RA/Gout Med Chem Flashcards
What RA drug class is minocycline?
nonbiological DMARD
What RA drug class is azathioprine?
nonbiological DMARD
What RA drug class is gold?
nonbiological DMARD
What RA drug class is penicillamine?
nonbiological DMARD
What is the nonbiological DMARD methotrexate MOA?
inhibits DNA synthesis
What is the target of methotrexate?
dihydrofolate reductase (DHFR)
Main AE of methotrexate?
hepatotoxicity
What is the drug food interaction between cola and MTX?
increased MTX serum levels
MTX has limited solubility at pH below 7
What is the DDI between penicillin and MTX?
decreases elimination of MTX
What is the DDI between cyclosporine and MTX?
potentiates MTX’s hematologic effects
Do nsaids increase MTX toxicity?
yes
How does probenecid affect MTX?
inhibits MTX excretion
What are the 2 main contraindications for MTX use?
liver disease
immunodeficiency
What is the active form of leflunomide?
teriflunomide
What is the target of the nonbiological DMARD leflunomide?
dihydroorotate dehydrogenase (DHODH)
Leflunomide inhibits the denovo synthesis of ____.
pyrimidine
cytosine, thymine
What is the half life of teriflunomide?
14-18 day
2 main AEs of leflunomide?
infection
liver toxicity
What is the DDI between leflunomide and warfarin?
increased risk of bleeding
Which nonbiological DMARD cause increased levels of repaglinide, rosuvastatin, pioglitazone, and rosiglitazone?
leflunomide
2 main contraindications of leflunomide?
pregnancy
hepatic impairment
What is recommended a a binding agent for leflunomide toxicity?
cholestyramine
Which nonbiological DMARD has the possible target of toll-like receptor 9 (TLR9) family receptors?
hydroxychloroquine
Does hydroxychloroquine have rapid or slow GI absorption?
rapid
half life 32-50 days, but fast absorption means Sx of overdose can occur as early as 30mins
Hypersensitivity to ___ compound is a CI for hydroxychloroquine
4-aminoquinoline
Which nonbiological DMARD can cause increased serum digoxin concentrations?
hydroxychloroquine
Which portion of the TNF alpha inhibitor infliximab is from human IgG1?
Fc
Which portion of infliximab is murine?
Fab
What is the target of rituximab?
CD20 protein on cell
anti-CD20 antibody
Which med targets CD80/86 on APCs?
abatacept
Which cell targets CD20 of B cells?
rituximab
Which med targets IL6 signaling?
tociluzumab
Which med targets IL1 signaling?
anakinra
Which TNF alpha med targets soluble TNF receptors?
etanercept
infliximab, adalimumab, certolizumab, golimumab are anti-TNF alpha antibodies
2 main DDIs of etanercept?
anakinra
live vaccines
increased risk of infection
2 main AEs of etanercept?
injection site rxn
infections
Which TNF Alpha inhibitor is CI in heart failure?
infliximab
do not give doses greater than 5mg/kg
Which class of meds inhibits the formation of uric acid
xanthine oxidase inhibitors
Does colchicine have an effect on serum uric acid level?
no
What is the target of colchicine?
tubulin
arrests neutrophil motility, decreases inflammation
What CYP metabolizes colchicine?
CYP3A4
DDI with 3A4 inhibitors: azoles, macrolides, protease inhibitors
Colchicine has DDIs with inhibitors of?
P-gp
3A4
Why shouldn’t urate reducing therapy be initiated during an acute gout attack?
may prolong attack by changing equilibrium of body rate
Which xanthine oxidase inhibitor can cause hypersensitivity syndrome?
allopurinol
allopurinol hypersensitivity syndrome (AHS)
exfoliative dermatitis, vasculitis, fever, liver dysfunction, eosinophilia, acute interstitial nephritis,; most likely to occur in pts with renal disease along with diuretic therapy; may be fatal
Which XOI is NOT purine like?
febuxostat
Which XOI causes increased serum conc. of one metabolite of theophylline?
febuxostat
What is the target of probenecid?
urate anion exchange transporter (URAT1)
Probenecid is used to reduce hyperuricemia in pts who excrete < ___ mg of uric acid per day
600
What is the main CI for probenecid?
do not use during acute, gouty attack
What is the target of pegloticase?
uric acid
How does pegloticase lower uric acid level?
enhances uric acid degradation
What does pegloticase convert uric acid too?
allantoin
more excretable metabolite
What is major CI of pegloticase?
G6PD deficiency