effects

60
Q

Why might the same active glucocorticosteroid ingredient in an ointment be more potent than in a cream / solution?

A

Due to the occlusive nature of an ointment vehicle, the same active glucocorticosteroid
ingredient in an ointment vehicle will often be more potent than the same ingredient in a
cream, lotion, or solution vehicle. This is because the ointment vehicle enhances
hydration of the stratum corneum, which leads to improved penetration of the medication

61
Q

In general, where should you avoid potent / superpotent topical steroids and why?

A
hould be avoided for use on the face,
skin folds (axillary and intertriginous folds), and groin areas due to the risk of epidermal
atrophy and potential for steroid-induced rosacea/perioral dermatitis on the face
62
Q

most common adverse affect of topical glucocorticosteroids

A

most
common adverse effect is skin atrophy, and this is most commonly associated with longterm
use of potent to super-potent topical steroids.

63
Q

how does skin atrophy from glucocorticosteroid use manifest?

A

Skin atrophy may manifest as shiny,
thin skin, telangiectasia, and striae formation. Areas with baseline relatively thin
epidermis such as face and intertriginous areas are more susceptible to developing skin
atrophy compared to other areas of the body

64
Q

How can you have systemic effects from glucocorticosteroids?

A

Extensive and long-term use of potent or super-potent topical steroids have been
associated with systemic side effects due to increased systemic absorption of
percutaneously delivered active ingredient.

65
Q

Potential systemic effects of glucocorticosteroids

A

Potential systemic side effects include
adrenal suppression, Cushing’s syndrome, and growth retardation in children. For
example, psoriasis and atopic dermatitis patients may require longer-term use of potent
topical steroids to cover larger body surface areas than other dermatologic patient
populations. Systemic adverse effects of topical steroids are particularly relevant to these
populations

66
Q

AAD guideline for max class I

A
Currently, the AAD guideline for maximum use of class I topical steroids is
to not exceed 50 grams per week
67
Q

why are brand names better if they have the same active ingredient?

A

because they have better vehicles

68
Q

powder + grease =

A

protective paste

e.g. baby bottom

69
Q

grease + liquid =

A

ointment, creams, lotions

70
Q

oil in water

A

aqueous cream

71
Q

water in oil

A

ointments

72
Q

gel is good for treating which areas

A

hair

73
Q

factors influencing absorption

A

active concentration
composition of vehicle
molecular size
lipophilicity

74
Q

what type of vehicle would you choose for patient exposed to poison ivy?

A

ointment - best penetrating

75
Q

how much ointment needed to cover palmar x2

A

0.5 grams

76
Q

basic effetiveness of glucocorticosteroids

A

inhibit transcription of inflammatory cytokines e.g. NF-kB

77
Q

NF-kB and glucocorticoids

A

GC inhibit NF-kB mediated transcription of inflammatory cytokines

78
Q

vitamin D analog and retinoids block?

A

AP-1

Inhibit synthesis of cytokines

79
Q

Inhibitors of calcineurin block?

A

NF-AT - inihibit synthesis of cytokines

80
Q

Hydrocortisone

class?

A

7

81
Q

Triamicinolone Acetonide

A

4

82
Q

Clobetasol

A

1

83
Q

what would you use to treat on baby face?

A

hydrocortisone 2.5%

84
Q

step-down approach

A

start with very strong- 1

then step down

85
Q

extensive dermatitis on trunk what would you use

A

tiamicinolone 0.1% ointment

86
Q

best to use in
mild eczema children / adults
inflammatory dermatoses involving face / intertriginous / groin

A

hydrocortisone

87
Q

best to use in

acute eruptions that necessitate rapid relief such as contact dermatitis of acute drug eruptions

A

clobetasol propionate

88
Q

when should you avoid clobetasol propionate?

A

face
intertriginous
groin

long term

89
Q

best to use in
moderate spongiotic dermatitis (including eczematous dermatitis, atopic, allergic contact, athropod bite)
use on trunk and extremities

A

triamcinolone acetonide

90
Q

avoid triamcinolone acetonide

A

long term
facial
intertriginous
groin