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Drug Action III > Acne, Scars, Burns (Med Chem) - Block 1 > Flashcards

Acne, Scars, Burns (Med Chem) - Block 1 Flashcards

1
Q

What is the active for of vitamin A?

A

Trans-retinol

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2
Q

What is the absorbable form of vitamin a?

A

Retinol

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3
Q

Idetnify the structure

A

trans-retinol (vitamin A)

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4
Q

What is the circulating form of vitmain D?

A

25-hydroxycholecalciferol

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5
Q

What is the active form of vitamin D?

A

1,25-Dihydroxycholecalciferol (calcitriol)

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6
Q

Identify the structure?

A

25-hydroxycholecalciferol (inactive)

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7
Q

Describe and explain the 6 dermatological principles

A

Regional variation in permeation: areas of decreasing thickness are more permeable and may require less drug (Increasing thickness: Eyelid/scrotum< face/ear < general body < palm/sole)
Concentration gradient: Increasing concnetration gradient increases mass of drug transferred per unit time (overcome resistance by increasing concnetration)
Dosing schedule: Skin is a reservoir increasing half-life (dose QD)
Vehicles and occlusion: Need to select proper vehicle, hydrated skin is more absorption
Metabolism: No first-pass metabolism in the epidermis
Pediatrics: greater ratio of surface area/mass -> greater systemic exposure

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8
Q

What are the considerations when selecting a vehicle?

A
  1. Solubility of drug in vehicle
  2. Rate of release of drug from vehicle
  3. Ability of vehicle to hydrate stratum corneum enhancing penetration
  4. Stability of drug in vehicle
  5. Interactions of vehicle, stratum corneum and drug (emulsifying agenets can irritate)
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9
Q

Rank vehicles increasing ability to stop evaporation from surface of skin?

A

Tinctures < wet dressings < lotions < gels < aerosols < powders < pastes < creams < foams < ointments

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10
Q

Vehicles for acute inflammation and oozing?

A

Drying agents: tinctures, wet dressings, lotions

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11
Q

Vehicles for chronic inflammation with xerosis/scaling/lichenification?

A

Lubricating: creams, ointments

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12
Q

Vehicles for scalp or hair-bearing areas?

A

tinctures, lotions, gels, foams, aerosols

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13
Q

Vehicles for intertriginous areas?

A

Emulsified vanishing-type cream (no maceration)

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14
Q

Describe the properties of dermatological drugs?

A
  1. <500 Da
  2. High lipophilicity but not too high
  3. Small, water soluble compounds don’t penetrate through healthy stratum corneum
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15
Q

MOA of retinoids?

A

Activate retinoic acid receptors forming heterodimers to bind to DNA sequences (retinoic acid response elements (RAREs)) -> activate transcription of genes -> cellular differentiation and proliferation

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16
Q

Onset of retinoids?

A

May not see results for at least 4 weeks

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17
Q

Describe the SAR of retinoids?

A
  1. Cyclic end group
  2. Conjugated double bonds
  3. Polar end group
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18
Q

MOA of topical retinoids?

A

To correct abnormal follicular keratinization, reduce P acnes counts and reduce inflammation

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19
Q

Topical retinoids?

ADR, CI, Counseling

A

ADR:
1. Erythema, desquamation, xerosis, burning, stinging
2. Photosensitivity reactions can occur, risk for severe sunburns (wear sunscreen)

CI: Pregnancy
Counseling: Dry skin application

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20
Q

What is the acid form of Vitamin A?

A

tretinoin (alcohol form)

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21
Q

MOA of tretinoin?

A

Transforms closed comedones to open therefore aggravating acne during first 4-6 weeks

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22
Q

Outcomes of prolonged use of tretinoin?

A
  1. Dermal collagen syntheis
  2. New blood vessel formation
  3. Thickening of epidermis
  4. Deminishes fine lines and wrinkles
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23
Q

Tretinoin

ADR, COunseling, Interaction, Forms

A

ADR: Slight erythema with mild peeling (remains in epidermis, insoluble)
Counseling: apply at night due to photolabile
Interaction: Inactivated by benzoyl peroxide (OH)
Form: gel, cream, lotion, TR (microspheres) are less irritating

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24
Q

Adapalene

Brand, FOrm, Advantages, Interactions

A

Differin, Plixida
Form: gel, cream, lotion
Advatnages: Stable in sunlight and benzoyl peroxide, less irritating
Interactions: enhances permeation of clindamycin into the skin

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25
Q

Tazarotene

MOA, Indication, Form, DOA

A

MOA: Prodrug (acetylenic retinoid)
Indication: Photoaging, wrinkles, plaque psoriasis
FOrm: Cream, foam, gel, lotion
DOA: Retained in skin for 3 months

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26
Q

How does isotretinoin differ from other retinoids?

A

Synthetic: inhibits sebaceous gland size, function, and follicular keratinization

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27
Q

Isotretinoin

PK, Form, BBW

A

PK: Well absorbed but low bioavailability, high PPB, better absorption with fatty meals
FOrm: PO, Lipid-solubilized formulation – CIP-isotretinoin (Absorica)
BBW: Teratogenicity via iPLEDGE REMS

28
Q

What is iPLEDGE REMS?

A
  1. Women of childbearing potential must use two forms of contraception for at least one month before therapy through one or more menstrual cycles following discontinuance
  2. Also must obtain two negative serum pregnancy tests before, and one monthly during treatment

Drug: Isotretinoin

29
Q

Trifarotene

MOA, Form

A

MOA: Selective binding to RAR-γ receptors found on the skin
Form: Cream

30
Q

Azelaic Acid

MOA, Indication, Form, ADR, Onset

A

MOA: Antimicrobial against P acnes, in vitro inhibition of testosterone to DHT
Indication: Acne vulgaris, rosacea, post-inflammatory dyspigmentation
Form: cream, foam, gel
ADR: Irritation with redness and dryness of skin during first week
Onset: 6-8 weeks

31
Q

What medications are for acne?

A
  1. Retinoids
  2. Tretinoin
  3. Adapalene
  4. Tazarotene
  5. Isotretinoin
  6. Trifarotene
  7. Azelaic Acid
32
Q

Describe the structure of acitretin

A

Metabolite of retinoid etretinate that is reversible when exposed to alcohol

33
Q

What is etretinate?

A

Teratogen with 120 day half-life and found in the plasma fro up to 3 years

34
Q

Acitretin

Form, Disadvantages, Interactions, ADR

A

Form: PO
Disadvantages: More teratogenic than isotretinoin
Interactions: Pregnancy, No ethanol during and for 2 months after discontinuation
ADR: Hepatotoxicity with liver enzyme elevation

35
Q

Tazoretene

BBW

A
  1. Absorbed percutaneously, can get teratogenic systemic concentrations if applied to > 20% of total BSA
  2. Corticosteroids improve efficacy and reduce side effects of burning, itching and irritation
36
Q

Calcipotriene

MOA, Form, ADR, Counseling

A

MOA: Synthetic Vit D derivative that binds to VDR -> w/ RXR-a and binds to vit D respone elements on DNA -> Increases gene expression, epidermal defferentiation and inflammation
Forms: Cream, scalp lotion, foam
ADR: Perilesional irritatn, photosensitivity, hypercalcemia/uria from PPB
Counseling: Avoid facial contact, ocular irritation

37
Q

Calcitriol

MOA, Form, Advantages

A

MOA: Active form of vitamin D
Form: Ointment
Advantages: Better tolerated in intertriginous and sensitive areas of skin

38
Q

Tildrakizumab

MOA, Counseling, Form

A

MOA: Abti IL-23 antibody (prevention of receptor binding)
Counseling: Evaluation of active/prir TB infection before tx
Form: SQ self-admin

39
Q

What are the advantages of using topical CS?

A
  1. Anti-inflammatory
  2. Minimally absorbed fromnormalskin
  3. QD
  4. Ointment bases have better activity than creams/lotions
40
Q

What are the prominent ADRs of topical CS?

A
  1. Atrophy
  2. Acne
  3. Rosacea and dermatitis if use fluorinated compound on face
  4. hypopigmenttion
  5. Hypertrichosis
  6. Alterations of cutaneous infections
  7. Increased intraocular pressure
  8. Cintact dermatitis
  9. Potent CS for prolonged periods can need to systemic effects e.i. Cushings or retardation
41
Q

Anthralin

MOA, Form, ADR

A

MOA: Synthetic chrysarobin
Form: Cream
ADR: Irritant contact dermatitis, staining

42
Q

Medications that treat psoriasis?

A
  1. Acitretin
  2. Tazoretene
  3. Calcipotiene
  4. Calcitriol
  5. Tildrakizumab
  6. Topical CS
  7. Anthralin
43
Q

What are examples of macrolides?

A

Tacrolimus and Pimecrolimus

44
Q

Tacrolimus/Pimecrolimus

MOA, Form, BBW, Advantages

A

MOA: Bind to FKBP12 to inhibit calcineurin
* Inhibtis T cell activation and prevents release of inflammatory cytokines and mediators from mast cells after stimulation by IgE

Form: Ointment (tacrolimus), cream (pimecrolimus)
BBW: tumorgenicity
Advantages: No risk for skin atrophy

45
Q

Dupilumab

MOA, Form, ADR, Counseling

A

MOA: IL4 receptor a antagonist, inhibits IL4 and 13 signaling
Form: SQ
ADR: Injection site reaction, conjunctivitis, keratitis, nasopharyngitis, peripheral eosinophilia, face redness
Counseling: Montior eye sx

46
Q

Tralokinumab

MOA, Form, ADR, Advantages

A

MOA: Anti-IL-13 antibody (blocks receptors)
Form: SQ
ADR: Upper respiratory infection, HA, inj site reactions, conjunctivitis
Advantages: Conjunctivitis is less common than in dupilumab

47
Q

Abrocitinib

MOA, Frm, PK, Disadvantages, Interactions

A

MOA: JAK 1 inhibitor
Form: PO
PK: half life is 5-6 hr, metabolized by CYP2C19
Disadvantages: May impair fertility but is reversible
Interactions: Antiplatelets except low-dose aspirin during the first 3 months

48
Q

Ruxolitinib

MOA, Form, BBW

A

MOA: JAK1/JAK2 inhibitor
Form: Cream
BBW: Don’t exceed 20% of total BSA and max of 60 g/wk
* Serious infection
* Mortality
* Malignacies
* Major adverse CV events
* thrombosis

49
Q

Crisaborole

MOA, Form, Advantages

A

MOA: Anti-inflammatory PDE4B inhibitor
* Mimics phosphate of cAMP

Form: Ointment
Advantages: Good safety for long term tx

50
Q

Medications for atopic dermatitis?

A
  1. Tacrolimus/Pimecrolimus
  2. Dupilumab
  3. Tralokinumab
  4. Abrocitinib
  5. Ruxolitinib
  6. Crisaborole
51
Q

Monoxidil

MOA, DIsadvantages, Form, ADR

A

MOA: Potassium channel opener and reverses progressive miniaturization of terminal scalp hairs
Disadvantages: effects are not permanent, hair loss in 4-6 months after DC
Form: solution, foam
ADR: hypertrichosis
Counseling: Wash hands after applying
* Percutaneous absorption, watch out for patients with CVD, may cause hypotension
* Patients with increased sulfotransferase enzyme activity are more likely to respond

52
Q

What is the endogenous ligand of 5a reductase inhibitors?

A

Testosterone

53
Q

MOA of 5a reductase inhibitors?

A

Block conversion of testosterone to DHT in the indication of andrgenic alopecia

Irreversible inhibitors due to the adduction of NADPH

54
Q

How is 5a reductase inhibitors metabolized?

A

CYP3A4: interactions with inhibitors

55
Q

What are examples of 5a reductase inhibitors?

A

Dutasteride
Finasteride (Propecia)

56
Q

Finasteride

MOA, Indication, Form, ADR, CI

A

MOA: type II isozyme
Indication: requires continued tx necessary to sustain benefit, results in 3-6 months
Form: PO
ADR: decreased libido, ejaculation disorders, ED
CI: women who are pregnant or could become pregnant should not be exposed to (can be absorbed in skin)

57
Q

Dutasteride

MOA, Advantages, Disadvantages, Form, CI

A

MOA: Type 1 and 2 isozymes
Advantages: similar/greater efficacy and longer terminal elimination half life
Disadvantages: ADRs are more common
Form: PO
CI: Women who can or are pregnant

58
Q

What are the medications used for alopecia?

A
  1. Minoxidil
  2. Finasteride
  3. Dutasteride
58
Q

How does povidone iodine from rgular iodine?

A

Complex iodine with polyvinyl pyrolidone

Less irritating, skin hypersensitive, and staining than iodine tinctures

59
Q

What are the disadvantages of povidone iodine?

A

Requires drying time on skin before becoming active

59
Q

Silver Sulfadiazine

MOA, Dosage forms

A

MOA: silver salts are a bactericidal
Form: cream
* salt is slightly soluble therefore doesn’t penetrate cell wall

59
Q

Hydrogen peroxide

Indication, MOA, Advantages

A

Indication: Broad spectrum against bacteria, spores, viruses, and fungi
MOA: Rleases oxygen
Advantages: Decomposition products are water and oxygen

59
Q

What are the advatnages silver sulfadiazine?

A

A: Effective against Pseudomonas
* Not really absorbed into body fluids

60
Q

Dakin’s solution

MOA, Advantages, ADR

A

MOA: Sodium hypochlorite solution where chlorine reacts with water to form hyperchlorous acid
* Broad spectrum against bacteria, virus, fungus, spores, antibiotic-resistant bacteria

Advantages: bleach and sodium bicarb (buffer)
ADR: Corrosive (apply petroleum jelly to surround healthy tissue)

61
Q

What are the drugs used for wounds?

A
  1. Povidone iodine
  2. Silver sulfadiazine
  3. Hydrogen peroxide
  4. Dakin’s solution

Drug Action III (23 decks)

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