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
2
Q
Psoriasis treatment
Systemic
A
- Methotrexate
- Oral Retinoids
- PDE4 Inhibitors
- Biologics
3
Q
Calcipotriene
A
- synthetic Vitamin D3 deriv
- Does not cause Tachyphylaxis
- minimally absorbed systemically
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
5
Q
Acetylenic
Tazarotene
A
- Prodrug
- Rigid non-isomerizatable retinoid
- Limits systemic toxicity (rapid systemic metabolic inactivation)
- Selective to RAR-beta and -gamma
6
Q
All Trans Retinoic Acid (ATRA)
A
- Flexible due to alternate db
- double bonds undergo cis/trans-isomerization
- lose selectivity once isomerized
7
Q
Which RAR’s are pre-dominantly on the skin?
A
Beta and gamma
8
Q
Anthralin
A
- Inhibits DNA synthesis
- Very unstable (C10 oxidation)
- Prepared with antioxidants
9
Q
Tapinarof
A
- Structural analog of Resveratrol
- Anti-inflammatory
- Anti-oxidant
- develop and maintain skin barrier
10
Q
Aryl Hydrocarbon Receptor (AhR)
A
- widely expressed in the skin
- cystolic ligand-activated transcription factor
11
Q
Photochemotherapy
Methoxsalen
A
- For severe psoriasis
- photoactive substance
- Upon UV exposure, double bonds become reactive
12
Q
MOA
Methoxsalen
A
- Decreased DNA Synthesis
- Free radical-mediated covalent modification of thymine on DNA
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)
14
Q
MOA
Apremilast
A
- PDE4 Inhibitor
- Orally active, Non-selective
- increase cAMP = decrease pro-inflammatory cytokine
- increase anti-inflammatory cytokine
15
Q
Biologics
Alefacept
A
- Inhibit T-cell activation
- binds to CD2 on T-cell
- IM injection
16
Q
Biologic
Efalizumab
A
- inhibit T-cell activation
- mAb target LFA1
- Subq injection
17
Q
Biologic
Ustekinumab
A
- mAb
- Inhibit IL-12 and IL-23 (p40 subunit)
- Subq injection
18
Q
Biologic
Ixekizumab
A
- Anti-IL-17A mAb
- Moderate - severe plague psoriasis
19
Q
Acne
Treatment Goals
A
- Correct abnormalities of follicle maturation
- Decrease sebum production + P.acne colonization
- Decrease inflammation
20
Q
Acne
Drugs Used
A
- SA
- Benzoyl Peroxide
- Tretinoin
- Isotretinoin
- Azelaic Acid
- Adapalene
- Trifarotene
- Antibiotics
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
