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
RAR selectivity
* ATRA, selectivly activate RAR
* 9-cis RA activates both RXRs and RAR
26
Tretinoin
* ATRA
* Active form of Retinol (VitA)
* Nonselective agonist
* unplug follicles , clear pores
* increase speed of surface skin cell replacement
27
# Diterpenes (20 carbon)
Isotretinoin
* Non-selective RAR agonist
* inhibits sebaceous gland function + follicle keratinization
* For severe + recalcitrant cases of inflammatory acne
* oral capsule
28
Azelaic Acid
* Mild-Moderate inflammatory acne
* inhibits growth of Propionibacterium
* reduce keratinization by inhibiting bacterial thioredoxin reductase
29
Adapalene
* Synthetic retinoid-like compound
* Selective for beta and gamma
* affects the growth of skin cells (reduce formation of pimples)
30
Trifarotene
* 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
# Antibiotics topicals
Clindamycin and Erthromycin
* Slow to act
* decreases p.acne and free fatty acids
* for mild-moderate acne
* develops resistance
32
# Tetracycline, doxycycline, minocycline, sarecycline
Systemic Antibiotics
* for severe acne
* kills excess skin bacteria
* anti-inflammatory
* inhibit bacterial protein biosyn
33
# Gout
NSAIDs
* Indomethacin
* Ibuprofen
* Ketolorac
* Naproxen
34
Colchicine
* Inhibits acrotubule assembly
* disrupt inflammasone activation, microtubule-based inflammatory cell chemotaxis, generation of leukotrienes, phagocytosis
35
Probenacid
* Inhibits URAT1 transpoter
* inhibits reabsorption of UA from renal tubules
36
Lesinurad
* Selective inhibitor of URAT1
37
Allopurinol
* Structural analog of Hypoxanthine
* Inhibits Xanthine oxidase
* metabolized by aldehyde oxidase / XO forming Oxipurinol
38
Febuxostat
* Non-purine base carboxylic acid driv
* selectively inhibit XO
* Noncompetitive inhibitor of XO
* blocks access of stubtrate to active site
39
Pegloticase
* Oxidatively degrade uric acid to soluble allantoin
* Produce H2O2 (osidative stress)
* Cause hemolyitic anemia and Met-hb
* not useful in G6PD deficiency
40
Pegylation Advantage
* Hides surface from B-cell receptor (limit immune response)
* Impede access by proteases (increase half-life)
41
# -zolamide
Carbonic Anhydrase Inhibitor
| Enzyme plays key role in formation of aq. humor
* reduce production of fluid in the eye
42
# -olol
Beta-blockers
* Slow the production of aqueous humor in the eye to reduce IOP
43
# -onidine
A2-adrenergic agonist
* Reduce aqueous production
* increase aqueous drainage via uveoscleral
44
# -prost
Protaglandin F analog
* Increase the outflow of aqueous fluid from the eye via uveoscleral
* omega-chain modified
45
Rho Kinase Inhibitor (ROCK)
* reduce IOP by increasing fuild drainage
46
# AchE inhibitor
Physotigmine
* open-angle glaucoma
* reversible
* decrease IOP by stimulating ciliary contraction
* outflow into schlemn's canal
47
# Epinephrine, Dipivefrin (prodrug)
Sympathomimetic Amine
* Reduce aqueous humor formation
* Reduce the resistance to outflow of aqueous humor
48
Aryloxypropanolamine
* Non-selective Beta blocker
* timolol
* levobunolol
49
Lantanoprostene Bunod
* increase uveoscleral outflow
* increases trabecular outflow by relaxation
50
Netarsudil
* 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
