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Pharmacology > EXAM #5: TOPICAL AGENTS > Flashcards

EXAM #5: TOPICAL AGENTS Flashcards

1
Q

What are the layers of the epidermis?

A

1) Stratum corneum
2) Stratum granulosum
3) Stratum spinosum
4) Stratum basale

*All of which rest on a basal lamina

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2
Q

What is the stratum corneum?

A

Layer of dead keratinocytes

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3
Q

What are the living layers of the epidermis?

A

1) Stratum granulosum
2) Stratum spinosum (synthesis of epidermal proteins)
3) Stratum basale (cell division)

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4
Q

What is the major barrier to percutaneous absorption of drugs?

A

Stratum corneum i.e. the layer of dead keratinocytes

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5
Q

Why is the stratum corneum the major barrier to percutaneous absorption of drugs?

A

Contains corneyocytes that are:

  • Flattened and lipid depleted keratinocytes
  • Plasma membrane has been replaced with protein
  • Secrete lipids that are hydrophobic
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6
Q

What is the rule of thumb for choosing a vehicle for delivering drugs via the skin?

A

If it is wet, dry it; if it is dry, wet it.

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7
Q

What types of vehicles should be used in the scalp and hairy areas?

A 
Lotion
Gels 
Solution
Foams
Aerosols
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8
Q

What types of vehicles are good for intertriginious areas (two skin areas rubbing together)?

A

Creams
Lotion
Solutions

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9
Q

What vehicles are best for wetting?

A

Ointment
Creams
Gels
Lotions/solutions

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10
Q

What vehicles are good for drying?

A

Aerosols
Pastes
Powders
Tinctures

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11
Q

What is PCA?

A

Percutaneous Absorption

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12
Q

What factors affect PCA?

A

1) Concentration of drug in the vehicle
2) Drug diffusion coefficient/ molecular size (less MW gets absorbed faster)
3) Lipophilicity
4) Thickness of the stratum corneum
5) Cutaneous vasculature
6) SA of absorptive surface
7) Mucosal surface

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13
Q

How will skin inflammation affect PCA?

A

Inflammation will increase systemic absorption

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14
Q

How does skin hydration alter PCA?

A

Increased hydration increases PCA

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15
Q

How will occlusion of a topical medication i.e. in plastic wrap alter PCA?

A

Increase PCA

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16
Q

Explain the basic pathophysiology of acne.

A

1) Follicular epidermal hyperproliferation causes the formation of a “plug” limits the exit of sebum from the follicle
- Plus = “comedome”
2) Keratin, sebum, and bacteria* accumulate and cause inflammation

*Propionibacterium acnes

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17
Q

What topical antibiotics are used to treat acne?

A

1) Erythromycin
2) Clindamycin
3) Metronidazole
4) Sodium sulfacetamide
5) Azelaic acid
6) Benzoyl Peroxide

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18
Q

What is the MOA of Erythromycin and Clindamycin to treat acne?

A
  • Inhibit protein synthesis

- Directed against P. acnes bacteria

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19
Q

What is the MOA of Metronidazole to treat acne?

A

Kills bacteria by disrupting DNA

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20
Q

What is the MOA of Sodium Sulfacetamide?

A

Kills P. acnes by inhibiting dihydropteroate synthetase activity i.e. folic acid

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21
Q

What bacteria are treated with Azelaic acid?

A

P. acnes and S. epidermidis

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22
Q

What is the MOA of Azelaic acid?

A

1) Reduces inflammation (free radical scavenging)
2) Reduces keratinization
3) Keratolytic effects cause desquamation

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23
Q

What side effects are associated with Azelaic acid?

A

1) Lightening of the skin

2) Skin dryness

24
Q

What is the MOA of benzoyl peroxide?

A

Releases oxygen that is bactericidal against anaerobic bacteria

*Note that benzoyl peroxide does not lead to resistance

25
Q

How is benzoyl peroxide commonly administered?

A

In combination with erythromycin or clindamycin

26
Q

What is the MOA of Salicylic acid?

A

Topical keratolytic agent that helps to clear comodomes

27
Q

What are four indications for Retinoid drugs?

A

1) Acne
2) Psoriasis
3) Skin aging
4) Skin cancer

28
Q

What side effects are associated with the Retinoids?

A

1) Photosensitivity and increased risk of sunburn

2) Teratogenic

29
Q

What is the MOA of Tretinoin?

A

Activation of RAA receptors leads to:

1) Reduced cohesiveness of follicular epithelial cells that produce comodomes
2) Codemolytic via increasing mitotic activity of follicular epithelial cells to extrude comedomes
3) Reduces keratinization

30
Q

What drug should NOT be used with Tretinoin?

A

Benzoyl peroxidase–will inactive the drug

31
Q

What is the MOA of Adapalene?

A

Via activation of the RAR:

1) Reduced cellular proliferation
2) Reduced inflammation
2) Comedolysis

32
Q

What is the MOA of Isotretinoin?

A

Suppresses sebum production by inducing apoptosis sebum producing cells in the sebaceous glands

33
Q

What unique adverse effect is associated with Isotretoinoin?

A

Highly Teratogenic–must be on oral contraceptive to use

34
Q

What is Isotretinoin used to treat?

A

Oral retinoid used to treat severe acne (this is accutane)

35
Q

What is the MOA of Tazarotene?

A

This a topical retinoid prodrug. Activation of the RAR is thought to:

  • Decreases inflammation
  • Reduce epidermal proliferation
36
Q

What are the clinical uses for Tazarotene?

A

Psoriasis and acne

37
Q

What major adverse effect is associated with Tazarotene?

A

Teratogenic–must be on oral contraceptives to use

38
Q

What is the clinical indication for Acitretin? What type of drug is this?

A

Severe, recalcitrant psoriasis

*Oral retinoid

39
Q

What drug-drug interaction should you be aware of with Acitretin?

A

Alcohol use prolongs half-life for months

Women are advised to avoid pregnancy for 3x years

40
Q

What is Calcipotriene used to treat?

A

Psoriasis

41
Q

What is the MOA of Calcipotriene?

A

Binds to Vitamin D receptor to induce gene transcription changes that are beneficial in psoriasis

42
Q

What are the side effects associated with Calcipotriene?

A
  • Hypercalcemia

- Hypercalciuria

43
Q

What is the strength of hydrocortisone?

A

Weak

44
Q

What is the strength of mometasone furoate?

A

Intermediate

45
Q

What is the strength of clobetasol propionate?

A

High

46
Q

What potency corticosteroid should be applied to the face and intertriginous areas?

A

Low i.e. Hydrocortisone

47
Q

What potency corticosteroid should be applied to palms and soles?

A

High i.e. clobetasol propionate

48
Q

What type of corticosteroid should be avoided in kids?

A

High i.e. clobetasol propionate

49
Q

What are the side effects of topical corticosteroids?

A

1) Epidermal atrophy
2) Acne
3) Enhanced fungal infection
4) Delayed wound healing
5) Hypopigmentation

50
Q

What are the side effects of the systemic corticosteroids?

A

1) HPA-axis suppression
2) Cushing Syndrome
3) Growth retardation

51
Q

What is atopic dermatitis?

A

Eczema i.e. chronic skin disorder with intense pruritus and dried flaking skin

52
Q

How is eczema treated?

A

1) Corticosteroids for primary infection

2) Abx for secondary infection e.g. S. aureus

53
Q

What are Psoralens?

A
  • Topical or oral agents that are ACTIVATED BY LIGHT

- On activation they intercalate with DNA to mediate effects

54
Q

List the two Psoralens.

A

1) Methoxsalen

2) Trioxsalen

55
Q

List the conditions that the Psoralens are used to treat.

A

1) Alopecia
2) Cutaneous T-cell Lymphoma
3) Eczema
4) Psoriasis

56
Q

What are the short-term toxicities associated with the Psoralens?

A

1) Nausea
2) Blistering
3) Painful erythema

57
Q

What are the chronic effects of Psoralens?

A

1) Photoaging
2) Actinic keratoses
3) Nonmelanoma skin cancer

Pharmacology (64 decks)

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