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DnD-Skin/Con/Misc > Mchem of A/P/G/G > Flashcards

Mchem of A/P/G/G Flashcards

1
Q

Psoriasis Treatment

External

A
  • Calcipotriene, Vitamin A analog, Anthralin
  • AhR Agonist
  • Photo(chemo)therapy - PUVA
  • Corticosteroids
  • Calcineurin inhibitors
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2
Q

Psoriasis treatment

Systemic

A
  • Methotrexate
  • Oral Retinoids
  • PDE4 Inhibitors
  • Biologics
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3
Q

Calcipotriene

A
  • synthetic Vitamin D3 deriv
  • Does not cause Tachyphylaxis
  • minimally absorbed systemically
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4
Q

Vitamin D3 Receptor Signaling

A
  • Inhibits expresion of inflammatory cytokines
  • inhibits T-cell proliferation and induces T-regulatory cells
  • supresses proliferation of keratinocytes
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5
Q

Acetylenic

Tazarotene

A
  • Prodrug
  • Rigid non-isomerizatable retinoid
  • Limits systemic toxicity (rapid systemic metabolic inactivation)
  • Selective to RAR-beta and -gamma
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6
Q

All Trans Retinoic Acid (ATRA)

A
  • Flexible due to alternate db
  • double bonds undergo cis/trans-isomerization
  • lose selectivity once isomerized
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7
Q

Which RAR’s are pre-dominantly on the skin?

A

Beta and gamma

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8
Q

Anthralin

A
  • Inhibits DNA synthesis
  • Very unstable (C10 oxidation)
  • Prepared with antioxidants
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9
Q

Tapinarof

A
  • Structural analog of Resveratrol
  • Anti-inflammatory
  • Anti-oxidant
  • develop and maintain skin barrier
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10
Q

Aryl Hydrocarbon Receptor (AhR)

A
  • widely expressed in the skin
  • cystolic ligand-activated transcription factor
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11
Q

Photochemotherapy

Methoxsalen

A
  • For severe psoriasis
  • photoactive substance
  • Upon UV exposure, double bonds become reactive
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12
Q

MOA

Methoxsalen

A
  • Decreased DNA Synthesis
  • Free radical-mediated covalent modification of thymine on DNA
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13
Q

Etretinate

A
  • Tretinoin analog
  • Nonselective
  • First-pass metabolism to make active metabolite (acitretin)
  • accumulates in adipose tissue after repeat dosing (120 day half-life)
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14
Q

MOA

Apremilast

A
  • PDE4 Inhibitor
  • Orally active, Non-selective
  • increase cAMP = decrease pro-inflammatory cytokine
  • increase anti-inflammatory cytokine
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15
Q

Biologics

Alefacept

A
  • Inhibit T-cell activation
  • binds to CD2 on T-cell
  • IM injection
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16
Q

Biologic

Efalizumab

A
  • inhibit T-cell activation
  • mAb target LFA1
  • Subq injection
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17
Q

Biologic

Ustekinumab

A
  • mAb
  • Inhibit IL-12 and IL-23 (p40 subunit)
  • Subq injection
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18
Q

Biologic

Ixekizumab

A
  • Anti-IL-17A mAb
  • Moderate - severe plague psoriasis
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19
Q

Acne

Treatment Goals

A
  • Correct abnormalities of follicle maturation
  • Decrease sebum production + P.acne colonization
  • Decrease inflammation
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20
Q

Acne

Drugs Used

A
  • SA
  • Benzoyl Peroxide
  • Tretinoin
  • Isotretinoin
  • Azelaic Acid
  • Adapalene
  • Trifarotene
  • Antibiotics
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21
Q

Salicylic acid

A
  • Keratolytic, anti-inflammatory
  • exfoliates skin, clears pores
  • for mild acne
22
Q

Benzoyl Peroxide

A
  • topically (10%)
  • Anti-microbial
  • Oxidizing effect from benzoate free radicals
23
Q

Retinoic Acid Receptors

A
  • Ligand-controlled transcription factors
  • Activated by retinoid agonists
  • dimerize with RXR
  • regulate cell growth, differentiation, apoptosis
24
Q

RXR

A
  • can be homodimers and heterodimers
25
Q

RAR selectivity

A
  • ATRA, selectivly activate RAR
  • 9-cis RA activates both RXRs and RAR
26
Q

Tretinoin

A
  • ATRA
  • Active form of Retinol (VitA)
  • Nonselective agonist
  • unplug follicles , clear pores
  • increase speed of surface skin cell replacement
27
Q

Diterpenes (20 carbon)

Isotretinoin

A
  • Non-selective RAR agonist
  • inhibits sebaceous gland function + follicle keratinization
  • For severe + recalcitrant cases of inflammatory acne
  • oral capsule
28
Q

Azelaic Acid

A
  • Mild-Moderate inflammatory acne
  • inhibits growth of Propionibacterium
  • reduce keratinization by inhibiting bacterial thioredoxin reductase
29
Q

Adapalene

A
  • Synthetic retinoid-like compound
  • Selective for beta and gamma
  • affects the growth of skin cells (reduce formation of pimples)
30
Q

Trifarotene

A
  • for facial and truncal acne ( 9 y.o and above)
  • Potent and selective RAR-gamma agonist
  • Gamma is poorly expressed in placenta
  • Systemic abdorption is poor
31
Q

Antibiotics topicals

Clindamycin and Erthromycin

A
  • Slow to act
  • decreases p.acne and free fatty acids
  • for mild-moderate acne
  • develops resistance
32
Q

Tetracycline, doxycycline, minocycline, sarecycline

Systemic Antibiotics

A
  • for severe acne
  • kills excess skin bacteria
  • anti-inflammatory
  • inhibit bacterial protein biosyn
33
Q

Gout

NSAIDs

A
  • Indomethacin
  • Ibuprofen
  • Ketolorac
  • Naproxen
34
Q

Colchicine

A
  • Inhibits acrotubule assembly
  • disrupt inflammasone activation, microtubule-based inflammatory cell chemotaxis, generation of leukotrienes, phagocytosis
35
Q

Probenacid

A
  • Inhibits URAT1 transpoter
  • inhibits reabsorption of UA from renal tubules
36
Q

Lesinurad

A
  • Selective inhibitor of URAT1
37
Q

Allopurinol

A
  • Structural analog of Hypoxanthine
  • Inhibits Xanthine oxidase
  • metabolized by aldehyde oxidase / XO forming Oxipurinol
38
Q

Febuxostat

A
  • Non-purine base carboxylic acid driv
  • selectively inhibit XO
  • Noncompetitive inhibitor of XO
  • blocks access of stubtrate to active site
39
Q

Pegloticase

A
  • Oxidatively degrade uric acid to soluble allantoin
  • Produce H2O2 (osidative stress)
  • Cause hemolyitic anemia and Met-hb
  • not useful in G6PD deficiency
40
Q

Pegylation Advantage

A
  • Hides surface from B-cell receptor (limit immune response)
  • Impede access by proteases (increase half-life)
41
Q

-zolamide

Carbonic Anhydrase Inhibitor

Enzyme plays key role in formation of aq. humor

A
  • reduce production of fluid in the eye
42
Q

-olol

Beta-blockers

A
  • Slow the production of aqueous humor in the eye to reduce IOP
43
Q

-onidine

A2-adrenergic agonist

A
  • Reduce aqueous production
  • increase aqueous drainage via uveoscleral
44
Q

-prost

Protaglandin F analog

A
  • Increase the outflow of aqueous fluid from the eye via uveoscleral
  • omega-chain modified
45
Q

Rho Kinase Inhibitor (ROCK)

A
  • reduce IOP by increasing fuild drainage
46
Q

AchE inhibitor

Physotigmine

A
  • open-angle glaucoma
  • reversible
  • decrease IOP by stimulating ciliary contraction
  • outflow into schlemn’s canal
47
Q

Epinephrine, Dipivefrin (prodrug)

Sympathomimetic Amine

A
  • Reduce aqueous humor formation
  • Reduce the resistance to outflow of aqueous humor
48
Q

Aryloxypropanolamine

A
  • Non-selective Beta blocker
  • timolol
  • levobunolol
49
Q

Lantanoprostene Bunod

A
  • increase uveoscleral outflow
  • increases trabecular outflow by relaxation
50
Q

Netarsudil

A
  • alpha-aryl beta-amino isoquinoline amide analog
  • highly potent ROCk inhibitor
  • makes trabecular meshwork more flexible and allow the fluid into the schlemm’s canal

DnD-Skin/Con/Misc (5 decks)

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