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36 Cards in this Set

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What is the rate limiting step of topical drugs?

partition coefficient = absorption through the stratum corneum




(higher = faster absorption, better)




(palm/sole thickness > body > scrotum > face)




(absorption is faster w/ thinner skin, hydration, ointment, heat, & coverage)

What causes acne?

1. Hyperkeratinization--> Inc loose cells, clogs follicles, caused by Incr Androgens


2. Increased Sebum production, caused by Incr Androgens--> substrate for bacteria enzymes, clogs follicles


3. Propionibacterium acnes, use lipase to form FFA (free fatty acids) from sebum


4. Inflammation, response to FFA irritation

Hyperkeratinization, inc sebum & P. acnes form microcomedos (acne precursor), then mechanical insult causes comedo to close & inflammation leads to........

inflammation causes comedo to progress to papules, pustules, nodules, cysts (acne) w/ potential to scar

Mild acne, localized to face is not likely to scar & should be tx w a ____________




While ___________ is preferred for severe acne on back, chest, arms, that is more likely to scar

topical medication for mild




oral medication for severe, may use topical additionally

_________ is used for mild acne or in combos w/ erythromycin or clindomycin for more severe acne




MOA:


+Keratolytic- solubilizes intracellular connections btwn keratinocytes, reducing hyperkeratinization


+Comedolytic- prevents closure, reduces comedones


+Bactericidal- kills P. acnes via radical formation


Benzoyl Peroxide




*lipophillic, good penetration

What are the SEs of Benzoyl peroxide?

Irritation, dryness, peeling & erythema


Bleaching of hair/ clothes


Contact dermatitis (rare)

__________ is used for mild acne or psoriasis




MOA:


+keratolytic (solubilizes intracellular cement, reduces hyperkeratinization)




What are the SE's?

Salicylic Acid




SE:


salicylism (rare, life threatening)

________ is used for mild/ moderate acne & acne rosacea, hyperpigmentation




MOA:


+Keratolytic


Antimicrobial- Inhibitor of thioredoxin reductase & tyrosinase, inhibits DNA synthesis


Antiinflammatory- scavenger of free radicals

Azelaic Acid (azelex)

What are the SEs of Azelaic Acid?

irritation, itching


hypopigmentation (tyrosinase inhibition interferes w/ melanocyte)

First line acne therapy-




MOA?

Retinoids (Vit A analogs)




MOA:


retinoic acid (RA) binds endogenous Retinoic acid (RARs) & retinoic X (RXRs) nuclear receptors-->


RA-RAR complex forms transcription factor-->


regulate gene transcription & translation-->


altered cellular function of translated proteins-->


Regulate epithelial cell proliferation (hyperkeratinization)


Bone growth


Immune function


Reproductive function

1st & 2nd generation retinoids have more flexible structures, allowing them to _________




What does this cause?

allows binding to several retinoid receptors




*causes worse SE's than 3rd generation retinoids (arotinoids)

________, is a topical 1st gen topical retinoid, trans-retinoic acid, used for acne & as an anti-wrinkle cream




MOA: (binds RAR)


+Keratolysis- by incr mitosis (cell turnover)--> decr cell adhesion--> exfoliation & desquamation


+Anti-comedolytic- prevents formation of new microcomedones

Tretinoin (Retin A)

What are the SEs of Tretinoin?

Irritation, erythema, peeling dryness


Initial appearance of worsening acne (top layer sloughed & reveals comedones below)


De-activated by UV light & Benzoyl peroxide


(use at night & DONT use w/ Benzoyl peroxide)




*Antiwrinkle effects (vasodilation & inc collagen)

_________ is a 3rd gen topical retinoid, used for acne




MOA: same as Tretinon (binds RAR)


+Keratolysis


+Anti-comedolytic




How does this drug differ from Tretinon?

Adapalene (Differin)




* NOT degraded by UV or benzoyl peroxide


*similar SE's, but less severe

_______ is a 3rd gen topical, UV-stable retinoid, used for acne & psoriasis




MOA: Pro-drug, converted to tazarotenic acid (by esterase, when rubbed on skin)--> binds RAR-->


+Keratolysis- normalizes keratinocyte growth


+Anti-inflammatory




What are the SEs?

Tazarotene (tazorac, avage)




SE:


Similar SEs to Tretinoin (use every other day to reduce skin irritation)


Teratogen category X

_______ is a 3rd gen, ORAL, cis-retinoic acid, MOST EFFECTIVE acne tx


*short term use--> permanent effects




MOA: (binds RAR)


+keratolysis- normalizes follicular epithelium


+Decreases Sebum production


+Anti-inflammatory


+Bactericidal


(targets all 4 causes of acne!)

Isoretinoin (generic for accutane)

Despite being the most effective tx, Isoretinoin may not be used d/t neg SEs. What are they?




(Accutane no longer on market d/t these)

Dry, peeling, itchy skin


Dry eyes


Nosebleeds


Alopecia (reversible)


Inflammatory Bowel disease


Joint pain


Lipid profile changes


Depression/ Suicidal ideations (DO NOT used in pts predisposed to depression!)


Teratogen category X

Pts taking Isotretinoin must agree to do the following before starting;

Use 2 forms of birth control (severe teratogenesis)


Take pregnancy test


Not donate blood (for at least 1 month following discontinuation)


Not take Vitamin A supplements (toxicity)

________ is a macrolide Abx, used in BOTH Topical & Oral acne tx, alone or in combo w/ benzoyl peroxide




MOA:


+Bacteriostatic-


binds 50s ribosomal subunit-->


inhibits translocation-->


inhibits translation of mRNA to protein




What are the SEs?

Erythromycin




SE: (w/ oral use*)


(CYT P450) Liver enzyme inhibitor--> Incr concentration of theophylline, caffeine, coumadin, digoxin, warfarin, corticosteroid (toxicity)

_______ abx, used in BOTH topical & oral acne tx, alone or in combo w/ Benzoyl peroxide




MOA:


+Bacteriostatic-


binds 50s-->


inhibits protein synthesis




What SEs does it cause?

Clindamycin




SE: (w/ oral use)


pseudomembrane Colitis

______ abx, used in BOTH topical & oral acne tx




MOA:


+Bacteriostatic-


binds 30s-->


inhibits translation of mRNA into protein




What SEs does it cause?

Tetracycline




SE: (oral)


alters normal intestinal flora


Photosensitization


Binds Ca2+ (tooth & bone effects)--> absorption/ efficacy is decreased w/ Antacid use-->* Avoid dairy, antacids iron**





_______tetracyline class abx, use in oral acne tx only




MOA:


+Bacteriostatic-


same as tetracycline (binds 30s)




How does this differ from tetracycline?

Doxycycline




Oral use only & Increased incidence of SE's

_____ tetracycline class Abx, use in oral acne tx only, expensive**




MOA:


+Bacteriostatic-


same as tetracycline




SE:


less incidence of SEs than tetracycline


Ototoxicity* (vestibular effects)



Minocycline

________ is the only hormone therapy approved for acne tx in FEMALE pts




MOA:


Inc SHBG-->


Decreased free Androgen (testosterone)-->


+Keratolytic (decr hyperkeratinization)


+Decreased Sebum




What are the SEs?

Ortho-Tri-Cyclen


(ethinyl estradiol & noregestimate)




SE:


Inc risk of CVD (MI, stroke, etc) in smokers >35


Inc risk of clotting (dose related)


Inc risk of breast cancer


*takes a few months to see effects & acne relapse w/ discontinuation

What cause Plaque formation in psoriasis?

APC presents Ag to T cell in LN-->


clonal expansion-->


activated TH1 cell travels to dermis-->


encounters new APC-->


reactivation & further clonal expansion-->


cytokine release-->


keratinocyte inflammatory damage-->


plaque formation

Psoriasis is a disorder of hyperkeratinization (inc cell sloughing/turnover).




Somewhat genetic, onset usually after some "trigger"--> disruption in arachidonic acid metabolism (inc rate)




How does this present clinically?

thick plaques w/ silver scale


red skin (capillary dilation)


inflammation (lymphocytes in dermis & neutrophils in epidermis)

________ & _________ target the superficial epidermis & are used topically on reduce scales

Emolients (lotions)- minimize dryness, pruritis, soften scales


&


Keratolytics (Salicylic acid)- smooth skin & remove scale, decrease hyperkeratosis

__________ are used topically in severe psoriasis (start w/ more potent rx, followed by less potent rx)




MOA: immunosuppression


antimitotic effects on the epidermis-->


suppress proinflammatory genes (IL-1, IL-2, IL-6)-->


decrease inflammatory cell production & migration to dermis




SEs?

Corticosteroids




SE: (may have systemic SE at high dose*)


Steroid rosacea


contact dermatitis


skin atrophy


bruising


*NEVER use on face, only on small body areas

________ oral rx, used for psoriasis




MOA: immunosuppression


binds cyclophylin-->


inhibits calcineuron-->


prevents dephosphorylation of NFAT-->


decr IL-2 production-->


decr T cell activation




What are the SEs?

Cyclosporine (sandimmune)




SE:


renal dysfxn (nephrotoxicity)


hirsutism


HTN

___________ is a biologic used in the tx of moderate to severe chronic plaque psoriasis




MOA: immunosuppression


dimeric fusion protein binds to CD2 on T cells-->


interferes w/ T cell interaction w/ APC-->


reduces active T cells




SE?

Alefacept (amevive)




SE:


CD2 binding on T cell-->


Increased CD4+ apoptosis


*requires weekly CD4+ monitoring


*don't use in pts w/ infections

_______ is a biologic used to tx psoriasis




MOA: immunosuppresion


humanized monoclonal anti-TNF-alpha Ab-->


binds TNF-alpha-->


cell-toxic effects




What are the SEs?


What is required before starting?

Adalimumab (Humira)




SE:


allergic rxns


reactivation of latent Tb*


incr susceptibility to infection


lupus-like syndrome




Require Tb screen before starting, don't use w/ infeciton

___________ is a retinoid that can be used to tx moderate to severe psoriaisis (not commonly used for acne)



MOA: keratolytic


prodrug converted to etritinate




SEs?




What other retinoid can also be used to tx psoriasis?

Acitretin (soriatane)




SE:


similar to isoretinoin (dry skin, dry mucous membranes, hair thinning)


severe teratogenesis (worse than isoretinoin, caution in preg for 3 yr after discontinuing)


wait 1 month to donate blood after stopping




*Tazarotene also used to tx psoriaisis

________ are topicals used to tx psoriasis, dermatitis, lichen simplex chronicus (alt to corticosteroids)




MOA: Keratolytic


phenolic compounds--> antipruritic


cytostatic epidermal thinning




SE?

Tar compounds




SE:


transient epidermal hyperplasia (followed by epidermal thinning)


Difficult application--> staining, stinky


Irritant folliculitis


Phototoxicity

_________ topical ointment used for moderate plaque type psoriaisis




MOA: Vit D3 derivative-->


inhibit keratinocyte differentiation & proliferation (keratolytic)-->


Decrease TH1 stimulating cytokines (IL-2)




SEs?

Calcipotriene (Dovonex)




SE:


Avoid mucous membrane (eyes) & open skin (prevent systemic effects)


Irritation, drying, erythema

_______ is used in moderate to severe psoriaisis




MOA: anti-inflammatory


inhibits dihydrofolate reductase (DHFR)-->


blocks DNA synthesis (esp of rapidly dividing cells = immune cells)-->


Decrease IL-1-->


death of active T cells




SEs?

Methotrexate




SE:


hepatic fibrosis (d/t high dose req)


CI w/ sulfamethoxazole, probenecid, salicylates

__________ is used in combination w/ UV A light therapy (PUVA therapy) to tx psoriasis




*applied prior to light exposure




MOA:


photoaddition to pyrimidine in DNA-->


creates reactive oxygen-->


anti-proliferative, immunosuppressive, & anti-inflammatory




SE's?

Methoxalen/ Psoralens




SEs:


Nausea, cataracts (if oral, can be used in bathwater or lotion topically)


photosensitivity




(UVB is more likely than UVA to cause cancer)