Topical Agents Flashcards

1
Q

What are the layers of the skin from superficial to deep? (5)

A
Stratum corneum
Stratum lucidum
Stratum granulosum
Stratum spinosum
Stratum basale
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2
Q

Where does cell division occur within the skin?

A

Basal layer

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3
Q

Which cells of the skin synthesize epidermal proteins?

A

Spinous layers

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4
Q

What happens to the cell membrane of skin epithelial cell as they move toward the periphery?

A

Plasma membrane is replaced by an envelope of insoluble lipid compounds

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5
Q

What happens in the stratum lucidum?

A

Cell death

Strengthening of the keratin filaments via crosslinking

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6
Q

What are the cells that are a part of the stratum corneum?

A

Corneocytes (flattened and lipid depleted keratinocytes)

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7
Q

What is the rate limiting step (major barrier) in percutaneous absorption?

A

Stratum corneum

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8
Q

What are the appendages (shunt routes) through the skin?

A

Through hair follicles/ sweat glands

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9
Q

What are the two routes that drugs can go through corneocytes?

A

Intracellularly

Transcellularly

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10
Q

What are the drug “vehicles” for percutaneous drugs?

A

Inactive part of the preparation that carries the drug

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11
Q

What are the common vehicles for percutaneous drugs?

A

Ointments
Creams
Gels/foam

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12
Q

Where do you not want to apply ointments?

A

Areas where skin rubs against skin

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13
Q

What are ointments?

A

Water in oil emulsion

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14
Q

What are creams?

A

Oil in water emulsion

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15
Q

What are gels/foams?

A

Water-soluble emulsion

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16
Q

What types of vehicles are appropriate for intertriginous areas of the body?

A

Creams
Lotion
Solutions

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17
Q

What are aerosols?

A

Fine solid or liquid particles dispersed in gas

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18
Q

What type of vehicle is appropriate for the scalp and hairy areas?

A
Lotions
Gels
Solutions
Foams
Aerosols
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19
Q

Where are lotions, gels, solutions, and aerosols useful?

A

Scalp and hairy areas

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20
Q

Where are creams, lotions and solutions used?

A

Intertriginous areas

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21
Q

What is the golden rule of dermatology?

A

If it’s wet, dry it

If it’s dry, wet it

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22
Q

What are the factors that determine the rate of percutaneous absorption? (4)

A
  • Concentration
  • Partition of drug from the vehicle
  • Diffusion of drug across the skin layer
  • Thickness of the stratum corneum
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23
Q

What is the partition coefficient?

A

Partitioning of the drug from the vehicle into the stratum corneum

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24
Q

What is the drug diffusion coefficient?

A

Molecule aspect of the drug allowing diffusion across the skin layers

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25
Q

What is Fick’s law?

A

Determines the rate of drug diffusion across a barrier like the skin

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26
Q

How is concentration of a drug related to the rate of percutaneous absorption?

A

directly related

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27
Q

How is lipophilicity of a drug related to the rate of percutaneous absorption?

A

Direct

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28
Q

How is molecular size of a drug related to the rate of percutaneous absorption?

A

Inversely

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29
Q

How is the stratum corneum thickness related to the rate of percutaneous absorption?

A

Negative relation

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30
Q

How is cutaneous vasculature related to the rate of percutaneous absorption?

A

Direct

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31
Q

How is area of absorption surface related to the rate of percutaneous absorption?

A

Direct

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32
Q

Are mucosal surfaces better or worse at absorbing drugs?

A

Better

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33
Q

How is the moistness related to the rate of percutaneous absorption?

A

Direct

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34
Q

How is age of patient related to the rate of percutaneous absorption?

A

Younger = less total body, and increase SA, leading to increased toxicity

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35
Q

How is occlusion of the skin related to the rate of percutaneous absorption?

A

Increases PCA

36
Q

What is the effect of the stratum corneum in terms of drug absorption?

A

Holds drugs, increasing the duration of the drug

37
Q

What is the most penetrating area for percutaneous absorption? Second most? Least?

A

Mucus membranes
Scrotum
Nails

38
Q

What is the effect of inflamed skin on the rate of absorption of a topical drug? Why?

A

Increases due to increased permeability and vasodilation in that area

39
Q

What is the bacteria that is associated with acne?

A

Propionibacterium acnes

40
Q

What is the pathophysiology of acne?

A

Hyperkeratotic infundibulum cause clogging of the pore, in combination with increased sebum production.

This causes dilation of hair follicles

41
Q

What are the drugs that are used to treat acne?

A
Abx
Retinoids
Salicylic acid
Oral contraceptives
Anti-androgens
42
Q

What are the main topical abx to treat acne? MOA?

A
  • Erythromycin (macrolide, binds 50s)
  • Clindamycin (binds 50s)
  • Metronidazole (intercalating DNA)
43
Q

What is the MOA of sodium sulfacetamide? Use?

A

Kills by inhibiting folic acid biosynthesis (sulfa)

Abx used to treat acne

44
Q

What is the MOA of azelaic acid? Use?

A

Free radicalization
Reduces keratinization

Abx used to treat acne

45
Q

What are the side effects of Azelaic acid?

A

Lightening of skin and drying

46
Q

What is the MOA of sulfa drugs?

A

Inhibit folate synthetase

47
Q

What is the MOA of benzoyl peroxide? Which bacteria does this kill?

A

Kill anaerobic bacteria be releasing oxygen

48
Q

True or false: benzoyl peroxide has a high resistant rate

A

False- no resistance, even with long term use

49
Q

What are the comedones?

A

Plugs of the follicle

50
Q

What does it mean when Benzoyl peroxide if comedolytic?

A

Breaks comedones

51
Q

What is the MOA of salicylic acid? What is this used to treat?

A

Increases solubilization of stratum corneum by breaking keratin hydrogen bonds

Low doses = acne
High doses = warts

52
Q

What are retinoids? MOA? Use?

A

Chemical that have biological activity like Vit A

Binds to retinoic acid receptor (RXR or RAR), and induce cell death and differentiation

Acne treatment

53
Q

What are the side effects of the retinoids?

A

Photosensitivity

54
Q

What is the MOA of Tretinoin (3)? Use? Adverse effects?

A

Retinoid for the treatment of acne

Decreases cohesiveness of follicular epithelial cells, increases mitotic activity in basal follicular cells, and reduces keratinization, to break the comedone

Pruritus and photosensitivity

55
Q

What is the interaction of retinoid drugs and benzoyl peroxide?

A

Benzoyl peroxide inactivates retinoid drugs

56
Q

What is the pregnancy category of Tretinoin?

A

C

57
Q

What is the MOA of Adapalene? Use? Side effects?

A

Retinoid that reduces cellular proliferation and inflammation

Pruritis, xerosis

58
Q

What is the pregnancy category of Adapalene?

A

C

59
Q

What is the MOA of Isotretinoin? Use? Side effects?

A

Oral retinoid that suppresses sebum production by inducing apoptosis of cells in sebaceous glands

Severe acne

Teratogenesis

60
Q

What is the pregnancy risk of isotretinoin?

A

Significant teratogenic risk–women must be placed on birth control

61
Q

What is the MOA of Tazarotene? Use? Side effects?

A

Retinoid that decreases inflammation and epidermal hyperproliferation

Treats psoriasis

Photosensitivity and teratogenic

62
Q

What is the pregnancy risk of tazarotene?

A

X–contraceptives should be used

63
Q

What are the four retinoids?

A

Isotretinoin
Tazarotene
Tretinoin
Adapalene

64
Q

What are the two types of anti inflammatory drugs for acne?

A

abx

Retinoids

65
Q

What are the drugs that inhibit sebaceous gland function?

A

Antiandrogens
Oral contraceptives
Isotretinoin

66
Q

What is psoriasis? What is the most common type?

A

Autoimmune disease causing inflammation and keratinocyte hyperproliferation

Plaque psoriasis

67
Q

What is the MOA of acitretin? Use? Side effects?

A

Retinoid with unknown MOA

Treats recalcitrant psoriasis

Highly teratogenic

68
Q

What is the effect of EtOH with acitretin? What does this mean?

A

Converts it to etretinate, that has a half life of 3 months

Do not get prego

69
Q

What is the MOA of calcipotriene? Use? Side effects?

A

binds to Vit D receptor, and inhibits proliferation of keratinocytes, and inhibits IL-2 and IL-6 by T cells

Treats psoriasis

Hypercalcemia and hypercalciuria

70
Q

What are the three major corticosteroids used to treat skin disorders? What is the potency of each?

A

Hydrocortisone-low
Mometasone - med
Clobetasol propionate -high

71
Q

When there is a large surface area to treat, what strength of corticosteroids should be used?

A

Weak to med

72
Q

What strength of corticosteroids should be used for facial issues?

A

Low

73
Q

What strength of corticosteroids should be used for palms and soles?

A

High

74
Q

What is tachyphylaxis that can occur with high potency corticosteroids? How can this be prevented?

A

Diminished therapeutic benefit with prolonged use

Alternate day applications

75
Q

What are the adverse topical effects to topical corticosteroids?

A

Atrophy
Acne
Enhanced fungal infx
Retard wound healing

76
Q

What are the three major adverse systemic effects to topical corticosteroids?

A

HPA axis suppression
Cushing’s
Growth retardation

77
Q

What is atopic dermatitis?

A

Eczema–intense dryness and itching

78
Q

What causes atopic dermatitis?

A

Unknown, but predisposed if there are factors that inhibit epidermal barrier

79
Q

What is the treatment for atopic dermatitis?

A

Corticosteroids

80
Q

What is the the photochemical therapy that is used to treat eczema?

A

Psoralen + UV light (which activates them)

81
Q

What are the two psoralens that are used?

A

Methoxsalen

Trioxsalen

82
Q

What are the uses for Psoralens? (4)

A

Alopecia
Cutaneous T cell lymphoma
Eczema
Psoriasis

83
Q

What are the side effects of photochemical therapy?

A

Nausea, painful erythema

Photoaging

84
Q

What is the MOA of Mometasone? Use?

A

Intermediate Topical steroid used to treat psoriasis

85
Q

What is the MOA of Clobetasol? Use?

A

Strong Topical steroid used to treat psoriasis