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70 Cards in this Set

  • Front
  • Back
dead, highly keratinized lipophilic cells
stratum corneum (corneocyte)
1st line of defense against environment; 1st LIVE layer
epidermis
- rich in CT, fibroblasts, mast cells, macrophages, migratory cells.

- Contains sebaceous glands, BVs, hair & nail appendages.

- Supports/nourishes epidermis. Complex series of diffusion barriers
dermis
What are the 6 variables determining pharmacological response?
1. regional anatomical variations
2. concentration gradient
3. dosing schedule
4. vehicle
5. age
6. application frequency
What is regional anatomical variation?
permeability inversely proportional to thickness of S. corneum
What is concentration gradient?

What can it lead to??
inc tolerance gradient inc. mass of drug transferred

**can lead to tolerance-tachyphylaxis
What is dosing schedule?
Skin acts as reservoir -> half-life in skin may be longer than systemic so can use once daily w/ effectiveness
How can the vehicle used determine pharm response?
Appropriate vehicle can maximize efficacy.

Occlusion maximizes efficacy
How is age important in determining dose response?
Children have > SA: mass = high systemic quantity

**Careful esp w/ corticosteroids
How is application frequency important?
Intermittent pulse therapy prevents tachyphylaxis
Which 2 of the 6 variables determining pharm response were highlighted as important?

Define 'em
2. Concentration gradient
5. Age
What are 2 depigmentation agents?

What is their function?
1. Hydroquinone
2. Monobenzone

Reduce hyperpigmentation
Which of the depigmentation agents causes temporary lightening?

Which causes permanent (irreversible) lightening?
Hydroquinone - temporary

Monobenzone - permanent
What is the MOA of the depigmentation agents?
Inhibition of tyrosinase, interferes w/ production of melanin

--> Prevent oxidation of tyrosine to DOPA in melanocytes
What are the sfx of depigmentation agents?
systemic absorption (monobenzone) can lead to HYPOpigmentation at other sites in body
What are the 2 repigmentation agents?

What are they classified as?
1. Trioxsalen
2. Methoxsalen

Psoralens
What are psoralens?
Agents that must be photoactivated by UVA to produce beneficial effects
What do the psoralens used for?
Repigmentation of depigmented macules of vitiglio
What are the 3 functions of psoralens?
1. Erythemogenic
2. Melanogenic
3. Cytotoxic
What is the MOA of psoralens?
Once photochemotherapy is administered s/p oral use of psoralens, the -->

formation of DNA adducts inhibit DNA replication
What do psoralens inhibit?

What do they promote?
- inhibit cell proliferation

- promote differentiation of epithelial cells
What is the indication of use for Methoxsalen?
severe, recalcitrant, disabling psoriasis not responsive to other forms of therapy
What is Trioxsalen used for?
Vitiglio
What are the sfx of psoralens?
ocular damage, aging of skin, skin ca
Which of the 2 psoralens can be used for the pallative tx of cutaneous T-cell lymphoma?
Methoxsalen
What are the 5 different acne preperations?
1. Retinoic acid
2. Adapalene
3. Isotretinoin
4. Benzoyl peroxide
5. Azelaic acid
What are the 3 classifications of acne?
1. follicular
2. papular
3. pustular
Do the acne medications require UV activation for effects?
Nah
What are the routes of administration for the acne meds mentioned?
Oral or topical

NO IV
Retinoic acid is aka?

Retinoic acid is effective against?
all-trans retinoic acid

acne vulgaris
Retinoic acid and vitA relationship?
Analogue of vitA

EtOH to acid and cis to trans transformation to form retinoic acid
What are the biological effects of retinoic acid?
cellular proliferation & differentiation, immune function, inflammation & sebum production
What is the MOA of retinoic acid (RA)?
Ra binds w/ RXR/RAR --> RXR or RAR--Ra complex binds w/ RAREs (retinoic acid response elements) and result in ----> activation of gene transcription
What are the effects of Ra on skin?
-> inc epidermal cell turnover

-> stabilize lysosomes, inc PGE2, cAMP & cGMP levels, and incorporate thymidine into DNA in ----> epithelial tissue
effects of retinoids on P. acnes?

What does the "p" stand for?
-> decrease action & concentration, decrease PGE2, collagenase, and inflammation

-> propionibacterium

thus ==> there is possibly some anti-bacterial effects
Retinoic acid can cause what skin irritation?
slight erythema & mild peeling
Sfx of retinoic acid?
-> tumorigenic w/ UV irradiation
thus pts advised to avoid sun exposure
What is isotretinoin?

What is the spectrum of use?
1st generation retinoic acid

limited to only severe cystic acne
What is the MOA of Isotretinoin?
inhibits sebaceous gland size and fnxn
What are the adverse effects of Isotretinoin?
Hypervitaminosis-like symptoms
In what population are retinoids absolutely CI?
Pregos and women w/ potential for child bearing
What is etretinate?

What is the indication of use for it?
2nd generation retinoid

psoriasis
What is benzoyl peroxide used to tx?

What layer of the skin does it penetrate?
acne vulgaris

stratum corneum
What is azelaic acid used to treat?

What is its MOA?
acne

antimicrobial effects & inhibitory effect on conversion of testosterone -> DHT
What are the 3 meds used for psoriasis?
Acitertin
Tazarotene
Calcipotriene
What is psoriasis caused by?
increased epidermal cell proliferation (scaly silvery patches)
What is Etretinate and what is it used for?

Brand name?
Aromatic retinoid for pustular psoriasis

Tegison
What is Acitretin and what is it used for?

Brand name?
etretinate metabolite for pustular psoriasis

Soritane
What are the adverse effects of Acitretin (Soritane) and the contraindications?
Hypervitaminosis
elevated cholesterol & triglycerides
Teratogenic

CI in pregos and 3 yrs post therapy in women planning to have kids

EtOH should be avoided during & 2 mos post therapy

Can't donate blood for 3 yrs post
What is Tazarotene & its brand name?

What are its effects?
Acetylated retinoic acid

Tazorac

Inhibition of proliferation & differentiation of epithelial cells
Importance of photochemotherapy?
used in managing psoriasis

w/ administration of oral psoralen

DNA adduct formation inhibits DNA rep

Inhibits proliferation & promotes differentiation of epithelial cells
What is calcipotriene?

What are its actions?

On immune system?

Adverse effects?
synthetic vitD3 derivative

inhib proliferation & differentiation of epithelial cells

decrease local T-CMI (immunosup)

itching, dryness, burning, irritation, erythema
What are the properties of glucocorticoids?

What are the routes of administration?
immunosuppressive and anti-inflammatory

locally via topical & intralesional routes
What is the MOA of glucocorticoids?
varies

inhibitory effects on arachindonic acid cascade, depression of production of cytokines & effects on inflamm cells
What are glucocorticoids used for?
eczema, dermatitis, pruritis, mild psoriasis, inflammation
What are the different classes of glucocorticoids?
1. lowest efficacy
2. low efficacy
3. intermediate efficacy
4. high efficacy
5. highest efficacy
What are the toxic effects of glucocorticoids?
atrophy, striae/band formation, acneiform eruptions, dermatitis, hypopigmentation, rosacea, fungus overgrowth
What are the withdrawal symptoms of glucocorticoids?
perioral dermatitis & rosacea on the face
What are the toxic effects on children?
systemic toxicity (depression of hypothalamic-hypophyseal-adrenal axis and growth retardation)
What are insoluble preps of glucocorticoids?

What can they cause?
Triamcinolone

cause atrophy & hypopigmentation
What does Minoxidil do?

What disorder is it used to help?
Potent arterial vasodilator that also reverses progressive miniaturization of terminal scalp hairs

Adrogenic alopecia
What does stopping Minoxidil cause?
hair loss
What is the MOA of Minoxidil?

What can Minoxidil also do to androgens in scalp?
May either:
1. activate hair follicle directly
or
2. stimulation microcirculation surrounding the follicle, increasing cutaneous blood flow

May also alter metabolism of androgens in scalp
What does systemic therapy do?

What does topical therapy NOT cause?
Stimulate hair growth

does not lead to hypotension
What is Finasteride?

What does it do (physiologically)?

What are its 2 uses?
Testosterone analogue

5-alpha-reductase inhibitor (blocks conversion of T --> DHT)

orally for androgenic alopecia; BPH
What does Finasteride decrease concentrations of?

Where?

Why is this imporatant?
decreases DHT concentrations

in scalp and serum

in pattern hair loss, there is an inc amount of DHT
What are the adverse effects of Finasteride?
decreases libido, dec ejac vol, ejac dysfnxn, erectile dysfnxn
WHat does it cause in male fetuses if handled by pregos?
Hypospadias
What is hypospadias
developmental anomaly characterized by defect on ventral surface of penis --> urethral meatus is PROXIMAL to nL
Absolute CI of finasteride?
children, females, pregos