Stiefel Review - Dermatopharmacology Flashcards

Vitamin A
Terms Definitions
Vitamin A can exist in diifferent forms, give the names for the:
Vitamin A alcohol
Vitamin A aldehyde
Vitamin A acid
Vit A alcohol = retinol
Vit A aldehyde = retinal
Vit A acid = retinoic acid
What are the precursors of Vitamin A from plants?
Carotenoids
What transports retinol in the serum?
Retinol Binding Proteins
Transthyretin
What transports retinol in the cell for translocation to the nucleus?
cytosolic retinol binding protein
What are the 1st generation synthetic retinoids?
Tretinoin (all-trans RA) = Retin-A
Isotretinoin (13-cis-RA) = Accutane = water soluble
What are the 2nd generation synthetic retinoinds?
Etretinate = Tigason = removed from market and replaced by acitretin
Acitretin = Soriatane = metabolite of etretinate = water soluble
What are the 3rd generation synthetic retinoids?
aka polyaromatic retinoids:
tazarotene = tazorac
adapalene = differin
baxarotene = Targretin = used to treat MF = water soluble
Which retinoids are water soluble?
Isotretinoin
Acitretin
bexarotene
Levels are gone after 1 month of stopping therapy
Which retinoids are more lipophilic?
Etretinate & Acitretin
Which proliferative keratins are downregulated by retinoids?
K6 & K16
Retinoids enhance keratinocyte differentiation -- in which ways?
1. increased filaggrin production
2. increased keratohyalin granules
3. increased keratin filaments
4. increased odland body secretion of lipids
What does Accutane do to sebaceous glands?
reduces the size and decreases differentiation to mature sebocytes
(also inhibits ornithine decarboxylase which lessens inflammatory hyperplasia)
What are some common Sfx of systemic retinoids?
reduced night vision, diffuse interstitial skeletal hyperostosis (DISH), premature epiphyseal closure, elevated serum lipids and transaminases, pseudotumor cerebri (with TCNs), depression & myopathy
What endocrine abnormality has been seen with bexarotene?
reversible hypothyroidism
What are some birth defects from retinoids?
microtia, hearing loss, michrophthalmia, optic nerve atrophy, acral and axial skeletal abnormalities, cardiovascular defects, hydrocephalus, microcephaly, meningomyelocele, thymic aplasia, and anal&vaginal atresia
Which retinoids target RXR receptors?
Alitretinoin (9-cis-RA)
Bexarotene
Both hit RXR alpha, beta, & gamma
Which Abx inhibits bacterial cell wall synthesis by blocking the transpeptidation step?
Penicillins
This abx blocks bacterial cell wall synthesis through inhibition of penicillin-binding proteins that catalyze transpeptidation
Cephalosporins
Which cephalosporin has been associated with increased incidence of serum sickness in children?
Cefaclor
This abx inhibits protein synthesis by binding the 30S ribosomal subunit
Tetracyclines
This Abx inhibits the 50S ribosomal subunit
Macrolides
& Clindamycin
This Abx inhibits DNA gyrase
Fluoroquinolones
This Abx inhibits RNA synthesis by inhibiting DNA-dependent RNA polymerase
Rifampin (a rifamycin)
What drug is most common cause of fixed drug eruption?
Tetracycline
What is drug has been assoc with cholestatic hepatitis?
Erythromycin
Where is the teeth discoloration in minocycline vs. tetracycline?
TCN = Tots (in childhood) = in Top third of teeth (top gingival third)
Minocycline = Mid-portion of teeth
Imiqumod induces which cytokines?
TNF-alpha
IFN-gamma
IFN-alpha
IL-12
(leads to cell mediated immune response)
Podophyllin works how?
[extract of the May apple plant]
Is antimitotic, arresting cells in metaphase by binding protein tubulin
What is a serious side effect of Protease Inhibitors? and, which one is most commonly associated with this sfx?
Lipodystrophy - manifests as abnormal fatty deposits aka 'buffalo hump' and 'protease pouch'
Most notably = indinavir (also causes gynecomastia)
Which HIV medications have been reported to cause periungual/paronychial eruptions (PG-like lesions)?
Indinavir
Zidovudine
Lamivudine
What sfx is uniquely seen in Foscarnet?
Penile erosions are known to occur
What drug has been assoc with reversible obstructive nephropathy?
Acyclovir (rapid IV infusion)
What fatal/severe sfx is seen with valacyclovir when used in AIDS or transplant patients in high doses?
TTP/HUS syndrome
Mechanism of Terbinafine
blocks the biosynthesis of ergosterol, a sterol essential to the integrity of the fungal cell membrane; inhibits squalene epoxidase (fungal inhibited 4X more than mammalian)
What is the advantage of using Terbinafine (vs. the azoles)
No cytochrome p450 inhibition!! however, transformed in the liver, therefore slow elimination by 30% in liver pts
This drug blocks synthesis of ergosterol
Terbinafine
An allylamine
Terbinafine
A Triazole
Itraconazole
Pregnancy Category:
Acitretin
X
Pregnancy Category:
Etretinate
X
Pregnancy Category:
Estrogens
X
Pregnancy Category:
Finasteride
X
Pregnancy Category:
5-FU
X
Pregnancy Category:
Flutamide
X
Pregnancy Category:
MTX
X
Pregnancy Category:
Stanozolol
X
Pregnancy Category:
Tazarotene
X
Pregnancy Category:
Aspirin
D
Pregnancy Category:
Azathioprine
D
Pregnancy Category:
Bleomycin
D
Pregnancy Category:
Colchicine
D
Pregnancy Category: Cyclophosphamide
D
Pregnancy Category:
Hydroxyurea
D
Pregnancy Category:
Mechlorethamine
D
Pregnancy Category:
Penicillamine
D
Pregnancy Category:
Potassium iodide
D
Pregnancy Category:
Tetracycline
D
Pregnancy Category:
Griseofulvin
unrated, but probably D
Pregnancy Category:
Spironolactone
unrated, but probably D
Pregnancy Category:
Quinolones/ciprofloxacin
C
Pregnancy Category:
TMP/SMX
C
Pregnancy Category:
Cyclosporine
C (but believed to be safe in pregnancy)
Pregnancy Category:
Acyclovir
C
Pregnancy Category:
fluconazole, ketoconazole, itraconazole
C
Pregnancy Category:
Benzoyl peroxide
C
Pregnancy Category:
topical retin-A
C
Pregnancy Category:
topical and oral steroids
C
Pregnancy Category:
Efalizumab
C
Pregnancy Category:
Penicillin
B
Pregnancy Category:
Emycin
B (not estolate form due to hepatotoxicity in mother)
Pregnancy Category:
Dimenhydrinate
B
Pregnancy Category: Cyproheptadine
B
Pregnancy Category: azeleic acid
B
Pregnancy Category: Permethrin
B
Pregnancy Category: cephalosporins
B
Pregnancy Category: Lidocaine
B
Pregnancy Category:
etanercept, alefacept, infliximab
B
Pregnancy Category:
Folic Acid
A
Pregnancy Category:
Levothyroxine
A
What drugs have been assoc with IUD failure?
Azathioprine, NSAIDs
What drugs have been assoc with OCP failure?
griseofulvin, rifampin
~ by incr estrogen metabolism by hepatic enzyme induction
Nitrogen mustard derivative that is cell-cycle non-specific
Cyclophosphamide
What is the toxicity assoc with cyclophosphamide -- which metabolite causes it? And, what is used to reduce the effect?
Hemorrhagic cystitis (in 40%) of pts, can lead to transitional cell carcinoma.
Bladder toxicity is due to the acrolein metabolite
Mesna (aka sodium 2-mercaptoethanesulfonate) has been used to reduce this toxic effect
Which pt's are at higher risk for pancytopenia when using MTX?
renal patients
NSAIDS
Bactrim
What is used to rescue pts from MTX induced myelosuppression?
Leukovorin (folinic acid) -- can bypass dihydrofolate reductase in the cell division pathway
What is a unique side effect of MTX?
radiation recall (aka sunburn recall)
Purine analog that acts only during the S-phase of the cell cycle in the formation of adenine and guanine nucleotides
Azathioprine
There are three enzyme pathways for Azathioprine -- name them
1. Hypoxanthine guanine phosphoribosyl transferase (HGPRT)
2. Xanthine oxidase
3. Thiopurine methyltransferase (TPMT) activity

If pathway #1 becomes the primary pathway, toxic purine analogs can accumulate --> BM suppression!
This can happen in the setting of concurrent use of allopurinol (inhibits xanthine oxidase) or low TPMT allele activity
Rituximab is what type of drug?
Anti-CD20 antibody
Methotrexate blocks what?
Folic Acid Analog, inhibits dihydrofolate reductase
Mycophenolate Mofetil
Inhibits Inosine Monophosphate in de novo purine synthesis
Azathioprine
6-mercaptopurine analog that inhibits purine synthesis; check thiopurine methyl transferase levels prior to giving
Interferon Gamma
Inhibits TH2 cells
Cyclosporine
calcineurin inhibitor, blocks T-lymphocytes; reduces transcription of cytokines (IL-2); monitor BP, CBC, LFTs, Mg and Uric Acid
Efalizumab mechanism?
Recombinant monoclonal antibody that binds to CD11a, subunit of Leukocyte function antigen-1 to block ICAM-1;
Sfx of Raptiva?
Efalizumab
Thrombocytopenia, anemia, 5% of pts have anti-raptiva antibodies
Loading dose 0.7 mg/kg x 1 week, then 1mg/kg sc weekly.
Rituximab is approved for what use?
1997 FDA approved for B-cell lymphomas and treatment resistant RA

"off-label" use for pemphigus vulgaris, paraneoplastic pemphigus, all pemphigus
- Atopic dermatitis
- EBA
- ANCA-mediated vasculitis
- cryoglobulinemia
- dermatomysositis (unknown mechanism)
- Chronic GvHD
- Lupus
Target of Rituximab
CD20 receptor (B-cell specific antigen)

CD20 not found on plasma or stem cells (so they are spared!)

B-cells recover in appx 6 months
What type of antibody is rituximab?
Monoclonal IgG1 (chimeric murine-human antibody):

Fc fragment is human -- recruits immune cells to lyse CD20 cells

Fab fragment is mouse -- binds CD20 Ag
Side Effects of Rituximab?
IV infusion reactions are most common
RARE: PML
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